"Molecule ChEMBL ID"	"Molecule Name"	"Molecule Max Phase"	"Molecular Weight"	"#RO5 Violations"	"AlogP"	"Compound Key"	"Smiles"	"Standard Type"	"Standard Relation"	"Standard Value"	"Standard Units"	"pChEMBL Value"	"Data Validity Comment"	"Comment"	"Uo Units"	"Ligand Efficiency BEI"	"Ligand Efficiency LE"	"Ligand Efficiency LLE"	"Ligand Efficiency SEI"	"Potential Duplicate"	"Assay ChEMBL ID"	"Assay Description"	"Assay Type"	"BAO Format ID"	"BAO Label"	"Assay Organism"	"Assay Tissue ChEMBL ID"	"Assay Tissue Name"	"Assay Cell Type"	"Assay Subcellular Fraction"	"Assay Parameters"	"Assay Variant Accession"	"Assay Variant Mutation"	"Target ChEMBL ID"	"Target Name"	"Target Organism"	"Target Type"	"Document ChEMBL ID"	"Source ID"	"Source Description"	"Document Journal"	"Document Year"	"Cell ChEMBL ID"	"Properties"
"CHEMBL4740298"	""	"0"	"383.42"	"0"	"2.54"	"21, cis isomer"	"Cn1cc(-c2cn3nccc3c(-c3cnn([C@]4(CC#N)C[C@H](C#N)C4)c3)n2)cn1"	"IC50"	"'='"	"22.0"	"nM"	"7.66"	""	""	""	""	""	""	""	"False"	"CHEMBL4675820"	"Inhibition of JAK2 homodimer signaling pathway in human whole blood spiked with CD34 +ve cells assessed as reduction in EPO induced STAT5 phosphorylation preincubated for 45 mins followed by EPO addition and measured measured after 15 mins by immunostaining based FACS assay"	"A"	"BAO_0000221"	"tissue-based format"	"Homo sapiens"	"None"	"Blood"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4673239"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 1.0 hr"
"CHEMBL584944"	""	"0"	"377.43"	"0"	"3.86"	"45"	"CCC[C@@H](Nc1cc(-c2c(N)nn3cccnc23)ncn1)c1ccc(F)cc1"	"IC50"	"'='"	"75.0"	"nM"	"7.12"	""	""	"UO_0000065"	"18.88"	"0.35"	"3.26"	"7.58"	"False"	"CHEMBL1044320"	"Inhibition of JAK2-mediated STAT5 phosphorylation in GMCSF-stimulated human TF1 cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"CHEMBL3307972"	""
"CHEMBL584322"	""	"0"	"345.41"	"0"	"2.80"	"30"	"CCN(Cc1ccccc1)c1cc(-c2c(N)nn3cccnc23)ncn1"	"IC50"	"'='"	"34.0"	"nM"	"7.47"	""	""	"UO_0000065"	"21.62"	"0.39"	"4.67"	"8.76"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL569739"	""	"0"	"346.40"	"0"	"2.19"	"31"	"CCN(Cc1ccncc1)c1cc(-c2c(N)nn3cccnc23)ncn1"	"IC50"	"'='"	"560.0"	"nM"	"6.25"	""	""	"UO_0000065"	"18.05"	"0.33"	"4.06"	"6.37"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL4083249"	""	"0"	"409.42"	"1"	"5.54"	"25"	"C[C@@H](c1ccc(F)cc1)n1nnc2cnc3ccc(-c4ccc5ocnc5c4)cc3c21"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4014128"	"Inhibition of recombinant human JAK2 expressed in insect cells using Poly(Glu:Tyr) as substrate in presence of [gamma-32]-ATP"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4011657"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL1576722"	""	"0"	"334.32"	"0"	"1.93"	"SID14740354"	"COc1ccccc1-c1nnc(Sc2nc([N+](=O)[O-])nn2C)o1"	"IC50"	"'='"	"4653.0"	"nM"	"5.33"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1399938"	""	"0"	"273.76"	"0"	"3.77"	"SID24836633"	"Cc1cccc(N(Cc2ccccc2)C(=O)CCl)c1"	"IC50"	"'='"	"1631.0"	"nM"	"5.79"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL3975089"	""	"0"	"533.64"	"1"	"4.37"	"230"	"Cc1onc(-c2ccccc2)c1CN1CCC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'>'"	"100.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3954565"	""	"0"	"508.65"	"1"	"2.87"	"252"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(S(=O)(=O)C3CCCCC3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL2403108"	"CERITINIB"	"4"	"558.15"	"2"	"6.36"	"15b, LDK378"	"Cc1cc(Nc2ncc(Cl)c(Nc3ccccc3S(=O)(=O)C(C)C)n2)c(OC(C)C)cc1C1CCNCC1"	"IC50"	"'='"	"610.0"	"nM"	"6.21"	""	""	"UO_0000065"	"11.13"	"0.22"	"-0.15"	"5.91"	"False"	"CHEMBL2406333"	"Inhibition of JAK2 (unknown origin) after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2401692"	"1"	"Scientific Literature"	"J. Med. Chem."	"2013"	"None"	""
"CHEMBL3702906"	""	"0"	"479.57"	"0"	"2.85"	"BDBM147605"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)NCc3ccccn3)cc2)n1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"285535"	"UO_0000065"	"17.51"	"0.34"	"5.55"	"5.39"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3658096"	""	"0"	"643.71"	"2"	"6.19"	"BDBM148367"	"Cc1ccc(NC(=O)c2cccc(C(F)(F)F)c2)cc1N1CCc2nc(Nc3ccc(C(=O)NC4CCN(C)CC4)cc3)ncc2C1"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"286782"	"UO_0000065"	"12.67"	"0.24"	"1.96"	"7.96"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3905818"	""	"0"	"516.50"	"1"	"4.37"	"BDBM228901"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(c2ccc(C(O)C(F)(F)F)cc2)CC1"	"IC50"	"'='"	"37.0"	"nM"	"7.43"	""	"400648"	"UO_0000065"	"14.39"	"0.27"	"3.06"	"6.18"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3942738"	""	"0"	"485.47"	"0"	"3.77"	"BDBM228911"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(c2ccc(OC(F)F)cn2)CC1"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	"400658"	"UO_0000065"	"15.95"	"0.30"	"3.97"	"6.34"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3702996"	""	"0"	"476.50"	"0"	"3.60"	"BDBM147706"	"CC1(CN[C@@H]2CC[C@H](n3cc(C(N)=O)c(Nc4ccc(C(F)(F)F)cc4)n3)[C@@H](C#N)C2)COC1"	"IC50"	"'='"	"21.0"	"nM"	"7.68"	""	"285640"	"UO_0000065"	"16.11"	"0.31"	"4.08"	"6.51"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702924"	""	"0"	"375.38"	"0"	"3.58"	"BDBM147623"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(OC(F)F)cc2)n1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"285553"	"UO_0000065"	"22.11"	"0.42"	"4.72"	"7.83"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645049"	""	"0"	"519.05"	"2"	"5.07"	"BDBM99816"	"COc1cc(Cl)ccc1-c1cccn2nc(Nc3cccc(C4CCN(CC(=O)N(C)C)CC4)c3)nc12"	"IC50"	"'='"	"15.23"	"nM"	"7.82"	""	"216489"	"UO_0000065"	"15.06"	"0.29"	"2.75"	"10.42"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703043"	""	"0"	"446.48"	"0"	"3.77"	"BDBM147753"	"N#C[C@H]1C[C@@H](N2CCC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(CC(F)(F)F)cc2)n1"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	"285687"	"UO_0000065"	"17.46"	"0.33"	"4.03"	"7.80"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3937204"	""	"0"	"320.36"	"0"	"1.33"	"BDBM228723"	"CN(c1cnc(C#N)cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399643"	"UO_0000065"	"32.03"	"0.58"	"8.93"	"10.51"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3937835"	""	"0"	"319.37"	"0"	"1.94"	"BDBM228676"	"CN(c1ccnc(C#N)c1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399657"	"UO_0000065"	"32.12"	"0.58"	"8.32"	"12.11"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3890208"	""	"0"	"492.53"	"0"	"3.41"	"BDBM228759"	"CN(c1c(F)cc(C(=O)N[C@H](CO)c2ccccc2)cc1F)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399690"	"UO_0000065"	"20.83"	"0.39"	"6.85"	"10.54"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3335692"	""	"0"	"428.56"	"0"	"3.13"	"BDBM112530"	"CC(C)CS(=O)(=O)N1C[C@@H](C)C[C@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.07"	"nM"	"10.15"	""	"233769"	"UO_0000065"	"23.70"	"0.46"	"7.02"	"9.78"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3980318"	""	"0"	"363.38"	"0"	"2.45"	"BDBM228786"	"CN(c1ccc(C#N)cc1[N+](=O)[O-])[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399724"	"UO_0000065"	"25.48"	"0.47"	"6.81"	"8.05"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL2062807"	""	"0"	"511.63"	"1"	"2.77"	"BDBM99619"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4cccc(CN5CCS(=O)(=O)CC5)c4)nc23)cc1"	"IC50"	"'='"	"0.67"	"nM"	"9.17"	""	"216309"	"UO_0000065"	"17.93"	"0.36"	"6.40"	"8.07"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647853"	""	"0"	"391.38"	"0"	"2.55"	"BDBM147963"	"N#C[C@H]1C[C@@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(OC(F)F)cc2)n1"	"IC50"	"'='"	"75.0"	"nM"	"7.12"	""	"285897"	"UO_0000065"	"18.20"	"0.35"	"4.57"	"5.65"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665174"	""	"0"	"406.90"	"0"	"2.51"	"BDBM112567"	"CS(=O)(=O)N1CCC[C@H](Nc2ncccc2-c2cnc3[nH]cc(Cl)c3n2)C1"	"IC50"	"'='"	"0.0398"	"nM"	"10.40"	""	"233804"	"UO_0000065"	"25.56"	"0.53"	"7.89"	"10.01"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3699472"	""	"0"	"325.37"	"0"	"1.95"	"BDBM147487"	"N#C[C@H]1C(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCC[C@@H]1O"	"IC50"	"'='"	"100.0"	"nM"	"7.00"	""	"285412"	"UO_0000065"	"21.51"	"0.40"	"5.05"	"5.98"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702890"	""	"0"	"546.70"	"1"	"4.62"	"BDBM147589"	"N#C[C@@H]1CCCC[C@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)N3CCC(Cc4ccccc4)CC3)cc2)n1"	"IC50"	"'='"	"67.0"	"nM"	"7.17"	""	"285519"	"UO_0000065"	"13.12"	"0.25"	"2.55"	"5.35"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3658126"	""	"0"	"581.99"	"2"	"5.46"	"BDBM148448"	"CNC(=O)c1ccc(Nc2ncc3c(n2)CCN(c2cc(NC(=O)c4cc(C(F)(F)F)ccn4)ccc2Cl)C3)cc1"	"IC50"	"'='"	"6.4"	"nM"	"8.19"	""	"286811"	"UO_0000065"	"14.08"	"0.27"	"2.73"	"7.31"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3360354"	""	"0"	"390.49"	"0"	"2.49"	"BDBM103732"	"CN1CCN(Cc2ccc(-c3cccc4nc(NC(=O)C5CC5)nn34)cc2)CC1"	"IC50"	"'='"	"5070.0"	"nM"	"5.29"	""	"221717"	"UO_0000065"	"13.56"	"0.25"	"2.80"	"8.05"	"False"	"CHEMBL3707887"	"Inhibition Assay: In vitro inhibition assay using various enzyme."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638964"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3694595"	""	"0"	"518.00"	"1"	"4.65"	"BDBM125916"	"N#Cc1ccccc1S(=O)(=O)Nc1ccc2cc1CCc1cncc(c1)Nc1ncc(Cl)c(n1)NC2"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"255689"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707544"	"In Vitro Kinase Assay: One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Biochemistry 1999, 269, 94-104. The catalytic domains of human JAK1 (a.a. 837-1142), JAK2 (a.a. 828-1132) and JAK3 (a.a. 781-1124) with an N-terminal His tag were expressed using baculovirus in insect cells and purified. The catalytic activity of JAK1, JAK2 or JAK3 was assayed by measuring the phosphorylation of a biotinylated peptide. The phosphorylated peptide was detected by homogenous time resolved fluorescence (HTRF). IC50s of compounds were measured for each kinase in the reactions that contain the enzyme, ATP and 500 nM peptide in 50 mM Tris (pH 7.8) buffer with 100 mM NaCl, 5 mM DTT, and 0.1 mg/mL (0.01%) BSA. The ATP concentration in the reactions was 90 uM for JAK1, 30 uM for JAK2 and 3 uM for JAK3. Reactions were carried out at room temperature for 1 hr and then stopped with 20 uL 45 mM EDTA."	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639093"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL2376439"	""	"0"	"513.56"	"1"	"2.36"	"12d"	"CC(=O)N[C@@H]1CCc2ccc(Oc3cnc4[nH]cc(C(=O)N[C@@H](C(=O)N5CC(C#N)C5)C5CC5)c4n3)cc21"	"IC50"	"'='"	"39.0"	"nM"	"7.41"	""	""	"UO_0000065"	"14.43"	"0.27"	"5.05"	"4.84"	"False"	"CHEMBL2378977"	"Inhibition of JAK2 (unknown origin) expressed in SF21 cells using Biotin-KAIETDKEYYTVKD as substrate and [33Pgamma]ATP incubated for 10 mins prior to substrate addition measured after 30 mins by Topcount analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375291"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"CHEMBL4106362"	""
"CHEMBL3644620"	""	"0"	"566.64"	"2"	"5.01"	"2; PF-06263276"	"CCc1cc(O)c(F)cc1-c1ccc2c(-c3nc4c([nH]3)CCN(C(=O)c3cnc(N5CCCCC5)cn3)C4)n[nH]c2c1"	"IC50"	"'='"	"23.1"	"nM"	"7.64"	""	""	"UO_0000065"	"13.48"	"0.25"	"2.63"	"6.02"	"False"	"CHEMBL4003453"	"Inhibition of GST tagged human recombinant JAK2 catalytic domain expressed in baculovirus using peptide substrate preincubated for 60 mins followed by substrate addition and measured after 60 mins by microfluidic assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4002590"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL2376332"	""	"0"	"324.38"	"0"	"3.45"	"1c"	"CCc1cccc(Oc2cnc3[nH]cc(C(=O)NC(C)C)c3n2)c1"	"IC50"	"'='"	"1210.0"	"nM"	"5.92"	""	""	"UO_0000065"	"18.24"	"0.34"	"2.47"	"7.41"	"False"	"CHEMBL2378977"	"Inhibition of JAK2 (unknown origin) expressed in SF21 cells using Biotin-KAIETDKEYYTVKD as substrate and [33Pgamma]ATP incubated for 10 mins prior to substrate addition measured after 30 mins by Topcount analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375291"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"CHEMBL4106362"	""
"CHEMBL2325894"	""	"0"	"338.37"	"0"	"0.94"	"2b"	"C[C@@H](NC(=O)c1c[nH]c2ncc(C3CC3)nc12)C(=O)N1CC(C#N)C1"	"IC50"	"'='"	"37.0"	"nM"	"7.43"	""	""	"UO_0000065"	"21.96"	"0.41"	"6.49"	"6.48"	"False"	"CHEMBL2378515"	"Inhibition of JAK2 (unknown origin) using [33gammaP]ATP and Biotin-KAIETDKEYYTVKD as substrate incubated for 10 mins prior to substrate addition measured after 30 mins by filtration assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375236"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL4638906"	""	"0"	"412.43"	"0"	"0.40"	"14"	"N#C[C@H]1C[C@@H]1C(=O)N[C@@]12C[C@@H]1CN(c1nc(Nc3cnn(CCO)c3)ncc1F)C2"	"IC50"	"'='"	"2167.0"	"nM"	"5.66"	""	""	"UO_0000065"	"13.73"	"0.26"	"5.26"	"4.29"	"False"	"CHEMBL4620433"	"Inhibition of human recombinant JAK2 assessed as level of phosphorylation in presence of peptide substrate FITC-KGGEEEEYFELVKK and ATP by mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4619733"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2020"	"None"	""
"CHEMBL2414549"	""	"0"	"359.43"	"0"	"4.15"	"19"	"CC(C)c1cccc(-c2cccc3nc(Nc4ccnc(CO)c4)nn23)c1"	"IC50"	"'='"	"117.0"	"nM"	"6.93"	""	""	"UO_0000065"	"19.29"	"0.35"	"2.78"	"9.20"	"False"	"CHEMBL2415128"	"Inhibition of JAK2 in human SET2 cells assessed as reduction of phosphorylated STAT5 level"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2412966"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL3921295"	""	"0"	"354.84"	"0"	"3.94"	"BDBM195908"	"CN(C)C/C=C/C(=O)Nc1cccc(-c2cnc3[nH]cc(Cl)c3c2)c1"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	"348614"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3887689"	"Biochemical Inhibition Assay: 1H-pyrrolo[2,3-b]pyridine, 1H-pyrazolo[3,4-b]pyridine and 5H-pyrrolo[2,3-b]pyrazine series of compounds exhibited over >100 fold selective against Janus and TEC family of kinases except for the BMX and TXK it had activity of 30 and 45 nM respectively."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886406"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4110902"	""	"0"	"438.53"	"0"	"3.75"	"BDBM228880"	"C[C@@H]1C[C@](CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN1C(=O)OC(C)(C)C"	"IC50"	"'='"	"614.0"	"nM"	"6.21"	""	"400627"	"UO_0000065"	"14.17"	"0.27"	"2.46"	"4.92"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3943435"	""	"0"	"428.51"	"1"	"5.40"	"BDBM195904"	"Cc1cccc(-c2c[nH]c3ncc(-c4cccc(NC(=O)/C=C/CN(C)C)c4)cc23)c1F"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	"348610"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3887689"	"Biochemical Inhibition Assay: 1H-pyrrolo[2,3-b]pyridine, 1H-pyrazolo[3,4-b]pyridine and 5H-pyrrolo[2,3-b]pyrazine series of compounds exhibited over >100 fold selective against Janus and TEC family of kinases except for the BMX and TXK it had activity of 30 and 45 nM respectively."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886406"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3906494"	""	"0"	"334.42"	"0"	"3.59"	"BDBM195907"	"Cc1c[nH]c2ncc(-c3cccc(NC(=O)/C=C/CN(C)C)c3)cc12"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	"348613"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3887689"	"Biochemical Inhibition Assay: 1H-pyrrolo[2,3-b]pyridine, 1H-pyrazolo[3,4-b]pyridine and 5H-pyrrolo[2,3-b]pyrazine series of compounds exhibited over >100 fold selective against Janus and TEC family of kinases except for the BMX and TXK it had activity of 30 and 45 nM respectively."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886406"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL2414535"	""	"0"	"477.55"	"0"	"3.02"	"31"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4ccc(C(=O)N5CCOCC5)cc4)nc23)cc1"	"IC50"	"'='"	"53.4"	"nM"	"7.27"	""	""	"UO_0000065"	"15.23"	"0.29"	"4.25"	"6.87"	"False"	"CHEMBL2415128"	"Inhibition of JAK2 in human SET2 cells assessed as reduction of phosphorylated STAT5 level"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2412966"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2414531"	""	"0"	"335.37"	"0"	"2.24"	"27"	"CCn1cc(-c2cccc3nc(Nc4ccnc(CO)c4)nn23)cn1"	"IC50"	"'='"	"115.0"	"nM"	"6.94"	""	""	"UO_0000065"	"20.69"	"0.38"	"4.70"	"7.45"	"False"	"CHEMBL2415128"	"Inhibition of JAK2 in human SET2 cells assessed as reduction of phosphorylated STAT5 level"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2412966"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL3905904"	""	"0"	"555.64"	"1"	"4.16"	"BDBM228873"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3cccc(Cn4nnc5ccccc54)c3)n2)CC1"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	"400620"	"UO_0000065"	"13.94"	"0.26"	"3.58"	"4.93"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL1835144"	""	"0"	"430.43"	"0"	"4.21"	"55"	"CC(C)[C@@H](Nc1ncc(C(N)=O)c2[nH]c3cc(-c4cnn(C)c4)ccc3c12)C(F)(F)F"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"19.80"	"0.38"	"4.31"	"8.39"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1501466"	""	"0"	"293.33"	"0"	"4.50"	"SID24809724"	"Cc1ccc2nc(C)cc(Nc3ccc([N+](=O)[O-])cc3)c2c1"	"IC50"	"'='"	"3311.0"	"nM"	"5.48"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL3214200"	""	"0"	"323.35"	"0"	"2.64"	"SID858893"	"CCCc1nc2ccccc2c(=O)n1/N=C/c1ccc(O)c(O)c1"	"IC50"	"'='"	"3619.0"	"nM"	"5.44"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1423501"	""	"0"	"343.81"	"0"	"3.74"	"SID24832230"	"O=C(CCl)N(C/C=C/c1ccccc1)c1ccc2c(c1)OCCO2"	"IC50"	"'='"	"2506.0"	"nM"	"5.60"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1560296"	""	"0"	"334.33"	"0"	"3.37"	"SID7976801"	"Cc1oc2c(O)c(O)ccc2c(=O)c1-c1cnn(-c2ccccc2)c1"	"IC50"	"'='"	"2966.0"	"nM"	"5.53"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL585"	"TRIAMTERENE"	"4"	"253.27"	"0"	"0.83"	"SID855896"	"Nc1nc(N)c2nc(-c3ccccc3)c(N)nc2n1"	"IC50"	"'='"	"4613.0"	"nM"	"5.34"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1476181"	""	"0"	"401.96"	"0"	"4.95"	"SID24783175"	"CC1CCCN(CCCNC(=O)c2cc3c(Cl)nc4ccccc4c3s2)C1"	"IC50"	"'='"	"3503.0"	"nM"	"5.46"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1416895"	""	"0"	"329.21"	"0"	"3.14"	"SID26661971"	"O=S(=O)(c1cnc(Cl)c(Cl)c1)N1CCc2ccccc21"	"IC50"	"'='"	"15840.0"	"nM"	"4.80"	""	"Not Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1444859"	""	"0"	"292.24"	"0"	"2.16"	"SID4243100"	"CS(=O)(=O)c1nc(-c2ccco2)cc(C(F)(F)F)n1"	"IC50"	"'='"	"2283.0"	"nM"	"5.64"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1467766"	""	"0"	"426.49"	"0"	"2.90"	"SID24834323"	"CN(c1ccccc1)S(=O)(=O)c1cccc(C(=O)NCCc2ccc(O)c(O)c2)c1"	"IC50"	"'>'"	"40000.0"	"nM"	""	""	"Not Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1585185"	""	"0"	"375.90"	"0"	"3.38"	"SID14729694"	"CCOc1ccc(C(=O)C(CN2CCOCC2)c2ccccc2)cc1.Cl"	"IC50"	"'='"	"2404.0"	"nM"	"5.62"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1524363"	""	"0"	"380.44"	"0"	"4.27"	"SID17402789"	"COc1ccc(N2CCc3c(C)nc4c(OC)cc(OC)cc4c32)c(OC)c1"	"IC50"	"'='"	"8322.0"	"nM"	"5.08"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL3966967"	""	"0"	"514.63"	"2"	"5.34"	"BDBM229043"	"Cc1ccc(-c2cccc(Nc3nn(C4(CC#N)CCN(C(=O)OC(C)(C)C)CC4)cc3C(N)=O)c2)cc1"	"IC50"	"'='"	"1481.0"	"nM"	"5.83"	""	"400788"	"UO_0000065"	"11.33"	"0.21"	"0.49"	"4.62"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3689518"	""	"0"	"310.36"	"0"	"1.30"	"BDBM109868"	"CC1CN(C(=O)CC#N)C12CCN(c1ncnc3[nH]ccc13)C2"	"IC50"	"'='"	"2.1"	"nM"	"8.68"	""	"230598"	"UO_0000065"	"27.96"	"0.52"	"7.38"	"9.76"	"False"	"CHEMBL3705639"	"Inhibition Assay: In the kinase reactions, fused proteins (6His tag-fused hJAK2 kinase domain (aa808-end)) which were coexpressed in Sf21 cells and purified by Ni2+/NTA agarose were used."	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638515"	"37"	"BindingDB Database"	""	"2013"	"CHEMBL4106362"	""
"CHEMBL3689519"	""	"0"	"324.39"	"0"	"1.83"	"BDBM109869"	"N#CCC(=O)N1CCCC12CCCN(c1ncnc3[nH]ccc13)C2"	"IC50"	"'='"	"4.7"	"nM"	"8.33"	""	"230599"	"UO_0000065"	"25.67"	"0.47"	"6.50"	"9.37"	"False"	"CHEMBL3705639"	"Inhibition Assay: In the kinase reactions, fused proteins (6His tag-fused hJAK2 kinase domain (aa808-end)) which were coexpressed in Sf21 cells and purified by Ni2+/NTA agarose were used."	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638515"	"37"	"BindingDB Database"	""	"2013"	"CHEMBL4106362"	""
"CHEMBL4110763"	""	"0"	"328.35"	"0"	"1.54"	"BDBM237718"	"N#C[C@H]1CCNC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"125.0"	"nM"	"6.90"	""	"414822"	"UO_0000065"	"21.02"	"0.39"	"5.36"	"6.35"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL1650725"	""	"0"	"328.36"	"0"	"2.66"	"9f"	"Cc1cc(Nc2nc(N[C@@H](C)c3ncc(F)cn3)ncc2C)n[nH]1"	"IC50"	"'<'"	"3.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1656588"	"Inhibition of JAK2 using Km ATP concentration"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1650731"	""	"0"	"361.36"	"0"	"2.25"	"9l"	"C[C@H](Nc1ncc(F)c(Nc2cc(N(C)C)[nH]n2)n1)c1ncc(F)cn1"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	""	"UO_0000065"	"21.57"	"0.41"	"5.55"	"7.25"	"False"	"CHEMBL1656588"	"Inhibition of JAK2 using Km ATP concentration"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1650736"	""	"0"	"433.42"	"0"	"2.03"	"16e"	"COc1cc(Nc2nc(N[C@@H](C)c3ncc(F)cn3)nc(N3CCOCC3)c2F)n[nH]1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	""	"UO_0000065"	"19.38"	"0.37"	"6.37"	"6.67"	"False"	"CHEMBL1656588"	"Inhibition of JAK2 using Km ATP concentration"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1650728"	""	"0"	"409.22"	"0"	"2.82"	"9i"	"COc1cc(Nc2nc(N[C@@H](C)c3ncc(F)cn3)ncc2Br)n[nH]1"	"IC50"	"'='"	"108.0"	"nM"	"6.97"	""	""	"UO_0000065"	"17.02"	"0.38"	"4.15"	"6.14"	"False"	"CHEMBL1656589"	"Inhibition of JAK2 using 5 mM of ATP"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL3360318"	""	"0"	"308.34"	"0"	"2.75"	"3"	"COc1ccc(-c2cccc3nc(NC(=O)C4CC4)nn23)cc1"	"IC50"	"'='"	"138.0"	"nM"	"6.86"	""	""	"UO_0000065"	"22.25"	"0.41"	"4.11"	"10.01"	"False"	"CHEMBL3388144"	"Inhibition of human recombinant JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351789"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL3907944"	""	"0"	"364.43"	"0"	"3.91"	"BDBM198323"	"CN(c1ccc(F)cc1)C1CCC(c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"24.0"	"nM"	"7.62"	""	"352401"	"UO_0000065"	"20.91"	"0.39"	"3.71"	"12.27"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3934814"	""	"0"	"360.46"	"0"	"3.46"	"BDBM198329"	"c1ccc(CCN[C@H]2CC[C@@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"940.0"	"nM"	"6.03"	""	"352407"	"UO_0000065"	"16.72"	"0.30"	"2.57"	"8.50"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3899570"	""	"0"	"418.40"	"0"	"4.14"	"BDBM198353"	"Fc1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cc1C(F)(F)F"	"IC50"	"'='"	"24.0"	"nM"	"7.62"	""	"352431"	"UO_0000065"	"18.21"	"0.35"	"3.48"	"12.27"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3974904"	""	"0"	"242.29"	"0"	"1.07"	"BDBM198219"	"c1cc2c(ncn3nnc(C4CCNCC4)c23)[nH]1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"352301"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3943768"	""	"0"	"382.45"	"0"	"2.78"	"BDBM198223"	"Cc1cc(NC(=O)N2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)sn1"	"IC50"	"'='"	"210.0"	"nM"	"6.68"	""	"352305"	"UO_0000065"	"17.46"	"0.34"	"3.90"	"6.41"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3945787"	""	"0"	"256.31"	"0"	"1.59"	"BDBM198254"	"N[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"150.0"	"nM"	"6.82"	""	"352336"	"UO_0000065"	"26.62"	"0.49"	"5.23"	"8.04"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4068357"	""	"0"	"342.45"	"0"	"2.32"	"17"	"C[C@@H]1CCN(C(=O)N2CCCC2)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"7.1"	"nM"	"8.15"	""	""	""	"23.80"	"0.45"	"5.83"	"11.92"	"False"	"CHEMBL4668313"	"Inhibition of human JAK2 using FITC-KGGEEEEYFELVKK as substrate by caliper microfluidic mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4665673"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL3936802"	""	"0"	"452.47"	"0"	"2.70"	"BDBM229121"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2cccc(F)n2)CC1"	"IC50"	"'='"	"83.0"	"nM"	"7.08"	""	"400857"	"UO_0000065"	"15.65"	"0.29"	"4.38"	"5.63"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3893287"	""	"0"	"450.42"	"0"	"2.97"	"BDBM229180"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(C(=O)OCC(F)F)CC1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"400917"	"UO_0000065"	"17.86"	"0.34"	"5.08"	"6.37"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3902263"	""	"0"	"464.45"	"0"	"3.01"	"BDBM229182"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(C(=O)OC(CF)CF)CC1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"400919"	"UO_0000065"	"17.87"	"0.34"	"5.29"	"6.57"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3950104"	""	"0"	"484.53"	"0"	"3.13"	"BDBM229194"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(C(=O)OCC2CCOCC2)CC1"	"IC50"	"'='"	"145.0"	"nM"	"6.84"	""	"400931"	"UO_0000065"	"14.11"	"0.27"	"3.71"	"5.05"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3969761"	""	"0"	"462.94"	"0"	"3.92"	"BDBM229272"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)c2ccc(Cl)cc2)CC1"	"IC50"	"'='"	"184.0"	"nM"	"6.74"	""	"401011"	"UO_0000065"	"14.55"	"0.28"	"2.82"	"5.75"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL2376152"	""	"0"	"480.89"	"0"	"2.40"	"6i"	"C[C@@H](NC(=O)c1c[nH]c2ncc(-c3nn(C)c4cc(Cl)cc(F)c34)nc12)C(=O)N1CC(C#N)C1"	"IC50"	"'='"	"56.0"	"nM"	"7.25"	""	""	"UO_0000065"	"15.08"	"0.29"	"4.85"	"5.47"	"False"	"CHEMBL2378515"	"Inhibition of JAK2 (unknown origin) using [33gammaP]ATP and Biotin-KAIETDKEYYTVKD as substrate incubated for 10 mins prior to substrate addition measured after 30 mins by filtration assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375236"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2376143"	""	"0"	"461.91"	"0"	"2.87"	"5"	"C[C@@H](NC(=O)c1c[nH]c2ncc(-c3cn(C)c4cc(Cl)ccc34)nc12)C(=O)N1CC(C#N)C1"	"IC50"	"'='"	"3.3"	"nM"	"8.48"	""	""	"UO_0000065"	"18.36"	"0.35"	"5.61"	"7.09"	"False"	"CHEMBL2378515"	"Inhibition of JAK2 (unknown origin) using [33gammaP]ATP and Biotin-KAIETDKEYYTVKD as substrate incubated for 10 mins prior to substrate addition measured after 30 mins by filtration assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375236"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2381977"	""	"0"	"434.48"	"0"	"3.06"	"1"	"Cc1cnc(Nc2nc(N[C@@H](C)c3ncc(F)cn3)c(F)c(N3CCOCC3)n2)s1"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	""	"UO_0000065"	"17.72"	"0.35"	"4.64"	"7.62"	"False"	"CHEMBL2383938"	"Inhibition of JAK2 (unknown origin) using biotinylated TYK2 peptide as substrate after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2380256"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL3651022"	""	"0"	"378.39"	"0"	"2.89"	"BDBM153199"	"CCOC(=O)c1c[nH]c2ncnc(-c3cccc(NC(=O)/C=C/C(C)=O)c3)c12"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294147"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665119"	""	"0"	"372.45"	"0"	"1.86"	"BDBM112506"	"CS(=O)(=O)N1CCC[C@@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.0292"	"nM"	"10.53"	""	"233745"	"UO_0000065"	"28.28"	"0.55"	"8.67"	"10.14"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652320"	""	"0"	"497.67"	"0"	"3.34"	"BDBM113130"	"Cc1ccc(CC2CCN(S(=O)(=O)C[C@H]3CC[C@H](N(C)c4ncnc5[nH]ccc45)CC3)CC2)nn1"	"IC50"	"'='"	"84.9"	"nM"	"7.07"	""	"234573"	"UO_0000065"	"14.21"	"0.28"	"3.73"	"6.55"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL4165758"	""	"0"	"476.58"	"0"	"3.44"	"4"	"Cc1cnc(Nc2cc(N3CCOCC3)cc(N3CCOCC3)c2)nc1Nc1cccc(CO)c1"	"IC50"	"'<'"	"3.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4145184"	"Inhibition of recombinant human JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate after 10 mins by caliper assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4138312"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4162065"	""	"0"	"547.48"	"1"	"3.37"	"9"	"CN1CCN(c2cc(Nc3ncc(Br)c(Nc4cccc(CO)c4)n3)cc(S(C)(=O)=O)c2)CC1"	"IC50"	"'='"	"363.0"	"nM"	"6.44"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4145184"	"Inhibition of recombinant human JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate after 10 mins by caliper assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4138312"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4165506"	""	"0"	"404.52"	"0"	"3.52"	"11"	"Cc1cnc(Nc2cccc(N3CCN(C)CC3)c2)nc1Nc1cccc(CO)c1"	"IC50"	"'='"	"357.0"	"nM"	"6.45"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4145184"	"Inhibition of recombinant human JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate after 10 mins by caliper assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4138312"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4166565"	""	"0"	"526.66"	"1"	"2.94"	"16"	"COCCN1CCN(c2cc(Nc3ncc(C)c(Nc4cccc(CO)c4)n3)cc(S(C)(=O)=O)c2)CC1"	"IC50"	"'='"	"1030.0"	"nM"	"5.99"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4145184"	"Inhibition of recombinant human JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate after 10 mins by caliper assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4138312"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL2381986"	""	"0"	"464.50"	"0"	"2.33"	"15"	"Cc1cc(Nc2nc(N[C@@H](C)c3ccc(F)cn3)c(F)c(N3CCS(=O)(=O)CC3)n2)n[nH]1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"18.35"	"0.36"	"6.19"	"6.62"	"False"	"CHEMBL2383938"	"Inhibition of JAK2 (unknown origin) using biotinylated TYK2 peptide as substrate after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2380256"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL3647834"	""	"0"	"479.50"	"0"	"3.54"	"BDBM147941"	"CC(C)(c1ccc(Nc2nn([C@H]3CC[C@@](C)(O)C[C@@H]3C#N)cc2C(N)=O)cc1)C(O)C(F)(F)F"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"285879"	"UO_0000065"	"17.31"	"0.33"	"4.76"	"6.05"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665204"	""	"0"	"398.45"	"0"	"1.12"	"BDBM112603"	"CS(=O)(=O)N1CCC[C@H](Nc2nc(C#N)ncc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.6186"	"nM"	"9.21"	""	"233840"	"UO_0000065"	"23.11"	"0.45"	"8.09"	"6.55"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL4283964"	""	"0"	"413.50"	"0"	"2.26"	"52"	"COc1ccc(S(=O)(=O)N2C[C@H](N(C)c3ncnc4[nH]ccc34)C3(CC3)C2)cc1"	"IC50"	"'='"	"180.0"	"nM"	"6.75"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL3765822"	""	"0"	"358.45"	"0"	"2.15"	"20"	"CC(C)[C@@H](C)n1cc(-c2cc(C(C)(C)O)n(C)n2)c2[nH]nc(N)c2c1=O"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	""	"UO_0000065"	"21.68"	"0.41"	"5.62"	"6.77"	"False"	"CHEMBL3766653"	"Inhibition of JAK2 (unknown origin) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent substrate phosphorylation after 45 mins by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3763089"	"1"	"Scientific Literature"	"J. Med. Chem."	"2016"	"None"	""
"CHEMBL1650551"	""	"0"	"454.93"	"0"	"3.47"	"25"	"Cl.[2H]C([2H])(c1cc(Nc2nc(C)cn3c(-c4cn[nH]c4)cnc23)sn1)N1CCC(F)(F)C1"	"IC50"	"'>'"	"100.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1656192"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649074"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL4290647"	""	"0"	"347.42"	"0"	"2.70"	"18"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(C(=O)c2ccccc2)CC12CC2"	"IC50"	"'='"	"6300.0"	"nM"	"5.20"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4293482"	""	"0"	"380.43"	"0"	"3.23"	"30"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(C(=O)Nc2ccc(F)cc2)CC12CC2"	"IC50"	"'='"	"1000.0"	"nM"	"6.00"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL2035185"	""	"0"	"462.55"	"0"	"4.56"	"14l, SB1578, 67:33 trans/Cis mixture"	"C1=C/COCc2cc(ccc2OCCN2CCCC2)Nc2nccc(n2)-c2ccc(o2)COC/1"	"IC50"	"'='"	"46.0"	"nM"	"7.34"	""	""	"UO_0000065"	"15.86"	"0.29"	"2.78"	"8.96"	"False"	"CHEMBL2040119"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2034857"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL3741589"	""	"0"	"366.24"	"0"	"4.09"	"29; A-971432"	"O=C(O)C1CN(Cc2ccc(OCc3ccc(Cl)c(Cl)c3)cc2)C1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3742717"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3739276"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL3262625"	""	"0"	"402.50"	"0"	"4.14"	"10d"	"Cc1c[nH]c2c(Nc3nc(N[C@@H]4CCCC[C@@H]4N)cc4cc[nH]c(=O)c34)cccc12"	"IC50"	"'='"	"300.0"	"nM"	"6.52"	""	""	"UO_0000065"	"16.21"	"0.30"	"2.38"	"5.84"	"False"	"CHEMBL3268711"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3259804"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL2103874"	"OCLACITINIB"	"0"	"337.45"	"0"	"1.50"	"BDBM185700"	"CNS(=O)(=O)C[C@H]1CC[C@H](N(C)c2ncnc3[nH]ccc23)CC1"	"IC50"	"'='"	"17.5"	"nM"	"7.76"	""	"370424"	"UO_0000065"	"22.99"	"0.46"	"6.26"	"8.53"	"False"	"CHEMBL3888064"	"JAK Enzymatic Assay: Methods: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK-2 and JAK-3) or the IRS-1 peptide (JAK-1 and Tyk-2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 microliter total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 micromolar for JAK-2 and JAK-3, 40 micromolar for JAK-1 and 7 micromolar for Tyk-2)), 2% DMSO and 1 micromolar peptide substrate (JAKtide for JAK-2 and JAK-3 or IRS-1 peptide for JAK-1 and Tyk-2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 microliter reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK-2, 1 nM JAK-3, 7 nM Tyk2 or 20 nM JAK-1. The assay was run for 240 minutes for JAK-1, 150 minutes for JAK-2, 90 minutes for JAK-3 and 60 minutes for Tyk-2."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886558"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL564365"	""	"0"	"369.47"	"0"	"4.44"	"1"	"Cc1cc2c(c(=O)[nH]1)-c1[nH]c3ccccc3c1CCN2CCc1ccccc1"	"IC50"	"'='"	"16900.0"	"nM"	"4.77"	""	""	"UO_0000065"	"12.92"	"0.23"	"0.33"	"9.20"	"False"	"CHEMBL1036442"	"Inhibition of recombinant JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1151875"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2009"	"None"	""
"CHEMBL562943"	""	"0"	"491.82"	"1"	"6.73"	"26a"	"Clc1nccc2c1-c1[nH]c3ccc(Br)cc3c1CCN2CCc1c[nH]c2ccccc12"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1036442"	"Inhibition of recombinant JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1151875"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2009"	"None"	""
"CHEMBL3262359"	""	"0"	"403.49"	"0"	"3.24"	"3e"	"Cn1ccc2cccc(Nc3nc(N[C@@H]4CCCC[C@@H]4N)cc4nc[nH]c(=O)c34)c21"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3268711"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3259804"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3652406"	""	"0"	"407.54"	"0"	"1.74"	"BDBM113218"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCC(C)(O)C2)CC1"	"IC50"	"'='"	"0.0366"	"nM"	"10.44"	""	"234661"	"UO_0000065"	"25.61"	"0.51"	"8.70"	"10.19"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3699519"	""	"0"	"327.36"	"0"	"3.12"	"BDBM147537"	"N#C[C@H]1CCCCC1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"22.0"	"nM"	"7.66"	""	"285467"	"UO_0000065"	"23.39"	"0.44"	"4.54"	"7.92"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3116064"	""	"0"	"366.36"	"0"	"2.00"	"13g"	"C[C@H](Nc1nc(Nc2cn(C)cn2)c2nccnc2n1)c1ncc(F)cn1"	"IC50"	"'='"	"800.0"	"nM"	"6.10"	""	""	"UO_0000065"	"16.64"	"0.31"	"4.10"	"5.11"	"False"	"CHEMBL3118240"	"Inhibition of Jak2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112447"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL1923570"	""	"0"	"346.39"	"0"	"4.16"	"8"	"COc1ccc(Nc2ncc3ccc(-c4ccccc4OC)n3n2)cc1"	"IC50"	"'='"	"0.5"	"nM"	"9.30"	""	""	"UO_0000065"	"26.85"	"0.49"	"5.14"	"15.33"	"False"	"CHEMBL1926252"	"Inhibition of human recombinant JAK2 using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate after 20 mins by fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1921765"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1923589"	""	"0"	"433.49"	"0"	"3.43"	"30"	"COc1ccc(-c2ccc3cnc(Nc4ccc(N5CCN(C)CC5)c(F)c4)nn23)cn1"	"IC50"	"'='"	"0.4"	"nM"	"9.40"	""	""	"UO_0000065"	"21.68"	"0.40"	"5.97"	"13.27"	"False"	"CHEMBL1926252"	"Inhibition of human recombinant JAK2 using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate after 20 mins by fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1921765"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL3676073"	""	"0"	"455.49"	"0"	"2.84"	"BDBM127834"	"CC1(C)OCC(COc2cc(F)cc([C@H]3CCCN3c3ccn4ncc(C(N)=O)c4n3)c2)O1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258502"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL1923574"	""	"0"	"458.57"	"0"	"3.65"	"13"	"COc1ccccc1-c1ccc2cnc(Nc3ccc(N4CCN(C[C@H](C)O)CC4)cc3)nn12"	"IC50"	"'='"	"0.47"	"nM"	"9.33"	""	""	"UO_0000065"	"20.34"	"0.37"	"5.68"	"11.93"	"False"	"CHEMBL1926252"	"Inhibition of human recombinant JAK2 using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate after 20 mins by fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1921765"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1091190"	""	"0"	"561.66"	"1"	"4.10"	"11"	"COc1cc(-c2cnc3cc(C)cc(-c4ccc(CC(=O)N5CCS(=O)(=O)CC5)cc4)c3n2)cc(OC)c1OC"	"IC50"	"'='"	"4200.0"	"nM"	"5.38"	""	""	"UO_0000065"	"9.57"	"0.18"	"1.28"	"4.98"	"False"	"CHEMBL1116984"	"Inhibition of recombinant GST tagged JAK2 protein after 60 mins using FITC-GGEEEEYFELVKKKK-NH2 substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156975"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL3968775"	""	"0"	"473.52"	"0"	"3.04"	"BDBM229107"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2ccnc3[nH]ccc23)CC1"	"IC50"	"'='"	"72.0"	"nM"	"7.14"	""	"400843"	"UO_0000065"	"15.08"	"0.28"	"4.10"	"5.05"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3932521"	""	"0"	"472.52"	"0"	"3.13"	"BDBM227957"	"COCC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CC1"	"IC50"	"'='"	"74.0"	"nM"	"7.13"	""	"400908"	"UO_0000065"	"15.09"	"0.29"	"4.00"	"5.26"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3932521"	""	"0"	"472.52"	"0"	"3.13"	"BDBM227957"	"COCC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CC1"	"IC50"	"'='"	"40.0"	"nM"	"7.40"	""	"400910"	"UO_0000065"	"15.66"	"0.30"	"4.27"	"5.46"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3911136"	""	"0"	"482.44"	"0"	"3.66"	"BDBM229176"	"CC(OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CC1)C(F)(F)F"	"IC50"	"'='"	"28.0"	"nM"	"7.55"	""	"400913"	"UO_0000065"	"15.66"	"0.30"	"3.89"	"5.98"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3976884"	""	"0"	"391.44"	"0"	"1.87"	"BDBM229319"	"N#CCC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)CC1"	"IC50"	"'='"	"77.0"	"nM"	"7.11"	""	"401058"	"UO_0000065"	"18.17"	"0.34"	"5.24"	"5.05"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3906783"	""	"0"	"402.48"	"0"	"1.39"	"BDBM229322"	"CS(=O)(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)CC1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"401061"	"UO_0000065"	"21.18"	"0.42"	"7.13"	"6.36"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3979025"	""	"0"	"499.00"	"0"	"3.47"	"BDBM229332"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(S(=O)(=O)c2ccccc2Cl)CC1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"401071"	"UO_0000065"	"16.12"	"0.32"	"4.58"	"6.00"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4107427"	""	"0"	"457.54"	"0"	"3.81"	"BDBM229352"	"Cc1cc(C)c(NC(=O)N2CC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)C2)c(C)c1"	"IC50"	"'='"	"1435.0"	"nM"	"5.84"	""	"401091"	"UO_0000065"	"12.77"	"0.23"	"2.03"	"4.53"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4115252"	""	"0"	"451.44"	"0"	"3.16"	"BDBM229361"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CN(C(=O)Nc2ccc(F)c(F)c2)C1"	"IC50"	"'='"	"173.0"	"nM"	"6.76"	""	"401100"	"UO_0000065"	"14.98"	"0.28"	"3.60"	"5.24"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4110229"	""	"0"	"463.93"	"0"	"3.84"	"BDBM229362"	"Cc1c(Cl)cccc1NC(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"249.0"	"nM"	"6.60"	""	"401101"	"UO_0000065"	"14.23"	"0.27"	"2.76"	"5.12"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3966245"	""	"0"	"544.58"	"1"	"4.09"	"BDBM229397"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)F)cc3)n2)CCC(Nc2ccc(O)cc2)CC1"	"IC50"	"'='"	"36.0"	"nM"	"7.44"	""	"401136"	"UO_0000065"	"13.67"	"0.27"	"3.35"	"4.56"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3951181"	""	"0"	"450.49"	"0"	"4.67"	"BDBM228196"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(Nc2ccc(F)cc2)CC1"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	"401148"	"UO_0000065"	"17.76"	"0.33"	"3.33"	"7.36"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3974509"	""	"0"	"513.60"	"1"	"3.11"	"BDBM229284"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)c2ccc(N3CCOCC3)cc2)CC1"	"IC50"	"'='"	"704.0"	"nM"	"6.15"	""	"401023"	"UO_0000065"	"11.98"	"0.22"	"3.04"	"4.75"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3898144"	""	"0"	"465.44"	"0"	"1.51"	"BDBM229314"	"CC(O)(C(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CC1)C(F)F"	"IC50"	"'='"	"38.0"	"nM"	"7.42"	""	"401053"	"UO_0000065"	"15.94"	"0.31"	"5.91"	"4.94"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3938808"	""	"0"	"452.41"	"0"	"3.05"	"BDBM229316"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(C(=O)CC(F)(F)F)CC1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"401055"	"UO_0000065"	"18.35"	"0.35"	"5.25"	"7.09"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3956020"	""	"0"	"481.96"	"0"	"4.25"	"BDBM229492"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(NCc2cccc(Cl)c2)CC1"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	"401257"	"UO_0000065"	"16.12"	"0.31"	"3.52"	"6.39"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3894692"	""	"0"	"448.51"	"0"	"3.76"	"BDBM229521"	"N#CC[C@]1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CC[C@@H](n2cc(C3CC3)nn2)CC1"	"IC50"	"'='"	"195.0"	"nM"	"6.71"	""	"401272"	"UO_0000065"	"14.96"	"0.28"	"2.95"	"5.27"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3930998"	""	"0"	"455.49"	"0"	"2.06"	"BDBM229292"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(C(=O)CC2CCCO2)CC1"	"IC50"	"'='"	"42.0"	"nM"	"7.38"	""	"401031"	"UO_0000065"	"16.20"	"0.31"	"5.32"	"5.30"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3907066"	""	"0"	"468.54"	"0"	"1.55"	"BDBM229327"	"Cn1cnc(S(=O)(=O)N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)CC2)c1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"401066"	"UO_0000065"	"17.17"	"0.33"	"6.50"	"5.30"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3908148"	""	"0"	"478.58"	"0"	"2.96"	"BDBM229328"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(S(=O)(=O)Cc2ccccc2)CC1"	"IC50"	"'='"	"35.0"	"nM"	"7.46"	""	"401067"	"UO_0000065"	"15.58"	"0.30"	"4.50"	"5.56"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3900229"	""	"0"	"457.54"	"0"	"3.75"	"BDBM229363"	"CCc1cccc(C)c1NC(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"1194.0"	"nM"	"5.92"	""	"401102"	"UO_0000065"	"12.95"	"0.24"	"2.17"	"4.59"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4107692"	""	"0"	"459.51"	"0"	"3.20"	"BDBM229376"	"COc1ccc(NC(=O)N2CC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)C2)c(C)c1"	"IC50"	"'='"	"233.0"	"nM"	"6.63"	""	"401115"	"UO_0000065"	"14.43"	"0.27"	"3.43"	"4.80"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3925801"	""	"0"	"441.51"	"0"	"2.27"	"BDBM229403"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(N2CCC(O)CC2)CC1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"401142"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3902507"	""	"0"	"528.59"	"1"	"4.43"	"BDBM229434"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc([S+]([O-])C(F)F)cc3)n2)CCC(Nc2ccc(O)cc2)CC1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"401188"	"UO_0000065"	"16.12"	"0.31"	"4.09"	"5.84"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3923485"	""	"0"	"437.48"	"0"	"1.90"	"BDBM229118"	"Cn1nccc1CN1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CC1"	"IC50"	"'='"	"37.0"	"nM"	"7.43"	""	"400854"	"UO_0000065"	"16.99"	"0.32"	"5.53"	"5.69"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3919665"	""	"0"	"510.54"	"1"	"2.93"	"BDBM229471"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)F)cc3)n2)CCC(N2CC(F)C2)CC1"	"IC50"	"'='"	"323.0"	"nM"	"6.49"	""	"401219"	"UO_0000065"	"12.71"	"0.25"	"3.56"	"4.84"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3919665"	""	"0"	"510.54"	"1"	"2.93"	"BDBM229471"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)F)cc3)n2)CCC(N2CC(F)C2)CC1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"401233"	"UO_0000065"	"17.63"	"0.35"	"6.07"	"6.71"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL2062796"	""	"0"	"364.43"	"0"	"3.54"	"21"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4ccccc4)nc23)cc1"	"IC50"	"'='"	"1.5"	"nM"	"8.82"	""	""	"UO_0000065"	"24.21"	"0.46"	"5.28"	"11.56"	"False"	"CHEMBL2067611"	"Inhibition of human JAK2 expressed in baculovirus using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate preincubated for 1 hr measured after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL3915696"	""	"0"	"453.57"	"0"	"3.98"	"BDBM229482"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(NCC2CCCCC2)CC1"	"IC50"	"'='"	"153.0"	"nM"	"6.82"	""	"401245"	"UO_0000065"	"15.03"	"0.28"	"2.84"	"5.60"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3937127"	""	"0"	"465.51"	"0"	"3.74"	"BDBM229486"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(NCc2ccc(F)cc2)CC1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"401249"	"UO_0000065"	"17.28"	"0.32"	"4.31"	"6.61"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3920570"	""	"0"	"481.96"	"0"	"4.25"	"BDBM228301"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(NCc2ccc(Cl)cc2)CC1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"401252"	"UO_0000065"	"18.05"	"0.35"	"4.45"	"7.15"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3970367"	""	"0"	"465.51"	"0"	"3.74"	"BDBM229491"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(NCc2cccc(F)c2)CC1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"401256"	"UO_0000065"	"17.28"	"0.32"	"4.31"	"6.61"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3904265"	""	"0"	"469.47"	"0"	"4.20"	"BDBM228214"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(Nc2ccc(F)cc2F)CC1"	"IC50"	"'='"	"506.0"	"nM"	"6.30"	""	"401166"	"UO_0000065"	"13.41"	"0.25"	"2.10"	"5.18"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3959238"	""	"0"	"536.61"	"1"	"2.73"	"BDBM228244"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)F)cc3)n2)CCC(N2CCC(O)CC2)CC1"	"IC50"	"'='"	"773.0"	"nM"	"6.11"	""	"401196"	"UO_0000065"	"11.39"	"0.23"	"3.38"	"3.96"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3952669"	""	"0"	"460.50"	"0"	"4.15"	"BDBM229439"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(N2CCC(F)(F)CC2)CC1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"401199"	"UO_0000065"	"17.47"	"0.33"	"3.90"	"8.05"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3922614"	""	"0"	"476.58"	"0"	"2.39"	"BDBM229441"	"CN(CCS(C)(=O)=O)C1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CC1"	"IC50"	"'='"	"37.0"	"nM"	"7.43"	""	"401201"	"UO_0000065"	"15.59"	"0.31"	"5.04"	"5.54"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3909552"	""	"0"	"402.45"	"0"	"2.98"	"BDBM229447"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(NCCF)CC1"	"IC50"	"'='"	"133.0"	"nM"	"6.88"	""	"401208"	"UO_0000065"	"17.09"	"0.32"	"3.90"	"6.32"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3923034"	""	"0"	"427.48"	"0"	"2.14"	"BDBM229449"	"COC1CN(C2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccnc(F)c4)n3)CC2)C1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"401210"	"UO_0000065"	"19.42"	"0.37"	"6.16"	"6.80"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3905158"	""	"0"	"421.43"	"0"	"2.67"	"BDBM229455"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(NCC(F)F)CC1"	"IC50"	"'='"	"524.0"	"nM"	"6.28"	""	"401215"	"UO_0000065"	"14.90"	"0.29"	"3.61"	"5.16"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3953754"	""	"0"	"439.42"	"0"	"2.96"	"BDBM229462"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(NCC(F)(F)F)CC1"	"IC50"	"'='"	"794.0"	"nM"	"6.10"	""	"401223"	"UO_0000065"	"13.88"	"0.27"	"3.14"	"5.01"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3950965"	""	"0"	"432.50"	"0"	"4.53"	"BDBM229470"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(Nc2ccccc2)CC1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"401231"	"UO_0000065"	"19.71"	"0.36"	"3.99"	"7.84"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3675992"	""	"0"	"398.44"	"0"	"2.37"	"BDBM127745"	"COCC(C)NC(=O)c1cnn2ccc(N3CCCC3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258419"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675997"	""	"0"	"394.45"	"0"	"3.13"	"BDBM127750"	"C[C@@H](NC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cncc(F)c3)nc12)C1CC1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258424"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676089"	""	"0"	"398.44"	"0"	"2.05"	"BDBM127854"	"CC(C)NC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)cn(C)c3=O)nc12"	"IC50"	"'='"	"445.8"	"nM"	"6.35"	""	"258519"	"UO_0000065"	"15.94"	"0.30"	"4.30"	"7.51"	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3919799"	""	"0"	"374.25"	"0"	"2.23"	"BDBM228728"	"CN(c1ncc(Br)cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399649"	"UO_0000065"	"27.41"	"0.61"	"8.03"	"13.90"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3671133"	""	"0"	"437.45"	"0"	"4.18"	"BDBM127632"	"Cc1ccc(CNC(=O)c2cnn3ccc(N4CCC[C@@H]4c4cc(F)ccc4F)nc23)o1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258306"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3671136"	""	"0"	"415.44"	"0"	"2.85"	"BDBM127635"	"CC(C)(CO)NC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258309"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3671137"	""	"0"	"484.55"	"0"	"3.19"	"BDBM127636"	"CC(C)(CN1CCOCC1)NC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258310"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3671138"	""	"0"	"357.36"	"0"	"2.71"	"BDBM127637"	"CNC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258311"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3671157"	""	"0"	"417.42"	"0"	"1.43"	"BDBM127656"	"O=C(NC[C@H](O)CO)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258330"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675909"	""	"0"	"399.40"	"0"	"2.17"	"BDBM127658"	"O=C(c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12)N1CC(O)C1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258332"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3916880"	""	"0"	"455.51"	"0"	"3.77"	"BDBM127678"	"CC1(O)CCC(NC(=O)c2cnn3ccc(N4CCC[C@@H]4c4cc(F)ccc4F)nc23)CC1"	"IC50"	"'='"	"186.0"	"nM"	"6.73"	""	"258352"	"UO_0000065"	"14.78"	"0.28"	"2.96"	"8.13"	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675948"	""	"0"	"356.36"	"0"	"1.90"	"BDBM127700"	"CONC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258374"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675950"	""	"0"	"355.37"	"0"	"2.50"	"BDBM127702"	"CONC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cccc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258376"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675951"	""	"0"	"454.51"	"0"	"2.02"	"BDBM127703"	"NC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)cc(OCCN4CCOCC4)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258377"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675999"	""	"0"	"412.47"	"0"	"2.35"	"BDBM127752"	"CC(C)(CO)CNC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258426"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676011"	""	"0"	"394.45"	"0"	"3.23"	"BDBM127764"	"O=C(c1cnn2ccc(N3CCC[C@@H]3c3cncc(F)c3)nc12)N1CCCCC1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258438"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3947883"	""	"0"	"382.42"	"0"	"2.20"	"BDBM229171"	"COC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)CC1"	"IC50"	"'='"	"235.0"	"nM"	"6.63"	""	"400907"	"UO_0000065"	"17.33"	"0.32"	"4.43"	"5.25"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3952853"	""	"0"	"471.54"	"0"	"4.25"	"BDBM229132"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(Cc2cc3ccccc3[nH]2)CC1"	"IC50"	"'='"	"64.0"	"nM"	"7.19"	""	"400868"	"UO_0000065"	"15.26"	"0.28"	"2.94"	"6.21"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3899688"	""	"0"	"422.46"	"0"	"3.36"	"BDBM229143"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(Cc2ccco2)CC1"	"IC50"	"'='"	"28.0"	"nM"	"7.55"	""	"400879"	"UO_0000065"	"17.88"	"0.33"	"4.19"	"6.68"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3975786"	""	"0"	"450.48"	"0"	"1.85"	"BDBM229156"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2cccc(=O)[nH]2)CC1"	"IC50"	"'='"	"68.0"	"nM"	"7.17"	""	"400892"	"UO_0000065"	"15.91"	"0.30"	"5.32"	"4.92"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3933703"	""	"0"	"438.53"	"0"	"3.61"	"BDBM229202"	"CC(C)(C)COC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)CC1"	"IC50"	"'='"	"249.0"	"nM"	"6.60"	""	"400939"	"UO_0000065"	"15.06"	"0.28"	"2.99"	"5.23"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4111807"	""	"0"	"386.39"	"0"	"1.76"	"BDBM229221"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CN(C(=O)OCCF)C1"	"IC50"	"'='"	"27.0"	"nM"	"7.57"	""	"400960"	"UO_0000065"	"19.59"	"0.37"	"5.81"	"5.99"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4111110"	""	"0"	"410.48"	"0"	"2.83"	"BDBM229227"	"CC(C)(C)COC(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"373.0"	"nM"	"6.43"	""	"400966"	"UO_0000065"	"15.66"	"0.29"	"3.60"	"5.09"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4115595"	""	"0"	"422.49"	"0"	"3.12"	"BDBM229228"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CN(C(=O)OC2CCCCC2)C1"	"IC50"	"'='"	"466.0"	"nM"	"6.33"	""	"400967"	"UO_0000065"	"14.99"	"0.28"	"3.21"	"5.01"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4107353"	""	"0"	"410.43"	"0"	"1.58"	"BDBM229233"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CN(C(=O)OC2CCOC2)C1"	"IC50"	"'='"	"102.0"	"nM"	"6.99"	""	"400972"	"UO_0000065"	"17.03"	"0.32"	"5.41"	"5.16"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4106727"	""	"0"	"431.46"	"0"	"2.38"	"BDBM229236"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CN(C(=O)OCc2cccnc2)C1"	"IC50"	"'='"	"271.0"	"nM"	"6.57"	""	"400975"	"UO_0000065"	"15.22"	"0.28"	"4.19"	"4.72"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4110847"	""	"0"	"338.37"	"0"	"1.20"	"BDBM229251"	"CC(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"510.0"	"nM"	"6.29"	""	"400990"	"UO_0000065"	"18.60"	"0.34"	"5.09"	"5.38"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3983063"	""	"0"	"408.51"	"0"	"3.00"	"BDBM229256"	"CC(C)(C)C(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)CC1"	"IC50"	"'='"	"91.0"	"nM"	"7.04"	""	"400995"	"UO_0000065"	"17.24"	"0.32"	"4.04"	"6.02"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3973983"	""	"0"	"458.52"	"0"	"3.36"	"BDBM229070"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(Cc2ccc3c(c2)OCO3)CC1"	"IC50"	"'='"	"78.0"	"nM"	"7.11"	""	"400806"	"UO_0000065"	"15.50"	"0.29"	"3.75"	"6.00"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3982398"	""	"0"	"467.94"	"0"	"3.82"	"BDBM229160"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2ccc(Cl)cc2)CC1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"400896"	"UO_0000065"	"17.95"	"0.35"	"4.58"	"7.44"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3974409"	""	"0"	"446.53"	"0"	"4.33"	"BDBM229162"	"CC(c1ccccc1)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CC1"	"IC50"	"'='"	"105.0"	"nM"	"6.98"	""	"400898"	"UO_0000065"	"15.63"	"0.29"	"2.65"	"6.98"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3974257"	""	"0"	"458.49"	"0"	"2.74"	"BDBM229197"	"COC(C)COC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CC1"	"IC50"	"'='"	"96.0"	"nM"	"7.02"	""	"400934"	"UO_0000065"	"15.31"	"0.29"	"4.28"	"5.18"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3946164"	""	"0"	"466.95"	"0"	"4.42"	"BDBM229081"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(Cc2ccc(Cl)cc2F)CC1"	"IC50"	"'='"	"44.0"	"nM"	"7.36"	""	"400817"	"UO_0000065"	"15.75"	"0.30"	"2.94"	"7.36"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3940820"	""	"0"	"472.59"	"0"	"4.42"	"BDBM229087"	"CC(C)Oc1ccc(CN2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)CC2)cc1"	"IC50"	"'='"	"809.0"	"nM"	"6.09"	""	"400823"	"UO_0000065"	"12.89"	"0.24"	"1.67"	"5.58"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3953137"	""	"0"	"451.51"	"0"	"2.38"	"BDBM229090"	"CCn1ccnc1CN1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CC1"	"IC50"	"'='"	"447.0"	"nM"	"6.35"	""	"400826"	"UO_0000065"	"14.06"	"0.26"	"3.97"	"4.86"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3949845"	""	"0"	"434.48"	"0"	"2.56"	"BDBM229091"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2cccnc2)CC1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"400827"	"UO_0000065"	"19.11"	"0.35"	"5.74"	"6.60"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3969454"	""	"0"	"423.46"	"0"	"1.89"	"BDBM229094"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2cn[nH]c2)CC1"	"IC50"	"'='"	"70.0"	"nM"	"7.16"	""	"400830"	"UO_0000065"	"16.90"	"0.32"	"5.26"	"5.06"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3945594"	""	"0"	"451.48"	"0"	"3.30"	"BDBM229098"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2ccccc2F)CC1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"400834"	"UO_0000065"	"19.27"	"0.36"	"5.40"	"7.71"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3948522"	""	"0"	"423.46"	"0"	"1.89"	"BDBM229102"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2ccn[nH]2)CC1"	"IC50"	"'='"	"39.0"	"nM"	"7.41"	""	"400838"	"UO_0000065"	"17.50"	"0.33"	"5.52"	"5.23"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3891090"	""	"0"	"435.47"	"0"	"1.95"	"BDBM229103"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2cnccn2)CC1"	"IC50"	"'='"	"28.0"	"nM"	"7.55"	""	"400839"	"UO_0000065"	"17.34"	"0.32"	"5.60"	"5.45"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3930143"	""	"0"	"412.56"	"0"	"3.18"	"BDBM229075"	"CSCCCN1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)CC1"	"IC50"	"'='"	"242.0"	"nM"	"6.62"	""	"400811"	"UO_0000065"	"16.04"	"0.31"	"3.44"	"6.62"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL1774056"	""	"0"	"355.35"	"0"	"3.57"	"1d"	"Cc1cc(Nc2nc(N[C@@H](C)c3ccc(F)cn3)c(C#N)cc2F)n[nH]1"	"IC50"	"'<'"	"1.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1776842"	"Inhibition of human JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1772962"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL3901137"	""	"0"	"558.59"	"1"	"4.16"	"BDBM230137"	"Cc1c(-c2c(F)cc(C(N)=O)c3[nH]c4c(c23)CC[C@H](C(C)(C)O)C4)cccc1-n1c(=O)cc2c(F)cccn2c1=O"	"IC50"	"'='"	"350.0"	"nM"	"6.46"	""	"402079"	"UO_0000065"	"11.56"	"0.22"	"2.30"	"5.27"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3959154"	""	"0"	"540.53"	"1"	"3.97"	"BDBM230139"	"Cc1c(-c2c(F)cc(C(N)=O)c3[nH]c4cc(CCO)ccc4c23)cccc1-n1c(=O)cc2c(F)cccn2c1=O"	"IC50"	"'='"	"550.0"	"nM"	"6.26"	""	"402081"	"UO_0000065"	"11.58"	"0.21"	"2.29"	"5.11"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4109645"	""	"0"	"409.43"	"0"	"2.44"	"BDBM237837"	"N#C[C@@H]1CN(Cc2ccon2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"34.0"	"nM"	"7.47"	""	"414941"	"UO_0000065"	"18.24"	"0.34"	"5.03"	"5.93"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4089234"	""	"0"	"345.79"	"0"	"2.48"	"BDBM237869"	"N#C[C@H]1CCOC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"414971"	"UO_0000065"	"24.65"	"0.48"	"6.04"	"8.04"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3900421"	""	"0"	"409.37"	"0"	"2.42"	"BDBM237872"	"N#C[C@@H]1CCOC[C@H]1n1cc(C(N)=O)c(Nc2ccc([C@H](O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"27.0"	"nM"	"7.57"	""	"414974"	"UO_0000065"	"18.49"	"0.36"	"5.15"	"6.00"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4111960"	""	"0"	"409.37"	"0"	"2.42"	"BDBM237873"	"N#C[C@H]1CCOC[C@@H]1n1cc(C(N)=O)c(Nc2ccc([C@@H](O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"0.6"	"nM"	"9.22"	""	"414975"	"UO_0000065"	"22.53"	"0.43"	"6.80"	"7.31"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4110471"	""	"0"	"362.34"	"0"	"2.16"	"BDBM237897"	"N#C[C@H]1CCOC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)F)nc2)n1"	"IC50"	"'='"	"134.0"	"nM"	"6.87"	""	"414999"	"UO_0000065"	"18.97"	"0.36"	"4.71"	"5.78"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3642302"	""	"0"	"531.69"	"1"	"3.12"	"BDBM99572"	"CN1CCN(c2ccc(Nc3nc4cccc(-c5ccc(CN6CCS(=O)(=O)CC6)cc5)n4n3)cc2)CC1"	"IC50"	"'='"	"1.1"	"nM"	"8.96"	""	"216262"	"UO_0000065"	"16.85"	"0.32"	"5.84"	"10.41"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642254"	""	"0"	"372.43"	"0"	"3.37"	"BDBM99512"	"c1cncc(-c2cccn3nc(Nc4ccc(N5CCOCC5)cc4)nc23)c1"	"IC50"	"'='"	"25.9"	"nM"	"7.59"	""	"216204"	"UO_0000065"	"20.37"	"0.37"	"4.22"	"11.23"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647730"	""	"0"	"591.64"	"1"	"1.73"	"BDBM147833"	"CN(C)S(=O)(=O)CCNC1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	"285767"	"UO_0000065"	"13.33"	"0.28"	"6.16"	"4.37"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699515"	""	"0"	"366.43"	"0"	"2.34"	"BDBM147533"	"CNC(=O)c1ccc(Nc2nn([C@H]3CCCC[C@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"226.0"	"nM"	"6.65"	""	"285463"	"UO_0000065"	"18.14"	"0.34"	"4.31"	"5.28"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647917"	""	"0"	"450.95"	"0"	"2.50"	"BDBM148029"	"CN([C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@@H](C#N)C1)S(C)(=O)=O"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"285966"	"UO_0000065"	"18.23"	"0.37"	"5.72"	"6.13"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699534"	""	"0"	"467.47"	"0"	"4.32"	"BDBM147552"	"CC(C)(c1ccc(Nc2nn([C@H]3CCCC[C@@H]3C#N)cc2C(N)=O)cc1F)[C@@H](O)C(F)(F)F"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"285482"	"UO_0000065"	"17.96"	"0.35"	"4.08"	"7.18"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642359"	""	"0"	"521.65"	"1"	"2.63"	"BDBM99635"	"CN1CCN(c2cccc(Nc3nc4c(NCc5cccnc5N(C)S(C)(=O)=O)cccn4n3)c2)CC1"	"IC50"	"'='"	"77.18"	"nM"	"7.11"	""	"216325"	"UO_0000065"	"13.63"	"0.26"	"4.48"	"6.41"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3645011"	""	"0"	"553.59"	"1"	"4.83"	"BDBM99763"	"COc1ncc(C(F)(F)F)cc1-c1cccn2nc(Nc3ccc(C4CCN(CC(=O)N(C)C)CC4)cc3)nc12"	"IC50"	"'='"	"74.59"	"nM"	"7.13"	""	"216450"	"UO_0000065"	"12.87"	"0.24"	"2.30"	"8.11"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647765"	""	"0"	"514.47"	"1"	"4.91"	"BDBM147868"	"N#C[C@H]1C[C@@H](N[C@H](C2CC2)C(F)(F)F)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"67.0"	"nM"	"7.17"	""	"285802"	"UO_0000065"	"13.94"	"0.27"	"2.26"	"6.60"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647843"	""	"0"	"373.84"	"0"	"2.99"	"BDBM147952"	"C[C@@]1(O)CC[C@H](n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	"285886"	"UO_0000065"	"20.78"	"0.41"	"4.78"	"6.64"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3891047"	""	"0"	"329.80"	"0"	"2.12"	"BDBM228780"	"CN(c1ccc(Cl)nn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399718"	"UO_0000065"	"28.08"	"0.55"	"7.14"	"12.54"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3898201"	""	"0"	"439.52"	"0"	"3.07"	"BDBM228982"	"Cc1cc(Nc2nn(C3(CC#N)CCN(C(=O)OC(C)(C)C)CC3)cc2C(N)=O)ccn1"	"IC50"	"'='"	"133.0"	"nM"	"6.88"	""	"400727"	"UO_0000065"	"15.64"	"0.29"	"3.81"	"4.94"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3899737"	""	"0"	"473.48"	"0"	"3.10"	"BDBM229006"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(C4CC4)c3)n2)CCN(C(=O)OCC(F)F)CC1"	"IC50"	"'='"	"201.0"	"nM"	"6.70"	""	"400751"	"UO_0000065"	"14.14"	"0.27"	"3.60"	"4.81"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3968445"	""	"0"	"496.57"	"0"	"3.08"	"BDBM229020"	"COC(=O)Cc1ccc(Nc2nn(C3(CC#N)CCN(C(=O)OC(C)(C)C)CC3)cc2C(N)=O)cc1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"400764"	"UO_0000065"	"17.16"	"0.32"	"5.44"	"5.59"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3647729"	""	"0"	"574.61"	"1"	"2.03"	"BDBM147832"	"N#C[C@H]1CC(NC2CCS(=O)(=O)C2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"285766"	"UO_0000065"	"14.19"	"0.29"	"6.12"	"4.61"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3899411"	""	"0"	"575.60"	"1"	"4.64"	"BDBM230148"	"Cc1c(-c2c(C#N)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)c2cccc(F)c2n(C)c1=O"	"IC50"	"'='"	"1900.0"	"nM"	"5.72"	""	"402027"	"UO_0000065"	"9.94"	"0.18"	"1.08"	"3.89"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3928976"	""	"0"	"587.46"	"2"	"5.69"	"BDBM230107"	"Cc1c(-c2c(Cl)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)cc2c(Cl)cccn2c1=O"	"IC50"	"'='"	"1400.0"	"nM"	"5.85"	""	"402043"	"UO_0000065"	"9.96"	"0.19"	"0.16"	"4.78"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3912426"	""	"0"	"589.00"	"2"	"5.25"	"BDBM230130"	"Cn1c(=O)n(-c2cccc(-c3c(F)cc(C(N)=O)c4[nH]c5cc(C(C)(C)O)ccc5c34)c2Cl)c(=O)c2cccc(F)c21"	"IC50"	"'>'"	"2000.0"	"nM"	""	""	"402073"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3984475"	""	"0"	"575.04"	"1"	"4.67"	"BDBM230133"	"Cc1c(-c2c(F)cc(C(N)=O)c3[nH]c4c(c23)CC[C@H](C(C)(C)O)C4)cccc1-n1c(=O)cc2c(Cl)cccn2c1=O"	"IC50"	"'>'"	"2000.0"	"nM"	""	""	"402075"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3984475"	""	"0"	"575.04"	"1"	"4.67"	"BDBM230133"	"Cc1c(-c2c(F)cc(C(N)=O)c3[nH]c4c(c23)CC[C@H](C(C)(C)O)C4)cccc1-n1c(=O)cc2c(Cl)cccn2c1=O"	"IC50"	"'>'"	"2000.0"	"nM"	""	""	"402076"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3987197"	""	"0"	"571.01"	"2"	"5.41"	"BDBM230135"	"Cc1cc(C(N)=O)c2[nH]c3cc(C(C)(C)O)ccc3c2c1-c1cccc(-n2c(=O)[nH]c3c(F)cccc3c2=O)c1Cl"	"IC50"	"'='"	"290.0"	"nM"	"6.54"	""	"402077"	"UO_0000065"	"11.45"	"0.22"	"1.13"	"4.88"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4114536"	""	"0"	"558.59"	"1"	"4.39"	"BDBM230136"	"Cc1c(-c2c(F)cc(C(N)=O)c3[nH]c4c(c23)CC[C@@H](C(C)(C)O)C4)cccc1-n1c(=O)[nH]c2c(F)cccc2c1=O"	"IC50"	"'='"	"16000.0"	"nM"	"4.80"	""	"402078"	"UO_0000065"	"8.59"	"0.16"	"0.41"	"3.58"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3932965"	""	"0"	"567.05"	"2"	"5.35"	"BDBM230140"	"Cc1cc(C(N)=O)c2[nH]c3cc(C(C)(C)O)ccc3c2c1-c1cccc(-n2c(=O)cc3c(Cl)cccn3c2=O)c1C"	"IC50"	"'='"	"800.0"	"nM"	"6.10"	""	"402082"	"UO_0000065"	"10.75"	"0.20"	"0.75"	"4.97"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4111002"	""	"0"	"363.78"	"0"	"2.62"	"BDBM237877"	"N#C[C@H]1CCOC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)c(F)c2)n1"	"IC50"	"'='"	"121.0"	"nM"	"6.92"	""	"414979"	"UO_0000065"	"19.01"	"0.38"	"4.30"	"6.53"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4108622"	""	"0"	"346.78"	"0"	"1.88"	"BDBM237892"	"N#C[C@H]1CCOC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)nc2)n1"	"IC50"	"'='"	"134.0"	"nM"	"6.87"	""	"414994"	"UO_0000065"	"19.82"	"0.39"	"4.99"	"5.78"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4108999"	""	"0"	"344.35"	"0"	"1.75"	"BDBM237915"	"C[C@H]1OCC[C@@H](C#N)[C@@H]1n1cc(C(N)=O)c(Nc2ccnc(F)c2)n1"	"IC50"	"'='"	"206.0"	"nM"	"6.69"	""	"415007"	"UO_0000065"	"19.42"	"0.37"	"4.94"	"5.63"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3652355"	""	"0"	"517.63"	"1"	"2.94"	"BDBM113166"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC[C@@](O)(COc3cccc(F)c3)C2)CC1"	"IC50"	"'='"	"26.2"	"nM"	"7.58"	""	"234609"	"UO_0000065"	"14.65"	"0.29"	"4.64"	"6.79"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3702977"	""	"0"	"520.48"	"1"	"3.11"	"BDBM147687"	"N#C[C@H]1C[C@@H](NCC(F)(F)F)CCC1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)F)cc2)n1"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	"285620"	"UO_0000065"	"15.37"	"0.31"	"4.89"	"5.60"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647841"	""	"0"	"451.45"	"0"	"3.11"	"BDBM147950"	"C[C@@]1(O)CC[C@H](n2cc(C(N)=O)c(Nc3ccc([C@@](C)(O)C(F)(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"285884"	"UO_0000065"	"18.60"	"0.36"	"5.29"	"6.12"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3671135"	""	"0"	"441.48"	"0"	"3.38"	"BDBM127634"	"O=C(N[C@H]1CC[C@H](O)CC1)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'='"	"106.8"	"nM"	"6.97"	""	"258308"	"UO_0000065"	"15.79"	"0.30"	"3.59"	"8.42"	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3671143"	""	"0"	"437.49"	"0"	"4.27"	"BDBM127642"	"O=C(N[C@H]1CC2CCC1C2)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'='"	"156.0"	"nM"	"6.81"	""	"258316"	"UO_0000065"	"15.56"	"0.29"	"2.54"	"10.89"	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3671152"	""	"0"	"455.47"	"0"	"2.10"	"BDBM127651"	"O=C(NCCN1CCNC1=O)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258325"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675914"	""	"0"	"381.46"	"0"	"3.74"	"BDBM127663"	"CC(C)(C)NC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cccc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258337"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675921"	""	"0"	"355.37"	"0"	"1.54"	"BDBM127670"	"CNC(=O)c1cnn2ccc(N3C[C@H](O)C[C@@H]3c3cccc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258344"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675939"	""	"0"	"467.42"	"0"	"2.31"	"BDBM127690"	"O=C(NC[C@@H](O)CO)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3C(F)(F)F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258364"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675940"	""	"0"	"393.34"	"0"	"3.33"	"BDBM127691"	"NC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3C(F)(F)F)nc12"	"IC50"	"'='"	"575.0"	"nM"	"6.24"	""	"258365"	"UO_0000065"	"15.86"	"0.30"	"2.91"	"8.16"	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675952"	""	"0"	"439.49"	"0"	"3.13"	"BDBM127704"	"COCCOc1cc(F)cc([C@H]2CCCN2c2ccn3ncc(C(=O)NC4CC4)c3n2)c1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258378"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675973"	""	"0"	"434.40"	"0"	"3.43"	"BDBM127725"	"O=C(NC1(C(F)(F)F)CC1)c1cnn2ccc(N3CCC[C@@H]3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258399"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3902802"	""	"0"	"424.48"	"0"	"2.64"	"BDBM127727"	"O=C(NC1CCC(O)CC1)c1cnn2ccc(N3CCC[C@@H]3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258401"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675993"	""	"0"	"414.44"	"0"	"1.34"	"BDBM127746"	"COCC(O)CNC(=O)c1cnn2ccc(N3CCCC3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258420"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675996"	""	"0"	"412.47"	"0"	"2.35"	"BDBM127749"	"CC(C)[C@H](CO)NC(=O)c1cnn2ccc(N3CCCC3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258423"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676000"	""	"0"	"366.40"	"0"	"2.45"	"BDBM127753"	"O=C(c1cnn2ccc(N3CCC[C@@H]3c3cncc(F)c3)nc12)N1CCC1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258427"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676007"	""	"0"	"410.45"	"0"	"2.25"	"BDBM127760"	"O=C(N[C@@H]1CCC[C@H]1O)c1cnn2ccc(N3CCC[C@@H]3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258434"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676009"	""	"0"	"410.45"	"0"	"2.25"	"BDBM127762"	"O=C(N[C@@H]1CCC[C@@H]1O)c1cnn2ccc(N3CCC[C@@H]3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258436"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676027"	""	"0"	"414.44"	"0"	"1.72"	"BDBM127783"	"COc1ncc(F)cc1[C@H]1CCCN1c1ccn2ncc(C(=O)NC[C@H](C)O)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258454"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676032"	""	"0"	"449.45"	"0"	"2.55"	"BDBM127788"	"COc1ncc(F)cc1[C@H]1CCCN1c1ccn2ncc(C(=O)Nc3ccc(=O)[nH]c3)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258459"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676034"	""	"0"	"387.39"	"0"	"2.07"	"BDBM127792"	"O=C(NCCO)c1cnn2ccc(N3CCCC3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258461"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676035"	""	"0"	"401.42"	"0"	"2.46"	"BDBM127793"	"C[C@H](O)CNC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258462"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676049"	""	"0"	"380.43"	"0"	"2.81"	"BDBM127808"	"Cc1ncc(F)cc1[C@H]1CCCN1c1ccn2ncc(C(=O)NC3CC3)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258477"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676057"	""	"0"	"398.44"	"0"	"2.02"	"BDBM127816"	"Cc1ncc(F)cc1[C@H]1CCCN1c1ccn2ncc(C(=O)NC[C@@H](C)O)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258485"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676060"	""	"0"	"396.43"	"0"	"1.73"	"BDBM127819"	"Cc1ncc(F)cc1C1CCCN1c1ccn2ncc(C(=O)N3CC(O)C3)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258488"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676086"	""	"0"	"381.42"	"0"	"2.03"	"BDBM127848"	"Nc1ncc(F)cc1[C@H]1CCCN1c1ccn2ncc(C(=O)N3CCC3)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258516"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676088"	""	"0"	"412.47"	"0"	"2.44"	"BDBM127853"	"Cn1cc(F)cc([C@H]2CCCN2c2ccn3ncc(C(=O)NC(C)(C)C)c3n2)c1=O"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258518"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676099"	""	"0"	"410.45"	"0"	"2.19"	"BDBM127864"	"Cn1cc(F)cc([C@H]2CCCN2c2ccn3ncc(C(=O)NC4(C)CC4)c3n2)c1=O"	"IC50"	"'='"	"616.0"	"nM"	"6.21"	""	"258529"	"UO_0000065"	"15.13"	"0.28"	"4.02"	"7.35"	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3647911"	""	"0"	"401.90"	"0"	"3.78"	"BDBM148023"	"[C-]#[N+][C@H]1C[C@@H](C(C)(C)O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"285958"	"UO_0000065"	"20.90"	"0.41"	"4.62"	"8.61"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652364"	""	"0"	"471.60"	"0"	"3.91"	"BDBM113175"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC[C@H](c3ccccc3F)C2)CC1"	"IC50"	"'='"	"37.4"	"nM"	"7.43"	""	"234618"	"UO_0000065"	"15.75"	"0.31"	"3.52"	"9.04"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3652306"	""	"0"	"469.63"	"0"	"1.65"	"BDBM113115"	"C[C@H]1CN(S(=O)(=O)C[C@H]2CC[C@H](N(C)c3ncnc4[nH]ccc34)CC2)C[C@H]1S(C)(=O)=O"	"IC50"	"'='"	"32.2"	"nM"	"7.49"	""	"234559"	"UO_0000065"	"15.95"	"0.33"	"5.84"	"6.44"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3665191"	""	"0"	"417.50"	"0"	"1.65"	"BDBM112588"	"CCOc1ncc(-c2cnc3[nH]ccc3n2)c(N[C@H]2CCCN(S(C)(=O)=O)C2)n1"	"IC50"	"'='"	"0.1413"	"nM"	"9.85"	""	"233825"	"UO_0000065"	"23.59"	"0.46"	"8.20"	"7.82"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703076"	""	"0"	"538.47"	"1"	"3.40"	"BDBM147788"	"N#C[C@H]1C[C@@H](NCC(F)(F)F)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"31.0"	"nM"	"7.51"	""	"285722"	"UO_0000065"	"13.94"	"0.28"	"4.11"	"5.25"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652360"	""	"0"	"561.73"	"1"	"2.98"	"BDBM113171"	"COc1ccccc1CS(=O)(=O)[C@H]1CCN(S(=O)(=O)C[C@H]2CC[C@H](N(C)c3ncnc4[nH]ccc34)CC2)C1"	"IC50"	"'='"	"17.5"	"nM"	"7.76"	""	"234614"	"UO_0000065"	"13.81"	"0.28"	"4.78"	"6.18"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3647797"	""	"0"	"440.86"	"0"	"3.76"	"BDBM147900"	"N#C[C@H]1C[C@@H](NCC(F)(F)F)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"34.0"	"nM"	"7.47"	""	"285834"	"UO_0000065"	"16.94"	"0.34"	"3.71"	"6.87"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3658855"	""	"0"	"375.46"	"0"	"0.60"	"BDBM159774"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@H](NS(=O)(=O)N2CCC(C#N)C2)C1"	"IC50"	"'='"	"3370.0"	"nM"	"5.47"	""	"302584"	"UO_0000065"	"14.58"	"0.29"	"4.87"	"4.64"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665178"	""	"0"	"429.55"	"0"	"2.53"	"BDBM112571"	"CC(C)(C)NS(=O)(=O)N1CCC[C@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.2215"	"nM"	"9.65"	""	"233808"	"UO_0000065"	"22.48"	"0.44"	"7.12"	"8.33"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647855"	""	"0"	"394.36"	"0"	"2.37"	"BDBM147965"	"N#C[C@H]1C[C@@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)nc2)n1"	"IC50"	"'='"	"65.0"	"nM"	"7.19"	""	"285899"	"UO_0000065"	"18.22"	"0.35"	"4.82"	"5.53"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645092"	""	"0"	"570.59"	"2"	"5.21"	"BDBM99866"	"CN(C)C(=O)CN1CCc2ccc(Nc3nc4c(-c5cc(C(F)F)ccc5OCC(F)F)cccn4n3)cc2CC1"	"IC50"	"'='"	"269.87"	"nM"	"6.57"	""	"216534"	"UO_0000065"	"11.51"	"0.22"	"1.36"	"8.76"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647883"	""	"0"	"468.87"	"0"	"3.54"	"BDBM147995"	"N#C[C@@H]1C[C@H](C(=O)NCC(F)(F)F)CCC1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"38.0"	"nM"	"7.42"	""	"285930"	"UO_0000065"	"15.83"	"0.32"	"3.88"	"5.90"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL1446198"	""	"0"	"277.33"	"0"	"3.65"	"BDBM107122"	"CCC(=O)Nc1cccc(-c2cnc3ccccc3n2)c1"	"IC50"	"'>'"	"50000.0"	"nM"	""	""	"226359"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703078"	""	"0"	"383.43"	"0"	"2.20"	"BDBM147791"	"N#C[C@H]1C[C@@H](N2CCC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccnc(F)c2)n1"	"IC50"	"'='"	"37.0"	"nM"	"7.43"	""	"285725"	"UO_0000065"	"19.38"	"0.36"	"5.23"	"6.58"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642327"	""	"0"	"323.40"	"0"	"1.66"	"BDBM99599"	"NC1CCN(c2nc3c(NCc4cccnc4)cccn3n2)CC1"	"IC50"	"'='"	"9999.0"	"nM"	"5.00"	""	"216289"	"UO_0000065"	"15.46"	"0.28"	"3.34"	"5.93"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642369"	""	"0"	"492.57"	"0"	"2.39"	"BDBM99645"	"CN1C(=O)Cc2cc(Nc3nc4c(NCc5cccnc5N(C)S(C)(=O)=O)cccn4n3)ccc21"	"IC50"	"'='"	"27.42"	"nM"	"7.56"	""	"216335"	"UO_0000065"	"15.35"	"0.30"	"5.17"	"6.06"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652386"	""	"0"	"481.64"	"0"	"1.79"	"BDBM113198"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC(S(=O)(=O)CC3CC3)C2)CC1"	"IC50"	"'='"	"49.9"	"nM"	"7.30"	""	"234641"	"UO_0000065"	"15.16"	"0.31"	"5.51"	"6.28"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3702957"	""	"0"	"403.46"	"0"	"1.35"	"BDBM147664"	"CS(=O)(=O)c1ccc(Nc2nn([C@H]3CC[C@@H](O)C[C@@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"285596"	"UO_0000065"	"21.12"	"0.42"	"7.17"	"5.64"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652388"	""	"0"	"483.64"	"0"	"2.81"	"BDBM113200"	"Cc1ccc(N2CCN(S(=O)(=O)C[C@H]3CC[C@H](N(C)c4ncnc5[nH]ccc45)CC3)CC2)nc1"	"IC50"	"'='"	"50.8"	"nM"	"7.29"	""	"234643"	"UO_0000065"	"15.08"	"0.29"	"4.48"	"7.42"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3703030"	""	"0"	"478.52"	"0"	"3.94"	"BDBM147740"	"CC(C)(C)N[C@@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc([C@H](O)C(F)(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"23.0"	"nM"	"7.64"	""	"285674"	"UO_0000065"	"15.96"	"0.31"	"3.70"	"5.92"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652376"	""	"0"	"531.68"	"1"	"1.30"	"BDBM113187"	"CCN1CCN(C[C@H]2CCN(S(=O)(=O)C[C@H]3CC[C@H](N(C)c4ncnc5[nH]ccc45)CC3)C2)C(=O)C1=O"	"IC50"	"'='"	"90.4"	"nM"	"7.04"	""	"234630"	"UO_0000065"	"13.25"	"0.26"	"5.74"	"5.74"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3703490"	""	"0"	"271.32"	"0"	"3.09"	"BDBM153134"	"CCOC(=O)c1c[nH]c2ncnc(C3=CCCCC3)c12"	"IC50"	"'='"	"62.0"	"nM"	"7.21"	""	"294082"	"UO_0000065"	"26.56"	"0.49"	"4.12"	"10.62"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652353"	""	"0"	"531.70"	"1"	"2.97"	"BDBM113164"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC[C@H](S(=O)(=O)Cc3ccccc3)C2)CC1"	"IC50"	"'='"	"17.4"	"nM"	"7.76"	""	"234607"	"UO_0000065"	"14.59"	"0.29"	"4.79"	"6.67"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3645048"	""	"0"	"491.00"	"0"	"4.25"	"BDBM99815"	"COc1cc(Cl)ccc1-c1cccn2nc(Nc3ccc4c(c3)CCN(CC(=O)N(C)C)C4)nc12"	"IC50"	"'='"	"21.25"	"nM"	"7.67"	""	"216488"	"UO_0000065"	"15.63"	"0.30"	"3.42"	"10.23"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3644991"	""	"0"	"497.52"	"1"	"5.64"	"BDBM99743"	"COc1ccc(C(F)(F)F)cc1-c1cccn2nc(Nc3ccc(OCCN4CCCC4)cc3)nc12"	"IC50"	"'='"	"73.74"	"nM"	"7.13"	""	"216431"	"UO_0000065"	"14.34"	"0.27"	"1.49"	"11.16"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL1553519"	""	"0"	"299.36"	"0"	"2.67"	"BDBM107130"	"CS(=O)(=O)Nc1cccc(-c2cnc3ccccc3n2)c1"	"IC50"	"'='"	"18500.0"	"nM"	"4.73"	""	"226368"	"UO_0000065"	"15.81"	"0.31"	"2.06"	"6.58"	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647789"	""	"0"	"378.48"	"0"	"3.10"	"BDBM147892"	"CC1(N[C@H]2CCC(n3cc(C(N)=O)c(Nc4ccccc4)n3)[C@@H](C#N)C2)CC1"	"IC50"	"'='"	"24.0"	"nM"	"7.62"	""	"285826"	"UO_0000065"	"20.13"	"0.37"	"4.52"	"7.01"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645073"	""	"0"	"517.61"	"2"	"6.40"	"BDBM99841"	"COc1ccc(-c2cccn3nc(Nc4ccc(C5CCN(C(=O)OC(C)(C)C)CC5)cc4)nc23)c(F)c1"	"IC50"	"'='"	"163.75"	"nM"	"6.79"	""	"216514"	"UO_0000065"	"13.11"	"0.24"	"0.39"	"8.38"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL1650953"	""	"0"	"440.43"	"0"	"3.16"	"7"	"O=C1NC(=O)C(c2c[nH]c3ccccc23)=C1c1cc(N2CCNCC2)ccc1C(F)(F)F"	"IC50"	"'='"	"4700.0"	"nM"	"5.33"	""	""	"UO_0000065"	"12.10"	"0.23"	"2.17"	"6.90"	"False"	"CHEMBL1657171"	"Inhibition of GST-tagged Jak2 expressed in insect cells using 20 uM ATP"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649080"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"2, CP-690550"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	""	"UO_0000065"	"25.36"	"0.47"	"6.38"	"8.91"	"False"	"CHEMBL1657171"	"Inhibition of GST-tagged Jak2 expressed in insect cells using 20 uM ATP"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649080"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL3645042"	""	"0"	"505.02"	"1"	"4.29"	"BDBM99809"	"COc1cc(Cl)ccc1-c1cccn2nc(Nc3ccc4c(c3)CCN(CC(=O)N(C)C)CC4)nc12"	"IC50"	"'='"	"8.48"	"nM"	"8.07"	""	"216482"	"UO_0000065"	"15.98"	"0.31"	"3.78"	"10.76"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647898"	""	"0"	"508.93"	"1"	"4.32"	"BDBM148010"	"N#C[C@@H]1C[C@H](C(=O)N[C@H](C2CC2)C(F)(F)F)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"306.0"	"nM"	"6.51"	""	"285945"	"UO_0000065"	"12.80"	"0.25"	"2.19"	"5.18"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3903725"	""	"0"	"450.38"	"0"	"3.29"	"BDBM236557"	"Nc1ccc(-c2ccc3ncc4c(=O)[nH]c(=O)n(-c5cccc(C(F)(F)F)c5)c4c3n2)cn1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	"412026"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888669"	"Mobility Shift Assay: Agents: 1-fold kinase buffer without MnCl2: 50 mM HEPES, pH 7.5, 0.0015% Brij-35, 10 mM MgCl2, 2 mM DTT. 1-fold kinase buffer with MnCl2: 50 mM HEPES, pH 7.5, 0.0015% Brij-35, 10 mM MgCl2, 10 mM MnCl2, 2 mM DTT. Termination solution: 100 mM HEPES, pH 7.5, 0.0015% Brij-35, 0.2% Coating Reagent#3, 50 mM EDTA. 2.5-fold kinase solution: The kinase was added to the 1-fold kinase buffer to form a 2.5-fold kinase solution. 2.5-fold substrate solution: FAM fluorescence-labelled polypeptide and ATP were added to the 1-fold kinase buffer to form a 2.5-fold substrate solution. Compounds: The final test concentration of the compound was 10 μM at maximum. Firstly, a 50-fold concentration (i.e. 500 μM) was prepared with 100% DMSO. The compound was diluted with 100% DMSO by 5 folds at 5 concentrations (successively 500 μM, 100 μM, 20 μM, 4 μM, and 0.8 μM). After diluting with 1-fold kinase buffer by 10 folds, 5 μl of the samples were transferred to a 384-well reaction plate. Two negative control wells and two positive control wells were set at each line respectively. Replication was made in a 96-well plate in five concentrations of 5-fold compound. 10% DMSO was added to the positive control well, and 5 μl of EDTA (250 mM) was added to the negative control well. Procedure: To the 384-well reaction plate was added 5-fold compound dissolved in 10% DMSO at 5 μl/well. To the 384-well reaction plate was added 2.5-fold kinase solution at 10 Î¼l/well. The plate was incubated at room temperature for 10 mins. To the 384-well reaction plate was added 2.5-fold substrate solution at 10 μl/well. The plate was incubated at 28° C. for a certain period. 25 μl termination solution was added to terminate the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886794"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3894307"	""	"0"	"463.45"	"0"	"2.24"	"BDBM229004"	"COc1cc(Nc2nn(C3(CC#N)CCN(C(=O)OCC(F)F)CC3)cc2C(N)=O)ccn1"	"IC50"	"'='"	"348.0"	"nM"	"6.46"	""	"400749"	"UO_0000065"	"13.94"	"0.27"	"4.22"	"4.35"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3973429"	""	"0"	"406.88"	"0"	"3.51"	"BDBM198420"	"Clc1n[nH]c2ccc(CN3CCC(c4nnn5cnc6[nH]ccc6c45)CC3)cc12"	"IC50"	"'='"	"180.0"	"nM"	"6.75"	""	"352498"	"UO_0000065"	"16.58"	"0.32"	"3.23"	"7.43"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3892159"	""	"0"	"324.43"	"0"	"2.88"	"BDBM198494"	"CC1CC1NC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"100.0"	"nM"	"7.00"	""	"352572"	"UO_0000065"	"21.58"	"0.40"	"4.12"	"9.87"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3916636"	""	"0"	"378.40"	"0"	"3.56"	"BDBM198495"	"FC(F)(F)C1(NC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)CC1"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	"352573"	"UO_0000065"	"20.53"	"0.39"	"4.21"	"10.96"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3942120"	""	"0"	"328.42"	"0"	"1.80"	"BDBM198500"	"CN(CCO)C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"100.0"	"nM"	"7.00"	""	"352578"	"UO_0000065"	"21.31"	"0.40"	"5.20"	"8.50"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3909751"	""	"0"	"399.50"	"0"	"4.30"	"BDBM198503"	"N#CCCN(C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1)c1ccccc1"	"IC50"	"'='"	"59.0"	"nM"	"7.23"	""	"352581"	"UO_0000065"	"18.10"	"0.33"	"2.93"	"8.42"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3964133"	""	"0"	"382.43"	"0"	"2.73"	"BDBM198445"	"N#Cc1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cc1C#N"	"IC50"	"'='"	"52.0"	"nM"	"7.28"	""	"352523"	"UO_0000065"	"19.05"	"0.34"	"4.55"	"6.64"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3978620"	""	"0"	"478.91"	"0"	"4.32"	"BDBM198402"	"OC(CN[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1)(c1ccc(Cl)cc1)C(F)(F)F"	"IC50"	"'='"	"35.0"	"nM"	"7.46"	""	"352480"	"UO_0000065"	"15.57"	"0.31"	"3.14"	"8.18"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3935174"	""	"0"	"366.86"	"0"	"4.40"	"BDBM198408"	"Clc1ccc(NC2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"250.0"	"nM"	"6.60"	""	"352486"	"UO_0000065"	"18.00"	"0.35"	"2.20"	"9.31"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3947749"	""	"0"	"387.45"	"0"	"2.89"	"BDBM198416"	"N#CCOc1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"190.0"	"nM"	"6.72"	""	"352494"	"UO_0000065"	"17.35"	"0.32"	"3.83"	"7.07"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3928338"	""	"0"	"438.51"	"0"	"2.43"	"BDBM198567"	"O=C(NCS(=O)(=O)c1ccccc1)[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	"352645"	"UO_0000065"	"18.15"	"0.35"	"5.53"	"6.52"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3934116"	""	"0"	"381.22"	"0"	"3.31"	"BDBM198570"	"IC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"4.3"	"nM"	"8.37"	""	"352648"	"UO_0000065"	"21.95"	"0.57"	"5.06"	"14.21"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4112119"	""	"0"	"342.42"	"0"	"2.92"	"BDBM198288"	"F[C@@H]1CCN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C1"	"IC50"	"'='"	"83.0"	"nM"	"7.08"	""	"352366"	"UO_0000065"	"20.68"	"0.39"	"4.16"	"11.40"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3906967"	""	"0"	"271.32"	"0"	"1.87"	"BDBM198202"	"OC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	"352418"	"UO_0000065"	"28.95"	"0.54"	"5.98"	"9.93"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3985119"	""	"0"	"374.47"	"0"	"1.96"	"BDBM198624"	"O=S(=O)(C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1)NC1CC1"	"IC50"	"'='"	"26.0"	"nM"	"7.58"	""	"352702"	"UO_0000065"	"20.26"	"0.40"	"5.63"	"7.22"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3622823"	""	"0"	"294.36"	"0"	"2.15"	"4b"	"NCCCn1c(-c2ccccc2)nc2cc(C(N)=O)ccc21"	"IC50"	"'='"	"20500.0"	"nM"	"4.69"	""	""	"UO_0000065"	"15.93"	"0.29"	"2.54"	"5.39"	"False"	"CHEMBL3625898"	"Inhibition of JAK2 (unknown origin) using 35 uM of ATP and Tyr6 peptide by Z'-LYTE kinase assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621116"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL3622826"	""	"0"	"287.37"	"0"	"0.56"	"5c"	"NCCn1c(C2CCNCC2)nc2cc(C(N)=O)ccc21"	"IC50"	"'='"	"437300.0"	"nM"	""	"Outside typical range"	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3625905"	"Inhibition of JAK2 (unknown origin) using 1 mM of ATP and Tyr6 peptide by Z'-LYTE kinase assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621116"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL3702963"	""	"0"	"477.49"	"0"	"3.98"	"BDBM147670"	"N#C[C@H]1C[C@H](OCC2CC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc([C@@H](O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	"285602"	"UO_0000065"	"16.45"	"0.32"	"3.87"	"6.22"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642404"	""	"0"	"505.60"	"1"	"2.15"	"BDBM99682"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4cccc(N5CCN(CC(N)=O)CC5)c4)nc23)cc1"	"IC50"	"'='"	"0.65"	"nM"	"9.19"	""	"216371"	"UO_0000065"	"18.17"	"0.35"	"7.04"	"7.30"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652334"	""	"0"	"435.59"	"0"	"2.38"	"BDBM113145"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCC[C@@](C)(CO)C2)CC1"	"IC50"	"'='"	"50.7"	"nM"	"7.29"	""	"234588"	"UO_0000065"	"16.75"	"0.33"	"4.91"	"7.12"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3622822"	""	"0"	"261.33"	"0"	"-0.01"	"4a"	"NCCCn1c(CCN)nc2cc(C(N)=O)ccc21"	"IC50"	"'='"	"2200.0"	"nM"	"5.66"	""	""	"UO_0000065"	"21.65"	"0.41"	"5.67"	"5.01"	"False"	"CHEMBL3625898"	"Inhibition of JAK2 (unknown origin) using 35 uM of ATP and Tyr6 peptide by Z'-LYTE kinase assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621116"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL3622832"	""	"0"	"322.41"	"0"	"2.88"	"5i"	"CC(C)c1ccc(-c2nc3cc(C(N)=O)ccc3n2CCN)cc1"	"IC50"	"'='"	"5900.0"	"nM"	"5.23"	""	""	"UO_0000065"	"16.22"	"0.30"	"2.35"	"6.02"	"False"	"CHEMBL3625898"	"Inhibition of JAK2 (unknown origin) using 35 uM of ATP and Tyr6 peptide by Z'-LYTE kinase assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621116"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL3622835"	""	"0"	"312.33"	"0"	"1.17"	"5l"	"NCCn1c(-c2ccc(O)cc2O)nc2cc(C(N)=O)ccc21"	"IC50"	"'='"	"2500.0"	"nM"	"5.60"	""	""	"UO_0000065"	"17.94"	"0.33"	"4.43"	"4.40"	"False"	"CHEMBL3625898"	"Inhibition of JAK2 (unknown origin) using 35 uM of ATP and Tyr6 peptide by Z'-LYTE kinase assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621116"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL3647733"	""	"0"	"542.56"	"1"	"3.69"	"BDBM147836"	"N#C[C@H]1CC(N2CCC[C@H]2CF)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"28.0"	"nM"	"7.55"	""	"285770"	"UO_0000065"	"13.92"	"0.28"	"3.86"	"5.63"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665158"	""	"0"	"415.52"	"0"	"2.28"	"BDBM112551"	"CC(C)CS(=O)(=O)N1CCC[C@H](Nc2ncccc2-c2cnc3[nH]ncc3n2)C1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"233789"	"UO_0000065"	"21.66"	"0.42"	"6.72"	"7.71"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3655092"	""	"0"	"337.45"	"0"	"1.64"	"BDBM159759"	"CCCS(=O)(=O)N[C@H]1CC[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"574.0"	"nM"	"6.24"	""	"302569"	"UO_0000065"	"18.49"	"0.37"	"4.60"	"6.86"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647783"	""	"0"	"430.94"	"0"	"2.97"	"BDBM147886"	"CC(C)(CO)N[C@H]1CCC(n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"41.0"	"nM"	"7.39"	""	"285820"	"UO_0000065"	"17.14"	"0.34"	"4.42"	"5.73"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3896712"	""	"0"	"332.41"	"0"	"2.99"	"BDBM198208"	"c1ccc(CN2CCCC(c3nnn4cnc5[nH]ccc5c34)C2)cc1"	"IC50"	"'='"	"570.0"	"nM"	"6.24"	""	"352290"	"UO_0000065"	"18.78"	"0.34"	"3.25"	"10.05"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3933612"	""	"0"	"376.42"	"0"	"3.12"	"BDBM198218"	"O=C(OCc1ccccc1)N1CCC(c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"210.0"	"nM"	"6.68"	""	"352300"	"UO_0000065"	"17.74"	"0.33"	"3.56"	"7.55"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3974254"	""	"0"	"287.37"	"0"	"1.80"	"BDBM228763"	"CCCC(=O)N(C)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399697"	"UO_0000065"	"32.22"	"0.60"	"7.46"	"14.22"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3949963"	""	"0"	"379.86"	"0"	"3.27"	"BDBM228778"	"CN(c1nc(Cl)nc2ccccc12)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399716"	"UO_0000065"	"24.38"	"0.47"	"5.99"	"12.54"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL1822792"	"MK-2461"	"2"	"495.56"	"0"	"2.15"	"81, MK-2461"	"CN(C[C@@H]1COCCO1)S(=O)(=O)Nc1ccc2ccc3ncc(-c4cnn(C)c4)cc3c(=O)c2c1"	"IC50"	"'='"	"230.0"	"nM"	"6.64"	""	""	"UO_0000065"	"13.40"	"0.26"	"4.49"	"5.74"	"False"	"CHEMBL1804347"	"Inhibition of human JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1800066"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL3896885"	""	"0"	"466.49"	"0"	"3.92"	"BDBM228903"	"COc1cc(N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)CC2)ccc1F"	"IC50"	"'='"	"74.0"	"nM"	"7.13"	""	"400650"	"UO_0000065"	"15.29"	"0.29"	"3.21"	"6.53"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3920686"	""	"0"	"504.60"	"1"	"3.61"	"BDBM228951"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3cccc(Cn4ccnc4)c3)n2)CC1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	"400698"	"UO_0000065"	"15.77"	"0.29"	"4.35"	"5.52"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3919288"	""	"0"	"482.56"	"0"	"4.14"	"BDBM228956"	"CC(C)(C)OC(=O)N1CCC(C(C#N)C2CC2)(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CC1"	"IC50"	"'='"	"738.0"	"nM"	"6.13"	""	"400703"	"UO_0000065"	"12.71"	"0.24"	"1.99"	"4.86"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3892636"	""	"0"	"459.53"	"0"	"2.06"	"BDBM228961"	"CS(=O)(=O)c1ccc(Nc2nn(C3(CC#N)CCC4(CC3)OCCO4)cc2C(N)=O)cc1"	"IC50"	"'='"	"206.0"	"nM"	"6.69"	""	"400708"	"UO_0000065"	"14.55"	"0.29"	"4.63"	"4.48"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3949440"	""	"0"	"460.49"	"0"	"3.64"	"BDBM229021"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3cc(F)cc(F)c3)n2)CC1"	"IC50"	"'='"	"42.0"	"nM"	"7.38"	""	"400765"	"UO_0000065"	"16.02"	"0.31"	"3.74"	"5.84"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3897680"	""	"0"	"426.48"	"0"	"2.16"	"BDBM229031"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3cccnn3)n2)CC1"	"IC50"	"'='"	"179.0"	"nM"	"6.75"	""	"400775"	"UO_0000065"	"15.82"	"0.30"	"4.59"	"4.44"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3645117"	""	"0"	"552.60"	"2"	"5.43"	"BDBM99891"	"COc1ccc(C(F)(F)F)cc1-c1cccn2nc(Nc3cccc(C4CCN(CC(=O)N(C)C)CC4)c3)nc12"	"IC50"	"'='"	"75.48"	"nM"	"7.12"	""	"216559"	"UO_0000065"	"12.89"	"0.24"	"1.69"	"9.50"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3941400"	""	"0"	"509.55"	"1"	"3.06"	"66"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(C#N)c(F)c3)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3958880"	""	"0"	"510.60"	"1"	"3.18"	"234"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(Cc3ccc4c(c3)OCCO4)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3968145"	""	"0"	"501.54"	"1"	"3.93"	"277"	"N#CCC1(n2ccc(-c3ncnc4[nH]ccc34)c2)CN(C2CCN(C(=O)c3ccc(F)c(F)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3920539"	""	"0"	"1093.73"	"1"	"3.40"	"378"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc(CN4CC[C@@H](F)C4)nc(C(F)(F)F)n3)CC2)C1.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3647775"	""	"0"	"460.50"	"0"	"4.32"	"BDBM147878"	"CC1(C)CN([C@H]2CC[C@H](n3cc(C(N)=O)c(Nc4ccc(C(F)(F)F)cc4)n3)[C@@H](C#N)C2)C1"	"IC50"	"'='"	"39.0"	"nM"	"7.41"	""	"285812"	"UO_0000065"	"16.09"	"0.31"	"3.09"	"7.41"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL2062809"	""	"0"	"461.59"	"0"	"4.35"	"BDBM99563"	"CN1CCC(c2cccc(Nc3nc4c(-c5ccc(S(C)(=O)=O)cc5)cccn4n3)c2)CC1"	"IC50"	"'='"	"0.7"	"nM"	"9.15"	""	"216253"	"UO_0000065"	"19.83"	"0.38"	"4.80"	"11.50"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3639640"	""	"0"	"384.87"	"0"	"3.40"	"BDBM112543"	"CC(=O)N1CCCC(Nc2nc(C)ccc2-c2cnc3[nH]cc(Cl)c3n2)C1"	"IC50"	"'='"	"0.1466"	"nM"	"9.83"	""	"233782"	"UO_0000065"	"25.55"	"0.50"	"6.43"	"11.33"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652297"	""	"0"	"483.64"	"0"	"3.27"	"BDBM113106"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCC(O)(c3ccccc3)CC2)CC1"	"IC50"	"'='"	"7.42"	"nM"	"8.13"	""	"234550"	"UO_0000065"	"16.81"	"0.33"	"4.86"	"7.94"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3702929"	""	"0"	"359.38"	"0"	"3.46"	"BDBM147631"	"C[C@]1(C#N)CC[C@@H](F)C[C@@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	"285562"	"UO_0000065"	"22.15"	"0.42"	"4.50"	"8.23"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647910"	""	"0"	"468.95"	"0"	"2.72"	"BDBM148022"	"N#C[C@H]1C[C@@H](C(=O)N2CC3(COC3)C2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'>'"	"500.0"	"nM"	""	""	"285957"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647723"	""	"0"	"440.94"	"0"	"3.09"	"BDBM147825"	"N#C[C@H]1C[C@@H](N2CCC23COC3)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"285759"	"UO_0000065"	"19.05"	"0.37"	"5.31"	"7.69"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642339"	""	"0"	"511.63"	"1"	"2.77"	"BDBM99613"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4ccc(CN5CCS(=O)(=O)CC5)cc4)nc23)cc1"	"IC50"	"'='"	"0.75"	"nM"	"9.12"	""	"216303"	"UO_0000065"	"17.84"	"0.36"	"6.35"	"8.02"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3658866"	""	"0"	"391.54"	"0"	"2.07"	"BDBM159785"	"CC(C)N1CCC(S(=O)(=O)C[C@H]2C[C@@H](N(C)c3ncnc4[nH]ccc34)C2)C1"	"IC50"	"'='"	"3760.0"	"nM"	"5.42"	""	"302595"	"UO_0000065"	"13.86"	"0.27"	"3.35"	"6.60"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665139"	""	"0"	"350.43"	"0"	"2.69"	"BDBM112526"	"CC(C)C(=O)N1CC[C@@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.1684"	"nM"	"9.77"	""	"233765"	"UO_0000065"	"27.89"	"0.51"	"7.08"	"11.26"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3907279"	""	"0"	"590.64"	"2"	"5.28"	"93"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc4c(C(F)(F)F)cccc4s3)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3984673"	""	"0"	"511.59"	"1"	"3.45"	"181"	"COc1cccc(NC(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)c1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3962003"	""	"0"	"488.55"	"0"	"3.69"	"215"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(Cc3cc(F)cc(F)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3970916"	""	"0"	"527.61"	"1"	"2.47"	"248"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(S(=O)(=O)c3cccc(C#N)c3)CC2)C1"	"IC50"	"'>'"	"100.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3895426"	""	"0"	"440.53"	"0"	"1.17"	"254"	"CS(=O)(=O)N1CCC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3707409"	"ITACITINIB ADIPATE"	"2"	"699.67"	"1"	"3.60"	"358"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccnc(C(F)(F)F)c3F)CC2)C1.O=C(O)CCCCC(=O)O"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL4083094"	""	"0"	"299.38"	"0"	"1.82"	"3"	"C=CC(=O)N1CC[C@@H](C)[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"2030.0"	"nM"	"5.69"	""	""	"UO_0000065"	"19.01"	"0.35"	"3.87"	"8.74"	"False"	"CHEMBL4005719"	"Inhibition of recombinant human GST-tagged cytoplasmic JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by microfluidic assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4004825"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL3647823"	""	"0"	"502.54"	"1"	"4.09"	"BDBM147928"	"N#C[C@H]1C[C@H](N(CC2CC2)C2COC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"1200.0"	"nM"	"5.92"	""	"285862"	"UO_0000065"	"11.78"	"0.22"	"1.83"	"5.42"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651060"	""	"0"	"393.45"	"0"	"2.86"	"BDBM47231"	"CCOC(=O)c1c[nH]c2ncnc(-c3cccc(NC(=O)/C=C/CN(C)C)c3)c12"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"198763"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652309"	""	"0"	"418.52"	"0"	"1.10"	"BDBM113118"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2C[C@@H](O)[C@H](C#N)C2)CC1"	"IC50"	"'='"	"18.7"	"nM"	"7.73"	""	"234562"	"UO_0000065"	"18.47"	"0.36"	"6.63"	"6.12"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3652399"	""	"0"	"435.59"	"0"	"2.23"	"BDBM113211"	"C[C@@H]1C[C@@H](CS(=O)(=O)N2CCC(CO)CC2)CC[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"32.5"	"nM"	"7.49"	""	"234654"	"UO_0000065"	"17.19"	"0.34"	"5.26"	"7.31"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3642362"	""	"0"	"491.62"	"0"	"3.24"	"BDBM99638"	"CN1CCN(c2cccc(Nc3nc4c(NCc5ccccc5S(C)(=O)=O)cccn4n3)c2)CC1"	"IC50"	"'='"	"26.32"	"nM"	"7.58"	""	"216328"	"UO_0000065"	"15.42"	"0.30"	"4.34"	"7.99"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647742"	""	"0"	"496.52"	"0"	"2.96"	"BDBM147845"	"N#C[C@H]1C[C@H](N2CCC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"285779"	"UO_0000065"	"16.72"	"0.33"	"5.34"	"6.19"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647871"	""	"0"	"400.41"	"0"	"2.45"	"BDBM147983"	"CNC(=O)O[C@@H]1CCC(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	"285917"	"UO_0000065"	"19.78"	"0.37"	"5.47"	"5.86"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647839"	""	"0"	"451.45"	"0"	"3.11"	"BDBM147948"	"C[C@](O)(c1ccc(Nc2nn([C@H]3CC[C@@](C)(O)C[C@@H]3C#N)cc2C(N)=O)cc1)C(F)(F)F"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"285882"	"UO_0000065"	"18.60"	"0.36"	"5.29"	"6.12"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3644984"	""	"0"	"541.58"	"1"	"3.91"	"BDBM99735"	"CS(=O)(=O)CCN1CCc2ccc(Nc3nc4c(-c5cccc6c5OC(F)(F)O6)cccn4n3)cc2CC1"	"IC50"	"'='"	"24.83"	"nM"	"7.61"	""	"216424"	"UO_0000065"	"14.04"	"0.27"	"3.70"	"7.76"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"Tofacitinib"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"71.0"	"nM"	"7.15"	""	""	"UO_0000065"	"22.88"	"0.42"	"5.61"	"8.04"	"False"	"CHEMBL3784147"	"Inhibition of JAK2 in human CD34+ cells assessed as inhibition of EPO-mediated cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"CD34+ cell"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3779778"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3893970"	""	"0"	"530.63"	"1"	"4.67"	"34"	"O=C(O)C1CCN(CCOc2ccc3cc2COC/C=C/COCc2cccc(c2)-c2ccnc(n2)N3)CC1"	"IC50"	"'<'"	"39.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3877345"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3877241"	"1"	"Scientific Literature"	"J Med Chem"	"2016"	"None"	""
"CHEMBL3920872"	""	"0"	"503.60"	"2"	"5.90"	"40"	"O=C(O)CCCCCCOc1ccc2cc1COC/C=C/COCc1cccc(c1)-c1ccnc(n1)N2"	"IC50"	"'='"	"2.57"	"nM"	"8.59"	""	""	"UO_0000065"	"17.06"	"0.32"	"2.69"	"8.36"	"False"	"CHEMBL3877344"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]ATP addition measured after 120 mins by Hotspot assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3877241"	"1"	"Scientific Literature"	"J Med Chem"	"2016"	"None"	""
"CHEMBL3945293"	""	"0"	"532.64"	"2"	"5.72"	"52"	"O=C(CCCCCCCOc1ccc2cc1COC/C=C/COCc1cccc(c1)-c1ccnc(n1)N2)NO"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	""	"UO_0000065"	"15.58"	"0.29"	"2.58"	"7.23"	"False"	"CHEMBL3877344"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]ATP addition measured after 120 mins by Hotspot assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3877241"	"1"	"Scientific Literature"	"J Med Chem"	"2016"	"None"	""
"CHEMBL3622127"	""	"0"	"398.47"	"0"	"1.08"	"3"	"CNc1nc2c(cc(C(=O)N(C3CC3)C3CC3)n2C[C@H](O)CO)c2c1ncn2C"	"IC50"	"'='"	"720.0"	"nM"	"6.14"	""	""	"UO_0000065"	"15.42"	"0.29"	"5.06"	"5.66"	"False"	"CHEMBL3625474"	"Inhibition of JAK2 in human SET2 cells assessed as inhibition of cell proliferation after 72 hrs by [3H]-thymidine incorporation assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621098"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3622138"	""	"0"	"383.42"	"1"	"0.31"	"1"	"CNc1nc2c(cc(-c3nnnn3C3CC3)n2C[C@H](O)CO)c2c1ncn2C"	"IC50"	"'='"	"7.8"	"nM"	"8.11"	""	""	"UO_0000065"	"21.15"	"0.40"	"7.80"	"6.15"	"False"	"CHEMBL3625473"	"Inhibition of JAK2 (unknown origin) using 5-FAMKKKKEEIYFFFG-OH as substrate after 60 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621098"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3982857"	""	"0"	"538.60"	"2"	"5.68"	"32"	"O=C(O)c1cccc(NCCOc2ccc3cc2COC/C=C/COCc2cccc(c2)-c2ccnc(n2)N3)c1"	"IC50"	"'<'"	"39.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3877345"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3877241"	"1"	"Scientific Literature"	"J Med Chem"	"2016"	"None"	""
"CHEMBL3671130"	""	"0"	"420.42"	"0"	"4.00"	"BDBM127629"	"O=C(Nc1ccccn1)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258303"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3671141"	""	"0"	"383.40"	"0"	"3.24"	"BDBM127640"	"O=C(NC1CC1)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258314"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675930"	""	"0"	"382.44"	"0"	"3.13"	"BDBM127680"	"CC(C)(C)NC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258354"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675938"	""	"0"	"467.42"	"0"	"2.31"	"BDBM127689"	"O=C(NC[C@H](O)CO)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3C(F)(F)F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258363"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3639749"	""	"0"	"431.44"	"0"	"1.82"	"BDBM127801"	"C[C@@H](O)[C@H](CO)NC(=O)c1cnn2ccc(N3CCCC3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258470"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676069"	""	"0"	"398.44"	"0"	"2.43"	"BDBM127829"	"CC(C)(C)NC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)c[nH]c3=O)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258498"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3926544"	""	"0"	"552.54"	"1"	"4.21"	"261"	"N#CCC1(n2ccc(-c3ncnc4[nH]ccc34)c2)CN(C2CCN(C(=O)c3ccnc(C(F)(F)F)c3F)CC2)C1"	"IC50"	"'>'"	"100.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3960627"	""	"0"	"533.01"	"1"	"4.84"	"289"	"N#CCC1(n2ccc(-c3ncnc4[nH]ccc34)c2)CN(C2CCN(C(=O)Nc3ccc(F)cc3Cl)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3985568"	""	"0"	"552.54"	"1"	"4.21"	"294"	"N#CCC1(n2cc(-c3ccnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccnc(C(F)(F)F)c3F)CC2)C1"	"IC50"	"'>'"	"100.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3931216"	""	"0"	"511.59"	"1"	"3.45"	"306"	"COc1ncccc1NC(=O)N1CCC(N2CC(CC#N)(n3cc(-c4ccnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3946326"	""	"0"	"553.52"	"1"	"3.60"	"352"	"N#CCC1(n2cc(-c3c(F)cnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cncc(C(F)(F)F)n3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL1235315"	""	"0"	"455.40"	"0"	"2.71"	"12"	"O=C1CCN(c2ncc(C(F)(F)F)c(C3=C(c4c[nH]c5ccccc45)C(=O)NC3=O)n2)CC1"	"IC50"	"'='"	"330.0"	"nM"	"6.48"	""	""	"UO_0000065"	"14.23"	"0.27"	"3.77"	"6.00"	"False"	"CHEMBL1657171"	"Inhibition of GST-tagged Jak2 expressed in insect cells using 20 uM ATP"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649080"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL3908945"	""	"0"	"535.44"	"1"	"4.36"	"24"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc(Cl)cc(Cl)c3)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3984246"	""	"0"	"563.44"	"1"	"3.95"	"29"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc(F)cc(Br)c3)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3917446"	""	"0"	"518.98"	"1"	"3.84"	"63"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(Cl)c(F)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3898382"	""	"0"	"506.61"	"1"	"3.47"	"99"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)C3CCc4ccccc43)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3952213"	""	"0"	"575.68"	"1"	"2.92"	"106"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)C3CCN(c4ccc(C#N)cn4)CC3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3937156"	""	"0"	"516.01"	"1"	"4.10"	"163"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3ccccc3Cl)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3962987"	""	"0"	"517.54"	"1"	"3.72"	"176"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3ccc(F)c(F)c3)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3904053"	""	"0"	"534.00"	"1"	"4.23"	"178"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3ccc(Cl)cc3F)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3932380"	""	"0"	"538.64"	"1"	"4.05"	"193"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3nc4ccccc4s3)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3912827"	""	"0"	"500.58"	"1"	"3.56"	"218"	"COc1cccc(F)c1CN1CCC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3924512"	""	"0"	"520.60"	"1"	"3.46"	"221"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(Cc3ccc(-c4conn4)cc3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL2208026"	""	"0"	"389.46"	"0"	"3.68"	"9a"	"CC(=O)Nc1ccc(-c2cc(Nc3ccc(N4CCOCC4)cc3)ncn2)cc1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2214785"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT1 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL2208027"	""	"0"	"407.45"	"0"	"3.82"	"9b"	"CC(=O)Nc1ccc(-c2nc(Nc3ccc(N4CCOCC4)cc3)ncc2F)cc1"	"IC50"	"'='"	"4.4"	"nM"	"8.36"	""	""	"UO_0000065"	"20.51"	"0.38"	"4.54"	"10.53"	"False"	"CHEMBL2214787"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL1077458"	""	"0"	"389.46"	"0"	"3.68"	"7c"	"CC(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"3.6"	"nM"	"8.44"	""	""	"UO_0000065"	"21.68"	"0.40"	"4.76"	"10.64"	"False"	"CHEMBL2214787"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL2208023"	""	"0"	"304.35"	"0"	"3.85"	"6c"	"CC(=O)Nc1ccc(-c2ccnc(Nc3ccccc3)n2)cc1"	"IC50"	"'='"	"12.8"	"nM"	"7.89"	""	""	"UO_0000065"	"25.93"	"0.47"	"4.04"	"11.80"	"False"	"CHEMBL2214787"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL2207763"	""	"0"	"470.36"	"0"	"4.59"	"4"	"CC(=O)Nc1ccc(-c2ccnc(NCC3CN(C(=O)c4c(Cl)cccc4Cl)C3)n2)cc1"	"IC50"	"'='"	"5000.0"	"nM"	"5.30"	""	""	"UO_0000065"	"11.27"	"0.23"	"0.71"	"6.08"	"False"	"CHEMBL2214787"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL3941414"	""	"0"	"472.58"	"0"	"3.11"	"69"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cccs3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3907878"	""	"0"	"537.05"	"1"	"3.77"	"74"	"COc1c(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)csc1Cl"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3977313"	""	"0"	"486.61"	"0"	"3.42"	"80"	"Cc1ccc(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)s1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3912772"	""	"0"	"458.57"	"0"	"2.93"	"101"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)C3CCCC3)CC2)C1"	"IC50"	"'>'"	"100.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3928285"	""	"0"	"480.58"	"0"	"2.98"	"109"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Cc3ccccc3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3916632"	""	"0"	"542.65"	"1"	"4.72"	"114"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(-c4ccccc4)cc3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3938229"	""	"0"	"601.65"	"1"	"5.00"	"137"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(-c4nc5ccccc5o4)c(F)c3)CC2)C1"	"IC50"	"'>'"	"100.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3983501"	""	"0"	"534.62"	"1"	"4.09"	"148"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CC3CCC(C2)N3C(=O)C2CCC(F)(F)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3967511"	""	"0"	"565.56"	"1"	"4.34"	"158"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3ccccc3OC(F)(F)F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3897634"	""	"0"	"549.56"	"1"	"4.46"	"167"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3ccc(C(F)(F)F)cc3)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3952589"	""	"0"	"499.55"	"0"	"3.58"	"169"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3ccccc3F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3915423"	""	"0"	"518.53"	"1"	"3.12"	"203"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3ncc(F)cc3F)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3946142"	""	"0"	"538.55"	"1"	"4.57"	"212"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(Cc3cccc(C(F)(F)F)c3F)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3973731"	""	"0"	"538.55"	"1"	"4.57"	"216"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(Cc3ccc(C(F)(F)F)cc3F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3897688"	""	"0"	"532.45"	"1"	"3.57"	"226"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(Cc3ccnc(Br)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3924081"	""	"0"	"539.54"	"1"	"3.96"	"231"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(Cc3ccnc(C(F)(F)F)c3F)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3977176"	""	"0"	"466.57"	"0"	"1.70"	"256"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(S(=O)(=O)C3CC3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3938051"	""	"0"	"506.60"	"1"	"1.33"	"258"	"Cn1cnc(S(=O)(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)c1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3884319"	""	"0"	"386.45"	"0"	"4.24"	"33"	"CC1(C)C(=O)N([C@H]2CCc3c(O)cccc32)c2nc(Nc3ccccc3)ncc21"	"IC50"	"'='"	"1173.0"	"nM"	"5.93"	""	""	"UO_0000065"	"15.35"	"0.28"	"1.69"	"7.57"	"False"	"CHEMBL3876058"	"Inhibition of human recombinant GST-tagged JAK2 cytoplasmic domain (809 to 1153 +9 residues) expressed in baculovirus expression system"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3875183"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL1835028"	""	"0"	"312.35"	"0"	"2.94"	"31"	"NC(=O)c1cnc(N2CCCCC2)c2c1[nH]c1ccc(F)cc12"	"IC50"	"'='"	"190.0"	"nM"	"6.72"	""	""	"UO_0000065"	"21.52"	"0.40"	"3.78"	"8.96"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835038"	""	"0"	"374.45"	"0"	"3.95"	"41"	"NC(=O)c1cnc(NC2CCCCC2)c2c1[nH]c1cc(-c3ccn[nH]3)ccc12"	"IC50"	"'='"	"23.0"	"nM"	"7.64"	""	""	"UO_0000065"	"20.40"	"0.37"	"3.69"	"6.79"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835043"	""	"0"	"402.50"	"0"	"4.31"	"47"	"C[C@H](Nc1ccc(C(N)=O)c2[nH]c3cc(-c4ccc(N)nn4)ccc3c12)C(C)(C)C"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	""	"UO_0000065"	"19.88"	"0.36"	"3.69"	"6.52"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835146"	""	"0"	"386.46"	"0"	"3.81"	"57"	"NC(=O)c1cnc(NC(C2CC2)C2CC2)c2c1[nH]c1cc(-c3cn[nH]c3)ccc12"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"22.05"	"0.40"	"4.71"	"7.58"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1972249"	""	"0"	"265.27"	"0"	"3.26"	"SID26661883"	"O=C1/C(=N\c2ccc(O)cc2)C=C(O)c2ccccc21"	"IC50"	"'='"	"7532.0"	"nM"	"5.12"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1427185"	""	"0"	"319.67"	"0"	"2.09"	"SID24817594"	"O=C1C=CC(=O)N1CCNc1ncc(C(F)(F)F)cc1Cl"	"IC50"	"'='"	"1760.0"	"nM"	"5.75"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL3545215"	"BMS-911543"	"2"	"432.53"	"0"	"3.50"	"11, BMS-911543"	"CCn1c(C(=O)N(C2CC2)C2CC2)cc2c3c(ncn3C)c(Nc3cc(C)n(C)n3)nc21"	"IC50"	"'='"	"1.1"	"nM"	"8.96"	""	""	"UO_0000065"	"20.71"	"0.38"	"5.46"	"10.44"	"False"	"CHEMBL3625512"	"Inhibition of recombinant JAK2 (unknown origin) using 5-FAM-KKKKEEIYFFFG-OH substrate and ATP incubated for 180 mins by scintillation counting method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621135"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3702909"	""	"0"	"492.61"	"0"	"4.40"	"BDBM147608"	"Cc1cccc(C)c1NS(=O)(=O)c1ccc(Nc2nn([C@H]3CCCC[C@@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"285538"	"UO_0000065"	"16.33"	"0.31"	"3.65"	"5.63"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL1650698"	""	"0"	"358.36"	"0"	"3.06"	"9d"	"C[C@H](Nc1ncc(F)c(Nc2cc(C3CC3)[nH]n2)n1)c1ncc(F)cn1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"23.78"	"0.45"	"5.46"	"8.17"	"False"	"CHEMBL1656588"	"Inhibition of JAK2 using Km ATP concentration"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1650725"	""	"0"	"328.36"	"0"	"2.66"	"9f"	"Cc1cc(Nc2nc(N[C@@H](C)c3ncc(F)cn3)ncc2C)n[nH]1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	""	"UO_0000065"	"25.58"	"0.48"	"5.74"	"8.05"	"False"	"CHEMBL1656589"	"Inhibition of JAK2 using 5 mM of ATP"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL2325896"	""	"0"	"364.41"	"0"	"1.33"	"3r"	"N#CC1CN(C(=O)[C@H](NC(=O)c2c[nH]c3ncc(C4CC4)nc23)C2CC2)C1"	"IC50"	"'<'"	"0.6"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2329570"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 30 mins by scintillation counting analysis in presence of [gamma-33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321829"	"1"	"Scientific Literature"	"J. Med. Chem."	"2013"	"None"	""
"CHEMBL2325903"	""	"0"	"286.38"	"0"	"3.00"	"3e"	"C[C@H](NC(=O)c1c[nH]c2ncc(C3CC3)nc12)C(C)(C)C"	"IC50"	"'='"	"10.8"	"nM"	"7.97"	""	""	"UO_0000065"	"27.82"	"0.52"	"4.97"	"11.27"	"False"	"CHEMBL2329570"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 30 mins by scintillation counting analysis in presence of [gamma-33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321829"	"1"	"Scientific Literature"	"J. Med. Chem."	"2013"	"None"	""
"CHEMBL2325902"	""	"0"	"258.32"	"0"	"2.36"	"3b"	"CC[C@H](C)NC(=O)c1c[nH]c2ncc(C3CC3)nc12"	"IC50"	"'='"	"44.3"	"nM"	"7.35"	""	""	"UO_0000065"	"28.47"	"0.53"	"4.99"	"10.41"	"False"	"CHEMBL2329570"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 30 mins by scintillation counting analysis in presence of [gamma-33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321829"	"1"	"Scientific Literature"	"J. Med. Chem."	"2013"	"None"	""
"CHEMBL1682384"	""	"0"	"434.48"	"0"	"2.53"	"24"	"Cc1cc(Nc2nc(N3CCN(C(=O)Cc4ccc(F)cc4)CC3)nn3cccc23)n[nH]1"	"IC50"	"'='"	"0.9"	"nM"	"9.05"	""	""	"UO_0000065"	"20.82"	"0.39"	"6.52"	"9.58"	"False"	"CHEMBL1685409"	"Inhibition of JAK2 after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1681645"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1615027"	""	"0"	"482.50"	"0"	"2.68"	"29"	"COc1cc(F)c(CC(=O)N2CCN(c3nc(Nc4cc(C)n[nH]4)c4cccn4n3)CC2)c(F)c1"	"IC50"	"'='"	"1.8"	"nM"	"8.74"	""	""	"UO_0000065"	"18.12"	"0.34"	"6.06"	"8.43"	"False"	"CHEMBL1685409"	"Inhibition of JAK2 after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1681645"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1682379"	""	"0"	"481.36"	"0"	"3.23"	"19"	"Cc1cc(Nc2nc(N3CCN(C(=O)c4ccccc4Br)CC3)nn3cccc23)n[nH]1"	"IC50"	"'='"	"2.1"	"nM"	"8.68"	""	""	"UO_0000065"	"18.03"	"0.38"	"5.45"	"9.19"	"False"	"CHEMBL1685409"	"Inhibition of JAK2 after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1681645"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1682371"	""	"0"	"402.46"	"0"	"2.47"	"11"	"Cc1cc(Nc2nc(N3CCN(C(=O)c4ccccc4)CC3)nn3cccc23)n[nH]1"	"IC50"	"'='"	"2.2"	"nM"	"8.66"	""	""	"UO_0000065"	"21.51"	"0.39"	"6.19"	"9.17"	"False"	"CHEMBL1685409"	"Inhibition of JAK2 after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1681645"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1682383"	""	"0"	"434.48"	"0"	"2.53"	"23"	"Cc1cc(Nc2nc(N3CCN(C(=O)Cc4ccccc4F)CC3)nn3cccc23)n[nH]1"	"IC50"	"'='"	"4.6"	"nM"	"8.34"	""	""	"UO_0000065"	"19.19"	"0.36"	"5.81"	"8.83"	"False"	"CHEMBL1685409"	"Inhibition of JAK2 after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1681645"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1682364"	""	"0"	"444.54"	"0"	"3.14"	"4"	"CC(C)n1cnc(Nc2nc(N3CCN(C(=O)Cc4ccccc4)CC3)nn3cccc23)c1"	"IC50"	"'='"	"110.0"	"nM"	"6.96"	""	""	"UO_0000065"	"15.65"	"0.29"	"3.82"	"8.32"	"False"	"CHEMBL1685409"	"Inhibition of JAK2 after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1681645"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL3639444"	""	"0"	"275.31"	"0"	"3.42"	"BDBM107137"	"C=CC(=O)Nc1cccc(-c2cnc3ccccc3n2)c1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	"226375"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3702908"	""	"0"	"485.61"	"0"	"2.35"	"BDBM147607"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)NCCN3CCCC3)cc2)n1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"285537"	"UO_0000065"	"17.91"	"0.35"	"6.35"	"5.95"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645076"	""	"0"	"502.59"	"1"	"4.56"	"BDBM99844"	"COc1ccc(-c2cccn3nc(Nc4ccc(C5CCN(CC(=O)N(C)C)CC5)cc4)nc23)c(F)c1"	"IC50"	"'='"	"4.41"	"nM"	"8.36"	""	"216517"	"UO_0000065"	"16.63"	"0.31"	"3.80"	"11.14"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703095"	""	"0"	"371.42"	"0"	"2.05"	"BDBM147809"	"CN(C)[C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"110.0"	"nM"	"6.96"	""	"285743"	"UO_0000065"	"18.74"	"0.35"	"4.91"	"6.17"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642368"	""	"0"	"517.66"	"1"	"4.12"	"BDBM99644"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4ccc5c(c4)CCC(N4CCOCC4)CC5)nc23)cc1"	"IC50"	"'='"	"1.55"	"nM"	"8.81"	""	"216334"	"UO_0000065"	"17.02"	"0.33"	"4.69"	"9.92"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL1933343"	""	"0"	"386.50"	"0"	"4.97"	"28c"	"Cc1cnc2nc1-c1cccc(c1)OCC/C=C/CN(C)Cc1cccc(c1)N2"	"IC50"	"'='"	"180.0"	"nM"	"6.75"	""	""	"UO_0000065"	"17.45"	"0.32"	"1.77"	"13.41"	"True"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1946443"	""	"0"	"402.50"	"0"	"4.67"	"28e"	"COc1ccc2cc1OCC/C=C/CN(C)Cc1cccc(c1)Nc1nccc-2n1"	"IC50"	"'='"	"510.0"	"nM"	"6.29"	""	""	"UO_0000065"	"15.63"	"0.29"	"1.62"	"10.57"	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL3671147"	""	"0"	"413.43"	"0"	"2.56"	"BDBM127646"	"O=C(c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12)N1CC[C@@H](O)C1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258320"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3671153"	""	"0"	"437.45"	"0"	"3.04"	"BDBM127652"	"O=C(NCCc1cnc[nH]1)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258326"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3671155"	""	"0"	"371.39"	"0"	"3.05"	"BDBM127654"	"CN(C)C(=O)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258328"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675912"	""	"0"	"453.52"	"0"	"2.74"	"BDBM127661"	"O=C(NC1CCC(O)CC1)c1cnn2ccc(N3CCCC3c3cc(F)ccc3CO)nc12"	"IC50"	"'='"	"42.3"	"nM"	"7.37"	""	"258335"	"UO_0000065"	"16.26"	"0.31"	"4.63"	"7.16"	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675970"	""	"0"	"421.41"	"0"	"3.39"	"BDBM127722"	"O=C(Nc1ccc(F)cn1)c1cnn2ccc(N3CCC[C@@H]3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258396"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675975"	""	"0"	"380.43"	"0"	"2.89"	"BDBM127728"	"O=C(NC1CCC1)c1cnn2ccc(N3CCC[C@@H]3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258402"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676082"	""	"0"	"383.43"	"0"	"2.32"	"BDBM127844"	"CC(C)NC(=O)c1cnn2ccc(N3C[C@@H](O)C[C@@H]3c3cccc(F)c3)nc12"	"IC50"	"'='"	"551.0"	"nM"	"6.26"	""	"258512"	"UO_0000065"	"16.32"	"0.31"	"3.94"	"7.56"	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676085"	""	"0"	"466.44"	"0"	"3.04"	"BDBM127847"	"CC(NC(=O)c1cnn2ccc(N3C(c4cncc(F)c4)CCC3(C)CO)nc12)C(F)(F)F"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258515"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676094"	""	"0"	"410.45"	"0"	"2.05"	"BDBM127859"	"Cn1cc(F)cc([C@H]2CCCN2c2ccn3ncc(C(=O)NCC4CC4)c3n2)c1=O"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258524"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676096"	""	"0"	"454.51"	"0"	"1.94"	"BDBM127861"	"Cn1cc(F)cc([C@H]2CCCN2c2ccn3ncc(C(=O)N[C@@H]4CCCC[C@H]4O)c3n2)c1=O"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258526"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675915"	""	"0"	"365.41"	"0"	"3.10"	"BDBM127664"	"O=C(NC1CC1)c1cnn2ccc(N3CCC[C@@H]3c3cccc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258338"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675944"	""	"0"	"393.43"	"0"	"2.64"	"BDBM127696"	"CC(C)(C#N)NC(=O)c1cnn2ccc(N3CCCC3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258370"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675945"	""	"0"	"487.56"	"0"	"1.76"	"BDBM127697"	"CS(=O)(=O)N1CCC(NC(=O)c2cnn3ccc(N4CCCC4c4cncc(F)c4)nc23)CC1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258371"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675967"	""	"0"	"396.43"	"0"	"1.81"	"BDBM127719"	"CC1(O)CN(C(=O)c2cnn3ccc(N4CCC[C@@H]4c4cncc(F)c4)nc23)C1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258393"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676002"	""	"0"	"396.43"	"0"	"1.81"	"BDBM127755"	"O=C(c1cnn2ccc(N3CCC[C@@H]3c3cncc(F)c3)nc12)N1CC[C@H](O)C1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258429"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3904952"	""	"0"	"454.51"	"0"	"2.65"	"BDBM127767"	"COc1ncc(F)cc1[C@H]1CCCN1c1ccn2ncc(C(=O)NC3CCC(O)CC3)c2n1"	"IC50"	"'='"	"76.7"	"nM"	"7.12"	""	"258441"	"UO_0000065"	"15.65"	"0.29"	"4.47"	"6.78"	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676033"	""	"0"	"517.59"	"1"	"1.77"	"BDBM127789"	"COc1ncc(F)cc1[C@H]1CCCN1c1ccn2ncc(C(=O)NC3CCN(S(C)(=O)=O)CC3)c2n1"	"IC50"	"'='"	"444.0"	"nM"	"6.35"	""	"258460"	"UO_0000065"	"12.27"	"0.24"	"4.58"	"5.21"	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676076"	""	"0"	"455.49"	"0"	"1.83"	"BDBM127837"	"O=C(NC1CC1)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3OCC(O)CO)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258505"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676078"	""	"0"	"452.41"	"0"	"2.65"	"BDBM127839"	"CC(NC(=O)c1cnn2ccc(N3C(CO)CCC3c3cncc(F)c3)nc12)C(F)(F)F"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258507"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL2207761"	""	"0"	"458.35"	"0"	"4.64"	"1"	"CC(=O)Nc1ccc(-c2ccnc(NCCCNC(=O)c3c(Cl)cccc3Cl)n2)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL2214784"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT3 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL3947866"	""	"0"	"551.55"	"1"	"4.81"	"272"	"N#CCC1(n2ccc(-c3ncnc4[nH]ccc34)c2)CN(C2CCN(C(=O)c3ccc(C(F)(F)F)cc3F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3921384"	""	"0"	"516.56"	"1"	"4.33"	"286"	"N#CCC1(n2ccc(-c3ncnc4[nH]ccc34)c2)CN(C2CCN(C(=O)Nc3ccc(F)cc3F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3951506"	""	"0"	"526.55"	"1"	"3.81"	"325"	"N#CCC1(n2cc(-c3c(F)cnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(C#N)c(F)c3)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3897382"	""	"0"	"540.59"	"1"	"3.27"	"337"	"N#CCC1(n2cc(-c3c(C#N)cnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc(C#N)ccc3C#N)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3944041"	""	"0"	"553.52"	"1"	"3.60"	"343"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc(C(F)(F)F)ncc3F)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3924975"	""	"0"	"439.55"	"0"	"1.77"	"348"	"CS(=O)(=O)N1CCC(N2CC(CC#N)(n3ccc(-c4ncnc5[nH]ccc45)c3)C2)CC1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3964438"	""	"0"	"474.57"	"0"	"3.15"	"392"	"CC1(COC(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)CC1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3983534"	""	"0"	"535.53"	"1"	"3.46"	"299"	"N#CCC1(n2cc(-c3ccnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccnc(C(F)(F)F)n3)CC2)C1"	"IC50"	"'>'"	"100.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3966546"	""	"0"	"570.53"	"1"	"4.35"	"314"	"N#CCC1(n2cc(-c3c(F)cnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccnc(C(F)(F)F)c3F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3973843"	""	"0"	"533.57"	"1"	"3.54"	"315"	"N#CCC1(n2cc(-c3c(F)cnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc(C#N)cc(C#N)c3)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3941898"	""	"0"	"532.56"	"1"	"3.83"	"394"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)OCc3ccc(F)c(F)c3)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL2207762"	""	"0"	"498.41"	"1"	"5.56"	"3"	"CC(=O)Nc1ccc(-c2ccnc(NC3CCCC(NC(=O)c4c(Cl)cccc4Cl)C3)n2)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL2214784"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT3 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL2208024"	""	"0"	"387.49"	"0"	"4.84"	"7a"	"CC(=O)Nc1ccc(-c2ccnc(Nc3cccc(N4CCCCC4)c3)n2)cc1"	"IC50"	"'='"	"956.1"	"nM"	"6.02"	""	""	"UO_0000065"	"15.53"	"0.28"	"1.18"	"8.58"	"False"	"CHEMBL2214785"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT1 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL2207759"	""	"0"	"458.57"	"0"	"3.76"	"10g"	"CN1CCC[C@@H]1C(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"5.2"	"nM"	"8.28"	""	""	"UO_0000065"	"18.06"	"0.33"	"4.52"	"10.03"	"False"	"CHEMBL2214787"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL3968688"	""	"0"	"458.57"	"0"	"4.03"	"BDBM229076"	"CCOc1ccccc1CN1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)CC1"	"IC50"	"'='"	"842.0"	"nM"	"6.08"	""	"400812"	"UO_0000065"	"13.25"	"0.24"	"2.04"	"5.56"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3911100"	""	"0"	"482.51"	"0"	"4.65"	"BDBM229079"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(Cc2ccc(C(F)(F)F)cc2)CC1"	"IC50"	"'='"	"460.0"	"nM"	"6.34"	""	"400815"	"UO_0000065"	"13.13"	"0.25"	"1.69"	"6.34"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL473773"	""	"0"	"376.21"	"0"	"3.86"	"WHI-P154"	"COc1cc2ncnc(Nc3ccc(O)c(Br)c3)c2cc1OC"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1016953"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1152817"	"1"	"Scientific Literature"	"Science"	"2003"	"None"	""
"CHEMBL3746249"	""	"0"	"385.90"	"0"	"4.04"	"3"	"COc1ccccc1-c1nc2c(NCC3CCN(C)CC3)c(Cl)cnc2[nH]1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3751000"	"Inhibition of N-terminal GST-fused recombinant JAK2 (831 to 1132 residues) (unknown origin) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate by microfluidic capillary electrophoresis method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3745697"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3746766"	""	"0"	"385.90"	"0"	"4.01"	"27"	"COc1ccc(-c2nc3c(NCC4CCNCC4)c(Cl)cnc3[nH]2)c(C)c1"	"IC50"	"'='"	"2890.0"	"nM"	"5.54"	""	""	"UO_0000065"	"14.35"	"0.28"	"1.53"	"7.40"	"False"	"CHEMBL3751000"	"Inhibition of N-terminal GST-fused recombinant JAK2 (831 to 1132 residues) (unknown origin) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate by microfluidic capillary electrophoresis method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3745697"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3703065"	""	"0"	"370.43"	"0"	"2.66"	"BDBM147775"	"CN(C)[C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"620.0"	"nM"	"6.21"	""	"285744"	"UO_0000065"	"16.76"	"0.31"	"3.55"	"6.21"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645051"	""	"0"	"467.50"	"1"	"5.63"	"BDBM99818"	"COc1ccc(C(F)(F)F)cc1-c1cccn2nc(Nc3ccc(C4CCNCC4)cc3)nc12"	"IC50"	"'='"	"79.87"	"nM"	"7.10"	""	"216491"	"UO_0000065"	"15.18"	"0.29"	"1.47"	"11.18"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"CP-690550"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	""	"UO_0000065"	"24.65"	"0.46"	"6.16"	"8.66"	"True"	"CHEMBL1016953"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1152817"	"1"	"Scientific Literature"	"Science"	"2003"	"None"	""
"CHEMBL56543"	""	"0"	"294.31"	"0"	"2.32"	"AG-490"	"N#C/C(=C\c1ccc(O)c(O)c1)C(=O)NCc1ccccc1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1016953"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1152817"	"1"	"Scientific Literature"	"Science"	"2003"	"None"	""
"CHEMBL3703024"	""	"0"	"504.56"	"1"	"4.07"	"BDBM147734"	"CC1(C)CN([C@@H]2CC[C@H](n3cc(C(N)=O)c(Nc4ccc([C@](C)(O)C(F)(F)F)cc4)n3)[C@@H](C#N)C2)C1"	"IC50"	"'='"	"24.0"	"nM"	"7.62"	""	"285668"	"UO_0000065"	"15.10"	"0.29"	"3.55"	"6.34"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3655088"	""	"0"	"388.50"	"0"	"1.93"	"BDBM159755"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)[C@H]2C[C@](C)(CC#N)C2)C1"	"IC50"	"'='"	"750.0"	"nM"	"6.12"	""	"302565"	"UO_0000065"	"15.77"	"0.31"	"4.19"	"5.34"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3747205"	""	"0"	"385.90"	"0"	"4.04"	"1"	"COc1ccc(-c2nc3c(NCC4CCN(C)CC4)c(Cl)cnc3[nH]2)cc1"	"IC50"	"'='"	"9620.0"	"nM"	"5.02"	""	""	"UO_0000065"	"13.00"	"0.25"	"0.98"	"7.59"	"False"	"CHEMBL3751000"	"Inhibition of N-terminal GST-fused recombinant JAK2 (831 to 1132 residues) (unknown origin) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate by microfluidic capillary electrophoresis method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3745697"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3645536"	""	"0"	"332.41"	"0"	"3.33"	"BDBM107119"	"O=C(CN1CCCC1)Nc1cccc(-c2cnc3ccccc3n2)c1"	"IC50"	"'>'"	"20000.0"	"nM"	""	""	"226356"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703072"	""	"0"	"430.46"	"0"	"3.27"	"BDBM147784"	"N#C[C@H]1C[C@@H](N2CCC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(OC(F)F)cc2)n1"	"IC50"	"'='"	"147.0"	"nM"	"6.83"	""	"285718"	"UO_0000065"	"15.87"	"0.30"	"3.56"	"6.26"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665130"	""	"0"	"366.43"	"0"	"3.05"	"BDBM112517"	"COC(=O)N1CCCCC(Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.0106"	"nM"	"10.97"	""	"233756"	"UO_0000065"	"29.95"	"0.56"	"7.92"	"11.43"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647913"	""	"0"	"420.47"	"0"	"1.65"	"BDBM148025"	"CS(=O)(=O)N[C@H]1CCC(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	"285961"	"UO_0000065"	"18.68"	"0.37"	"6.20"	"5.50"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3622150"	""	"0"	"418.51"	"0"	"3.49"	"14"	"CCn1c(C(=O)N(C2CC2)C2CC2)cc2c3c(ncn3C)c(Nc3cc(C)[nH]n3)nc21"	"IC50"	"'='"	"1.2"	"nM"	"8.92"	""	""	"UO_0000065"	"21.32"	"0.39"	"5.43"	"9.23"	"False"	"CHEMBL3625512"	"Inhibition of recombinant JAK2 (unknown origin) using 5-FAM-KKKKEEIYFFFG-OH substrate and ATP incubated for 180 mins by scintillation counting method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621135"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3622146"	""	"0"	"596.74"	"2"	"3.09"	"8"	"CCn1c(C(=O)N(C2CC2)C2CC2)cc2c3c(ncn3C)c(Nc3nc(C)c(C(=O)N4CCS(=O)(=O)CC4)s3)nc21"	"IC50"	"'='"	"0.7"	"nM"	"9.15"	""	""	"UO_0000065"	"15.34"	"0.30"	"6.06"	"6.77"	"False"	"CHEMBL3625512"	"Inhibition of recombinant JAK2 (unknown origin) using 5-FAM-KKKKEEIYFFFG-OH substrate and ATP incubated for 180 mins by scintillation counting method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621135"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3622142"	""	"0"	"463.61"	"0"	"4.78"	"4"	"CCc1nc(Nc2nc3c(cc(C(=O)N(C4CC4)C4CC4)n3CC)c3c2ncn3C)sc1C"	"IC50"	"'='"	"1.4"	"nM"	"8.85"	""	""	"UO_0000065"	"19.10"	"0.37"	"4.07"	"10.95"	"False"	"CHEMBL3625512"	"Inhibition of recombinant JAK2 (unknown origin) using 5-FAM-KKKKEEIYFFFG-OH substrate and ATP incubated for 180 mins by scintillation counting method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621135"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3941571"	""	"0"	"483.59"	"0"	"3.27"	"16e"	"CS(=O)(=O)N1CCc2oc(-c3ccnc(Nc4ccc(OCCN5CCCC5)cc4)n3)cc2C1"	"IC50"	"'='"	"164.0"	"nM"	"6.79"	""	""	"UO_0000065"	"14.03"	"0.27"	"3.52"	"6.73"	"False"	"CHEMBL3868063"	"Inhibition of GST-tagged recombinant human JAK2 expressed in baculovirus using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3867460"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2017"	"None"	""
"CHEMBL3966342"	""	"0"	"411.47"	"0"	"4.65"	"5f"	"Cc1cnc(Nc2ccc(N3CCOCC3)cc2)nc1-c1cc2cc(C#N)ccc2o1"	"IC50"	"'='"	"1052.0"	"nM"	"5.98"	""	""	"UO_0000065"	"14.53"	"0.26"	"1.33"	"6.85"	"False"	"CHEMBL3868066"	"Inhibition of JAK2 in human TF1 cells assessed as suppression of cell growth"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3867460"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2017"	"CHEMBL3307972"	""
"CHEMBL3902351"	""	"0"	"381.44"	"0"	"0.79"	"BDBM228755"	"CN(c1ccc(C(=O)NCCO)cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399685"	"UO_0000065"	"26.90"	"0.50"	"9.47"	"9.30"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3906692"	""	"0"	"431.48"	"0"	"3.46"	"BDBM228756"	"CN(c1ccc(C(=O)Nc2ccccc2F)cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399686"	"UO_0000065"	"23.78"	"0.44"	"6.80"	"11.39"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL388978"	"STAUROSPORINE"	"0"	"466.54"	"0"	"4.35"	"Staurosporine"	"CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4c(c5c6ccccc6n2c5c31)C(=O)NC4"	"IC50"	"'='"	"0.4"	"nM"	"9.40"	""	""	"UO_0000065"	"20.14"	"0.37"	"5.05"	"13.53"	"False"	"CHEMBL3820655"	"Inhibition of JAK2 (unknown origin) incubated for 1 hr by spectrophotometric analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3817824"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2016"	"None"	""
"CHEMBL3764383"	""	"0"	"382.47"	"0"	"2.42"	"15"	"CC(C)[C@@H](C)n1cc(-c2ccc(N3CCOCC3)cn2)c2[nH]nc(N)c2c1=O"	"IC50"	"'='"	"140.0"	"nM"	"6.85"	""	""	"UO_0000065"	"17.92"	"0.33"	"4.43"	"6.72"	"False"	"CHEMBL3766653"	"Inhibition of JAK2 (unknown origin) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent substrate phosphorylation after 45 mins by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3763089"	"1"	"Scientific Literature"	"J. Med. Chem."	"2016"	"None"	""
"CHEMBL3652347"	""	"0"	"455.61"	"0"	"1.40"	"BDBM113158"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC[C@H](S(C)(=O)=O)C2)CC1"	"IC50"	"'='"	"27.2"	"nM"	"7.57"	""	"234601"	"UO_0000065"	"16.61"	"0.34"	"6.17"	"6.50"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3651001"	""	"0"	"376.42"	"0"	"3.27"	"BDBM153177"	"C=C(C)C(=O)N1CCc2ccc(-c3ncnc4[nH]cc(C(=O)OCC)c34)cc21"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294125"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3649620"	""	"0"	"550.06"	"1"	"4.07"	"BDBM130314"	"NC(=O)c1cc(-c2ccc(OCCN3CCCOCC3)c(Cl)c2)nc2c1[nH]c1cc(N3CCOCC3)ccc12"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"262100"	"UO_0000065"	"14.95"	"0.29"	"4.15"	"7.76"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649629"	""	"0"	"401.43"	"0"	"2.35"	"BDBM130323"	"NC(=O)c1cc(-c2ncccn2)cc2c1[nH]c1cc(C(=O)N3CCOCC3)ccc12"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"262109"	"UO_0000065"	"22.42"	"0.41"	"6.65"	"7.88"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649636"	""	"0"	"472.43"	"0"	"2.71"	"BDBM130330"	"Cn1nc(C(F)(F)F)cc1-c1cc(C(N)=O)c2[nH]c3cc(C(=O)N4CCOCC4)ccc3c2n1"	"IC50"	"'='"	"314.0"	"nM"	"6.50"	""	"262116"	"UO_0000065"	"13.77"	"0.26"	"3.79"	"5.46"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649649"	""	"0"	"475.52"	"0"	"4.22"	"BDBM130344"	"COc1ccc(-c2cc(C(N)=O)c3[nH]c4cc(C(=O)N5CCCC(C)(O)C5)ccc4c3c2)cc1F"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"262130"	"UO_0000065"	"18.93"	"0.35"	"4.78"	"8.28"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3642385"	""	"0"	"491.62"	"0"	"3.51"	"BDBM99663"	"CN1CCN(c2ccc(Nc3nc4c(Nc5ccccc5CS(C)(=O)=O)cccn4n3)cc2)CC1"	"IC50"	"'='"	"22.1"	"nM"	"7.66"	""	"216353"	"UO_0000065"	"15.57"	"0.30"	"4.15"	"8.07"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL1650735"	""	"0"	"415.43"	"0"	"1.89"	"16d"	"COc1cc(Nc2cc(N3CCOCC3)nc(N[C@@H](C)c3ncc(F)cn3)n2)n[nH]1"	"IC50"	"'='"	"30.0"	"nM"	"7.52"	""	""	"UO_0000065"	"18.11"	"0.34"	"5.63"	"5.97"	"False"	"CHEMBL1656589"	"Inhibition of JAK2 using 5 mM of ATP"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL3703491"	""	"0"	"316.75"	"0"	"3.04"	"BDBM153135"	"CCOC(=O)c1c[nH]c2ncnc(-c3ccc(Cl)c(N)c3)c12"	"IC50"	"'='"	"125.0"	"nM"	"6.90"	""	"294083"	"UO_0000065"	"21.79"	"0.43"	"3.86"	"7.35"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703077"	""	"0"	"398.90"	"0"	"3.32"	"BDBM147790"	"N#C[C@H]1C[C@H](N2CCC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"110.0"	"nM"	"6.96"	""	"285724"	"UO_0000065"	"17.44"	"0.34"	"3.64"	"6.96"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665135"	""	"0"	"386.48"	"0"	"2.24"	"BDBM112522"	"CC(C)S(=O)(=O)N1CC[C@@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.5728"	"nM"	"9.24"	""	"233761"	"UO_0000065"	"23.91"	"0.47"	"7.00"	"8.90"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3651051"	""	"0"	"344.38"	"0"	"3.53"	"BDBM153228"	"C=C(C)C(=O)Nc1cccc(-c2ncnc3[nH]cc(-c4cnc[nH]4)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294176"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3352835"	""	"0"	"473.36"	"0"	"4.79"	"3"	"COC1CCN(c2nccc(Nc3cc(NC(=O)c4c(Cl)cccc4Cl)ccn3)n2)CC1"	"IC50"	"'='"	"44.0"	"nM"	"7.36"	""	""	"UO_0000065"	"15.54"	"0.31"	"2.57"	"7.97"	"False"	"CHEMBL3375809"	"Inhibition of Jak2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351701"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL1341981"	""	"0"	"423.54"	"0"	"3.96"	"SID862668"	"Cc1ccccc1CS(=O)(=O)c1nnc([C@H](CC(C)C)NC(=O)OC(C)(C)C)o1"	"IC50"	"'='"	"1676.0"	"nM"	"5.78"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1502358"	""	"0"	"288.31"	"0"	"3.02"	"SID26665838"	"O=C(C=C=Nc1ccccc1)C(=O)N=C=Cc1ccccc1"	"IC50"	"'='"	"10680.0"	"nM"	"4.97"	""	"Not Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1375393"	""	"0"	"346.34"	"0"	"2.19"	"SID24782033"	"O=C(CSc1nnnn1-c1ccc(F)cc1)c1ccc(O)c(O)c1"	"IC50"	"'='"	"11060.0"	"nM"	"4.96"	""	"Not Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1365696"	""	"0"	"423.54"	"0"	"3.96"	"SID864233"	"CCC(C)[C@@H](NC(=O)OC(C)(C)C)c1nnc(S(=O)(=O)Cc2cccc(C)c2)o1"	"IC50"	"'='"	"4670.0"	"nM"	"5.33"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL3589167"	""	"0"	"468.34"	"0"	"4.87"	"BDBM130283"	"NC(=O)c1cc(-c2ccc(Cl)cc2Cl)cc2c1[nH]c1ccc(C(=O)N3CCOCC3)cc12"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"262069"	"UO_0000065"	"17.41"	"0.35"	"3.28"	"9.22"	"True"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3946034"	""	"0"	"472.53"	"0"	"3.47"	"BDBM229488"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(NCc2cccc(C#N)c2)CC1"	"IC50"	"'='"	"1419.0"	"nM"	"5.85"	""	"401251"	"UO_0000065"	"12.38"	"0.23"	"2.38"	"4.02"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3970367"	""	"0"	"465.51"	"0"	"3.74"	"BDBM228310"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(NCc2cccc(F)c2)CC1"	"IC50"	"'='"	"1029.0"	"nM"	"5.99"	""	"401261"	"UO_0000065"	"12.86"	"0.24"	"2.25"	"4.92"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3622828"	""	"0"	"280.33"	"0"	"1.76"	"5e"	"NCCn1c(-c2ccccc2)nc2cc(C(N)=O)ccc21"	"IC50"	"'='"	"2800.0"	"nM"	"5.55"	""	""	"UO_0000065"	"19.81"	"0.36"	"3.79"	"6.39"	"False"	"CHEMBL3625898"	"Inhibition of JAK2 (unknown origin) using 35 uM of ATP and Tyr6 peptide by Z'-LYTE kinase assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621116"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL4641076"	""	"0"	"217.27"	"0"	"1.90"	"9"	"Cc1[nH]nc2[nH]c(=O)cc(CC3CCC3)c12"	"IC50"	"'>'"	"40000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL4648246"	""	"0"	"257.34"	"0"	"3.18"	"16"	"O=c1cc(C2CCCCC2)c2c(C3CC3)[nH]nc2[nH]1"	"IC50"	"'>'"	"40000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL4643061"	""	"0"	"282.35"	"0"	"2.60"	"40"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3C[C@H]4C[C@@H]3C[C@@H]4CC#N)c12"	"IC50"	"'='"	"2800.0"	"nM"	"5.55"	""	""	"UO_0000065"	"19.67"	"0.36"	"2.95"	"6.51"	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL3955948"	""	"0"	"284.32"	"0"	"0.91"	"BDBM228661"	"CN(C(=O)CC#N)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399625"	"UO_0000065"	"36.08"	"0.67"	"9.35"	"11.54"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3976708"	""	"0"	"352.40"	"0"	"1.85"	"BDBM228746"	"COC(=O)c1ccc(N(C)[C@@H]2CCN(c3ncnc4[nH]ccc34)C2)nc1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399676"	"UO_0000065"	"29.11"	"0.54"	"8.41"	"11.76"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3902542"	""	"0"	"377.45"	"0"	"1.96"	"BDBM228747"	"CN(c1ccc(C(=O)NC2CC2)cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399677"	"UO_0000065"	"27.18"	"0.50"	"8.30"	"11.39"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3951623"	""	"0"	"458.54"	"0"	"4.30"	"BDBM228751"	"C[C@@H](NC(=O)c1ccc(N(C)[C@@H]2CCN(c3ncnc4[nH]ccc34)C2)c(F)c1)c1ccccc1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399681"	"UO_0000065"	"22.37"	"0.41"	"5.96"	"13.30"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3911346"	""	"0"	"464.93"	"0"	"4.72"	"BDBM228753"	"CN(c1ccc(C(=O)Nc2cccc(Cl)c2)cc1F)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399683"	"UO_0000065"	"22.07"	"0.42"	"5.54"	"13.30"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3593584"	""	"0"	"320.82"	"0"	"3.35"	"6j"	"CC[C@@H]1CCCC[C@@H]1n1c(=O)[nH]c2cnc3[nH]ccc3c21.Cl"	"IC50"	"'='"	"3.6"	"nM"	"8.44"	""	""	"UO_0000065"	"29.69"	"0.55"	"5.09"	"12.70"	"False"	"CHEMBL3594576"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate and ATP incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593193"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3606021"	""	"0"	"395.43"	"0"	"2.92"	"20by, NMS-P118"	"NC(=O)c1cc(F)cc2c1C(=O)N(C1CCN(C3CCC(F)(F)CC3)CC1)C2"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3607969"	"Inhibition of human JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3603755"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL3593775"	""	"0"	"362.40"	"0"	"1.40"	"11e"	"N#Cc1cnc(N2CCC(Nc3c(C(N)=O)cnc4[nH]ccc34)CC2)cn1"	"IC50"	"'='"	"41.0"	"nM"	"7.39"	""	""	"UO_0000065"	"20.38"	"0.37"	"5.99"	"5.41"	"False"	"CHEMBL3594790"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593212"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL4109703"	""	"0"	"438.53"	"0"	"3.61"	"BDBM229515"	"C[C@@H]1CN(C(=O)OC(C)(C)C)CC[C@]1(CC#N)n1cc(C(N)=O)c(Nc2ccccc2)n1"	"IC50"	"'='"	"24.0"	"nM"	"7.62"	""	"401278"	"UO_0000065"	"17.38"	"0.33"	"4.01"	"6.03"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3973996"	""	"0"	"439.54"	"0"	"3.54"	"BDBM229092"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(CC2CCCCC2)CC1"	"IC50"	"'='"	"57.0"	"nM"	"7.24"	""	"400828"	"UO_0000065"	"16.48"	"0.31"	"3.70"	"6.42"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3972223"	""	"0"	"423.45"	"0"	"2.76"	"BDBM229108"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2ccco2)CC1"	"IC50"	"'='"	"25.0"	"nM"	"7.60"	""	"400844"	"UO_0000065"	"17.95"	"0.33"	"4.84"	"6.03"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3944488"	""	"0"	"452.47"	"0"	"2.70"	"BDBM229112"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2cccnc2F)CC1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"400848"	"UO_0000065"	"18.17"	"0.34"	"5.52"	"6.54"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3930094"	""	"0"	"438.47"	"0"	"2.46"	"BDBM229116"	"Cc1cc(CN2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccnc(F)c4)n3)CC2)no1"	"IC50"	"'='"	"157.0"	"nM"	"6.80"	""	"400852"	"UO_0000065"	"15.52"	"0.29"	"4.34"	"4.90"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3957604"	""	"0"	"424.44"	"0"	"2.15"	"BDBM229117"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2ncco2)CC1"	"IC50"	"'='"	"73.0"	"nM"	"7.14"	""	"400853"	"UO_0000065"	"16.81"	"0.31"	"4.99"	"5.14"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3914676"	""	"0"	"486.55"	"0"	"3.20"	"BDBM228758"	"CN(c1ccc(C(=O)N[C@H]2c3ccccc3C[C@@H]2O)cc1F)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399689"	"UO_0000065"	"21.09"	"0.39"	"7.06"	"10.54"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3589165"	""	"0"	"399.45"	"0"	"3.56"	"2"	"NC(=O)c1cc(-c2ccccc2)cc2c1[nH]c1ccc(C(=O)N3CCOCC3)cc12"	"IC50"	"'='"	"120.0"	"nM"	"6.92"	""	""	"UO_0000065"	"17.33"	"0.32"	"3.36"	"7.83"	"False"	"CHEMBL3592855"	"Inhibition of JAK2 in human SET2 cells assessed as inhibition of cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3589176"	""	"0"	"447.47"	"0"	"3.71"	"13"	"COc1ccc(-c2cc(C(N)=O)c3[nH]c4cc(C(=O)N5CCOCC5)ccc4c3c2)cc1F"	"IC50"	"'='"	"110.0"	"nM"	"6.96"	""	""	"UO_0000065"	"15.55"	"0.29"	"3.25"	"7.13"	"False"	"CHEMBL3592855"	"Inhibition of JAK2 in human SET2 cells assessed as inhibition of cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3665196"	""	"0"	"506.61"	"1"	"0.49"	"BDBM112594"	"CS(=O)(=O)N1CCC[C@H](Nc2nc(N3CCS(=O)(=O)CC3)ncc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.2551"	"nM"	"9.59"	""	"233831"	"UO_0000065"	"18.94"	"0.39"	"9.10"	"6.22"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3593761"	""	"0"	"272.35"	"0"	"2.65"	"2"	"C[C@@H]1CCCC[C@@H]1Nc1c(C(N)=O)cnc2[nH]ccc12"	"IC50"	"'='"	"30.0"	"nM"	"7.52"	""	""	"UO_0000065"	"27.62"	"0.51"	"4.87"	"8.98"	"True"	"CHEMBL3594790"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593212"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3650675"	""	"0"	"430.46"	"0"	"3.41"	"BDBM148056"	"[C-]#[N+][C@H]1C[C@H](N2CCC2)CC[C@@H]1n1cc(Nc2ccc(OC(F)F)nc2)c(C(N)=O)c1"	"IC50"	"'='"	"87.0"	"nM"	"7.06"	""	"285627"	"UO_0000065"	"16.40"	"0.31"	"3.65"	"7.87"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3648430"	""	"0"	"342.20"	"0"	"3.63"	"BDBM107139"	"O=C(CBr)Nc1cccc(-c2cnc3ccccc3n2)c1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	"226377"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703500"	""	"0"	"343.39"	"0"	"4.47"	"BDBM153144"	"CCOC(=O)c1c[nH]c2ncnc(-c3ccc(-c4ccccc4)cc3)c12"	"IC50"	"'='"	"47.0"	"nM"	"7.33"	""	"294092"	"UO_0000065"	"21.34"	"0.38"	"2.86"	"10.80"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642304"	""	"0"	"477.59"	"0"	"3.37"	"BDBM99574"	"CN1CCN(c2ccc(Nc3nc4c(Nc5ccccc5S(C)(=O)=O)cccn4n3)cc2)CC1"	"IC50"	"'='"	"8.3"	"nM"	"8.08"	""	"216264"	"UO_0000065"	"16.92"	"0.32"	"4.71"	"8.52"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3593427"	""	"0"	"229.33"	"0"	"3.33"	"3"	"CN(c1ccnc2[nH]ccc12)C1CCCCC1"	"IC50"	"'='"	"1800.0"	"nM"	"5.75"	""	""	"UO_0000065"	"25.05"	"0.46"	"2.41"	"18.00"	"False"	"CHEMBL3594576"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate and ATP incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593193"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3650674"	""	"0"	"484.50"	"0"	"2.81"	"BDBM147682"	"CN(C)[C@@H]1CCC(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"285615"	"UO_0000065"	"16.61"	"0.33"	"5.24"	"6.00"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3658859"	""	"0"	"374.47"	"0"	"1.35"	"BDBM159778"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](CS(=O)(=O)N2CC[C@H](C#N)C2)C1"	"IC50"	"'='"	"372.0"	"nM"	"6.43"	""	"302588"	"UO_0000065"	"17.17"	"0.34"	"5.08"	"6.07"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3797276"	""	"0"	"438.49"	"0"	"2.59"	"14d"	"C[C@H](NC(=O)OC(C)(C)C)C(=O)Nc1ccc(-c2ncnc3c2cc(C(N)=O)n3C)cc1"	"IC50"	"'='"	"4800.0"	"nM"	"5.32"	""	""	"UO_0000065"	"12.13"	"0.23"	"2.73"	"3.77"	"False"	"CHEMBL3802364"	"Inhibition of JAK2 in GMCSF-stimulated human TF1 cells assessed as suppression of STAT5 phosphorylation preincubated for 2 hrs followed by GMCSF stimulation for 50 mins by FACS reader analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"CHEMBL3307972"	""
"CHEMBL3798416"	""	"0"	"487.52"	"1"	"5.12"	"12g"	"Cn1c(C(=O)OCc2ccccc2)cc2c(-c3ccc(NC(=O)c4ccc(C#N)cc4)cc3)ncnc21"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL3802364"	"Inhibition of JAK2 in GMCSF-stimulated human TF1 cells assessed as suppression of STAT5 phosphorylation preincubated for 2 hrs followed by GMCSF stimulation for 50 mins by FACS reader analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"CHEMBL3307972"	""
"CHEMBL3797848"	""	"0"	"565.68"	"1"	"2.94"	"16d"	"C[C@H](NC(=O)OC(C)(C)C)C(=O)Nc1ccc(-c2ncnc3c2cc(C(=O)NCCCN2CCOCC2)n3C)cc1"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	""	"UO_0000065"	"13.73"	"0.26"	"4.83"	"5.56"	"False"	"CHEMBL3802363"	"Inhibition of recombinant human GST-tagged JAK2 expressed in baculovirus expression system using Z'-LYTE Try6 peptide as substrate incubated for 1 hr by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3799630"	""	"0"	"450.54"	"0"	"2.44"	"16b"	"CCC(=O)Nc1ccc(-c2ncnc3c2cc(C(=O)NCCCN2CCOCC2)n3C)cc1"	"IC50"	"'='"	"23.0"	"nM"	"7.64"	""	""	"UO_0000065"	"16.95"	"0.32"	"5.20"	"7.53"	"False"	"CHEMBL3802363"	"Inhibition of recombinant human GST-tagged JAK2 expressed in baculovirus expression system using Z'-LYTE Try6 peptide as substrate incubated for 1 hr by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3798894"	""	"0"	"371.40"	"0"	"2.99"	"14f"	"Cn1c(C(N)=O)cc2c(-c3ccc(NC(=O)c4ccccc4)cc3)ncnc21"	"IC50"	"'='"	"908.0"	"nM"	"6.04"	""	""	"UO_0000065"	"16.27"	"0.29"	"3.05"	"5.87"	"False"	"CHEMBL3802363"	"Inhibition of recombinant human GST-tagged JAK2 expressed in baculovirus expression system using Z'-LYTE Try6 peptide as substrate incubated for 1 hr by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3797364"	""	"0"	"323.36"	"0"	"2.08"	"14b"	"CCC(=O)Nc1ccc(-c2ncnc3c2cc(C(N)=O)n3C)cc1"	"IC50"	"'='"	"97.0"	"nM"	"7.01"	""	""	"UO_0000065"	"21.69"	"0.40"	"4.93"	"6.82"	"False"	"CHEMBL3802363"	"Inhibition of recombinant human GST-tagged JAK2 expressed in baculovirus expression system using Z'-LYTE Try6 peptide as substrate incubated for 1 hr by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3798416"	""	"0"	"487.52"	"1"	"5.12"	"12g"	"Cn1c(C(=O)OCc2ccccc2)cc2c(-c3ccc(NC(=O)c4ccc(C#N)cc4)cc3)ncnc21"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3802363"	"Inhibition of recombinant human GST-tagged JAK2 expressed in baculovirus expression system using Z'-LYTE Try6 peptide as substrate incubated for 1 hr by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3649607"	""	"0"	"420.90"	"0"	"3.97"	"BDBM130300"	"NC(=O)c1cc(-c2cccc(Cl)c2)nc2c1[nH]c1ccc(CN3CCOCC3)cc12"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"262086"	"UO_0000065"	"21.38"	"0.41"	"5.03"	"10.68"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649608"	""	"0"	"407.42"	"0"	"4.03"	"BDBM130301"	"Cc1ccc(-c2cc(C(N)=O)c3[nH]c4cc(N5CCC(F)(F)C5)ccc4c3n2)cn1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"262087"	"UO_0000065"	"20.18"	"0.37"	"4.19"	"9.35"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649609"	""	"0"	"419.92"	"0"	"3.89"	"BDBM130302"	"CN1CCN(c2ccc3c(c2)[nH]c2c(C(N)=O)cc(-c4cccc(Cl)c4)nc23)CC1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"262088"	"UO_0000065"	"21.43"	"0.41"	"5.11"	"11.50"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL479620"	""	"0"	"210.24"	"0"	"2.21"	"5"	"Nc1n[nH]c2ccc(-c3ccncc3)cc12"	"IC50"	"'='"	"1950.0"	"nM"	"5.71"	""	""	"UO_0000065"	"27.16"	"0.49"	"3.50"	"8.45"	"False"	"CHEMBL1011746"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139271"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL481583"	""	"0"	"243.70"	"0"	"3.47"	"9"	"Nc1n[nH]c2ccc(-c3cccc(Cl)c3)cc12"	"IC50"	"'='"	"740.0"	"nM"	"6.13"	""	""	"UO_0000065"	"25.16"	"0.49"	"2.66"	"11.21"	"False"	"CHEMBL1011746"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139271"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL3894803"	""	"0"	"408.51"	"0"	"2.75"	"BDBM239951"	"Cc1cnc(Nc2cnn(C)c2)nc1NC1CCC2(CC1)CCN(C(=O)CC#N)C2"	"IC50"	"'='"	"129.0"	"nM"	"6.89"	""	"418570"	"UO_0000065"	"16.86"	"0.31"	"4.14"	"6.16"	"False"	"CHEMBL3888834"	"Kinase Assay: JAK2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 100 μM KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC, 10 mM MgAcetate and [γ-33P-ATP](specific activity approx. 500 cpm/pmol, concentration as required). The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of 3% phosphoric acid solution. 10 μL of the reaction is then spotted onto a P30 filtermat and washed three times for 5 minutes in 75 mM phosphoric acid and once in methanol prior to drying and scintillation counting."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886854"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3917346"	""	"0"	"333.83"	"0"	"2.02"	"BDBM239952"	"Cn1cc(Nc2ncc(Cl)c(NC3CC4CNCC4C3)n2)cn1"	"IC50"	"'='"	"176.0"	"nM"	"6.75"	""	"418571"	"UO_0000065"	"20.23"	"0.40"	"4.73"	"8.48"	"False"	"CHEMBL3888834"	"Kinase Assay: JAK2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 100 μM KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC, 10 mM MgAcetate and [γ-33P-ATP](specific activity approx. 500 cpm/pmol, concentration as required). The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of 3% phosphoric acid solution. 10 μL of the reaction is then spotted onto a P30 filtermat and washed three times for 5 minutes in 75 mM phosphoric acid and once in methanol prior to drying and scintillation counting."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886854"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3931866"	""	"0"	"442.95"	"0"	"3.12"	"BDBM239957"	"CN(c1nc(Nc2cnn(C)c2)ncc1Cl)C1CCC2(CCCN(C(=O)CC#N)C2)C1"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"418577"	"UO_0000065"	"18.41"	"0.36"	"5.03"	"7.92"	"False"	"CHEMBL3888834"	"Kinase Assay: JAK2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 100 μM KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC, 10 mM MgAcetate and [γ-33P-ATP](specific activity approx. 500 cpm/pmol, concentration as required). The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of 3% phosphoric acid solution. 10 μL of the reaction is then spotted onto a P30 filtermat and washed three times for 5 minutes in 75 mM phosphoric acid and once in methanol prior to drying and scintillation counting."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886854"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3934612"	""	"0"	"456.98"	"0"	"3.51"	"BDBM239959"	"CN(c1nc(Nc2cnn(C)c2)ncc1Cl)C1CCC2(CC1)CCN(C(=O)CC#N)CC2"	"IC50"	"'='"	"39.0"	"nM"	"7.41"	""	"418579"	"UO_0000065"	"16.21"	"0.32"	"3.90"	"7.20"	"False"	"CHEMBL3888834"	"Kinase Assay: JAK2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 100 μM KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC, 10 mM MgAcetate and [γ-33P-ATP](specific activity approx. 500 cpm/pmol, concentration as required). The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of 3% phosphoric acid solution. 10 μL of the reaction is then spotted onto a P30 filtermat and washed three times for 5 minutes in 75 mM phosphoric acid and once in methanol prior to drying and scintillation counting."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886854"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3905686"	""	"0"	"417.95"	"0"	"3.59"	"BDBM239963"	"CC(=O)N1CCC2(CCC(Nc3nc(Nc4cnn(C)c4)ncc3Cl)CC2)CC1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"418583"	"UO_0000065"	"20.09"	"0.40"	"4.81"	"9.55"	"False"	"CHEMBL3888834"	"Kinase Assay: JAK2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 100 μM KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC, 10 mM MgAcetate and [γ-33P-ATP](specific activity approx. 500 cpm/pmol, concentration as required). The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of 3% phosphoric acid solution. 10 μL of the reaction is then spotted onto a P30 filtermat and washed three times for 5 minutes in 75 mM phosphoric acid and once in methanol prior to drying and scintillation counting."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886854"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3929488"	""	"0"	"454.00"	"0"	"3.00"	"BDBM239964"	"Cn1cc(Nc2ncc(Cl)c(NC3CCC4(CC3)CCN(S(C)(=O)=O)CC4)n2)cn1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"418584"	"UO_0000065"	"18.28"	"0.38"	"5.30"	"7.90"	"False"	"CHEMBL3888834"	"Kinase Assay: JAK2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 100 μM KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC, 10 mM MgAcetate and [γ-33P-ATP](specific activity approx. 500 cpm/pmol, concentration as required). The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of 3% phosphoric acid solution. 10 μL of the reaction is then spotted onto a P30 filtermat and washed three times for 5 minutes in 75 mM phosphoric acid and once in methanol prior to drying and scintillation counting."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886854"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3891708"	""	"0"	"442.50"	"0"	"3.43"	"BDBM237801"	"CC(C)(C)COC(=O)N1CC[C@@H](C#N)[C@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)C1"	"IC50"	"'='"	"145.0"	"nM"	"6.84"	""	"414905"	"UO_0000065"	"15.45"	"0.29"	"3.41"	"5.42"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3934188"	""	"0"	"443.48"	"0"	"1.95"	"BDBM237807"	"CN(C)CCOC(=O)N1CC[C@@H](C#N)[C@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)C1"	"IC50"	"'='"	"352.0"	"nM"	"6.45"	""	"414911"	"UO_0000065"	"14.55"	"0.28"	"4.50"	"4.98"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3897260"	""	"0"	"494.53"	"0"	"3.02"	"BDBM237813"	"CC(C)(COC(=O)N1CC[C@@H](C#N)[C@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)C1)n1cccn1"	"IC50"	"'='"	"383.0"	"nM"	"6.42"	""	"414917"	"UO_0000065"	"12.98"	"0.24"	"3.40"	"4.45"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3982494"	""	"0"	"409.43"	"0"	"2.44"	"BDBM237817"	"N#C[C@@H]1CCN(Cc2cocn2)C[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	"414921"	"UO_0000065"	"18.92"	"0.35"	"5.30"	"6.15"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3897013"	""	"0"	"425.49"	"0"	"2.91"	"BDBM237819"	"N#C[C@@H]1CCN(Cc2cscn2)C[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"19.0"	"nM"	"7.72"	""	"414923"	"UO_0000065"	"18.15"	"0.35"	"4.81"	"6.84"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3986662"	""	"0"	"423.45"	"0"	"2.75"	"BDBM237827"	"Cc1cc(CN2CC[C@@H](C#N)[C@H](n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)C2)no1"	"IC50"	"'='"	"42.0"	"nM"	"7.38"	""	"414931"	"UO_0000065"	"17.42"	"0.32"	"4.63"	"5.85"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4113820"	""	"0"	"437.45"	"0"	"2.99"	"BDBM237848"	"N#C[C@@H]1CN(Cc2cccnc2F)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"79.0"	"nM"	"7.10"	""	"414952"	"UO_0000065"	"16.24"	"0.30"	"4.11"	"6.29"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4114824"	""	"0"	"377.40"	"0"	"1.36"	"BDBM237912"	"C[C@@]1(C#N)CS(=O)(=O)C[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	"415017"	"UO_0000065"	"20.52"	"0.41"	"6.38"	"5.92"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3622195"	""	"0"	"433.90"	"0"	"4.21"	"37"	"NC(=O)c1cc(-c2cccc(Cl)c2)cc2c1[nH]c1ccc(C(=O)N3CCOCC3)cc12"	"IC50"	"'='"	"1.7"	"nM"	"8.77"	""	""	"UO_0000065"	"20.21"	"0.39"	"4.56"	"9.92"	"False"	"CHEMBL3627422"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621099"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3622198"	""	"0"	"442.52"	"0"	"3.48"	"42"	"COc1cccc(-c2cc(C(N)=O)c3[nH]c4cc(C(=O)N5CCN(C)CC5)ccc4c3c2)c1"	"IC50"	"'='"	"4.3"	"nM"	"8.37"	""	""	"UO_0000065"	"18.91"	"0.35"	"4.89"	"9.13"	"False"	"CHEMBL3627422"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621099"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3622201"	""	"0"	"469.55"	"0"	"3.43"	"45"	"CC(=O)Nc1cccc(-c2cc(C(N)=O)c3[nH]c4cc(C(=O)N5CCN(C)CC5)ccc4c3c2)c1"	"IC50"	"'='"	"27.0"	"nM"	"7.57"	""	""	"UO_0000065"	"16.12"	"0.30"	"4.14"	"6.79"	"False"	"CHEMBL3627422"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621099"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3589179"	""	"0"	"371.44"	"0"	"3.92"	"16"	"NC(=O)c1cc(-c2ccccc2)cc2c1[nH]c1cc(N3CCOCC3)ccc12"	"IC50"	"'='"	"7.4"	"nM"	"8.13"	""	""	"UO_0000065"	"21.89"	"0.40"	"4.21"	"11.40"	"False"	"CHEMBL3592849"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3589176"	""	"0"	"447.47"	"0"	"3.71"	"13"	"COc1ccc(-c2cc(C(N)=O)c3[nH]c4cc(C(=O)N5CCOCC5)ccc4c3c2)cc1F"	"IC50"	"'='"	"5.5"	"nM"	"8.26"	""	""	"UO_0000065"	"18.46"	"0.34"	"4.55"	"8.46"	"False"	"CHEMBL3592849"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3589178"	""	"0"	"443.50"	"0"	"4.46"	"15"	"COc1cccc(-c2cc(C(N)=O)c3[nH]c4cc(NC(=O)C5CCOCC5)ccc4c3c2)c1"	"IC50"	"'='"	"10.2"	"nM"	"7.99"	""	""	"UO_0000065"	"18.02"	"0.33"	"3.53"	"7.51"	"False"	"CHEMBL3592849"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3589175"	""	"0"	"429.48"	"0"	"3.57"	"12"	"COc1cccc(-c2cc(C(N)=O)c3[nH]c4cc(C(=O)N5CCOCC5)ccc4c3c2)c1"	"IC50"	"'='"	"5.7"	"nM"	"8.24"	""	""	"UO_0000065"	"19.20"	"0.35"	"4.67"	"8.44"	"False"	"CHEMBL3592849"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3699492"	""	"0"	"442.50"	"0"	"3.62"	"BDBM147507"	"CC(C)(C)OC(=O)NC1CC[C@H](C#N)C(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)C1"	"IC50"	"'='"	"22.0"	"nM"	"7.66"	""	"285437"	"UO_0000065"	"17.31"	"0.33"	"4.04"	"5.67"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3650676"	""	"0"	"454.96"	"0"	"3.88"	"BDBM148057"	"[C-]#[N+][C@@H]1C[C@H](C(=O)N2CC(C)(C)C2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"290.0"	"nM"	"6.54"	""	"285922"	"UO_0000065"	"14.37"	"0.28"	"2.66"	"6.70"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651003"	""	"0"	"375.39"	"0"	"3.19"	"BDBM153179"	"C=C(C)C(=O)Nc1cc(C#N)cc(-c2ncnc3[nH]cc(C(=O)OCC)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294127"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651028"	""	"0"	"419.47"	"0"	"3.91"	"BDBM153205"	"CCOC(=O)c1c[nH]c2ncnc(-c3cccc(NC(=O)/C=C/c4nccs4)c3)c12"	"IC50"	"'='"	"496.0"	"nM"	"6.30"	""	"294153"	"UO_0000065"	"15.03"	"0.29"	"2.39"	"5.74"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL570217"	""	"0"	"377.43"	"0"	"3.72"	"46"	"CC(C)[C@@H](Nc1cc(-c2c(N)nn3cccnc23)ncn1)c1ccc(F)cc1"	"IC50"	"'='"	"470.0"	"nM"	"6.33"	""	""	"UO_0000065"	"16.77"	"0.31"	"2.61"	"6.73"	"False"	"CHEMBL1044320"	"Inhibition of JAK2-mediated STAT5 phosphorylation in GMCSF-stimulated human TF1 cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"CHEMBL3307972"	""
"CHEMBL3651021"	""	"0"	"372.33"	"0"	"3.36"	"BDBM153198"	"C=C(F)C(=O)Nc1cc(-c2ncnc3[nH]cc(C(=O)OCC)c23)ccc1F"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294146"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL1650955"	""	"0"	"468.44"	"0"	"3.03"	"9"	"O=CN1CCN(c2ccc(C(F)(F)F)c(C3=C(c4c[nH]c5ccccc45)C(=O)NC3=O)c2)CC1"	"IC50"	"'='"	"1444.0"	"nM"	"5.84"	""	""	"UO_0000065"	"12.47"	"0.23"	"2.81"	"6.83"	"False"	"CHEMBL1657171"	"Inhibition of GST-tagged Jak2 expressed in insect cells using 20 uM ATP"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649080"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL2208033"	""	"0"	"434.50"	"0"	"1.98"	"10c"	"N[C@H](CO)C(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"1391.0"	"nM"	"5.86"	""	""	"UO_0000065"	"13.48"	"0.25"	"3.88"	"4.66"	"False"	"CHEMBL2214784"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT3 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL576862"	""	"0"	"331.38"	"0"	"2.94"	"38"	"C[C@H](Nc1cc(-c2c(N)nn3cccnc23)ncn1)c1ccccc1"	"IC50"	"'='"	"18000.0"	"nM"	"4.75"	""	""	"UO_0000065"	"14.32"	"0.26"	"1.80"	"5.05"	"False"	"CHEMBL1044320"	"Inhibition of JAK2-mediated STAT5 phosphorylation in GMCSF-stimulated human TF1 cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"CHEMBL3307972"	""
"CHEMBL3814099"	""	"0"	"316.41"	"0"	"1.50"	"3e"	"NCCCn1c2ccc(C(N)=O)cc2nc1[C@H]1CC[C@H](O)CC1"	"IC50"	"'='"	"18500.0"	"nM"	"4.73"	""	""	"UO_0000065"	"14.96"	"0.28"	"3.23"	"4.42"	"False"	"CHEMBL3817413"	"Inhibition of JAK2 (unknown origin) using tyrosine 6 peptide as substrate by z'-lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3813615"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3814951"	""	"0"	"317.39"	"0"	"1.54"	"3b"	"NC(=O)c1ccc2c(c1)nc([C@H]1CC[C@H](O)CC1)n2CCCO"	"IC50"	"'='"	"29700.0"	"nM"	"4.53"	""	""	"UO_0000065"	"14.26"	"0.27"	"2.99"	"4.47"	"False"	"CHEMBL3817413"	"Inhibition of JAK2 (unknown origin) using tyrosine 6 peptide as substrate by z'-lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3813615"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL571118"	""	"0"	"339.36"	"0"	"0.77"	"19"	"COC(=O)C1CCN(c2cc(-c3c(N)nn4cccnc34)ncn2)C1"	"IC50"	"'='"	"87.0"	"nM"	"7.06"	""	""	"UO_0000065"	"20.81"	"0.39"	"6.29"	"6.33"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL569091"	""	"0"	"422.54"	"0"	"2.63"	"25"	"CCCN(CCC)C(=O)C1CCCN(c2cc(-c3c(N)nn4cccnc34)ncn2)C1"	"IC50"	"'='"	"4.7"	"nM"	"8.33"	""	""	"UO_0000065"	"19.71"	"0.37"	"5.70"	"7.89"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL569957"	""	"0"	"462.48"	"0"	"2.79"	"27"	"CCCN(CC(F)(F)F)C(=O)C1CCCN(c2cc(-c3c(N)nn4cccnc34)ncn2)C1"	"IC50"	"'='"	"3.1"	"nM"	"8.51"	""	""	"UO_0000065"	"18.40"	"0.35"	"5.72"	"8.06"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL570890"	""	"0"	"317.36"	"0"	"2.38"	"29"	"Nc1nn2cccnc2c1-c1cc(NCc2ccccc2)ncn1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	""	"UO_0000065"	"25.91"	"0.47"	"5.84"	"8.74"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL570206"	""	"0"	"365.83"	"0"	"3.60"	"39"	"C[C@@H](Nc1cc(-c2c(N)nn3cccnc23)ncn1)c1ccc(Cl)cc1"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	""	"UO_0000065"	"22.13"	"0.43"	"4.50"	"8.61"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL570229"	""	"0"	"343.39"	"0"	"2.87"	"42"	"Nc1nn2cccnc2c1-c1cc(N[C@@H]2CCc3ccccc32)ncn1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	""	"UO_0000065"	"23.18"	"0.42"	"5.09"	"8.46"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL3814934"	""	"0"	"301.39"	"0"	"0.82"	"3f"	"CNCCn1c(C2CCNCC2)nc2cc(C(N)=O)ccc21"	"IC50"	"'='"	"3100.0"	"nM"	"5.51"	""	""	"UO_0000065"	"18.28"	"0.34"	"4.69"	"6.48"	"False"	"CHEMBL3817413"	"Inhibition of JAK2 (unknown origin) using tyrosine 6 peptide as substrate by z'-lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3813615"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL1682376"	""	"0"	"427.47"	"0"	"2.34"	"16"	"Cc1cc(Nc2nc(N3CCN(C(=O)c4ccc(C#N)cc4)CC3)nn3cccc23)n[nH]1"	"IC50"	"'='"	"4.8"	"nM"	"8.32"	""	""	"UO_0000065"	"19.46"	"0.36"	"5.98"	"7.04"	"False"	"CHEMBL1685409"	"Inhibition of JAK2 after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1681645"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1682368"	""	"0"	"298.35"	"0"	"0.91"	"8"	"Cc1cc(Nc2nc(N3CCNCC3)nn3cccc23)n[nH]1"	"IC50"	"'='"	"31.0"	"nM"	"7.51"	""	""	"UO_0000065"	"25.17"	"0.47"	"6.60"	"8.71"	"False"	"CHEMBL1685409"	"Inhibition of JAK2 after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1681645"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL3593591"	""	"0"	"338.37"	"0"	"1.53"	"19"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1n1c(=O)[nH]c2cnc3[nH]ccc3c21"	"IC50"	"'='"	"2.6"	"nM"	"8.59"	""	""	"UO_0000065"	"25.37"	"0.47"	"7.06"	"7.76"	"False"	"CHEMBL3594576"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate and ATP incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593193"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3856117"	""	"0"	"270.34"	"0"	"3.10"	"6c"	"O=c1[nH]c2cnc3[nH]ccc3c2n1C1CCCCCC1"	"IC50"	"'='"	"23.0"	"nM"	"7.64"	""	""	"UO_0000065"	"28.25"	"0.52"	"4.54"	"11.49"	"False"	"CHEMBL3594576"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate and ATP incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593193"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3954183"	""	"0"	"538.60"	"2"	"5.68"	"31"	"O=C(O)c1ccc(NCCOc2ccc3cc2COC/C=C/COCc2cccc(c2)-c2ccnc(n2)N3)cc1"	"IC50"	"'<'"	"39.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3877344"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]ATP addition measured after 120 mins by Hotspot assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3877241"	"1"	"Scientific Literature"	"J Med Chem"	"2016"	"None"	""
"CHEMBL3964125"	""	"0"	"665.79"	"2"	"7.34"	"36"	"O=C(O)CCCCCCC(=O)Nc1ccc(NCCOc2ccc3cc2COC/C=C/COCc2cccc(c2)-c2ccnc(n2)N3)cc1"	"IC50"	"'='"	"2.31"	"nM"	"8.64"	""	""	"UO_0000065"	"12.97"	"0.24"	"1.30"	"6.00"	"False"	"CHEMBL3877344"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]ATP addition measured after 120 mins by Hotspot assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3877241"	"1"	"Scientific Literature"	"J Med Chem"	"2016"	"None"	""
"CHEMBL3917405"	""	"0"	"518.61"	"2"	"5.32"	"51"	"O=C(CCCCCCOc1ccc2cc1COC/C=C/COCc1cccc(c1)-c1ccnc(n1)N2)NO"	"IC50"	"'='"	"1.4"	"nM"	"8.85"	""	""	"UO_0000065"	"17.07"	"0.32"	"3.53"	"7.71"	"False"	"CHEMBL3877344"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]ATP addition measured after 120 mins by Hotspot assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3877241"	"1"	"Scientific Literature"	"J Med Chem"	"2016"	"None"	""
"CHEMBL3948663"	""	"0"	"444.50"	"0"	"3.12"	"16b"	"N#CCC(=O)N1CCc2oc(-c3ccnc(Nc4ccc(N5CCOCC5)cc4)n3)cc2C1"	"IC50"	"'='"	"13.2"	"nM"	"7.88"	""	""	"UO_0000065"	"17.73"	"0.33"	"4.76"	"7.33"	"False"	"CHEMBL3868063"	"Inhibition of GST-tagged recombinant human JAK2 expressed in baculovirus using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3867460"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2017"	"None"	""
"CHEMBL3955194"	""	"0"	"491.52"	"1"	"7.01"	"5h"	"CC1CC(C)CN(c2ccc(Nc3ncc(C(F)(F)F)c(-c4cc5ccc(C#N)cc5o4)n3)cc2)C1"	"IC50"	"'='"	"7089.0"	"nM"	"5.15"	""	""	"UO_0000065"	"10.48"	"0.20"	"-1.86"	"6.60"	"False"	"CHEMBL3868063"	"Inhibition of GST-tagged recombinant human JAK2 expressed in baculovirus using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3867460"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2017"	"None"	""
"CHEMBL3966342"	""	"0"	"411.47"	"0"	"4.65"	"5f"	"Cc1cnc(Nc2ccc(N3CCOCC3)cc2)nc1-c1cc2cc(C#N)ccc2o1"	"IC50"	"'='"	"10.4"	"nM"	"7.98"	""	""	"UO_0000065"	"19.40"	"0.35"	"3.33"	"9.15"	"False"	"CHEMBL3868063"	"Inhibition of GST-tagged recombinant human JAK2 expressed in baculovirus using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3867460"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2017"	"None"	""
"CHEMBL4243822"	""	"0"	"638.77"	"2"	"6.99"	"13g"	"O=C(CCCCCCC(=O)Nc1ccc(Nc2nc(-c3cnn(CCCCCCOc4ccccc4)c3)c3cc[nH]c3n2)cc1)NO"	"IC50"	"'='"	"19.0"	"nM"	"7.72"	""	""	"UO_0000065"	"12.09"	"0.22"	"0.73"	"4.85"	"False"	"CHEMBL4233426"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma-33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229421"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2018"	"None"	""
"CHEMBL3622133"	""	"0"	"439.52"	"0"	"2.48"	"14"	"CCn1c(C(=O)N(C2CC2)C2CC2)cc2c3c(ncn3C)c(NC(=O)NCCOC)nc21"	"IC50"	"'='"	"210.0"	"nM"	"6.68"	""	""	"UO_0000065"	"15.19"	"0.29"	"4.20"	"6.28"	"False"	"CHEMBL3625474"	"Inhibition of JAK2 in human SET2 cells assessed as inhibition of cell proliferation after 72 hrs by [3H]-thymidine incorporation assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621098"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL4228189"	""	"0"	"581.71"	"2"	"5.46"	"19"	"CCNC(=O)c1cc2c(-c3cccc(OCCCCCCn4cc(-c5ncnc6[nH]ccc56)cn4)c3)nc(N)nc2s1"	"IC50"	"'='"	"1420.0"	"nM"	"5.85"	""	""	"UO_0000065"	"10.05"	"0.19"	"0.39"	"3.91"	"False"	"CHEMBL4222523"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma33P]-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219149"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2018"	"None"	""
"CHEMBL481584"	""	"0"	"228.25"	"0"	"2.42"	"6"	"Cc1noc(C)c1-c1ccc2[nH]nc(N)c2c1"	"IC50"	"'='"	"28600.0"	"nM"	"4.54"	""	""	"UO_0000065"	"19.91"	"0.37"	"2.12"	"5.63"	"False"	"CHEMBL1011746"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139271"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL480412"	""	"0"	"323.40"	"0"	"3.73"	"15"	"CC(C)(C)NC(=O)Nc1ccc(-c2ccc3[nH]nc(N)c3c2)cc1"	"IC50"	"'='"	"3900.0"	"nM"	"5.41"	""	""	"UO_0000065"	"16.73"	"0.31"	"1.68"	"5.64"	"False"	"CHEMBL1011746"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139271"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"Tofacitinib"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"4.2"	"nM"	"8.38"	""	""	"UO_0000065"	""	""	""	""	"True"	"CHEMBL4220907"	"Inhibition of recombinant GST-tagged human JAK2 (809 to 1153 residues) catalytic cytoplasmic domain expressed in baculovirus expression system using IRS-1 as substrate in presence of 4 uM ATP by mobility shift assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL3622128"	""	"0"	"382.47"	"0"	"2.11"	"6"	"CNc1nc2c(cc(C(=O)N(C3CC3)C3CC3)n2CCCO)c2c1ncn2C"	"IC50"	"'='"	"4.5"	"nM"	"8.35"	""	""	"UO_0000065"	"21.82"	"0.41"	"6.24"	"9.46"	"False"	"CHEMBL3625473"	"Inhibition of JAK2 (unknown origin) using 5-FAMKKKKEEIYFFFG-OH as substrate after 60 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621098"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3622127"	""	"0"	"398.47"	"0"	"1.08"	"3"	"CNc1nc2c(cc(C(=O)N(C3CC3)C3CC3)n2C[C@H](O)CO)c2c1ncn2C"	"IC50"	"'='"	"8.2"	"nM"	"8.09"	""	""	"UO_0000065"	"20.29"	"0.38"	"7.01"	"7.46"	"False"	"CHEMBL3625473"	"Inhibition of JAK2 (unknown origin) using 5-FAMKKKKEEIYFFFG-OH as substrate after 60 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621098"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL4636371"	""	"0"	"231.30"	"0"	"2.61"	"7"	"Cc1[nH]nc2[nH]c(=O)cc(C3CCCCC3)c12"	"IC50"	"'>'"	"40000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL4640521"	""	"0"	"245.33"	"0"	"2.85"	"10"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CCCC[C@H]3C)c12"	"IC50"	"'='"	"8900.0"	"nM"	"5.05"	""	""	"UO_0000065"	"20.59"	"0.38"	"2.20"	"8.21"	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL4636507"	""	"0"	"384.52"	"0"	"3.87"	"38"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](CC(=O)N4CCC(C)(C)CC4)CC3)c12"	"IC50"	"'='"	"3400.0"	"nM"	"5.47"	""	""	"UO_0000065"	"14.22"	"0.27"	"1.60"	"6.68"	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL2062797"	""	"0"	"394.46"	"0"	"3.55"	"22"	"COc1ccccc1Nc1nc2c(-c3ccc(S(C)(=O)=O)cc3)cccn2n1"	"IC50"	"'='"	"1615.0"	"nM"	"5.79"	""	""	"UO_0000065"	"14.68"	"0.28"	"2.24"	"6.77"	"False"	"CHEMBL2067611"	"Inhibition of human JAK2 expressed in baculovirus using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate preincubated for 1 hr measured after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL3593580"	""	"0"	"270.34"	"0"	"2.96"	"6f"	"C[C@H]1CCCC[C@H]1n1c(=O)[nH]c2cnc3[nH]ccc3c21"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	""	"UO_0000065"	"28.74"	"0.53"	"4.81"	"11.69"	"False"	"CHEMBL3594576"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate and ATP incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593193"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL2062807"	""	"0"	"511.63"	"1"	"2.77"	"32"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4cccc(CN5CCS(=O)(=O)CC5)c4)nc23)cc1"	"IC50"	"'='"	"107.0"	"nM"	"6.97"	""	""	"UO_0000065"	"13.62"	"0.27"	"4.20"	"6.13"	"False"	"CHEMBL2067179"	"Inhibition of JAK2 in human TF-1 cells using GM-CSF pretreated for 1 hr prior to GM-CSF addition measured after 5 hrs by FRET based GeneBLAzer assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"CHEMBL3307972"	""
"CHEMBL1934336"	""	"0"	"533.66"	"1"	"3.20"	"3b"	"CN(c1ccccc1-c1ccc2cnc(Nc3ccc(C4CCN(CC(N)=O)CC4)cc3)nn12)S(C)(=O)=O"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	""	"UO_0000065"	"16.30"	"0.31"	"5.50"	"6.91"	"False"	"CHEMBL1936085"	"Inhibition of human recombinant JAK2 expressed in baculovirus expression system after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL1938652"	""	"0"	"367.35"	"0"	"3.80"	"17"	"CNC(=O)c1cnc(N)c2cc(-c3ccc(OC(F)(F)F)cc3)sc12"	"IC50"	"'='"	"2890.0"	"nM"	"5.54"	""	""	"UO_0000065"	"15.08"	"0.30"	"1.74"	"7.17"	"False"	"CHEMBL1941390"	"Inhibition of TEL-fused JAK2 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3307634"	""
"CHEMBL1938657"	""	"0"	"475.64"	"0"	"2.91"	"23"	"CN(C)CCNC(=O)c1cnc(N)c2cc(-c3ccc(S(=O)(=O)NC(C)(C)C)cc3)sc12"	"IC50"	"'='"	"2400.0"	"nM"	"5.62"	""	""	"UO_0000065"	"11.82"	"0.24"	"2.71"	"4.79"	"False"	"CHEMBL1941390"	"Inhibition of TEL-fused JAK2 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3307634"	""
"CHEMBL3601231"	""	"0"	"464.96"	"0"	"4.45"	"21"	"C=CC(=O)Nc1cccc(CNc2nc(Nc3ccc(N4CCOCC4)cc3)ncc2Cl)c1"	"IC50"	"'='"	"17.6"	"nM"	"7.75"	""	""	"UO_0000065"	"16.68"	"0.32"	"3.30"	"8.48"	"False"	"CHEMBL3603319"	"Inhibition of JAK2 (unknown origin) by Z'-Lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3600288"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL3601120"	""	"0"	"413.87"	"0"	"2.80"	"50"	"C=CC(=O)Nc1cccc(CNc2nc(Nc3cnn(CCO)c3)ncc2Cl)c1"	"IC50"	"'='"	"32.0"	"nM"	"7.50"	""	""	"UO_0000065"	"18.11"	"0.35"	"4.69"	"6.41"	"False"	"CHEMBL3603319"	"Inhibition of JAK2 (unknown origin) by Z'-Lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3600288"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL3647753"	""	"0"	"550.61"	"1"	"4.03"	"BDBM147856"	"N#C[C@H]1C[C@@H](NC(C2CC2)C2CC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"39.0"	"nM"	"7.41"	""	"285790"	"UO_0000065"	"13.46"	"0.27"	"3.38"	"5.18"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3797795"	""	"0"	"309.33"	"0"	"1.69"	"14a"	"CC(=O)Nc1ccc(-c2ncnc3c2cc(C(N)=O)n3C)cc1"	"IC50"	"'>'"	"20000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3802364"	"Inhibition of JAK2 in GMCSF-stimulated human TF1 cells assessed as suppression of STAT5 phosphorylation preincubated for 2 hrs followed by GMCSF stimulation for 50 mins by FACS reader analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"CHEMBL3307972"	""
"CHEMBL3799642"	""	"0"	"523.60"	"1"	"3.21"	"16g"	"Cn1c(C(=O)NCCCN2CCOCC2)cc2c(-c3ccc(NC(=O)c4ccc(C#N)cc4)cc3)ncnc21"	"IC50"	"'='"	"81.0"	"nM"	"7.09"	""	""	"UO_0000065"	"13.54"	"0.25"	"3.88"	"5.67"	"False"	"CHEMBL3802363"	"Inhibition of recombinant human GST-tagged JAK2 expressed in baculovirus expression system using Z'-LYTE Try6 peptide as substrate incubated for 1 hr by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3800528"	""	"0"	"498.59"	"0"	"3.34"	"16f"	"Cn1c(C(=O)NCCCN2CCOCC2)cc2c(-c3ccc(NC(=O)c4ccccc4)cc3)ncnc21"	"IC50"	"'='"	"94.0"	"nM"	"7.03"	""	""	"UO_0000065"	"14.09"	"0.26"	"3.69"	"6.93"	"False"	"CHEMBL3802363"	"Inhibition of recombinant human GST-tagged JAK2 expressed in baculovirus expression system using Z'-LYTE Try6 peptide as substrate incubated for 1 hr by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3798482"	""	"0"	"478.60"	"0"	"3.07"	"16c"	"Cn1c(C(=O)NCCCN2CCOCC2)cc2c(-c3ccc(NC(=O)C(C)(C)C)cc3)ncnc21"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	""	"UO_0000065"	"17.18"	"0.32"	"5.15"	"8.11"	"False"	"CHEMBL3802363"	"Inhibition of recombinant human GST-tagged JAK2 expressed in baculovirus expression system using Z'-LYTE Try6 peptide as substrate incubated for 1 hr by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3798686"	""	"0"	"436.52"	"0"	"2.05"	"16a"	"CC(=O)Nc1ccc(-c2ncnc3c2cc(C(=O)NCCCN2CCOCC2)n3C)cc1"	"IC50"	"'='"	"36.0"	"nM"	"7.44"	""	""	"UO_0000065"	"17.05"	"0.32"	"5.39"	"7.34"	"False"	"CHEMBL3802363"	"Inhibition of recombinant human GST-tagged JAK2 expressed in baculovirus expression system using Z'-LYTE Try6 peptide as substrate incubated for 1 hr by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3800009"	""	"0"	"420.52"	"0"	"2.81"	"15b"	"CCC(=O)Nc1ccc(-c2ncnc3c2cc(C(=O)NCCN2CCCC2)n3C)cc1"	"IC50"	"'='"	"67.0"	"nM"	"7.17"	""	""	"UO_0000065"	"17.06"	"0.32"	"4.36"	"7.79"	"False"	"CHEMBL3802363"	"Inhibition of recombinant human GST-tagged JAK2 expressed in baculovirus expression system using Z'-LYTE Try6 peptide as substrate incubated for 1 hr by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3799984"	""	"0"	"462.51"	"1"	"5.24"	"12f"	"Cn1c(C(=O)OCc2ccccc2)cc2c(-c3ccc(NC(=O)c4ccccc4)cc3)ncnc21"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3802363"	"Inhibition of recombinant human GST-tagged JAK2 expressed in baculovirus expression system using Z'-LYTE Try6 peptide as substrate incubated for 1 hr by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3799424"	""	"0"	"400.44"	"0"	"3.95"	"12a"	"CC(=O)Nc1ccc(-c2ncnc3c2cc(C(=O)OCc2ccccc2)n3C)cc1"	"IC50"	"'='"	"732.0"	"nM"	"6.13"	""	""	"UO_0000065"	"15.32"	"0.28"	"2.19"	"7.13"	"False"	"CHEMBL3802363"	"Inhibition of recombinant human GST-tagged JAK2 expressed in baculovirus expression system using Z'-LYTE Try6 peptide as substrate incubated for 1 hr by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL4107757"	""	"0"	"349.44"	"0"	"2.72"	"BDBM198386"	"N#C[C@H]1CCN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C1"	"IC50"	"'='"	"38.0"	"nM"	"7.42"	""	"352464"	"UO_0000065"	"21.23"	"0.39"	"4.70"	"8.64"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3890951"	""	"0"	"362.39"	"0"	"2.73"	"BDBM198414"	"O=C(OCc1ccccc1)N1CCC(c2nnn3cnc4[nH]ccc4c23)C1"	"IC50"	"'='"	"740.0"	"nM"	"6.13"	""	"352492"	"UO_0000065"	"16.92"	"0.31"	"3.40"	"6.93"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3953550"	""	"0"	"357.42"	"0"	"2.86"	"BDBM198226"	"N#Cc1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	"352308"	"UO_0000065"	"22.38"	"0.40"	"5.14"	"9.31"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3900724"	""	"0"	"468.40"	"1"	"5.02"	"BDBM198239"	"FC(F)(F)c1cc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cc(C(F)(F)F)c1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"352321"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3973453"	""	"0"	"338.46"	"0"	"3.37"	"BDBM198242"	"c1cc2c(ncn3nnc(C4CCN(CC5CCCCC5)CC4)c23)[nH]1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"352324"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3593776"	""	"0"	"362.40"	"0"	"1.40"	"11f"	"N#Cc1ccc(N2CCC(Nc3c(C(N)=O)cnc4[nH]ccc34)CC2)nn1"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	""	"UO_0000065"	"21.86"	"0.40"	"6.52"	"5.80"	"False"	"CHEMBL3594790"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593212"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3906263"	""	"0"	"360.46"	"0"	"3.46"	"BDBM198330"	"c1ccc(CCN[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"94.0"	"nM"	"7.03"	""	"352408"	"UO_0000065"	"19.49"	"0.36"	"3.57"	"9.91"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3980041"	""	"0"	"374.49"	"0"	"3.85"	"BDBM198331"	"c1ccc(CCCN[C@H]2CC[C@@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"352409"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3947711"	""	"0"	"430.43"	"0"	"3.54"	"BDBM198415"	"OC(CN1CCC(c2nnn3cnc4[nH]ccc4c23)CC1)c1ccc(C(F)(F)F)cc1"	"IC50"	"'='"	"47.0"	"nM"	"7.33"	""	"352493"	"UO_0000065"	"17.02"	"0.32"	"3.79"	"8.90"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3984960"	""	"0"	"378.45"	"0"	"3.81"	"BDBM198294"	"Fc1ccc(CNC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"46.0"	"nM"	"7.34"	""	"352372"	"UO_0000065"	"19.39"	"0.36"	"3.53"	"10.35"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3937827"	""	"0"	"439.45"	"0"	"4.88"	"BDBM198298"	"N#Cc1ccc(NC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1C(F)(F)F"	"IC50"	"'='"	"190.0"	"nM"	"6.72"	""	"352376"	"UO_0000065"	"15.29"	"0.29"	"1.84"	"7.10"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3894366"	""	"0"	"412.40"	"0"	"3.31"	"BDBM198432"	"FC1(F)Oc2cccc(CN3CCC(c4nnn5cnc6[nH]ccc6c45)CC3)c2O1"	"IC50"	"'='"	"87.0"	"nM"	"7.06"	""	"352510"	"UO_0000065"	"17.12"	"0.32"	"3.75"	"8.76"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3923184"	""	"0"	"270.34"	"0"	"1.84"	"BDBM198574"	"NC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"35.0"	"nM"	"7.46"	""	"352652"	"UO_0000065"	"27.58"	"0.51"	"5.62"	"8.78"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3920329"	""	"0"	"380.37"	"0"	"2.95"	"BDBM198576"	"O=C(CC(F)(F)F)NC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	"352654"	"UO_0000065"	"20.92"	"0.40"	"5.01"	"9.05"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3940316"	""	"0"	"371.45"	"0"	"2.90"	"BDBM198578"	"N#Cc1ccc(CCN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"330.0"	"nM"	"6.48"	""	"352656"	"UO_0000065"	"17.45"	"0.32"	"3.58"	"7.55"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3973102"	""	"0"	"399.24"	"0"	"3.21"	"BDBM198586"	"FC(F)(Br)CN[C@H]1CC[C@@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"63.0"	"nM"	"7.20"	""	"352664"	"UO_0000065"	"18.04"	"0.41"	"3.99"	"10.16"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3934891"	""	"0"	"269.31"	"0"	"2.08"	"BDBM198609"	"O=C[C@H]1CC[C@@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"30.0"	"nM"	"7.52"	""	"352687"	"UO_0000065"	"27.93"	"0.51"	"5.44"	"9.91"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3975399"	""	"0"	"419.41"	"0"	"3.18"	"BDBM198614"	"N#CCC(=O)N(CC(F)(F)F)C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"7.3"	"nM"	"8.14"	""	"352692"	"UO_0000065"	"19.40"	"0.37"	"4.96"	"7.90"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3942459"	""	"0"	"363.47"	"0"	"3.11"	"BDBM198621"	"N#CCN(CC1CC1)C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"130.0"	"nM"	"6.89"	""	"352699"	"UO_0000065"	"18.95"	"0.35"	"3.78"	"8.02"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3896324"	""	"0"	"373.44"	"0"	"1.32"	"BDBM198626"	"N#CCNS(=O)(=O)C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"6.1"	"nM"	"8.21"	""	"352704"	"UO_0000065"	"22.00"	"0.43"	"6.89"	"6.38"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3984562"	""	"0"	"348.43"	"0"	"1.43"	"BDBM198634"	"CS(=O)(=O)NC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"1.2"	"nM"	"8.92"	""	"352712"	"UO_0000065"	"25.60"	"0.51"	"7.49"	"8.49"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3911332"	""	"0"	"464.57"	"0"	"3.37"	"BDBM198635"	"CC(C)(C)OC(=O)N1CC(CC#N)(NC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C1"	"IC50"	"'='"	"750.0"	"nM"	"6.12"	""	"352713"	"UO_0000065"	"13.18"	"0.25"	"2.75"	"4.93"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3907503"	""	"0"	"253.31"	"0"	"2.82"	"BDBM198640"	"C=C1CCC(c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"27.0"	"nM"	"7.57"	""	"352718"	"UO_0000065"	"29.88"	"0.54"	"4.75"	"12.86"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3974289"	""	"0"	"380.37"	"0"	"2.95"	"BDBM198651"	"O=C(C[C@H]1CC[C@@H](c2nnn3cnc4[nH]ccc4c23)CC1)NCC(F)(F)F"	"IC50"	"'='"	"61.0"	"nM"	"7.21"	""	"352729"	"UO_0000065"	"18.97"	"0.36"	"4.26"	"8.20"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL2062804"	""	"0"	"462.58"	"0"	"3.30"	"29, CEP-33779"	"CN1CCN(c2cccc(Nc3nc4c(-c5ccc(S(C)(=O)=O)cc5)cccn4n3)c2)CC1"	"IC50"	"'='"	"61.0"	"nM"	"7.21"	""	""	"UO_0000065"	"15.60"	"0.30"	"3.91"	"8.71"	"False"	"CHEMBL2067179"	"Inhibition of JAK2 in human TF-1 cells using GM-CSF pretreated for 1 hr prior to GM-CSF addition measured after 5 hrs by FRET based GeneBLAzer assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"CHEMBL3307972"	""
"CHEMBL3939415"	""	"0"	"487.59"	"0"	"3.50"	"179"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3ccsc3)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3965520"	""	"0"	"390.47"	"0"	"4.08"	"BDBM198378"	"Fc1ccc2c(c1)CCN2C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"94.0"	"nM"	"7.03"	""	"352456"	"UO_0000065"	"18.00"	"0.33"	"2.95"	"11.31"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4109199"	""	"0"	"328.42"	"0"	"1.85"	"BDBM198384"	"C[C@@H](O)CNC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"51.0"	"nM"	"7.29"	""	"352462"	"UO_0000065"	"22.20"	"0.41"	"5.44"	"8.00"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3896784"	""	"0"	"390.49"	"0"	"3.20"	"BDBM198385"	"OC(CNC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1)c1ccccc1"	"IC50"	"'='"	"27.0"	"nM"	"7.57"	""	"352463"	"UO_0000065"	"19.38"	"0.36"	"4.37"	"8.31"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3966425"	""	"0"	"380.88"	"0"	"4.08"	"BDBM198399"	"Clc1ccc(CN[C@H]2CC[C@@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"400.0"	"nM"	"6.40"	""	"352477"	"UO_0000065"	"16.80"	"0.32"	"2.32"	"9.02"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3946125"	""	"0"	"462.45"	"0"	"3.81"	"BDBM198403"	"OC(CN[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1)(c1ccc(F)cc1)C(F)(F)F"	"IC50"	"'='"	"32.0"	"nM"	"7.50"	""	"352481"	"UO_0000065"	"16.21"	"0.31"	"3.68"	"8.22"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3983447"	""	"0"	"378.45"	"0"	"3.60"	"BDBM198404"	"Fc1ccc(CCN[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"66.0"	"nM"	"7.18"	""	"352482"	"UO_0000065"	"18.97"	"0.35"	"3.58"	"10.13"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3892296"	""	"0"	"313.36"	"0"	"2.44"	"BDBM198265"	"CC(=O)OC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"7.7"	"nM"	"8.11"	""	"352345"	"UO_0000065"	"25.89"	"0.48"	"5.67"	"9.53"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3940267"	""	"0"	"351.39"	"0"	"2.52"	"BDBM198360"	"Fc1cnccc1CN1CCC(c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	"352438"	"UO_0000065"	"22.65"	"0.42"	"5.44"	"10.61"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3906687"	""	"0"	"448.42"	"0"	"4.22"	"BDBM198368"	"FC(F)C(F)(F)Oc1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"52.0"	"nM"	"7.28"	""	"352446"	"UO_0000065"	"16.24"	"0.31"	"3.06"	"10.21"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3940421"	""	"0"	"478.50"	"0"	"4.29"	"BDBM198372"	"O=S(=O)(c1ccc(NC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1)C(F)(F)F"	"IC50"	"'='"	"260.0"	"nM"	"6.58"	""	"352450"	"UO_0000065"	"13.76"	"0.27"	"2.30"	"6.27"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3896566"	""	"0"	"417.34"	"0"	"3.81"	"BDBM198440"	"Brc1csc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)c1"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	"352518"	"UO_0000065"	"19.17"	"0.44"	"4.19"	"12.88"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3902123"	""	"0"	"281.32"	"0"	"1.31"	"BDBM198449"	"N#CCN1CCC(c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"19.0"	"nM"	"7.72"	""	"352527"	"UO_0000065"	"27.45"	"0.50"	"6.41"	"8.99"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3956550"	""	"0"	"389.44"	"0"	"4.00"	"BDBM198455"	"N#Cc1cc(NC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)ccc1F"	"IC50"	"'='"	"60.0"	"nM"	"7.22"	""	"352533"	"UO_0000065"	"18.54"	"0.34"	"3.22"	"7.63"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3904312"	""	"0"	"314.39"	"0"	"1.46"	"BDBM198475"	"OCCNC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"53.0"	"nM"	"7.28"	""	"352553"	"UO_0000065"	"23.14"	"0.43"	"5.82"	"7.98"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4110648"	""	"0"	"354.46"	"0"	"2.65"	"BDBM198492"	"c1cc2c(ncn3nnc([C@H]4CC[C@H](CNC[C@H]5CCCO5)CC4)c23)[nH]1"	"IC50"	"'='"	"150.0"	"nM"	"6.82"	""	"352570"	"UO_0000065"	"19.25"	"0.36"	"4.17"	"8.52"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3904186"	""	"0"	"324.43"	"0"	"3.02"	"BDBM198498"	"CC1(NC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)CC1"	"IC50"	"'='"	"64.0"	"nM"	"7.19"	""	"352576"	"UO_0000065"	"22.17"	"0.41"	"4.17"	"10.15"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3971717"	""	"0"	"358.45"	"0"	"1.17"	"BDBM198501"	"OCCN(CCO)C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"110.0"	"nM"	"6.96"	""	"352579"	"UO_0000065"	"19.41"	"0.37"	"5.79"	"6.78"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3914847"	""	"0"	"382.51"	"0"	"3.16"	"BDBM198516"	"OC1(CNC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)CCCCC1"	"IC50"	"'='"	"51.0"	"nM"	"7.29"	""	"352594"	"UO_0000065"	"19.06"	"0.36"	"4.13"	"8.00"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3916687"	""	"0"	"409.42"	"0"	"2.15"	"BDBM198544"	"O=C(CNC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1)NCC(F)(F)F"	"IC50"	"'='"	"59.0"	"nM"	"7.23"	""	"352622"	"UO_0000065"	"17.66"	"0.34"	"5.08"	"7.23"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3983344"	""	"0"	"284.32"	"0"	"1.36"	"BDBM198551"	"NC(=O)[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"51.0"	"nM"	"7.29"	""	"352629"	"UO_0000065"	"25.65"	"0.47"	"5.93"	"7.15"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3945378"	""	"0"	"399.46"	"0"	"3.07"	"BDBM198553"	"N#Cc1ccc(CNC(=O)[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"47.0"	"nM"	"7.33"	""	"352631"	"UO_0000065"	"18.34"	"0.33"	"4.26"	"6.56"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3894516"	""	"0"	"366.35"	"0"	"2.56"	"BDBM198557"	"O=C(NCC(F)(F)F)[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"26.0"	"nM"	"7.58"	""	"352635"	"UO_0000065"	"20.70"	"0.40"	"5.03"	"8.62"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3962300"	""	"0"	"328.38"	"0"	"0.99"	"BDBM198563"	"O=C(NCCO)[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"100.0"	"nM"	"7.00"	""	"352641"	"UO_0000065"	"21.32"	"0.40"	"6.01"	"6.47"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3975088"	""	"0"	"413.48"	"0"	"3.49"	"BDBM198568"	"O=S(=O)(C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1)c1ccc(F)cc1"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	"352646"	"UO_0000065"	"18.85"	"0.37"	"4.31"	"8.38"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3954249"	""	"0"	"391.87"	"0"	"3.51"	"BDBM198580"	"N#Cc1ccc(CN2CCC(c3nnn4cnc5[nH]cc(Cl)c5c34)CC2)cc1"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	"352658"	"UO_0000065"	"19.83"	"0.38"	"4.26"	"9.04"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3952261"	""	"0"	"419.41"	"0"	"3.18"	"BDBM198619"	"N#CCN(C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1)C(=O)CC(F)(F)F"	"IC50"	"'='"	"5.6"	"nM"	"8.25"	""	"352697"	"UO_0000065"	"19.67"	"0.38"	"5.07"	"8.01"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3906460"	""	"0"	"408.43"	"0"	"3.14"	"BDBM198628"	"FC(F)(F)COC1CN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C1"	"IC50"	"'='"	"170.0"	"nM"	"6.77"	""	"352706"	"UO_0000065"	"16.57"	"0.32"	"3.63"	"9.49"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3985603"	""	"0"	"435.45"	"0"	"2.49"	"BDBM198633"	"O=C(NCC(F)(F)F)C1CN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C1"	"IC50"	"'='"	"62.0"	"nM"	"7.21"	""	"352711"	"UO_0000065"	"16.55"	"0.32"	"4.72"	"7.90"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3971373"	""	"0"	"292.35"	"0"	"2.96"	"BDBM198649"	"N#C/C=C/[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"31.0"	"nM"	"7.51"	""	"352727"	"UO_0000065"	"25.68"	"0.47"	"4.55"	"9.08"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3929124"	""	"0"	"291.31"	"0"	"3.14"	"BDBM198272"	"FC(F)[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	"352352"	"UO_0000065"	"26.43"	"0.50"	"4.56"	"13.08"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3940750"	""	"0"	"491.56"	"0"	"2.92"	"12"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(C#N)cc3)CC2)C1"	"IC50"	"'>'"	"100.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3985038"	""	"0"	"538.51"	"1"	"3.61"	"54"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc(F)c(F)c(F)c3F)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3898273"	""	"0"	"534.63"	"1"	"2.99"	"59"	"CN(C)c1ccc(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)cc1C#N"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3898930"	""	"0"	"522.99"	"1"	"4.34"	"228"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(Cc3c(F)ccc(Cl)c3F)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3911659"	""	"0"	"563.59"	"1"	"4.77"	"285"	"Cc1nc(C(F)(F)F)ccc1NC(=O)N1CCC(N2CC(CC#N)(n3ccc(-c4ncnc5[nH]ccc45)c3)C2)CC1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3939867"	""	"0"	"464.56"	"0"	"1.65"	"357"	"CS(=O)(=O)N1CCC(N2CC(CC#N)(n3cc(-c4c(C#N)cnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3937622"	""	"0"	"548.66"	"1"	"2.98"	"369"	"CN(C)Cc1cc(C#N)cc(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)c1"	"IC50"	"'>'"	"100.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL412099"	""	"0"	"378.82"	"1"	"5.93"	"3, MF63"	"N#Cc1cccc(C#N)c1-c1nc2c3ccc(Cl)cc3c3ccccc3c2[nH]1"	"IC50"	"'='"	"100.0"	"nM"	"7.00"	""	""	"UO_0000065"	"18.48"	"0.34"	"1.07"	"9.18"	"False"	"CHEMBL945937"	"Inhibition of human JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1142217"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2007"	"None"	""
"CHEMBL3885292"	""	"0"	"534.69"	"1"	"3.97"	"5d"	"Cc1cc(Nc2ncc(C#N)c(Nc3cccc(S(=O)(=O)NC(C)(C)C)c3)n2)ccc1N1CCN(C)CC1"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3875838"	"Inhibition of human JAK2 using poly (Glu:Tyr) as substrate"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3875172"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2016"	"None"	""
"CHEMBL3884104"	""	"0"	"453.57"	"0"	"2.67"	"5k"	"Cc1cc(Nc2nccc(Nc3cccc(S(N)(=O)=O)c3)n2)ccc1N1CCN(C)CC1"	"IC50"	"'='"	"126.0"	"nM"	"6.90"	""	""	"UO_0000065"	"15.21"	"0.29"	"4.23"	"5.92"	"False"	"CHEMBL3875838"	"Inhibition of human JAK2 using poly (Glu:Tyr) as substrate"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3875172"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2016"	"None"	""
"CHEMBL3883652"	""	"0"	"374.49"	"0"	"4.02"	"5o"	"Cc1cccc(Nc2ccnc(Nc3ccc(N4CCN(C)CC4)cc3)n2)c1"	"IC50"	"'='"	"140.0"	"nM"	"6.85"	""	""	"UO_0000065"	"18.30"	"0.33"	"2.83"	"12.17"	"False"	"CHEMBL3875838"	"Inhibition of human JAK2 using poly (Glu:Tyr) as substrate"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3875172"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2016"	"None"	""
"CHEMBL3262357"	""	"0"	"403.49"	"0"	"3.53"	"3c"	"Cc1c[nH]c2c(Nc3nc(N[C@@H]4CCCC[C@@H]4N)cc4nc[nH]c(=O)c34)cccc12"	"IC50"	"'='"	"190.0"	"nM"	"6.72"	""	""	"UO_0000065"	"16.66"	"0.31"	"3.19"	"5.40"	"False"	"CHEMBL3268711"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3259804"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3262616"	""	"0"	"389.46"	"0"	"3.22"	"3f"	"N[C@H]1CCCC[C@H]1Nc1cc2nc[nH]c(=O)c2c(Nc2cccc3[nH]ccc23)n1"	"IC50"	"'='"	"83.0"	"nM"	"7.08"	""	""	"UO_0000065"	"18.18"	"0.33"	"3.86"	"5.69"	"False"	"CHEMBL3268711"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3259804"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3649617"	""	"0"	"536.03"	"1"	"3.68"	"BDBM130311"	"NC(=O)c1cc(-c2ccc(OCCN3CCOCC3)c(Cl)c2)nc2c1[nH]c1cc(N3CCOCC3)ccc12"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"262097"	"UO_0000065"	"16.79"	"0.32"	"5.32"	"8.50"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL2178352"	""	"0"	"468.61"	"1"	"5.18"	"9e"	"CN1CCN(c2ccc(Nc3ncc4nc(Nc5ccccc5)n(C5CCCC5)c4n3)cc2)CC1"	"IC50"	"'='"	"1200.0"	"nM"	"5.92"	""	""	"UO_0000065"	"12.63"	"0.23"	"0.74"	"7.99"	"False"	"CHEMBL2188525"	"Inhibition of human recombinant JAK2 by radiometric kinase assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2177100"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL21156"	""	"0"	"309.34"	"0"	"3.99"	"K00013, Pyridone 6"	"CC(C)(C)c1nc2c3ccc(F)cc3c3c(=O)[nH]ccc3c2[nH]1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	""	"UO_0000065"	"29.09"	"0.53"	"5.01"	"14.62"	"True"	"CHEMBL937065"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1145498"	"1"	"Scientific Literature"	"Proc. Natl. Acad. Sci. U.S.A."	"2007"	"None"	""
"CHEMBL3915844"	""	"0"	"323.36"	"0"	"1.47"	"BDBM198204"	"CC1CCN(C(=O)CC#N)CC1c1nnn2cnc3[nH]ccc3c12"	"IC50"	"'='"	"220.0"	"nM"	"6.66"	""	"352286"	"UO_0000065"	"20.59"	"0.38"	"5.19"	"6.47"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3969865"	""	"0"	"369.41"	"0"	"1.87"	"BDBM198222"	"O=C(Nc1nncs1)N1CCC(c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"64.0"	"nM"	"7.19"	""	"352304"	"UO_0000065"	"19.47"	"0.38"	"5.32"	"6.15"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3900224"	""	"0"	"309.30"	"0"	"3.44"	"BDBM198262"	"FC(F)(F)[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"26.0"	"nM"	"7.58"	""	"352343"	"UO_0000065"	"24.52"	"0.47"	"4.15"	"12.88"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3911186"	""	"0"	"255.28"	"0"	"1.83"	"BDBM198275"	"O=C1CCC(c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"300.0"	"nM"	"6.52"	""	"352354"	"UO_0000065"	"25.55"	"0.47"	"4.69"	"8.59"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3925854"	""	"0"	"384.85"	"0"	"3.78"	"BDBM198364"	"Fc1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)c(Cl)c1"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	"352442"	"UO_0000065"	"20.01"	"0.39"	"3.92"	"12.40"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3980241"	""	"0"	"340.43"	"0"	"1.95"	"BDBM198312"	"O[C@H]1CCN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C1"	"IC50"	"'='"	"39.0"	"nM"	"7.41"	""	"352390"	"UO_0000065"	"21.76"	"0.40"	"5.46"	"9.00"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3898916"	""	"0"	"400.41"	"0"	"4.76"	"BDBM198321"	"FC(F)(F)c1ccc(NC2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"352399"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3911874"	""	"0"	"249.28"	"0"	"2.58"	"BDBM198197"	"Cc1ccccc1-c1nnn2cnc3[nH]ccc3c12"	"IC50"	"'='"	"130.0"	"nM"	"6.89"	""	"351819"	"UO_0000065"	"27.62"	"0.49"	"4.31"	"11.70"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652357"	""	"0"	"391.54"	"0"	"2.77"	"BDBM113168"	"C[C@H]1CCCN1S(=O)(=O)C[C@H]1CC[C@H](N(C)c2ncnc3[nH]ccc23)CC1"	"IC50"	"'='"	"42.8"	"nM"	"7.37"	""	"234611"	"UO_0000065"	"18.82"	"0.37"	"4.60"	"8.97"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL1923592"	""	"0"	"534.69"	"1"	"4.10"	"33"	"C[C@H](O)CN1CCC(c2ccc(Nc3ncc4ccc(-c5ccccc5N(C)S(C)(=O)=O)n4n3)cc2)CC1"	"IC50"	"'='"	"0.9"	"nM"	"9.05"	""	""	"UO_0000065"	"16.92"	"0.33"	"4.95"	"8.78"	"False"	"CHEMBL1926252"	"Inhibition of human recombinant JAK2 using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate after 20 mins by fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1921765"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL2414547"	""	"0"	"462.58"	"0"	"3.30"	"BDBM99582"	"CN1CCN(c2ccc(Nc3nc4cccc(-c5ccc(S(C)(=O)=O)cc5)n4n3)cc2)CC1"	"IC50"	"'='"	"6.9"	"nM"	"8.16"	""	"216272"	"UO_0000065"	"17.64"	"0.34"	"4.86"	"9.85"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3622825"	""	"0"	"261.33"	"0"	"-0.01"	"5b"	"NCCCc1nc2cc(C(N)=O)ccc2n1CCN"	"IC50"	"'='"	"1600.0"	"nM"	"5.80"	""	""	"UO_0000065"	"22.18"	"0.42"	"5.81"	"5.13"	"False"	"CHEMBL3625898"	"Inhibition of JAK2 (unknown origin) using 35 uM of ATP and Tyr6 peptide by Z'-LYTE kinase assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621116"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL3648432"	""	"0"	"359.31"	"0"	"3.76"	"BDBM107141"	"O=C(CC(=O)C(F)(F)F)Nc1cccc(-c2cnc3ccccc3n2)c1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	"226379"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647764"	""	"0"	"460.50"	"0"	"4.37"	"BDBM147867"	"C[C@H](NC1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(C(F)(F)F)cc3)n2)[C@@H](C#N)C1)C1CC1"	"IC50"	"'='"	"104.0"	"nM"	"6.98"	""	"285801"	"UO_0000065"	"15.16"	"0.29"	"2.61"	"6.42"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665129"	""	"0"	"350.43"	"0"	"2.83"	"BDBM112516"	"CC(=O)N1CCCCC(Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.0191"	"nM"	"10.72"	""	"233755"	"UO_0000065"	"30.59"	"0.56"	"7.89"	"12.35"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL1947161"	""	"0"	"344.42"	"0"	"4.64"	"26e"	"C1=C/CNc2cccc(c2)Nc2nccc(n2)-c2cccc(c2)OCC/1"	"IC50"	"'='"	"3300.0"	"nM"	"5.48"	""	""	"UO_0000065"	"15.92"	"0.29"	"0.84"	"9.28"	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1944699"	""	"0"	"372.47"	"0"	"4.41"	"26i"	"CN1C/C=C/COCc2cccc(c2)-c2ccnc(n2)Nc2cccc(c2)C1"	"IC50"	"'='"	"1700.0"	"nM"	"5.77"	""	""	"UO_0000065"	"15.49"	"0.28"	"1.36"	"11.47"	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1944701"	""	"0"	"398.51"	"1"	"5.19"	"26k"	"C1=C/CN(C2CC2)Cc2cccc(c2)Nc2nccc(n2)-c2cccc(c2)OCC/1"	"IC50"	"'='"	"90.0"	"nM"	"7.05"	""	""	"UO_0000065"	"17.68"	"0.32"	"1.86"	"14.01"	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1944870"	""	"0"	"414.55"	"1"	"5.68"	"26l"	"CC(C)CN1C/C=C/CCOc2cccc(c2)-c2ccnc(n2)Nc2cccc(c2)C1"	"IC50"	"'='"	"1500.0"	"nM"	"5.82"	""	""	"UO_0000065"	"14.05"	"0.26"	"0.14"	"11.58"	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"20, CP-690550"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	""	"UO_0000065"	"26.88"	"0.50"	"6.86"	"9.45"	"True"	"CHEMBL1941383"	"Inhibition of human recombinant N-terminal GST-tagged JAK2 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308860"	""
"CHEMBL1938656"	""	"0"	"462.60"	"0"	"3.00"	"22"	"COCCNC(=O)c1cnc(N)c2cc(-c3ccc(S(=O)(=O)NC(C)(C)C)cc3)sc12"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"18.42"	"0.38"	"5.52"	"6.91"	"False"	"CHEMBL1941383"	"Inhibition of human recombinant N-terminal GST-tagged JAK2 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308860"	""
"CHEMBL3647887"	""	"0"	"508.93"	"1"	"4.32"	"BDBM147999"	"N#C[C@H]1C[C@@H](C(=O)N[C@H](C2CC2)C(F)(F)F)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'>'"	"500.0"	"nM"	""	""	"285934"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"20, CP-690550"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"155.0"	"nM"	"6.81"	""	""	"UO_0000065"	"21.80"	"0.40"	"5.27"	"7.66"	"False"	"CHEMBL1941458"	"Inhibition of JAK2 in human PBMC assessed as inhibition of TPO-stimulated STAT5 phosphorylation preincubated for 30 mins prior to TPO challenge measured after 15 mins by intracellular phosflow staining"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1938657"	""	"0"	"475.64"	"0"	"2.91"	"23"	"CN(C)CCNC(=O)c1cnc(N)c2cc(-c3ccc(S(=O)(=O)NC(C)(C)C)cc3)sc12"	"IC50"	"'='"	"515.0"	"nM"	"6.29"	""	""	"UO_0000065"	"13.22"	"0.27"	"3.38"	"5.36"	"False"	"CHEMBL1941458"	"Inhibition of JAK2 in human PBMC assessed as inhibition of TPO-stimulated STAT5 phosphorylation preincubated for 30 mins prior to TPO challenge measured after 15 mins by intracellular phosflow staining"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1938659"	""	"0"	"517.68"	"1"	"2.68"	"25"	"CC(C)(C)NS(=O)(=O)c1ccc(-c2cc3c(N)ncc(C(=O)NCCN4CCOCC4)c3s2)cc1"	"IC50"	"'='"	"148.0"	"nM"	"6.83"	""	""	"UO_0000065"	"13.19"	"0.27"	"4.15"	"5.39"	"False"	"CHEMBL1941458"	"Inhibition of JAK2 in human PBMC assessed as inhibition of TPO-stimulated STAT5 phosphorylation preincubated for 30 mins prior to TPO challenge measured after 15 mins by intracellular phosflow staining"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL3645022"	""	"0"	"497.53"	"0"	"5.00"	"BDBM99774"	"COc1ccc(C(F)(F)F)cc1Nc1cccn2nc(Nc3cccc(N4CCN(C)CC4)c3)nc12"	"IC50"	"'='"	"2999.0"	"nM"	"5.52"	""	"216461"	"UO_0000065"	"11.10"	"0.21"	"0.52"	"7.89"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703008"	""	"0"	"490.53"	"0"	"3.68"	"BDBM147718"	"CC(C)(O)C1CN([C@H]2CC[C@H](n3cc(C(N)=O)c(Nc4ccc(C(F)(F)F)cc4)n3)[C@@H](C#N)C2)C1"	"IC50"	"'='"	"77.0"	"nM"	"7.11"	""	"285652"	"UO_0000065"	"14.50"	"0.28"	"3.43"	"5.92"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645055"	""	"0"	"524.55"	"1"	"4.61"	"BDBM99822"	"COc1ccc(C(F)(F)F)cc1-c1cccn2nc(Nc3ccc4c(c3)CCN(CC(=O)N(C)C)C4)nc12"	"IC50"	"'='"	"41.4"	"nM"	"7.38"	""	"216495"	"UO_0000065"	"14.07"	"0.27"	"2.77"	"9.84"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3622147"	""	"0"	"433.52"	"0"	"2.89"	"10"	"CCn1c(C(=O)N(C2CC2)C2CC2)cc2c3c(ncn3C)c(Nc3nc(C)n(C)n3)nc21"	"IC50"	"'='"	"33.0"	"nM"	"7.48"	""	""	"UO_0000065"	"17.26"	"0.32"	"4.59"	"7.58"	"False"	"CHEMBL3625512"	"Inhibition of recombinant JAK2 (unknown origin) using 5-FAM-KKKKEEIYFFFG-OH substrate and ATP incubated for 180 mins by scintillation counting method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621135"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3658861"	""	"0"	"322.43"	"0"	"2.00"	"BDBM159780"	"CCCS(=O)(=O)C[C@H]1C[C@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"946.0"	"nM"	"6.02"	""	"302590"	"UO_0000065"	"18.68"	"0.37"	"4.02"	"7.63"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647750"	""	"0"	"524.57"	"1"	"3.64"	"BDBM147853"	"CC(N[C@@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)(F)F)cc3)n2)[C@@H](C#N)C1)C1CC1"	"IC50"	"'='"	"43.0"	"nM"	"7.37"	""	"285787"	"UO_0000065"	"14.04"	"0.28"	"3.73"	"5.16"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652378"	""	"0"	"454.60"	"0"	"3.17"	"BDBM113189"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC[C@H](c3ccccn3)C2)CC1"	"IC50"	"'='"	"6.22"	"nM"	"8.21"	""	"234632"	"UO_0000065"	"18.05"	"0.35"	"5.04"	"8.63"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3665171"	""	"0"	"397.46"	"0"	"1.73"	"BDBM112564"	"CS(=O)(=O)N1CCC[C@H](Nc2ncccc2-c2cnc3[nH]cc(C#N)c3n2)C1"	"IC50"	"'='"	"0.1236"	"nM"	"9.91"	""	"233801"	"UO_0000065"	"24.93"	"0.48"	"8.18"	"7.76"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3655089"	""	"0"	"383.44"	"0"	"1.17"	"BDBM159756"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)c2cc(C#N)ccn2)C1"	"IC50"	"'='"	"700.0"	"nM"	"6.16"	""	"302566"	"UO_0000065"	"16.05"	"0.31"	"4.98"	"4.82"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652354"	""	"0"	"545.73"	"1"	"3.01"	"BDBM113165"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC[C@H](S(=O)(=O)CCc3ccccc3)C2)CC1"	"IC50"	"'='"	"16.7"	"nM"	"7.78"	""	"234608"	"UO_0000065"	"14.25"	"0.29"	"4.77"	"6.69"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3699471"	""	"0"	"325.37"	"0"	"1.95"	"BDBM147486"	"N#C[C@@H]1C(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCC[C@H]1O"	"IC50"	"'='"	"202.0"	"nM"	"6.70"	""	"285411"	"UO_0000065"	"20.58"	"0.38"	"4.74"	"5.72"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665173"	""	"0"	"412.52"	"0"	"2.73"	"BDBM112566"	"CS(=O)(=O)N1CCC[C@H](Nc2ncccc2-c2cnc3[nH]cc(C4CC4)c3n2)C1"	"IC50"	"'='"	"0.0384"	"nM"	"10.42"	""	"233803"	"UO_0000065"	"25.25"	"0.49"	"7.69"	"10.03"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642318"	""	"0"	"505.60"	"1"	"3.20"	"BDBM99590"	"CN1CCN(c2ccc(NC(=O)Nc3nc4cccc(-c5cccc(S(C)(=O)=O)c5)n4n3)cc2)CC1"	"IC50"	"'='"	"229.5"	"nM"	"6.64"	""	"216280"	"UO_0000065"	"13.13"	"0.25"	"3.44"	"5.93"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647901"	""	"0"	"476.92"	"0"	"3.73"	"BDBM148013"	"N#C[C@H]1C[C@@H](C(=O)N2CCC(F)(F)C2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"115.0"	"nM"	"6.94"	""	"285948"	"UO_0000065"	"14.55"	"0.29"	"3.21"	"5.93"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642337"	""	"0"	"477.59"	"0"	"3.37"	"BDBM99609"	"CN1CCN(c2cccc(Nc3nc4c(Nc5cccc(S(C)(=O)=O)c5)cccn4n3)c2)CC1"	"IC50"	"'='"	"1312.24"	"nM"	"5.88"	""	"216299"	"UO_0000065"	"12.32"	"0.24"	"2.51"	"6.20"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3622134"	""	"0"	"421.53"	"0"	"3.91"	"15"	"CCn1c(C(=O)N(C2CC2)C2CC2)cc2c3c(ncn3C)c(Nc3nccs3)nc21"	"IC50"	"'='"	"1.4"	"nM"	"8.85"	""	""	"UO_0000065"	"21.00"	"0.40"	"4.94"	"10.95"	"False"	"CHEMBL3625473"	"Inhibition of JAK2 (unknown origin) using 5-FAMKKKKEEIYFFFG-OH as substrate after 60 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621098"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3639412"	""	"0"	"491.62"	"0"	"3.24"	"BDBM99659"	"CN1CCN(c2ccc(Nc3nc4c(NCc5cccc(S(C)(=O)=O)c5)cccn4n3)cc2)CC1"	"IC50"	"'='"	"262.42"	"nM"	"6.58"	""	"216349"	"UO_0000065"	"13.39"	"0.26"	"3.34"	"6.94"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647724"	""	"0"	"526.54"	"1"	"2.58"	"BDBM147826"	"COC1CN(C2CC[C@H](n3cc(C(N)=O)c(Nc4ccc(S(=O)(=O)C(F)(F)F)cc4)n3)[C@@H](C#N)C2)C1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"285760"	"UO_0000065"	"15.77"	"0.31"	"5.72"	"5.79"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642342"	""	"0"	"476.61"	"0"	"3.29"	"BDBM99617"	"CN1CCN(Cc2cccc(Nc3nc4cccc(-c5ccc(S(C)(=O)=O)cc5)n4n3)c2)CC1"	"IC50"	"'='"	"1.43"	"nM"	"8.85"	""	"216307"	"UO_0000065"	"18.56"	"0.36"	"5.55"	"10.68"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642291"	""	"0"	"414.51"	"0"	"3.90"	"BDBM99557"	"COc1ccccc1-c1cccn2nc(Nc3ccc(N4CCN(C)CC4)cc3)nc12"	"IC50"	"'='"	"38.4"	"nM"	"7.42"	""	"216248"	"UO_0000065"	"17.89"	"0.33"	"3.52"	"12.80"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3645546"	""	"0"	"361.45"	"0"	"2.48"	"BDBM107132"	"CN1CCN(CC(=O)Nc2cccc(-c3cnc4ccccc4n3)c2)CC1"	"IC50"	"'>'"	"50000.0"	"nM"	""	""	"226370"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3694582"	""	"0"	"352.83"	"0"	"4.94"	"BDBM125903"	"C[C@H]1Nc2nc(ncc2Cl)Nc2cccc(c2)COc2cccc1c2"	"IC50"	"'='"	"350.0"	"nM"	"6.46"	""	"255676"	"UO_0000065"	"18.30"	"0.35"	"1.52"	"10.93"	"False"	"CHEMBL3707544"	"In Vitro Kinase Assay: One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Biochemistry 1999, 269, 94-104. The catalytic domains of human JAK1 (a.a. 837-1142), JAK2 (a.a. 828-1132) and JAK3 (a.a. 781-1124) with an N-terminal His tag were expressed using baculovirus in insect cells and purified. The catalytic activity of JAK1, JAK2 or JAK3 was assayed by measuring the phosphorylation of a biotinylated peptide. The phosphorylated peptide was detected by homogenous time resolved fluorescence (HTRF). IC50s of compounds were measured for each kinase in the reactions that contain the enzyme, ATP and 500 nM peptide in 50 mM Tris (pH 7.8) buffer with 100 mM NaCl, 5 mM DTT, and 0.1 mg/mL (0.01%) BSA. The ATP concentration in the reactions was 90 uM for JAK1, 30 uM for JAK2 and 3 uM for JAK3. Reactions were carried out at room temperature for 1 hr and then stopped with 20 uL 45 mM EDTA."	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639093"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3642400"	""	"0"	"548.67"	"1"	"4.60"	"BDBM99678"	"CC(C)(C)OC(=O)N1CCN(c2cccc(Nc3nc4c(-c5ccc(S(C)(=O)=O)cc5)cccn4n3)c2)CC1"	"IC50"	"'='"	"3.72"	"nM"	"8.43"	""	"216368"	"UO_0000065"	"15.36"	"0.30"	"3.83"	"7.72"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652328"	""	"0"	"475.66"	"0"	"3.42"	"BDBM113138"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCC(COCC3CC3)CC2)CC1"	"IC50"	"'='"	"59.8"	"nM"	"7.22"	""	"234581"	"UO_0000065"	"15.19"	"0.30"	"3.80"	"7.90"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3652343"	""	"0"	"409.51"	"0"	"0.32"	"BDBM113154"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2C[C@@H](O)[C@H](O)C2)CC1"	"IC50"	"'='"	"39.6"	"nM"	"7.40"	""	"234597"	"UO_0000065"	"18.08"	"0.36"	"7.08"	"6.04"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3652287"	""	"0"	"407.54"	"0"	"1.74"	"BDBM113096"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCC[C@H](O)C2)CC1"	"IC50"	"'='"	"16.2"	"nM"	"7.79"	""	"234540"	"UO_0000065"	"19.12"	"0.38"	"6.05"	"7.61"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3642274"	""	"0"	"399.48"	"0"	"2.53"	"BDBM99536"	"COc1ccc(Nc2nc3c(C4=CCN(S(C)(=O)=O)CC4)cccn3n2)cc1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"216228"	"UO_0000065"	"22.53"	"0.44"	"6.47"	"10.13"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703487"	""	"0"	"297.31"	"0"	"2.81"	"BDBM153131"	"CCOC(=O)c1c[nH]c2ncnc(-c3ccc(OC)cc3)c12"	"IC50"	"'='"	"134.0"	"nM"	"6.87"	""	"294079"	"UO_0000065"	"23.12"	"0.43"	"4.06"	"8.91"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652349"	""	"0"	"413.49"	"0"	"2.27"	"BDBM113160"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2C[C@@H](F)[C@H](F)C2)CC1"	"IC50"	"'='"	"34.3"	"nM"	"7.46"	""	"234603"	"UO_0000065"	"18.05"	"0.36"	"5.19"	"9.08"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3642288"	""	"0"	"545.71"	"1"	"3.76"	"BDBM99553"	"CN1CCN(C2CCN(c3ccc(Nc4nc5c(-c6ccc(S(C)(=O)=O)cc6)cccn5n4)cc3)CC2)CC1"	"IC50"	"'='"	"1.8"	"nM"	"8.74"	""	"216244"	"UO_0000065"	"16.02"	"0.31"	"4.98"	"10.16"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3658110"	""	"0"	"568.64"	"2"	"5.85"	"BDBM148418"	"Cc1ccc(NC(=O)CCC(F)(F)F)cc1N1CCc2nc(Nc3ccc(OCCN4CCCC4)cc3)ncc2C1"	"IC50"	"'='"	"21.0"	"nM"	"7.68"	""	"286796"	"UO_0000065"	"13.50"	"0.26"	"1.83"	"9.29"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645023"	""	"0"	"427.55"	"0"	"4.86"	"BDBM99776"	"CC(C)COc1ccccc1-c1cccn2nc(Nc3ccc4c(c3)CCNCC4)nc12"	"IC50"	"'='"	"1792.1"	"nM"	"5.75"	""	"216462"	"UO_0000065"	"13.44"	"0.25"	"0.89"	"9.05"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647820"	""	"0"	"460.50"	"0"	"4.46"	"BDBM147925"	"CN(C1CCC1)[C@H]1CC[C@@H](n2cc(C(N)=O)c(Nc3ccc(C(F)(F)F)cc3)n2)[C@H](C#N)C1"	"IC50"	"'='"	"240.0"	"nM"	"6.62"	""	"285859"	"UO_0000065"	"14.38"	"0.27"	"2.16"	"6.62"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699542"	""	"0"	"378.41"	"0"	"3.67"	"BDBM147560"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2cnc3cc(F)ccc3c2)n1"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	"285490"	"UO_0000065"	"20.60"	"0.38"	"4.13"	"7.11"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647892"	""	"0"	"426.91"	"0"	"3.14"	"BDBM148004"	"N#C[C@@H]1C[C@H](C(=O)NC2CC2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"23.0"	"nM"	"7.64"	""	"285939"	"UO_0000065"	"17.89"	"0.35"	"4.50"	"6.07"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652366"	""	"0"	"451.59"	"0"	"1.35"	"BDBM113177"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC[C@](CO)(CCO)C2)CC1"	"IC50"	"'='"	"45.8"	"nM"	"7.34"	""	"234620"	"UO_0000065"	"16.25"	"0.32"	"5.99"	"5.98"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3703096"	""	"0"	"482.61"	"0"	"2.85"	"BDBM147811"	"CS(=O)(=O)c1ccc(Nc2nn([C@H]3CC[C@H](N4CC5(CCC5)C4)C[C@@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"285745"	"UO_0000065"	"17.20"	"0.33"	"5.45"	"6.19"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3658853"	""	"0"	"387.47"	"0"	"0.60"	"BDBM159772"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)N2C[C@H]3C[C@@]3(C#N)C2)C1"	"IC50"	"'='"	"551.0"	"nM"	"6.26"	""	"302582"	"UO_0000065"	"16.15"	"0.32"	"5.66"	"5.30"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703052"	""	"0"	"450.54"	"0"	"3.03"	"BDBM147762"	"CC(C)(C(=O)O)c1ccc(Nc2nn([C@H]3CC[C@@H](N4CCC4)C[C@@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"130.0"	"nM"	"6.89"	""	"285696"	"UO_0000065"	"15.28"	"0.28"	"3.86"	"5.02"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652363"	""	"0"	"506.67"	"1"	"3.22"	"BDBM113174"	"CN(C(=O)OC(C)(C)C)[C@H]1CCN(S(=O)(=O)C[C@H]2CC[C@H](N(C)c3ncnc4[nH]ccc34)CC2)C1"	"IC50"	"'='"	"81.0"	"nM"	"7.09"	""	"234617"	"UO_0000065"	"14.00"	"0.28"	"3.87"	"6.35"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3642422"	""	"0"	"422.51"	"0"	"3.48"	"BDBM99700"	"CN(c1ccccc1CNc1cccn2nc(Nc3ccccc3)nc12)S(C)(=O)=O"	"IC50"	"'='"	"571.33"	"nM"	"6.24"	""	"216390"	"UO_0000065"	"14.78"	"0.28"	"2.76"	"6.81"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3650681"	""	"0"	"367.41"	"0"	"2.33"	"BDBM148065"	"N#C[C@H]1CCC2(C[C@@H]1n1cc(C(N)=O)c(Nc3ccccc3)n1)OCCO2"	"IC50"	"'='"	"59.0"	"nM"	"7.23"	""	"285989"	"UO_0000065"	"19.68"	"0.37"	"4.90"	"6.28"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665165"	""	"0"	"372.45"	"0"	"1.86"	"BDBM112558"	"CS(=O)(=O)N1CCC[C@H](Nc2ncccc2-c2cnc3cc[nH]c3n2)C1"	"IC50"	"'='"	"1.23"	"nM"	"8.91"	""	"233796"	"UO_0000065"	"23.92"	"0.47"	"7.05"	"8.58"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642262"	""	"0"	"447.56"	"0"	"4.53"	"BDBM99520"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4ccc(N5CCCCC5)cc4)nc23)cc1"	"IC50"	"'='"	"0.6"	"nM"	"9.22"	""	"216212"	"UO_0000065"	"20.60"	"0.39"	"4.69"	"11.59"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3650992"	""	"0"	"364.41"	"0"	"3.62"	"BDBM153167"	"C=C(C)C(=O)Nc1cc(-c2ncnc3[nH]cc(C(=O)OCC)c23)ccc1C"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294115"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3644978"	""	"0"	"499.62"	"1"	"5.87"	"BDBM99729"	"CCOc1ccccc1-c1cccn2nc(Nc3ccc4c(c3)CCN(C(=O)OC(C)(C)C)CC4)nc12"	"IC50"	"'='"	"1103.03"	"nM"	"5.96"	""	"216418"	"UO_0000065"	"11.92"	"0.22"	"0.09"	"7.36"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647835"	""	"0"	"479.50"	"0"	"3.54"	"BDBM147942"	"CC(C)(c1ccc(Nc2nn([C@H]3CC[C@](C)(O)C[C@@H]3C#N)cc2C(N)=O)cc1)C(O)C(F)(F)F"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"285877"	"UO_0000065"	"18.14"	"0.35"	"5.16"	"6.34"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647760"	""	"0"	"510.54"	"1"	"3.20"	"BDBM147863"	"CC1CN([C@@H]2CC[C@H](n3cc(C(N)=O)c(Nc4ccc(S(=O)(=O)C(F)(F)F)cc4)n3)[C@@H](C#N)C2)C1"	"IC50"	"'='"	"25.0"	"nM"	"7.60"	""	"285797"	"UO_0000065"	"14.89"	"0.30"	"4.40"	"5.67"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699556"	""	"0"	"378.26"	"0"	"4.29"	"BDBM147574"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2cc(Cl)cc(Cl)c2)n1"	"IC50"	"'='"	"119.0"	"nM"	"6.92"	""	"285504"	"UO_0000065"	"18.31"	"0.38"	"2.63"	"7.16"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL2006765"	""	"0"	"392.39"	"0"	"3.82"	"5"	"CCCNC(=O)c1ccc(Nc2nc(NCC(F)(F)F)c3cc[nH]c3n2)cc1"	"IC50"	"'='"	"57.0"	"nM"	"7.24"	""	""	"UO_0000065"	"18.46"	"0.35"	"3.42"	"7.65"	"False"	"CHEMBL4007715"	"Inhibition of JAK2 (unknown origin) after 60 mins by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4007384"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2016"	"None"	""
"CHEMBL4078893"	""	"0"	"427.81"	"0"	"4.43"	"7"	"FC(F)(F)CNc1nc(Nc2ccc(N3CCOCC3)c(Cl)c2)nc2ccoc12"	"IC50"	"'='"	"2320.0"	"nM"	"5.63"	""	""	"UO_0000065"	"13.17"	"0.27"	"1.20"	"7.47"	"False"	"CHEMBL4007715"	"Inhibition of JAK2 (unknown origin) after 60 mins by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4007384"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2016"	"None"	""
"CHEMBL3938017"	""	"0"	"443.48"	"0"	"2.90"	"BDBM228966"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CC1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"400711"	"UO_0000065"	"18.72"	"0.35"	"5.40"	"5.97"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3956882"	""	"0"	"506.56"	"1"	"4.07"	"BDBM228760"	"COC[C@@H](NC(=O)c1cc(F)c(N(C)[C@@H]2CCN(c3ncnc4[nH]ccc34)C2)c(F)c1)c1ccccc1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399691"	"UO_0000065"	"20.25"	"0.38"	"6.19"	"11.88"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3905754"	""	"0"	"457.56"	"0"	"1.53"	"BDBM228698"	"CN(c1ccc(S(=O)(=O)NC[C@@H]2CCCO2)cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399695"	"UO_0000065"	"22.42"	"0.44"	"8.73"	"8.82"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3979629"	""	"0"	"361.41"	"0"	"2.57"	"BDBM228662"	"CN(C(=O)Nc1cccc(C#N)c1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399702"	"UO_0000065"	"25.62"	"0.47"	"6.69"	"9.17"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3929901"	""	"0"	"285.40"	"0"	"2.41"	"BDBM228771"	"CN(C1CCCC1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399707"	"UO_0000065"	"32.44"	"0.60"	"6.85"	"19.27"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL2035046"	""	"0"	"360.42"	"0"	"3.89"	"13f, 95:5 trans/Cis mixture"	"C1=C/COCc2cncc(c2)-c2ccnc(n2)Nc2cccc(c2)COC/1"	"IC50"	"'='"	"930.0"	"nM"	"6.03"	""	""	"UO_0000065"	"16.73"	"0.31"	"2.14"	"8.72"	"False"	"CHEMBL2040119"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2034857"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2035184"	""	"0"	"478.62"	"1"	"5.03"	"14k, 95:5 trans/Cis mixture"	"C1=C/COCc2cc(ccc2OCCN2CCCC2)Nc2nccc(n2)-c2csc(c2)COC/1"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	""	"UO_0000065"	"16.23"	"0.31"	"2.74"	"11.30"	"False"	"CHEMBL2040119"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2034857"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL3942917"	""	"0"	"555.61"	"1"	"2.98"	"BDBM228989"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(C(=O)N4CCOCC4)c(F)c3)n2)CC1"	"IC50"	"'='"	"0.7"	"nM"	"9.15"	""	"400734"	"UO_0000065"	"16.48"	"0.31"	"6.17"	"5.88"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3951216"	""	"0"	"503.40"	"1"	"4.13"	"BDBM229019"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3cccc(Br)c3)n2)CC1"	"IC50"	"'='"	"37.0"	"nM"	"7.43"	""	"400763"	"UO_0000065"	"14.76"	"0.32"	"3.30"	"5.89"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3919105"	""	"0"	"398.27"	"0"	"2.70"	"BDBM228781"	"CN(c1ncc(Br)cc1C#N)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399719"	"UO_0000065"	"23.25"	"0.51"	"6.56"	"10.93"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3964318"	""	"0"	"353.82"	"0"	"2.59"	"BDBM228782"	"CN(c1ccc(C#N)c(Cl)n1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399720"	"UO_0000065"	"26.17"	"0.51"	"6.67"	"10.93"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3913608"	""	"0"	"354.36"	"0"	"2.82"	"BDBM228787"	"CN(c1c(F)cc(C#N)cc1F)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399725"	"UO_0000065"	"26.13"	"0.49"	"6.44"	"12.89"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3985350"	""	"0"	"491.98"	"0"	"3.18"	"BDBM228798"	"CN(c1ccc(C(=O)NC(CO)c2ccccc2Cl)cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399737"	"UO_0000065"	"18.82"	"0.36"	"6.08"	"8.40"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3965713"	""	"0"	"415.52"	"0"	"2.22"	"BDBM228691"	"CC(C)S(=O)(=O)Nc1ccc(N(C)[C@@H]2CCN(c3ncnc4[nH]ccc34)C2)nc1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399739"	"UO_0000065"	"22.28"	"0.44"	"7.04"	"8.64"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3907106"	""	"0"	"391.47"	"0"	"3.22"	"BDBM255036"	"CCN1CN([C@H]2CC[C@H](CNCC(F)F)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"27.0"	"nM"	"7.57"	""	"443908"	"UO_0000065"	"19.33"	"0.37"	"4.35"	"11.78"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3671151"	""	"0"	"451.48"	"0"	"3.06"	"BDBM127650"	"Cn1cncc1CCNC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258324"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675908"	""	"0"	"343.34"	"0"	"2.45"	"BDBM127657"	"NC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258331"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675911"	""	"0"	"469.49"	"0"	"3.72"	"BDBM127660"	"O=C(NC1CCC(C(=O)O)CC1)c1cnn2ccc(N3CCCC3c3cc(F)ccc3F)nc12"	"IC50"	"'='"	"23.4"	"nM"	"7.63"	""	"258334"	"UO_0000065"	"16.25"	"0.31"	"3.91"	"7.64"	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675918"	""	"0"	"417.44"	"0"	"3.83"	"BDBM127667"	"CC(C)(CF)NC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258341"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675922"	""	"0"	"504.56"	"1"	"2.50"	"BDBM127671"	"CS(=O)(=O)N1CCC(NC(=O)c2cnn3ccc(N4CCCC4c4cc(F)ccc4F)nc23)CC1"	"IC50"	"'='"	"388.0"	"nM"	"6.41"	""	"258345"	"UO_0000065"	"12.71"	"0.25"	"3.91"	"6.42"	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675931"	""	"0"	"468.53"	"0"	"1.76"	"BDBM127681"	"O=C(NCCN1CCOCC1)c1cnn2ccc(N3CCCC3c3cc(F)ccc3CO)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258355"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675932"	""	"0"	"429.45"	"0"	"0.79"	"BDBM127682"	"O=C(NCC(O)CO)c1cnn2ccc(N3CCCC3c3cc(F)ccc3CO)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258356"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675934"	""	"0"	"414.46"	"0"	"2.82"	"BDBM127685"	"CC(C)(N)CNC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258359"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675982"	""	"0"	"382.40"	"0"	"1.42"	"BDBM127735"	"O=C(c1cnn2ccc(N3CCCC3c3cncc(F)c3)nc12)N1CC(O)C1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258409"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675983"	""	"0"	"384.42"	"0"	"1.72"	"BDBM127736"	"C[C@H](O)CNC(=O)c1cnn2ccc(N3CCCC3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258410"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675985"	""	"0"	"398.44"	"0"	"2.11"	"BDBM127738"	"CC(C)(O)CNC(=O)c1cnn2ccc(N3CCCC3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258412"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676036"	""	"0"	"401.42"	"0"	"2.46"	"BDBM127794"	"C[C@@H](O)CNC(=O)c1cnn2ccc(N3CCCC3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258463"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676044"	""	"0"	"431.44"	"0"	"1.82"	"BDBM127803"	"C[C@H](O)[C@@H](CO)NC(=O)c1cnn2ccc(N3CCCC3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258472"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676051"	""	"0"	"396.47"	"0"	"3.44"	"BDBM127810"	"Cc1ncc(F)cc1[C@H]1CCCN1c1ccn2ncc(C(=O)NC(C)(C)C)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258479"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676054"	""	"0"	"354.39"	"0"	"2.27"	"BDBM127813"	"CNC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)cnc3C)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258482"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676081"	""	"0"	"437.40"	"0"	"2.86"	"BDBM127843"	"CC(NC(=O)c1cnn2ccc(N3CC(O)CC3c3cccc(F)c3)nc12)C(F)(F)F"	"IC50"	"'='"	"670.0"	"nM"	"6.17"	""	"258511"	"UO_0000065"	"14.12"	"0.27"	"3.31"	"7.46"	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676084"	""	"0"	"412.47"	"0"	"2.49"	"BDBM127846"	"CC(C)NC(=O)c1cnn2ccc(N3[C@@H](c4cncc(F)c4)CC[C@@]3(C)CO)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258514"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL2178258"	""	"0"	"384.85"	"0"	"3.65"	"7g"	"Cc1nc(-c2cccc(Cl)c2)c(NC(=O)c2cnn3ccc(N)nc23)s1"	"IC50"	"'='"	"176.0"	"nM"	"6.75"	""	""	"UO_0000065"	"17.55"	"0.35"	"3.10"	"6.88"	"False"	"CHEMBL2186598"	"Inhibition of JAK2 V617F mutant in human SET2 cells assessed as reduction in STAT5 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176876"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL4087076"	""	"0"	"368.44"	"1"	"5.60"	"7"	"CC(C)c1cc(O)ccc1-c1ccc2c(-c3nc4ccccc4[nH]3)n[nH]c2c1"	"IC50"	"'='"	"79.6"	"nM"	"7.10"	""	""	"UO_0000065"	"19.27"	"0.35"	"1.50"	"9.15"	"False"	"CHEMBL4003453"	"Inhibition of GST tagged human recombinant JAK2 catalytic domain expressed in baculovirus using peptide substrate preincubated for 60 mins followed by substrate addition and measured after 60 mins by microfluidic assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4002590"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL2207762"	""	"0"	"498.41"	"1"	"5.56"	"3"	"CC(=O)Nc1ccc(-c2ccnc(NC3CCCC(NC(=O)c4c(Cl)cccc4Cl)C3)n2)cc1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2214785"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT1 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL2208032"	""	"0"	"418.50"	"0"	"3.01"	"10b"	"C[C@@H](N)C(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"1.7"	"nM"	"8.77"	""	""	"UO_0000065"	"20.95"	"0.39"	"5.76"	"8.32"	"False"	"CHEMBL2214787"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL3975430"	""	"0"	"404.40"	"0"	"3.72"	"BDBM228664"	"CN(C(=O)Nc1ccc(C(F)(F)F)cc1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399704"	"UO_0000065"	"22.90"	"0.44"	"5.54"	"12.00"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3942396"	""	"0"	"311.39"	"0"	"1.26"	"BDBM228773"	"C#CCN(C1CCOC1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399709"	"UO_0000065"	"29.74"	"0.55"	"8.00"	"16.17"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3890611"	""	"0"	"353.82"	"0"	"2.59"	"BDBM228779"	"CN(c1ncc(C#N)cc1Cl)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399717"	"UO_0000065"	"26.17"	"0.51"	"6.67"	"10.93"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3939566"	""	"0"	"423.52"	"0"	"3.87"	"BDBM228887"	"CC(C)(C)OC(=O)C1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)CC1"	"IC50"	"'='"	"91.0"	"nM"	"7.04"	""	"400634"	"UO_0000065"	"16.62"	"0.31"	"3.17"	"5.72"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3889509"	""	"0"	"448.50"	"0"	"3.78"	"BDBM228933"	"COc1ccccc1N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CC1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"400680"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3964457"	""	"0"	"454.46"	"0"	"4.05"	"BDBM228937"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(c2ccc(F)c(F)c2)CC1"	"IC50"	"'='"	"70.0"	"nM"	"7.16"	""	"400684"	"UO_0000065"	"15.74"	"0.30"	"3.10"	"7.16"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3949472"	""	"0"	"503.59"	"1"	"2.01"	"BDBM228985"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(S(N)(=O)=O)cc3)n2)CC1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"400730"	"UO_0000065"	"17.87"	"0.35"	"6.99"	"4.83"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL2376152"	""	"0"	"480.89"	"0"	"2.40"	"6i"	"C[C@@H](NC(=O)c1c[nH]c2ncc(-c3nn(C)c4cc(Cl)cc(F)c34)nc12)C(=O)N1CC(C#N)C1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2378509"	"Inhibition of JAK2 in human monocytes expressing CD14 assessed as inhibition of GM-CSF-stimulated STAT5a phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375236"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2178801"	""	"0"	"382.81"	"0"	"3.04"	"14j"	"COc1ccc(Cl)cc1-c1nn(C)cc1NC(=O)c1cnn2cccnc12"	"IC50"	"'='"	"22.4"	"nM"	"7.65"	""	""	"UO_0000065"	"19.98"	"0.39"	"4.61"	"8.86"	"False"	"CHEMBL2186603"	"Inhibition of JAK2 in human TF1 cells assessed as reduction in STAT5 phosphorylation incubated for 30 mins in presence of human recombinant EPO"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176876"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"CHEMBL3307972"	""
"CHEMBL3403540"	""	"0"	"341.80"	"0"	"3.04"	"13"	"CNc1cc(-c2cc(C(N)=O)n(-c3cc(Cl)ccc3C)c2)ncn1"	"IC50"	"'='"	"131.0"	"nM"	"6.88"	""	""	"UO_0000065"	"20.14"	"0.39"	"3.84"	"8.02"	"False"	"CHEMBL3404501"	"Inhibition of recombinant epitope-tagged JAK2 (808 to 1132) (unknown origin) using LPLDKDYYVVREPGQ as substrate by beta-countiing analysis in presence of 33P-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3400063"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3402480"	""	"0"	"327.77"	"0"	"2.58"	"6"	"Cc1ccc(Cl)cc1-c1cn(-c2ccnc(N)n2)cc1C(N)=O"	"IC50"	"'='"	"220.0"	"nM"	"6.66"	""	""	"UO_0000065"	"20.31"	"0.40"	"4.08"	"6.67"	"False"	"CHEMBL3404501"	"Inhibition of recombinant epitope-tagged JAK2 (808 to 1132) (unknown origin) using LPLDKDYYVVREPGQ as substrate by beta-countiing analysis in presence of 33P-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3400063"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3642275"	""	"0"	"449.54"	"0"	"3.38"	"BDBM99538"	"CS(=O)(=O)c1ccc(-c2ccc3nc(Nc4ccc(N5CCOCC5)cc4)nn3c2)cc1"	"IC50"	"'='"	"9999.0"	"nM"	"5.00"	""	"216230"	"UO_0000065"	"11.12"	"0.21"	"1.62"	"5.63"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647885"	""	"0"	"440.94"	"0"	"3.53"	"BDBM147997"	"N#C[C@H]1C[C@@H](C(=O)NC2CCC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"103.0"	"nM"	"6.99"	""	"285932"	"UO_0000065"	"15.85"	"0.31"	"3.46"	"5.55"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642363"	""	"0"	"490.63"	"0"	"4.30"	"BDBM99639"	"CN1CCC(c2ccc(Nc3nc4c(NCc5ccccc5S(C)(=O)=O)cccn4n3)cc2)CC1"	"IC50"	"'='"	"22.59"	"nM"	"7.65"	""	"216329"	"UO_0000065"	"15.58"	"0.30"	"3.35"	"8.34"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3645102"	""	"0"	"431.52"	"0"	"3.98"	"BDBM99876"	"CN1CCN(c2cccc(Nc3nc4c(NCc5ccccc5F)cccn4n3)c2)CC1"	"IC50"	"'='"	"180.36"	"nM"	"6.74"	""	"216544"	"UO_0000065"	"15.63"	"0.29"	"2.76"	"11.10"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3694594"	""	"0"	"456.94"	"1"	"5.23"	"BDBM125915"	"O=C(Nc1ccc2cc1CCc1cncc(c1)Nc1ncc(Cl)c(n1)NC2)c1ccccc1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"255688"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707544"	"In Vitro Kinase Assay: One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Biochemistry 1999, 269, 94-104. The catalytic domains of human JAK1 (a.a. 837-1142), JAK2 (a.a. 828-1132) and JAK3 (a.a. 781-1124) with an N-terminal His tag were expressed using baculovirus in insect cells and purified. The catalytic activity of JAK1, JAK2 or JAK3 was assayed by measuring the phosphorylation of a biotinylated peptide. The phosphorylated peptide was detected by homogenous time resolved fluorescence (HTRF). IC50s of compounds were measured for each kinase in the reactions that contain the enzyme, ATP and 500 nM peptide in 50 mM Tris (pH 7.8) buffer with 100 mM NaCl, 5 mM DTT, and 0.1 mg/mL (0.01%) BSA. The ATP concentration in the reactions was 90 uM for JAK1, 30 uM for JAK2 and 3 uM for JAK3. Reactions were carried out at room temperature for 1 hr and then stopped with 20 uL 45 mM EDTA."	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639093"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3647856"	""	"0"	"423.40"	"0"	"2.55"	"BDBM147966"	"N#C[C@H]1C[C@@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc([C@H](O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"285900"	"UO_0000065"	"20.55"	"0.40"	"6.15"	"6.34"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703085"	""	"0"	"386.89"	"0"	"3.17"	"BDBM147798"	"CN(C)[C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"23.0"	"nM"	"7.64"	""	"285732"	"UO_0000065"	"19.74"	"0.39"	"4.47"	"7.64"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665156"	""	"0"	"373.44"	"0"	"1.25"	"BDBM112549"	"CS(=O)(=O)N1CCC[C@H](Nc2ncccc2-c2cnc3[nH]ncc3n2)C1"	"IC50"	"'='"	"0.8586"	"nM"	"9.07"	""	"233787"	"UO_0000065"	"24.28"	"0.48"	"7.82"	"7.76"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652283"	""	"0"	"409.53"	"0"	"2.72"	"BDBM113092"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCCC(F)C2)CC1"	"IC50"	"'='"	"26.2"	"nM"	"7.58"	""	"234536"	"UO_0000065"	"18.51"	"0.37"	"4.86"	"9.22"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3702998"	""	"0"	"421.43"	"0"	"2.93"	"BDBM147708"	"CN(C)[C@@H]1CC[C@@H](n2cc(C(N)=O)c(Nc3ccc(C(F)(F)F)nc3)n2)[C@H](C#N)C1"	"IC50"	"'='"	"400.0"	"nM"	"6.40"	""	"285642"	"UO_0000065"	"15.18"	"0.29"	"3.47"	"5.67"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665213"	""	"0"	"485.62"	"0"	"1.39"	"BDBM112613"	"CN(C)[C@@H]1CCN(c2ncc(-c3cnc4[nH]ccc4n3)c(N[C@H]3CCCN(S(C)(=O)=O)C3)n2)C1"	"IC50"	"'='"	"0.0708"	"nM"	"10.15"	""	"233850"	"UO_0000065"	"20.90"	"0.41"	"8.76"	"8.24"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3650684"	""	"0"	"457.43"	"0"	"2.24"	"BDBM47171"	"N#C[C@H]1C[C@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"198682"	"UO_0000065"	"18.63"	"0.38"	"6.28"	"5.64"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642294"	""	"0"	"462.58"	"0"	"3.30"	"BDBM99562"	"CN1CCN(c2cccc(Nc3nc4c(-c5cccc(S(C)(=O)=O)c5)cccn4n3)c2)CC1"	"IC50"	"'='"	"6.4"	"nM"	"8.19"	""	"216252"	"UO_0000065"	"17.71"	"0.34"	"4.89"	"9.89"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647825"	""	"0"	"446.48"	"0"	"4.12"	"BDBM147930"	"N#C[C@H]1C[C@H](NC2CCC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"1050.0"	"nM"	"5.98"	""	"285864"	"UO_0000065"	"13.39"	"0.26"	"1.86"	"5.50"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652382"	""	"0"	"381.48"	"0"	"1.94"	"BDBM113194"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC(F)C2)CC1"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	"234637"	"UO_0000065"	"20.18"	"0.40"	"5.76"	"9.37"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3651042"	""	"0"	"366.38"	"0"	"2.53"	"BDBM153219"	"CCOC(=O)c1c[nH]c2ncnc(-c3cccc(NC(=O)C4(C)CO4)c3)c12"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294167"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652409"	""	"0"	"543.63"	"1"	"3.94"	"BDBM113221"	"CCOP(=O)(OCC)O[C@@H]1CCCN(S(=O)(=O)C[C@H]2CC[C@H](N(C)c3ncnc4[nH]ccc34)CC2)C1"	"IC50"	"'='"	"0.116"	"nM"	"9.94"	""	"234664"	"UO_0000065"	"18.28"	"0.38"	"6.00"	"7.83"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3702987"	""	"0"	"490.53"	"0"	"3.68"	"BDBM147697"	"CC(C)(O)C1CN([C@@H]2CC[C@H](n3cc(C(N)=O)c(Nc4ccc(C(F)(F)F)cc4)n3)[C@@H](C#N)C2)C1"	"IC50"	"'='"	"49.0"	"nM"	"7.31"	""	"285631"	"UO_0000065"	"14.90"	"0.29"	"3.63"	"6.08"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3694584"	""	"0"	"352.83"	"0"	"4.42"	"BDBM125905"	"Clc1cnc2nc1NCCc1cccc(c1)OCc1cccc(c1)N2"	"IC50"	"'='"	"333.0"	"nM"	"6.48"	""	"255678"	"UO_0000065"	"18.36"	"0.35"	"2.06"	"10.97"	"False"	"CHEMBL3707544"	"In Vitro Kinase Assay: One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Biochemistry 1999, 269, 94-104. The catalytic domains of human JAK1 (a.a. 837-1142), JAK2 (a.a. 828-1132) and JAK3 (a.a. 781-1124) with an N-terminal His tag were expressed using baculovirus in insect cells and purified. The catalytic activity of JAK1, JAK2 or JAK3 was assayed by measuring the phosphorylation of a biotinylated peptide. The phosphorylated peptide was detected by homogenous time resolved fluorescence (HTRF). IC50s of compounds were measured for each kinase in the reactions that contain the enzyme, ATP and 500 nM peptide in 50 mM Tris (pH 7.8) buffer with 100 mM NaCl, 5 mM DTT, and 0.1 mg/mL (0.01%) BSA. The ATP concentration in the reactions was 90 uM for JAK1, 30 uM for JAK2 and 3 uM for JAK3. Reactions were carried out at room temperature for 1 hr and then stopped with 20 uL 45 mM EDTA."	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639093"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3647849"	""	"0"	"359.82"	"0"	"2.60"	"BDBM147958"	"N#C[C@H]1C[C@@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"285892"	"UO_0000065"	"22.85"	"0.45"	"5.62"	"7.03"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652324"	""	"0"	"490.67"	"0"	"2.86"	"BDBM113134"	"CCN(CC)C(=O)C1CCN(S(=O)(=O)C[C@H]2CC[C@H](N(C)c3ncnc4[nH]ccc34)CC2)CC1"	"IC50"	"'='"	"115.0"	"nM"	"6.94"	""	"234577"	"UO_0000065"	"14.14"	"0.28"	"4.08"	"6.77"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3642373"	""	"0"	"535.67"	"1"	"3.96"	"BDBM99649"	"CN(c1ccccc1CNc1cccn2nc(Nc3ccc(OCCN4CCCC4)cc3)nc12)S(C)(=O)=O"	"IC50"	"'='"	"43.74"	"nM"	"7.36"	""	"216339"	"UO_0000065"	"13.74"	"0.26"	"3.40"	"7.07"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703041"	""	"0"	"392.46"	"0"	"2.48"	"BDBM147751"	"N#C[C@H]1C[C@@H](N2CCC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C=O)cc2)n1"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	"285685"	"UO_0000065"	"19.86"	"0.37"	"5.32"	"6.66"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702990"	""	"0"	"446.48"	"0"	"3.98"	"BDBM147700"	"N#C[C@H]1C[C@@H](NCC2CC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"64.0"	"nM"	"7.19"	""	"285634"	"UO_0000065"	"16.11"	"0.31"	"3.21"	"6.61"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642335"	""	"0"	"464.56"	"0"	"2.09"	"BDBM99607"	"CN1CCN(c2cncc(Nc3nc4cncc(-c5ccc(S(C)(=O)=O)cc5)n4n3)c2)CC1"	"IC50"	"'='"	"927.1"	"nM"	"6.03"	""	"216297"	"UO_0000065"	"12.99"	"0.25"	"3.94"	"5.55"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652400"	""	"0"	"421.57"	"0"	"1.99"	"BDBM113212"	"C[C@@H]1C[C@@H](CS(=O)(=O)N2CCC[C@H](O)C2)CC[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	"234655"	"UO_0000065"	"18.79"	"0.37"	"5.93"	"7.73"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3658113"	""	"0"	"582.67"	"2"	"6.09"	"BDBM148424"	"Cc1ccc(NC(=O)CC(C)C(F)(F)F)cc1N1CCc2nc(Nc3ccc(OCCN4CCCC4)cc3)ncc2C1"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	"286798"	"UO_0000065"	"13.29"	"0.25"	"1.65"	"9.37"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645039"	""	"0"	"559.61"	"1"	"4.61"	"BDBM99806"	"COc1ccc(C(F)(F)F)cc1-c1cccn2nc(Nc3ccc4c(c3)CCN(CCS(C)(=O)=O)CC4)nc12"	"IC50"	"'='"	"12.74"	"nM"	"7.89"	""	"216479"	"UO_0000065"	"14.11"	"0.28"	"3.28"	"8.89"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652292"	""	"0"	"531.65"	"1"	"3.33"	"BDBM113101"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCCC(O)(COc3cccc(F)c3)C2)CC1"	"IC50"	"'='"	"46.8"	"nM"	"7.33"	""	"234545"	"UO_0000065"	"13.79"	"0.27"	"4.00"	"6.56"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3702901"	""	"0"	"350.43"	"0"	"3.25"	"BDBM147600"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C3CC3)nc2)n1"	"IC50"	"'='"	"26.0"	"nM"	"7.58"	""	"285530"	"UO_0000065"	"21.64"	"0.40"	"4.34"	"6.92"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642358"	""	"0"	"501.59"	"1"	"2.28"	"BDBM99634"	"CN(c1ncccc1CNc1cccn2nc(Nc3cccc(S(C)(=O)=O)c3)nc12)S(C)(=O)=O"	"IC50"	"'='"	"77.84"	"nM"	"7.11"	""	"216324"	"UO_0000065"	"14.17"	"0.29"	"4.83"	"5.13"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3651059"	""	"0"	"319.34"	"0"	"4.44"	"BDBM153236"	"COc1ccc(F)cc1-c1c[nH]c2ncnc(-c3ccccc3)c12"	"IC50"	"'='"	"71.0"	"nM"	"7.15"	""	"294184"	"UO_0000065"	"22.39"	"0.41"	"2.71"	"14.07"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3650991"	""	"0"	"384.82"	"0"	"3.97"	"BDBM153166"	"C=C(C)C(=O)Nc1cc(-c2ncnc3[nH]cc(C(=O)OCC)c23)ccc1Cl"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294114"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699502"	""	"0"	"441.44"	"0"	"3.27"	"BDBM147519"	"N#C[C@H]1CCCCC1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	"285449"	"UO_0000065"	"17.60"	"0.35"	"4.50"	"5.94"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3658115"	""	"0"	"636.08"	"2"	"6.10"	"BDBM148431"	"CN1CCN(c2ccc(Nc3ncc4c(n3)CCN(c3cc(NC(=O)c5cccc(C(F)(F)F)c5)ccc3Cl)C4=O)cc2)CC1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"286799"	"UO_0000065"	"12.93"	"0.25"	"2.12"	"8.77"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3675935"	""	"0"	"417.44"	"0"	"3.98"	"BDBM127686"	"CC(C)(C)NC(=O)c1cnn2ccc(N3CC(F)(F)C[C@@H]3c3cccc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258360"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675937"	""	"0"	"444.46"	"0"	"2.78"	"BDBM127688"	"O=C(N[C@@H]1CCNC[C@@H]1F)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'='"	"699.0"	"nM"	"6.16"	""	"258362"	"UO_0000065"	"13.85"	"0.26"	"3.38"	"8.26"	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675953"	""	"0"	"399.43"	"0"	"2.33"	"BDBM127705"	"COCCOc1cc(F)cc([C@H]2CCCN2c2ccn3ncc(C(N)=O)c3n2)c1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258379"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675961"	""	"0"	"454.51"	"0"	"2.02"	"BDBM127713"	"NC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3OCCN3CCOCC3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258387"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675971"	""	"0"	"396.43"	"0"	"2.08"	"BDBM127723"	"COC1CN(C(=O)c2cnn3ccc(N4CCC[C@@H]4c4cncc(F)c4)nc23)C1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258397"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675987"	""	"0"	"394.45"	"0"	"3.13"	"BDBM127740"	"CC(NC(=O)c1cnn2ccc(N3CCCC3c3cncc(F)c3)nc12)C1CC1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258414"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675988"	""	"0"	"340.36"	"0"	"1.96"	"BDBM127741"	"CNC(=O)c1cnn2ccc(N3CCCC3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258415"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676004"	""	"0"	"422.39"	"0"	"3.29"	"BDBM127757"	"C[C@H](NC(=O)c1cnn2ccc(N3CCCC3c3cncc(F)c3)nc12)C(F)(F)F"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258431"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676016"	""	"0"	"399.43"	"0"	"0.98"	"BDBM127769"	"NCCCNC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)c[nH]c3=O)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258443"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676037"	""	"0"	"429.47"	"0"	"3.10"	"BDBM127795"	"CC(C)(CO)CNC(=O)c1cnn2ccc(N3CCCC3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258464"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676059"	""	"0"	"398.44"	"0"	"2.29"	"BDBM127818"	"COCCNC(=O)c1cnn2ccc(N3CCCC3c3cc(F)cnc3C)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258487"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676070"	""	"0"	"495.56"	"0"	"3.63"	"BDBM127831"	"CC1(C)OCC(COc2ccc(F)cc2[C@H]2CCCN2c2ccn3ncc(C(=O)NC4CC4)c3n2)O1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258499"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676079"	""	"0"	"410.45"	"0"	"2.25"	"BDBM127841"	"CC1(NC(=O)c2cnn3ccc(N4[C@H](CO)CC[C@@H]4c4cncc(F)c4)nc23)CC1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258509"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3702949"	""	"0"	"423.40"	"0"	"2.55"	"BDBM147651"	"N#C[C@H]1C[C@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc([C@H](O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"285583"	"UO_0000065"	"20.13"	"0.39"	"5.97"	"6.21"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702937"	""	"0"	"409.37"	"0"	"3.00"	"BDBM147639"	"[C-]#[N+][C@H]1C[C@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(OC(F)(F)F)cc2)n1"	"IC50"	"'='"	"61.0"	"nM"	"7.21"	""	"285571"	"UO_0000065"	"17.62"	"0.34"	"4.21"	"6.76"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3927234"	""	"0"	"568.74"	"1"	"4.45"	"BDBM113086"	"CCC1(NC(=O)OCc2ccccc2)CCCN(S(=O)(=O)CC2CCC(N(C)c3ncnc4[nH]ccc34)CC2)C1"	"IC50"	"'='"	"71.7"	"nM"	"7.14"	""	"234530"	"UO_0000065"	"12.56"	"0.24"	"2.69"	"5.93"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675957"	""	"0"	"356.36"	"0"	"1.20"	"BDBM127709"	"NC(=O)c1cnn2ccc(N3CCCC3c3cc(F)cnc3CO)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258383"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3902802"	""	"0"	"424.48"	"0"	"2.64"	"BDBM127726"	"O=C(NC1CCC(O)CC1)c1cnn2ccc(N3CCC[C@@H]3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258400"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675989"	""	"0"	"384.42"	"0"	"1.72"	"BDBM127742"	"C[C@H](CO)NC(=O)c1cnn2ccc(N3CCCC3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258416"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675991"	""	"0"	"326.33"	"0"	"1.70"	"BDBM127744"	"NC(=O)c1cnn2ccc(N3CCCC3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258418"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676021"	""	"0"	"430.44"	"0"	"0.70"	"BDBM127777"	"COc1ncc(F)cc1[C@H]1CCCN1c1ccn2ncc(C(=O)NC[C@@H](O)CO)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258448"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3671148"	""	"0"	"427.46"	"0"	"3.26"	"BDBM127647"	"O=C(NC1CCOCC1)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'='"	"257.0"	"nM"	"6.59"	""	"258321"	"UO_0000065"	"15.42"	"0.29"	"3.33"	"9.18"	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675919"	""	"0"	"381.41"	"0"	"2.07"	"BDBM127668"	"O=C(NC1CC1)c1cnn2ccc(N3C[C@H](O)C[C@@H]3c3cccc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258342"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL4640981"	""	"0"	"387.42"	"0"	"0.65"	"10"	"O=C(N[C@@]12C[C@@H]1CN(c1nc(Nc3cnn(CCO)c3)ncc1F)C2)C1CC1"	"IC50"	"'='"	"5663.0"	"nM"	"5.25"	""	""	"UO_0000065"	"13.54"	"0.26"	"4.60"	"4.85"	"False"	"CHEMBL4620433"	"Inhibition of human recombinant JAK2 assessed as level of phosphorylation in presence of peptide substrate FITC-KGGEEEEYFELVKK and ATP by mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4619733"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2020"	"None"	""
"CHEMBL4635625"	""	"0"	"407.40"	"0"	"1.69"	"19"	"C[C@@H]1[C@@H]2CN(c3nc(Nc4cnn(C)c4)ncc3F)C[C@]12NC(=O)[C@@H]1CC1(F)F"	"IC50"	"'='"	"652.0"	"nM"	"6.19"	""	""	"UO_0000065"	"15.18"	"0.29"	"4.50"	"7.03"	"False"	"CHEMBL4620433"	"Inhibition of human recombinant JAK2 assessed as level of phosphorylation in presence of peptide substrate FITC-KGGEEEEYFELVKK and ATP by mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4619733"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2020"	"None"	""
"CHEMBL3675978"	""	"0"	"410.45"	"0"	"2.25"	"BDBM127731"	"O=C(N[C@H]1CCC[C@H]1O)c1cnn2ccc(N3CCCC3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258405"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675984"	""	"0"	"384.42"	"0"	"1.72"	"BDBM127737"	"C[C@@H](O)CNC(=O)c1cnn2ccc(N3CCCC3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258411"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676013"	""	"0"	"412.43"	"0"	"1.43"	"BDBM127766"	"COc1ncc(F)cc1[C@H]1CCCN1c1ccn2ncc(C(=O)N3CC(O)C3)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258440"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3955007"	""	"0"	"438.51"	"0"	"2.95"	"BDBM127822"	"Cc1ncc(F)cc1C1CCCN1c1ccn2ncc(C(=O)NC3CCC(O)CC3)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258491"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676065"	""	"0"	"449.53"	"0"	"2.74"	"BDBM127825"	"Cc1ncc(F)cc1C1CCCN1c1ccn2ncc(C(=O)N[C@H]3CN4CCC3CC4)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258494"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3971680"	""	"0"	"452.53"	"0"	"3.20"	"BDBM127826"	"CCc1ncc(F)cc1[C@H]1CCCN1c1ccn2ncc(C(=O)NC3CCC(O)CC3)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258495"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676080"	""	"0"	"398.44"	"0"	"2.10"	"BDBM127842"	"CC(C)NC(=O)c1cnn2ccc(N3[C@H](CO)CC[C@@H]3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258510"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3903416"	""	"0"	"605.45"	"2"	"5.76"	"BDBM230115"	"Cn1c(=O)n(-c2cccc(-c3c(Cl)cc(C(N)=O)c4[nH]c5cc(C(C)(C)O)ccc5c34)c2Cl)c(=O)c2cccc(F)c21"	"IC50"	"'='"	"3700.0"	"nM"	"5.43"	""	"402056"	"UO_0000065"	"8.97"	"0.18"	"-0.33"	"4.41"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3907348"	""	"0"	"554.55"	"1"	"4.89"	"BDBM230149"	"Cc1c(-c2c(F)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)[nH]c2c(F)cccc2c1=O"	"IC50"	"'='"	"1700.0"	"nM"	"5.77"	""	"402033"	"UO_0000065"	"10.40"	"0.19"	"0.88"	"4.31"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3900554"	"BMS-986142"	"2"	"572.61"	"1"	"4.40"	"BDBM230104"	"Cc1c(-c2c(F)cc(C(N)=O)c3[nH]c4c(c23)CC[C@H](C(C)(C)O)C4)cccc1-n1c(=O)c2cccc(F)c2n(C)c1=O"	"IC50"	"'='"	"32000.0"	"nM"	"4.50"	""	"402039"	"UO_0000065"	"7.85"	"0.15"	"0.09"	"3.65"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3917869"	""	"0"	"559.05"	"2"	"5.10"	"BDBM230153"	"Cc1c(-c2c(Cl)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)cc2sccn2c1=O"	"IC50"	"'='"	"370.0"	"nM"	"6.43"	""	"402050"	"UO_0000065"	"11.50"	"0.23"	"1.33"	"5.25"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3642406"	""	"0"	"534.69"	"1"	"3.26"	"BDBM99684"	"CN1CCN(c2ccc(Nc3nc4c(N(C)Cc5ccccc5N(C)S(C)(=O)=O)cccn4n3)cc2)CC1"	"IC50"	"'='"	"51.06"	"nM"	"7.29"	""	"216373"	"UO_0000065"	"13.64"	"0.26"	"4.03"	"8.16"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652346"	""	"0"	"488.54"	"0"	"2.04"	"BDBM113157"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC[C@H](NC(=O)C(F)(F)F)C2)CC1"	"IC50"	"'='"	"62.2"	"nM"	"7.21"	""	"234600"	"UO_0000065"	"14.75"	"0.30"	"5.17"	"6.48"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL1427221"	""	"0"	"297.75"	"0"	"3.47"	"BDBM67818"	"O=C(CCl)Nc1cccc(-c2cnc3ccccc3n2)c1"	"IC50"	"'>'"	"20000.0"	"nM"	""	""	"226354"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL2035045"	""	"0"	"373.46"	"0"	"3.80"	"13e, 95:5 trans/Cis mixture"	"CN1C/C=C/COCc2cncc(c2)-c2ccnc(n2)Nc2cccc(c2)C1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2040119"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2034857"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2035048"	""	"0"	"349.39"	"0"	"4.08"	"13h, 95:5 trans/Cis mixture"	"C1=C/COCc2ccc(o2)-c2ccnc(n2)Nc2cccc(c2)COC/1"	"IC50"	"'='"	"220.0"	"nM"	"6.66"	""	""	"UO_0000065"	"19.05"	"0.35"	"2.58"	"9.59"	"False"	"CHEMBL2040119"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2034857"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL4789273"	""	"0"	"520.64"	"2"	"5.61"	"13al"	"Cc1ccc(C(=O)/C=C/C(=O)N2CCc3ccc(Nc4ncc(C)c(-c5cnn(C(C)C)c5)n4)cc3C2)cc1"	"IC50"	"'='"	"0.9"	"nM"	"9.05"	""	""	""	"17.37"	"0.32"	"3.44"	"9.73"	"False"	"CHEMBL4723820"	"Inhibition of recombinant human JAK2 (808 to end residues) KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate measured after 40 mins in presence of [gamm33P]ATP by scintillation counting method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 0.6667 hr"
"CHEMBL4747449"	""	"0"	"392.51"	"0"	"3.32"	"13d"	"Cc1cnc(Nc2ccc3c(c2)CCN(CCO)C3)nc1-c1cnn(C(C)C)c1"	"IC50"	"'='"	"323.0"	"nM"	"6.49"	""	""	""	"16.54"	"0.31"	"3.17"	"8.21"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL4447631"	""	"0"	"467.59"	"0"	"4.01"	"18e"	"Cc1cnc(Nc2ccc(N3CCC(N(C)CCO)CC3)c(F)c2)nc1-c1cnn(C(C)C)c1"	"IC50"	"'='"	"270.0"	"nM"	"6.57"	""	""	""	"14.05"	"0.26"	"2.56"	"7.98"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL4760064"	""	"0"	"502.02"	"2"	"6.22"	"13g"	"Cc1cnc(Nc2ccc3c(c2)CCN(C(=O)Nc2cccc(Cl)c2)C3)nc1-c1cnn(C(C)C)c1"	"IC50"	"'='"	"3450.0"	"nM"	"5.46"	""	""	""	"10.88"	"0.21"	"-0.76"	"6.21"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL4744889"	""	"0"	"410.50"	"0"	"3.46"	"13k"	"Cc1cnc(Nc2cc3c(cc2F)CN(CCO)CC3)nc1-c1cnn(C(C)C)c1"	"IC50"	"'='"	"4460.0"	"nM"	"5.35"	""	""	""	"13.03"	"0.24"	"1.89"	"6.76"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL4778749"	""	"0"	"396.47"	"0"	"3.15"	"13l"	"CC(C)n1cc(-c2nc(Nc3ccc4c(c3)CCN(CCO)C4)ncc2F)cn1"	"IC50"	"'='"	"651.0"	"nM"	"6.19"	""	""	""	"15.60"	"0.29"	"3.04"	"7.82"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL4776245"	""	"0"	"446.56"	"0"	"4.06"	"13ak"	"COC(=O)/C=C/CN1CCc2ccc(Nc3ncc(C)c(-c4cnn(C(C)C)c4)n3)cc2C1"	"IC50"	"'='"	"72.0"	"nM"	"7.14"	""	""	""	"15.99"	"0.30"	"3.08"	"8.39"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL3646835"	""	"0"	"483.45"	"0"	"4.46"	"BDBM130282"	"NC(=O)c1cc(-c2ccc(OC(F)(F)F)cc2)cc2c1[nH]c1cc(C(=O)N3CCOCC3)ccc12"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"262068"	"UO_0000065"	"17.01"	"0.32"	"3.76"	"8.42"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3952936"	""	"0"	"339.40"	"0"	"1.86"	"BDBM255003"	"N#CCN1CN([C@H]2CC[C@H](CO)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"30.0"	"nM"	"7.52"	""	"443859"	"UO_0000065"	"22.17"	"0.41"	"5.66"	"7.82"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3976846"	""	"0"	"378.48"	"0"	"2.62"	"BDBM255004"	"N#CCNC[C@H]1CC[C@H](N2CN(C3CC3)C(=O)c3cnc4[nH]ccc4c32)CC1"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	"443860"	"UO_0000065"	"20.53"	"0.38"	"5.15"	"8.82"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3647813"	""	"0"	"342.38"	"0"	"2.06"	"BDBM147918"	"N#C[C@H]1C[C@@H](N)CCC1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"35.0"	"nM"	"7.46"	""	"285852"	"UO_0000065"	"21.78"	"0.41"	"5.40"	"6.07"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647740"	""	"0"	"552.50"	"1"	"3.79"	"BDBM147843"	"N#C[C@H]1C[C@H](NCCC(F)(F)F)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"82.0"	"nM"	"7.09"	""	"285777"	"UO_0000065"	"12.83"	"0.26"	"3.30"	"4.96"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3655081"	"ABROCITINIB"	"3"	"323.42"	"0"	"1.25"	"BDBM159748"	"CCCS(=O)(=O)N[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"803.0"	"nM"	"6.09"	""	"302558"	"UO_0000065"	"18.85"	"0.38"	"4.85"	"6.70"	"True"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3330129"	""	"0"	"341.80"	"0"	"3.04"	"32"	"CCc1ccc(Cl)cc1-c1[nH]c(-c2ccnc(N)n2)cc1C(N)=O"	"IC50"	"'='"	"210.0"	"nM"	"6.68"	""	""	"UO_0000065"	"19.54"	"0.38"	"3.64"	"6.03"	"False"	"CHEMBL3374497"	"Inhibition of JAK2 V617F mutant in human SET2 cells"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL2207762"	""	"0"	"498.41"	"1"	"5.56"	"3"	"CC(=O)Nc1ccc(-c2ccnc(NC3CCCC(NC(=O)c4c(Cl)cccc4Cl)C3)n2)cc1"	"IC50"	"'>'"	"980.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2214787"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL4114877"	""	"0"	"426.45"	"0"	"2.80"	"BDBM237767"	"N#C[C@@H]1CN(C(=O)OCC2CC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"414871"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4107499"	""	"0"	"490.54"	"0"	"4.02"	"BDBM237776"	"N#C[C@@H]1CN(C(=O)OCCCc2ccccc2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"414880"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3356117"	""	"0"	"484.98"	"0"	"2.86"	"4"	"CC(=O)c1ccc(N2CCN(C(=O)CN3CC[C@@H](C(=O)Nc4ccc(O)c(Cl)c4)C3)CC2)cc1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3376482"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351461"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL3642388"	""	"0"	"477.59"	"0"	"3.43"	"BDBM99666"	"CN1Cc2ccc(Nc3nc4c(NCc5ccccc5N(C)S(C)(=O)=O)cccn4n3)cc2C1"	"IC50"	"'='"	"9.19"	"nM"	"8.04"	""	"216356"	"UO_0000065"	"16.83"	"0.32"	"4.61"	"8.47"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647763"	""	"0"	"460.50"	"0"	"4.37"	"BDBM147866"	"C[C@H](N[C@@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(C(F)(F)F)cc3)n2)[C@@H](C#N)C1)C1CC1"	"IC50"	"'='"	"270.0"	"nM"	"6.57"	""	"285800"	"UO_0000065"	"14.26"	"0.27"	"2.20"	"6.04"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645026"	""	"0"	"409.50"	"0"	"3.71"	"BDBM99782"	"Cn1ncc2c(-c3cccn4nc(Nc5ccc6c(c5)CCNCC6)nc34)cccc21"	"IC50"	"'='"	"16.54"	"nM"	"7.78"	""	"216465"	"UO_0000065"	"19.00"	"0.34"	"4.07"	"10.80"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3665149"	""	"0"	"426.55"	"0"	"2.94"	"BDBM112539"	"Cc1ccc(-c2cnc3[nH]ccc3n2)c(NC2CCCN(S(=O)(=O)CC3CC3)C2)n1"	"IC50"	"'='"	"0.1669"	"nM"	"9.78"	""	"233778"	"UO_0000065"	"22.92"	"0.45"	"6.84"	"9.41"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3301607"	"FILGOTINIB"	"4"	"425.51"	"0"	"1.98"	"65, GLPG0634"	"O=C(Nc1nc2cccc(-c3ccc(CN4CCS(=O)(=O)CC4)cc3)n2n1)C1CC1"	"IC50"	"'='"	"4546.0"	"nM"	"5.34"	""	""	"UO_0000065"	"12.56"	"0.24"	"3.36"	"5.53"	"False"	"CHEMBL3382732"	"Inhibition of JAK2 in IL3-induced human BaF3 cells assessed as cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351789"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"CHEMBL3307634"	""
"CHEMBL3360840"	""	"0"	"357.44"	"0"	"1.21"	"66"	"Nc1nc2cccc(-c3ccc(CN4CCS(=O)(=O)CC4)cc3)n2n1"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3382736"	"Inhibition of JAK2 in human whole blood assessed as inhibition of GM-CSF-induced pSTAT5"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"CHEMBL3638178"	"Blood"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351789"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL3960656"	""	"0"	"439.52"	"0"	"3.50"	"BDBM229063"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(Cc2cccc(C#N)c2)CC1"	"IC50"	"'='"	"234.0"	"nM"	"6.63"	""	"400799"	"UO_0000065"	"15.09"	"0.27"	"3.13"	"5.36"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL2207760"	""	"0"	"472.59"	"0"	"4.15"	"10h"	"CCN1CCC[C@@H]1C(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"2166.0"	"nM"	"5.66"	""	""	"UO_0000065"	"11.99"	"0.22"	"1.51"	"6.86"	"False"	"CHEMBL2214784"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT3 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL3926399"	""	"0"	"530.63"	"2"	"5.04"	"BDBM229041"	"COc1ccc(-c2cccc(Nc3nn(C4(CC#N)CCN(C(=O)OC(C)(C)C)CC4)cc3C(N)=O)c2)cc1"	"IC50"	"'='"	"958.0"	"nM"	"6.02"	""	"400786"	"UO_0000065"	"11.34"	"0.21"	"0.98"	"4.44"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4106753"	""	"0"	"410.48"	"0"	"3.05"	"BDBM237713"	"CC(C)(C)OC(=O)N1CC[C@H](n2cc(C(N)=O)c(Nc3ccccc3)n2)[C@H](C#N)C1"	"IC50"	"'='"	"1270.0"	"nM"	"5.90"	""	"414816"	"UO_0000065"	"14.36"	"0.27"	"2.85"	"4.67"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3983502"	""	"0"	"410.48"	"0"	"3.05"	"BDBM237913"	"CC(C)(C)OC(=O)N1CC[C@H](n2cc(C(N)=O)c(Nc3ccccc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"496.0"	"nM"	"6.30"	""	"414817"	"UO_0000065"	"15.36"	"0.29"	"3.25"	"4.99"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4109976"	""	"0"	"456.48"	"0"	"2.57"	"BDBM237734"	"N#C[C@@H]1CN(C(=O)OC2CCOCC2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"432.0"	"nM"	"6.37"	""	"414838"	"UO_0000065"	"13.94"	"0.26"	"3.79"	"4.70"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4114118"	""	"0"	"450.42"	"0"	"2.70"	"BDBM237752"	"N#C[C@@H]1CN(C(=O)OC(CF)CF)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"133.0"	"nM"	"6.88"	""	"414856"	"UO_0000065"	"15.27"	"0.29"	"4.18"	"5.45"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4107255"	""	"0"	"456.48"	"0"	"2.42"	"BDBM237766"	"CC1(COC(=O)N2CC[C@H](n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)[C@H](C#N)C2)COC1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"414870"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3934456"	""	"0"	"279.30"	"0"	"2.37"	"BDBM195906"	"C=CC(=O)Nc1cccc(-c2cnc3c(c2)CC(=O)N3)c1"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	"348612"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3887689"	"Biochemical Inhibition Assay: 1H-pyrrolo[2,3-b]pyridine, 1H-pyrazolo[3,4-b]pyridine and 5H-pyrrolo[2,3-b]pyrazine series of compounds exhibited over >100 fold selective against Janus and TEC family of kinases except for the BMX and TXK it had activity of 30 and 45 nM respectively."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886406"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4785050"	""	"0"	"544.67"	"2"	"5.90"	"4"	"Cc1cnc(Nc2ccc(C3CCN(C)CC3)c(F)c2)nc1Nc1ccc(F)c(NS(=O)(=O)C(C)(C)C)c1"	"IC50"	"'='"	"6.5"	"nM"	"8.19"	""	""	""	"15.03"	"0.29"	"2.29"	"8.25"	"False"	"CHEMBL4714135"	"Inhibition of human JAK2 by radiometric assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEK293F"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706688"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	""
"CHEMBL388978"	"STAUROSPORINE"	"0"	"466.54"	"0"	"4.35"	"Staurosporine"	"CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4c(c5c6ccccc6n2c5c31)C(=O)NC4"	"IC50"	"'='"	"0.115"	"nM"	"9.94"	""	""	""	"21.30"	"0.39"	"5.59"	"14.31"	"False"	"CHEMBL4720693"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715818"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL3193058"	""	"0"	"301.20"	"0"	"2.92"	"SID26657548"	"O=C(CCl)/N=c1\sccn1Cc1ccccc1Cl"	"IC50"	"'='"	"1110.0"	"nM"	"5.96"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1326817"	""	"0"	"334.33"	"0"	"0.08"	"SID26730295"	"COc1ccccc1C(C[N+](=O)[O-])c1c(N)n(C)c(=O)n(C)c1=O"	"IC50"	"'='"	"6492.0"	"nM"	"5.19"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL3984764"	""	"0"	"345.41"	"0"	"2.47"	"BDBM228710"	"N#Cc1ccc(N(C2CC2)[C@@H]2CCN(c3ncnc4[nH]ccc34)C2)nc1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399627"	"UO_0000065"	"29.70"	"0.54"	"7.79"	"12.11"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3925605"	""	"0"	"312.35"	"0"	"2.21"	"BDBM228718"	"CN(c1ccc(F)cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399637"	"UO_0000065"	"32.85"	"0.61"	"8.05"	"16.84"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3921320"	""	"0"	"397.28"	"0"	"3.31"	"BDBM228734"	"CN(c1ccc(C#N)c(Br)c1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399656"	"UO_0000065"	"25.82"	"0.56"	"6.95"	"14.28"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3959909"	""	"0"	"343.39"	"0"	"1.94"	"BDBM228682"	"C#CCN(c1ccc(C#N)cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399663"	"UO_0000065"	"29.88"	"0.54"	"8.32"	"12.11"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3942728"	""	"0"	"380.46"	"0"	"1.30"	"BDBM228738"	"CN(c1cnc(N2CCOCC2)cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399666"	"UO_0000065"	"26.97"	"0.50"	"8.96"	"11.89"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3675956"	""	"0"	"430.46"	"0"	"2.58"	"BDBM127708"	"CC(C)(CF)NC(=O)c1cnn2ccc(N3CCCC3c3cc(F)cnc3CO)nc12"	"IC50"	"'='"	"666.0"	"nM"	"6.18"	""	"258382"	"UO_0000065"	"14.35"	"0.27"	"3.60"	"6.46"	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675969"	""	"0"	"380.43"	"0"	"2.84"	"BDBM127721"	"O=C(c1cnn2ccc(N3CCC[C@@H]3c3cncc(F)c3)nc12)N1CCCC1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258395"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676090"	""	"0"	"396.43"	"0"	"1.80"	"BDBM127855"	"Cn1cc(F)cc([C@H]2CCCN2c2ccn3ncc(C(=O)NC4CC4)c3n2)c1=O"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258520"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676098"	""	"0"	"424.48"	"0"	"2.44"	"BDBM127863"	"C[C@H](NC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)cn(C)c3=O)nc12)C1CC1"	"IC50"	"'='"	"419.0"	"nM"	"6.38"	""	"258528"	"UO_0000065"	"15.02"	"0.28"	"3.94"	"7.54"	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676101"	""	"0"	"451.44"	"0"	"2.70"	"BDBM127866"	"Cn1cc(F)cc([C@H]2CCCN2c2ccn3ncc(C(=O)Nc4ccc(F)cn4)c3n2)c1=O"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258531"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3746074"	""	"0"	"389.86"	"0"	"3.84"	"26"	"COc1ccc(-c2nc3c(NCC4CCNCC4)c(Cl)cnc3[nH]2)c(F)c1"	"IC50"	"'='"	"11800.0"	"nM"	"4.93"	""	""	"UO_0000065"	"12.64"	"0.25"	"1.09"	"6.58"	"False"	"CHEMBL3751000"	"Inhibition of N-terminal GST-fused recombinant JAK2 (831 to 1132 residues) (unknown origin) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate by microfluidic capillary electrophoresis method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3745697"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL2178257"	""	"0"	"354.76"	"0"	"2.87"	"7f"	"Nc1ccn2ncc(C(=O)Nc3conc3-c3cccc(Cl)c3)c2n1"	"IC50"	"'='"	"158.0"	"nM"	"6.80"	""	""	"UO_0000065"	"19.17"	"0.37"	"3.93"	"6.11"	"False"	"CHEMBL2186598"	"Inhibition of JAK2 V617F mutant in human SET2 cells assessed as reduction in STAT5 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176876"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2178248"	""	"0"	"349.78"	"0"	"3.70"	"10a"	"O=C(Nc1cccnc1-c1cccc(Cl)c1)c1cnn2cccnc12"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL2186598"	"Inhibition of JAK2 V617F mutant in human SET2 cells assessed as reduction in STAT5 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176876"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2178249"	""	"0"	"349.78"	"0"	"3.70"	"10b"	"O=C(Nc1ccncc1-c1cccc(Cl)c1)c1cnn2cccnc12"	"IC50"	"'='"	"250.0"	"nM"	"6.60"	""	""	"UO_0000065"	"18.87"	"0.36"	"2.90"	"9.15"	"False"	"CHEMBL2186598"	"Inhibition of JAK2 V617F mutant in human SET2 cells assessed as reduction in STAT5 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176876"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL3646841"	""	"0"	"459.48"	"0"	"3.85"	"BDBM130290"	"COc1ccc(-c2cc(C(N)=O)c3[nH]c4ccc(C(=O)N5C[C@@H]6C[C@H]5CO6)cc4c3c2)cc1F"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"262076"	"UO_0000065"	"19.59"	"0.36"	"5.15"	"9.22"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649615"	""	"0"	"420.44"	"0"	"3.47"	"BDBM130309"	"COc1ccc(-c2cc(C(N)=O)c3[nH]c4cc(N5CCOCC5)ccc4c3n2)cc1F"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"262095"	"UO_0000065"	"21.41"	"0.40"	"5.53"	"9.63"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649638"	""	"0"	"400.44"	"0"	"2.95"	"BDBM130332"	"NC(=O)c1nc(-c2ccccc2)cc2c1[nH]c1cc(C(=O)N3CCOCC3)ccc12"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	"262118"	"UO_0000065"	"19.87"	"0.36"	"5.01"	"7.86"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL261386"	""	"0"	"363.78"	"1"	"5.02"	"1"	"O=c1[nH]ccc2c3[nH]c(-c4ccccc4Cl)nc3c3ccc(F)cc3c12"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"23.43"	"0.45"	"3.50"	"13.85"	"False"	"CHEMBL1840115"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835019"	""	"0"	"300.34"	"0"	"3.02"	"22"	"CC(C)CNc1ncc(C(N)=O)c2[nH]c3ccc(F)cc3c12"	"IC50"	"'='"	"74.0"	"nM"	"7.13"	""	""	"UO_0000065"	"23.74"	"0.44"	"4.11"	"8.51"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835022"	""	"0"	"298.32"	"0"	"2.92"	"25"	"NC(=O)c1cnc(NC2CCC2)c2c1[nH]c1ccc(F)cc12"	"IC50"	"'='"	"83.0"	"nM"	"7.08"	""	""	"UO_0000065"	"23.74"	"0.44"	"4.16"	"8.45"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835032"	""	"0"	"342.83"	"0"	"4.21"	"35"	"NC(=O)c1cnc(NC2CCCCC2)c2c1[nH]c1cccc(Cl)c12"	"IC50"	"'='"	"110.0"	"nM"	"6.96"	""	""	"UO_0000065"	"20.30"	"0.40"	"2.75"	"8.30"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835037"	""	"0"	"373.46"	"0"	"4.55"	"40"	"NC(=O)c1ccc(NC2CCCCC2)c2c1[nH]c1cc(-c3cn[nH]c3)ccc12"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	""	"UO_0000065"	"21.12"	"0.38"	"3.34"	"7.92"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1833986"	""	"0"	"413.49"	"0"	"3.45"	"60"	"NC(=O)c1cnc(NC(C2CC2)C2CC2)c2c1[nH]c1cc(-c3cnc(N)nc3)ccc12"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	""	"UO_0000065"	"21.77"	"0.40"	"5.55"	"6.64"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835153"	""	"0"	"441.42"	"0"	"3.61"	"65"	"NC(=O)c1cnc(N[C@H](C2CC2)C(F)(F)F)c2c1[nH]c1cc(-c3cnc(N)nc3)ccc12"	"IC50"	"'='"	"25.0"	"nM"	"7.60"	""	""	"UO_0000065"	"17.22"	"0.32"	"3.99"	"5.61"	"False"	"CHEMBL1840130"	"Inhibition of JAK2-mediated STAT5 phosphorylation in human HEL 92.1.7 irf1-bla cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308090"	""
"CHEMBL3646830"	""	"0"	"431.49"	"1"	"5.44"	"BDBM130276"	"COc1cccc(-c2cc(C(N)=O)c3[nH]c4cc(NC(=O)OC(C)(C)C)ccc4c3c2)c1"	"IC50"	"'='"	"160.0"	"nM"	"6.80"	""	"262062"	"UO_0000065"	"15.75"	"0.29"	"1.36"	"6.38"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3745960"	""	"0"	"372.86"	"0"	"3.67"	"16"	"COc1ccc(-c2nc3c(OCC4CCNCC4)c(Cl)cnc3[nH]2)cc1"	"IC50"	"'='"	"10100.0"	"nM"	"5.00"	""	""	"UO_0000065"	"13.40"	"0.26"	"1.33"	"6.93"	"False"	"CHEMBL3751000"	"Inhibition of N-terminal GST-fused recombinant JAK2 (831 to 1132 residues) (unknown origin) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate by microfluidic capillary electrophoresis method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3745697"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3745993"	""	"0"	"403.89"	"0"	"4.18"	"9"	"COc1ccc(F)c(-c2nc3c(NCC4CCN(C)CC4)c(Cl)cnc3[nH]2)c1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3751000"	"Inhibition of N-terminal GST-fused recombinant JAK2 (831 to 1132 residues) (unknown origin) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate by microfluidic capillary electrophoresis method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3745697"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL2208026"	""	"0"	"389.46"	"0"	"3.68"	"9a"	"CC(=O)Nc1ccc(-c2cc(Nc3ccc(N4CCOCC4)cc3)ncn2)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL2214784"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT3 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL2208034"	""	"0"	"444.54"	"0"	"3.41"	"10d, XL019"	"O=C(Nc1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1)[C@H]1CCCN1"	"IC50"	"'='"	"386.4"	"nM"	"6.41"	""	""	"UO_0000065"	"14.43"	"0.27"	"3.00"	"7.02"	"False"	"CHEMBL2214785"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT1 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL2208031"	""	"0"	"418.50"	"0"	"3.01"	"10a"	"C[C@H](N)C(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"1052.5"	"nM"	"5.98"	""	""	"UO_0000065"	"14.28"	"0.26"	"2.97"	"5.67"	"False"	"CHEMBL2214785"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT1 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL2208030"	""	"0"	"403.49"	"0"	"3.99"	"9e"	"CC(=O)Nc1ccc(-c2cc(C)nc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2214785"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT1 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL2208025"	""	"0"	"389.46"	"0"	"3.68"	"7b"	"CC(=O)Nc1ccc(-c2ccnc(Nc3cccc(N4CCOCC4)c3)n2)cc1"	"IC50"	"'='"	"615.0"	"nM"	"6.21"	""	""	"UO_0000065"	"15.95"	"0.29"	"2.53"	"7.82"	"False"	"CHEMBL2214785"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT1 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL2208023"	""	"0"	"304.35"	"0"	"3.85"	"6c"	"CC(=O)Nc1ccc(-c2ccnc(Nc3ccccc3)n2)cc1"	"IC50"	"'='"	"1004.3"	"nM"	"6.00"	""	""	"UO_0000065"	"19.71"	"0.36"	"2.15"	"8.96"	"False"	"CHEMBL2214785"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT1 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL2207758"	""	"0"	"444.54"	"0"	"3.27"	"10f"	"O=C(Nc1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1)[C@H]1CCNC1"	"IC50"	"'='"	"5.7"	"nM"	"8.24"	""	""	"UO_0000065"	"18.55"	"0.34"	"4.97"	"9.02"	"False"	"CHEMBL2214787"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL1835017"	""	"0"	"300.34"	"0"	"3.17"	"20"	"CCCCNc1ncc(C(N)=O)c2[nH]c3ccc(F)cc3c12"	"IC50"	"'='"	"49.0"	"nM"	"7.31"	""	""	"UO_0000065"	"24.34"	"0.45"	"4.14"	"8.72"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835018"	""	"0"	"286.31"	"0"	"2.77"	"21"	"CC(C)Nc1ncc(C(N)=O)c2[nH]c3ccc(F)cc3c12"	"IC50"	"'='"	"100.0"	"nM"	"7.00"	""	""	"UO_0000065"	"24.45"	"0.46"	"4.23"	"8.35"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835152"	""	"0"	"559.57"	"1"	"3.26"	"64"	"NC(=O)c1cnc(N[C@H](C2CC2)C(F)(F)F)c2c1[nH]c1cc(-c3ccc(N4CCS(=O)(=O)CC4)nn3)ccc12"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	""	"UO_0000065"	"15.55"	"0.30"	"5.44"	"5.92"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL3908325"	""	"0"	"467.55"	"0"	"2.58"	"BDBM229444"	"CC(=O)N1CCN(C2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)CC2)CC1"	"IC50"	"'='"	"225.0"	"nM"	"6.65"	""	"401205"	"UO_0000065"	"14.22"	"0.27"	"4.07"	"5.53"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3892599"	""	"0"	"528.59"	"1"	"4.39"	"BDBM229456"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)F)cc3)n2)CCC(Nc2ccccc2)CC1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"401216"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3953754"	""	"0"	"439.42"	"0"	"2.96"	"BDBM229461"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(NCC(F)(F)F)CC1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"401221"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3922069"	""	"0"	"600.58"	"1"	"3.83"	"BDBM229385"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)(F)F)cc3)n2)CCN(C(=O)Nc2ccc(C#N)cc2)CC1"	"IC50"	"'='"	"0.5"	"nM"	"9.30"	""	"401124"	"UO_0000065"	"15.49"	"0.30"	"5.47"	"4.97"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3938031"	""	"0"	"528.59"	"1"	"4.43"	"BDBM229404"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc([S+]([O-])C(F)F)cc3)n2)CCC(Nc2cccc(O)c2)CC1"	"IC50"	"'='"	"65.0"	"nM"	"7.19"	""	"401143"	"UO_0000065"	"13.60"	"0.27"	"2.76"	"4.92"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3954866"	""	"0"	"528.59"	"1"	"4.43"	"BDBM229417"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc([S+]([O-])C(F)F)cc3)n2)CCC(Nc2ccccc2O)CC1"	"IC50"	"'='"	"177.0"	"nM"	"6.75"	""	"401161"	"UO_0000065"	"12.77"	"0.25"	"2.32"	"4.62"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3234881"	""	"0"	"327.38"	"0"	"4.10"	"16"	"Cc1cccc(Nc2sc(-c3ccc(F)cc3)cc2C(N)=O)n1"	"IC50"	"'='"	"140.0"	"nM"	"6.85"	""	""	"UO_0000065"	"20.94"	"0.41"	"2.75"	"10.08"	"False"	"CHEMBL3239499"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3232939"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3904265"	""	"0"	"469.47"	"0"	"4.20"	"BDBM229418"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(Nc2ccc(F)cc2F)CC1"	"IC50"	"'='"	"0.8"	"nM"	"9.10"	""	"401162"	"UO_0000065"	"19.38"	"0.37"	"4.90"	"7.48"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3892671"	""	"0"	"423.45"	"0"	"2.76"	"BDBM229134"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(Cc2ccon2)CC1"	"IC50"	"'='"	"34.0"	"nM"	"7.47"	""	"400870"	"UO_0000065"	"17.64"	"0.33"	"4.71"	"5.93"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3959656"	""	"0"	"463.52"	"0"	"3.17"	"BDBM229152"	"COc1cccc(CN2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccnc(F)c4)n3)CC2)c1"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	"400888"	"UO_0000065"	"16.61"	"0.31"	"4.53"	"6.31"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3905008"	""	"0"	"450.48"	"0"	"2.27"	"BDBM229157"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2ccc(O)nc2)CC1"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	"400893"	"UO_0000065"	"17.97"	"0.34"	"5.83"	"5.55"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3956545"	""	"0"	"458.49"	"0"	"2.48"	"BDBM229173"	"CC(C)(CO)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CC1"	"IC50"	"'='"	"96.0"	"nM"	"7.02"	""	"400909"	"UO_0000065"	"15.31"	"0.29"	"4.54"	"4.79"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3969749"	""	"0"	"442.45"	"0"	"2.10"	"BDBM229191"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(C(=O)OC2COC2)CC1"	"IC50"	"'='"	"44.0"	"nM"	"7.36"	""	"400928"	"UO_0000065"	"16.63"	"0.31"	"5.26"	"5.43"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3974659"	""	"0"	"486.55"	"0"	"2.13"	"BDBM229245"	"CS(=O)(=O)c1ccc(Nc2nn(C3(CC#N)CN(C(=O)OC4CCCC4)C3)cc2C(N)=O)cc1"	"IC50"	"'='"	"132.0"	"nM"	"6.88"	""	"400984"	"UO_0000065"	"14.14"	"0.28"	"4.75"	"4.29"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3969943"	""	"0"	"380.45"	"0"	"2.37"	"BDBM229252"	"CCC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)CC1"	"IC50"	"'='"	"26.0"	"nM"	"7.58"	""	"400991"	"UO_0000065"	"19.94"	"0.37"	"5.22"	"6.48"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3891937"	""	"0"	"438.53"	"0"	"3.61"	"BDBM228878"	"C[C@H]1CN(C(=O)OC(C)(C)C)CC[C@]1(CC#N)n1cc(C(N)=O)c(Nc2ccccc2)n1"	"IC50"	"'='"	"21.0"	"nM"	"7.68"	""	"400625"	"UO_0000065"	"17.51"	"0.33"	"4.07"	"6.08"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4113838"	""	"0"	"440.47"	"0"	"2.75"	"BDBM229355"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CN(C(=O)Nc2ccc(C#N)cc2)C1"	"IC50"	"'='"	"21.0"	"nM"	"7.68"	""	"401094"	"UO_0000065"	"17.43"	"0.32"	"4.93"	"5.02"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4110088"	""	"0"	"443.51"	"0"	"3.50"	"BDBM229371"	"Cc1cccc(C)c1NC(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"656.0"	"nM"	"6.18"	""	"401110"	"UO_0000065"	"13.94"	"0.26"	"2.68"	"4.79"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3931206"	""	"0"	"472.53"	"0"	"3.65"	"BDBM229142"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(Cc2ccnc3[nH]ccc23)CC1"	"IC50"	"'='"	"87.0"	"nM"	"7.06"	""	"400878"	"UO_0000065"	"14.94"	"0.28"	"3.41"	"5.49"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3909449"	""	"0"	"471.54"	"0"	"4.25"	"BDBM229146"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(Cc2cccc3[nH]ccc23)CC1"	"IC50"	"'='"	"280.0"	"nM"	"6.55"	""	"400882"	"UO_0000065"	"13.90"	"0.26"	"2.30"	"5.66"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3901593"	""	"0"	"458.50"	"0"	"3.04"	"BDBM229158"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2ccc(C#N)cc2)CC1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"400894"	"UO_0000065"	"17.55"	"0.32"	"5.01"	"5.89"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3953266"	""	"0"	"454.51"	"0"	"3.51"	"BDBM229178"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(C(=O)OCC2CCC2)CC1"	"IC50"	"'='"	"120.0"	"nM"	"6.92"	""	"400915"	"UO_0000065"	"15.23"	"0.29"	"3.41"	"5.48"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3897977"	""	"0"	"481.96"	"0"	"4.25"	"BDBM229484"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(NCc2ccccc2Cl)CC1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"401247"	"UO_0000065"	"18.05"	"0.35"	"4.45"	"7.15"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3982523"	""	"0"	"504.59"	"1"	"4.94"	"BDBM229282"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)c2ccccc2-c2ccccc2)CC1"	"IC50"	"'='"	"1481.0"	"nM"	"5.83"	""	"401021"	"UO_0000065"	"11.55"	"0.21"	"0.89"	"4.98"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3898103"	""	"0"	"526.65"	"1"	"3.02"	"BDBM229287"	"CN1CCN(c2ccc(C(=O)N3CCC(CC#N)(n4cc(C(N)=O)c(Nc5ccccc5)n4)CC3)cc2)CC1"	"IC50"	"'='"	"830.0"	"nM"	"6.08"	""	"401026"	"UO_0000065"	"11.55"	"0.21"	"3.06"	"4.92"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3920186"	""	"0"	"435.41"	"0"	"2.15"	"BDBM229293"	"CC(F)(F)C(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CC1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"401032"	"UO_0000065"	"19.98"	"0.38"	"6.55"	"6.70"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3907611"	""	"0"	"463.46"	"0"	"2.44"	"BDBM229294"	"CC(CF)(CF)C(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CC1"	"IC50"	"'='"	"48.0"	"nM"	"7.32"	""	"401033"	"UO_0000065"	"15.79"	"0.30"	"4.88"	"5.63"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3933409"	""	"0"	"410.41"	"0"	"1.40"	"BDBM229302"	"N#CCC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CC1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"401041"	"UO_0000065"	"19.60"	"0.37"	"6.65"	"5.23"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3982364"	""	"0"	"479.44"	"0"	"2.83"	"BDBM229309"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(C(=O)C2(C(F)(F)F)CC2)CC1"	"IC50"	"'='"	"40.0"	"nM"	"7.40"	""	"401048"	"UO_0000065"	"15.43"	"0.30"	"4.57"	"5.69"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3985654"	""	"0"	"430.53"	"0"	"2.17"	"BDBM229321"	"CC(C)S(=O)(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)CC1"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	"401060"	"UO_0000065"	"18.32"	"0.36"	"5.72"	"5.88"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4111876"	""	"0"	"433.45"	"0"	"3.02"	"BDBM229341"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CN(C(=O)Nc2cccc(F)c2)C1"	"IC50"	"'='"	"68.0"	"nM"	"7.17"	""	"401080"	"UO_0000065"	"16.54"	"0.31"	"4.15"	"5.55"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3981696"	""	"0"	"395.47"	"0"	"2.16"	"BDBM229345"	"CCCCNC(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"214.0"	"nM"	"6.67"	""	"401084"	"UO_0000065"	"16.86"	"0.31"	"4.51"	"5.17"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4466059"	""	"0"	"393.88"	"0"	"3.10"	"8i"	"O=C(CCCCCCn1cc(Nc2ncc(Cl)c(NC3CC3)n2)cn1)NO"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	""	"UO_0000065"	"21.08"	"0.42"	"5.20"	"7.10"	"False"	"CHEMBL4347596"	"Inhibition of recombinant human JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate measured after 60 mins by LANCE assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4346670"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL2414550"	""	"0"	"343.43"	"0"	"4.97"	"20"	"Cc1ccnc(Nc2nc3cccc(-c4cccc(C(C)C)c4)n3n2)c1"	"IC50"	"'='"	"1400.0"	"nM"	"5.85"	""	""	"UO_0000065"	"17.05"	"0.31"	"0.88"	"10.62"	"False"	"CHEMBL2415128"	"Inhibition of JAK2 in human SET2 cells assessed as reduction of phosphorylated STAT5 level"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2412966"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2414545"	""	"0"	"462.58"	"0"	"3.30"	"10"	"CN1CCN(c2ccc(Nc3nc4cccc(-c5cccc(S(C)(=O)=O)c5)n4n3)cc2)CC1"	"IC50"	"'='"	"73.1"	"nM"	"7.14"	""	""	"UO_0000065"	"15.43"	"0.30"	"3.84"	"8.61"	"False"	"CHEMBL2415128"	"Inhibition of JAK2 in human SET2 cells assessed as reduction of phosphorylated STAT5 level"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2412966"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL3942660"	""	"0"	"514.63"	"2"	"5.34"	"BDBM229044"	"Cc1ccccc1-c1cccc(Nc2nn(C3(CC#N)CCN(C(=O)OC(C)(C)C)CC3)cc2C(N)=O)c1"	"IC50"	"'='"	"1481.0"	"nM"	"5.83"	""	"400789"	"UO_0000065"	"11.33"	"0.21"	"0.49"	"4.62"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3961250"	""	"0"	"516.60"	"1"	"4.74"	"BDBM229048"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3cccc(-c4ccccc4O)c3)n2)CC1"	"IC50"	"'='"	"182.0"	"nM"	"6.74"	""	"400793"	"UO_0000065"	"13.05"	"0.24"	"2.00"	"4.60"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3932767"	""	"0"	"466.95"	"1"	"5.18"	"BDBM229426"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(Nc2cccc(Cl)c2)CC1"	"IC50"	"'='"	"60.0"	"nM"	"7.22"	""	"401175"	"UO_0000065"	"15.47"	"0.30"	"2.04"	"6.64"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3947052"	""	"0"	"451.48"	"0"	"4.06"	"BDBM228224"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(Nc2ccc(F)cc2)CC1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"401176"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3901464"	""	"0"	"461.55"	"0"	"3.63"	"BDBM228231"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(N2CCC3C=CC=CC32)CC1"	"IC50"	"'='"	"24.0"	"nM"	"7.62"	""	"401183"	"UO_0000065"	"16.51"	"0.31"	"3.99"	"6.75"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3986677"	""	"0"	"440.52"	"0"	"2.12"	"BDBM229431"	"N#CCC1(C2C=C(C(N)=O)C(Nc3ccnc(F)c3)=N2)CCC(N2CCC(O)CC2)CC1"	"IC50"	"'='"	"159.0"	"nM"	"6.80"	""	"401185"	"UO_0000065"	"15.43"	"0.29"	"4.68"	"5.33"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3893735"	""	"0"	"467.94"	"0"	"4.58"	"BDBM228239"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(Nc2cccc(Cl)c2)CC1"	"IC50"	"'='"	"832.0"	"nM"	"6.08"	""	"401191"	"UO_0000065"	"12.99"	"0.25"	"1.50"	"5.00"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3947540"	""	"0"	"534.51"	"1"	"3.43"	"BDBM229453"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)F)cc3)n2)CCC(NCC(F)(F)F)CC1"	"IC50"	"'='"	"0.2"	"nM"	"9.70"	""	"401213"	"UO_0000065"	"18.15"	"0.37"	"6.27"	"6.79"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3980737"	""	"0"	"415.45"	"0"	"2.46"	"BDBM228281"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(N2CC(F)C2)CC1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	"401232"	"UO_0000065"	"19.16"	"0.36"	"5.50"	"7.05"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3915313"	""	"0"	"483.50"	"0"	"3.88"	"BDBM229474"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(NCc2ccc(F)cc2F)CC1"	"IC50"	"'='"	"218.0"	"nM"	"6.66"	""	"401236"	"UO_0000065"	"13.78"	"0.26"	"2.78"	"5.48"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3932209"	""	"0"	"443.51"	"0"	"3.44"	"BDBM229379"	"CCc1ccccc1NC(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"303.0"	"nM"	"6.52"	""	"401118"	"UO_0000065"	"14.70"	"0.27"	"3.08"	"5.05"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3967309"	""	"0"	"467.94"	"0"	"3.82"	"BDBM229150"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2cccc(Cl)c2)CC1"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	"400886"	"UO_0000065"	"17.10"	"0.33"	"4.18"	"7.09"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3899546"	""	"0"	"458.50"	"0"	"3.04"	"BDBM229151"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2cccc(C#N)c2)CC1"	"IC50"	"'='"	"33.0"	"nM"	"7.48"	""	"400887"	"UO_0000065"	"16.32"	"0.30"	"4.44"	"5.47"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4110226"	""	"0"	"482.44"	"0"	"3.66"	"BDBM229187"	"C[C@@H](OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CC1)C(F)(F)F"	"IC50"	"'='"	"30.0"	"nM"	"7.52"	""	"400924"	"UO_0000065"	"15.59"	"0.30"	"3.86"	"5.96"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3961164"	""	"0"	"436.52"	"0"	"3.51"	"BDBM229203"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)OC2CCCC2)CC1"	"IC50"	"'='"	"50.0"	"nM"	"7.30"	""	"400940"	"UO_0000065"	"16.73"	"0.31"	"3.79"	"5.78"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3962407"	""	"0"	"438.49"	"0"	"2.36"	"BDBM229209"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)OC2CCOC2)CC1"	"IC50"	"'='"	"40.0"	"nM"	"7.40"	""	"400946"	"UO_0000065"	"16.87"	"0.32"	"5.04"	"5.46"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3922412"	""	"0"	"481.56"	"0"	"1.90"	"BDBM229214"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)OCCN2CCOCC2)CC1"	"IC50"	"'='"	"336.0"	"nM"	"6.47"	""	"400951"	"UO_0000065"	"13.44"	"0.25"	"4.57"	"4.67"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4115395"	""	"0"	"453.50"	"0"	"1.12"	"BDBM229226"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CN(C(=O)OCCN2CCOCC2)C1"	"IC50"	"'='"	"491.0"	"nM"	"6.31"	""	"400965"	"UO_0000065"	"13.91"	"0.26"	"5.19"	"4.55"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4110427"	""	"0"	"451.53"	"0"	"2.13"	"BDBM229244"	"CN1CCC(COC(=O)N2CC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)C2)CC1"	"IC50"	"'='"	"1481.0"	"nM"	"5.83"	""	"400983"	"UO_0000065"	"12.91"	"0.24"	"3.70"	"4.50"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4111724"	""	"0"	"455.49"	"0"	"2.90"	"BDBM229249"	"C[C@@H](OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CC1)C1CC1"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	"400988"	"UO_0000065"	"17.39"	"0.33"	"5.02"	"5.69"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3921761"	""	"0"	"429.48"	"0"	"2.67"	"BDBM229261"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)c2cccnc2)CC1"	"IC50"	"'='"	"191.0"	"nM"	"6.72"	""	"401000"	"UO_0000065"	"15.64"	"0.29"	"4.05"	"5.17"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3896472"	""	"0"	"451.47"	"0"	"1.39"	"BDBM229305"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(C(=O)Cn2ccnc2)CC1"	"IC50"	"'='"	"154.0"	"nM"	"6.81"	""	"401044"	"UO_0000065"	"15.09"	"0.28"	"5.42"	"4.61"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3908689"	""	"0"	"532.55"	"1"	"3.84"	"BDBM229333"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(S(=O)(=O)c2ccc(C(F)(F)F)cc2)CC1"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	"401072"	"UO_0000065"	"15.20"	"0.30"	"4.26"	"6.04"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3899765"	""	"0"	"540.65"	"1"	"4.49"	"BDBM229334"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(S(=O)(=O)c2ccc(-c3ccccc3)cc2)CC1"	"IC50"	"'='"	"24.0"	"nM"	"7.62"	""	"401073"	"UO_0000065"	"14.09"	"0.27"	"3.13"	"5.68"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3903172"	""	"0"	"428.52"	"0"	"1.92"	"BDBM229335"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(S(=O)(=O)C2CC2)CC1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"401074"	"UO_0000065"	"19.89"	"0.39"	"6.60"	"6.36"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4107433"	""	"0"	"418.40"	"0"	"2.36"	"BDBM237779"	"N#C[C@@H]1CN(C(=O)OCCF)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"1124.0"	"nM"	"5.95"	""	"414883"	"UO_0000065"	"14.22"	"0.27"	"3.59"	"4.71"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4113584"	""	"0"	"454.38"	"0"	"2.95"	"BDBM237787"	"N#C[C@@H]1CN(C(=O)OCC(F)(F)F)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"994.0"	"nM"	"6.00"	""	"414891"	"UO_0000065"	"13.21"	"0.26"	"3.05"	"4.75"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3910184"	""	"0"	"428.47"	"0"	"3.04"	"BDBM237798"	"CC(C)COC(=O)N1CC[C@@H](C#N)[C@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)C1"	"IC50"	"'='"	"76.0"	"nM"	"7.12"	""	"414902"	"UO_0000065"	"16.62"	"0.31"	"4.08"	"5.64"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4113261"	""	"0"	"428.47"	"0"	"3.19"	"BDBM237715"	"CC(C)(C)OC(=O)N1CC[C@H](C#N)[C@@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)C1"	"IC50"	"'='"	"39.0"	"nM"	"7.41"	""	"414819"	"UO_0000065"	"17.29"	"0.33"	"4.22"	"5.87"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4108307"	""	"0"	"428.42"	"0"	"1.79"	"BDBM237726"	"N#C[C@@H]1CN(C(=O)OC2COC2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"185.0"	"nM"	"6.73"	""	"414830"	"UO_0000065"	"15.72"	"0.30"	"4.94"	"4.97"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4110673"	""	"0"	"462.49"	"0"	"3.59"	"BDBM237733"	"N#C[C@@H]1CN(C(=O)OCc2ccccc2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"369.0"	"nM"	"6.43"	""	"414837"	"UO_0000065"	"13.91"	"0.26"	"2.84"	"5.09"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4290597"	""	"0"	"445.48"	"0"	"3.13"	"18"	"COc1cc2c(=O)n([C@@H]3CCCN(C(=O)CC#N)C3)c3c4cc[nH]c4ncc3c2cc1OC"	"IC50"	"'='"	"3.12"	"nM"	"8.51"	""	""	"UO_0000065"	"19.09"	"0.35"	"5.38"	"7.51"	"False"	"CHEMBL4261266"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]-ATP addition measured after 2 hrs by filter-binding method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257589"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4115006"	""	"0"	"494.53"	"0"	"3.02"	"BDBM237748"	"CC(C)(COC(=O)N1CC[C@@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@H](C#N)C1)n1cccn1"	"IC50"	"'='"	"1304.0"	"nM"	"5.88"	""	"414852"	"UO_0000065"	"11.90"	"0.22"	"2.86"	"4.08"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3646845"	""	"0"	"348.36"	"0"	"2.89"	"BDBM130294"	"COc1ccc(-c2nc(C(N)=O)c3[nH]c4cc(OC)ccc4c3n2)cc1"	"IC50"	"'='"	"170.0"	"nM"	"6.77"	""	"262080"	"UO_0000065"	"19.43"	"0.36"	"3.88"	"6.56"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3646849"	""	"0"	"485.37"	"0"	"4.50"	"BDBM130298"	"NC(=O)c1cc(-c2ccc(Cl)c(Cl)c2)nc2c1[nH]c1cc(OCCN3CCOCC3)ccc12"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"262084"	"UO_0000065"	"16.80"	"0.34"	"3.65"	"8.72"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649613"	""	"0"	"519.63"	"1"	"2.55"	"BDBM130307"	"NC(=O)c1cc(-c2ccc(CN3CCOCC3)cc2)nc2c1[nH]c1cc(N3CCS(=O)(=O)CC3)ccc12"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"262093"	"UO_0000065"	"17.32"	"0.33"	"6.45"	"7.40"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649618"	""	"0"	"480.95"	"0"	"4.00"	"BDBM130312"	"COCCOc1ccc(-c2cc(C(N)=O)c3[nH]c4cc(N5CCOCC5)ccc4c3n2)cc1Cl"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"262098"	"UO_0000065"	"17.10"	"0.33"	"4.22"	"8.01"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649624"	""	"0"	"422.49"	"0"	"1.04"	"BDBM130318"	"CN1CCN(c2cc(C(N)=O)c3[nH]c4cc(C(=O)N5CCOCC5)ccc4c3n2)CC1"	"IC50"	"'='"	"220.0"	"nM"	"6.66"	""	"262104"	"UO_0000065"	"15.76"	"0.29"	"5.62"	"6.18"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649626"	""	"0"	"492.58"	"0"	"1.59"	"BDBM130320"	"NC(=O)c1cc(N2CCC(N3CCOCC3)CC2)nc2c1[nH]c1cc(C(=O)N3CCOCC3)ccc12"	"IC50"	"'='"	"262.0"	"nM"	"6.58"	""	"262106"	"UO_0000065"	"13.36"	"0.25"	"4.99"	"5.62"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649647"	""	"0"	"458.52"	"0"	"2.55"	"BDBM130342"	"NC(=O)c1cc(-c2ccc(N3CCOCC3)nc2)nc2c1[nH]c1cc(N3CCOCC3)ccc12"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"262128"	"UO_0000065"	"19.63"	"0.36"	"6.45"	"8.21"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649653"	""	"0"	"486.53"	"0"	"2.19"	"BDBM130348"	"NC(=O)c1cc(-c2cnc(N3CCOCC3)nc2)cc2c1[nH]c1cc(C(=O)N3CCOCC3)ccc12"	"IC50"	"'='"	"108.0"	"nM"	"6.97"	""	"262134"	"UO_0000065"	"14.32"	"0.26"	"4.78"	"5.50"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL231948"	""	"0"	"470.54"	"0"	"3.25"	"16"	"COCCNC(=O)c1cc2c(N[C@@H](C)c3ccccc3)nc(-n3cnc4ccncc43)nc2n1C"	"IC50"	"'='"	"25.0"	"nM"	"7.60"	""	""	"UO_0000065"	"16.16"	"0.30"	"4.35"	"6.80"	"False"	"CHEMBL897052"	"Inhibition of JAK2 by kinase-Glo luminescent assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1148837"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2007"	"None"	""
"CHEMBL3965889"	""	"0"	"310.36"	"0"	"1.30"	"BDBM228764"	"CN(C(=O)C1(C#N)CC1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399698"	"UO_0000065"	"29.84"	"0.55"	"7.96"	"10.41"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3910166"	""	"0"	"296.38"	"0"	"1.91"	"BDBM228770"	"N#CCN(C1CCC1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399706"	"UO_0000065"	"31.24"	"0.57"	"7.35"	"12.89"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3948936"	""	"0"	"367.84"	"0"	"2.90"	"BDBM228777"	"Cc1cc(N(C)[C@@H]2CCN(c3ncnc4[nH]ccc34)C2)nc(Cl)c1C#N"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399714"	"UO_0000065"	"25.17"	"0.49"	"6.36"	"10.93"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3919101"	""	"0"	"294.36"	"0"	"3.47"	"BDBM197717"	"CCCCC(CC#N)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"0.65"	"nM"	"9.19"	""	"351118"	"UO_0000065"	"31.21"	"0.57"	"5.72"	"11.04"	"False"	"CHEMBL3887743"	"Kinase Assay: The compounds of the invention were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Biochemistry 1999, 269, 94-104. The catalytic domains of human JAK1 (a.a. 837-1142), JAK2 (a.a. 828-1132) and JAK3 (a.a. 781-1124) with an N-terminal His tag were expressed using baculovirus in insect cells and purified. The catalytic activity of JAK1, JAK2 or JAK3 was assayed by measuring the phosphorylation of a biotinylated peptide. The phosphorylated peptide was detected by homogenous time resolved fluorescence (HTRF). IC50 was measured for each kinase in the 40 uL reactions that contain the enzyme, ATP and 500 nM peptide in 50 mM Tris (pH 7.8) buffer with 100 mM NaCl, 5 mM DTT, and 0.1 mg/mL (0.01%) BSA. The ATP concentration in the reactions was 90 uM for Jak1, 30 uM for Jak2 and 3 uM for Jak3. Reactions were carried out at room temperature for 1 hr and then stopped with 20 uL 45 mM EDTA."	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886433"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3939451"	""	"0"	"458.54"	"0"	"4.65"	"BDBM228909"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(c2cccc(C3CC3)c2)CC1"	"IC50"	"'='"	"780.0"	"nM"	"6.11"	""	"400656"	"UO_0000065"	"13.32"	"0.25"	"1.46"	"6.11"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3889521"	""	"0"	"444.47"	"0"	"3.04"	"BDBM228910"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(c2cccc(C#N)n2)CC1"	"IC50"	"'='"	"89.0"	"nM"	"7.05"	""	"400657"	"UO_0000065"	"15.86"	"0.29"	"4.01"	"5.16"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3924220"	""	"0"	"468.52"	"0"	"1.86"	"BDBM228992"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccnc(C(N)=O)c3)n2)CC1"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"400737"	"UO_0000065"	"17.41"	"0.33"	"6.29"	"4.47"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3945622"	""	"0"	"487.51"	"0"	"3.49"	"BDBM229003"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(C4CCC4)nc3)n2)CCN(C(=O)OCC(F)F)CC1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"400748"	"UO_0000065"	"17.48"	"0.33"	"5.03"	"6.12"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4115107"	""	"0"	"440.48"	"0"	"3.19"	"BDBM237756"	"CC(OC(=O)N1CC[C@@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@H](C#N)C1)C1CC1"	"IC50"	"'='"	"468.0"	"nM"	"6.33"	""	"414860"	"UO_0000065"	"14.37"	"0.27"	"3.14"	"5.01"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4113743"	""	"0"	"488.52"	"0"	"3.56"	"BDBM237758"	"N#C[C@@H]1CN(C(=O)OC2Cc3ccccc3C2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"414862"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4111098"	""	"0"	"400.41"	"0"	"2.41"	"BDBM237765"	"CCOC(=O)N1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@H](C#N)C1"	"IC50"	"'='"	"1196.0"	"nM"	"5.92"	""	"414869"	"UO_0000065"	"14.79"	"0.28"	"3.51"	"4.69"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4115248"	""	"0"	"440.48"	"0"	"3.33"	"BDBM237770"	"N#C[C@@H]1CN(C(=O)OC2CCCC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"414874"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3646817"	""	"0"	"557.65"	"1"	"4.83"	"BDBM130263"	"COc1cc(-c2cc(C(N)=O)c3[nH]c4cc(C(=O)N5CCN(C)CC5)ccc4c3c2)ccc1NC(=O)OC(C)(C)C"	"IC50"	"'='"	"160.0"	"nM"	"6.80"	""	"262049"	"UO_0000065"	"12.19"	"0.23"	"1.97"	"5.23"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL2035187"	"PACRITINIB"	"3"	"472.59"	"0"	"4.96"	"2; SB1518"	"C1=C/COCc2cc(ccc2OCCN2CCCC2)Nc2nccc(n2)-c2cccc(c2)COC/1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	""	"UO_0000065"	"19.04"	"0.35"	"4.04"	"13.09"	"False"	"CHEMBL3877344"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]ATP addition measured after 120 mins by Hotspot assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3877241"	"1"	"Scientific Literature"	"J Med Chem"	"2016"	"None"	""
"CHEMBL3981879"	""	"0"	"461.52"	"0"	"4.73"	"37"	"O=C(O)CCCOc1ccc2cc1COC/C=C/COCc1cccc(c1)-c1ccnc(n1)N2"	"IC50"	"'='"	"47.0"	"nM"	"7.33"	""	""	"UO_0000065"	"15.88"	"0.29"	"2.60"	"7.13"	"False"	"CHEMBL3877344"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]ATP addition measured after 120 mins by Hotspot assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3877241"	"1"	"Scientific Literature"	"J Med Chem"	"2016"	"None"	""
"CHEMBL3943650"	""	"0"	"517.63"	"2"	"6.29"	"41"	"O=C(O)CCCCCCCOc1ccc2cc1COC/C=C/COCc1cccc(c1)-c1ccnc(n1)N2"	"IC50"	"'<'"	"39.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3877345"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3877241"	"1"	"Scientific Literature"	"J Med Chem"	"2016"	"None"	""
"CHEMBL2103874"	"OCLACITINIB"	"0"	"337.45"	"0"	"1.50"	"BDBM185700"	"CNS(=O)(=O)C[C@H]1CC[C@H](N(C)c2ncnc3[nH]ccc23)CC1"	"IC50"	"'='"	"17.5"	"nM"	"7.76"	""	"335039"	"UO_0000065"	"22.99"	"0.46"	"6.26"	"8.53"	"True"	"CHEMBL3887373"	"Enzymatic Assay: Methods: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK-2 and JAK-3) or the IRS-1 peptide (JAK-1 and Tyk-2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 microliter total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 micromolar for JAK-2 and JAK-3, 40 micromolar for JAK-1 and 7 micromolar for Tyk-2)), 2% DMSO and 1 micromolar peptide substrate (JAKtide for JAK-2 and JAK-3 or IRS-1 peptide for JAK-1 and Tyk-2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 microliter reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK-2, 1 nM JAK-3, 7 nM Tyk2 or 20 nM JAK-1. The assay was run for 240 minutes for JAK-1, 150 minutes for JAK-2, 90 minutes for JAK-3."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886293"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4462728"	""	"0"	"520.59"	"1"	"4.70"	"7q"	"Cc1cnc(Nc2ccc(N3CCOCC3)cc2)nc1-c1cc2c(o1)CCN(C(=O)c1cccc(C#N)c1)C2"	"IC50"	"'='"	"35.4"	"nM"	"7.45"	""	""	"UO_0000065"	"14.31"	"0.26"	"2.75"	"6.93"	"False"	"CHEMBL4341343"	"Inhibition of JAK2 (unknown origin) using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition and measured by 30 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4464597"	""	"0"	"447.54"	"0"	"3.92"	"7o"	"CCC(=O)N1CCc2oc(-c3nc(Nc4ccc(N5CCOCC5)cc4)ncc3C)cc2C1"	"IC50"	"'='"	"5.8"	"nM"	"8.24"	""	""	"UO_0000065"	"18.40"	"0.34"	"4.32"	"9.84"	"False"	"CHEMBL4341343"	"Inhibition of JAK2 (unknown origin) using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition and measured by 30 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4552039"	""	"0"	"486.58"	"0"	"4.06"	"7l"	"Cc1cnc(Nc2ccc(OCCN3CCCC3)cc2)nc1-c1cc2c(o1)CCN(C(=O)CC#N)C2"	"IC50"	"'='"	"9.6"	"nM"	"8.02"	""	""	"UO_0000065"	"16.48"	"0.30"	"3.96"	"7.46"	"False"	"CHEMBL4341343"	"Inhibition of JAK2 (unknown origin) using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition and measured by 30 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4583532"	""	"0"	"373.42"	"0"	"3.59"	"7g"	"Cc1cnc(Nc2ccccc2)nc1-c1cc2c(o1)CCN(C(=O)CC#N)C2"	"IC50"	"'='"	"2.9"	"nM"	"8.54"	""	""	"UO_0000065"	"22.86"	"0.42"	"4.95"	"8.98"	"False"	"CHEMBL4341343"	"Inhibition of JAK2 (unknown origin) using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition and measured by 30 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4569551"	""	"0"	"402.45"	"0"	"3.25"	"7b"	"Cc1cnc(Nc2ccc(F)cc2)nc1-c1cc2c(o1)CCN(S(C)(=O)=O)C2"	"IC50"	"'='"	"12.1"	"nM"	"7.92"	""	""	"UO_0000065"	"19.67"	"0.39"	"4.67"	"8.96"	"False"	"CHEMBL4341343"	"Inhibition of JAK2 (unknown origin) using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition and measured by 30 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4238926"	""	"0"	"326.40"	"0"	"2.01"	"2"	"NC(=O)c1cnc2[nH]ccc2c1NC1C2CC3CC1CC(O)(C3)C2"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	""	"UO_0000065"	"25.43"	"0.47"	"6.29"	"7.98"	"True"	"CHEMBL4341334"	"Inhibition of human JAK2 kinase-domain using Biotin-Lyn-Substrate-2 as substrate incubated for 1 hr by ELISA"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4590082"	""	"0"	"458.52"	"0"	"3.42"	"7j"	"Cc1cnc(Nc2ccc(N3CCOCC3)cc2)nc1-c1cc2c(o1)CCN(C(=O)CC#N)C2"	"IC50"	"'='"	"1028.0"	"nM"	"5.99"	""	""	"UO_0000065"	"13.06"	"0.24"	"2.57"	"5.57"	"False"	"CHEMBL4341350"	"Inhibition of JAK2 V617F mutant in human HEL cells assessed as reduction in cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"CHEMBL3308090"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"1"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"4724.0"	"nM"	"5.33"	""	""	"UO_0000065"	"17.05"	"0.32"	"3.79"	"5.99"	"False"	"CHEMBL4341350"	"Inhibition of JAK2 V617F mutant in human HEL cells assessed as reduction in cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"CHEMBL3308090"	""
"CHEMBL3911395"	""	"0"	"477.54"	"0"	"3.96"	"BDBM228907"	"CC(C)Oc1cccc(N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)CC2)n1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"400654"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL2208035"	""	"0"	"458.52"	"0"	"2.94"	"10e"	"O=C1CC[C@H](C(=O)Nc2ccc(-c3ccnc(Nc4ccc(N5CCOCC5)cc4)n3)cc2)N1"	"IC50"	"'='"	"0.9"	"nM"	"9.05"	""	""	"UO_0000065"	"19.73"	"0.36"	"6.11"	"8.34"	"False"	"CHEMBL2214787"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL2207761"	""	"0"	"458.35"	"0"	"4.64"	"1"	"CC(=O)Nc1ccc(-c2ccnc(NCCCNC(=O)c3c(Cl)cccc3Cl)n2)cc1"	"IC50"	"'='"	"104.0"	"nM"	"6.98"	""	""	"UO_0000065"	"15.24"	"0.31"	"2.34"	"7.27"	"False"	"CHEMBL2214787"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL3646834"	""	"0"	"374.40"	"0"	"3.88"	"BDBM130280"	"COC(=O)c1cccc2[nH]c3c(C(N)=O)cc(-c4cccc(OC)c4)cc3c12"	"IC50"	"'='"	"110.0"	"nM"	"6.96"	""	"262066"	"UO_0000065"	"18.59"	"0.34"	"3.08"	"7.37"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3646837"	""	"0"	"498.37"	"0"	"4.23"	"BDBM130285"	"NC(=O)c1cc(-c2ccc(Cl)c(Cl)c2)cc2c1[nH]c1ccc(C(=O)N3CCOC(CO)C3)cc12"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"262071"	"UO_0000065"	"17.45"	"0.35"	"4.47"	"8.01"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL2208029"	""	"0"	"457.46"	"0"	"4.70"	"9d"	"CC(=O)Nc1ccc(-c2nc(Nc3ccc(N4CCOCC4)cc3)ncc2C(F)(F)F)cc1"	"IC50"	"'='"	"39.6"	"nM"	"7.40"	""	""	"UO_0000065"	"16.18"	"0.31"	"2.70"	"9.33"	"False"	"CHEMBL2214787"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL3646820"	""	"0"	"412.49"	"0"	"3.47"	"BDBM130266"	"CN1CCN(C(=O)c2ccc3c(c2)[nH]c2c(C(N)=O)cc(-c4ccccc4)cc23)CC1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"262052"	"UO_0000065"	"19.93"	"0.36"	"4.75"	"9.97"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3646829"	""	"0"	"418.45"	"0"	"3.60"	"BDBM130275"	"COc1cccc(-c2cc(C(N)=O)c3[nH]c4cc(NC(=O)OCCN)ccc4c3c2)c1"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"262061"	"UO_0000065"	"19.49"	"0.36"	"4.55"	"6.16"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL4109520"	""	"0"	"557.63"	"1"	"1.46"	"BDBM228877"	"CC(C)(C)OC(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(C(=O)N4CCS(=O)(=O)CC4)cc3)n2)C1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"400624"	"UO_0000065"	"14.89"	"0.29"	"6.84"	"4.59"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3916449"	""	"0"	"438.53"	"0"	"3.75"	"BDBM228879"	"C[C@H]1C[C@](CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN1C(=O)OC(C)(C)C"	"IC50"	"'='"	"21.0"	"nM"	"7.68"	""	"400626"	"UO_0000065"	"17.51"	"0.33"	"3.93"	"6.08"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3911561"	""	"0"	"401.49"	"0"	"2.70"	"BDBM228883"	"CS(=O)(=O)c1ccc(Nc2nn(C3(CC#N)CCCCC3)cc2C(N)=O)cc1"	"IC50"	"'='"	"193.0"	"nM"	"6.71"	""	"400630"	"UO_0000065"	"16.72"	"0.33"	"4.01"	"5.13"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3912439"	""	"0"	"410.48"	"0"	"2.98"	"BDBM228886"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"27.0"	"nM"	"7.57"	""	"400633"	"UO_0000065"	"18.44"	"0.34"	"4.59"	"5.99"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3972275"	""	"0"	"535.05"	"2"	"5.69"	"BDBM229045"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3cccc(-c4cccc(Cl)c4)c3)n2)CC1"	"IC50"	"'='"	"1481.0"	"nM"	"5.83"	""	"400790"	"UO_0000065"	"10.90"	"0.21"	"0.14"	"4.62"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3954817"	""	"0"	"550.66"	"2"	"6.19"	"BDBM229046"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3cccc(-c4ccc5ccccc5c4)c3)n2)CC1"	"IC50"	"'='"	"1481.0"	"nM"	"5.83"	""	"400791"	"UO_0000065"	"10.59"	"0.19"	"-0.36"	"4.62"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4110852"	""	"0"	"378.36"	"0"	"2.21"	"BDBM229059"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CN(CC(F)(F)F)C1"	"IC50"	"'='"	"870.0"	"nM"	"6.06"	""	"400795"	"UO_0000065"	"16.02"	"0.31"	"3.85"	"6.06"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4279819"	""	"0"	"310.36"	"0"	"1.30"	"(R)-6c"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(C(=O)CC#N)CC12CC2"	"IC50"	"'='"	"410.0"	"nM"	"6.39"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4283095"	""	"0"	"271.37"	"0"	"1.88"	"7"	"CCN1C[C@H](N(C)c2ncnc3[nH]ccc23)C2(CC2)C1"	"IC50"	"'='"	"30000.0"	"nM"	"4.52"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4276863"	""	"0"	"343.43"	"0"	"2.65"	"26"	"CC(C)COC(=O)N1C[C@H](N(C)c2ncnc3[nH]ccc23)C2(CC2)C1"	"IC50"	"'='"	"1200.0"	"nM"	"5.92"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4290931"	""	"0"	"362.44"	"0"	"3.09"	"29"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(C(=O)Nc2ccccc2)CC12CC2"	"IC50"	"'='"	"420.0"	"nM"	"6.38"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4277099"	""	"0"	"431.33"	"0"	"4.40"	"34"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(C(=O)Nc2cccc(Cl)c2Cl)CC12CC2"	"IC50"	"'='"	"1300.0"	"nM"	"5.89"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4276966"	""	"0"	"428.47"	"0"	"2.16"	"50"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(S(=O)(=O)c2ccc([N+](=O)[O-])cc2)CC12CC2"	"IC50"	"'='"	"30.0"	"nM"	"7.52"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL3649612"	""	"0"	"401.47"	"0"	"2.90"	"BDBM130306"	"NC(=O)c1cc(-c2ccc(CN3CCOCC3)cc2)nc2c1[nH]c1cc(N)ccc12"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"262092"	"UO_0000065"	"22.42"	"0.41"	"6.10"	"8.16"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649616"	""	"0"	"477.59"	"0"	"3.21"	"BDBM130310"	"NC(=O)c1cc(-c2ccc(CN3CCOCC3)s2)nc2c1[nH]c1cc(N3CCOCC3)ccc12"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"262096"	"UO_0000065"	"18.84"	"0.36"	"5.79"	"9.31"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL4285755"	""	"0"	"336.40"	"0"	"2.76"	"11"	"Cc1cc(C)cc(Nc2cc(NC3CC3)c3ncc(C(N)=O)n3n2)c1"	"IC50"	"'>'"	"50000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4251837"	"Inhibition of JAK2 JH2 domain (unknown origin)"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4251544"	"1"	"Scientific Literature"	"MedChemComm"	"2017"	"None"	""
"CHEMBL4240238"	""	"0"	"366.43"	"0"	"1.23"	"10a"	"C=CC(=O)N1CCC(Cn2nc(-c3cnn(C)c3)c3c(N)ncnc32)CC1"	"IC50"	"'='"	"469.3"	"nM"	"6.33"	""	""	"UO_0000065"	"17.27"	"0.32"	"5.10"	"5.87"	"False"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4245604"	""	"0"	"383.46"	"0"	"0.53"	"13e"	"CN(C)CC(=O)N1CCC(n2nc(-c3cnn(C)c3)c3c(N)ncnc32)CC1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4291402"	""	"0"	"374.48"	"0"	"4.33"	"44; GSK2646264"	"COc1cccc(OCc2cc(C)ccn2)c1-c1ccc2c(c1)CCNCC2"	"IC50"	"'='"	"10000.0"	"nM"	"5.00"	""	""	"UO_0000065"	"13.35"	"0.24"	"0.67"	"11.53"	"False"	"CHEMBL4268693"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4265956"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2018"	"None"	""
"CHEMBL4284912"	""	"0"	"397.50"	"0"	"2.56"	"51"	"Cc1cccc(S(=O)(=O)N2C[C@H](N(C)c3ncnc4[nH]ccc34)C3(CC3)C2)c1"	"IC50"	"'='"	"66.0"	"nM"	"7.18"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4278853"	""	"0"	"462.43"	"0"	"3.68"	"20b"	"CC[C@H](C(=O)NCC(F)(F)F)n1c(=O)c2cc(OC)c(OC)cc2c2cnc3[nH]ccc3c21"	"IC50"	"'='"	"140.2"	"nM"	"6.85"	""	""	"UO_0000065"	"14.82"	"0.28"	"3.17"	"6.98"	"False"	"CHEMBL4261266"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]-ATP addition measured after 2 hrs by filter-binding method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257589"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4238357"	""	"0"	"379.43"	"0"	"0.96"	"9c"	"Cn1cc(-c2nn(CC3CCCN(C(=O)CC#N)C3)c3ncnc(N)c23)cn1"	"IC50"	"'='"	"78.4"	"nM"	"7.11"	""	""	"UO_0000065"	"18.73"	"0.35"	"6.15"	"5.40"	"False"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4245422"	""	"0"	"382.43"	"0"	"0.88"	"11b"	"C=CC(=O)N1CCC(n2nc(-c3cnn(CCOC)c3)c3c(N)ncnc32)C1"	"IC50"	"'='"	"508.6"	"nM"	"6.29"	""	""	"UO_0000065"	"16.46"	"0.31"	"5.41"	"5.38"	"False"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL247866"	""	"0"	"442.56"	"1"	"5.85"	"32"	"CC(C)Nc1ncnc2oc(-c3ccc(OCCN4CCCC4)cc3)c(-c3ccccc3)c12"	"IC50"	"'='"	"4891.0"	"nM"	"5.31"	""	""	"UO_0000065"	"12.00"	"0.22"	"-0.54"	"8.37"	"False"	"CHEMBL886500"	"Inhibition of Jak2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139142"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2007"	"None"	""
"CHEMBL4280294"	""	"0"	"289.34"	"0"	"3.03"	"15"	"CN(C#N)C1CCc2ccc(-c3ncnc4[nH]ccc34)cc21"	"IC50"	"'='"	"8623.0"	"nM"	"5.06"	""	""	"UO_0000065"	"17.50"	"0.31"	"2.03"	"7.38"	"False"	"CHEMBL4265556"	"Inhibition of recombinant human GST-tagged JAK2 using KAIETDKEYYTVKD-NH2 as substrate in presence of 1 mM ATP concentration by coupled PK/LDH assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4261650"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4288201"	""	"0"	"291.31"	"0"	"2.52"	"16"	"N#CNC1CCOc2ccc(-c3ncnc4[nH]ccc34)cc21"	"IC50"	"'='"	"783.0"	"nM"	"6.11"	""	""	"UO_0000065"	"20.96"	"0.38"	"3.59"	"7.05"	"False"	"CHEMBL4265556"	"Inhibition of recombinant human GST-tagged JAK2 using KAIETDKEYYTVKD-NH2 as substrate in presence of 1 mM ATP concentration by coupled PK/LDH assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4261650"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4209458"	""	"0"	"336.40"	"0"	"3.15"	"7"	"C=CC(=O)Nc1ccc2ncn(-c3cncc(NC(C)(C)C)n3)c2c1"	"IC50"	"'='"	"40.0"	"nM"	"7.40"	""	""	"UO_0000065"	"21.99"	"0.40"	"4.25"	"8.73"	"False"	"CHEMBL4179014"	"Time-dependent inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in sf21 cells using biotinylated peptide substrate after 1 hr by DELFIA"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4177572"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4226000"	""	"0"	"396.48"	"0"	"2.12"	"13"	"CCN(c1ncnc2[nH]ccc12)[C@@H]1CCN(S(=O)(=O)c2cccc(C#N)c2)C1"	"IC50"	"'='"	"110.0"	"nM"	"6.96"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4225471"	""	"0"	"300.33"	"0"	"1.31"	"17"	"CN(c1ncnc2[nH]ccc12)[C@@H]1CCN(C(=O)CN=[N+]=[N-])C1"	"IC50"	"'='"	"170.0"	"nM"	"6.77"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4227307"	""	"0"	"295.37"	"0"	"0.43"	"21"	"CN(c1ncnc2[nH]ccc12)[C@@H]1CCN(S(C)(=O)=O)C1"	"IC50"	"'='"	"4700.0"	"nM"	"5.33"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4228613"	""	"0"	"402.44"	"0"	"1.77"	"33"	"CN(c1ncnc2[nH]ccc12)[C@@H]1CCN(S(=O)(=O)c2ccccc2[N+](=O)[O-])C1"	"IC50"	"'='"	"1100.0"	"nM"	"5.96"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4636144"	""	"0"	"425.44"	"0"	"3.62"	"J-5"	"O=C(Nc1nc2cccc(-c3ccc(C(=O)N4CCC(F)(F)CC4)cc3)n2n1)C1CC1"	"IC50"	"'='"	"401.0"	"nM"	"6.40"	""	""	"UO_0000065"	"15.04"	"0.28"	"2.78"	"8.04"	"False"	"CHEMBL4624516"	"Inhibition of JAK2 (unknown origin) in presence of ATP at Km concentration by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4622902"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL3301607"	"FILGOTINIB"	"4"	"425.51"	"0"	"1.98"	"5"	"O=C(Nc1nc2cccc(-c3ccc(CN4CCS(=O)(=O)CC4)cc3)n2n1)C1CC1"	"IC50"	"'='"	"74.0"	"nM"	"7.13"	""	""	"UO_0000065"	"16.76"	"0.32"	"5.15"	"7.38"	"False"	"CHEMBL4624516"	"Inhibition of JAK2 (unknown origin) in presence of ATP at Km concentration by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4622902"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL4100288"	""	"0"	"311.35"	"0"	"1.83"	"7; 13"	"N#C[C@H]1CCOC[C@@H]1n1cc(C(N)=O)c(Nc2ccccc2)n1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4032997"	"Inhibition of GST-tagged recombinant human JAK2 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 as substrate preincubated for 30 mins followed by ATP addition measured after 120 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4089234"	""	"0"	"345.79"	"0"	"2.48"	"14"	"N#C[C@H]1CCOC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"1.5"	"nM"	"8.82"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4032997"	"Inhibition of GST-tagged recombinant human JAK2 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 as substrate preincubated for 30 mins followed by ATP addition measured after 120 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4096821"	""	"0"	"378.40"	"0"	"1.41"	"19"	"N#C[C@H]1CCOC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(-n3ccnn3)cc2)n1"	"IC50"	"'='"	"0.7"	"nM"	"9.15"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4032997"	"Inhibition of GST-tagged recombinant human JAK2 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 as substrate preincubated for 30 mins followed by ATP addition measured after 120 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4098999"	""	"0"	"376.42"	"0"	"2.58"	"25"	"N#Cc1ccc(Nc2nn([C@H]3COCC[C@@H]3C#N)cc2C(N)=O)cc1C1CC1"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4032997"	"Inhibition of GST-tagged recombinant human JAK2 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 as substrate preincubated for 30 mins followed by ATP addition measured after 120 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4077886"	""	"0"	"351.41"	"0"	"2.70"	"16"	"N#C[C@H]1CCOC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C3CC3)cc2)n1"	"IC50"	"'='"	"200.0"	"nM"	"6.70"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4033007"	"Inhibition of JAK2 in EPO-stimulated human TF1 cells expressing stably integrated beta-lactamase reporter gene under control of STAT5 response elements in interferon regulatory factor 1 gene promoter by fluorescence assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4645814"	""	"0"	"270.34"	"0"	"2.75"	"21"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](CC#N)CC3)c12"	"IC50"	"'>'"	"40000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL4226257"	""	"0"	"375.43"	"0"	"2.00"	"29"	"CN(c1ncnc2[nH]ccc12)[C@@H]1CCN(S(=O)(=O)c2cccc(F)c2)C1"	"IC50"	"'='"	"53.0"	"nM"	"7.28"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4549369"	""	"0"	"405.82"	"0"	"3.24"	"8u"	"O=C(CCCn1cc(Nc2ncc(Cl)c(Nc3ccc(F)cc3)n2)cn1)NO"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	""	"UO_0000065"	"19.71"	"0.39"	"4.76"	"6.84"	"False"	"CHEMBL4347596"	"Inhibition of recombinant human JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate measured after 60 mins by LANCE assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4346670"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4644138"	""	"0"	"412.43"	"0"	"0.40"	"13"	"N#C[C@@H]1C[C@H]1C(=O)N[C@@]12C[C@@H]1CN(c1nc(Nc3cnn(CCO)c3)ncc1F)C2"	"IC50"	"'='"	"340.0"	"nM"	"6.47"	""	""	"UO_0000065"	"15.68"	"0.29"	"6.07"	"4.90"	"False"	"CHEMBL4620433"	"Inhibition of human recombinant JAK2 assessed as level of phosphorylation in presence of peptide substrate FITC-KGGEEEEYFELVKK and ATP by mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4619733"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2020"	"None"	""
"CHEMBL4648631"	""	"0"	"396.43"	"0"	"1.19"	"18"	"C[C@@H]1[C@@H]2CN(c3nc(Nc4cnn(C)c4)ncc3F)C[C@]12NC(=O)[C@H]1C[C@@H]1C#N"	"IC50"	"'='"	"1168.0"	"nM"	"5.93"	""	""	"UO_0000065"	"14.96"	"0.28"	"4.74"	"5.31"	"False"	"CHEMBL4620433"	"Inhibition of human recombinant JAK2 assessed as level of phosphorylation in presence of peptide substrate FITC-KGGEEEEYFELVKK and ATP by mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4619733"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2020"	"None"	""
"CHEMBL4640289"	""	"0"	"408.38"	"0"	"2.44"	"J-9"	"O=C(Nc1nc2cccc(C3=CCN(C(=O)NCC(F)(F)F)CC3)n2n1)C1CC1"	"IC50"	"'='"	"347.0"	"nM"	"6.46"	""	""	"UO_0000065"	"15.82"	"0.30"	"4.02"	"7.05"	"False"	"CHEMBL4624516"	"Inhibition of JAK2 (unknown origin) in presence of ATP at Km concentration by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4622902"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL3301607"	"FILGOTINIB"	"4"	"425.51"	"0"	"1.98"	"5"	"O=C(Nc1nc2cccc(-c3ccc(CN4CCS(=O)(=O)CC4)cc3)n2n1)C1CC1"	"IC50"	"'='"	"4450.0"	"nM"	"5.35"	""	""	"UO_0000065"	"12.58"	"0.24"	"3.37"	"5.54"	"False"	"CHEMBL4624521"	"Inhibition of JAK2 (unknown origin) expressed in mouse BAF3 cells assessed as antiproliferative activity by cell-based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4622902"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"CHEMBL3307634"	""
"CHEMBL2208031"	""	"0"	"418.50"	"0"	"3.01"	"10a"	"C[C@H](N)C(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"8.7"	"nM"	"8.06"	""	""	"UO_0000065"	"19.26"	"0.36"	"5.05"	"7.65"	"False"	"CHEMBL2214787"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL4448906"	""	"0"	"420.38"	"0"	"3.08"	"2"	"O=c1[nH]c2cnc(-c3cnc4ccc(F)cn34)nc2n1[C@@H]1CCOc2c(F)cccc21"	"IC50"	"'='"	"1.2"	"nM"	"8.92"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4549136"	""	"0"	"382.40"	"0"	"2.44"	"16"	"C[C@]1(O)CC[C@H](n2c(=O)[nH]c3cnc(-c4cnc5ccc(F)cn45)nc32)CC1"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL3914756"	""	"0"	"508.56"	"1"	"3.67"	"263"	"N#CCC1(n2ccc(-c3ncnc4[nH]ccc34)c2)CN(C2CCN(C(=O)c3cc(F)cc(C#N)c3)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3956200"	""	"0"	"551.55"	"1"	"4.81"	"275"	"N#CCC1(n2ccc(-c3ncnc4[nH]ccc34)c2)CN(C2CCN(C(=O)c3ccc(F)c(C(F)(F)F)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3921074"	""	"0"	"568.99"	"1"	"4.72"	"298"	"N#CCC1(n2cc(-c3ccnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc(C(F)(F)F)ncc3Cl)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3928484"	""	"0"	"533.01"	"1"	"4.84"	"305"	"N#CCC1(n2cc(-c3ccnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3ccc(F)cc3Cl)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3932892"	""	"0"	"520.52"	"1"	"3.47"	"321"	"N#CCC1(n2cc(-c3c(F)cnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3c(F)cncc3F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3898620"	""	"0"	"533.57"	"1"	"3.54"	"324"	"N#CCC1(n2cc(-c3c(F)cnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc(C#N)ccc3C#N)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3892282"	""	"0"	"525.58"	"1"	"4.31"	"327"	"N#CCC1(n2cc(-c3c(F)cnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)C3CCC(F)(F)CC3)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3905971"	""	"0"	"553.52"	"1"	"3.60"	"354"	"N#CCC1(n2cc(-c3c(F)cnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cnc(C(F)(F)F)cn3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3939733"	""	"0"	"566.55"	"1"	"2.48"	"360"	"CO[C@@H]1CN(C(=O)c2ccnc(C(F)(F)F)n2)CC[C@@H]1N1CC(CC#N)(n2cc(-c3ncnc4[nH]ccc34)cn2)C1"	"IC50"	"'>'"	"100.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3934829"	""	"0"	"593.62"	"1"	"2.92"	"370"	"CN(C)Cc1cc(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)nc(C(F)(F)F)n1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3949147"	""	"0"	"607.65"	"1"	"3.31"	"374"	"CCN(C)Cc1cc(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)nc(C(F)(F)F)n1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3930452"	""	"0"	"1075.74"	"1"	"3.46"	"376"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc(CN4CCCC4)nc(C(F)(F)F)n3)CC2)C1.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3913286"	""	"0"	"1111.72"	"1"	"3.70"	"379"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc(CN4CCC(F)(F)C4)nc(C(F)(F)F)n3)CC2)C1.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3894187"	""	"0"	"593.62"	"1"	"2.97"	"383"	"CCNCc1cc(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)nc(C(F)(F)F)n1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3914575"	""	"0"	"448.53"	"0"	"2.76"	"386"	"CCCOC(=O)N1CCC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3968973"	""	"0"	"488.60"	"0"	"3.54"	"397"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)OCC3CCCC3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL4645613"	""	"0"	"243.31"	"0"	"2.46"	"11"	"Cc1[nH]nc2[nH]c(=O)cc([C@@H]3C[C@H]4CC[C@@H]3C4)c12"	"IC50"	"'='"	"380.0"	"nM"	"6.42"	""	""	"UO_0000065"	"26.39"	"0.49"	"3.96"	"10.43"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4638696"	""	"0"	"261.32"	"0"	"2.10"	"17"	"Cc1[nH]nc2[nH]c(=O)c(CO)c(C3CCCCC3)c12"	"IC50"	"'='"	"2800.0"	"nM"	"5.55"	""	""	"UO_0000065"	"21.25"	"0.40"	"3.45"	"6.79"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4522317"	""	"0"	"403.36"	"0"	"3.90"	"25"	"CCc1cc(O)c(F)cc1-c1cc(NS(=O)(=O)C(F)(F)F)c2cn[nH]c2c1"	"IC50"	"'='"	"158.49"	"nM"	"6.80"	""	""	"UO_0000065"	"16.86"	"0.34"	"2.90"	"7.15"	"False"	"CHEMBL4478762"	"Inhibition of human His-tagged JAK2 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4477220"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2016"	"None"	""
"CHEMBL4521312"	""	"0"	"403.48"	"0"	"4.32"	"24"	"CCc1cc(O)c(F)cc1-c1cc(NS(=O)(=O)C2CCCC2)c2cn[nH]c2c1"	"IC50"	"'='"	"25.12"	"nM"	"7.60"	""	""	"UO_0000065"	"18.84"	"0.37"	"3.28"	"7.99"	"False"	"CHEMBL4478762"	"Inhibition of human His-tagged JAK2 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4477220"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2016"	"None"	""
"CHEMBL4532948"	""	"0"	"434.44"	"0"	"1.90"	"6"	"CNc1cc(Nc2cccn(-c3ccccn3)c2=O)nn2c(C(=O)N[C@@H]3C[C@@H]3F)cnc12"	"IC50"	"'>'"	"2000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4402476"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4400582"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2019"	"None"	""
"CHEMBL4162254"	""	"0"	"471.52"	"0"	"2.86"	"8"	"N#CCNC(=O)c1ccc(-c2ccnc(Nc3ccc(N4CCC(C(=O)NO)CC4)cc3)n2)cc1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	""	"UO_0000065"	"17.81"	"0.33"	"5.54"	"5.86"	"False"	"CHEMBL4150584"	"Inhibition of JAK2 (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition and measured after 25 mins in presence of ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4145634"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4164238"	""	"0"	"557.68"	"1"	"4.70"	"18"	"CS(=O)(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCC(C(=O)Nc5ccccc5N)CC4)cc3)n2)cc1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	""	"UO_0000065"	"15.60"	"0.30"	"4.00"	"6.11"	"False"	"CHEMBL4150584"	"Inhibition of JAK2 (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition and measured after 25 mins in presence of ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4145634"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4174879"	""	"0"	"466.54"	"0"	"4.59"	"18"	"Cc1cnc(Nc2cc(C(F)F)cc(N3C[C@@H]4C[C@H]3CN4C)c2)nc1Nc1cccc(CO)c1"	"IC50"	"'='"	"376.0"	"nM"	"6.42"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4145184"	"Inhibition of recombinant human JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate after 10 mins by caliper assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4138312"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL2207758"	""	"0"	"444.54"	"0"	"3.27"	"10f"	"O=C(Nc1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1)[C@H]1CCNC1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2214785"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT1 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL2207766"	""	"0"	"457.92"	"1"	"5.75"	"6a"	"CC(=O)Nc1ccc(-c2ccnc(Nc3cccc(NC(=O)c4ccccc4Cl)c3)n2)cc1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2214785"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT1 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL4647966"	""	"0"	"245.33"	"0"	"2.86"	"15"	"CCc1[nH]nc2[nH]c(=O)cc(C3CCCCC3)c12"	"IC50"	"'>'"	"40000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL4639048"	""	"0"	"378.50"	"0"	"2.31"	"31"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](NS(=O)(=O)CC4CCC4)CC3)c12"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL4228831"	""	"0"	"312.38"	"0"	"1.54"	"7"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(C(=O)CC#N)CC1(C)C"	"IC50"	"'='"	"5900.0"	"nM"	"5.23"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4227802"	""	"0"	"371.47"	"0"	"2.17"	"37"	"Cc1ccc(S(=O)(=O)N2CC[C@@H](N(C)c3ncnc4[nH]ccc34)C2)cc1"	"IC50"	"'='"	"1800.0"	"nM"	"5.75"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4642546"	""	"0"	"275.35"	"0"	"2.14"	"18"	"Cc1[nH]nc2[nH]c(=O)c(CCO)c(C3CCCCC3)c12"	"IC50"	"'>'"	"40000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL4647276"	""	"0"	"353.43"	"0"	"2.21"	"34"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](CC(=O)N4CC(C#N)C4)CC3)c12"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL221976"	""	"0"	"334.36"	"0"	"3.52"	"10"	"C[C@H](Nc1ccnc(-n2cnc3ccncc32)n1)c1ccc(F)cc1"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	""	"UO_0000065"	"24.22"	"0.44"	"4.58"	"11.82"	"False"	"CHEMBL908418"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139695"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2006"	"None"	""
"CHEMBL221029"	""	"0"	"316.37"	"0"	"3.38"	"2"	"C[C@H](Nc1ccnc(-n2cnc3ccncc32)n1)c1ccccc1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	""	"UO_0000065"	"26.54"	"0.48"	"5.02"	"12.26"	"False"	"CHEMBL908418"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139695"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2006"	"None"	""
"CHEMBL490355"	"SULFURETIN"	"0"	"270.24"	"0"	"2.42"	"67"	"O=C1/C(=C/c2ccc(O)c(O)c2)Oc2cc(O)ccc21"	"IC50"	"'='"	"9320.0"	"nM"	"5.03"	""	""	"UO_0000065"	"18.62"	"0.34"	"2.61"	"5.78"	"False"	"CHEMBL4014517"	"Inhibition of human JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4014275"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2017"	"None"	""
"CHEMBL4226571"	""	"0"	"324.39"	"0"	"1.69"	"10"	"N#CCC(=O)N1CC[C@@H](N(CC2CC2)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"1700.0"	"nM"	"5.77"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4226780"	""	"0"	"323.42"	"0"	"1.21"	"25"	"CCCS(=O)(=O)N1CC[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"460.0"	"nM"	"6.34"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4225425"	""	"0"	"375.43"	"0"	"2.00"	"28"	"CN(c1ncnc2[nH]ccc12)[C@@H]1CCN(S(=O)(=O)c2ccccc2F)C1"	"IC50"	"'='"	"130.0"	"nM"	"6.89"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4089515"	""	"0"	"498.61"	"0"	"2.48"	"4"	"C[C@@H]1CCN(C(=O)N2CC[C@@H](S(=O)(=O)c3cccc(O)c3)C2)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"21.2"	"nM"	"7.67"	""	""	"UO_0000065"	"15.39"	"0.30"	"5.19"	"6.25"	"False"	"CHEMBL4003453"	"Inhibition of GST tagged human recombinant JAK2 catalytic domain expressed in baculovirus using peptide substrate preincubated for 60 mins followed by substrate addition and measured after 60 mins by microfluidic assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4002590"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL3929865"	""	"0"	"326.36"	"0"	"4.48"	"6"	"Oc1cccc(-c2ccc3c(-c4nc5ccccc5[nH]4)n[nH]c3c2)c1"	"IC50"	"'='"	"100.8"	"nM"	"7.00"	""	""	"UO_0000065"	"21.44"	"0.38"	"2.52"	"9.02"	"False"	"CHEMBL4003453"	"Inhibition of GST tagged human recombinant JAK2 catalytic domain expressed in baculovirus using peptide substrate preincubated for 60 mins followed by substrate addition and measured after 60 mins by microfluidic assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4002590"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4066236"	""	"0"	"373.46"	"0"	"3.88"	"18"	"CCc1cc(O)ccc1-c1ccc2c(-c3nc4c([nH]3)CN(C)CC4)n[nH]c2c1"	"IC50"	"'='"	"6.4"	"nM"	"8.19"	""	""	"UO_0000065"	"21.94"	"0.40"	"4.31"	"10.14"	"False"	"CHEMBL4003453"	"Inhibition of GST tagged human recombinant JAK2 catalytic domain expressed in baculovirus using peptide substrate preincubated for 60 mins followed by substrate addition and measured after 60 mins by microfluidic assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4002590"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4069951"	""	"0"	"437.53"	"0"	"3.21"	"20"	"CCc1cc(O)ccc1-c1ccc2c(-c3nc4c([nH]3)CN(S(C)(=O)=O)CC4)n[nH]c2c1"	"IC50"	"'='"	"5.6"	"nM"	"8.25"	""	""	"UO_0000065"	"18.86"	"0.36"	"5.04"	"7.18"	"False"	"CHEMBL4003453"	"Inhibition of GST tagged human recombinant JAK2 catalytic domain expressed in baculovirus using peptide substrate preincubated for 60 mins followed by substrate addition and measured after 60 mins by microfluidic assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4002590"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4097152"	""	"0"	"467.55"	"1"	"5.59"	"21"	"CCc1cc(O)c(F)cc1-c1ccc2c(-c3nc4c([nH]3)CN(Cc3ccccc3)CC4)n[nH]c2c1"	"IC50"	"'='"	"15.9"	"nM"	"7.80"	""	""	"UO_0000065"	"16.68"	"0.30"	"2.21"	"9.65"	"False"	"CHEMBL4003453"	"Inhibition of GST tagged human recombinant JAK2 catalytic domain expressed in baculovirus using peptide substrate preincubated for 60 mins followed by substrate addition and measured after 60 mins by microfluidic assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4002590"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4573218"	""	"0"	"430.51"	"0"	"3.79"	"11d"	"C=CC(=O)Nc1cccc(CNc2cc(Nc3ccc(N4CCOCC4)cc3)ncn2)c1"	"IC50"	"'='"	"1096.0"	"nM"	"5.96"	""	""	"UO_0000065"	"13.84"	"0.25"	"2.17"	"6.52"	"False"	"CHEMBL4482009"	"Inhibition of human JAK2 using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and further incubated for 30 mins and subsequently measured after 1 hr by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480445"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4588496"	""	"0"	"457.58"	"0"	"4.10"	"12e'"	"C/C=C/C(=O)Nc1ccc(CNc2cc(Nc3ccc(N4CCN(C)CC4)cc3)ncn2)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4482009"	"Inhibition of human JAK2 using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and further incubated for 30 mins and subsequently measured after 1 hr by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480445"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4518786"	""	"0"	"443.51"	"0"	"3.52"	"14d"	"N#CCC(=O)Nc1ccc(CNc2cc(Nc3ccc(N4CCOCC4)cc3)ncn2)cc1"	"IC50"	"'='"	"1444.0"	"nM"	"5.84"	""	""	"UO_0000065"	"13.17"	"0.24"	"2.32"	"5.07"	"False"	"CHEMBL4482009"	"Inhibition of human JAK2 using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and further incubated for 30 mins and subsequently measured after 1 hr by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480445"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4589415"	""	"0"	"472.47"	"0"	"4.17"	"16d'"	"O=C(Nc1ccc(CNc2cc(Nc3ccc(N4CCOCC4)cc3)ncn2)cc1)C(F)(F)F"	"IC50"	"'='"	"280.0"	"nM"	"6.55"	""	""	"UO_0000065"	"13.87"	"0.26"	"2.38"	"7.17"	"False"	"CHEMBL4482009"	"Inhibition of human JAK2 using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and further incubated for 30 mins and subsequently measured after 1 hr by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480445"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4541547"	""	"0"	"379.42"	"0"	"2.15"	"11b'"	"C=CC(=O)Nc1ccc(CNc2cc(Nc3cnn(CCO)c3)ncn2)cc1"	"IC50"	"'='"	"2098.0"	"nM"	"5.68"	""	""	"UO_0000065"	"14.97"	"0.28"	"3.53"	"4.85"	"False"	"CHEMBL4482009"	"Inhibition of human JAK2 using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and further incubated for 30 mins and subsequently measured after 1 hr by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480445"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL1789941"	"RUXOLITINIB"	"4"	"306.37"	"0"	"3.47"	"1"	"N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"2.8"	"nM"	"8.55"	""	""	"UO_0000065"	"27.92"	"0.51"	"5.08"	"10.28"	"True"	"CHEMBL4481927"	"Inhibition of human JAK2 (828 to 1132 residues) expressed in baculovirus infected Sf9 insect cells using EQEDEPEGDYFEWLE as substrate after 1 hr by fluorescence assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480435"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"CHEMBL3308860"	""
"CHEMBL4545256"	""	"0"	"345.39"	"0"	"3.33"	"16a"	"c1ccc(-n2cnnn2)c(-c2nc(-c3ccc4[nH]ncc4c3)cs2)c1"	"IC50"	"'='"	"1540.0"	"nM"	"5.81"	""	""	"UO_0000065"	"16.83"	"0.32"	"2.48"	"6.82"	"False"	"CHEMBL4481929"	"Inhibition of JAK2 (unknown origin) after 1 hr FRET-based Z'-Lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480435"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL1270230"	""	"0"	"279.30"	"0"	"1.82"	"18"	"NC(=O)c1cc(-c2ccnc(N)n2)[nH]c1-c1ccccc1"	"IC50"	"'='"	"3300.0"	"nM"	"5.48"	""	""	"UO_0000065"	"19.63"	"0.36"	"3.66"	"4.95"	"False"	"CHEMBL1274134"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1268909"	"1"	"Scientific Literature"	"J. Med. Chem."	"2010"	"None"	""
"CHEMBL4525213"	""	"0"	"321.17"	"0"	"3.70"	"30d"	"Nc1n[nH]c2ccc(NC(=O)c3cccc(Cl)c3Cl)cc12"	"IC50"	"'='"	"411.0"	"nM"	"6.39"	""	""	"UO_0000065"	"19.88"	"0.42"	"2.69"	"7.62"	"False"	"CHEMBL4481929"	"Inhibition of JAK2 (unknown origin) after 1 hr FRET-based Z'-Lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480435"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL600875"	""	"0"	"313.36"	"0"	"4.45"	"13u"	"Oc1ccc(C2Nc3ccccc3-c3ccnc4[nH]cc2c34)cc1"	"IC50"	"'='"	"1100.0"	"nM"	"5.96"	""	""	"UO_0000065"	"19.02"	"0.34"	"1.51"	"9.78"	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL591800"	""	"0"	"347.81"	"1"	"5.10"	"13y"	"Oc1ccc(C2Nc3ccccc3-c3ccnc4[nH]cc2c34)c(Cl)c1"	"IC50"	"'='"	"5600.0"	"nM"	"5.25"	""	""	"UO_0000065"	"15.10"	"0.29"	"0.15"	"8.62"	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL3912101"	""	"0"	"508.56"	"1"	"3.67"	"264"	"N#CCC1(n2ccc(-c3ncnc4[nH]ccc34)c2)CN(C2CCN(C(=O)c3ccc(C#N)cc3F)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3945402"	""	"0"	"501.54"	"1"	"3.93"	"278"	"N#CCC1(n2ccc(-c3ncnc4[nH]ccc34)c2)CN(C2CCN(C(=O)c3cc(F)ccc3F)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3911880"	""	"0"	"549.56"	"1"	"4.46"	"308"	"N#CCC1(n2cc(-c3ccnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3cnccc3C(F)(F)F)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3982699"	""	"0"	"526.55"	"1"	"3.81"	"317"	"N#CCC1(n2cc(-c3c(F)cnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(C#N)cc3F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3978536"	""	"0"	"648.36"	"2"	"5.05"	"335"	"N#CCC1(n2cc(-c3c(C#N)cnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc(Br)ccc3Br)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3976063"	""	"0"	"648.36"	"2"	"5.05"	"336"	"N#CCC1(n2cc(-c3c(C#N)cnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc(Br)cc(Br)c3)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3934692"	""	"0"	"535.53"	"1"	"3.46"	"347"	"N#CCC1(n2ccc(-c3ncnc4[nH]ccc34)c2)CN(C2CCN(C(=O)c3cnc(C(F)(F)F)cn3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3895070"	""	"0"	"595.56"	"1"	"3.09"	"365"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2C3COCC2CN(C(=O)c2ccnc(C(F)(F)F)c2F)C3)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3925144"	""	"0"	"532.56"	"1"	"3.83"	"393"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)OCc3ccc(F)cc3F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL4547761"	""	"0"	"371.40"	"0"	"0.66"	"21"	"COc1ccc(-c2cc3c(N[C@H](CO)[C@@H](C)O)c(C(N)=O)cnn3c2)cn1"	"IC50"	"'='"	"57.0"	"nM"	"7.24"	""	""	"UO_0000065"	"19.50"	"0.37"	"6.58"	"5.37"	"False"	"CHEMBL4339747"	"Inhibition of GST-tagged JAK2 (unknown origin) using fluoresceinated peptide as substrate measured after 3 hrs by electrophoresis method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4339199"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2019"	"None"	""
"CHEMBL4638953"	""	"0"	"350.37"	"0"	"2.36"	"28"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](NC(=O)[C@H]4CC4(F)F)CC3)c12"	"IC50"	"'='"	"1700.0"	"nM"	"5.77"	""	""	"UO_0000065"	"16.47"	"0.32"	"3.41"	"6.37"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4634289"	""	"0"	"282.35"	"0"	"2.60"	"41"	"Cc1[nH]nc2[nH]c(=O)cc([C@@H]3C[C@@H]4C[C@H]3C[C@@H]4CC#N)c12"	"IC50"	"'='"	"150.0"	"nM"	"6.82"	""	""	"UO_0000065"	"24.17"	"0.44"	"4.22"	"8.00"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL3765517"	""	"0"	"433.54"	"0"	"1.16"	"19"	"CC(C)[C@H](C)n1cc(-c2cc(N3CCS(=O)(=O)CC3)n(C)n2)c2[nH]nc(N)c2c1=O"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	""	"UO_0000065"	"18.19"	"0.36"	"6.73"	"5.98"	"False"	"CHEMBL3766653"	"Inhibition of JAK2 (unknown origin) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent substrate phosphorylation after 45 mins by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3763089"	"1"	"Scientific Literature"	"J. Med. Chem."	"2016"	"None"	""
"CHEMBL4472924"	""	"0"	"320.40"	"0"	"3.45"	"15"	"NC(=O)c1cnn2cc(-c3ccccc3)cc2c1NC1CCCC1"	"IC50"	"'='"	"50.0"	"nM"	"7.30"	""	""	"UO_0000065"	"22.79"	"0.42"	"3.85"	"10.08"	"False"	"CHEMBL4339747"	"Inhibition of GST-tagged JAK2 (unknown origin) using fluoresceinated peptide as substrate measured after 3 hrs by electrophoresis method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4339199"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2019"	"None"	""
"CHEMBL4295224"	""	"0"	"477.57"	"0"	"4.99"	"50"	"CC(=O)Nc1ccc(-c2nc(Nc3cccc(OCCCCCCC(=O)NO)c3)ncc2C)cc1"	"IC50"	"'='"	"3.9"	"nM"	"8.41"	""	""	"UO_0000065"	"17.61"	"0.33"	"3.42"	"6.70"	"False"	"CHEMBL4268221"	"Inhibition of human JAK2 using poly(Glu:Tyr)(4:1) as substrate preincubated for 20 mins followed by [gamma33P]ATP addition measured after 120 mins by ion exchange filter paper method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4265943"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2018"	"None"	""
"CHEMBL4285223"	""	"0"	"516.65"	"2"	"5.66"	"69e"	"O=C(CCCCCCC(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCCCC4)cc3)n2)cc1)NO"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	""	"UO_0000065"	"14.99"	"0.28"	"2.08"	"6.48"	"False"	"CHEMBL4268221"	"Inhibition of human JAK2 using poly(Glu:Tyr)(4:1) as substrate preincubated for 20 mins followed by [gamma33P]ATP addition measured after 120 mins by ion exchange filter paper method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4265943"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2018"	"None"	""
"CHEMBL1289095"	""	"0"	"299.35"	"0"	"3.67"	"36"	"CC(C)[C@H](C)Nc1nc2cc[nH]c(=O)c2c2cc(F)ccc12"	"IC50"	"'='"	"27.0"	"nM"	"7.57"	""	""	"UO_0000065"	"25.28"	"0.47"	"3.90"	"13.10"	"False"	"CHEMBL1291235"	"Inhibition of JAK2 in cell-free system"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287746"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL4469681"	""	"0"	"358.35"	"0"	"2.03"	"8"	"NC(=O)c1c(N)nn2cc(N3CCC[C@@H]3c3cc(F)ccc3F)cnc12"	"IC50"	"'>'"	"2000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4349458"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain (826 to 1132 end residues) expressed in baculovirus expression system using TK peptide as substrate after 120 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4346723"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2019"	"None"	""
"CHEMBL4587735"	""	"0"	"345.41"	"0"	"3.96"	"7"	"C=CC(=O)Nc1cccc(CNc2cc(Nc3ccccc3)ncn2)c1"	"IC50"	"'>'"	"3000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4482009"	"Inhibition of human JAK2 using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and further incubated for 30 mins and subsequently measured after 1 hr by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480445"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4539137"	""	"0"	"349.40"	"0"	"2.69"	"11a"	"C=CC(=O)Nc1cccc(CNc2cc(Nc3cnn(C)c3)ncn2)c1"	"IC50"	"'>'"	"3000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4482009"	"Inhibition of human JAK2 using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and further incubated for 30 mins and subsequently measured after 1 hr by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480445"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4574614"	""	"0"	"393.45"	"0"	"2.80"	"11c"	"C=CC(=O)Nc1cccc(CNc2cc(Nc3cnn(CCOC)c3)ncn2)c1"	"IC50"	"'='"	"2043.0"	"nM"	"5.69"	""	""	"UO_0000065"	"14.46"	"0.27"	"2.89"	"5.37"	"False"	"CHEMBL4482009"	"Inhibition of human JAK2 using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and further incubated for 30 mins and subsequently measured after 1 hr by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480445"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4435170"	"DEUCRAVACITINIB"	"3"	"425.47"	"0"	"1.73"	"11; BMS-986165"	"[2H]C([2H])([2H])NC(=O)c1nnc(NC(=O)C2CC2)cc1Nc1cccc(-c2ncn(C)n2)c1OC"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4377389"	"Inhibition of JAK2 in human TF1 cells assessed as decrease in EPO-induced STAT5A phosphorylation incubated for 10 mins by ELISA"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4376812"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4581532"	""	"0"	"414.52"	"0"	"3.48"	"15e"	"CN1CCN(c2ccc(Nc3cc(NCc4cccc(NC#N)c4)ncn3)cc2)CC1"	"IC50"	"'='"	"350.0"	"nM"	"6.46"	""	""	"UO_0000065"	"15.57"	"0.28"	"2.98"	"7.01"	"False"	"CHEMBL4482009"	"Inhibition of human JAK2 using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and further incubated for 30 mins and subsequently measured after 1 hr by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480445"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4242999"	""	"0"	"407.31"	"0"	"2.01"	"18, trans-isomer"	"Br.NC(=O)c1cnc2[nH]ccc2c1NC1C2CC3CC1CC(O)(C3)C2"	"IC50"	"'='"	"248.0"	"nM"	"6.61"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4236477"	"Inhibition of JAK2 in human TF1 cells assessed as reduction in EPO-induced cell proliferation after 2 days by alamar blue assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229549"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4238926"	""	"0"	"326.40"	"0"	"2.01"	"17b"	"NC(=O)c1cnc2[nH]ccc2c1NC1C2CC3CC1CC(O)(C3)C2"	"IC50"	"'='"	"1.7"	"nM"	"8.77"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4236469"	"Inhibition of recombinant human N-terminal His-tagged JAK2 catalytic domain (826 to 1132 residues) expressed in baculovirus expression system using Biotin-Lyn-Substrate2 after 1 hr by ELISA"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229549"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4284952"	""	"0"	"291.31"	"0"	"2.52"	"17"	"N#CN[C@H]1CCOc2ccc(-c3ncnc4[nH]ccc34)cc21"	"IC50"	"'='"	"876.0"	"nM"	"6.06"	""	""	"UO_0000065"	"20.79"	"0.38"	"3.54"	"6.99"	"False"	"CHEMBL4265556"	"Inhibition of recombinant human GST-tagged JAK2 using KAIETDKEYYTVKD-NH2 as substrate in presence of 1 mM ATP concentration by coupled PK/LDH assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4261650"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4288935"	""	"0"	"412.48"	"0"	"1.75"	"29"	"COCCS(=O)(=O)N[C@@H]1C[C@H](NC#N)c2cc(-c3ncnc4[nH]ccc34)ccc21"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4265556"	"Inhibition of recombinant human GST-tagged JAK2 using KAIETDKEYYTVKD-NH2 as substrate in presence of 1 mM ATP concentration by coupled PK/LDH assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4261650"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4277610"	""	"0"	"448.48"	"0"	"3.30"	"32"	"N#CN[C@H]1C[C@@H](NS(=O)(=O)c2cccc(F)c2)c2ccc(-c3ncnc4[nH]ccc34)cc21"	"IC50"	"'='"	"3012.0"	"nM"	"5.52"	""	""	"UO_0000065"	"12.31"	"0.24"	"2.22"	"4.47"	"False"	"CHEMBL4265556"	"Inhibition of recombinant human GST-tagged JAK2 using KAIETDKEYYTVKD-NH2 as substrate in presence of 1 mM ATP concentration by coupled PK/LDH assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4261650"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4286562"	""	"0"	"349.39"	"0"	"2.71"	"19"	"COCCc1c[nH]c2ncnc(-c3ccc4c(c3)C(NC#N)CCO4)c12"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4265556"	"Inhibition of recombinant human GST-tagged JAK2 using KAIETDKEYYTVKD-NH2 as substrate in presence of 1 mM ATP concentration by coupled PK/LDH assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4261650"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3671150"	""	"0"	"437.45"	"0"	"3.01"	"BDBM127649"	"Cn1cc(CNC(=O)c2cnn3ccc(N4CCC[C@@H]4c4cc(F)ccc4F)nc23)cn1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258323"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL4645039"	""	"0"	"406.49"	"0"	"2.17"	"9"	"CCNC(=O)c1ccc(Nc2nccc(N3CC4CC(C3)N4C(=O)C3CC3)n2)cc1"	"IC50"	"'='"	"9644.0"	"nM"	"5.02"	""	""	"UO_0000065"	"12.34"	"0.23"	"2.85"	"5.54"	"False"	"CHEMBL4620433"	"Inhibition of human recombinant JAK2 assessed as level of phosphorylation in presence of peptide substrate FITC-KGGEEEEYFELVKK and ATP by mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4619733"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2020"	"None"	""
"CHEMBL4640335"	""	"0"	"217.27"	"0"	"2.22"	"8"	"Cc1[nH]nc2[nH]c(=O)cc(C3CCCC3)c12"	"IC50"	"'='"	"13000.0"	"nM"	"4.89"	""	""	"UO_0000065"	"22.49"	"0.42"	"2.67"	"7.94"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4633028"	""	"0"	"314.39"	"0"	"2.11"	"24"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](NC(=O)C4CC4)CC3)c12"	"IC50"	"'='"	"2100.0"	"nM"	"5.68"	""	""	"UO_0000065"	"18.06"	"0.34"	"3.57"	"6.26"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4638808"	""	"0"	"350.44"	"0"	"1.67"	"30"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](NS(=O)(=O)C4CC4)CC3)c12"	"IC50"	"'='"	"2500.0"	"nM"	"5.60"	""	""	"UO_0000065"	"15.99"	"0.32"	"3.93"	"5.20"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL1081846"	""	"0"	"396.33"	"0"	"2.92"	"6g"	"O=c1[nH]c2cnc(-n3cnc4ccc(F)cc43)nc2n1Cc1cccc(F)c1F"	"IC50"	"'='"	"1000.0"	"nM"	"6.00"	""	""	"UO_0000065"	"15.14"	"0.28"	"3.08"	"7.37"	"False"	"CHEMBL1102456"	"Inhibition of human JAK2 (532-1132) by time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154364"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1078276"	""	"0"	"437.57"	"0"	"4.24"	"14"	"CS(=O)(=O)Nc1ccc(-c2ccnc(Nc3ccc(CN4CCCCC4)cc3)n2)cc1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	""	"UO_0000065"	"18.19"	"0.35"	"3.72"	"9.12"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1078866"	""	"0"	"452.58"	"0"	"3.01"	"19"	"CN1CCN(Cc2cccc(Nc3nccc(-c4ccc(NS(C)(=O)=O)cc4)n3)c2)CC1"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	""	"UO_0000065"	"17.35"	"0.34"	"4.84"	"8.68"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1078165"	""	"0"	"400.49"	"0"	"3.34"	"26"	"N#CCNCc1cccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)c1"	"IC50"	"'='"	"132.0"	"nM"	"6.88"	""	""	"UO_0000065"	"17.18"	"0.31"	"3.54"	"7.99"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1242977"	""	"0"	"479.46"	"1"	"5.95"	"6a"	"CNc1nccc(-c2cccnc2Oc2ccc(NC(=O)c3cccc(C(F)(F)F)c3)cc2C)n1"	"IC50"	"'>'"	"8000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1247968"	"Inhibition of Jak2 by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1240487"	"1"	"Scientific Literature"	"J. Med. Chem."	"2010"	"None"	""
"CHEMBL4476380"	""	"0"	"447.43"	"0"	"0.79"	"10"	"Nc1nc(Nc2ccc(S(N)(=O)=O)cc2)nn1C(=O)Nc1ccc(OCC(=O)O)cc1"	"IC50"	"'='"	"46530.0"	"nM"	"4.33"	""	""	"UO_0000065"	"9.68"	"0.19"	"3.54"	"2.12"	"False"	"CHEMBL4359666"	"Inhibition of wild type full length human JAK2 (1 to 1132 residues) autophosphorylation expressed in HEK293T cells incubated in buffer with compound for 1 hr followed by treatment with enzyme and [gamma32P]-ATP for 15 mins by immunoprecipitation assay based autoradiography"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4354882"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4095629"	""	"0"	"285.35"	"0"	"1.94"	"9"	"C/C=C/C(=O)N1CCC[C@@H](Nc2ncnc3[nH]ccc23)C1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4005719"	"Inhibition of recombinant human GST-tagged cytoplasmic JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by microfluidic assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4004825"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL2208028"	""	"0"	"403.49"	"0"	"3.99"	"9c"	"CC(=O)Nc1ccc(-c2nc(Nc3ccc(N4CCOCC4)cc3)ncc2C)cc1"	"IC50"	"'='"	"608.9"	"nM"	"6.21"	""	""	"UO_0000065"	"15.40"	"0.28"	"2.23"	"7.83"	"False"	"CHEMBL2214785"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT1 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL2207765"	""	"0"	"493.35"	"1"	"5.80"	"6"	"CC(=O)Nc1ccc(-c2ccnc(Nc3cccc(NC(=O)c4c(Cl)cccc4Cl)n3)n2)cc1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2214785"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT1 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL1081376"	""	"0"	"418.84"	"0"	"3.48"	"21g"	"O=c1[nH]c2cnc(-n3cnc4ccccc43)nc2n1C1CCOc2c(Cl)cccc21"	"IC50"	"'='"	"840.0"	"nM"	"6.08"	""	""	"UO_0000065"	"14.51"	"0.28"	"2.60"	"6.70"	"False"	"CHEMBL1102456"	"Inhibition of human JAK2 (532-1132) by time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154364"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1081290"	""	"0"	"376.41"	"1"	"5.26"	"2"	"COc1cc(Nc2nc3cccc(-c4ccccc4)c3o2)cc(OC)c1OC"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	""	"UO_0000065"	"20.79"	"0.38"	"2.56"	"11.90"	"False"	"CHEMBL1107850"	"Inhibition of recombinant GST tagged JAK2 after 60 mins by Caliper mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1155411"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL3890579"	""	"0"	"447.52"	"0"	"3.21"	"BDBM229153"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(CCc2ccccc2)CC1"	"IC50"	"'='"	"156.0"	"nM"	"6.81"	""	"400889"	"UO_0000065"	"15.21"	"0.28"	"3.60"	"6.03"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3954705"	""	"0"	"457.47"	"0"	"1.89"	"BDBM229189"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(C(=O)OC2CCOC2)CC1"	"IC50"	"'='"	"38.0"	"nM"	"7.42"	""	"400926"	"UO_0000065"	"16.22"	"0.31"	"5.53"	"5.00"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3972281"	""	"0"	"424.51"	"0"	"3.22"	"BDBM229201"	"CC(C)COC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)CC1"	"IC50"	"'='"	"102.0"	"nM"	"6.99"	""	"400938"	"UO_0000065"	"16.47"	"0.31"	"3.77"	"5.54"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4110575"	""	"0"	"477.45"	"0"	"1.13"	"BDBM237862"	"N#C[C@@H]1CS(=O)(=O)C[C@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	"414966"	"UO_0000065"	"16.39"	"0.34"	"6.69"	"4.74"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3951449"	""	"0"	"479.59"	"0"	"2.91"	"BDBM229217"	"CN1CCC(COC(=O)N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)CC2)CC1"	"IC50"	"'='"	"318.0"	"nM"	"6.50"	""	"400954"	"UO_0000065"	"13.55"	"0.25"	"3.59"	"5.02"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3981780"	""	"0"	"467.43"	"0"	"2.83"	"BDBM229310"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(C(=O)CCC(F)(F)F)CC1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"401049"	"UO_0000065"	"17.21"	"0.33"	"5.22"	"6.19"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4110851"	""	"0"	"467.89"	"0"	"3.67"	"BDBM229380"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CN(C(=O)Nc2ccc(F)c(Cl)c2)C1"	"IC50"	"'='"	"279.0"	"nM"	"6.55"	""	"401119"	"UO_0000065"	"14.01"	"0.27"	"2.88"	"5.08"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3932064"	""	"0"	"430.92"	"0"	"3.58"	"BDBM229388"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)CCC(N2CC(F)C2)CC1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"401127"	"UO_0000065"	"20.19"	"0.40"	"5.12"	"8.70"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3957937"	""	"0"	"350.40"	"0"	"3.12"	"BDBM198247"	"Fc1cccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)c1"	"IC50"	"'='"	"30.0"	"nM"	"7.52"	""	"352329"	"UO_0000065"	"21.47"	"0.40"	"4.40"	"12.11"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3951060"	""	"0"	"271.32"	"0"	"2.28"	"BDBM198256"	"CO[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"40.0"	"nM"	"7.40"	""	"352338"	"UO_0000065"	"27.27"	"0.51"	"5.12"	"10.86"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3917774"	""	"0"	"255.32"	"0"	"3.04"	"BDBM198259"	"c1cc2c(ncn3nnc(C4CCCCCC4)c23)[nH]1"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	"352341"	"UO_0000065"	"30.89"	"0.57"	"4.85"	"13.40"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3918308"	""	"0"	"334.22"	"0"	"3.27"	"BDBM198267"	"BrC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"352347"	"UO_0000065"	"25.50"	"0.58"	"5.25"	"14.48"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3971898"	""	"0"	"374.44"	"0"	"3.61"	"BDBM198290"	"FC1(F)CCN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)CC1"	"IC50"	"'='"	"100.0"	"nM"	"7.00"	""	"352368"	"UO_0000065"	"18.69"	"0.35"	"3.39"	"11.27"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4109194"	""	"0"	"456.48"	"0"	"2.49"	"BDBM229524"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(C(=O)O[C@@H]2CCOC2)CC1"	"IC50"	"'='"	"62.0"	"nM"	"7.21"	""	"401283"	"UO_0000065"	"15.79"	"0.30"	"4.72"	"5.32"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3973507"	""	"0"	"439.54"	"0"	"3.04"	"BDBM229435"	"N#CCC1(C2C=C(C(N)=O)C(Nc3ccc(F)cc3)=N2)CCC(NC2CCOCC2)CC1"	"IC50"	"'='"	"129.0"	"nM"	"6.89"	""	"401194"	"UO_0000065"	"15.67"	"0.29"	"3.85"	"6.12"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3929898"	""	"0"	"400.46"	"0"	"2.00"	"BDBM229437"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(NCCO)CC1"	"IC50"	"'='"	"981.0"	"nM"	"6.01"	""	"401197"	"UO_0000065"	"15.00"	"0.28"	"4.01"	"4.66"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3922061"	""	"0"	"452.49"	"0"	"2.23"	"BDBM229477"	"N#CC[C@]1(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)F)cc3)n2)CC[C@@H](N)CC1"	"IC50"	"'='"	"33.0"	"nM"	"7.48"	""	"401240"	"UO_0000065"	"16.53"	"0.33"	"5.25"	"4.77"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3970415"	""	"0"	"361.88"	"0"	"2.94"	"BDBM239954"	"Cn1cc(Nc2ncc(Cl)c(NC3CCC4(CCNC4)CC3)n2)cn1"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	"418574"	"UO_0000065"	"21.70"	"0.43"	"4.91"	"9.86"	"False"	"CHEMBL3888834"	"Kinase Assay: JAK2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 100 μM KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC, 10 mM MgAcetate and [γ-33P-ATP](specific activity approx. 500 cpm/pmol, concentration as required). The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of 3% phosphoric acid solution. 10 μL of the reaction is then spotted onto a P30 filtermat and washed three times for 5 minutes in 75 mM phosphoric acid and once in methanol prior to drying and scintillation counting."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886854"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3889517"	""	"0"	"463.52"	"0"	"3.17"	"BDBM229154"	"COc1ccc(CN2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccnc(F)c4)n3)CC2)cc1"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	"400890"	"UO_0000065"	"16.82"	"0.31"	"4.63"	"6.39"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3933592"	""	"0"	"468.41"	"0"	"3.27"	"BDBM229175"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(C(=O)OCC(F)(F)F)CC1"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	"400912"	"UO_0000065"	"16.70"	"0.32"	"4.55"	"6.20"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3953411"	""	"0"	"470.51"	"0"	"2.74"	"BDBM229195"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(C(=O)OCC2CCOC2)CC1"	"IC50"	"'='"	"123.0"	"nM"	"6.91"	""	"400932"	"UO_0000065"	"14.69"	"0.28"	"4.17"	"5.10"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3944827"	""	"0"	"458.49"	"0"	"2.74"	"BDBM229196"	"COCC(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CC1"	"IC50"	"'='"	"40.0"	"nM"	"7.40"	""	"400933"	"UO_0000065"	"16.14"	"0.31"	"4.66"	"5.46"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4113325"	""	"0"	"396.45"	"0"	"2.44"	"BDBM229222"	"CC(C)COC(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"298.0"	"nM"	"6.53"	""	"400961"	"UO_0000065"	"16.46"	"0.31"	"4.09"	"5.17"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL185140"	""	"0"	"389.89"	"1"	"5.31"	"1"	"O=C(CCc1cn(Cc2ccc(Cl)cc2)c2ccccc12)Nc1ccncc1"	"IC50"	"'='"	"133600.0"	"nM"	""	"Outside typical range"	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1227372"	"Inhibition of recombinant JAK2 after 1 hr"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1221237"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL3971389"	""	"0"	"352.32"	"0"	"2.26"	"BDBM198209"	"O=C(CC(F)(F)F)N1CCCC(c2nnn3cnc4[nH]ccc4c23)C1"	"IC50"	"'='"	"76.0"	"nM"	"7.12"	""	"352291"	"UO_0000065"	"20.21"	"0.39"	"4.86"	"8.99"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3936616"	""	"0"	"400.41"	"0"	"4.00"	"BDBM198231"	"FC(F)(F)c1cccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)c1"	"IC50"	"'='"	"28.0"	"nM"	"7.55"	""	"352313"	"UO_0000065"	"18.86"	"0.36"	"3.55"	"12.16"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3943946"	""	"0"	"310.41"	"0"	"2.73"	"BDBM198243"	"c1cc2c(ncn3nnc(C4CCN(C5CCCC5)CC4)c23)[nH]1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"352325"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3899650"	""	"0"	"385.48"	"0"	"4.17"	"BDBM198296"	"Cc1cc(C#N)ccc1NC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"170.0"	"nM"	"6.77"	""	"352374"	"UO_0000065"	"17.56"	"0.32"	"2.60"	"7.15"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3983231"	""	"0"	"350.40"	"0"	"3.88"	"BDBM198324"	"Fc1ccc(NC2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"32.0"	"nM"	"7.50"	""	"352402"	"UO_0000065"	"21.39"	"0.39"	"3.61"	"10.57"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3945740"	""	"0"	"265.28"	"0"	"1.76"	"BDBM198339"	"OCc1ccc(-c2nnn3cnc4[nH]ccc4c23)cc1"	"IC50"	"'='"	"39.0"	"nM"	"7.41"	""	"352417"	"UO_0000065"	"27.93"	"0.51"	"5.65"	"9.37"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3949195"	""	"0"	"385.47"	"0"	"2.31"	"BDBM198370"	"CC(C)(C)OC(=O)NCCN1CCC(c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"940.0"	"nM"	"6.03"	""	"352448"	"UO_0000065"	"15.64"	"0.29"	"3.72"	"6.00"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3891937"	""	"0"	"438.53"	"0"	"3.61"	"BDBM228342"	"C[C@H]1CN(C(=O)OC(C)(C)C)CC[C@]1(CC#N)n1cc(C(N)=O)c(Nc2ccccc2)n1"	"IC50"	"'='"	"487.0"	"nM"	"6.31"	""	"401279"	"UO_0000065"	"14.39"	"0.27"	"2.70"	"5.00"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3941871"	""	"0"	"515.55"	"1"	"2.93"	"BDBM229497"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(NS(=O)(=O)c2cccc(F)c2)CC1"	"IC50"	"'='"	"336.0"	"nM"	"6.47"	""	"401266"	"UO_0000065"	"12.56"	"0.25"	"3.54"	"4.16"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3981942"	""	"0"	"466.50"	"0"	"3.01"	"BDBM229111"	"Cc1cnc(F)c(CN2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccnc(F)c4)n3)CC2)c1"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	"400847"	"UO_0000065"	"16.90"	"0.32"	"4.88"	"6.27"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3975194"	""	"0"	"426.43"	"0"	"1.35"	"BDBM229231"	"CCOC(=O)COC(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"484.0"	"nM"	"6.32"	""	"400970"	"UO_0000065"	"14.81"	"0.28"	"4.97"	"4.14"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4111111"	""	"0"	"424.46"	"0"	"1.97"	"BDBM229234"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CN(C(=O)OC2CCOCC2)C1"	"IC50"	"'='"	"258.0"	"nM"	"6.59"	""	"400973"	"UO_0000065"	"15.52"	"0.29"	"4.62"	"4.86"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4108565"	""	"0"	"395.34"	"0"	"2.73"	"BDBM237868"	"N#C[C@H]1CCOC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(OC(F)(F)F)cc2)n1"	"IC50"	"'='"	"52.0"	"nM"	"7.28"	""	"414987"	"UO_0000065"	"18.42"	"0.36"	"4.55"	"6.32"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3954615"	""	"0"	"429.48"	"0"	"2.67"	"BDBM229263"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)c2ccncc2)CC1"	"IC50"	"'='"	"318.0"	"nM"	"6.50"	""	"401002"	"UO_0000065"	"15.13"	"0.28"	"3.83"	"5.00"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3940215"	""	"0"	"462.94"	"0"	"3.92"	"BDBM229273"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)c2ccccc2Cl)CC1"	"IC50"	"'='"	"115.0"	"nM"	"6.94"	""	"401012"	"UO_0000065"	"14.99"	"0.29"	"3.02"	"5.93"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3930602"	""	"0"	"510.52"	"1"	"4.22"	"BDBM229283"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)Cc2ccc(C(F)(F)F)cc2)CC1"	"IC50"	"'='"	"363.0"	"nM"	"6.44"	""	"401022"	"UO_0000065"	"12.61"	"0.24"	"2.22"	"5.50"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3945985"	""	"0"	"467.43"	"0"	"2.69"	"BDBM229301"	"CC(C(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CC1)C(F)(F)F"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	"401040"	"UO_0000065"	"16.87"	"0.33"	"5.20"	"6.07"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3894596"	""	"0"	"377.40"	"0"	"1.36"	"BDBM237856"	"N#C[C@H]1CS(=O)(=O)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"415012"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3959023"	""	"0"	"437.45"	"0"	"2.99"	"BDBM237829"	"N#C[C@@H]1CCN(Cc2ccc(F)cn2)C[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	"414933"	"UO_0000065"	"17.95"	"0.34"	"4.86"	"6.96"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3926188"	""	"0"	"468.48"	"0"	"4.81"	"BDBM229428"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(Nc2cc(F)ccc2F)CC1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"401179"	"UO_0000065"	"17.55"	"0.33"	"3.41"	"7.56"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3985102"	""	"0"	"463.52"	"0"	"3.31"	"BDBM229479"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(NCc2cccc(O)c2)CC1"	"IC50"	"'='"	"595.0"	"nM"	"6.22"	""	"401242"	"UO_0000065"	"13.43"	"0.25"	"2.92"	"4.39"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3947161"	""	"0"	"472.53"	"0"	"3.47"	"BDBM229495"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(NCc2ccccc2C#N)CC1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"401264"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3948691"	""	"0"	"364.45"	"0"	"3.57"	"BDBM198381"	"Cc1ccc(CNC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)o1"	"IC50"	"'='"	"39.0"	"nM"	"7.41"	""	"352459"	"UO_0000065"	"20.33"	"0.37"	"3.84"	"8.82"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3978202"	""	"0"	"352.36"	"0"	"3.03"	"BDBM198387"	"FC(F)(F)CNC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"8.4"	"nM"	"8.08"	""	"352465"	"UO_0000065"	"22.92"	"0.44"	"5.05"	"11.39"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3963428"	""	"0"	"444.46"	"0"	"3.67"	"BDBM198398"	"OC(CN[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1)(c1ccccc1)C(F)(F)F"	"IC50"	"'='"	"36.0"	"nM"	"7.44"	""	"352476"	"UO_0000065"	"16.75"	"0.32"	"3.77"	"8.17"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3940782"	""	"0"	"394.91"	"0"	"4.12"	"BDBM198401"	"Clc1ccc(CCN[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"37.0"	"nM"	"7.43"	""	"352479"	"UO_0000065"	"18.82"	"0.36"	"3.31"	"10.48"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL1938652"	""	"0"	"367.35"	"0"	"3.80"	"17"	"CNC(=O)c1cnc(N)c2cc(-c3ccc(OC(F)(F)F)cc3)sc12"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	""	"UO_0000065"	"21.56"	"0.43"	"4.12"	"10.25"	"False"	"CHEMBL1941383"	"Inhibition of human recombinant N-terminal GST-tagged JAK2 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308860"	""
"CHEMBL4536419"	""	"0"	"408.39"	"0"	"2.37"	"25"	"Cc1c[nH]c(=O)c(Nc2ncc3[nH]c(=O)n([C@@H]4CCOc5c(F)cccc54)c3n2)c1"	"IC50"	"'='"	"1.9"	"nM"	"8.72"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4463007"	""	"0"	"365.40"	"0"	"2.20"	"34"	"N#CC[C@H]1CC[C@H](n2c(=O)[nH]c3cnc(Nc4ccc[nH]c4=O)nc32)CC1"	"IC50"	"'='"	"1.5"	"nM"	"8.82"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4473572"	""	"0"	"408.51"	"0"	"2.99"	"2"	"CC(C)(O)CNC(=O)Cc1nc2cnc3[nH]ccc3c2n1[C@H]1CC[C@H](CC#N)CC1"	"IC50"	"'='"	"8.6"	"nM"	"8.07"	""	""	"UO_0000065"	"19.74"	"0.37"	"5.08"	"6.74"	"False"	"CHEMBL4404825"	"Inhibition of JAK2-JH1/JH2 domain (532 to 1132 residues) (unknown origin) pre-incubated before NH2-KGGEEEEYFELVKK-CO2 substrate addition and measured after 90 mins by MS analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402578"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL1093749"	""	"0"	"465.53"	"0"	"3.90"	"4"	"CNS(=O)(=O)c1ccc(-c2cccc3ncc(-c4cc(OC)c(OC)c(OC)c4)nc23)cc1"	"IC50"	"'='"	"42.0"	"nM"	"7.38"	""	""	"UO_0000065"	"15.85"	"0.31"	"3.48"	"7.40"	"True"	"CHEMBL1107850"	"Inhibition of recombinant GST tagged JAK2 after 60 mins by Caliper mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1155411"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL3941334"	""	"0"	"486.61"	"0"	"3.42"	"73"	"Cc1cc(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)cs1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3970607"	""	"0"	"502.60"	"1"	"3.12"	"81"	"COc1ccsc1C(=O)N1CCC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3908619"	""	"0"	"522.64"	"1"	"4.27"	"90"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc4ccccc4s3)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3908490"	""	"0"	"499.58"	"0"	"2.48"	"197"	"Cc1cc(NC(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)n(C)n1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3903620"	""	"0"	"550.55"	"1"	"3.86"	"155"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3ccncc3C(F)(F)F)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3948793"	""	"0"	"555.01"	"2"	"5.08"	"211"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(Cc3cc(C(F)(F)F)ccc3Cl)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3983841"	""	"0"	"495.57"	"0"	"3.42"	"229"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(Cc3ccc(C#N)c(F)c3)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL1822515"	""	"0"	"414.51"	"0"	"3.90"	"12"	"COc1ccccc1-c1ccc2cnc(Nc3ccc(N4CCN(C)CC4)cc3)nn12"	"IC50"	"'='"	"0.19"	"nM"	"9.72"	""	""	"UO_0000065"	"23.45"	"0.43"	"5.82"	"16.78"	"False"	"CHEMBL1926252"	"Inhibition of human recombinant JAK2 using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate after 20 mins by fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1921765"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL3975691"	""	"0"	"417.54"	"0"	"2.05"	"BDBM254987"	"CS(=O)(=O)NC[C@H]1CC[C@H](N2CN(C3CC3)C(=O)c3cnc4[nH]ccc4c32)CC1"	"IC50"	"'='"	"4.9"	"nM"	"8.31"	""	"443894"	"UO_0000065"	"19.90"	"0.39"	"6.26"	"8.44"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4754005"	""	"0"	"383.42"	"0"	"2.54"	"28, trans isomer"	"Cn1ccc(-c2cn3nccc3c(-c3cnn([C@]4(CC#N)C[C@@H](C#N)C4)c3)n2)n1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4675820"	"Inhibition of JAK2 homodimer signaling pathway in human whole blood spiked with CD34 +ve cells assessed as reduction in EPO induced STAT5 phosphorylation preincubated for 45 mins followed by EPO addition and measured measured after 15 mins by immunostaining based FACS assay"	"A"	"BAO_0000221"	"tissue-based format"	"Homo sapiens"	"None"	"Blood"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4673239"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 1.0 hr"
"CHEMBL4791733"	""	"0"	"369.39"	"0"	"2.53"	"25, cis isomer"	"N#CC[C@]1(n2cc(-c3nc(-c4cc[nH]n4)cn4nccc34)cn2)C[C@@H](C#N)C1"	"IC50"	"'='"	"31.0"	"nM"	"7.51"	""	""	""	""	""	""	""	"False"	"CHEMBL4675813"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using FITC-KGGEEEEYFELVKK as substrate in presence of ATP at Km by microfluidic assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4673239"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4740831"	""	"0"	"369.39"	"0"	"2.53"	"24, trans isomer"	"N#CC[C@]1(n2cc(-c3nc(-c4cn[nH]c4)cn4nccc34)cn2)C[C@H](C#N)C1"	"IC50"	"'='"	"280.0"	"nM"	"6.55"	""	""	""	""	""	""	""	"False"	"CHEMBL4675813"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using FITC-KGGEEEEYFELVKK as substrate in presence of ATP at Km by microfluidic assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4673239"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL3906070"	""	"0"	"270.34"	"0"	"2.40"	"BDBM254978"	"O=C1NCN(C2CCCCC2)c2c1cnc1[nH]ccc21"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	"443852"	"UO_0000065"	"29.05"	"0.54"	"5.45"	"12.87"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3947499"	""	"0"	"353.47"	"0"	"2.72"	"BDBM255019"	"CN1CN([C@H]2CC[C@H](CNC3CC3)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"71.0"	"nM"	"7.15"	""	"443875"	"UO_0000065"	"20.22"	"0.38"	"4.43"	"11.12"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL1923577"	""	"0"	"458.57"	"0"	"3.65"	"16"	"COc1ccccc1-c1ccc2cnc(Nc3cccc(N4CCN(C[C@H](C)O)CC4)c3)nn12"	"IC50"	"'='"	"0.54"	"nM"	"9.27"	""	""	"UO_0000065"	"20.21"	"0.37"	"5.62"	"11.86"	"False"	"CHEMBL1926252"	"Inhibition of human recombinant JAK2 using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate after 20 mins by fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1921765"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1923580"	""	"0"	"581.72"	"1"	"3.86"	"19"	"C[C@H](O)CN1CCN(c2ccc(Nc3ncc4ccc(-c5cccc(S(=O)(=O)NC(C)(C)C)c5)n4n3)cc2F)CC1"	"IC50"	"'='"	"0.36"	"nM"	"9.44"	""	""	"UO_0000065"	"16.23"	"0.31"	"5.58"	"8.20"	"False"	"CHEMBL1926252"	"Inhibition of human recombinant JAK2 using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate after 20 mins by fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1921765"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1938647"	""	"0"	"410.54"	"0"	"3.91"	"12"	"CC(C)(C)NC(=O)c1cnc(N)c2cc(-c3ccc(N4CCOCC4)cc3)sc12"	"IC50"	"'='"	"1170.0"	"nM"	"5.93"	""	""	"UO_0000065"	"14.45"	"0.28"	"2.02"	"7.37"	"False"	"CHEMBL1941383"	"Inhibition of human recombinant N-terminal GST-tagged JAK2 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308860"	""
"CHEMBL3980883"	""	"0"	"461.61"	"0"	"3.04"	"BDBM255029"	"N#CCCN1CCN(C[C@H]2CC[C@H](N3CN(C4CC4)C(=O)c4cnc5[nH]ccc5c43)CC2)CC1"	"IC50"	"'='"	"790.0"	"nM"	"6.10"	""	"443885"	"UO_0000065"	"13.22"	"0.25"	"3.06"	"7.40"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3892444"	""	"0"	"409.46"	"0"	"3.47"	"BDBM254984"	"CN(CC(F)(F)F)C[C@H]1CC[C@H](N2CN(C)C(=O)c3cnc4[nH]ccc4c32)CC1"	"IC50"	"'='"	"3.1"	"nM"	"8.51"	""	"443891"	"UO_0000065"	"20.78"	"0.40"	"5.04"	"15.34"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3983594"	""	"0"	"446.48"	"0"	"3.55"	"BDBM255038"	"N#CCN1CN([C@H]2CC[C@H](CNC3(C(F)(F)F)CC3)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	"443910"	"UO_0000065"	"17.52"	"0.33"	"4.27"	"8.89"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3892672"	""	"0"	"395.43"	"0"	"3.12"	"BDBM255007"	"CN1CN([C@H]2CC[C@H](CNCC(F)(F)F)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	"443863"	"UO_0000065"	"19.71"	"0.38"	"4.68"	"12.13"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3934061"	""	"0"	"442.31"	"0"	"3.21"	"BDBM254979"	"O=C1NCN([C@H]2CC[C@H](CNCC(F)(F)Br)CC2)c2c1cnc1[nH]ccc21"	"IC50"	"'='"	"2.1"	"nM"	"8.68"	""	"443853"	"UO_0000065"	"19.62"	"0.44"	"5.47"	"11.88"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3967370"	""	"0"	"459.49"	"0"	"2.45"	"BDBM255001"	"CS(=O)(=O)NC[C@H]1CC[C@H](N2CN(CC(F)(F)F)C(=O)c3cnc4[nH]ccc4c32)CC1"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	"443857"	"UO_0000065"	"17.24"	"0.35"	"5.47"	"8.05"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3952221"	""	"0"	"405.52"	"0"	"1.86"	"BDBM255014"	"CN1CN([C@H]2CC[C@H](CN(C)S(C)(=O)=O)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"7.6"	"nM"	"8.12"	""	"443870"	"UO_0000065"	"20.02"	"0.40"	"6.26"	"9.06"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3981038"	""	"0"	"439.48"	"0"	"3.14"	"BDBM255015"	"COCCN1CN([C@H]2CC[C@H](CNCC(F)(F)F)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	"443871"	"UO_0000065"	"17.74"	"0.34"	"4.66"	"10.61"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3916308"	""	"0"	"465.52"	"0"	"3.67"	"BDBM255021"	"O=C1c2cnc3[nH]ccc3c2N([C@H]2CC[C@H](CNCC(F)(F)F)CC2)CN1CC1CCCO1"	"IC50"	"'='"	"5.8"	"nM"	"8.24"	""	"443877"	"UO_0000065"	"17.69"	"0.34"	"4.57"	"11.21"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3892991"	""	"0"	"473.52"	"0"	"2.80"	"BDBM255026"	"CN(C[C@H]1CC[C@H](N2CN(CC(F)(F)F)C(=O)c3cnc4[nH]ccc4c32)CC1)S(C)(=O)=O"	"IC50"	"'='"	"29.0"	"nM"	"7.54"	""	"443882"	"UO_0000065"	"15.92"	"0.32"	"4.74"	"8.41"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3911589"	""	"0"	"443.57"	"0"	"2.54"	"BDBM254988"	"O=C1c2cnc3[nH]ccc3c2N([C@H]2CC[C@H](CN3CCCS3(=O)=O)CC2)CN1C1CC1"	"IC50"	"'='"	"7.6"	"nM"	"8.12"	""	"443895"	"UO_0000065"	"18.30"	"0.36"	"5.58"	"9.06"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3981587"	""	"0"	"338.42"	"0"	"1.74"	"BDBM254989"	"N#CCNC[C@H]1CC[C@H](N2CNC(=O)c3cnc4[nH]ccc4c32)CC1"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"443896"	"UO_0000065"	"24.10"	"0.45"	"6.41"	"8.42"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3893247"	""	"0"	"473.52"	"0"	"2.84"	"BDBM254990"	"CCN1CN([C@H]2CC[C@H](CNS(=O)(=O)CC(F)(F)F)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"6.4"	"nM"	"8.19"	""	"443897"	"UO_0000065"	"17.30"	"0.35"	"5.35"	"8.33"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3913622"	""	"0"	"431.56"	"0"	"2.44"	"BDBM254991"	"CCN1CN([C@H]2CC[C@H](CNS(=O)(=O)C3CC3)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	"443898"	"UO_0000065"	"17.95"	"0.35"	"5.30"	"7.87"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3896113"	""	"0"	"367.45"	"0"	"2.90"	"BDBM255032"	"CN1CN([C@H]2CC[C@H](COCCC#N)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"1.9"	"nM"	"8.72"	""	"443904"	"UO_0000065"	"23.73"	"0.44"	"5.82"	"10.23"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4778704"	""	"0"	"441.42"	"0"	"2.48"	"11"	"Cn1cc(-c2cn3nccc3c(-c3cnn(C4(CC#N)CN(CC(F)(F)F)C4)c3)n2)cn1"	"IC50"	"'='"	"65.0"	"nM"	"7.19"	""	""	""	""	""	""	""	"False"	"CHEMBL4675813"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using FITC-KGGEEEEYFELVKK as substrate in presence of ATP at Km by microfluidic assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4673239"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL388978"	"STAUROSPORINE"	"0"	"466.54"	"0"	"4.35"	"Staurosporine"	"CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4c(c5c6ccccc6n2c5c31)C(=O)NC4"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	""	"UO_0000065"	"18.65"	"0.34"	"4.35"	"12.53"	"True"	"CHEMBL4431266"	"Inhibition of human recombinant JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate by LANCE assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4428138"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2016"	"None"	""
"CHEMBL3354187"	""	"0"	"432.53"	"0"	"4.16"	"6"	"COC1CCN(c2nccc(Nc3cc4c(cn3)cc(-c3cn[nH]c3)n4C(C)C)n2)CC1"	"IC50"	"'='"	"154.0"	"nM"	"6.81"	""	""	"UO_0000065"	"15.75"	"0.29"	"2.65"	"7.04"	"False"	"CHEMBL3375809"	"Inhibition of Jak2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351701"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL1789941"	"RUXOLITINIB"	"4"	"306.37"	"0"	"3.47"	"1"	"N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"4.1"	"nM"	"8.39"	""	""	"UO_0000065"	"27.38"	"0.50"	"4.92"	"10.08"	"False"	"CHEMBL4429697"	"Inhibition of recombinant human C-terminal 6His-tagged JAK2 (808 to end amino acids) expressed in Sf21 cells measured after 1 hr in presence of ATP by TR-FRET assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4428074"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2016"	"CHEMBL4106362"	""
"CHEMBL3593777"	""	"0"	"379.40"	"0"	"1.96"	"4"	"N#Cc1ccc(N2CC[C@@H](Nc3c(C(N)=O)cnc4[nH]ccc34)[C@@H](F)C2)nc1"	"IC50"	"'='"	"3.2"	"nM"	"8.49"	""	""	"UO_0000065"	"22.39"	"0.41"	"6.53"	"6.87"	"False"	"CHEMBL4429528"	"Inhibition of human JAK2 assessed as reduction in phosphorylation of Biotin-Lyn-Substrate-2 after 1 hr in presence of ATP by ELISA"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4428070"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2016"	"None"	""
"CHEMBL4556463"	""	"0"	"423.91"	"0"	"2.36"	"8g"	"O=C(CCCCCCn1cc(Nc2ncc(Cl)c(N3CCOCC3)n2)cn1)NO"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	""	"UO_0000065"	"18.16"	"0.36"	"5.34"	"6.56"	"False"	"CHEMBL4347596"	"Inhibition of recombinant human JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate measured after 60 mins by LANCE assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4346670"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4636371"	""	"0"	"231.30"	"0"	"2.61"	"7"	"Cc1[nH]nc2[nH]c(=O)cc(C3CCCCC3)c12"	"IC50"	"'='"	"1300.0"	"nM"	"5.89"	""	""	"UO_0000065"	"25.45"	"0.47"	"3.28"	"9.56"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4636220"	""	"0"	"243.31"	"0"	"2.46"	"12"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3C[C@H]4CC[C@@H]3C4)c12"	"IC50"	"'='"	"430.0"	"nM"	"6.37"	""	""	"UO_0000065"	"26.17"	"0.48"	"3.91"	"10.35"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4636368"	""	"0"	"246.31"	"0"	"1.54"	"32"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](N)CC3)c12"	"IC50"	"'='"	"18000.0"	"nM"	"4.75"	""	""	"UO_0000065"	"19.26"	"0.36"	"3.20"	"5.42"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL3655081"	"ABROCITINIB"	"3"	"323.42"	"0"	"1.25"	"Abrocitinib"	"CCCS(=O)(=O)N[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"36.0"	"nM"	"7.44"	""	""	"UO_0000065"	"23.02"	"0.46"	"6.19"	"8.18"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4517840"	""	"0"	"392.46"	"0"	"2.78"	"14"	"Cc1cnc(NC(=O)C2CC2)nc1-c1c[nH]c2c(NC(=O)CN(C)C)cccc12"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4406243"	"Inhibition of recombinant human N-terminal GST-tagged JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-labeled GEEPLYWSFPAKKK-NH2 peptide as substrate after 10 mins in presence of 5 mM ATP by caliper mobility shift assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402602"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4450982"	""	"0"	"503.61"	"1"	"2.99"	"17"	"COc1nn(C)cc1Nc1ncc(C)c(-c2c[nH]c3c(NC(=O)[C@@H](C)N4CCN(C)CC4)cccc23)n1"	"IC50"	"'='"	"5400.0"	"nM"	"5.27"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4406243"	"Inhibition of recombinant human N-terminal GST-tagged JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-labeled GEEPLYWSFPAKKK-NH2 peptide as substrate after 10 mins in presence of 5 mM ATP by caliper mobility shift assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402602"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4277098"	""	"0"	"392.49"	"0"	"0.44"	"56"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(S(=O)(=O)N2CCOCC2)CC12CC2"	"IC50"	"'='"	"260.0"	"nM"	"6.58"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4295175"	""	"0"	"337.38"	"0"	"2.29"	"17"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(C(=O)c2ccco2)CC12CC2"	"IC50"	"'='"	"930.0"	"nM"	"6.03"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4285042"	""	"0"	"410.91"	"0"	"4.05"	"35"	"Cc1ccc(NC(=O)N2C[C@H](N(C)c3ncnc4[nH]ccc34)C3(CC3)C2)cc1Cl"	"IC50"	"'='"	"1300.0"	"nM"	"5.89"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL3301607"	"FILGOTINIB"	"4"	"425.51"	"0"	"1.98"	"Filgotinib"	"O=C(Nc1nc2cccc(-c3ccc(CN4CCS(=O)(=O)CC4)cc3)n2n1)C1CC1"	"IC50"	"'='"	"28.0"	"nM"	"7.55"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4280523"	""	"0"	"431.33"	"0"	"4.40"	"32"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC12CC2"	"IC50"	"'='"	"1300.0"	"nM"	"5.89"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4291528"	""	"0"	"431.33"	"0"	"4.40"	"33"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(C(=O)Nc2cc(Cl)ccc2Cl)CC12CC2"	"IC50"	"'='"	"2800.0"	"nM"	"5.55"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4101374"	""	"0"	"357.44"	"0"	"1.90"	"4"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)c2ccccc2)C1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4059894"	""	"0"	"337.45"	"0"	"1.50"	"22"	"CCCNS(=O)(=O)C[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4065613"	""	"0"	"339.42"	"0"	"0.49"	"33"	"COCCS(=O)(=O)N[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'>'"	"15606.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3622821"	"UPADACITINIB"	"4"	"380.37"	"0"	"2.91"	"Upadacitinib"	"CC[C@@H]1CN(C(=O)NCC(F)(F)F)C[C@@H]1c1cnc2cnc3[nH]ccc3n12"	"IC50"	"'='"	"600.0"	"nM"	"6.22"	""	""	"UO_0000065"	""	""	""	""	"True"	"CHEMBL4258533"	"Inhibition of JAK2 (unknown origin) by cell-based assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL1789941"	"RUXOLITINIB"	"4"	"306.37"	"0"	"3.47"	"2"	"N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"60.0"	"nM"	"7.22"	""	""	"UO_0000065"	"23.57"	"0.43"	"3.75"	"8.68"	"False"	"CHEMBL4145181"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4138312"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4173835"	""	"0"	"496.64"	"0"	"3.35"	"13"	"Cc1cnc(Nc2cc(N3C[C@H](C)N[C@H](C)C3)cc(S(C)(=O)=O)c2)nc1Nc1cccc(CO)c1"	"IC50"	"'='"	"996.0"	"nM"	"6.00"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4145184"	"Inhibition of recombinant human JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate after 10 mins by caliper assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4138312"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4169221"	""	"0"	"385.49"	"0"	"3.17"	"24; AZ-3"	"CC[C@@H](C)Nc1nc(Nc2cc(N3C[C@@H]4C[C@H]3CN4C)cnc2F)ncc1C"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4145184"	"Inhibition of recombinant human JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate after 10 mins by caliper assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4138312"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3955496"	""	"0"	"256.31"	"0"	"2.55"	"BDBM198201"	"O=c1[nH]c(C2CCCCC2)c2c3cc[nH]c3ncn12"	"IC50"	"'='"	"46.0"	"nM"	"7.34"	""	"351823"	"UO_0000065"	"28.63"	"0.53"	"4.79"	"11.13"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3891204"	""	"0"	"213.24"	"0"	"1.87"	"BDBM198260"	"c1cc2c(ncn3nnc(C4CCC4)c23)[nH]1"	"IC50"	"'='"	"200.0"	"nM"	"6.70"	""	"352342"	"UO_0000065"	"31.42"	"0.57"	"4.83"	"11.38"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3896777"	""	"0"	"388.50"	"0"	"1.61"	"BDBM198281"	"O=S1(=O)CCN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)CC1"	"IC50"	"'='"	"26.0"	"nM"	"7.58"	""	"352359"	"UO_0000065"	"19.52"	"0.38"	"5.98"	"7.88"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3895546"	""	"0"	"342.42"	"0"	"2.92"	"BDBM198287"	"F[C@H]1CCN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C1"	"IC50"	"'='"	"41.0"	"nM"	"7.39"	""	"352365"	"UO_0000065"	"21.57"	"0.40"	"4.47"	"11.89"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3970198"	""	"0"	"338.46"	"0"	"3.22"	"BDBM198289"	"CC1(C)CN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C1"	"IC50"	"'='"	"210.0"	"nM"	"6.68"	""	"352367"	"UO_0000065"	"19.73"	"0.36"	"3.46"	"10.75"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3976885"	""	"0"	"414.44"	"1"	"5.01"	"BDBM198292"	"FC(F)(F)c1ccc(NC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"420.0"	"nM"	"6.38"	""	"352370"	"UO_0000065"	"15.39"	"0.29"	"1.37"	"8.99"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3949323"	""	"0"	"392.48"	"0"	"3.85"	"BDBM198304"	"Fc1ccc(CCNC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"27.0"	"nM"	"7.57"	""	"352382"	"UO_0000065"	"19.28"	"0.36"	"3.72"	"10.68"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4290689"	""	"0"	"491.59"	"1"	"5.38"	"51"	"CC(=O)Nc1ccc(-c2nc(Nc3cccc(OCCCCCCCC(=O)NO)c3)ncc2C)cc1"	"IC50"	"'='"	"2.93"	"nM"	"8.53"	""	""	"UO_0000065"	"17.36"	"0.32"	"3.15"	"6.80"	"False"	"CHEMBL4268221"	"Inhibition of human JAK2 using poly(Glu:Tyr)(4:1) as substrate preincubated for 20 mins followed by [gamma33P]ATP addition measured after 120 mins by ion exchange filter paper method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4265943"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2018"	"None"	""
"CHEMBL4290748"	""	"0"	"485.97"	"0"	"4.29"	"45h"	"CC(=O)Nc1ccc(-c2ccnc(Nc3ccc(OCCCCCC(=O)NO)cc3)n2)cc1.Cl"	"IC50"	"'='"	"33.0"	"nM"	"7.48"	""	""	"UO_0000065"	"16.64"	"0.31"	"3.19"	"5.96"	"False"	"CHEMBL4268221"	"Inhibition of human JAK2 using poly(Glu:Tyr)(4:1) as substrate preincubated for 20 mins followed by [gamma33P]ATP addition measured after 120 mins by ion exchange filter paper method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4265943"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2018"	"None"	""
"CHEMBL4290297"	""	"0"	"402.50"	"0"	"3.60"	"64f"	"CC(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCN(C)CC4)cc3)n2)cc1"	"IC50"	"'='"	"7.9"	"nM"	"8.10"	""	""	"UO_0000065"	"20.13"	"0.37"	"4.50"	"11.04"	"False"	"CHEMBL4268221"	"Inhibition of human JAK2 using poly(Glu:Tyr)(4:1) as substrate preincubated for 20 mins followed by [gamma33P]ATP addition measured after 120 mins by ion exchange filter paper method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4265943"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2018"	"None"	""
"CHEMBL4574929"	""	"0"	"369.51"	"0"	"3.80"	"12o"	"CC(Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)C1CCCCC1"	"IC50"	"'='"	"3400.0"	"nM"	"5.47"	""	""	"UO_0000065"	"14.80"	"0.28"	"1.67"	"7.01"	"False"	"CHEMBL4341687"	"Inhibition of human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr by Z'-LYTE assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340536"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2019"	"CHEMBL3308860"	""
"CHEMBL4470100"	""	"0"	"449.36"	"1"	"5.07"	"12d"	"CC(Nc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl"	"IC50"	"'='"	"126.0"	"nM"	"6.90"	""	""	"UO_0000065"	"15.35"	"0.31"	"1.83"	"8.54"	"False"	"CHEMBL4341687"	"Inhibition of human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr by Z'-LYTE assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340536"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2019"	"CHEMBL3308860"	""
"CHEMBL3983078"	""	"0"	"339.43"	"0"	"2.44"	"BDBM198236"	"c1cc2c(ncn3nnc(C4CCN(Cc5cncs5)CC4)c23)[nH]1"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	"352318"	"UO_0000065"	"23.23"	"0.45"	"5.45"	"10.51"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4467503"	""	"0"	"405.42"	"0"	"1.12"	"6"	"N#Cc1ccc2ncc(-c3ncc4c(n3)n(C3CCOCC3)c(=O)n4CCO)n2c1"	"IC50"	"'='"	"77.0"	"nM"	"7.11"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4441500"	""	"0"	"432.49"	"0"	"1.69"	"12"	"CN(C)CCn1c(=O)n(C2CCOCC2)c2nc(-c3cnc4ccc(C#N)cn34)ncc21"	"IC50"	"'='"	"800.0"	"nM"	"6.10"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4562564"	""	"0"	"353.43"	"0"	"1.54"	"24"	"Cn1cc(Nc2nccc(N3C[C@H]4CC[C@H](C3)N4C(=O)C3CC3)n2)cn1"	"IC50"	"'='"	"684.0"	"nM"	"6.17"	""	""	"UO_0000065"	"17.44"	"0.32"	"4.62"	"7.79"	"False"	"CHEMBL4411595"	"Inhibition of human JAK2 using fluorescence labeled peptide as substrate and using 1 mM ATP by microfluidic based mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4411260"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4471304"	""	"0"	"389.41"	"0"	"1.79"	"25"	"Cn1cc(Nc2nccc(N3C[C@H]4CC[C@H](C3)N4C(=O)[C@H]3CC3(F)F)n2)cn1"	"IC50"	"'='"	"5655.0"	"nM"	"5.25"	""	""	"UO_0000065"	"13.48"	"0.26"	"3.46"	"6.63"	"False"	"CHEMBL4411592"	"Inhibition of JAK2 homodimer signaling pathway in human spiked CD34 +ve cells of whole blood assessed as reduction in EPO induced STAT5 phosphorylation preincubated for 45 mins followed by EPO addition and measured measured after 15 mins by FACS assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4411260"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4580985"	""	"0"	"371.42"	"0"	"1.68"	"17"	"Cn1cc(Nc2ncc(F)c(N3C[C@H]4CC[C@H](C3)N4C(=O)C3CC3)n2)cn1"	"IC50"	"'='"	"6285.0"	"nM"	"5.20"	""	""	"UO_0000065"	"14.00"	"0.26"	"3.52"	"6.57"	"False"	"CHEMBL4411592"	"Inhibition of JAK2 homodimer signaling pathway in human spiked CD34 +ve cells of whole blood assessed as reduction in EPO induced STAT5 phosphorylation preincubated for 45 mins followed by EPO addition and measured measured after 15 mins by FACS assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4411260"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4101374"	""	"0"	"357.44"	"0"	"1.90"	"4"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)c2ccccc2)C1"	"IC50"	"'='"	"413.0"	"nM"	"6.38"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4100431"	""	"0"	"295.37"	"0"	"0.47"	"5"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(C)(=O)=O)C1"	"IC50"	"'='"	"1290.0"	"nM"	"5.89"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3655080"	""	"0"	"363.37"	"0"	"1.41"	"8"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)CC(F)(F)F)C1"	"IC50"	"'='"	"381.0"	"nM"	"6.42"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4101725"	""	"0"	"323.42"	"0"	"1.25"	"26"	"CCCS(=O)(=O)N[C@H]1C[C@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'>'"	"9297.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4087961"	""	"0"	"337.45"	"0"	"1.64"	"27"	"CCCCS(=O)(=O)N[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"788.0"	"nM"	"6.10"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4059667"	""	"0"	"321.41"	"0"	"1.01"	"28"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)C2CC2)C1"	"IC50"	"'='"	"770.0"	"nM"	"6.11"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL2322141"	""	"0"	"241.30"	"0"	"2.65"	"41"	"c1cc2c(ncc3nnc(C4CCCCC4)n32)[nH]1"	"IC50"	"'='"	"90.0"	"nM"	"7.05"	""	""	"UO_0000065"	"29.20"	"0.53"	"4.40"	"11.97"	"False"	"CHEMBL2327345"	"Inhibition of JAK2 (unknown origin) after 2.5 hrs by time-resolved fluorescence resonance energy transfer assay in presence of 1 uM ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321825"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL4084173"	""	"0"	"505.40"	"1"	"3.76"	"13f"	"NC(=O)c1cnn2cccc2c1NCc1cccc(NC(=O)COc2c(F)c(F)c(F)c(F)c2F)c1"	"IC50"	"'>'"	"2000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4047228"	"Inhibition of GST-tagged JAK2 (unknown origin) using fluoresceinated peptide as substrate after 3 hrs by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4043231"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4562491"	""	"0"	"421.93"	"0"	"3.52"	"8h"	"O=C(CCCCCCn1cc(Nc2ncc(Cl)c(N3CCCCC3)n2)cn1)NO"	"IC50"	"'='"	"50.0"	"nM"	"7.30"	""	""	"UO_0000065"	"17.30"	"0.34"	"3.78"	"6.75"	"False"	"CHEMBL4347596"	"Inhibition of recombinant human JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate measured after 60 mins by LANCE assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4346670"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4634073"	""	"0"	"532.60"	"1"	"4.31"	"3"	"COC(=O)Nc1ccc(-c2c(OC3CCN(C)CC3)nc3c(-c4ccc(OC)c(OC)c4)cnn3c2N)cc1"	"IC50"	"'='"	"84.0"	"nM"	"7.08"	""	""	"UO_0000065"	"13.29"	"0.25"	"2.77"	"5.64"	"False"	"CHEMBL4605806"	"Inhibition of JAK2 (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction in cell viability incubated for 48 hrs by brightglo-luciferase reporter gene assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4602715"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2020"	"CHEMBL3307634"	""
"CHEMBL1934342"	""	"0"	"504.62"	"1"	"3.21"	"3h"	"CS(=O)(=O)c1ccc(-c2ccc3cnc(Nc4ccc(C5CCN(CC(N)=O)CC5)cc4)nn23)cc1"	"IC50"	"'='"	"29.0"	"nM"	"7.54"	""	""	"UO_0000065"	"14.94"	"0.29"	"4.33"	"6.14"	"False"	"CHEMBL1936009"	"Inhibition of JAK2 in GM-CSF-stimulated human TF1 cells preincubated for 1 hr prior to challenge"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3307972"	""
"CHEMBL1934353"	""	"0"	"568.10"	"1"	"3.85"	"14b"	"CN(c1ccccc1-c1cc(Cl)c2cnc(Nc3ccc(C4CCN(CC(N)=O)CC4)cc3)nn12)S(C)(=O)=O"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	""	"UO_0000065"	"13.94"	"0.28"	"4.07"	"6.29"	"False"	"CHEMBL1936009"	"Inhibition of JAK2 in GM-CSF-stimulated human TF1 cells preincubated for 1 hr prior to challenge"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3307972"	""
"CHEMBL3911929"	""	"0"	"475.55"	"1"	"5.12"	"38"	"O=C(O)CCCCOc1ccc2cc1COC/C=C/COCc1cccc(c1)-c1ccnc(n1)N2"	"IC50"	"'<'"	"39.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3877345"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3877241"	"1"	"Scientific Literature"	"J Med Chem"	"2016"	"None"	""
"CHEMBL3930290"	""	"0"	"378.39"	"0"	"2.83"	"BDBM228736"	"C#CCN(c1c(F)cc(C#N)cc1F)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399664"	"UO_0000065"	"27.11"	"0.50"	"7.43"	"14.28"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3896837"	""	"0"	"508.99"	"1"	"3.93"	"BDBM228757"	"CN(c1ccc(C(=O)NC(CO)c2ccc(Cl)cc2)cc1F)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399687"	"UO_0000065"	"20.16"	"0.39"	"6.33"	"10.54"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3702972"	""	"0"	"484.50"	"0"	"2.86"	"BDBM147680"	"CCNC1CCC(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	"285613"	"UO_0000065"	"16.43"	"0.33"	"5.10"	"5.57"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651601"	""	"0"	"375.48"	"0"	"3.73"	"BDBM103733"	"O=C(Nc1nc2cccc(-c3ccc(CN4CCCCC4)cc3)n2n1)C1CC1"	"IC50"	"'='"	"6449.0"	"nM"	"5.19"	""	"221718"	"UO_0000065"	"13.82"	"0.25"	"1.46"	"8.30"	"False"	"CHEMBL3707887"	"Inhibition Assay: In vitro inhibition assay using various enzyme."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638964"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647834"	""	"0"	"479.50"	"0"	"3.54"	"BDBM147941"	"CC(C)(c1ccc(Nc2nn([C@H]3CC[C@@](C)(O)C[C@@H]3C#N)cc2C(N)=O)cc1)C(O)C(F)(F)F"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"285875"	"UO_0000065"	"17.51"	"0.34"	"4.86"	"6.12"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699485"	""	"0"	"432.50"	"0"	"3.89"	"BDBM147500"	"N#C[C@H]1CC[C@@H](NCc2ccccc2)C[C@@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"170.0"	"nM"	"6.77"	""	"285427"	"UO_0000065"	"15.65"	"0.29"	"2.88"	"6.22"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645094"	""	"0"	"443.56"	"0"	"3.85"	"BDBM99868"	"COc1ccccc1CNc1cccn2nc(Nc3ccc(N4CCN(C)CC4)cc3)nc12"	"IC50"	"'='"	"12.26"	"nM"	"7.91"	""	"216536"	"UO_0000065"	"17.84"	"0.33"	"4.06"	"11.31"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3665188"	""	"0"	"489.67"	"0"	"3.78"	"BDBM112583"	"CSc1ncc(-c2cnc3[nH]ccc3n2)c(N[C@H]2CCCN(S(=O)(=O)CCC(C)(C)C)C2)n1"	"IC50"	"'='"	"0.0293"	"nM"	"10.53"	""	"233820"	"UO_0000065"	"21.51"	"0.44"	"6.75"	"9.02"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642350"	""	"0"	"491.62"	"0"	"3.29"	"BDBM99626"	"CN1CCN(c2ccc(Nc3nc4c(-c5cccc(N(C)S(C)(=O)=O)c5)cccn4n3)cc2)CC1"	"IC50"	"'='"	"18.68"	"nM"	"7.73"	""	"216316"	"UO_0000065"	"15.72"	"0.30"	"4.44"	"8.98"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3650977"	""	"0"	"308.34"	"0"	"2.77"	"BDBM153151"	"CCOC(=O)c1c[nH]c2ncnc(-c3ccc4c(c3)CCN4)c12"	"IC50"	"'='"	"35.0"	"nM"	"7.46"	""	"294099"	"UO_0000065"	"24.18"	"0.44"	"4.69"	"9.33"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3658116"	""	"0"	"581.64"	"1"	"4.76"	"BDBM148433"	"Cc1ccc(NC(=O)CCC(F)(F)F)cc1N1CCc2nc(Nc3ccc(C(=O)N4CCN(C)CC4)cc3)ncc2C1"	"IC50"	"'='"	"46.0"	"nM"	"7.34"	""	"286800"	"UO_0000065"	"12.61"	"0.24"	"2.58"	"7.83"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3650681"	""	"0"	"367.41"	"0"	"2.33"	"BDBM148065"	"N#C[C@H]1CCC2(C[C@@H]1n1cc(C(N)=O)c(Nc3ccccc3)n1)OCCO2"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"285987"	"UO_0000065"	"22.86"	"0.42"	"6.07"	"7.29"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3650990"	""	"0"	"364.41"	"0"	"3.71"	"BDBM153165"	"C=C(CC)C(=O)Nc1cccc(-c2ncnc3[nH]cc(C(=O)OCC)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294113"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665157"	""	"0"	"401.50"	"0"	"2.03"	"BDBM112550"	"CCCS(=O)(=O)N1CCC[C@H](Nc2ncccc2-c2cnc3[nH]ncc3n2)C1"	"IC50"	"'='"	"0.8331"	"nM"	"9.08"	""	"233788"	"UO_0000065"	"22.61"	"0.44"	"7.05"	"7.78"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652340"	""	"0"	"421.57"	"0"	"2.39"	"BDBM113151"	"COC[C@H]1CCCN1S(=O)(=O)C[C@H]1CC[C@H](N(C)c2ncnc3[nH]ccc23)CC1"	"IC50"	"'='"	"56.2"	"nM"	"7.25"	""	"234594"	"UO_0000065"	"17.20"	"0.34"	"4.86"	"7.93"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675943"	""	"0"	"371.39"	"0"	"3.23"	"BDBM127694"	"CC1(C)CC[C@H](c2cc(F)ccc2F)N1c1ccn2ncc(C(N)=O)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258368"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675998"	""	"0"	"394.45"	"0"	"3.13"	"BDBM127751"	"C[C@H](NC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cncc(F)c3)nc12)C1CC1"	"IC50"	"'='"	"759.0"	"nM"	"6.12"	""	"258425"	"UO_0000065"	"15.51"	"0.29"	"2.99"	"8.11"	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676005"	""	"0"	"408.36"	"0"	"2.90"	"BDBM127758"	"O=C(NCC(F)(F)F)c1cnn2ccc(N3CCC[C@@H]3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258432"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675927"	""	"0"	"427.48"	"0"	"2.20"	"BDBM127676"	"CC(C)(O)CNC(=O)c1cnn2ccc(N3CCCC3c3cc(F)ccc3CO)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258350"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675966"	""	"0"	"380.43"	"0"	"2.89"	"BDBM127718"	"CC1(NC(=O)c2cnn3ccc(N4CCC[C@@H]4c4cncc(F)c4)nc23)CC1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258392"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676043"	""	"0"	"431.44"	"0"	"1.82"	"BDBM127802"	"C[C@H](O)[C@H](CO)NC(=O)c1cnn2ccc(N3CCCC3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258471"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676071"	""	"0"	"455.49"	"0"	"2.84"	"BDBM127832"	"CC1(C)OCC(COc2ccc(F)cc2[C@H]2CCCN2c2ccn3ncc(C(N)=O)c3n2)O1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258500"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676087"	""	"0"	"420.83"	"0"	"1.91"	"BDBM127852"	"O=C(NOCCO)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)cnc3Cl)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258517"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL2181311"	""	"0"	"502.62"	"1"	"4.97"	"22d, 85:15 trans/cis mixture"	"COc1ccc2cc1-c1ccnc(n1)Nc1ccc(OCCN3CCCC3)c(c1)COCC=CCOC2"	"IC50"	"'='"	"330.0"	"nM"	"6.48"	""	""	"UO_0000065"	"12.90"	"0.24"	"1.51"	"8.31"	"False"	"CHEMBL2184201"	"Inhibition of recombinant JAK2 using Poly (Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176955"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL2181324"	""	"0"	"487.60"	"0"	"3.60"	"17e, 85:15 trans/cis mixture"	"OCCN1CCN(c2ccc3cc2COCC=CCOCc2cccc(c2)-c2ccnc(n2)N3)CC1"	"IC50"	"'='"	"84.0"	"nM"	"7.08"	""	""	"UO_0000065"	"14.51"	"0.27"	"3.48"	"8.53"	"False"	"CHEMBL2184201"	"Inhibition of recombinant JAK2 using Poly (Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176955"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL2181316"	""	"0"	"345.40"	"0"	"4.60"	"16b, 85:15 trans/cis mixture"	"C1=CCOc2cccc(c2)Nc2nccc(n2)-c2cccc(c2)OCC1"	"IC50"	"'='"	"230.0"	"nM"	"6.64"	""	""	"UO_0000065"	"19.22"	"0.35"	"2.04"	"11.80"	"False"	"CHEMBL2184201"	"Inhibition of recombinant JAK2 using Poly (Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176955"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL2181315"	""	"0"	"359.43"	"0"	"4.99"	"16a, 85:15 trans/cis mixture"	"C1=CCCOc2cccc(c2)-c2ccnc(n2)Nc2cccc(c2)OCC1"	"IC50"	"'='"	"1200.0"	"nM"	"5.92"	""	""	"UO_0000065"	"16.47"	"0.30"	"0.93"	"10.52"	"False"	"CHEMBL2184201"	"Inhibition of recombinant JAK2 using Poly (Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176955"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL3981673"	""	"0"	"485.53"	"0"	"2.99"	"BDBM255002"	"O=C1c2cnc3[nH]ccc3c2N([C@H]2CC[C@H](CNS(=O)(=O)C3CC3)CC2)CN1CC(F)(F)F"	"IC50"	"'='"	"32.0"	"nM"	"7.50"	""	"443858"	"UO_0000065"	"15.44"	"0.31"	"4.50"	"7.62"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4536380"	""	"0"	"433.47"	"0"	"1.90"	"11"	"CC(C)(O)Cn1c(=O)n(C2CCOCC2)c2nc(-c3cnc4ccc(C#N)cn34)ncc21"	"IC50"	"'='"	"380.0"	"nM"	"6.42"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL3651056"	""	"0"	"373.41"	"0"	"4.02"	"BDBM153233"	"COC(=O)Cc1ccc(OC)c(-c2c[nH]c3ncnc(-c4ccccc4)c23)c1"	"IC50"	"'='"	"93.0"	"nM"	"7.03"	""	"294181"	"UO_0000065"	"18.83"	"0.34"	"3.01"	"9.12"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652323"	""	"0"	"405.57"	"0"	"3.01"	"BDBM113133"	"CC1CCN(S(=O)(=O)C[C@H]2CC[C@H](N(C)c3ncnc4[nH]ccc34)CC2)CC1"	"IC50"	"'='"	"85.1"	"nM"	"7.07"	""	"234576"	"UO_0000065"	"17.43"	"0.34"	"4.06"	"8.60"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL4635464"	""	"0"	"225.25"	"0"	"2.23"	"6"	"Cc1[nH]nc2[nH]c(=O)cc(-c3ccccc3)c12"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL4645113"	""	"0"	"217.27"	"0"	"2.30"	"14"	"O=c1cc(C2CCCCC2)c2c[nH]nc2[nH]1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL4639973"	""	"0"	"350.37"	"0"	"2.36"	"27"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](NC(=O)[C@@H]4CC4(F)F)CC3)c12"	"IC50"	"'>'"	"7000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL3642316"	""	"0"	"463.56"	"0"	"3.38"	"BDBM99588"	"CS(=O)(=O)c1cccc(-c2cccc3nc(Nc4ccc(CN5CCOCC5)cc4)nn23)c1"	"IC50"	"'='"	"4.9"	"nM"	"8.31"	""	"216278"	"UO_0000065"	"17.93"	"0.34"	"4.93"	"9.35"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3689514"	""	"0"	"324.39"	"0"	"1.69"	"BDBM109863"	"CC1CN(C(=O)CC#N)C12CCCN(c1ncnc3[nH]ccc13)C2"	"IC50"	"'='"	"1.7"	"nM"	"8.77"	""	"230594"	"UO_0000065"	"27.03"	"0.50"	"7.08"	"9.86"	"False"	"CHEMBL3705639"	"Inhibition Assay: In the kinase reactions, fused proteins (6His tag-fused hJAK2 kinase domain (aa808-end)) which were coexpressed in Sf21 cells and purified by Ni2+/NTA agarose were used."	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638515"	"37"	"BindingDB Database"	""	"2013"	"CHEMBL4106362"	""
"CHEMBL3703050"	""	"0"	"476.50"	"0"	"3.43"	"BDBM147760"	"C[C@](O)(c1ccc(Nc2nn([C@H]3CC[C@H](N4CCC4)C[C@@H]3C#N)cc2C(N)=O)cc1)C(F)(F)F"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"285694"	"UO_0000065"	"17.11"	"0.33"	"4.72"	"6.78"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665146"	""	"0"	"386.48"	"0"	"2.16"	"BDBM112535"	"Cc1ccc(-c2cnc3[nH]ccc3n2)c(NC2CCCN(S(C)(=O)=O)C2)n1"	"IC50"	"'='"	"0.0464"	"nM"	"10.33"	""	"233774"	"UO_0000065"	"26.74"	"0.52"	"8.17"	"9.95"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647868"	""	"0"	"462.49"	"0"	"4.35"	"BDBM147980"	"N#C[C@H]1C[C@H](OC(=O)Nc2ccccc2)CCC1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	"285914"	"UO_0000065"	"17.05"	"0.32"	"3.54"	"5.84"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642387"	""	"0"	"478.58"	"0"	"2.82"	"BDBM99665"	"CN1Cc2ccc(Nc3nc4c(NCc5cccnc5N(C)S(C)(=O)=O)cccn4n3)cc2C1"	"IC50"	"'='"	"12.82"	"nM"	"7.89"	""	"216355"	"UO_0000065"	"16.49"	"0.32"	"5.07"	"7.32"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3934227"	""	"0"	"456.98"	"0"	"3.79"	"BDBM239971"	"Cc1cc(Nc2ncc(Cl)c(NC3CCC4(CC3)CCN(C(=O)CC#N)CC4)n2)nn1C"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	"418591"	"UO_0000065"	"17.42"	"0.34"	"4.17"	"7.12"	"False"	"CHEMBL3888834"	"Kinase Assay: JAK2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 100 μM KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC, 10 mM MgAcetate and [γ-33P-ATP](specific activity approx. 500 cpm/pmol, concentration as required). The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of 3% phosphoric acid solution. 10 μL of the reaction is then spotted onto a P30 filtermat and washed three times for 5 minutes in 75 mM phosphoric acid and once in methanol prior to drying and scintillation counting."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886854"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3947974"	""	"0"	"437.45"	"0"	"2.99"	"BDBM237830"	"N#C[C@@H]1CCN(Cc2cccnc2F)C[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	"414934"	"UO_0000065"	"18.11"	"0.34"	"4.93"	"7.02"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3904885"	""	"0"	"396.84"	"0"	"3.03"	"BDBM237886"	"N#C[C@@H]1CCOC[C@H]1n1cc(C(N)=O)c(Nc2cnc3cc(Cl)ccc3c2)n1"	"IC50"	"'='"	"118.0"	"nM"	"6.93"	""	"414988"	"UO_0000065"	"17.46"	"0.34"	"3.90"	"5.83"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4114981"	""	"0"	"344.35"	"0"	"1.75"	"BDBM237904"	"C[C@@H]1C[C@H](C#N)[C@@H](n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CO1"	"IC50"	"'='"	"25.0"	"nM"	"7.60"	""	"415006"	"UO_0000065"	"22.08"	"0.42"	"5.85"	"6.40"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3939630"	""	"0"	"442.96"	"0"	"3.48"	"BDBM239961"	"Cn1cc(Nc2ncc(Cl)c(NC3CCC4(CC3)CCN(C(=O)CC#N)CC4)n2)cn1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"418581"	"UO_0000065"	"18.56"	"0.36"	"4.74"	"7.36"	"False"	"CHEMBL3888834"	"Kinase Assay: JAK2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 100 μM KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC, 10 mM MgAcetate and [γ-33P-ATP](specific activity approx. 500 cpm/pmol, concentration as required). The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of 3% phosphoric acid solution. 10 μL of the reaction is then spotted onto a P30 filtermat and washed three times for 5 minutes in 75 mM phosphoric acid and once in methanol prior to drying and scintillation counting."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886854"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3906000"	""	"0"	"429.83"	"0"	"2.82"	"BDBM239969"	"Cn1cc(Nc2ncc(Cl)c(NC3CC4CN(C(=O)C(F)(F)F)CC4C3)n2)cn1"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	"418589"	"UO_0000065"	"18.08"	"0.37"	"4.95"	"8.83"	"False"	"CHEMBL3888834"	"Kinase Assay: JAK2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 100 μM KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC, 10 mM MgAcetate and [γ-33P-ATP](specific activity approx. 500 cpm/pmol, concentration as required). The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of 3% phosphoric acid solution. 10 μL of the reaction is then spotted onto a P30 filtermat and washed three times for 5 minutes in 75 mM phosphoric acid and once in methanol prior to drying and scintillation counting."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886854"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4108063"	""	"0"	"409.43"	"0"	"2.44"	"BDBM237838"	"N#C[C@@H]1CN(Cc2cocn2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"52.0"	"nM"	"7.28"	""	"414942"	"UO_0000065"	"17.79"	"0.33"	"4.84"	"5.78"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3335695"	""	"0"	"389.44"	"0"	"0.54"	"BDBM112587"	"CS(=O)(=O)N1CCC[C@H](Nc2[nH]c(=O)ncc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.1294"	"nM"	"9.89"	""	"233824"	"UO_0000065"	"25.39"	"0.50"	"9.35"	"7.23"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3359928"	""	"0"	"276.32"	"0"	"2.13"	"5h"	"C[C@@]1(F)CCC[C@@H]1Nc1c(C(N)=O)cnn2cccc12"	"IC50"	"'='"	"130.0"	"nM"	"6.89"	""	""	"UO_0000065"	"24.92"	"0.47"	"4.76"	"9.51"	"False"	"CHEMBL3377596"	"Inhibition of JAK2 (unknown origin) by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352641"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL4113249"	""	"0"	"405.41"	"0"	"2.30"	"BDBM237881"	"C[C@](O)(c1ccc(Nc2nn([C@H]3COCC[C@@H]3C#N)cc2C(N)=O)cc1)C(F)F"	"IC50"	"'='"	"0.2"	"nM"	"9.70"	""	"414983"	"UO_0000065"	"23.92"	"0.46"	"7.40"	"7.69"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3895925"	""	"0"	"381.44"	"0"	"2.11"	"BDBM237891"	"CC1(c2ccc(Nc3nn([C@@H]4COCC[C@H]4C#N)cc3C(N)=O)cc2)COC1"	"IC50"	"'='"	"21.0"	"nM"	"7.68"	""	"414993"	"UO_0000065"	"20.13"	"0.37"	"5.57"	"6.67"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4110738"	""	"0"	"330.32"	"0"	"1.36"	"BDBM237894"	"N#C[C@H]1CCOC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(F)nc2)n1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"414996"	"UO_0000065"	"25.13"	"0.47"	"6.94"	"6.98"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4111682"	""	"0"	"330.32"	"0"	"1.36"	"BDBM237905"	"N#C[C@@H]1COCC[C@H]1n1cc(C(N)=O)c(Nc2ccnc(F)c2)n1"	"IC50"	"'='"	"323.0"	"nM"	"6.49"	""	"415008"	"UO_0000065"	"19.65"	"0.37"	"5.13"	"5.46"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL1789941"	"RUXOLITINIB"	"4"	"306.37"	"0"	"3.47"	"Jakafi"	"N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"27.82"	"0.51"	"5.05"	"10.25"	"False"	"CHEMBL3804597"	"Inhibition of human recombinant JAK2 expressed in Sf21 cells assessed as reduction in Ulight-CAGAGAIETDKEYYTVKD phosphorylation pre-incubated before substrate addition and measured after 60 mins by LANCE detection method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797141"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2016"	"CHEMBL4106362"	""
"CHEMBL4473572"	""	"0"	"408.51"	"0"	"2.99"	"2"	"CC(C)(O)CNC(=O)Cc1nc2cnc3[nH]ccc3c2n1[C@H]1CC[C@H](CC#N)CC1"	"IC50"	"'='"	"83.0"	"nM"	"7.08"	""	""	"UO_0000065"	"17.33"	"0.32"	"4.09"	"5.92"	"False"	"CHEMBL4404829"	"Inhibition of JAK2/JAK2 in human PBMC assessed as reduction in GM-CSF-induced STAT5 phosphorylation pre-incubated for 30 mins before GM-CSF stimulation for 30 mins AlphaLISAassay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402578"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4470339"	""	"0"	"293.37"	"0"	"3.87"	"1"	"Cc1nc2cnc3[nH]ccc3c2n1[C@H]1CC[C@H](CC#N)CC1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4404829"	"Inhibition of JAK2/JAK2 in human PBMC assessed as reduction in GM-CSF-induced STAT5 phosphorylation pre-incubated for 30 mins before GM-CSF stimulation for 30 mins AlphaLISAassay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402578"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL3676097"	""	"0"	"424.48"	"0"	"2.44"	"BDBM127862"	"C[C@@H](NC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)cn(C)c3=O)nc12)C1CC1"	"IC50"	"'='"	"311.0"	"nM"	"6.51"	""	"258527"	"UO_0000065"	"15.33"	"0.29"	"4.07"	"7.70"	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3589325"	""	"0"	"384.48"	"0"	"3.84"	"17"	"CN1CCN(c2ccc3c(c2)[nH]c2c(C(N)=O)cc(-c4ccccc4)cc23)CC1"	"IC50"	"'='"	"2.1"	"nM"	"8.68"	""	""	"UO_0000065"	"22.57"	"0.41"	"4.84"	"13.28"	"False"	"CHEMBL3592849"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL4439418"	""	"0"	"418.42"	"0"	"3.78"	"7"	"N#CC[C@H]1CC[C@H](n2c(CC(=O)NCC(F)(F)F)nc3cnc4[nH]ccc4c32)CC1"	"IC50"	"'='"	"5.6"	"nM"	"8.25"	""	""	"UO_0000065"	"19.72"	"0.38"	"4.47"	"8.30"	"False"	"CHEMBL4404825"	"Inhibition of JAK2-JH1/JH2 domain (532 to 1132 residues) (unknown origin) pre-incubated before NH2-KGGEEEEYFELVKK-CO2 substrate addition and measured after 90 mins by MS analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402578"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL3589167"	""	"0"	"468.34"	"0"	"4.87"	"4"	"NC(=O)c1cc(-c2ccc(Cl)cc2Cl)cc2c1[nH]c1ccc(C(=O)N3CCOCC3)cc12"	"IC50"	"'='"	"216.0"	"nM"	"6.67"	""	""	"UO_0000065"	"14.23"	"0.28"	"1.80"	"7.54"	"False"	"CHEMBL3592855"	"Inhibition of JAK2 in human SET2 cells assessed as inhibition of cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3589174"	""	"0"	"399.45"	"0"	"3.56"	"11"	"NC(=O)c1cc(-c2ccccc2)cc2c1[nH]c1cc(C(=O)N3CCOCC3)ccc12"	"IC50"	"'='"	"170.0"	"nM"	"6.77"	""	""	"UO_0000065"	"16.95"	"0.31"	"3.21"	"7.66"	"False"	"CHEMBL3592855"	"Inhibition of JAK2 in human SET2 cells assessed as inhibition of cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3359913"	""	"0"	"288.35"	"0"	"1.39"	"4b"	"CC1(C)[C@H](O)CC[C@H]1Nc1c(C(N)=O)cnn2cccc12"	"IC50"	"'='"	"42.0"	"nM"	"7.38"	""	""	"UO_0000065"	"25.58"	"0.48"	"5.99"	"7.96"	"False"	"CHEMBL3377596"	"Inhibition of JAK2 (unknown origin) by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352641"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3972506"	""	"0"	"316.38"	"0"	"2.44"	"BDBM198300"	"FCCNC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"55.0"	"nM"	"7.26"	""	"352378"	"UO_0000065"	"22.95"	"0.43"	"4.82"	"10.24"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3957990"	""	"0"	"410.47"	"0"	"4.51"	"BDBM198302"	"CC(NC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1)c1ccc(F)c(F)c1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	"352380"	"UO_0000065"	"19.39"	"0.36"	"3.45"	"11.23"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3943994"	""	"0"	"438.56"	"0"	"3.07"	"BDBM198306"	"CS(=O)(=O)c1ccc(CNC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"89.0"	"nM"	"7.05"	""	"352384"	"UO_0000065"	"16.08"	"0.31"	"3.98"	"6.71"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3943501"	""	"0"	"431.54"	"0"	"3.83"	"BDBM198311"	"c1cc2c(ncn3nnc([C@H]4CC[C@H](CNc5ccc(N6CCOCC6)cc5)CC4)c23)[nH]1"	"IC50"	"'='"	"35.0"	"nM"	"7.46"	""	"352389"	"UO_0000065"	"17.28"	"0.32"	"3.63"	"8.94"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3949040"	""	"0"	"384.85"	"0"	"3.78"	"BDBM198357"	"Fc1cc(Cl)ccc1CN1CCC(c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"4.4"	"nM"	"8.36"	""	"352435"	"UO_0000065"	"21.71"	"0.42"	"4.58"	"13.45"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3986377"	""	"0"	"384.85"	"0"	"3.78"	"BDBM198358"	"Fc1cc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)ccc1Cl"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	"352436"	"UO_0000065"	"20.68"	"0.40"	"4.18"	"12.81"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3931226"	""	"0"	"418.40"	"0"	"4.14"	"BDBM198366"	"Fc1cc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)ccc1C(F)(F)F"	"IC50"	"'='"	"30.0"	"nM"	"7.52"	""	"352444"	"UO_0000065"	"17.98"	"0.34"	"3.38"	"12.11"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3904756"	""	"0"	"380.88"	"0"	"4.08"	"BDBM198400"	"Clc1ccc(CN[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"45.0"	"nM"	"7.35"	""	"352478"	"UO_0000065"	"19.29"	"0.37"	"3.27"	"10.36"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3926930"	""	"0"	"320.36"	"0"	"1.33"	"BDBM228713"	"CN(c1ccc(C#N)nn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399632"	"UO_0000065"	"32.03"	"0.58"	"8.93"	"10.51"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3941211"	""	"0"	"329.80"	"0"	"2.12"	"BDBM228716"	"CN(c1ccnc(Cl)n1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399635"	"UO_0000065"	"31.11"	"0.61"	"8.14"	"13.90"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3896481"	""	"0"	"319.37"	"0"	"1.94"	"BDBM228719"	"CN(c1ccc(C#N)cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399639"	"UO_0000065"	"32.12"	"0.58"	"8.32"	"12.11"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3914739"	""	"0"	"361.41"	"0"	"1.65"	"BDBM228739"	"CN(c1cncc(-n2ccnc2)n1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399667"	"UO_0000065"	"28.39"	"0.52"	"8.61"	"11.19"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3984793"	""	"0"	"457.54"	"0"	"2.53"	"BDBM228748"	"CN(c1ccc(C(=O)N[C@H](CO)c2ccccc2)cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399678"	"UO_0000065"	"22.42"	"0.41"	"7.73"	"9.30"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3933796"	""	"0"	"444.51"	"0"	"3.74"	"BDBM228754"	"CN(c1ccc(C(=O)NCc2ccccc2)cc1F)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399684"	"UO_0000065"	"23.08"	"0.42"	"6.52"	"13.30"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3927252"	""	"0"	"287.39"	"0"	"2.81"	"BDBM198269"	"SC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"2.2"	"nM"	"8.66"	""	"352349"	"UO_0000065"	"30.12"	"0.59"	"5.85"	"14.71"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3958601"	""	"0"	"407.50"	"0"	"4.39"	"BDBM198278"	"O=C(OCc1ccccc1)N1CCC(c2[nH]c(=S)n3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"310.0"	"nM"	"6.51"	""	"352357"	"UO_0000065"	"15.97"	"0.31"	"2.12"	"8.30"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3986660"	""	"0"	"444.46"	"0"	"4.57"	"BDBM198303"	"FC(F)(F)Oc1ccc(CNC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"91.0"	"nM"	"7.04"	""	"352381"	"UO_0000065"	"15.84"	"0.30"	"2.47"	"8.79"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3967682"	""	"0"	"360.46"	"0"	"3.46"	"BDBM198316"	"c1ccc(CCNC2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"190.0"	"nM"	"6.72"	""	"352394"	"UO_0000065"	"18.65"	"0.34"	"3.26"	"9.48"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3900189"	""	"0"	"428.46"	"0"	"4.48"	"BDBM198318"	"FC(F)(F)c1cccc(CCNC2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)c1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"352396"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3927316"	""	"0"	"369.47"	"0"	"1.55"	"BDBM198319"	"c1cc2c(ncn3nnc(C4CCC(NCCN5CCOCC5)CC4)c23)[nH]1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"352397"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3922392"	""	"0"	"357.42"	"0"	"3.62"	"BDBM198327"	"N#Cc1ccc(N[C@H]2CC[C@@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"95.0"	"nM"	"7.02"	""	"352405"	"UO_0000065"	"19.65"	"0.36"	"3.40"	"7.42"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3909146"	""	"0"	"390.37"	"0"	"3.60"	"BDBM198342"	"FC(F)(F)c1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)o1"	"IC50"	"'='"	"5.6"	"nM"	"8.25"	""	"352420"	"UO_0000065"	"21.14"	"0.40"	"4.65"	"10.97"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3937067"	""	"0"	"363.45"	"0"	"2.92"	"BDBM198343"	"N#Cc1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)s1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"352421"	"UO_0000065"	"23.11"	"0.44"	"5.48"	"9.78"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3953486"	""	"0"	"368.39"	"0"	"3.26"	"BDBM198365"	"Fc1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cc1F"	"IC50"	"'='"	"23.0"	"nM"	"7.64"	""	"352443"	"UO_0000065"	"20.73"	"0.39"	"4.38"	"12.30"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3907227"	""	"0"	"378.41"	"0"	"3.66"	"BDBM198409"	"O=C(Nc1ccc(F)cc1)[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"352487"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3936927"	""	"0"	"256.31"	"0"	"1.41"	"BDBM198419"	"CN1CCC(c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"352497"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3980737"	""	"0"	"415.45"	"0"	"2.46"	"BDBM229450"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(N2CC(F)C2)CC1"	"IC50"	"'='"	"444.0"	"nM"	"6.35"	""	"401211"	"UO_0000065"	"15.29"	"0.29"	"3.89"	"5.63"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3959005"	""	"0"	"446.53"	"0"	"4.21"	"BDBM229460"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(NCc2ccccc2)CC1"	"IC50"	"'='"	"0.2"	"nM"	"9.70"	""	"401220"	"UO_0000065"	"21.72"	"0.40"	"5.49"	"8.92"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3892599"	""	"0"	"528.59"	"1"	"4.39"	"BDBM229469"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)F)cc3)n2)CCC(Nc2ccccc2)CC1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"401230"	"UO_0000065"	"17.03"	"0.33"	"4.61"	"6.30"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3909605"	""	"0"	"357.39"	"0"	"1.77"	"BDBM229475"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(N)CC1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"401237"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3943909"	""	"0"	"465.51"	"0"	"3.74"	"BDBM228307"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(NCc2ccccc2F)CC1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"401248"	"UO_0000065"	"18.69"	"0.35"	"4.96"	"7.15"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3961060"	""	"0"	"448.51"	"0"	"3.00"	"BDBM229487"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(NCc2ccncc2)CC1"	"IC50"	"'='"	"1004.0"	"nM"	"6.00"	""	"401250"	"UO_0000065"	"13.37"	"0.25"	"3.00"	"4.46"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3943909"	""	"0"	"465.51"	"0"	"3.74"	"BDBM228307"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(NCc2ccccc2F)CC1"	"IC50"	"'='"	"308.0"	"nM"	"6.51"	""	"401258"	"UO_0000065"	"13.99"	"0.26"	"2.77"	"5.35"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3956020"	""	"0"	"481.96"	"0"	"4.25"	"BDBM228309"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(NCc2cccc(Cl)c2)CC1"	"IC50"	"'='"	"1430.0"	"nM"	"5.84"	""	"401260"	"UO_0000065"	"12.13"	"0.23"	"1.59"	"4.80"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3937127"	""	"0"	"465.51"	"0"	"3.74"	"BDBM228311"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(NCc2ccc(F)cc2)CC1"	"IC50"	"'='"	"1078.0"	"nM"	"5.97"	""	"401262"	"UO_0000065"	"12.82"	"0.24"	"2.23"	"4.91"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3895727"	""	"0"	"447.52"	"0"	"3.60"	"BDBM229496"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(NCc2ccccc2)CC1"	"IC50"	"'='"	"735.0"	"nM"	"6.13"	""	"401265"	"UO_0000065"	"13.71"	"0.25"	"2.53"	"5.04"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3965448"	""	"0"	"469.40"	"0"	"2.31"	"BDBM229507"	"N#CC[C@@]1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(C(=O)OCC(F)F)C[C@@H]1F"	"IC50"	"'='"	"0.1"	"nM"	"10.00"	""	"401275"	"UO_0000065"	"21.30"	"0.41"	"7.69"	"7.19"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3593762"	""	"0"	"273.34"	"0"	"1.17"	"7a"	"CN1CCC(Nc2c(C(N)=O)cnc3[nH]ccc23)CC1"	"IC50"	"'='"	"310.0"	"nM"	"6.51"	""	""	"UO_0000065"	"23.81"	"0.44"	"5.34"	"7.48"	"False"	"CHEMBL3594790"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593212"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3593592"	""	"0"	"352.40"	"0"	"1.54"	"26"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1n1c(=O)n(C)c2cnc3[nH]ccc3c21"	"IC50"	"'='"	"7.3"	"nM"	"8.14"	""	""	"UO_0000065"	"23.09"	"0.43"	"6.60"	"8.16"	"False"	"CHEMBL3594576"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate and ATP incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593193"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3593586"	""	"0"	"257.30"	"0"	"1.13"	"9a"	"O=c1[nH]c2cnc3[nH]ccc3c2n1C1CCNCC1"	"IC50"	"'='"	"1300.0"	"nM"	"5.89"	""	""	"UO_0000065"	"22.88"	"0.42"	"4.76"	"7.50"	"False"	"CHEMBL3594576"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate and ATP incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593193"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL1946005"	""	"0"	"483.49"	"1"	"5.16"	"27r"	"CN1C/C=C/CCOc2cccc(c2)-c2ccnc(n2)Nc2cc(cc(NC(=O)C(F)(F)F)c2)C1"	"IC50"	"'='"	"50.0"	"nM"	"7.30"	""	""	"UO_0000065"	"15.10"	"0.28"	"2.14"	"9.20"	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL3785500"	""	"0"	"459.59"	"0"	"4.43"	"3"	"Nc1ncnc2c1c(-c1cccc(OCC34CCC(CC3)O4)c1)cn2[C@H]1C[C@@H](CN2CCC2)C1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3789994"	"Inhibition of JAK2 (unknown origin) in presence of [gamma33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3785066"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3593770"	""	"0"	"360.42"	"0"	"2.61"	"11a"	"N#Cc1ccc(N2CCC(Nc3c(C(N)=O)cnc4[nH]ccc34)CC2)cc1"	"IC50"	"'='"	"49.0"	"nM"	"7.31"	""	""	"UO_0000065"	"20.28"	"0.37"	"4.70"	"6.60"	"False"	"CHEMBL3594790"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593212"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL1947162"	""	"0"	"358.45"	"0"	"4.32"	"26g"	"C1=C/CNCc2cccc(c2)Nc2nccc(n2)-c2cccc(c2)OCC/1"	"IC50"	"'='"	"150.0"	"nM"	"6.82"	""	""	"UO_0000065"	"19.04"	"0.35"	"2.50"	"11.55"	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1944700"	""	"0"	"372.47"	"0"	"4.41"	"26j"	"CN1C/C=C/COCc2cccc(c2)Nc2nccc(n2)-c2cccc(c2)C1"	"IC50"	"'='"	"230.0"	"nM"	"6.64"	""	""	"UO_0000065"	"17.82"	"0.32"	"2.23"	"13.20"	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1947158"	""	"0"	"372.43"	"0"	"4.55"	"49"	"O=C1CC/C=C\COc2cccc(c2)-c2ccnc(n2)Nc2cccc(c2)N1"	"IC50"	"'='"	"1700.0"	"nM"	"5.77"	""	""	"UO_0000065"	"15.49"	"0.28"	"1.22"	"7.58"	"False"	"CHEMBL3856507"	"Inhibition of human recombinant GST-tagged JAK2 expressed in baculovirus expression system"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3856187"	"1"	"Scientific Literature"	"J Med Chem"	"2016"	"None"	""
"CHEMBL495727"	"AT-9283"	"2"	"381.44"	"0"	"2.07"	"10, AT-9283"	"O=C(Nc1c[nH]nc1-c1nc2ccc(CN3CCOCC3)cc2[nH]1)NC1CC1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	""	"UO_0000065"	"23.59"	"0.44"	"6.93"	"8.11"	"False"	"CHEMBL981410"	"Binding affinity to Jak2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154007"	"1"	"Scientific Literature"	"J. Med. Chem."	"2009"	"None"	""
"CHEMBL1945705"	""	"0"	"501.63"	"1"	"4.37"	"27n"	"CN1C/C=C/CCOc2cccc(c2)-c2ccnc(n2)Nc2ccc(OCCN3CCOCC3)c(c2)C1"	"IC50"	"'='"	"120.0"	"nM"	"6.92"	""	""	"UO_0000065"	"13.80"	"0.26"	"2.55"	"9.61"	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1945822"	""	"0"	"553.63"	"2"	"6.06"	"27l"	"FC(F)(F)CN1C/C=C/CCOc2cccc(c2)-c2ccnc(n2)Nc2ccc(OCCN3CCCC3)c(c2)C1"	"IC50"	"'='"	"220.0"	"nM"	"6.66"	""	""	"UO_0000065"	"12.03"	"0.23"	"0.60"	"10.61"	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1287970"	""	"0"	"387.35"	"0"	"2.75"	"16"	"CCOC(=O)c1cccc(Nc2nc(N)nn2C(=O)c2c(F)cccc2F)c1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1292866"	"Inhibition of human recombinant JAK2 by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287810"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1288093"	""	"0"	"394.44"	"0"	"2.54"	"25"	"CCOC(=O)c1cccc(Nc2nc(N)n(C(=O)c3ccc(N(C)C)cc3)n2)c1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1292866"	"Inhibition of human recombinant JAK2 by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287810"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1287883"	""	"0"	"394.36"	"0"	"1.22"	"11"	"Nc1nc(Nc2cccc(S(N)(=O)=O)c2)nn1C(=O)c1c(F)cccc1F"	"IC50"	"'='"	"2500.0"	"nM"	"5.60"	""	""	"UO_0000065"	"14.21"	"0.28"	"4.38"	"3.84"	"False"	"CHEMBL1292866"	"Inhibition of human recombinant JAK2 by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287810"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL3956837"	""	"0"	"561.63"	"1"	"4.25"	"120"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(-c4cccnc4)cc3F)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3978490"	""	"0"	"530.04"	"1"	"4.40"	"161"	"Cc1cccc(Cl)c1NC(=O)N1CCC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3898820"	""	"0"	"495.59"	"0"	"3.75"	"185"	"Cc1ccccc1NC(=O)N1CCC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3908824"	""	"0"	"513.58"	"1"	"3.89"	"187"	"Cc1cc(F)ccc1NC(=O)N1CCC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3979671"	""	"0"	"514.57"	"1"	"3.29"	"199"	"Cc1nc(F)ccc1NC(=O)N1CCC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3902594"	""	"0"	"557.59"	"1"	"3.37"	"207"	"COC(=O)c1cc(F)ccc1NC(=O)N1CCC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3938758"	""	"0"	"508.59"	"1"	"2.69"	"224"	"COc1nc(CN2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)ccc1C#N"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3953383"	""	"0"	"527.61"	"1"	"2.47"	"247"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(S(=O)(=O)c3ccccc3C#N)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3904170"	""	"0"	"538.06"	"1"	"4.61"	"214"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(Cc3cc4ccccc4nc3Cl)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3940789"	""	"0"	"468.59"	"0"	"1.95"	"257"	"CC(C)S(=O)(=O)N1CCC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL4559521"	""	"0"	"394.41"	"0"	"2.95"	"6"	"CCNC(=O)c1cnc(Nc2ccc(F)cn2)cc1Nc1ccccc1C(N)=O"	"IC50"	"'>'"	"2000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4414788"	"Inhibition of JAK2 JH1 domain (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414548"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4530719"	""	"0"	"401.42"	"0"	"2.61"	"29"	"CS(=O)(=O)c1ccccc1Nc1cc(Nc2ccc(F)cn2)ncc1C(N)=O"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	""	"UO_0000065"	"19.29"	"0.38"	"5.13"	"6.09"	"False"	"CHEMBL4414788"	"Inhibition of JAK2 JH1 domain (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414548"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4440718"	""	"0"	"401.47"	"0"	"2.12"	"48"	"[2H]C([2H])([2H])NC(=O)c1nnc(Nc2ccccn2)cc1Nc1ccccc1S(C)(=O)=O"	"IC50"	"'>'"	"50000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4414788"	"Inhibition of JAK2 JH1 domain (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414548"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4444178"	""	"0"	"392.46"	"0"	"1.33"	"47"	"[2H]C([2H])([2H])NC(=O)c1nnc(NC(=O)C2CC2)cc1Nc1ccccc1S(C)(=O)=O"	"IC50"	"'>'"	"50000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4414788"	"Inhibition of JAK2 JH1 domain (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414548"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4550310"	""	"0"	"394.40"	"0"	"0.63"	"31"	"N#CCC(=O)N1CCC[C@H](n2c(=O)[nH]c3cnc(Nc4ccc[nH]c4=O)nc32)C1"	"IC50"	"'='"	"1.7"	"nM"	"8.77"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4526485"	""	"0"	"399.84"	"0"	"2.85"	"35"	"N#CC[C@H]1CC[C@H](n2c(=O)[nH]c3cnc(Nc4cc(Cl)c[nH]c4=O)nc32)CC1"	"IC50"	"'='"	"3.6"	"nM"	"8.44"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4520559"	""	"0"	"424.39"	"0"	"2.07"	"26"	"COc1c[nH]c(=O)c(Nc2ncc3[nH]c(=O)n([C@@H]4CCOc5c(F)cccc54)c3n2)c1"	"IC50"	"'='"	"24.0"	"nM"	"7.62"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL3343039"	""	"0"	"443.46"	"0"	"3.50"	"7c"	"COc1cc2c(Nc3ccc(NC(=O)c4ccccc4)cc3)ncnc2cc1OCC(N)=O"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3380804"	"Inhibition of human JAK2 incubated for 20 mins prior to MgCl2 addition measured after 90 mins by mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351874"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3341771"	""	"0"	"457.45"	"0"	"2.64"	"24a"	"COc1cc(C(=O)Nc2ccc(NC(=O)c3ccccn3)cc2)cc(-c2c[nH]c(=O)[nH]c2=O)c1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3380804"	"Inhibition of human JAK2 incubated for 20 mins prior to MgCl2 addition measured after 90 mins by mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351874"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL4444169"	""	"0"	"418.47"	"0"	"2.87"	"30"	"[2H]C([2H])([2H])NC(=O)c1cnc(Nc2ccc(F)cn2)cc1Nc1ccccc1S(C)(=O)=O"	"IC50"	"'>'"	"50000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4414788"	"Inhibition of JAK2 JH1 domain (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414548"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4437684"	""	"0"	"380.46"	"0"	"1.54"	"11s"	"C=CC(=O)N1CCC(Cn2nc(-c3cc(C)n(C)n3)c3c(N)ncnc32)CC1"	"IC50"	"'='"	"437.0"	"nM"	"6.36"	""	""	"UO_0000065"	"16.72"	"0.31"	"4.82"	"5.90"	"False"	"CHEMBL4402146"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-biotin as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4400567"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4436334"	""	"0"	"366.43"	"0"	"1.47"	"11r"	"C=CC(=O)N1CCC(n2nc(-c3cc(C)n(C)n3)c3c(N)ncnc32)CC1"	"IC50"	"'='"	"642.1"	"nM"	"6.19"	""	""	"UO_0000065"	"16.90"	"0.31"	"4.72"	"5.75"	"False"	"CHEMBL4402146"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-biotin as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4400567"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4455024"	""	"0"	"432.49"	"0"	"2.21"	"11d"	"C=CC(=O)Nc1cccc(Cn2nc(-c3cc(C(C)(C)O)n(C)n3)c3c(N)ncnc32)c1"	"IC50"	"'='"	"102.0"	"nM"	"6.99"	""	""	"UO_0000065"	"16.17"	"0.30"	"4.78"	"5.11"	"False"	"CHEMBL4402146"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-biotin as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4400567"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4460560"	""	"0"	"437.51"	"0"	"1.00"	"11c"	"C=CC(=O)N1CCCC(n2nc(-c3cc(N4CCOCC4)n(C)n3)c3c(N)ncnc32)C1"	"IC50"	"'='"	"13.1"	"nM"	"7.88"	""	""	"UO_0000065"	"18.02"	"0.34"	"6.88"	"6.56"	"False"	"CHEMBL4402146"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-biotin as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4400567"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4576447"	""	"0"	"459.51"	"0"	"1.82"	"11a"	"C=CC(=O)Nc1cccc(Cn2nc(-c3cc(N4CCOCC4)n(C)n3)c3c(N)ncnc32)c1"	"IC50"	"'='"	"160.3"	"nM"	"6.79"	""	""	"UO_0000065"	"14.79"	"0.27"	"4.98"	"5.27"	"False"	"CHEMBL4402146"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-biotin as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4400567"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL3955045"	""	"0"	"486.61"	"0"	"3.42"	"78"	"Cc1ccsc1C(=O)N1CCC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3890357"	""	"0"	"583.66"	"1"	"4.86"	"136"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(-c4nc5ccccc5o4)cc3)CC2)C1"	"IC50"	"'>'"	"100.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3958043"	""	"0"	"541.62"	"1"	"3.46"	"186"	"COc1ccc(OC)c(NC(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)c1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3903569"	""	"0"	"550.55"	"1"	"3.86"	"201"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3ncccc3C(F)(F)F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3899050"	""	"0"	"500.54"	"1"	"2.90"	"58"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(F)c(O)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3938623"	""	"0"	"486.61"	"0"	"3.42"	"79"	"Cc1csc(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)c1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3936415"	""	"0"	"561.63"	"1"	"4.25"	"117"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(-c4ccncc4)c(F)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3977160"	""	"0"	"484.61"	"0"	"3.46"	"145"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CC3CCC(C2)N3C(=O)C2CCCC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3910630"	""	"0"	"519.03"	"1"	"4.59"	"245"	"CC1CC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CCN1Cc1c(F)cccc1Cl"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL4476445"	""	"0"	"361.37"	"0"	"1.66"	"3"	"N#Cc1ccc2ncc(-c3ncc4[nH]c(=O)n(C5CCOCC5)c4n3)n2c1"	"IC50"	"'='"	"74.0"	"nM"	"7.13"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4440240"	""	"0"	"474.53"	"1"	"1.46"	"13"	"N#Cc1ccc2ncc(-c3ncc4c(n3)n(C3CCOCC3)c(=O)n4CCN3CCOCC3)n2c1"	"IC50"	"'='"	"340.0"	"nM"	"6.47"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL2325899"	""	"0"	"272.35"	"0"	"2.61"	"3c"	"CC(C)[C@H](C)NC(=O)c1c[nH]c2ncc(C3CC3)nc12"	"IC50"	"'='"	"32.6"	"nM"	"7.49"	""	""	"UO_0000065"	"27.49"	"0.51"	"4.88"	"10.59"	"False"	"CHEMBL2329570"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 30 mins by scintillation counting analysis in presence of [gamma-33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321829"	"1"	"Scientific Literature"	"J. Med. Chem."	"2013"	"None"	""
"CHEMBL2325912"	""	"0"	"352.40"	"0"	"1.33"	"3n"	"C[C@@H](NC(=O)c1c[nH]c2ncc(C3CC3)nc12)C(=O)N1CCC(C#N)C1"	"IC50"	"'='"	"23.1"	"nM"	"7.64"	""	""	"UO_0000065"	"21.67"	"0.40"	"6.31"	"6.65"	"False"	"CHEMBL2329570"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 30 mins by scintillation counting analysis in presence of [gamma-33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321829"	"1"	"Scientific Literature"	"J. Med. Chem."	"2013"	"None"	""
"CHEMBL3965049"	""	"0"	"520.52"	"1"	"3.47"	"49"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3c(F)cc(F)cc3F)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3931739"	""	"0"	"514.57"	"1"	"3.20"	"38"	"COc1ccc(F)cc1C(=O)N1CCC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3954991"	""	"0"	"502.53"	"1"	"3.33"	"44"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3c(F)cccc3F)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3918237"	""	"0"	"520.52"	"1"	"3.47"	"47"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3c(F)ccc(F)c3F)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3898766"	""	"0"	"552.54"	"1"	"4.21"	"52"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(C(F)(F)F)c(F)c3)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL4637972"	""	"0"	"508.69"	"2"	"5.16"	"5"	"Cc1cnc(Nc2ccc(OCCN3CCCC3)cc2)nc1Nc1cccc([S+]([O-])NC(C)(C)C)c1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"16.75"	"0.32"	"3.36"	"9.32"	"False"	"CHEMBL4628503"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4627317"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL4645258"	""	"0"	"432.48"	"0"	"1.79"	"22"	"N#C[C@]1(C2CC2)C(=O)N2C[C@H]1COCC(=O)NCCc1cccc(n1)Nc1cc2ccn1"	"IC50"	"'='"	"180.0"	"nM"	"6.75"	""	""	"UO_0000065"	"15.60"	"0.29"	"4.95"	"5.61"	"False"	"CHEMBL4627620"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4627255"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL3589166"	""	"0"	"429.48"	"0"	"3.57"	"3"	"COc1cccc(-c2cc(C(N)=O)c3[nH]c4ccc(C(=O)N5CCOCC5)cc4c3c2)c1"	"IC50"	"'='"	"2.8"	"nM"	"8.55"	""	""	"UO_0000065"	"19.91"	"0.37"	"4.98"	"8.76"	"True"	"CHEMBL3592849"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL2322139"	""	"0"	"308.31"	"0"	"4.44"	"24"	"FC(F)(F)c1nc2cnc3[nH]ccc3c2n1C1CCCCC1"	"IC50"	"'='"	"11400.0"	"nM"	"4.94"	""	""	"UO_0000065"	"16.03"	"0.31"	"0.50"	"10.63"	"False"	"CHEMBL2327181"	"Inhibition of JAK2 (unknown origin) after 2.5 hrs by time-resolved fluorescence resonance energy transfer assay in presence of 100 uM ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321825"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL375296"	""	"0"	"414.52"	"0"	"3.14"	"19"	"C[C@H](Nc1cc(N2CCN(C)CC2)nc(-n2cnc3ccncc32)n1)c1ccccc1"	"IC50"	"'='"	"19.0"	"nM"	"7.72"	""	""	"UO_0000065"	"18.63"	"0.34"	"4.58"	"10.29"	"False"	"CHEMBL908418"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139695"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2006"	"None"	""
"CHEMBL217937"	""	"0"	"330.40"	"0"	"3.69"	"16"	"Cc1nc2ccncc2n1-c1nccc(N[C@@H](C)c2ccccc2)n1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL908418"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139695"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2006"	"None"	""
"CHEMBL4640647"	""	"0"	"443.19"	"None"	"None"	"14m"	"C=CC(=O)Nc1cccc(Nc2nc(Nc3ccc(B(O)O)cc3)ncc2C(F)(F)F)c1"	"IC50"	"'='"	"891.5"	"nM"	"6.05"	""	""	"UO_0000065"	"13.65"	"None"	"None"	"None"	"False"	"CHEMBL4610789"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using Ulight-Poly GT as substrate incubated for 2 hrs by Lanthascreen TR-FRET assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610007"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2020"	"None"	""
"CHEMBL4648104"	""	"0"	"469.23"	"None"	"None"	"14i"	"C=CC(=O)Nc1cccc(Nc2nc(Nc3ccc4c(c3)B(O)OCC4)ncc2C(F)(F)F)c1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4610789"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using Ulight-Poly GT as substrate incubated for 2 hrs by Lanthascreen TR-FRET assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610007"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2020"	"None"	""
"CHEMBL3234884"	""	"0"	"373.46"	"0"	"3.06"	"12"	"CS(=O)(=O)c1ccc(Nc2sc(-c3ccccc3)cc2C(N)=O)nc1"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	""	"UO_0000065"	"20.87"	"0.43"	"4.74"	"7.63"	"False"	"CHEMBL3239499"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3232939"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3234873"	""	"0"	"452.58"	"0"	"3.71"	"24"	"CC(C)(O)c1ccc(-c2cc(C(N)=O)c(Nc3cccc(CN4CCOCC4)n3)s2)cc1"	"IC50"	"'='"	"520.0"	"nM"	"6.28"	""	""	"UO_0000065"	"13.88"	"0.27"	"2.57"	"6.24"	"False"	"CHEMBL3239512"	"Inhibition of JAK2 (unknown origin)-mediated STAT5 phosphorylation by AlphaScreen assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3232939"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3647732"	""	"0"	"542.56"	"1"	"3.69"	"BDBM147835"	"N#C[C@H]1CC(N2CCC[C@@H]2CF)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	"285769"	"UO_0000065"	"14.48"	"0.29"	"4.16"	"5.86"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3897349"	""	"0"	"589.07"	"1"	"4.91"	"BDBM230101"	"Cc1c(-c2c(Cl)cc(C(N)=O)c3[nH]c4c(c23)CC[C@H](C(C)(C)O)C4)cccc1-n1c(=O)c2cccc(F)c2n(C)c1=O"	"IC50"	"'>'"	"2000.0"	"nM"	""	""	"402036"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3897349"	""	"0"	"589.07"	"1"	"4.91"	"BDBM230101"	"Cc1c(-c2c(Cl)cc(C(N)=O)c3[nH]c4c(c23)CC[C@H](C(C)(C)O)C4)cccc1-n1c(=O)c2cccc(F)c2n(C)c1=O"	"IC50"	"'='"	"7500.0"	"nM"	"5.12"	""	"402037"	"UO_0000065"	"8.70"	"0.17"	"0.21"	"4.16"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3944101"	""	"0"	"571.01"	"2"	"5.18"	"BDBM230108"	"Cc1c(-c2c(Cl)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)cc2c(F)cccn2c1=O"	"IC50"	"'='"	"370.0"	"nM"	"6.43"	""	"402045"	"UO_0000065"	"11.26"	"0.21"	"1.25"	"5.25"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3891767"	""	"0"	"583.04"	"2"	"5.05"	"BDBM230110"	"COc1cccn2c(=O)n(-c3cccc(-c4c(Cl)cc(C(N)=O)c5[nH]c6cc(C(C)(C)O)ccc6c45)c3C)c(=O)cc12"	"IC50"	"'='"	"630.0"	"nM"	"6.20"	""	"402048"	"UO_0000065"	"10.64"	"0.20"	"1.15"	"4.70"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3894000"	""	"0"	"572.54"	"2"	"5.03"	"BDBM230120"	"Cc1c(-c2c(F)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)[nH]c2c(F)cc(F)cc2c1=O"	"IC50"	"'>'"	"2000.0"	"nM"	""	""	"402060"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3901137"	""	"0"	"558.59"	"1"	"4.16"	"BDBM230137"	"Cc1c(-c2c(F)cc(C(N)=O)c3[nH]c4c(c23)CC[C@H](C(C)(C)O)C4)cccc1-n1c(=O)cc2c(F)cccn2c1=O"	"IC50"	"'='"	"9500.0"	"nM"	"5.02"	""	"402080"	"UO_0000065"	"8.99"	"0.17"	"0.86"	"4.10"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4640601"	""	"0"	"459.55"	"0"	"4.14"	"2"	"COc1ccc(-c2cnn3c(N)c(-c4ccccc4)c(OC4CCN(C)CC4)nc23)cc1OC"	"IC50"	"'>'"	"1300.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4605806"	"Inhibition of JAK2 (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction in cell viability incubated for 48 hrs by brightglo-luciferase reporter gene assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4602715"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2020"	"CHEMBL3307634"	""
"CHEMBL3798090"	""	"0"	"442.52"	"0"	"4.98"	"12c"	"Cn1c(C(=O)OCc2ccccc2)cc2c(-c3ccc(NC(=O)C(C)(C)C)cc3)ncnc21"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL3802364"	"Inhibition of JAK2 in GMCSF-stimulated human TF1 cells assessed as suppression of STAT5 phosphorylation preincubated for 2 hrs followed by GMCSF stimulation for 50 mins by FACS reader analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"CHEMBL3307972"	""
"CHEMBL3797300"	""	"0"	"406.49"	"0"	"2.42"	"15a"	"CC(=O)Nc1ccc(-c2ncnc3c2cc(C(=O)NCCN2CCCC2)n3C)cc1"	"IC50"	"'='"	"155.0"	"nM"	"6.81"	""	""	"UO_0000065"	"16.75"	"0.31"	"4.39"	"7.39"	"False"	"CHEMBL3802363"	"Inhibition of recombinant human GST-tagged JAK2 expressed in baculovirus expression system using Z'-LYTE Try6 peptide as substrate incubated for 1 hr by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3799170"	""	"0"	"464.53"	"0"	"3.07"	"14e"	"Cn1c(C(N)=O)cc2c(-c3ccc(NC(=O)[C@@H]4CCCN4C(=O)OC(C)(C)C)cc3)ncnc21"	"IC50"	"'='"	"33.0"	"nM"	"7.48"	""	""	"UO_0000065"	"16.11"	"0.30"	"4.41"	"5.65"	"False"	"CHEMBL3802363"	"Inhibition of recombinant human GST-tagged JAK2 expressed in baculovirus expression system using Z'-LYTE Try6 peptide as substrate incubated for 1 hr by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3800205"	""	"0"	"529.60"	"1"	"4.84"	"12d"	"C[C@H](NC(=O)OC(C)(C)C)C(=O)Nc1ccc(-c2ncnc3c2cc(C(=O)OCc2ccccc2)n3C)cc1"	"IC50"	"'='"	"475.0"	"nM"	"6.32"	""	""	"UO_0000065"	"11.94"	"0.22"	"1.48"	"5.08"	"False"	"CHEMBL3802363"	"Inhibition of recombinant human GST-tagged JAK2 expressed in baculovirus expression system using Z'-LYTE Try6 peptide as substrate incubated for 1 hr by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3545215"	"BMS-911543"	"2"	"432.53"	"0"	"3.50"	"11, BMS-911543"	"CCn1c(C(=O)N(C2CC2)C2CC2)cc2c3c(ncn3C)c(Nc3cc(C)n(C)n3)nc21"	"IC50"	"'='"	"80.0"	"nM"	"7.10"	""	""	"UO_0000065"	"16.41"	"0.30"	"3.60"	"8.27"	"False"	"CHEMBL3624169"	"Inhibition of JAK2 in human SET2 cells assessed as reduction in STAT5 phosphorylation incubated for 2 hrs by Western blot method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621135"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3651055"	""	"0"	"361.43"	"0"	"4.26"	"BDBM153232"	"C=C(C)C(=O)Nc1cccc(-c2ncnc3[nH]cc(-c4cncs4)c23)c1"	"IC50"	"'>'"	"500.0"	"nM"	""	""	"294180"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645104"	""	"0"	"360.42"	"0"	"3.80"	"BDBM99878"	"COc1cccc(CNc2cccn3nc(Nc4ccnc(C)c4)nc23)c1"	"IC50"	"'='"	"591.96"	"nM"	"6.23"	""	"216546"	"UO_0000065"	"17.28"	"0.32"	"2.43"	"8.15"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"CP-690550"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	""	"UO_0000065"	"25.48"	"0.47"	"6.42"	"8.95"	"True"	"CHEMBL897052"	"Inhibition of JAK2 by kinase-Glo luminescent assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1148837"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2007"	"None"	""
"CHEMBL3703065"	""	"0"	"370.43"	"0"	"2.66"	"BDBM147775"	"CN(C)[C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"44.0"	"nM"	"7.36"	""	"285709"	"UO_0000065"	"19.86"	"0.37"	"4.70"	"7.36"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3658122"	""	"0"	"654.07"	"2"	"6.24"	"BDBM148441"	"CN1CCN(c2ccc(Nc3ncc4c(n3)CCN(c3cc(NC(=O)c5cc(F)cc(C(F)(F)F)c5)ccc3Cl)C4=O)cc2)CC1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"286806"	"UO_0000065"	"12.30"	"0.24"	"1.81"	"8.59"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702953"	""	"0"	"437.42"	"0"	"2.72"	"BDBM147655"	"C[C@@](O)(c1ccc(Nc2nn([C@H]3CC[C@@H](O)C[C@@H]3C#N)cc2C(N)=O)cc1)C(F)(F)F"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"285587"	"UO_0000065"	"19.89"	"0.38"	"5.98"	"6.34"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3928999"	""	"0"	"552.54"	"1"	"4.21"	"7"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cccc(C(F)(F)F)c3F)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3945039"	""	"0"	"501.98"	"1"	"3.10"	"13"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cccc(Cl)n3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3984476"	""	"0"	"545.45"	"1"	"3.81"	"20"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cccc(Br)c3)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3963339"	""	"0"	"514.57"	"1"	"3.20"	"36"	"COc1cc(F)cc(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)c1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3914549"	""	"0"	"502.53"	"1"	"3.33"	"41"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cccc(F)c3F)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3639512"	""	"0"	"440.57"	"0"	"2.78"	"BDBM113193"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC(c3cccnc3)C2)CC1"	"IC50"	"'='"	"35.6"	"nM"	"7.45"	""	"234636"	"UO_0000065"	"16.91"	"0.33"	"4.67"	"7.83"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3652333"	""	"0"	"421.57"	"0"	"1.99"	"BDBM113144"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCC[C@H](CO)C2)CC1"	"IC50"	"'='"	"20.1"	"nM"	"7.70"	""	"234587"	"UO_0000065"	"18.26"	"0.36"	"5.71"	"7.51"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3699554"	""	"0"	"395.46"	"0"	"3.34"	"BDBM147572"	"CC(C)(C(=O)O)c1ccc(Nc2nn([C@H]3CCCC[C@@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"72.0"	"nM"	"7.14"	""	"285502"	"UO_0000065"	"18.06"	"0.34"	"3.80"	"5.33"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651047"	""	"0"	"406.85"	"1"	"5.60"	"BDBM153224"	"C=C(C)C(=O)Nc1cccc(-c2ncnc3[nH]cc(-c4cccc(F)c4Cl)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294172"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL2325906"	""	"0"	"297.36"	"0"	"2.50"	"3h"	"C[C@H](NC(=O)c1c[nH]c2ncc(C3CC3)nc12)C(C)(C)C#N"	"IC50"	"'='"	"1420.0"	"nM"	"5.85"	""	""	"UO_0000065"	"19.67"	"0.36"	"3.35"	"6.19"	"False"	"CHEMBL2329053"	"Inhibition of JAK2 in human PBMC expressing CD14 assessed as inhibition of GM-CSF-stimulated STAT5a phosphorylation after 30 mins by flow cytometric analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321829"	"1"	"Scientific Literature"	"J. Med. Chem."	"2013"	"None"	""
"CHEMBL3645001"	""	"0"	"541.55"	"2"	"6.63"	"BDBM99753"	"CC(C)(C)OC(=O)N1CCc2ccc(Nc3nc4c(-c5cc(C(F)(F)F)ccc5F)cccn4n3)cc2CC1"	"IC50"	"'='"	"586.02"	"nM"	"6.23"	""	"216441"	"UO_0000065"	"11.51"	"0.22"	"-0.40"	"8.68"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3301607"	"FILGOTINIB"	"4"	"425.51"	"0"	"1.98"	"BDBM103727"	"O=C(Nc1nc2cccc(-c3ccc(CN4CCS(=O)(=O)CC4)cc3)n2n1)C1CC1"	"IC50"	"'='"	"55.49"	"nM"	"7.26"	""	"221711"	"UO_0000065"	"17.05"	"0.33"	"5.28"	"7.51"	"False"	"CHEMBL3707887"	"Inhibition Assay: In vitro inhibition assay using various enzyme."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638964"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3651049"	""	"0"	"368.44"	"1"	"5.11"	"BDBM153226"	"C=C(C)C(=O)Nc1cccc(-c2ncnc3[nH]cc(-c4ccc(C)cc4)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294174"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652359"	""	"0"	"494.62"	"0"	"3.31"	"BDBM113170"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC[C@H](Oc3ccccc3C#N)C2)CC1"	"IC50"	"'='"	"23.4"	"nM"	"7.63"	""	"234613"	"UO_0000065"	"15.43"	"0.30"	"4.32"	"6.62"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3645105"	""	"0"	"346.39"	"0"	"3.49"	"BDBM99879"	"COc1cccc(CNc2cccn3nc(Nc4cccnc4)nc23)c1"	"IC50"	"'='"	"816.37"	"nM"	"6.09"	""	"216547"	"UO_0000065"	"17.58"	"0.32"	"2.60"	"7.97"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3650984"	""	"0"	"335.37"	"0"	"3.08"	"BDBM153158"	"CCCOC(=O)c1c[nH]c2ncnc(-c3ccc4cn(C)nc4c3)c12"	"IC50"	"'='"	"153.0"	"nM"	"6.82"	""	"294106"	"UO_0000065"	"20.32"	"0.37"	"3.74"	"7.95"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3951028"	""	"0"	"520.52"	"1"	"3.47"	"46"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(F)c(F)c3F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3926335"	""	"0"	"472.60"	"0"	"3.32"	"8"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)C3CCCCC3)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3932489"	""	"0"	"509.55"	"1"	"3.06"	"18"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc(F)cc(C#N)c3)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3890938"	""	"0"	"502.53"	"1"	"3.33"	"35"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(F)c(F)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL233151"	""	"0"	"495.59"	"0"	"3.26"	"4"	"C[C@H](Nc1nc(-n2cnc3ccncc32)nc2c1cc(C(=O)N1CCN(C)CC1)n2C)c1ccccc1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	""	"UO_0000065"	"16.06"	"0.29"	"4.70"	"8.20"	"False"	"CHEMBL897052"	"Inhibition of JAK2 by kinase-Glo luminescent assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1148837"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2007"	"None"	""
"CHEMBL3702958"	""	"0"	"325.37"	"0"	"1.95"	"BDBM147665"	"N#C[C@H]1C[C@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccccc2)n1"	"IC50"	"'='"	"26.0"	"nM"	"7.58"	""	"285597"	"UO_0000065"	"23.31"	"0.43"	"5.64"	"6.49"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645109"	""	"0"	"376.42"	"0"	"3.50"	"BDBM99883"	"COc1ccc(Nc2nc3c(NCc4ccccc4OC)cccn3n2)cn1"	"IC50"	"'='"	"42.66"	"nM"	"7.37"	""	"216551"	"UO_0000065"	"19.58"	"0.36"	"3.87"	"8.61"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647803"	""	"0"	"394.48"	"0"	"2.34"	"BDBM147906"	"CC1(N[C@H]2CCC(n3cc(C(N)=O)c(Nc4ccccc4)n3)[C@@H](C#N)C2)COC1"	"IC50"	"'='"	"24.0"	"nM"	"7.62"	""	"285840"	"UO_0000065"	"19.32"	"0.36"	"5.28"	"6.46"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702921"	""	"0"	"345.35"	"0"	"3.26"	"BDBM147620"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(F)c(F)c2)n1"	"IC50"	"'='"	"34.0"	"nM"	"7.47"	""	"285550"	"UO_0000065"	"21.63"	"0.41"	"4.21"	"7.72"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL391492"	""	"0"	"442.48"	"0"	"3.17"	"10"	"CONC(=O)c1cc2c(N[C@@H](C)c3ccccc3)nc(-n3cnc4ccncc43)nc2n1C"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	""	"UO_0000065"	"18.58"	"0.34"	"5.05"	"7.36"	"False"	"CHEMBL897052"	"Inhibition of JAK2 by kinase-Glo luminescent assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1148837"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2007"	"None"	""
"CHEMBL3652314"	""	"0"	"416.55"	"0"	"2.52"	"BDBM113124"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCC(C#N)CC2)CC1"	"IC50"	"'='"	"66.9"	"nM"	"7.17"	""	"234567"	"UO_0000065"	"17.22"	"0.34"	"4.65"	"6.77"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3699466"	""	"0"	"367.41"	"0"	"2.38"	"BDBM147481"	"COC(=O)C1CC[C@H](C#N)C(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'>'"	"1500.0"	"nM"	""	""	"285406"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652384"	""	"0"	"503.65"	"1"	"2.44"	"BDBM113196"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC(S(=O)(=O)c3ccccc3)C2)CC1"	"IC50"	"'='"	"9.2"	"nM"	"8.04"	""	"234639"	"UO_0000065"	"15.96"	"0.32"	"5.60"	"6.91"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL2062529"	""	"0"	"545.71"	"1"	"3.76"	"BDBM99560"	"CN1CCN(C2CCN(c3cccc(Nc4nc5c(-c6ccc(S(C)(=O)=O)cc6)cccn5n4)c3)CC2)CC1"	"IC50"	"'='"	"1.5"	"nM"	"8.82"	""	"216250"	"UO_0000065"	"16.17"	"0.31"	"5.06"	"10.25"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3936249"	""	"0"	"585.04"	"2"	"5.42"	"BDBM230081"	"Cc1c(-c2c(Cl)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)c2cccc(F)c2n(C)c1=O"	"IC50"	"'>'"	"2000.0"	"nM"	""	""	"402012"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3907348"	""	"0"	"554.55"	"1"	"4.89"	"BDBM230098"	"Cc1c(-c2c(F)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)[nH]c2c(F)cccc2c1=O"	"IC50"	"'='"	"760.0"	"nM"	"6.12"	""	"402032"	"UO_0000065"	"11.03"	"0.20"	"1.23"	"4.57"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3903416"	""	"0"	"605.45"	"2"	"5.76"	"BDBM230115"	"Cn1c(=O)n(-c2cccc(-c3c(Cl)cc(C(N)=O)c4[nH]c5cc(C(C)(C)O)ccc5c34)c2Cl)c(=O)c2cccc(F)c21"	"IC50"	"'='"	"710.0"	"nM"	"6.15"	""	"402055"	"UO_0000065"	"10.16"	"0.20"	"0.39"	"4.99"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3945408"	""	"0"	"575.04"	"1"	"4.90"	"BDBM230126"	"Cc1c(-c2c(Cl)cc(C(N)=O)c3[nH]c4c(c23)CC[C@H](C(C)(C)O)C4)cccc1-n1c(=O)[nH]c2c(F)cccc2c1=O"	"IC50"	"'='"	"9000.0"	"nM"	"5.05"	""	"402066"	"UO_0000065"	"8.77"	"0.17"	"0.15"	"3.77"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3912426"	""	"0"	"589.00"	"2"	"5.25"	"BDBM230130"	"Cn1c(=O)n(-c2cccc(-c3c(F)cc(C(N)=O)c4[nH]c5cc(C(C)(C)O)ccc5c34)c2Cl)c(=O)c2cccc(F)c21"	"IC50"	"'='"	"270.0"	"nM"	"6.57"	""	"402071"	"UO_0000065"	"11.15"	"0.21"	"1.32"	"5.34"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3965224"	""	"0"	"578.03"	"1"	"4.91"	"BDBM230141"	"Cc1c(-c2c(C#N)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)cc2c(Cl)cccn2c1=O"	"IC50"	"'='"	"770.0"	"nM"	"6.11"	""	"402083"	"UO_0000065"	"10.58"	"0.20"	"1.20"	"4.18"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3622144"	""	"0"	"492.61"	"0"	"3.58"	"6"	"CCn1c(C(=O)N(C2CC2)C2CC2)cc2c3c(ncn3C)c(Nc3nc(C(=O)NC)c(C)s3)nc21"	"IC50"	"'='"	"3.1"	"nM"	"8.51"	""	""	"UO_0000065"	"17.27"	"0.33"	"4.93"	"7.74"	"False"	"CHEMBL3625512"	"Inhibition of recombinant JAK2 (unknown origin) using 5-FAM-KKKKEEIYFFFG-OH substrate and ATP incubated for 180 mins by scintillation counting method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621135"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3971912"	""	"0"	"451.51"	"0"	"2.21"	"BDBM229129"	"Cc1c(CN2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccnc(F)c4)n3)CC2)cnn1C"	"IC50"	"'='"	"582.0"	"nM"	"6.24"	""	"400865"	"UO_0000065"	"13.81"	"0.26"	"4.03"	"4.77"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3973424"	""	"0"	"419.46"	"0"	"3.17"	"BDBM229165"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(c2ccccn2)CC1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"400901"	"UO_0000065"	"20.74"	"0.38"	"5.53"	"7.71"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3962864"	""	"0"	"462.94"	"0"	"3.92"	"BDBM229274"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)c2cccc(Cl)c2)CC1"	"IC50"	"'='"	"63.0"	"nM"	"7.20"	""	"401013"	"UO_0000065"	"15.55"	"0.30"	"3.28"	"6.15"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4113974"	""	"0"	"490.54"	"0"	"4.02"	"BDBM237724"	"N#C[C@@H]1CN(C(=O)OCCCc2ccccc2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"1005.0"	"nM"	"6.00"	""	"414828"	"UO_0000065"	"12.23"	"0.23"	"1.98"	"4.75"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4108322"	""	"0"	"443.48"	"0"	"1.95"	"BDBM237743"	"CN(C)CCOC(=O)N1CC[C@@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@H](C#N)C1"	"IC50"	"'='"	"1111.0"	"nM"	"5.95"	""	"414847"	"UO_0000065"	"13.43"	"0.25"	"4.00"	"4.60"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4108573"	""	"0"	"469.52"	"0"	"2.48"	"BDBM237747"	"CN1CCC(OC(=O)N2CC[C@@H](n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)[C@H](C#N)C2)CC1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"414851"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3900020"	""	"0"	"466.42"	"0"	"2.02"	"BDBM237795"	"N#C[C@@H]1CCN(C(=O)OCC(F)(F)CO)C[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	"414899"	"UO_0000065"	"16.84"	"0.33"	"5.83"	"5.36"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3896530"	""	"0"	"414.90"	"0"	"2.19"	"BDBM239987"	"CN(c1nc(Nc2cnn(C)c2)ncc1Cl)C1CC2CN(C(=O)CC#N)CC2C1"	"IC50"	"'='"	"41.0"	"nM"	"7.39"	""	"418595"	"UO_0000065"	"17.80"	"0.35"	"5.20"	"7.17"	"False"	"CHEMBL3888834"	"Kinase Assay: JAK2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 100 μM KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC, 10 mM MgAcetate and [γ-33P-ATP](specific activity approx. 500 cpm/pmol, concentration as required). The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of 3% phosphoric acid solution. 10 μL of the reaction is then spotted onto a P30 filtermat and washed three times for 5 minutes in 75 mM phosphoric acid and once in methanol prior to drying and scintillation counting."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886854"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3957147"	""	"0"	"409.43"	"0"	"2.44"	"BDBM237816"	"N#C[C@@H]1CCN(Cc2ccon2)C[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	"414920"	"UO_0000065"	"19.26"	"0.36"	"5.45"	"6.26"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3906718"	""	"0"	"426.50"	"0"	"2.68"	"BDBM237822"	"COC1CC(CN2CC[C@@H](C#N)[C@H](n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)C2)C1"	"IC50"	"'='"	"191.0"	"nM"	"6.72"	""	"414926"	"UO_0000065"	"15.75"	"0.30"	"4.04"	"6.15"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3980441"	""	"0"	"440.52"	"0"	"3.07"	"BDBM237823"	"N#C[C@@H]1CCN(CCC2CCOCC2)C[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"74.0"	"nM"	"7.13"	""	"414927"	"UO_0000065"	"16.19"	"0.30"	"4.06"	"6.53"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3954457"	""	"0"	"412.47"	"0"	"2.29"	"BDBM237834"	"N#C[C@@H]1CCN(CC2CCOC2)C[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"63.0"	"nM"	"7.20"	""	"414938"	"UO_0000065"	"17.46"	"0.33"	"4.91"	"6.59"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4110756"	""	"0"	"426.50"	"0"	"2.68"	"BDBM237843"	"COC1CC(CN2CC[C@@H](n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)[C@H](C#N)C2)C1"	"IC50"	"'='"	"166.0"	"nM"	"6.78"	""	"414947"	"UO_0000065"	"15.90"	"0.30"	"4.10"	"6.21"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3946652"	""	"0"	"428.54"	"0"	"3.94"	"BDBM229067"	"Cc1ccc(CN2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)CC2)cc1"	"IC50"	"'='"	"135.0"	"nM"	"6.87"	""	"400803"	"UO_0000065"	"16.03"	"0.29"	"2.93"	"6.87"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3956583"	""	"0"	"494.60"	"0"	"4.79"	"BDBM229073"	"COc1ccc2cc(CN3CCC(CC#N)(n4cc(C(N)=O)c(Nc5ccccc5)n4)CC3)ccc2c1"	"IC50"	"'='"	"297.0"	"nM"	"6.53"	""	"400809"	"UO_0000065"	"13.20"	"0.24"	"1.74"	"5.98"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3935566"	""	"0"	"440.55"	"0"	"4.14"	"BDBM229077"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C/C=C/c2ccccc2)CC1"	"IC50"	"'='"	"208.0"	"nM"	"6.68"	""	"400813"	"UO_0000065"	"15.17"	"0.28"	"2.54"	"6.68"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3918263"	""	"0"	"454.53"	"0"	"4.38"	"BDBM229080"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(Cc2cc3ccccc3o2)CC1"	"IC50"	"'='"	"105.0"	"nM"	"6.98"	""	"400816"	"UO_0000065"	"15.35"	"0.28"	"2.60"	"6.17"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3903806"	""	"0"	"456.59"	"0"	"4.75"	"BDBM229084"	"CC(C)c1ccc(CN2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)CC2)cc1"	"IC50"	"'='"	"1053.0"	"nM"	"5.98"	""	"400820"	"UO_0000065"	"13.09"	"0.24"	"1.23"	"5.98"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3930900"	""	"0"	"433.49"	"0"	"3.16"	"BDBM229097"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2ccccc2)CC1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"400833"	"UO_0000065"	"18.97"	"0.35"	"5.06"	"7.28"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3914149"	""	"0"	"451.48"	"0"	"3.30"	"BDBM229099"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2cccc(F)c2)CC1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"400835"	"UO_0000065"	"18.88"	"0.35"	"5.22"	"7.55"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3977268"	""	"0"	"473.52"	"0"	"2.81"	"BDBM229101"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2cn3ccccc3n2)CC1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"400837"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3965488"	""	"0"	"469.57"	"0"	"3.17"	"BDBM229105"	"CC1(C)CC(CN2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccnc(F)c4)n3)CC2)CCO1"	"IC50"	"'='"	"122.0"	"nM"	"6.91"	""	"400841"	"UO_0000065"	"14.72"	"0.28"	"3.74"	"5.66"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3973935"	""	"0"	"469.57"	"0"	"2.76"	"BDBM229113"	"CC(C)(O)C1CC(CN2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccnc(F)c4)n3)CC2)C1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"400849"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3589169"	""	"0"	"446.94"	"0"	"4.13"	"6"	"CN1CCN(C(=O)c2ccc3[nH]c4c(C(N)=O)cc(-c5ccc(Cl)cc5)cc4c3c2)CC1"	"IC50"	"'='"	"71.0"	"nM"	"7.15"	""	""	"UO_0000065"	"15.99"	"0.31"	"3.02"	"8.67"	"False"	"CHEMBL3592855"	"Inhibition of JAK2 in human SET2 cells assessed as inhibition of cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3589172"	""	"0"	"413.48"	"0"	"3.48"	"9"	"NC(=O)c1cc(Cc2ccccc2)cc2c1[nH]c1ccc(C(=O)N3CCOCC3)cc12"	"IC50"	"'='"	"210.0"	"nM"	"6.68"	""	""	"UO_0000065"	"16.15"	"0.29"	"3.20"	"7.55"	"False"	"CHEMBL3592855"	"Inhibition of JAK2 in human SET2 cells assessed as inhibition of cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3589177"	""	"0"	"456.55"	"0"	"3.87"	"14"	"COc1cccc(-c2cc(C(N)=O)c3[nH]c4cc(C(=O)N5CC[C@H](N(C)C)C5)ccc4c3c2)c1"	"IC50"	"'='"	"80.0"	"nM"	"7.10"	""	""	"UO_0000065"	"15.54"	"0.29"	"3.23"	"7.74"	"False"	"CHEMBL3592855"	"Inhibition of JAK2 in human SET2 cells assessed as inhibition of cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3589327"	""	"0"	"518.06"	"1"	"4.32"	"19"	"CN1CCN(c2ccc3c(c2)[nH]c2c(C(N)=O)cc(-c4ccc(CN5CCOCC5)c(Cl)c4)cc23)CC1"	"IC50"	"'='"	"260.0"	"nM"	"6.58"	""	""	"UO_0000065"	"12.71"	"0.24"	"2.27"	"8.46"	"False"	"CHEMBL3592855"	"Inhibition of JAK2 in human SET2 cells assessed as inhibition of cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3976766"	""	"0"	"440.48"	"0"	"2.13"	"BDBM229131"	"CC1=NOC(CN2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccnc(F)c4)n3)CC2)C1"	"IC50"	"'='"	"582.0"	"nM"	"6.24"	""	"400867"	"UO_0000065"	"14.16"	"0.27"	"4.11"	"4.64"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3922288"	""	"0"	"433.49"	"0"	"3.16"	"BDBM229140"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(Cc2cccnc2)CC1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"400876"	"UO_0000065"	"18.56"	"0.34"	"4.89"	"7.13"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3894262"	""	"0"	"434.48"	"0"	"2.56"	"BDBM229141"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(Cc2cnccn2)CC1"	"IC50"	"'='"	"25.0"	"nM"	"7.60"	""	"400877"	"UO_0000065"	"17.50"	"0.32"	"5.04"	"6.05"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3936674"	""	"0"	"471.54"	"0"	"4.25"	"BDBM229144"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(Cc2ccc3[nH]ccc3c2)CC1"	"IC50"	"'='"	"53.0"	"nM"	"7.28"	""	"400880"	"UO_0000065"	"15.43"	"0.28"	"3.03"	"6.29"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3908726"	""	"0"	"452.52"	"0"	"2.75"	"BDBM229210"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)OC2CCOCC2)CC1"	"IC50"	"'='"	"103.0"	"nM"	"6.99"	""	"400947"	"UO_0000065"	"15.44"	"0.29"	"4.24"	"5.16"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3893183"	""	"0"	"459.51"	"0"	"3.16"	"BDBM229213"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)OCc2ccncc2)CC1"	"IC50"	"'='"	"58.0"	"nM"	"7.24"	""	"400950"	"UO_0000065"	"15.75"	"0.29"	"4.08"	"5.20"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3963750"	""	"0"	"482.44"	"0"	"3.66"	"BDBM229218"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(C(=O)OCCC(F)(F)F)CC1"	"IC50"	"'='"	"97.0"	"nM"	"7.01"	""	"400955"	"UO_0000065"	"14.54"	"0.28"	"3.35"	"5.55"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4110158"	""	"0"	"445.48"	"0"	"2.42"	"BDBM229238"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CN(C(=O)OCCc2ccccn2)C1"	"IC50"	"'='"	"849.0"	"nM"	"6.07"	""	"400977"	"UO_0000065"	"13.63"	"0.25"	"3.65"	"4.36"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3916595"	""	"0"	"429.46"	"0"	"1.26"	"BDBM229296"	"CC(C)(O)C(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CC1"	"IC50"	"'='"	"234.0"	"nM"	"6.63"	""	"401035"	"UO_0000065"	"15.44"	"0.29"	"5.37"	"4.42"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4112365"	""	"0"	"463.93"	"0"	"3.84"	"BDBM229357"	"Cc1ccc(Cl)cc1NC(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"149.0"	"nM"	"6.83"	""	"401096"	"UO_0000065"	"14.72"	"0.28"	"2.99"	"5.29"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3892313"	""	"0"	"434.48"	"0"	"3.32"	"BDBM229395"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(Nc2ccccn2)CC1"	"IC50"	"'='"	"1333.0"	"nM"	"5.88"	""	"401133"	"UO_0000065"	"13.52"	"0.25"	"2.56"	"4.37"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3914703"	""	"0"	"433.49"	"0"	"3.92"	"BDBM229421"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(Nc2cccnc2)CC1"	"IC50"	"'='"	"760.0"	"nM"	"6.12"	""	"401168"	"UO_0000065"	"14.12"	"0.26"	"2.20"	"5.03"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3935010"	""	"0"	"544.58"	"1"	"4.09"	"BDBM228225"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)F)cc3)n2)CCC(Nc2ccccc2O)CC1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"401177"	"UO_0000065"	"15.10"	"0.30"	"4.13"	"5.04"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3916947"	""	"0"	"451.48"	"0"	"4.06"	"BDBM228241"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(Nc2cccc(F)c2)CC1"	"IC50"	"'='"	"409.0"	"nM"	"6.39"	""	"401184"	"UO_0000065"	"14.15"	"0.26"	"2.33"	"5.25"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4248386"	""	"0"	"383.47"	"0"	"3.74"	"31"	"C=CS(=O)(=O)Nc1cccc(-c2ccc(C(N)=O)c3[nH]c(C)c(C)c23)c1C"	"IC50"	"'='"	"1100.0"	"nM"	"5.96"	""	""	"UO_0000065"	"15.54"	"0.30"	"2.22"	"5.67"	"False"	"CHEMBL4235700"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229517"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2018"	"None"	""
"CHEMBL3763864"	""	"0"	"320.36"	"0"	"2.00"	"8"	"Cc1ccccc1-n1cc(-c2ccn(C)n2)c2[nH]nc(N)c2c1=O"	"IC50"	"'='"	"1700.0"	"nM"	"5.77"	""	""	"UO_0000065"	"18.01"	"0.33"	"3.77"	"6.10"	"False"	"CHEMBL3766653"	"Inhibition of JAK2 (unknown origin) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent substrate phosphorylation after 45 mins by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3763089"	"1"	"Scientific Literature"	"J. Med. Chem."	"2016"	"None"	""
"CHEMBL3764463"	""	"0"	"337.77"	"0"	"3.01"	"6"	"Nc1n[nH]c2c(-c3ccccn3)cn(-c3ccccc3Cl)c(=O)c12"	"IC50"	"'='"	"550.0"	"nM"	"6.26"	""	""	"UO_0000065"	"18.53"	"0.36"	"3.25"	"6.99"	"False"	"CHEMBL3766653"	"Inhibition of JAK2 (unknown origin) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent substrate phosphorylation after 45 mins by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3763089"	"1"	"Scientific Literature"	"J. Med. Chem."	"2016"	"None"	""
"CHEMBL3765822"	""	"0"	"358.45"	"0"	"2.15"	"20"	"CC(C)[C@@H](C)n1cc(-c2cc(C(C)(C)O)n(C)n2)c2[nH]nc(N)c2c1=O"	"IC50"	"'='"	"2600.0"	"nM"	"5.58"	""	""	"UO_0000065"	"15.58"	"0.29"	"3.44"	"4.87"	"False"	"CHEMBL3766669"	"Inhibition of JAK2 in human PBMC assessed as reduction in GM-CSF-induced STAT5 phosphorylation preincubated for 5 mins followed by GM-CSF stimulation for 15 to 60 mins by flow cytometry analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3763089"	"1"	"Scientific Literature"	"J. Med. Chem."	"2016"	"None"	""
"CHEMBL1938654"	""	"0"	"418.54"	"0"	"2.98"	"19"	"CNC(=O)c1cnc(N)c2cc(-c3ccc(S(=O)(=O)NC(C)(C)C)cc3)sc12"	"IC50"	"'='"	"1480.0"	"nM"	"5.83"	""	""	"UO_0000065"	"13.93"	"0.28"	"2.85"	"5.11"	"False"	"CHEMBL1941461"	"Inhibition of JAK2 in human whole blood assessed as inhibition of TPO-stimulated STAT5 phosphorylation preincubated for 30 mins prior to TPO challenge measured after 15 mins by intracellular phosflow staining"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"CHEMBL3638178"	"Blood"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1934337"	""	"0"	"561.71"	"1"	"3.88"	"3c"	"CC(C)(C)NS(=O)(=O)c1cccc(-c2ccc3cnc(Nc4ccc(C5CCN(CC(N)=O)CC5)cc4)nn23)c1"	"IC50"	"'='"	"0.64"	"nM"	"9.19"	""	""	"UO_0000065"	"16.37"	"0.31"	"5.31"	"6.82"	"False"	"CHEMBL1936085"	"Inhibition of human recombinant JAK2 expressed in baculovirus expression system after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL1934338"	""	"0"	"457.54"	"0"	"3.21"	"3d"	"COc1ccc(-c2ccc3cnc(Nc4ccc(C5CCN(CC(N)=O)CC5)cc4)nn23)cn1"	"IC50"	"'='"	"62.0"	"nM"	"7.21"	""	""	"UO_0000065"	"15.75"	"0.29"	"4.00"	"6.51"	"False"	"CHEMBL1936009"	"Inhibition of JAK2 in GM-CSF-stimulated human TF1 cells preincubated for 1 hr prior to challenge"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3307972"	""
"CHEMBL1938642"	""	"0"	"354.44"	"0"	"2.48"	"3"	"NC(=O)c1cnc(N)c2cc(-c3ccc(N4CCOCC4)cc3)sc12"	"IC50"	"'='"	"761.0"	"nM"	"6.12"	""	""	"UO_0000065"	"17.26"	"0.33"	"3.64"	"6.48"	"False"	"CHEMBL1941458"	"Inhibition of JAK2 in human PBMC assessed as inhibition of TPO-stimulated STAT5 phosphorylation preincubated for 30 mins prior to TPO challenge measured after 15 mins by intracellular phosflow staining"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL3901392"	""	"0"	"420.44"	"0"	"3.02"	"BDBM254986"	"N#CCN1CN([C@H]2CC[C@H](CNCC(F)(F)F)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	"443893"	"UO_0000065"	"18.54"	"0.35"	"4.78"	"8.85"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3968872"	""	"0"	"434.47"	"0"	"3.36"	"BDBM254995"	"CN(CC(F)(F)F)C[C@H]1CC[C@H](N2CN(CC#N)C(=O)c3cnc4[nH]ccc4c32)CC1"	"IC50"	"'='"	"6.8"	"nM"	"8.17"	""	"443902"	"UO_0000065"	"18.80"	"0.36"	"4.81"	"10.30"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3952017"	""	"0"	"473.52"	"0"	"2.81"	"BDBM229122"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2cccc3ccnn23)CC1"	"IC50"	"'='"	"81.0"	"nM"	"7.09"	""	"400858"	"UO_0000065"	"14.98"	"0.28"	"4.28"	"5.45"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3921194"	""	"0"	"471.54"	"0"	"4.25"	"BDBM229147"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(Cc2cccc3cc[nH]c23)CC1"	"IC50"	"'='"	"128.0"	"nM"	"6.89"	""	"400883"	"UO_0000065"	"14.62"	"0.27"	"2.64"	"5.95"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3927787"	""	"0"	"449.49"	"0"	"2.87"	"BDBM229149"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2ccc(O)cc2)CC1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"400885"	"UO_0000065"	"18.29"	"0.34"	"5.35"	"6.18"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3948300"	""	"0"	"558.54"	"1"	"2.51"	"BDBM229168"	"COCCOC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)(F)F)cc3)n2)CC1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"400904"	"UO_0000065"	"14.72"	"0.30"	"5.71"	"4.85"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3924793"	""	"0"	"556.52"	"1"	"2.26"	"BDBM229199"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)(F)F)cc3)n2)CCN(C(=O)OC2COC2)CC1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"400936"	"UO_0000065"	"15.31"	"0.31"	"6.26"	"5.02"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4107621"	""	"0"	"463.93"	"0"	"3.84"	"BDBM229364"	"Cc1cccc(Cl)c1NC(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"179.0"	"nM"	"6.75"	""	"401103"	"UO_0000065"	"14.54"	"0.28"	"2.91"	"5.23"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4111808"	""	"0"	"429.48"	"0"	"3.19"	"BDBM229367"	"Cc1ccccc1NC(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"162.0"	"nM"	"6.79"	""	"401106"	"UO_0000065"	"15.81"	"0.29"	"3.60"	"5.26"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3916587"	""	"0"	"468.52"	"0"	"3.53"	"BDBM229387"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)Nc2ccc(C#N)cc2)CC1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"401126"	"UO_0000065"	"17.55"	"0.32"	"4.69"	"5.38"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3890345"	""	"0"	"438.55"	"0"	"4.34"	"BDBM229392"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(NC2CCCCC2)CC1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"401129"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3916947"	""	"0"	"451.48"	"0"	"4.06"	"BDBM228241"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(Nc2cccc(F)c2)CC1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"401193"	"UO_0000065"	"19.27"	"0.36"	"4.64"	"7.15"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3907084"	""	"0"	"500.50"	"2"	"5.55"	"BDBM229442"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(Nc2ccc(C(F)(F)F)cc2)CC1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"401202"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3909471"	""	"0"	"441.47"	"0"	"2.51"	"BDBM229220"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(C(=O)OCC2CC2)CC1"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	"400959"	"UO_0000065"	"17.54"	"0.33"	"5.23"	"5.57"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4109140"	""	"0"	"408.46"	"0"	"2.73"	"BDBM229223"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CN(C(=O)OC2CCCC2)C1"	"IC50"	"'='"	"76.0"	"nM"	"7.12"	""	"400962"	"UO_0000065"	"17.43"	"0.32"	"4.39"	"5.64"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4109663"	""	"0"	"398.42"	"0"	"1.43"	"BDBM229230"	"COCCOC(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"336.0"	"nM"	"6.47"	""	"400969"	"UO_0000065"	"16.25"	"0.30"	"5.04"	"4.78"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3945544"	""	"0"	"458.52"	"0"	"3.28"	"BDBM229271"	"COc1ccc(C(=O)N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)CC2)cc1"	"IC50"	"'='"	"137.0"	"nM"	"6.86"	""	"401010"	"UO_0000065"	"14.97"	"0.28"	"3.58"	"5.44"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3892346"	""	"0"	"479.54"	"0"	"3.82"	"BDBM229285"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)c2ccc3ccccc3n2)CC1"	"IC50"	"'='"	"166.0"	"nM"	"6.78"	""	"401024"	"UO_0000065"	"14.14"	"0.26"	"2.96"	"5.22"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3900415"	""	"0"	"416.51"	"0"	"1.78"	"BDBM229323"	"CCS(=O)(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)CC1"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	"401062"	"UO_0000065"	"19.02"	"0.37"	"6.14"	"5.91"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3951724"	""	"0"	"439.48"	"0"	"1.31"	"BDBM229349"	"CCOC(=O)C(C)NC(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"558.0"	"nM"	"6.25"	""	"401088"	"UO_0000065"	"14.23"	"0.27"	"4.94"	"4.02"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3959238"	""	"0"	"536.61"	"1"	"2.73"	"BDBM229423"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)F)cc3)n2)CCC(N2CCC(O)CC2)CC1"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	"401172"	"UO_0000065"	"14.64"	"0.29"	"5.12"	"5.09"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3971240"	""	"0"	"518.63"	"1"	"4.53"	"BDBM229413"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc([S+]([O-])C(F)F)cc3)n2)CCC(NC2CCCCC2)CC1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"401186"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3931541"	""	"0"	"426.50"	"0"	"2.75"	"BDBM229443"	"COC1CN(C2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)CC2)C1"	"IC50"	"'='"	"35.0"	"nM"	"7.46"	""	"401203"	"UO_0000065"	"17.48"	"0.33"	"4.71"	"6.83"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4109360"	""	"0"	"442.50"	"0"	"3.43"	"BDBM237738"	"CC(C)(C)COC(=O)N1CC[C@@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@H](C#N)C1"	"IC50"	"'='"	"1231.0"	"nM"	"5.91"	""	"414842"	"UO_0000065"	"13.36"	"0.25"	"2.48"	"4.68"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4114171"	""	"0"	"454.51"	"0"	"3.72"	"BDBM237782"	"N#C[C@@H]1CN(C(=O)OC2CCCCC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"414886"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3649640"	""	"0"	"497.00"	"1"	"5.63"	"BDBM130334"	"NC(=O)c1cc(-c2ccc(CN3CCOCC3)c(Cl)c2)cc2c1[nH]c1cc(-c3cccnc3)ccc12"	"IC50"	"'='"	"133.0"	"nM"	"6.88"	""	"262120"	"UO_0000065"	"13.84"	"0.26"	"1.25"	"8.16"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649646"	""	"0"	"416.49"	"0"	"2.78"	"BDBM130341"	"CN(C)c1ccc(-c2cc(C(N)=O)c3[nH]c4cc(N5CCOCC5)ccc4c3n2)cn1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"262127"	"UO_0000065"	"21.61"	"0.40"	"6.22"	"8.97"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649648"	""	"0"	"504.52"	"1"	"3.76"	"BDBM130343"	"COC(=O)N1CCN(C(=O)c2ccc3c(c2)[nH]c2c(C(N)=O)cc(-c4ccc(OC)c(F)c4)cc23)CC1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"262129"	"UO_0000065"	"17.84"	"0.33"	"5.24"	"7.63"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649650"	""	"0"	"451.89"	"0"	"4.35"	"BDBM130345"	"NC(=O)c1cc(-c2ccc(F)c(Cl)c2)cc2c1[nH]c1cc(C(=O)N3CCOCC3)ccc12"	"IC50"	"'='"	"885.0"	"nM"	"6.05"	""	"262131"	"UO_0000065"	"13.39"	"0.26"	"1.70"	"6.85"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3646825"	""	"0"	"496.57"	"0"	"3.79"	"BDBM130271"	"COc1cccc(-c2cc(C(N)=O)c3[nH]c4cc(C(=O)N5CCN(C(=O)C6CC6)CC5)ccc4c3c2)c1"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"262057"	"UO_0000065"	"16.42"	"0.30"	"4.36"	"7.50"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3645072"	""	"0"	"479.59"	"0"	"4.28"	"BDBM99840"	"CN(C)C(=O)CN1CCC(c2ccc(Nc3nc4c(-c5ccc(C#N)cc5)cccn4n3)cc2)CC1"	"IC50"	"'='"	"3.88"	"nM"	"8.41"	""	"216513"	"UO_0000065"	"17.54"	"0.32"	"4.13"	"9.39"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL4560698"	""	"0"	"481.62"	"0"	"4.40"	"18f"	"Cc1cnc(Nc2ccc(N3CCC(N(C)CCCO)CC3)c(F)c2)nc1-c1cnn(C(C)C)c1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	""	"UO_0000065"	"18.69"	"0.35"	"4.60"	"10.93"	"False"	"CHEMBL4323930"	"Inhibition of human JAK2 (808 to end residues) using KTFCGTPEYLAP as substrate after 40 mins in presence of [gamma33P]-ATP by scintillation counting based radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4321837"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL3800205"	""	"0"	"529.60"	"1"	"4.84"	"12d"	"C[C@H](NC(=O)OC(C)(C)C)C(=O)Nc1ccc(-c2ncnc3c2cc(C(=O)OCc2ccccc2)n3C)cc1"	"IC50"	"'>'"	"20000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3802364"	"Inhibition of JAK2 in GMCSF-stimulated human TF1 cells assessed as suppression of STAT5 phosphorylation preincubated for 2 hrs followed by GMCSF stimulation for 50 mins by FACS reader analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"CHEMBL3307972"	""
"CHEMBL3800493"	""	"0"	"535.65"	"1"	"3.31"	"15d"	"C[C@H](NC(=O)OC(C)(C)C)C(=O)Nc1ccc(-c2ncnc3c2cc(C(=O)NCCN2CCCC2)n3C)cc1"	"IC50"	"'='"	"21.0"	"nM"	"7.68"	""	""	"UO_0000065"	"14.33"	"0.27"	"4.37"	"5.88"	"False"	"CHEMBL3802363"	"Inhibition of recombinant human GST-tagged JAK2 expressed in baculovirus expression system using Z'-LYTE Try6 peptide as substrate incubated for 1 hr by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3800434"	""	"0"	"396.41"	"0"	"2.86"	"14g"	"Cn1c(C(N)=O)cc2c(-c3ccc(NC(=O)c4ccc(C#N)cc4)cc3)ncnc21"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3802363"	"Inhibition of recombinant human GST-tagged JAK2 expressed in baculovirus expression system using Z'-LYTE Try6 peptide as substrate incubated for 1 hr by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3797902"	""	"0"	"493.57"	"0"	"3.58"	"15g"	"Cn1c(C(=O)NCCN2CCCC2)cc2c(-c3ccc(NC(=O)c4ccc(C#N)cc4)cc3)ncnc21"	"IC50"	"'='"	"17500.0"	"nM"	"4.76"	""	""	"UO_0000065"	"9.64"	"0.18"	"1.18"	"4.10"	"False"	"CHEMBL3802364"	"Inhibition of JAK2 in GMCSF-stimulated human TF1 cells assessed as suppression of STAT5 phosphorylation preincubated for 2 hrs followed by GMCSF stimulation for 50 mins by FACS reader analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"CHEMBL3307972"	""
"CHEMBL3799642"	""	"0"	"523.60"	"1"	"3.21"	"16g"	"Cn1c(C(=O)NCCCN2CCOCC2)cc2c(-c3ccc(NC(=O)c4ccc(C#N)cc4)cc3)ncnc21"	"IC50"	"'>'"	"20000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3802364"	"Inhibition of JAK2 in GMCSF-stimulated human TF1 cells assessed as suppression of STAT5 phosphorylation preincubated for 2 hrs followed by GMCSF stimulation for 50 mins by FACS reader analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"CHEMBL3307972"	""
"CHEMBL3426891"	""	"0"	"402.93"	"0"	"3.22"	"(R)-9b"	"CN1CCN(c2ccc(Nc3ncc(Cl)c(NC[C@H]4CCCO4)n3)cc2)CC1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	""	"UO_0000065"	"20.41"	"0.40"	"5.00"	"12.54"	"False"	"CHEMBL3429144"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) peptide substrate by 33P Hotspot assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3425491"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL3645550"	""	"0"	"311.77"	"0"	"3.86"	"BDBM107136"	"CC(Cl)C(=O)Nc1cccc(-c2cnc3ccccc3n2)c1"	"IC50"	"'>'"	"50000.0"	"nM"	""	""	"226374"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL4280050"	""	"0"	"463.54"	"0"	"4.60"	"52"	"CC(=O)Nc1ccc(-c2nc(Nc3ccc(OCCCCCC(=O)NO)cc3)ncc2C)cc1"	"IC50"	"'='"	"25.6"	"nM"	"7.59"	""	""	"UO_0000065"	"16.38"	"0.30"	"2.99"	"6.05"	"False"	"CHEMBL4268221"	"Inhibition of human JAK2 using poly(Glu:Tyr)(4:1) as substrate preincubated for 20 mins followed by [gamma33P]ATP addition measured after 120 mins by ion exchange filter paper method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4265943"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2018"	"None"	""
"CHEMBL3645082"	""	"0"	"513.57"	"1"	"3.88"	"BDBM99853"	"CS(=O)(=O)c1ccc(OCC(F)F)c(-c2cccn3nc(Nc4ccc5c(c4)CCNCC5)nc23)c1"	"IC50"	"'='"	"600.24"	"nM"	"6.22"	""	"216524"	"UO_0000065"	"12.11"	"0.24"	"2.34"	"6.37"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL4447631"	""	"0"	"467.59"	"0"	"4.01"	"18e"	"Cc1cnc(Nc2ccc(N3CCC(N(C)CCO)CC3)c(F)c2)nc1-c1cnn(C(C)C)c1"	"IC50"	"'='"	"10.4"	"nM"	"7.98"	""	""	"UO_0000065"	"17.07"	"0.32"	"3.97"	"9.70"	"False"	"CHEMBL4323962"	"Inhibition of JAK2 in human PBMC cells assessed as reduction in GM-CSF-induced STAT5 phosphorylation by flow cytometry"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4321837"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL1078720"	""	"0"	"458.57"	"0"	"4.25"	"36"	"CCN(CC)CCCOc1ccc(Nc2nccc(-c3ccc(C(=O)NCC#N)cc3)n2)cc1"	"IC50"	"'='"	"166.0"	"nM"	"6.78"	""	""	"UO_0000065"	"14.78"	"0.27"	"2.53"	"6.57"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL3960243"	""	"0"	"458.54"	"0"	"4.48"	"BDBM229427"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(N2CCc3ccccc32)CC1"	"IC50"	"'='"	"137.0"	"nM"	"6.86"	""	"401178"	"UO_0000065"	"14.97"	"0.28"	"2.38"	"6.87"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL1288062"	""	"0"	"369.36"	"0"	"2.61"	"23"	"CCOC(=O)c1cccc(Nc2nc(N)n(C(=O)c3ccccc3F)n2)c1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1292866"	"Inhibition of human recombinant JAK2 by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287810"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL3649611"	""	"0"	"467.50"	"1"	"5.01"	"BDBM130305"	"CN1CCC(Nc2ccc3c(c2)[nH]c2c(C(N)=O)cc(-c4cccc(C(F)(F)F)c4)nc23)CC1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"262091"	"UO_0000065"	"19.25"	"0.36"	"3.99"	"10.34"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3646836"	""	"0"	"459.50"	"0"	"3.58"	"BDBM130284"	"COc1ccc(-c2cc(C(N)=O)c3[nH]c4ccc(C(=O)N5CCOCC5)cc4c3c2)cc1OC"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"262070"	"UO_0000065"	"17.89"	"0.33"	"4.64"	"7.69"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3652396"	""	"0"	"441.58"	"0"	"1.01"	"BDBM113208"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCS(=O)(=O)CC2)CC1"	"IC50"	"'='"	"44.6"	"nM"	"7.35"	""	"234651"	"UO_0000065"	"16.65"	"0.35"	"6.34"	"6.32"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3655104"	""	"0"	"363.45"	"0"	"0.60"	"BDBM159771"	"CN(CCC#N)S(=O)(=O)N[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"412.0"	"nM"	"6.38"	""	"302581"	"UO_0000065"	"17.57"	"0.35"	"5.79"	"5.41"	"True"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652348"	""	"0"	"478.62"	"0"	"1.46"	"BDBM113159"	"CN(C)C(=O)CO[C@@H]1CCN(S(=O)(=O)C[C@H]2CC[C@H](N(C)c3ncnc4[nH]ccc34)CC2)C1"	"IC50"	"'='"	"50.2"	"nM"	"7.30"	""	"234602"	"UO_0000065"	"15.25"	"0.30"	"5.84"	"6.53"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3652299"	""	"0"	"492.65"	"0"	"2.88"	"BDBM113108"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC[C@H](NC(=O)OC(C)(C)C)C2)CC1"	"IC50"	"'='"	"48.4"	"nM"	"7.32"	""	"234552"	"UO_0000065"	"14.85"	"0.29"	"4.44"	"6.07"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3651061"	""	"0"	"407.47"	"0"	"3.25"	"BDBM47232"	"CCOC(=O)c1c[nH]c2ncnc(-c3cccc(NC(=O)/C(C)=C/CN(C)C)c3)c12"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"198765"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652405"	""	"0"	"406.56"	"0"	"1.53"	"BDBM113217"	"CN1CCN(S(=O)(=O)C[C@H]2CC[C@H](N(C)c3ncnc4[nH]ccc34)CC2)CC1"	"IC50"	"'='"	"0.109"	"nM"	"9.96"	""	"234660"	"UO_0000065"	"24.50"	"0.49"	"8.43"	"11.66"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3645098"	""	"0"	"443.56"	"0"	"3.85"	"BDBM99872"	"COc1ccc(CNc2cccn3nc(Nc4ccc(N5CCN(C)CC5)cc4)nc23)cc1"	"IC50"	"'='"	"3021.96"	"nM"	"5.52"	""	"216540"	"UO_0000065"	"12.44"	"0.23"	"1.67"	"7.89"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3665205"	""	"0"	"458.55"	"0"	"0.82"	"BDBM112604"	"CS(=O)(=O)N1CCC[C@H](Nc2nc(N3CC[C@H](O)C3)ncc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.1694"	"nM"	"9.77"	""	"233841"	"UO_0000065"	"21.31"	"0.42"	"8.95"	"6.97"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3665167"	""	"0"	"415.52"	"0"	"2.28"	"BDBM112560"	"CC(C)CS(=O)(=O)N1CCC[C@H](Nc2nccnc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.0797"	"nM"	"10.10"	""	"233798"	"UO_0000065"	"24.30"	"0.48"	"7.82"	"8.65"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3645040"	""	"0"	"488.57"	"0"	"3.78"	"BDBM99807"	"COc1ccc(F)cc1-c1cccn2nc(Nc3ccc4c(c3)CCN(CC(=O)N(C)C)CC4)nc12"	"IC50"	"'='"	"11.29"	"nM"	"7.95"	""	"216480"	"UO_0000065"	"16.27"	"0.30"	"4.17"	"10.60"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647842"	""	"0"	"399.88"	"0"	"3.38"	"BDBM147951"	"N#C[C@H]1C[C@](O)(C2CC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	"285885"	"UO_0000065"	"20.01"	"0.39"	"4.62"	"6.84"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652317"	""	"0"	"492.65"	"0"	"1.89"	"BDBM113127"	"COCCC1(C(N)=O)CCN(S(=O)(=O)C[C@H]2CC[C@H](N(C)c3ncnc4[nH]ccc34)CC2)CC1"	"IC50"	"'='"	"8.97"	"nM"	"8.05"	""	"234570"	"UO_0000065"	"16.33"	"0.32"	"6.16"	"5.98"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3645091"	""	"0"	"485.49"	"1"	"5.41"	"BDBM99865"	"FC(F)COc1ccc(C(F)F)cc1-c1cccn2nc(Nc3ccc4c(c3)CCNCC4)nc12"	"IC50"	"'='"	"203.1"	"nM"	"6.69"	""	"216533"	"UO_0000065"	"13.78"	"0.26"	"1.28"	"10.54"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3644970"	""	"0"	"399.50"	"0"	"3.97"	"BDBM99720"	"COCc1ccccc1-c1cccc2nc(Nc3ccc4c(c3)CCNCC4)nn12"	"IC50"	"'='"	"9999.0"	"nM"	"5.00"	""	"216410"	"UO_0000065"	"12.52"	"0.23"	"1.03"	"7.88"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL4476828"	""	"0"	"468.52"	"0"	"3.72"	"14h"	"Cc1nc2cc(Nc3cc(NC4CCN(c5ccc(C#N)cn5)CC4)c(C(N)=O)cn3)ccc2o1"	"IC50"	"'='"	"400.0"	"nM"	"6.40"	""	""	"UO_0000065"	"13.66"	"0.25"	"2.68"	"4.38"	"False"	"CHEMBL4429528"	"Inhibition of human JAK2 assessed as reduction in phosphorylation of Biotin-Lyn-Substrate-2 after 1 hr in presence of ATP by ELISA"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4428070"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2016"	"None"	""
"CHEMBL3645547"	""	"0"	"332.19"	"0"	"4.04"	"BDBM107133"	"O=C(Nc1cccc(-c2cnc3ccccc3n2)c1)C(Cl)Cl"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	"226371"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647925"	""	"0"	"442.50"	"0"	"3.62"	"BDBM148043"	"CC(C)(C)OC(=O)N[C@@H]1CC[C@H](C#N)C(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)C1"	"IC50"	"'='"	"43.0"	"nM"	"7.37"	""	"285984"	"UO_0000065"	"16.65"	"0.31"	"3.75"	"5.45"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651009"	""	"0"	"407.47"	"0"	"3.38"	"BDBM153185"	"C=C(C)C(=O)Nc1cc(-c2ncnc3[nH]cc(C(=O)OCC)c23)ccc1CN(C)C"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294133"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647889"	""	"0"	"508.93"	"1"	"4.32"	"BDBM148001"	"N#C[C@@H]1C[C@H](C(=O)N[C@@H](C2CC2)C(F)(F)F)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"58.0"	"nM"	"7.24"	""	"285936"	"UO_0000065"	"14.22"	"0.28"	"2.92"	"5.75"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651008"	""	"0"	"428.47"	"0"	"2.72"	"BDBM153184"	"C=C(C)C(=O)Nc1cc(-c2ncnc3[nH]cc(C(=O)OCC)c23)ccc1S(C)(=O)=O"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294132"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647851"	""	"0"	"393.37"	"0"	"2.97"	"BDBM147960"	"N#C[C@H]1C[C@@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"90.0"	"nM"	"7.05"	""	"285894"	"UO_0000065"	"17.91"	"0.34"	"4.08"	"6.02"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703492"	""	"0"	"339.33"	"0"	"2.83"	"BDBM153136"	"CCOC(=O)c1c[nH]c2ncnc(-c3ccc4c(F)n(C)nc4c3)c12"	"IC50"	"'='"	"339.0"	"nM"	"6.47"	""	"294084"	"UO_0000065"	"19.07"	"0.35"	"3.64"	"7.55"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3650978"	""	"0"	"307.31"	"0"	"3.55"	"BDBM153152"	"CCOC(=O)c1c[nH]c2ncnc(-c3cc4ccccc4o3)c12"	"IC50"	"'='"	"61.0"	"nM"	"7.21"	""	"294100"	"UO_0000065"	"23.48"	"0.43"	"3.66"	"8.91"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652404"	""	"0"	"421.57"	"0"	"1.84"	"BDBM113216"	"C[C@H]1CN(S(=O)(=O)C[C@H]2CC[C@H](N(C)c3ncnc4[nH]ccc34)CC2)C[C@@H]1CO"	"IC50"	"'='"	"0.0165"	"nM"	"10.78"	""	"234659"	"UO_0000065"	"25.58"	"0.51"	"8.94"	"10.53"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3650982"	""	"0"	"333.35"	"0"	"2.99"	"BDBM153156"	"CCOC(=O)c1c[nH]c2ncnc(-c3ccc(-n4cccn4)cc3)c12"	"IC50"	"'='"	"121.0"	"nM"	"6.92"	""	"294104"	"UO_0000065"	"20.75"	"0.38"	"3.93"	"8.07"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3650986"	""	"0"	"351.37"	"0"	"2.71"	"BDBM153161"	"C=C(C)C(=O)Nc1cncc(-c2ncnc3[nH]cc(C(=O)OCC)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294109"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645084"	""	"0"	"423.44"	"0"	"4.85"	"BDBM99856"	"FC(F)(F)c1cccc(-c2cccn3nc(Nc4ccc5c(c4)CCNCC5)nc23)c1"	"IC50"	"'='"	"42.52"	"nM"	"7.37"	""	"216526"	"UO_0000065"	"17.41"	"0.32"	"2.52"	"13.59"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3644992"	""	"0"	"448.96"	"0"	"4.46"	"BDBM99744"	"CN1CCN(c2ccc(Nc3nc4c(OCc5cccc(Cl)c5)cccn4n3)cc2)CC1"	"IC50"	"'='"	"43.55"	"nM"	"7.36"	""	"216432"	"UO_0000065"	"16.40"	"0.31"	"2.90"	"12.71"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3301607"	"FILGOTINIB"	"4"	"425.51"	"0"	"1.98"	"filgotinib"	"O=C(Nc1nc2cccc(-c3ccc(CN4CCS(=O)(=O)CC4)cc3)n2n1)C1CC1"	"IC50"	"'='"	"25.0"	"nM"	"7.60"	""	""	"UO_0000065"	"17.87"	"0.35"	"5.62"	"7.86"	"False"	"CHEMBL3625890"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621116"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL3702967"	""	"0"	"397.45"	"0"	"3.52"	"BDBM147674"	"N#C[C@H]1C[C@@H](OCC2CC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"33.0"	"nM"	"7.48"	""	"285606"	"UO_0000065"	"18.82"	"0.35"	"3.96"	"7.06"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647752"	""	"0"	"564.63"	"1"	"4.37"	"BDBM147855"	"CN(C(C1CC1)C1CC1)[C@@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"170.0"	"nM"	"6.77"	""	"285789"	"UO_0000065"	"11.99"	"0.24"	"2.40"	"5.05"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647799"	""	"0"	"466.90"	"0"	"4.30"	"BDBM147902"	"N#C[C@H]1C[C@@H](NC2(C(F)(F)F)CC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"36.0"	"nM"	"7.44"	""	"285836"	"UO_0000065"	"15.94"	"0.32"	"3.14"	"6.84"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652319"	""	"0"	"449.62"	"0"	"2.77"	"BDBM113129"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCC(C(C)(C)O)CC2)CC1"	"IC50"	"'='"	"68.4"	"nM"	"7.17"	""	"234572"	"UO_0000065"	"15.94"	"0.32"	"4.39"	"7.00"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3642313"	""	"0"	"477.59"	"0"	"3.26"	"BDBM99585"	"CN1CCN(c2ccc(Nc3nc4cccc(-c5ccc(NS(C)(=O)=O)cc5)n4n3)cc2)CC1"	"IC50"	"'='"	"2.8"	"nM"	"8.55"	""	"216275"	"UO_0000065"	"17.91"	"0.34"	"5.29"	"9.02"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642284"	""	"0"	"409.47"	"0"	"3.63"	"BDBM99549"	"COc1ccc(Nc2nc3c(Nc4ccccc4S(C)(=O)=O)cccn3n2)cc1"	"IC50"	"'='"	"12.8"	"nM"	"7.89"	""	"216241"	"UO_0000065"	"19.28"	"0.37"	"4.26"	"8.09"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3658125"	""	"0"	"601.63"	"2"	"5.41"	"BDBM148447"	"Cc1ccc(NC(=O)c2cccc(C(F)(F)F)c2)cc1N1CCc2nc(Nc3ccc(N4CCNCC4)cc3)ncc2C1=O"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"286810"	"UO_0000065"	"13.55"	"0.25"	"2.74"	"7.96"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645016"	""	"0"	"501.59"	"2"	"5.05"	"BDBM99768"	"COc1cnc(-c2cccn3nc(Nc4ccc(C5CCN(C(=O)OC(C)(C)C)CC5)cc4)nc23)cn1"	"IC50"	"'='"	"1491.53"	"nM"	"5.83"	""	"216455"	"UO_0000065"	"11.62"	"0.22"	"0.78"	"5.46"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703074"	""	"0"	"450.44"	"0"	"3.63"	"BDBM147786"	"N#C[C@H]1C[C@@H](N2CC(F)C2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"30.0"	"nM"	"7.52"	""	"285720"	"UO_0000065"	"16.70"	"0.32"	"3.89"	"7.53"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703001"	""	"0"	"460.50"	"0"	"4.46"	"BDBM147711"	"C[C@H]1C[C@H](C)N1[C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(C(F)(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"335.0"	"nM"	"6.47"	""	"285645"	"UO_0000065"	"14.06"	"0.27"	"2.01"	"6.48"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647921"	""	"0"	"441.44"	"0"	"3.27"	"BDBM148034"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"119.0"	"nM"	"6.92"	""	"285974"	"UO_0000065"	"15.69"	"0.32"	"3.65"	"5.29"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3963389"	""	"0"	"425.46"	"0"	"3.10"	"BDBM255018"	"COCN1CN([C@H]2CC[C@H](CNCC(F)(F)F)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	"443874"	"UO_0000065"	"18.80"	"0.36"	"4.90"	"10.89"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3936693"	""	"0"	"409.46"	"0"	"3.51"	"BDBM255024"	"CCN1CN([C@H]2CC[C@H](CNCC(F)(F)F)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"23.0"	"nM"	"7.64"	""	"443880"	"UO_0000065"	"18.65"	"0.36"	"4.13"	"11.89"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3947242"	""	"0"	"459.49"	"0"	"2.45"	"BDBM254980"	"CN1CN([C@H]2CC[C@H](CNS(=O)(=O)CC(F)(F)F)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"1.8"	"nM"	"8.74"	""	"443887"	"UO_0000065"	"19.03"	"0.39"	"6.29"	"8.89"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3702973"	""	"0"	"470.48"	"0"	"2.47"	"BDBM147681"	"CNC1CCC(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"285614"	"UO_0000065"	"17.64"	"0.35"	"5.83"	"5.81"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647788"	""	"0"	"380.50"	"0"	"3.35"	"BDBM147891"	"CC(C)(C)N[C@H]1CCC(n2cc(C(N)=O)c(Nc3ccccc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"28.0"	"nM"	"7.55"	""	"285825"	"UO_0000065"	"19.85"	"0.37"	"4.20"	"6.94"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647811"	""	"0"	"430.94"	"0"	"3.19"	"BDBM147915"	"COCCN(C)[C@H]1CCC(n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	"285849"	"UO_0000065"	"17.87"	"0.35"	"4.51"	"7.05"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4526032"	""	"0"	"410.40"	"0"	"1.88"	"21"	"Cn1cc(Nc2nccc(N3C[C@H]4CC[C@H](C3)N4C(=O)NCC(F)(F)F)n2)cn1"	"IC50"	"'='"	"146.0"	"nM"	"6.84"	""	""	"UO_0000065"	"16.66"	"0.32"	"4.96"	"7.49"	"False"	"CHEMBL4411595"	"Inhibition of human JAK2 using fluorescence labeled peptide as substrate and using 1 mM ATP by microfluidic based mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4411260"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3645114"	""	"0"	"393.47"	"0"	"2.85"	"BDBM99888"	"CS(=O)(=O)c1ccc(-c2cccn3nc(NCCc4cccnc4)nc23)cc1"	"IC50"	"'='"	"1977.01"	"nM"	"5.70"	""	"216556"	"UO_0000065"	"14.50"	"0.28"	"2.85"	"6.39"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL4084049"	""	"0"	"532.61"	"1"	"4.02"	"37"	"O=C(CCCCCCC(=O)Nc1ccc(NC(=O)CCCn2cc(-c3ncnc4[nH]ccc34)cn2)cc1)NO"	"IC50"	"'='"	"1200.0"	"nM"	"5.92"	""	""	"UO_0000065"	"11.12"	"0.21"	"1.90"	"3.55"	"False"	"CHEMBL4031305"	"Inhibition of human JAK2 using poly[Glu:Tyr] as substrate in presence of [gamma-33P]-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028864"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4588333"	""	"0"	"444.51"	"0"	"4.56"	"9"	"N#CC[C@H]1CC[C@H](n2c(CC(=O)NCc3ccc(F)cc3)nc3cnc4[nH]ccc4c32)CC1"	"IC50"	"'='"	"28.0"	"nM"	"7.55"	""	""	"UO_0000065"	"16.99"	"0.31"	"2.99"	"7.60"	"False"	"CHEMBL4404829"	"Inhibition of JAK2/JAK2 in human PBMC assessed as reduction in GM-CSF-induced STAT5 phosphorylation pre-incubated for 30 mins before GM-CSF stimulation for 30 mins AlphaLISAassay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402578"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL3647923"	""	"0"	"455.46"	"0"	"3.32"	"BDBM148039"	"N#C[C@@H]1CCCCC1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)CC(F)(F)F)cc2)n1"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	"285980"	"UO_0000065"	"17.00"	"0.34"	"4.42"	"5.92"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702934"	""	"0"	"327.36"	"0"	"2.93"	"BDBM147636"	"N#C[C@H]1CC(F)CCC1n1cc(C(N)=O)c(Nc2ccccc2)n1"	"IC50"	"'='"	"28.0"	"nM"	"7.55"	""	"285567"	"UO_0000065"	"23.07"	"0.43"	"4.62"	"7.81"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665222"	""	"0"	"411.49"	"0"	"2.00"	"BDBM112622"	"C[C@H]1C[C@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)CN(S(=O)(=O)CC#N)C1"	"IC50"	"'='"	"0.0332"	"nM"	"10.48"	""	"233859"	"UO_0000065"	"25.47"	"0.49"	"8.48"	"8.21"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3639467"	""	"0"	"399.48"	"0"	"2.31"	"BDBM148045"	"N#C[C@@H]1CCCC[C@H]1n1cc(C(N)=O)c(Nc2ccc3c(c2)CCS3(=O)=O)n1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"285991"	"UO_0000065"	"21.02"	"0.41"	"6.09"	"6.42"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4437638"	""	"0"	"390.49"	"0"	"3.97"	"8"	"N#CC[C@H]1CC[C@H](n2c(CNC(=O)CC3CC3)nc3cnc4[nH]ccc4c32)CC1"	"IC50"	"'='"	"22.0"	"nM"	"7.66"	""	""	"UO_0000065"	"19.61"	"0.36"	"3.69"	"7.70"	"False"	"CHEMBL4404825"	"Inhibition of JAK2-JH1/JH2 domain (532 to 1132 residues) (unknown origin) pre-incubated before NH2-KGGEEEEYFELVKK-CO2 substrate addition and measured after 90 mins by MS analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402578"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL3116051"	""	"0"	"367.39"	"0"	"2.55"	"19b"	"C[C@H](Nc1nc(Nc2cn(C)cn2)c2ccn(C)c2n1)c1ncc(F)cn1"	"IC50"	"'='"	"27.0"	"nM"	"7.57"	""	""	"UO_0000065"	"20.60"	"0.38"	"5.02"	"7.69"	"False"	"CHEMBL3118240"	"Inhibition of Jak2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112447"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL1290090"	""	"0"	"446.28"	"1"	"6.35"	"9"	"CC(Nc1nc2cc[nH]c(=O)c2cc1-c1ccc(F)cc1)c1cc(F)c(Cl)cc1Cl"	"IC50"	"'='"	"3940.0"	"nM"	"5.41"	""	""	"UO_0000065"	"12.11"	"0.25"	"-0.95"	"9.35"	"False"	"CHEMBL1291235"	"Inhibition of JAK2 in cell-free system"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287746"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL4452640"	""	"0"	"459.51"	"0"	"1.82"	"11b"	"C=CC(=O)Nc1ccc(Cn2nc(-c3cc(N4CCOCC4)n(C)n3)c3c(N)ncnc32)cc1"	"IC50"	"'='"	"604.7"	"nM"	"6.22"	""	""	"UO_0000065"	"13.53"	"0.25"	"4.40"	"4.82"	"False"	"CHEMBL4402146"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-biotin as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4400567"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4439150"	""	"0"	"378.23"	"0"	"1.32"	"10i"	"N#CCC(=O)N1CCCC(Cn2nc(Br)c3c(N)ncnc32)C1"	"IC50"	"'='"	"396.4"	"nM"	"6.40"	""	""	"UO_0000065"	"16.93"	"0.38"	"5.08"	"5.63"	"False"	"CHEMBL4402146"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-biotin as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4400567"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4526982"	""	"0"	"394.44"	"0"	"1.05"	"11m"	"C=CC(=O)N1CCC(Cn2nc(-c3cc(C=O)n(C)n3)c3c(N)ncnc32)CC1"	"IC50"	"'='"	"914.5"	"nM"	"6.04"	""	""	"UO_0000065"	"15.31"	"0.28"	"4.99"	"4.84"	"False"	"CHEMBL4402146"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-biotin as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4400567"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL2178252"	""	"0"	"352.79"	"0"	"3.04"	"13a"	"Cn1cc(NC(=O)c2cnn3cccnc23)c(-c2cccc(Cl)c2)n1"	"IC50"	"'='"	"89.8"	"nM"	"7.05"	""	""	"UO_0000065"	"19.97"	"0.38"	"4.01"	"9.14"	"False"	"CHEMBL2186598"	"Inhibition of JAK2 V617F mutant in human SET2 cells assessed as reduction in STAT5 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176876"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2178250"	""	"0"	"363.81"	"0"	"4.01"	"10c"	"Cc1cc(NC(=O)c2cnn3cccnc23)c(-c2cccc(Cl)c2)cn1"	"IC50"	"'='"	"1100.0"	"nM"	"5.96"	""	""	"UO_0000065"	"16.38"	"0.31"	"1.95"	"8.26"	"False"	"CHEMBL2186598"	"Inhibition of JAK2 V617F mutant in human SET2 cells assessed as reduction in STAT5 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176876"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1835148"	""	"0"	"413.49"	"0"	"3.45"	"59"	"NC(=O)c1cnc(NC(C2CC2)C2CC2)c2c1[nH]c1cc(-c3cnc(N)cn3)ccc12"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	""	"UO_0000065"	"20.31"	"0.37"	"4.95"	"6.19"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835016"	""	"0"	"286.31"	"0"	"2.78"	"19"	"CCCNc1ncc(C(N)=O)c2[nH]c3ccc(F)cc3c12"	"IC50"	"'='"	"68.0"	"nM"	"7.17"	""	""	"UO_0000065"	"25.03"	"0.47"	"4.39"	"8.55"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835035"	""	"0"	"387.49"	"0"	"4.57"	"38"	"Cn1cc(-c2ccc3c(c2)[nH]c2c(C(N)=O)ccc(NC4CCCCC4)c23)cn1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	""	"UO_0000065"	"21.42"	"0.39"	"3.73"	"9.36"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835039"	""	"0"	"389.50"	"0"	"4.67"	"42"	"C[C@H](Nc1ccc(C(N)=O)c2[nH]c3cc(-c4cnn(C)c4)ccc3c12)C(C)(C)C"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	""	"UO_0000065"	"21.31"	"0.39"	"3.63"	"9.36"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835040"	""	"0"	"431.58"	"1"	"5.79"	"43"	"CC(C)Cn1cc(-c2ccc3c(c2)[nH]c2c(C(N)=O)ccc(N[C@@H](C)C(C)(C)C)c23)cn1"	"IC50"	"'='"	"41.0"	"nM"	"7.39"	""	""	"UO_0000065"	"17.12"	"0.32"	"1.60"	"8.33"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835141"	""	"0"	"400.49"	"0"	"3.82"	"52"	"Cn1cc(-c2ccc3c(c2)[nH]c2c(C(N)=O)cnc(NC(C4CC4)C4CC4)c23)cn1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	""	"UO_0000065"	"21.72"	"0.40"	"4.88"	"8.56"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL3403550"	""	"0"	"405.77"	"0"	"3.96"	"23"	"NC(=O)c1cc(-c2ncnn3cccc23)cn1-c1cc(C(F)(F)F)ccc1Cl"	"IC50"	"'='"	"85.0"	"nM"	"7.07"	""	""	"UO_0000065"	"17.43"	"0.34"	"3.11"	"9.04"	"False"	"CHEMBL3404501"	"Inhibition of recombinant epitope-tagged JAK2 (808 to 1132) (unknown origin) using LPLDKDYYVVREPGQ as substrate by beta-countiing analysis in presence of 33P-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3400063"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3403549"	""	"0"	"405.77"	"0"	"4.19"	"22"	"NC(=O)c1cc(-c2ncnc3[nH]ccc23)cn1-c1cc(C(F)(F)F)ccc1Cl"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	""	"UO_0000065"	"22.18"	"0.44"	"4.81"	"10.05"	"False"	"CHEMBL3404501"	"Inhibition of recombinant epitope-tagged JAK2 (808 to 1132) (unknown origin) using LPLDKDYYVVREPGQ as substrate by beta-countiing analysis in presence of 33P-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3400063"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3402476"	""	"0"	"284.75"	"0"	"3.68"	"2"	"Cc1ccc(Cl)cc1-c1ccc(-c2ccnc(N)n2)[nH]1"	"IC50"	"'='"	"972.0"	"nM"	"6.01"	""	""	"UO_0000065"	"21.11"	"0.41"	"2.33"	"8.90"	"False"	"CHEMBL3404501"	"Inhibition of recombinant epitope-tagged JAK2 (808 to 1132) (unknown origin) using LPLDKDYYVVREPGQ as substrate by beta-countiing analysis in presence of 33P-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3400063"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3330104"	""	"0"	"327.78"	"0"	"2.78"	"1"	"Cc1ccc(Cl)cc1-c1[nH]c(-c2ccnc(N)n2)cc1C(N)=O"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	""	"UO_0000065"	"23.49"	"0.46"	"4.92"	"6.96"	"False"	"CHEMBL3404501"	"Inhibition of recombinant epitope-tagged JAK2 (808 to 1132) (unknown origin) using LPLDKDYYVVREPGQ as substrate by beta-countiing analysis in presence of 33P-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3400063"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL2376040"	""	"0"	"464.48"	"0"	"1.75"	"3"	"COc1cc(-c2cnc3[nH]cc(C(=O)N[C@H](C)C(=O)N4CC(C#N)C4)c3n2)cc(OC)c1OC"	"IC50"	"'='"	"0.8"	"nM"	"9.10"	""	""	"UO_0000065"	"19.59"	"0.37"	"7.35"	"6.39"	"False"	"CHEMBL2378515"	"Inhibition of JAK2 (unknown origin) using [33gammaP]ATP and Biotin-KAIETDKEYYTVKD as substrate incubated for 10 mins prior to substrate addition measured after 30 mins by filtration assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375236"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2325895"	""	"0"	"380.45"	"0"	"1.96"	"2a"	"CC(C)(C)[C@@H](NC(=O)c1c[nH]c2ncc(C3CC3)nc12)C(=O)N1CC(C#N)C1"	"IC50"	"'='"	"0.8"	"nM"	"9.10"	""	""	"UO_0000065"	"23.91"	"0.44"	"7.14"	"7.93"	"False"	"CHEMBL2378515"	"Inhibition of JAK2 (unknown origin) using [33gammaP]ATP and Biotin-KAIETDKEYYTVKD as substrate incubated for 10 mins prior to substrate addition measured after 30 mins by filtration assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375236"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2376157"	""	"0"	"432.42"	"0"	"1.51"	"8"	"C[C@@H](NC(=O)c1c[nH]c2ncc(-c3ncn4cc(F)ccc34)nc12)C(=O)N1CC(C#N)C1"	"IC50"	"'='"	"5.9"	"nM"	"8.23"	""	""	"UO_0000065"	"19.03"	"0.35"	"6.72"	"6.23"	"False"	"CHEMBL2378515"	"Inhibition of JAK2 (unknown origin) using [33gammaP]ATP and Biotin-KAIETDKEYYTVKD as substrate incubated for 10 mins prior to substrate addition measured after 30 mins by filtration assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375236"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2376148"	""	"0"	"453.47"	"0"	"1.48"	"6e"	"C[C@@H](NC(=O)c1c[nH]c2ncc(-c3nn(C)c4cc(C#N)ccc34)nc12)C(=O)N1CC(C#N)C1"	"IC50"	"'='"	"38.0"	"nM"	"7.42"	""	""	"UO_0000065"	"16.36"	"0.30"	"5.94"	"4.74"	"False"	"CHEMBL2378515"	"Inhibition of JAK2 (unknown origin) using [33gammaP]ATP and Biotin-KAIETDKEYYTVKD as substrate incubated for 10 mins prior to substrate addition measured after 30 mins by filtration assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375236"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2376143"	""	"0"	"461.91"	"0"	"2.87"	"5"	"C[C@@H](NC(=O)c1c[nH]c2ncc(-c3cn(C)c4cc(Cl)ccc34)nc12)C(=O)N1CC(C#N)C1"	"IC50"	"'='"	"170.0"	"nM"	"6.77"	""	""	"UO_0000065"	"14.66"	"0.28"	"3.90"	"5.66"	"False"	"CHEMBL2378509"	"Inhibition of JAK2 in human monocytes expressing CD14 assessed as inhibition of GM-CSF-stimulated STAT5a phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375236"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2376150"	""	"0"	"468.52"	"0"	"2.49"	"6g"	"C[C@@H](NC(=O)c1c[nH]c2ncc(-c3nn(C)c4cc(C5CC5)ccc34)nc12)C(=O)N1CC(C#N)C1"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	""	"UO_0000065"	"16.70"	"0.31"	"5.33"	"5.90"	"False"	"CHEMBL2378515"	"Inhibition of JAK2 (unknown origin) using [33gammaP]ATP and Biotin-KAIETDKEYYTVKD as substrate incubated for 10 mins prior to substrate addition measured after 30 mins by filtration assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375236"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL4249784"	""	"0"	"379.43"	"0"	"0.96"	"10c"	"Cn1cc(-c2nn(CC3CCN(C(=O)CC#N)CC3)c3ncnc(N)c23)cn1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4240663"	""	"0"	"323.36"	"0"	"0.93"	"12g"	"Cn1cc(-c2nn(C3CCCN(C#N)C3)c3ncnc(N)c23)cn1"	"IC50"	"'='"	"168.4"	"nM"	"6.77"	""	""	"UO_0000065"	"20.95"	"0.39"	"5.84"	"5.92"	"False"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL3747681"	""	"0"	"357.85"	"0"	"3.31"	"20"	"COc1ccc(-c2nc3c(NCC4CCNC4)c(Cl)cnc3[nH]2)cc1"	"IC50"	"'='"	"13900.0"	"nM"	"4.86"	""	""	"UO_0000065"	"13.57"	"0.27"	"1.55"	"6.49"	"False"	"CHEMBL3751000"	"Inhibition of N-terminal GST-fused recombinant JAK2 (831 to 1132 residues) (unknown origin) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate by microfluidic capillary electrophoresis method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3745697"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3747077"	""	"0"	"407.85"	"0"	"3.98"	"29"	"COc1cc(F)c(-c2nc3c(NCC4CCNCC4)c(Cl)cnc3[nH]2)cc1F"	"IC50"	"'>'"	"17000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3751000"	"Inhibition of N-terminal GST-fused recombinant JAK2 (831 to 1132 residues) (unknown origin) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate by microfluidic capillary electrophoresis method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3745697"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3799984"	""	"0"	"462.51"	"1"	"5.24"	"12f"	"Cn1c(C(=O)OCc2ccccc2)cc2c(-c3ccc(NC(=O)c4ccccc4)cc3)ncnc21"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL3802364"	"Inhibition of JAK2 in GMCSF-stimulated human TF1 cells assessed as suppression of STAT5 phosphorylation preincubated for 2 hrs followed by GMCSF stimulation for 50 mins by FACS reader analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"CHEMBL3307972"	""
"CHEMBL3699526"	""	"0"	"337.38"	"0"	"2.79"	"BDBM147544"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C=O)cc2)n1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"285474"	"UO_0000065"	"25.26"	"0.47"	"5.73"	"7.49"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3658869"	""	"0"	"378.48"	"0"	"1.67"	"BDBM159788"	"Cc1ncc(S(=O)(=O)N[C@H]2C[C@@H](N(C)c3ncnc4[nH]ccc34)C2)s1"	"IC50"	"'='"	"512.0"	"nM"	"6.29"	""	"302598"	"UO_0000065"	"16.62"	"0.34"	"4.62"	"6.06"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651027"	""	"0"	"390.40"	"0"	"3.03"	"BDBM153204"	"CCOC(=O)c1c[nH]c2ncnc(-c3cccc(NC(=O)C4=CC(=O)CC4)c3)c12"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294152"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703025"	""	"0"	"462.48"	"0"	"3.26"	"BDBM147735"	"N#C[C@H]1C[C@@H](N2CCC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc([C@H](O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	"285669"	"UO_0000065"	"17.21"	"0.33"	"4.70"	"6.62"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3644975"	""	"0"	"453.47"	"0"	"4.86"	"BDBM99725"	"COc1cc(C(F)(F)F)ccc1-c1cccc2nc(Nc3ccc4c(c3)CCNCC4)nn12"	"IC50"	"'='"	"7.4"	"nM"	"8.13"	""	"216415"	"UO_0000065"	"17.93"	"0.34"	"3.27"	"12.81"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3589328"	""	"0"	"386.46"	"0"	"3.63"	"20"	"Cc1ccc(-c2cc(C(N)=O)c3[nH]c4cc(N5CCOCC5)ccc4c3c2)cn1"	"IC50"	"'='"	"6.1"	"nM"	"8.21"	""	""	"UO_0000065"	"21.26"	"0.39"	"4.58"	"9.75"	"False"	"CHEMBL3592849"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3622820"	"ITACITINIB"	"3"	"553.52"	"1"	"3.60"	"1"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccnc(C(F)(F)F)c3F)CC2)C1"	"IC50"	"'>'"	"100.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3114761"	""	"0"	"483.50"	"0"	"3.84"	"11e"	"O=C1NC(=O)C(c2c[nH]c3ccccc23)=C1Nc1cccc(O[C@H]2CCN(c3ccnc(F)c3)C2)c1"	"IC50"	"'='"	"1480.0"	"nM"	"5.83"	""	""	"UO_0000065"	"12.06"	"0.22"	"1.99"	"5.87"	"False"	"CHEMBL3118993"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112442"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3647877"	""	"0"	"466.97"	"0"	"3.87"	"BDBM147989"	"N#C[C@@H]1C[C@H](C(=O)N2CC3(CCC3)C2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"133.0"	"nM"	"6.88"	""	"285924"	"UO_0000065"	"14.73"	"0.28"	"3.01"	"5.88"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642289"	""	"0"	"490.63"	"0"	"4.07"	"BDBM99554"	"CC(C)S(=O)(=O)c1ccc(-c2cccn3nc(Nc4ccc(N5CCN(C)CC5)cc4)nc23)cc1"	"IC50"	"'='"	"2.1"	"nM"	"8.68"	""	"216245"	"UO_0000065"	"17.69"	"0.34"	"4.61"	"10.48"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL1290308"	""	"0"	"359.47"	"0"	"2.06"	"14"	"CC(Nc1nc2cc[nH]c(=O)c2cc1C(=O)NCCN(C)C)C(C)(C)C"	"IC50"	"'='"	"8350.0"	"nM"	"5.08"	""	""	"UO_0000065"	"14.13"	"0.27"	"3.02"	"5.64"	"False"	"CHEMBL1291235"	"Inhibition of JAK2 in cell-free system"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287746"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1290651"	""	"0"	"375.74"	"0"	"4.89"	"31"	"O=c1[nH]ccc2nc(Nc3c(F)cc(F)cc3Cl)c3ccc(F)cc3c12"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	""	"UO_0000065"	"22.35"	"0.44"	"3.51"	"14.53"	"False"	"CHEMBL1291235"	"Inhibition of JAK2 in cell-free system"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287746"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL4465022"	""	"0"	"543.67"	"1"	"4.64"	"19a"	"CC(=O)c1ccc(NC(=O)N2CCN(c3ccnc(Nc4ccc(OCCCN5CCCC5)cc4)n3)CC2)cc1"	"IC50"	"'='"	"65.0"	"nM"	"7.19"	""	""	"UO_0000065"	"13.22"	"0.25"	"2.55"	"6.98"	"False"	"CHEMBL4362531"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain (826 to 1132 resiudes) expressed in baculovirus expression system using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition measured after 1 hr in presence of ATP by mobility shift assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4359878"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2019"	"None"	""
"CHEMBL4459585"	"ROPSACITINIB"	"2"	"383.42"	"0"	"2.54"	"10; PF-06826647"	"Cn1cc(-c2cn3nccc3c(-c3cnn([C@]4(CC#N)C[C@@H](C#N)C4)c3)n2)cn1"	"IC50"	"'='"	"74.0"	"nM"	"7.13"	""	""	"UO_0000065"	""	""	""	""	"True"	"CHEMBL4377465"	"Inhibition of recombinant human JAK2 kinase domain using FITC-KGGEEEEYFELVKK as substrate incubated for 60 mins by caliper method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4376812"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL3746397"	""	"0"	"394.48"	"0"	"2.49"	"24"	"COc1ccc(-c2nc3c(NCC4CCN(C)CC4)c(C(N)=O)cnc3[nH]2)cc1"	"IC50"	"'='"	"10300.0"	"nM"	"4.99"	""	""	"UO_0000065"	"12.64"	"0.23"	"2.50"	"4.57"	"False"	"CHEMBL3751000"	"Inhibition of N-terminal GST-fused recombinant JAK2 (831 to 1132 residues) (unknown origin) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate by microfluidic capillary electrophoresis method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3745697"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3114774"	""	"0"	"457.47"	"0"	"3.67"	"8d"	"O=C1NC(=O)C(c2c[nH]c3ccccc23)=C1Nc1cccc(OCCNc2ccnc(F)c2)c1"	"IC50"	"'='"	"2130.0"	"nM"	"5.67"	""	""	"UO_0000065"	"12.40"	"0.23"	"2.00"	"5.24"	"False"	"CHEMBL3118993"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112442"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3116050"	""	"0"	"353.37"	"0"	"2.54"	"19a"	"C[C@H](Nc1nc(Nc2cn(C)cn2)c2cc[nH]c2n1)c1ncc(F)cn1"	"IC50"	"'='"	"54.0"	"nM"	"7.27"	""	""	"UO_0000065"	"20.57"	"0.38"	"4.73"	"6.65"	"False"	"CHEMBL3116826"	"Inhibition of Jak2 V617F mutant in human SET2 cells assessed as inhibition of STAT5 phosphorylation after 24 hrs by Western blotting analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112447"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL3114773"	""	"0"	"457.47"	"0"	"3.67"	"8c"	"O=C1NC(=O)C(c2c[nH]c3ccccc23)=C1Nc1ccccc1OCCNc1ccnc(F)c1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3118993"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112442"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL366266"	""	"0"	"411.47"	"0"	"3.41"	"5, JP539654"	"O=C1NC(=O)C(c2cn(CCCn3ccnc3)c3ccccc23)=C1Nc1ccccc1"	"IC50"	"'='"	"3850.0"	"nM"	"5.42"	""	""	"UO_0000065"	"13.16"	"0.24"	"2.00"	"6.69"	"False"	"CHEMBL3118993"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112442"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3745777"	""	"0"	"337.43"	"0"	"3.05"	"22"	"COc1ccc(-c2nc3c(NCC4CCNCC4)ccnc3[nH]2)cc1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3751000"	"Inhibition of N-terminal GST-fused recombinant JAK2 (831 to 1132 residues) (unknown origin) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate by microfluidic capillary electrophoresis method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3745697"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3763289"	""	"0"	"260.68"	"0"	"1.95"	"3"	"Nc1n[nH]c2ccn(-c3ccccc3Cl)c(=O)c12"	"IC50"	"'='"	"1400.0"	"nM"	"5.85"	""	""	"UO_0000065"	"22.46"	"0.44"	"3.90"	"7.63"	"False"	"CHEMBL3766653"	"Inhibition of JAK2 (unknown origin) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent substrate phosphorylation after 45 mins by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3763089"	"1"	"Scientific Literature"	"J. Med. Chem."	"2016"	"None"	""
"CHEMBL4225827"	""	"0"	"912.90"	"4"	"9.88"	"47"	"CCNC(=O)c1cc2c(-c3cc(OCCCCCCn4cc(-c5nc(Nc6ccc(NC(=O)CCCCCCC(=O)O)cc6)nc6[nH]ccc56)cn4)c(Cl)cc3Cl)nc(N)nc2s1"	"IC50"	"'='"	"3760.0"	"nM"	"5.42"	""	""	"UO_0000065"	"5.94"	"0.12"	"-4.46"	"2.38"	"False"	"CHEMBL4222523"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma33P]-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219149"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2018"	"None"	""
"CHEMBL3645025"	""	"0"	"441.58"	"1"	"5.17"	"BDBM99780"	"Cc1ccc(-c2cccn3nc(Nc4ccc5c(c4)CCNCC5)nc23)c(OCC(C)C)c1"	"IC50"	"'='"	"2795.86"	"nM"	"5.55"	""	"216464"	"UO_0000065"	"12.58"	"0.23"	"0.38"	"8.75"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642309"	""	"0"	"449.54"	"0"	"3.38"	"BDBM99579"	"CS(=O)(=O)c1cccc(-c2cccc3nc(Nc4ccc(N5CCOCC5)cc4)nn23)c1"	"IC50"	"'='"	"3.2"	"nM"	"8.49"	""	"216269"	"UO_0000065"	"18.90"	"0.36"	"5.11"	"9.56"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647722"	""	"0"	"482.61"	"0"	"2.85"	"BDBM147824"	"CS(=O)(=O)c1ccc(Nc2nn([C@H]3CC[C@@H](N4CC5(CCC5)C4)C[C@@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	"285758"	"UO_0000065"	"16.21"	"0.31"	"4.97"	"5.83"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645036"	""	"0"	"467.50"	"1"	"5.25"	"BDBM99803"	"CCOc1ccc(C(F)(F)F)cc1-c1cccn2nc(Nc3ccc4c(c3)CCNCC4)nc12"	"IC50"	"'='"	"136.55"	"nM"	"6.87"	""	"216476"	"UO_0000065"	"14.68"	"0.28"	"1.61"	"10.81"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3694586"	""	"0"	"366.85"	"0"	"4.81"	"BDBM125907"	"Clc1cnc2nc1NCCCc1cccc(c1)OCc1cccc(c1)N2"	"IC50"	"'='"	"117.0"	"nM"	"6.93"	""	"255680"	"UO_0000065"	"18.90"	"0.36"	"2.12"	"11.73"	"False"	"CHEMBL3707544"	"In Vitro Kinase Assay: One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Biochemistry 1999, 269, 94-104. The catalytic domains of human JAK1 (a.a. 837-1142), JAK2 (a.a. 828-1132) and JAK3 (a.a. 781-1124) with an N-terminal His tag were expressed using baculovirus in insect cells and purified. The catalytic activity of JAK1, JAK2 or JAK3 was assayed by measuring the phosphorylation of a biotinylated peptide. The phosphorylated peptide was detected by homogenous time resolved fluorescence (HTRF). IC50s of compounds were measured for each kinase in the reactions that contain the enzyme, ATP and 500 nM peptide in 50 mM Tris (pH 7.8) buffer with 100 mM NaCl, 5 mM DTT, and 0.1 mg/mL (0.01%) BSA. The ATP concentration in the reactions was 90 uM for JAK1, 30 uM for JAK2 and 3 uM for JAK3. Reactions were carried out at room temperature for 1 hr and then stopped with 20 uL 45 mM EDTA."	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639093"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3764030"	""	"0"	"300.37"	"0"	"1.92"	"16"	"CC(C)[C@H](C)n1cc(-c2ccn(C)n2)c2[nH]nc(N)c2c1=O"	"IC50"	"'='"	"70.0"	"nM"	"7.16"	""	""	"UO_0000065"	"23.82"	"0.44"	"5.23"	"7.57"	"False"	"CHEMBL3766653"	"Inhibition of JAK2 (unknown origin) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent substrate phosphorylation after 45 mins by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3763089"	"1"	"Scientific Literature"	"J. Med. Chem."	"2016"	"None"	""
"CHEMBL1789941"	"RUXOLITINIB"	"4"	"306.37"	"0"	"3.47"	"2"	"N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"4982.0"	"nM"	"5.30"	""	""	"UO_0000065"	"17.31"	"0.31"	"1.83"	"6.37"	"False"	"CHEMBL3382736"	"Inhibition of JAK2 in human whole blood assessed as inhibition of GM-CSF-induced pSTAT5"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"CHEMBL3638178"	"Blood"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351789"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL3763213"	""	"0"	"385.47"	"0"	"1.76"	"17"	"CC(C)[C@H](C)n1cc(-c2cc(N3CCOCC3)n(C)n2)c2[nH]nc(N)c2c1=O"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	""	"UO_0000065"	"20.37"	"0.38"	"6.09"	"7.34"	"False"	"CHEMBL3766653"	"Inhibition of JAK2 (unknown origin) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent substrate phosphorylation after 45 mins by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3763089"	"1"	"Scientific Literature"	"J. Med. Chem."	"2016"	"None"	""
"CHEMBL2105759"	"BARICITINIB"	"4"	"371.43"	"0"	"1.10"	"Baricitinib"	"CCS(=O)(=O)N1CC(CC#N)(n2cc(-c3ncnc4[nH]ccc34)cn2)C1"	"IC50"	"'='"	"290.0"	"nM"	"6.54"	"Potential transcription error"	""	"UO_0000065"	""	""	""	""	"True"	"CHEMBL3766669"	"Inhibition of JAK2 in human PBMC assessed as reduction in GM-CSF-induced STAT5 phosphorylation preincubated for 5 mins followed by GM-CSF stimulation for 15 to 60 mins by flow cytometry analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3763089"	"1"	"Scientific Literature"	"J. Med. Chem."	"2016"	"None"	""
"CHEMBL2207766"	""	"0"	"457.92"	"1"	"5.75"	"6a"	"CC(=O)Nc1ccc(-c2ccnc(Nc3cccc(NC(=O)c4ccccc4Cl)c3)n2)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL2214784"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT3 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL2208029"	""	"0"	"457.46"	"0"	"4.70"	"9d"	"CC(=O)Nc1ccc(-c2nc(Nc3ccc(N4CCOCC4)cc3)ncc2C(F)(F)F)cc1"	"IC50"	"'='"	"2699.9"	"nM"	"5.57"	""	""	"UO_0000065"	"12.17"	"0.23"	"0.87"	"7.02"	"False"	"CHEMBL2214785"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT1 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL2208027"	""	"0"	"407.45"	"0"	"3.82"	"9b"	"CC(=O)Nc1ccc(-c2nc(Nc3ccc(N4CCOCC4)cc3)ncc2F)cc1"	"IC50"	"'='"	"6486.7"	"nM"	"5.19"	""	""	"UO_0000065"	"12.73"	"0.24"	"1.37"	"6.54"	"False"	"CHEMBL2214785"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT1 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL1077458"	""	"0"	"389.46"	"0"	"3.68"	"7c"	"CC(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"974.7"	"nM"	"6.01"	""	""	"UO_0000065"	"15.43"	"0.28"	"2.33"	"7.57"	"False"	"CHEMBL2214785"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT1 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL2207763"	""	"0"	"470.36"	"0"	"4.59"	"4"	"CC(=O)Nc1ccc(-c2ccnc(NCC3CN(C(=O)c4c(Cl)cccc4Cl)C3)n2)cc1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2214785"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT1 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL2208034"	""	"0"	"444.54"	"0"	"3.41"	"10d, XL019"	"O=C(Nc1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1)[C@H]1CCCN1"	"IC50"	"'='"	"2.2"	"nM"	"8.66"	""	""	"UO_0000065"	"19.48"	"0.36"	"5.25"	"9.47"	"False"	"CHEMBL2214787"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL2208030"	""	"0"	"403.49"	"0"	"3.99"	"9e"	"CC(=O)Nc1ccc(-c2cc(C)nc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'>'"	"980.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2214787"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL2207767"	""	"0"	"423.48"	"1"	"5.10"	"6b"	"CC(=O)Nc1ccc(-c2ccnc(Nc3cccc(NC(=O)c4ccccc4)c3)n2)cc1"	"IC50"	"'='"	"11.1"	"nM"	"7.96"	""	""	"UO_0000065"	"18.78"	"0.34"	"2.85"	"8.29"	"False"	"CHEMBL2214787"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL3622836"	""	"0"	"281.32"	"0"	"1.16"	"5m"	"NCCn1c(-c2ccncc2)nc2cc(C(N)=O)ccc21"	"IC50"	"'='"	"13500.0"	"nM"	"4.87"	""	""	"UO_0000065"	"17.31"	"0.32"	"3.71"	"4.88"	"False"	"CHEMBL3625898"	"Inhibition of JAK2 (unknown origin) using 35 uM of ATP and Tyr6 peptide by Z'-LYTE kinase assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621116"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL21156"	""	"0"	"309.34"	"0"	"3.99"	"pyridone-6"	"CC(C)(C)c1nc2c3ccc(F)cc3c3c(=O)[nH]ccc3c2[nH]1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	""	"UO_0000065"	"29.09"	"0.53"	"5.01"	"14.62"	"False"	"CHEMBL3625898"	"Inhibition of JAK2 (unknown origin) using 35 uM of ATP and Tyr6 peptide by Z'-LYTE kinase assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621116"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL498859"	""	"0"	"243.70"	"0"	"3.47"	"2"	"Nc1n[nH]c2ccc(-c3ccccc3Cl)cc12"	"IC50"	"'='"	"660.0"	"nM"	"6.18"	""	""	"UO_0000065"	"25.36"	"0.50"	"2.71"	"11.30"	"False"	"CHEMBL3766653"	"Inhibition of JAK2 (unknown origin) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent substrate phosphorylation after 45 mins by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3763089"	"1"	"Scientific Literature"	"J. Med. Chem."	"2016"	"None"	""
"CHEMBL3622193"	""	"0"	"592.68"	"1"	"4.93"	"34"	"CN1CCN(C(=O)c2ccc3c(c2)[nH]c2c(C(N)=O)ccc(-c4cccc(NC(=O)c5ccc(N(C)C)cc5)c4F)c23)CC1"	"IC50"	"'='"	"1020.0"	"nM"	"5.99"	""	""	"UO_0000065"	"10.11"	"0.19"	"1.06"	"5.22"	"False"	"CHEMBL3627422"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621099"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3665192"	""	"0"	"432.51"	"0"	"0.66"	"BDBM112589"	"CS(=O)(=O)N1CCC[C@H](Nc2nc(NCCO)ncc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.0668"	"nM"	"10.18"	""	"233826"	"UO_0000065"	"23.53"	"0.46"	"9.52"	"6.83"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642300"	""	"0"	"477.59"	"0"	"3.37"	"BDBM99570"	"CN1CCN(c2cccc(Nc3nc4c(Nc5ccccc5S(C)(=O)=O)cccn4n3)c2)CC1"	"IC50"	"'='"	"29.0"	"nM"	"7.54"	""	"216260"	"UO_0000065"	"15.78"	"0.30"	"4.17"	"7.95"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3645089"	""	"0"	"555.03"	"1"	"4.93"	"BDBM99862"	"CN(C)C(=O)CN1CCc2ccc(Nc3nc4c(-c5cc(Cl)ccc5OCC(F)F)cccn4n3)cc2CC1"	"IC50"	"'='"	"115.82"	"nM"	"6.94"	""	"216531"	"UO_0000065"	"12.50"	"0.24"	"2.01"	"9.25"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3699557"	""	"0"	"360.37"	"0"	"3.31"	"BDBM147575"	"N#C[C@@H]1CCCC[C@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)F)nc2)n1"	"IC50"	"'='"	"255.0"	"nM"	"6.59"	""	"285505"	"UO_0000065"	"18.30"	"0.35"	"3.28"	"6.01"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642255"	""	"0"	"402.46"	"0"	"3.38"	"BDBM99513"	"COc1ccc(-c2cccn3nc(Nc4ccc(N5CCOCC5)cc4)nc23)cn1"	"IC50"	"'='"	"13.4"	"nM"	"7.87"	""	"216205"	"UO_0000065"	"19.56"	"0.36"	"4.49"	"10.25"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642340"	""	"0"	"511.63"	"1"	"2.77"	"BDBM99614"	"CS(=O)(=O)c1ccc(-c2cccc3nc(Nc4ccc(CN5CCS(=O)(=O)CC5)cc4)nn23)cc1"	"IC50"	"'='"	"0.66"	"nM"	"9.18"	""	"216304"	"UO_0000065"	"17.94"	"0.36"	"6.41"	"8.07"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642258"	""	"0"	"449.54"	"0"	"3.38"	"BDBM99516"	"CS(=O)(=O)c1ccc(-c2cccc3nc(Nc4ccc(N5CCOCC5)cc4)nn23)cc1"	"IC50"	"'='"	"0.7"	"nM"	"9.15"	""	"216208"	"UO_0000065"	"20.37"	"0.39"	"5.77"	"10.31"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3039513"	"DECERNOTINIB"	"2"	"392.39"	"0"	"3.28"	"decernotinib"	"CC[C@@](C)(Nc1ccnc(-c2c[nH]c3ncccc23)n1)C(=O)NCC(F)(F)F"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	""	"UO_0000065"	"20.10"	"0.38"	"4.61"	"8.25"	"False"	"CHEMBL3625890"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621116"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL3622837"	""	"0"	"296.33"	"0"	"0.74"	"5n"	"NCCn1c(-c2cccnc2N)nc2cc(C(N)=O)ccc21"	"IC50"	"'='"	"4700.0"	"nM"	"5.33"	""	""	"UO_0000065"	"17.98"	"0.33"	"4.59"	"4.23"	"False"	"CHEMBL3625898"	"Inhibition of JAK2 (unknown origin) using 35 uM of ATP and Tyr6 peptide by Z'-LYTE kinase assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621116"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL3699470"	""	"0"	"325.37"	"0"	"1.95"	"BDBM147485"	"N#C[C@H]1C(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCC[C@H]1O"	"IC50"	"'='"	"635.0"	"nM"	"6.20"	""	"285410"	"UO_0000065"	"19.05"	"0.35"	"4.25"	"5.30"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702983"	""	"0"	"430.46"	"0"	"3.41"	"BDBM147693"	"[C-]#[N+][C@H]1C[C@@H](N2CCC2)CC[C@@H]1n1cc(Nc2ccc(OC(F)F)nc2)c(C(N)=O)c1"	"IC50"	"'='"	"67.0"	"nM"	"7.17"	""	"285626"	"UO_0000065"	"16.67"	"0.32"	"3.76"	"7.99"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642343"	""	"0"	"540.67"	"1"	"2.77"	"BDBM99618"	"CN(c1ccc(-c2cccn3nc(Nc4ccc(CN5CCS(=O)(=O)CC5)cc4)nc23)cc1)S(C)(=O)=O"	"IC50"	"'='"	"0.27"	"nM"	"9.57"	""	"216308"	"UO_0000065"	"17.70"	"0.35"	"6.80"	"8.18"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3665193"	""	"0"	"446.54"	"0"	"1.31"	"BDBM112590"	"COCCNc1ncc(-c2cnc3[nH]ccc3n2)c(N[C@H]2CCCN(S(C)(=O)=O)C2)n1"	"IC50"	"'='"	"0.0763"	"nM"	"10.12"	""	"233827"	"UO_0000065"	"22.66"	"0.45"	"8.81"	"7.33"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3665143"	""	"0"	"414.54"	"0"	"2.88"	"BDBM112531"	"CC(C)CCS(=O)(=O)N1CC[C@@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.8108"	"nM"	"9.09"	""	"233770"	"UO_0000065"	"21.93"	"0.43"	"6.21"	"8.75"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL4514898"	""	"0"	"475.64"	"0"	"4.34"	"3"	"CC(C)CN1CCC(NC(=O)Cc2nc3cnc4[nH]ccc4c3n2[C@H]2CC[C@H](CC#N)CC2)CC1"	"IC50"	"'='"	"2.1"	"nM"	"8.68"	""	""	"UO_0000065"	"18.24"	"0.34"	"4.34"	"8.46"	"False"	"CHEMBL4404825"	"Inhibition of JAK2-JH1/JH2 domain (532 to 1132 residues) (unknown origin) pre-incubated before NH2-KGGEEEEYFELVKK-CO2 substrate addition and measured after 90 mins by MS analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402578"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4582390"	""	"0"	"434.54"	"0"	"3.52"	"10"	"N#CC[C@H]1CC[C@H](n2c(CC(=O)N[C@H]3CC[C@H](O)CC3)nc3cnc4[nH]ccc4c32)CC1"	"IC50"	"'='"	"7.2"	"nM"	"8.14"	""	""	"UO_0000065"	"18.74"	"0.35"	"4.62"	"6.81"	"False"	"CHEMBL4404825"	"Inhibition of JAK2-JH1/JH2 domain (532 to 1132 residues) (unknown origin) pre-incubated before NH2-KGGEEEEYFELVKK-CO2 substrate addition and measured after 90 mins by MS analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402578"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4456630"	""	"0"	"489.62"	"0"	"3.42"	"5"	"N#CC[C@H]1CC[C@H](n2c(CC(=O)N3CCC(N4CCOCC4)CC3)nc3cnc4[nH]ccc4c32)CC1"	"IC50"	"'='"	"6.1"	"nM"	"8.21"	""	""	"UO_0000065"	"16.78"	"0.31"	"4.79"	"7.97"	"False"	"CHEMBL4404825"	"Inhibition of JAK2-JH1/JH2 domain (532 to 1132 residues) (unknown origin) pre-incubated before NH2-KGGEEEEYFELVKK-CO2 substrate addition and measured after 90 mins by MS analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402578"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4634634"	""	"0"	"365.44"	"0"	"1.44"	"29"	"C[C@@H]1C[C@H]1C(=O)N1CCN(c2cnc(C#N)c(-c3cnn(C)c3)n2)C[C@H]1C"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4603512"	"Inhibition of recombinant GST-tagged human JAK2-JH1/JH2 domain (574 to 1154 residues) expressed in baculovirus expression system using Tyr 06 as substrate after 1 hr in presence of ATP by Z'LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4602617"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL3799424"	""	"0"	"400.44"	"0"	"3.95"	"12a"	"CC(=O)Nc1ccc(-c2ncnc3c2cc(C(=O)OCc2ccccc2)n3C)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL3802364"	"Inhibition of JAK2 in GMCSF-stimulated human TF1 cells assessed as suppression of STAT5 phosphorylation preincubated for 2 hrs followed by GMCSF stimulation for 50 mins by FACS reader analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"CHEMBL3307972"	""
"CHEMBL4634634"	""	"0"	"365.44"	"0"	"1.44"	"29"	"C[C@@H]1C[C@H]1C(=O)N1CCN(c2cnc(C#N)c(-c3cnn(C)c3)n2)C[C@H]1C"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4603511"	"Inhibition of human recombinant GST tagged JAK2 V617F mutant catalytic domain expressed in baculovirus expression system using Tyr6 peptide as substrate measured after 1 hr in presence of ATP by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4602617"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL3622821"	"UPADACITINIB"	"4"	"380.37"	"0"	"2.91"	"6"	"CC[C@@H]1CN(C(=O)NCC(F)(F)F)C[C@@H]1c1cnc2cnc3[nH]ccc3n12"	"IC50"	"'='"	"120.0"	"nM"	"6.92"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4377378"	"Inhibition of recombinant C-terminal His6-tagged human JAK2 kinase domain (808 to end residues) expressed in baculovirus-infected Sf21 cells in presence of 0.1 mM ATP"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4376812"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"CHEMBL4106362"	""
"CHEMBL4085457"	"PF-06651600"	"3"	"285.35"	"0"	"1.94"	"8; PF-06651600"	"C=CC(=O)N1C[C@H](Nc2ncnc3[nH]ccc23)CC[C@@H]1C"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"True"	"CHEMBL4377461"	"Inhibition of JAK2 (unknown origin)"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4376812"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4440718"	""	"0"	"401.47"	"0"	"2.12"	"12"	"[2H]C([2H])([2H])NC(=O)c1nnc(Nc2ccccn2)cc1Nc1ccccc1S(C)(=O)=O"	"IC50"	"'='"	"2700.0"	"nM"	"5.57"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4377476"	"Inhibition of JAK2 in GM-CSF-stimulated human TF-1 cells"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4376812"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"CHEMBL3307972"	""
"CHEMBL3800186"	""	"0"	"351.41"	"0"	"2.72"	"14c"	"Cn1c(C(N)=O)cc2c(-c3ccc(NC(=O)C(C)(C)C)cc3)ncnc21"	"IC50"	"'='"	"910.0"	"nM"	"6.04"	""	""	"UO_0000065"	"17.19"	"0.32"	"3.32"	"5.87"	"False"	"CHEMBL3802364"	"Inhibition of JAK2 in GMCSF-stimulated human TF1 cells assessed as suppression of STAT5 phosphorylation preincubated for 2 hrs followed by GMCSF stimulation for 50 mins by FACS reader analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"CHEMBL3307972"	""
"CHEMBL3797276"	""	"0"	"438.49"	"0"	"2.59"	"14d"	"C[C@H](NC(=O)OC(C)(C)C)C(=O)Nc1ccc(-c2ncnc3c2cc(C(N)=O)n3C)cc1"	"IC50"	"'='"	"51.0"	"nM"	"7.29"	""	""	"UO_0000065"	"16.63"	"0.31"	"4.70"	"5.16"	"False"	"CHEMBL3802363"	"Inhibition of recombinant human GST-tagged JAK2 expressed in baculovirus expression system using Z'-LYTE Try6 peptide as substrate incubated for 1 hr by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL4245633"	""	"0"	"365.40"	"0"	"0.89"	"13c"	"Cn1cc(-c2nn(C3CCN(C(=O)CC#N)CC3)c3ncnc(N)c23)cn1"	"IC50"	"'='"	"281.7"	"nM"	"6.55"	""	""	"UO_0000065"	"17.93"	"0.33"	"5.66"	"4.98"	"False"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL1703303"	""	"0"	"211.25"	"0"	"0.93"	"1"	"CS(=O)(=O)Nc1cccc2[nH]ncc12"	"IC50"	"'='"	"13000.0"	"nM"	"4.89"	""	""	"UO_0000065"	"23.13"	"0.48"	"3.96"	"6.53"	"False"	"CHEMBL4478766"	"Inhibition of human His-tagged JAK2 expressed in baculovirus using biotin-synthetic peptide as substrate by SPR assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4477220"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2016"	"None"	""
"CHEMBL4520790"	""	"0"	"367.42"	"0"	"0.84"	"20"	"Cn1cc(Nc2nccc(N3C[C@H]4CC[C@H](C3)N4C(=O)NCC#N)n2)cn1"	"IC50"	"'='"	"1229.0"	"nM"	"5.91"	""	""	"UO_0000065"	"16.09"	"0.30"	"5.07"	"5.14"	"False"	"CHEMBL4411592"	"Inhibition of JAK2 homodimer signaling pathway in human spiked CD34 +ve cells of whole blood assessed as reduction in EPO induced STAT5 phosphorylation preincubated for 45 mins followed by EPO addition and measured measured after 15 mins by FACS assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4411260"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4560212"	""	"0"	"445.90"	"1"	"5.09"	"31"	"CCc1cc(O)c(F)cc1-c1cc(NS(=O)(=O)c2ccccc2Cl)c2cn[nH]c2c1"	"IC50"	"'='"	"7.943"	"nM"	"8.10"	""	""	"UO_0000065"	"18.17"	"0.37"	"3.01"	"8.52"	"False"	"CHEMBL4478762"	"Inhibition of human His-tagged JAK2 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4477220"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2016"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"Tofacitinib"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	""	"UO_0000065"	"26.88"	"0.50"	"6.86"	"9.45"	"True"	"CHEMBL3802363"	"Inhibition of recombinant human GST-tagged JAK2 expressed in baculovirus expression system using Z'-LYTE Try6 peptide as substrate incubated for 1 hr by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL563257"	""	"0"	"383.50"	"1"	"5.15"	"13b"	"COc1cc(C)nc2c1-c1[nH]c3ccccc3c1CCN2CCc1ccccc1"	"IC50"	"'>'"	"40000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1036442"	"Inhibition of recombinant JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1151875"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2009"	"None"	""
"CHEMBL4634433"	""	"0"	"396.43"	"0"	"1.19"	"17"	"C[C@@H]1[C@@H]2CN(c3nc(Nc4cnn(C)c4)ncc3F)C[C@]12NC(=O)[C@@H]1C[C@H]1C#N"	"IC50"	"'='"	"228.0"	"nM"	"6.64"	""	""	"UO_0000065"	"16.75"	"0.31"	"5.45"	"5.94"	"False"	"CHEMBL4620433"	"Inhibition of human recombinant JAK2 assessed as level of phosphorylation in presence of peptide substrate FITC-KGGEEEEYFELVKK and ATP by mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4619733"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2020"	"None"	""
"CHEMBL388978"	"STAUROSPORINE"	"0"	"466.54"	"0"	"4.35"	"Staurosporine"	"CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4c(c5c6ccccc6n2c5c31)C(=O)NC4"	"IC50"	"'='"	"0.31"	"nM"	"9.51"	""	""	"UO_0000065"	"20.38"	"0.37"	"5.16"	"13.69"	"False"	"CHEMBL3807902"	"Inhibition of JAK2 (unknown origin) by mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3804794"	"1"	"Scientific Literature"	"Eur. J. Med. Chem."	"2016"	"None"	""
"CHEMBL3942555"	""	"0"	"476.53"	"0"	"4.15"	"48"	"O=C(CCCOc1ccc2cc1COC/C=C/COCc1cccc(c1)-c1ccnc(n1)N2)NO"	"IC50"	"'='"	"4.7"	"nM"	"8.33"	""	""	"UO_0000065"	"17.48"	"0.32"	"4.18"	"7.25"	"False"	"CHEMBL3877344"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]ATP addition measured after 120 mins by Hotspot assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3877241"	"1"	"Scientific Literature"	"J Med Chem"	"2016"	"None"	""
"CHEMBL4448796"	""	"0"	"439.50"	"0"	"2.09"	"19"	"CCNC(=O)c1ccc(Nc2ncc(F)c(N3C[C@H]4CC[C@H](C3)N4C(=O)C3CC3)n2)nc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4411592"	"Inhibition of JAK2 homodimer signaling pathway in human spiked CD34 +ve cells of whole blood assessed as reduction in EPO induced STAT5 phosphorylation preincubated for 45 mins followed by EPO addition and measured measured after 15 mins by FACS assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4411260"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"1"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"328.0"	"nM"	"6.48"	""	""	"UO_0000065"	"20.76"	"0.39"	"4.94"	"7.29"	"False"	"CHEMBL4411592"	"Inhibition of JAK2 homodimer signaling pathway in human spiked CD34 +ve cells of whole blood assessed as reduction in EPO induced STAT5 phosphorylation preincubated for 45 mins followed by EPO addition and measured measured after 15 mins by FACS assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4411260"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4458435"	""	"0"	"389.41"	"0"	"1.79"	"23; PF-06700841"	"Cn1cc(Nc2nccc(N3C[C@H]4CC[C@H](C3)N4C(=O)[C@@H]3CC3(F)F)n2)cn1"	"IC50"	"'='"	"577.0"	"nM"	"6.24"	""	""	"UO_0000065"	"16.02"	"0.30"	"4.45"	"7.88"	"False"	"CHEMBL4411592"	"Inhibition of JAK2 homodimer signaling pathway in human spiked CD34 +ve cells of whole blood assessed as reduction in EPO induced STAT5 phosphorylation preincubated for 45 mins followed by EPO addition and measured measured after 15 mins by FACS assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4411260"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3647875"	""	"0"	"454.96"	"0"	"3.88"	"BDBM147987"	"[C-]#[N+][C@H]1C[C@@H](C(=O)N2CC(C)(C)C2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"45.0"	"nM"	"7.35"	""	"285921"	"UO_0000065"	"16.15"	"0.31"	"3.47"	"7.53"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4467032"	""	"0"	"268.32"	"0"	"2.49"	"40"	"CC(C)=CCn1nc(C)c(-c2ncnc3[nH]ccc23)n1"	"IC50"	"'='"	"786.0"	"nM"	"6.11"	""	""	"UO_0000065"	"22.75"	"0.42"	"3.61"	"8.45"	"False"	"CHEMBL4429697"	"Inhibition of recombinant human C-terminal 6His-tagged JAK2 (808 to end amino acids) expressed in Sf21 cells measured after 1 hr in presence of ATP by TR-FRET assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4428074"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2016"	"CHEMBL4106362"	""
"CHEMBL4564551"	""	"0"	"254.30"	"0"	"1.93"	"54"	"Cc1nn(CC2CC2)nc1-c1ncnc2[nH]ccc12"	"IC50"	"'='"	"41.9"	"nM"	"7.38"	""	""	"UO_0000065"	"29.01"	"0.53"	"5.45"	"10.21"	"False"	"CHEMBL4429697"	"Inhibition of recombinant human C-terminal 6His-tagged JAK2 (808 to end amino acids) expressed in Sf21 cells measured after 1 hr in presence of ATP by TR-FRET assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4428074"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2016"	"CHEMBL4106362"	""
"CHEMBL3114775"	""	"0"	"471.49"	"0"	"3.68"	"8e"	"Cn1cc(C2=C(Nc3cccc(OCCNc4ccnc(F)c4)c3)C(=O)NC2=O)c2ccccc21"	"IC50"	"'='"	"1637.0"	"nM"	"5.79"	""	""	"UO_0000065"	"12.27"	"0.23"	"2.11"	"5.95"	"False"	"CHEMBL3118993"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112442"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL1650951"	""	"0"	"526.52"	"1"	"3.17"	"3"	"CC(C)(O)C(=O)N1CCN(c2ccc(C(F)(F)F)c(C3=C(c4c[nH]c5ccccc45)C(=O)NC3=O)c2)CC1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3118993"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112442"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3114786"	""	"0"	"483.50"	"0"	"3.84"	"11d"	"O=C1NC(=O)C(c2c[nH]c3ccccc23)=C1Nc1cccc(OC2CCN(c3ccnc(F)c3)C2)c1"	"IC50"	"'='"	"1238.0"	"nM"	"5.91"	""	""	"UO_0000065"	"12.22"	"0.22"	"2.07"	"5.95"	"False"	"CHEMBL3118993"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112442"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3114769"	""	"0"	"427.46"	"0"	"3.31"	"7d"	"O=C1NC(=O)C(c2c[nH]c3ccccc23)=C1Nc1ccc(OCCCn2ccnc2)cc1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3118993"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112442"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL1288033"	""	"0"	"351.37"	"0"	"2.47"	"22"	"CCOC(=O)c1cccc(Nc2nc(N)n(C(=O)c3ccccc3)n2)c1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1292866"	"Inhibition of human recombinant JAK2 by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287810"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL2205766"	""	"0"	"346.42"	"0"	"1.45"	"14, CZC24758"	"CC(C)(C)NS(=O)(=O)c1cncc(-c2ccn3nc(N)nc3c2)c1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2211514"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203257"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL3114783"	""	"0"	"497.53"	"0"	"4.23"	"11a"	"O=C1NC(=O)C(c2c[nH]c3ccccc23)=C1Nc1cccc(OC2CCN(c3ccnc(F)c3)CC2)c1"	"IC50"	"'='"	"1270.0"	"nM"	"5.90"	""	""	"UO_0000065"	"11.85"	"0.22"	"1.67"	"5.93"	"False"	"CHEMBL3118993"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112442"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL4537782"	""	"0"	"445.57"	"0"	"3.93"	"13e"	"CCC(=O)Nc1cccc(CNc2cc(Nc3ccc(N4CCN(C)CC4)cc3)ncn2)c1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4482009"	"Inhibition of human JAK2 using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and further incubated for 30 mins and subsequently measured after 1 hr by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480445"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL3114768"	""	"0"	"413.44"	"0"	"2.92"	"7c"	"O=C1NC(=O)C(c2c[nH]c3ccccc23)=C1Nc1ccc(OCCn2ccnc2)cc1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3118993"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112442"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL4556768"	""	"0"	"363.40"	"0"	"4.10"	"11f"	"C=CC(=O)Nc1cccc(CNc2cc(Nc3ccc(F)cc3)ncn2)c1"	"IC50"	"'>'"	"3000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4482009"	"Inhibition of human JAK2 using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and further incubated for 30 mins and subsequently measured after 1 hr by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480445"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4524497"	""	"0"	"414.52"	"0"	"3.48"	"15e'"	"CN1CCN(c2ccc(Nc3cc(NCc4ccc(NC#N)cc4)ncn3)cc2)CC1"	"IC50"	"'='"	"503.0"	"nM"	"6.30"	""	""	"UO_0000065"	"15.19"	"0.28"	"2.82"	"6.84"	"False"	"CHEMBL4482009"	"Inhibition of human JAK2 using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and further incubated for 30 mins and subsequently measured after 1 hr by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480445"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4525246"	""	"0"	"364.41"	"0"	"2.57"	"15c"	"COCCn1cc(Nc2cc(NCc3cccc(NC#N)c3)ncn2)cn1"	"IC50"	"'='"	"2790.0"	"nM"	"5.55"	""	""	"UO_0000065"	"15.24"	"0.28"	"2.98"	"4.93"	"False"	"CHEMBL4482009"	"Inhibition of human JAK2 using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and further incubated for 30 mins and subsequently measured after 1 hr by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480445"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL2035810"	""	"0"	"477.91"	"0"	"3.89"	"19a"	"C=CC(=O)NCc1coc(-c2c(N)ncnc2Nc2ccc(OCc3ccccn3)c(Cl)c2)n1"	"IC50"	"'>'"	"3000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2039260"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2034880"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL3747452"	""	"0"	"376.46"	"0"	"3.26"	"23"	"COc1ccc(-c2nc3c(NCC4CCN(C)CC4)c(C#N)cnc3[nH]2)cc1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3751000"	"Inhibition of N-terminal GST-fused recombinant JAK2 (831 to 1132 residues) (unknown origin) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate by microfluidic capillary electrophoresis method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3745697"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3694588"	""	"0"	"380.88"	"0"	"4.85"	"BDBM125909"	"Clc1cnc2nc1NCCc1cccc(c1)OCCCc1cccc(c1)N2"	"IC50"	"'='"	"120.0"	"nM"	"6.92"	""	"255682"	"UO_0000065"	"18.17"	"0.35"	"2.07"	"11.72"	"False"	"CHEMBL3707544"	"In Vitro Kinase Assay: One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Biochemistry 1999, 269, 94-104. The catalytic domains of human JAK1 (a.a. 837-1142), JAK2 (a.a. 828-1132) and JAK3 (a.a. 781-1124) with an N-terminal His tag were expressed using baculovirus in insect cells and purified. The catalytic activity of JAK1, JAK2 or JAK3 was assayed by measuring the phosphorylation of a biotinylated peptide. The phosphorylated peptide was detected by homogenous time resolved fluorescence (HTRF). IC50s of compounds were measured for each kinase in the reactions that contain the enzyme, ATP and 500 nM peptide in 50 mM Tris (pH 7.8) buffer with 100 mM NaCl, 5 mM DTT, and 0.1 mg/mL (0.01%) BSA. The ATP concentration in the reactions was 90 uM for JAK1, 30 uM for JAK2 and 3 uM for JAK3. Reactions were carried out at room temperature for 1 hr and then stopped with 20 uL 45 mM EDTA."	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639093"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3651033"	""	"0"	"386.43"	"0"	"3.08"	"BDBM153210"	"C/C=C/S(=O)(=O)Nc1cccc(-c2ncnc3[nH]cc(C(=O)OCC)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294158"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3589165"	""	"0"	"399.45"	"0"	"3.56"	"2"	"NC(=O)c1cc(-c2ccccc2)cc2c1[nH]c1ccc(C(=O)N3CCOCC3)cc12"	"IC50"	"'='"	"2.6"	"nM"	"8.59"	""	""	"UO_0000065"	"21.49"	"0.39"	"5.03"	"9.71"	"False"	"CHEMBL3592849"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3589173"	""	"0"	"472.37"	"0"	"4.20"	"10"	"NC(=O)c1cc(-c2ccc(Cl)c(Cl)c2)cc2c3c([nH]c12)CCC(C(=O)N1CCOCC1)C3"	"IC50"	"'='"	"86.0"	"nM"	"7.07"	""	""	"UO_0000065"	"14.96"	"0.30"	"2.87"	"7.99"	"False"	"CHEMBL3592849"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3703075"	""	"0"	"407.40"	"0"	"2.35"	"BDBM147787"	"N#C[C@H]1C[C@H](NCC(F)F)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccnc(F)c2)n1"	"IC50"	"'='"	"53.0"	"nM"	"7.28"	""	"285721"	"UO_0000065"	"17.86"	"0.34"	"4.93"	"5.98"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL1288063"	""	"0"	"419.36"	"0"	"3.49"	"24"	"CCOC(=O)c1cccc(Nc2nc(N)n(C(=O)c3ccc(C(F)(F)F)cc3)n2)c1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1292866"	"Inhibition of human recombinant JAK2 by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287810"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1288094"	""	"0"	"341.33"	"0"	"2.06"	"26"	"CCOC(=O)c1cccc(Nc2nc(N)n(C(=O)c3ccco3)n2)c1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1292866"	"Inhibition of human recombinant JAK2 by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287810"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL570192"	""	"0"	"353.36"	"0"	"3.11"	"7i"	"Cc1cc(Nc2nc(O[C@@H](C)c3ccc(F)cn3)c(C#N)nc2C)n[nH]1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	""	"UO_0000065"	"23.77"	"0.44"	"5.29"	"7.47"	"False"	"CHEMBL1043451"	"Inhibition of JAK2 using 2 mM ATP as a substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156131"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL583030"	""	"0"	"318.34"	"0"	"1.78"	"33"	"Nc1nn2cccnc2c1-c1cc(NCc2cccnc2)ncn1"	"IC50"	"'='"	"36.0"	"nM"	"7.44"	""	""	"UO_0000065"	"23.38"	"0.42"	"5.66"	"6.96"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL584944"	""	"0"	"377.43"	"0"	"3.86"	"45"	"CCC[C@@H](Nc1cc(-c2c(N)nn3cccnc23)ncn1)c1ccc(F)cc1"	"IC50"	"'='"	"0.5"	"nM"	"9.30"	""	""	"UO_0000065"	"24.64"	"0.45"	"5.44"	"9.89"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL2035052"	""	"0"	"473.58"	"0"	"4.61"	"14d, 95:5 trans/Cis mixture"	"C1=C/COCc2cc(ccc2OCCN2CCCC2)Nc2nccc(n2)-c2ccnc(c2)OCC/1"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	""	"UO_0000065"	"16.35"	"0.30"	"3.13"	"9.49"	"False"	"CHEMBL2040119"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2034857"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2035054"	""	"0"	"475.59"	"0"	"4.47"	"14f, 95:5 trans/Cis mixture"	"CN1C/C=C/COCc2ccc(o2)-c2ccnc(n2)Nc2ccc(OCCN3CCCC3)c(c2)C1"	"IC50"	"'='"	"330.0"	"nM"	"6.48"	""	""	"UO_0000065"	"13.63"	"0.25"	"2.01"	"8.54"	"False"	"CHEMBL2040119"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2034857"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2035042"	""	"0"	"395.51"	"1"	"5.23"	"13b, 95:5 trans/Cis mixture"	"CN1C/C=C/CCn2ccc3ccc(cc32)-c2ccnc(n2)Nc2cccc(c2)C1"	"IC50"	"'='"	"1600.0"	"nM"	"5.80"	""	""	"UO_0000065"	"14.65"	"0.26"	"0.57"	"12.61"	"False"	"CHEMBL2040119"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2034857"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL4463436"	""	"0"	"428.50"	"0"	"2.98"	"28"	"Cc1nccc(Nc2cc(NC3CCN(c4ccc(C#N)cc4)CC3)c(C(N)=O)cn2)n1"	"IC50"	"'='"	"3.5"	"nM"	"8.46"	""	""	"UO_0000065"	"19.73"	"0.36"	"5.48"	"6.37"	"False"	"CHEMBL4429528"	"Inhibition of human JAK2 assessed as reduction in phosphorylation of Biotin-Lyn-Substrate-2 after 1 hr in presence of ATP by ELISA"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4428070"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2016"	"None"	""
"CHEMBL2322138"	""	"0"	"240.31"	"0"	"3.42"	"15"	"c1cc2c(ncc3ncn(C4CCCCC4)c32)[nH]1"	"IC50"	"'='"	"5700.0"	"nM"	"5.24"	""	""	"UO_0000065"	"21.82"	"0.40"	"1.82"	"11.28"	"False"	"CHEMBL2327181"	"Inhibition of JAK2 (unknown origin) after 2.5 hrs by time-resolved fluorescence resonance energy transfer assay in presence of 100 uM ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321825"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2325904"	""	"0"	"288.35"	"0"	"1.72"	"3f"	"C[C@H](NC(=O)c1c[nH]c2ncc(C3CC3)nc12)C(C)(C)O"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2329053"	"Inhibition of JAK2 in human PBMC expressing CD14 assessed as inhibition of GM-CSF-stimulated STAT5a phosphorylation after 30 mins by flow cytometric analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321829"	"1"	"Scientific Literature"	"J. Med. Chem."	"2013"	"None"	""
"CHEMBL3665220"	""	"0"	"389.46"	"0"	"2.58"	"BDBM112620"	"N#CCC1(N2CCC[C@H](Nc3ncccc3-c3cnc4[nH]ccc4n3)C2)COC1"	"IC50"	"'='"	"0.2185"	"nM"	"9.66"	""	"233857"	"UO_0000065"	"24.80"	"0.45"	"7.08"	"9.40"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3702886"	""	"0"	"405.46"	"0"	"2.68"	"BDBM147585"	"N#C[C@H]1CCCCC1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)CF)cc2)n1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"285515"	"UO_0000065"	"21.45"	"0.42"	"6.02"	"6.65"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652361"	""	"0"	"473.60"	"0"	"1.62"	"BDBM113172"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC[C@@](O)(Cn3cccn3)C2)CC1"	"IC50"	"'='"	"9.3"	"nM"	"8.03"	""	"234615"	"UO_0000065"	"16.96"	"0.33"	"6.41"	"6.68"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3966746"	""	"0"	"441.52"	"0"	"3.81"	"BDBM255016"	"CSCN1CN([C@H]2CC[C@H](CNCC(F)(F)F)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"34.0"	"nM"	"7.47"	""	"443872"	"UO_0000065"	"16.92"	"0.34"	"3.66"	"11.62"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3944237"	""	"0"	"435.49"	"0"	"3.90"	"BDBM255020"	"O=C1c2cnc3[nH]ccc3c2N([C@H]2CC[C@H](CNCC(F)(F)F)CC2)CN1CC1CC1"	"IC50"	"'='"	"27.0"	"nM"	"7.57"	""	"443876"	"UO_0000065"	"17.38"	"0.33"	"3.67"	"11.78"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3981841"	""	"0"	"448.49"	"0"	"3.80"	"BDBM255022"	"N#CCCCN1CN([C@H]2CC[C@H](CNCC(F)(F)F)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"36.0"	"nM"	"7.44"	""	"443878"	"UO_0000065"	"16.60"	"0.32"	"3.64"	"8.45"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3642389"	""	"0"	"419.51"	"0"	"3.49"	"BDBM99667"	"CN1Cc2ccc(Nc3nc4c(-c5ccc(S(C)(=O)=O)cc5)cccn4n3)cc2C1"	"IC50"	"'='"	"0.73"	"nM"	"9.14"	""	"216357"	"UO_0000065"	"21.78"	"0.42"	"5.65"	"11.48"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652322"	""	"0"	"551.70"	"1"	"2.09"	"BDBM113132"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCC(c3nc(CS(C)(=O)=O)no3)CC2)CC1"	"IC50"	"'='"	"65.8"	"nM"	"7.18"	""	"234575"	"UO_0000065"	"13.02"	"0.27"	"5.09"	"4.63"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3647770"	""	"0"	"460.50"	"0"	"4.46"	"BDBM147873"	"CC1(C)CCN1[C@@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(C(F)(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"430.0"	"nM"	"6.37"	""	"285807"	"UO_0000065"	"13.83"	"0.26"	"1.91"	"6.37"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702927"	""	"0"	"393.37"	"0"	"3.88"	"BDBM147626"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(OC(F)(F)F)cc2)n1"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	"285556"	"UO_0000065"	"20.34"	"0.39"	"4.12"	"7.55"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703029"	""	"0"	"502.54"	"1"	"4.04"	"BDBM147739"	"N#C[C@H]1C[C@H](N2CC3(CCC3)C2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc([C@H](O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"37.0"	"nM"	"7.43"	""	"285673"	"UO_0000065"	"14.79"	"0.28"	"3.39"	"6.18"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL1289216"	""	"0"	"353.32"	"0"	"4.21"	"39"	"CC(C)[C@H](Nc1nc2cc[nH]c(=O)c2c2cc(F)ccc12)C(F)(F)F"	"IC50"	"'='"	"55.0"	"nM"	"7.26"	""	""	"UO_0000065"	"20.55"	"0.40"	"3.05"	"12.56"	"False"	"CHEMBL1291235"	"Inhibition of JAK2 in cell-free system"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287746"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL3699560"	""	"0"	"360.37"	"0"	"3.31"	"BDBM147579"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)F)nc2)n1"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	"285509"	"UO_0000065"	"21.88"	"0.41"	"4.58"	"7.19"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699496"	""	"0"	"456.52"	"0"	"3.87"	"BDBM147512"	"CC(C)(C)OC(=O)NCC1CC[C@@H](C#N)[C@@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)C1"	"IC50"	"'>'"	"1500.0"	"nM"	""	""	"285440"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4552370"	""	"0"	"438.51"	"0"	"2.70"	"15"	"CCNC(=O)c1ccc(Nc2ncc(F)c(N3C[C@H]4CC[C@H](C3)N4C(=O)C3CC3)n2)cc1"	"IC50"	"'='"	"306.0"	"nM"	"6.51"	""	""	"UO_0000065"	"14.86"	"0.28"	"3.81"	"7.20"	"False"	"CHEMBL4411595"	"Inhibition of human JAK2 using fluorescence labeled peptide as substrate and using 1 mM ATP by microfluidic based mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4411260"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3658109"	""	"0"	"602.67"	"2"	"5.51"	"BDBM148417"	"Cc1ccc(NC(=O)c2cc(C(F)(F)F)ccn2)cc1N1CCc2nc(Nc3ccc(N4CCN(C)CC4)cc3)ncc2C1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"286795"	"UO_0000065"	"13.77"	"0.26"	"2.79"	"9.27"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665169"	""	"0"	"336.40"	"0"	"2.44"	"BDBM112562"	"CC(=O)N1CCC[C@H](Nc2ncccc2-c2cnc3cc[nH]c3n2)C1"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	"233800"	"UO_0000065"	"23.78"	"0.44"	"5.56"	"9.22"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642301"	""	"0"	"457.54"	"0"	"3.02"	"BDBM99571"	"CS(=O)(=O)c1ccccc1Nc1nc2c(Nc3ccccc3S(C)(=O)=O)cccn2n1"	"IC50"	"'='"	"9999.0"	"nM"	"5.00"	""	"216261"	"UO_0000065"	"10.93"	"0.22"	"1.98"	"4.08"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL570899"	""	"0"	"314.33"	"0"	"2.35"	"4"	"Cc1cc(Nc2cncc(N[C@@H](C)c3ncc(F)cn3)n2)n[nH]1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"27.11"	"0.51"	"6.17"	"8.17"	"False"	"CHEMBL1103123"	"Inhibition of recombinant JAK2 kinase in presence of 5 mM ATP"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154970"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1088029"	""	"0"	"361.41"	"0"	"3.10"	"6a"	"COc1cc(Nc2ncc(C)s2)nc(N[C@@H](C)c2ncc(F)cn2)n1"	"IC50"	"'<'"	"3.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1103123"	"Inhibition of recombinant JAK2 kinase in presence of 5 mM ATP"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154970"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1087398"	""	"0"	"426.48"	"0"	"3.09"	"8a"	"C[C@H](Nc1nc(Nc2ncc(C#N)s2)cc(N2CCOCC2)n1)c1ccc(F)cn1"	"IC50"	"'<'"	"3.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1103123"	"Inhibition of recombinant JAK2 kinase in presence of 5 mM ATP"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154970"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"Tofacitinib"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"184.0"	"nM"	"6.74"	""	""	"UO_0000065"	"21.56"	"0.40"	"5.20"	"7.58"	"True"	"CHEMBL2329053"	"Inhibition of JAK2 in human PBMC expressing CD14 assessed as inhibition of GM-CSF-stimulated STAT5a phosphorylation after 30 mins by flow cytometric analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321829"	"1"	"Scientific Literature"	"J. Med. Chem."	"2013"	"None"	""
"CHEMBL2325896"	""	"0"	"364.41"	"0"	"1.33"	"3r"	"N#CC1CN(C(=O)[C@H](NC(=O)c2c[nH]c3ncc(C4CC4)nc23)C2CC2)C1"	"IC50"	"'='"	"206.0"	"nM"	"6.69"	""	""	"UO_0000065"	"18.35"	"0.34"	"5.36"	"5.83"	"False"	"CHEMBL2329053"	"Inhibition of JAK2 in human PBMC expressing CD14 assessed as inhibition of GM-CSF-stimulated STAT5a phosphorylation after 30 mins by flow cytometric analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321829"	"1"	"Scientific Literature"	"J. Med. Chem."	"2013"	"None"	""
"CHEMBL3650989"	""	"0"	"350.38"	"0"	"3.32"	"BDBM153164"	"C/C=C/C(=O)Nc1cccc(-c2ncnc3[nH]cc(C(=O)OCC)c23)c1"	"IC50"	"'='"	"483.0"	"nM"	"6.32"	""	"294112"	"UO_0000065"	"18.03"	"0.33"	"3.00"	"6.51"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651050"	""	"0"	"340.39"	"0"	"4.42"	"BDBM153227"	"C=CC(=O)Nc1cccc(-c2ncnc3[nH]cc(-c4ccccc4)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294175"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699493"	""	"0"	"442.50"	"0"	"3.62"	"BDBM147508"	"CC(C)(C)OC(=O)NC1CC[C@@H](C#N)C(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)C1"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	"285436"	"UO_0000065"	"17.40"	"0.33"	"4.08"	"5.70"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665125"	""	"0"	"336.40"	"0"	"2.44"	"BDBM112512"	"CC(=O)N1CCC(Nc2ncccc2-c2cnc3[nH]ccc3n2)CC1"	"IC50"	"'='"	"0.0765"	"nM"	"10.12"	""	"233751"	"UO_0000065"	"30.07"	"0.55"	"7.68"	"11.65"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3699507"	""	"0"	"391.44"	"0"	"3.34"	"BDBM147525"	"Cc1noc(-c2ccc(Nc3nn([C@H]4CCCC[C@@H]4C#N)cc3C(N)=O)cc2)n1"	"IC50"	"'='"	"25.0"	"nM"	"7.60"	""	"285455"	"UO_0000065"	"19.42"	"0.36"	"4.26"	"5.60"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665175"	""	"0"	"430.53"	"0"	"1.85"	"BDBM112568"	"CC(C)CS(=O)(=O)N1CC[C@@H](O)[C@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.09"	"nM"	"10.05"	""	"233805"	"UO_0000065"	"23.33"	"0.46"	"8.20"	"8.09"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642334"	""	"0"	"463.57"	"0"	"2.69"	"BDBM99606"	"CN1CCN(c2cccc(Nc3nc4cncc(-c5ccc(S(C)(=O)=O)cc5)n4n3)c2)CC1"	"IC50"	"'='"	"307.1"	"nM"	"6.51"	""	"216296"	"UO_0000065"	"14.05"	"0.27"	"3.82"	"6.80"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703000"	""	"0"	"460.50"	"0"	"4.46"	"BDBM147710"	"C[C@H]1C[C@H](C)N1[C@@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(C(F)(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"355.0"	"nM"	"6.45"	""	"285644"	"UO_0000065"	"14.01"	"0.27"	"1.99"	"6.45"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3671134"	""	"0"	"423.43"	"0"	"3.33"	"BDBM127633"	"Cn1ccc(NC(=O)c2cnn3ccc(N4CCC[C@@H]4c4cc(F)ccc4F)nc23)n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258307"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3671139"	""	"0"	"455.47"	"0"	"3.29"	"BDBM127638"	"O=C(O)C1CCN(C(=O)c2cnn3ccc(N4CCCC4c4cc(F)ccc4F)nc23)CC1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258312"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3671142"	""	"0"	"397.43"	"0"	"3.63"	"BDBM127641"	"O=C(NC1CCC1)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'='"	"470.0"	"nM"	"6.33"	""	"258315"	"UO_0000065"	"15.92"	"0.30"	"2.70"	"10.12"	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3671156"	""	"0"	"437.45"	"0"	"2.98"	"BDBM127655"	"O=C(NCCn1ccnc1)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258329"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675917"	""	"0"	"382.37"	"0"	"2.60"	"BDBM127666"	"N#CCNC(=O)c1cnn2ccc(N3CCCC3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258340"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675924"	""	"0"	"464.50"	"0"	"1.63"	"BDBM127673"	"CS(=O)(=O)NCCNC(=O)c1cnn2ccc(N3CCCC3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258347"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3639748"	""	"0"	"411.46"	"0"	"4.02"	"BDBM127695"	"CC1(C)CC[C@H](c2cc(F)ccc2F)N1c1ccn2ncc(C(=O)NC3CC3)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258369"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675947"	""	"0"	"410.45"	"0"	"2.51"	"BDBM127699"	"O=C(NC1CCOCC1)c1cnn2ccc(N3CCC[C@@H]3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258373"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675949"	""	"0"	"325.35"	"0"	"2.31"	"BDBM127701"	"NC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cccc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258375"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675954"	""	"0"	"396.43"	"0"	"1.99"	"BDBM127706"	"O=C(NC1CC1)c1cnn2ccc(N3CCCC3c3cc(F)cnc3CO)nc12"	"IC50"	"'='"	"698.0"	"nM"	"6.16"	""	"258380"	"UO_0000065"	"15.53"	"0.29"	"4.17"	"6.44"	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675959"	""	"0"	"427.41"	"0"	"2.70"	"BDBM127711"	"O=C(NC1(C(=O)O)CC1)c1cnn2ccc(N3CCCC3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258385"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675994"	""	"0"	"410.45"	"0"	"2.25"	"BDBM127747"	"O=C(NC1CCC[C@@H]1O)c1cnn2ccc(N3CCCC3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258421"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676018"	""	"0"	"426.45"	"0"	"1.82"	"BDBM127774"	"COc1ncc(F)cc1[C@H]1CCCN1c1ccn2ncc(C(=O)N3CC(C)(O)C3)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258445"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676046"	""	"0"	"415.44"	"0"	"2.85"	"BDBM127805"	"CC[C@@H](CO)NC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258474"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676053"	""	"0"	"394.45"	"0"	"3.20"	"BDBM127812"	"Cc1ncc(F)cc1C1CCCN1c1ccn2ncc(C(=O)NC3CCC3)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258481"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL4537718"	""	"0"	"417.52"	"0"	"3.77"	"6"	"CC(C)(C#N)CNC(=O)Cc1nc2cnc3[nH]ccc3c2n1[C@H]1CC[C@H](CC#N)CC1"	"IC50"	"'='"	"5.6"	"nM"	"8.25"	""	""	"UO_0000065"	"19.76"	"0.36"	"4.48"	"6.70"	"False"	"CHEMBL4404825"	"Inhibition of JAK2-JH1/JH2 domain (532 to 1132 residues) (unknown origin) pre-incubated before NH2-KGGEEEEYFELVKK-CO2 substrate addition and measured after 90 mins by MS analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402578"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL3114770"	""	"0"	"413.44"	"0"	"2.92"	"7e"	"O=C1NC(=O)C(c2c[nH]c3ccccc23)=C1Nc1ccccc1OCCn1ccnc1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3118993"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112442"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3676056"	""	"0"	"384.42"	"0"	"1.64"	"BDBM127815"	"Cc1ncc(F)cc1[C@H]1CCCN1c1ccn2ncc(C(=O)NCCO)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258484"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676077"	""	"0"	"415.43"	"0"	"1.04"	"BDBM127838"	"NC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3OCC(O)CO)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258506"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676095"	""	"0"	"456.52"	"0"	"2.05"	"BDBM127860"	"Cn1cc(F)cc([C@H]2CCCN2c2ccn3ncc(C(=O)N[C@H](CO)C(C)(C)C)c3n2)c1=O"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258525"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3114776"	""	"0"	"471.49"	"0"	"3.70"	"8f"	"CN(CCOc1cccc(NC2=C(c3c[nH]c4ccccc34)C(=O)NC2=O)c1)c1ccnc(F)c1"	"IC50"	"'='"	"490.0"	"nM"	"6.31"	""	""	"UO_0000065"	"13.38"	"0.25"	"2.61"	"6.35"	"False"	"CHEMBL3118993"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112442"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL1080323"	""	"0"	"361.37"	"0"	"1.68"	"5f"	"N#Cc1ccc2ncn(-c3ncc4[nH]c(=O)n(C5CCOCC5)c4n3)c2c1"	"IC50"	"'='"	"470.0"	"nM"	"6.33"	""	""	"UO_0000065"	"17.51"	"0.32"	"4.65"	"5.53"	"False"	"CHEMBL1102456"	"Inhibition of human JAK2 (532-1132) by time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154364"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL3703035"	""	"0"	"448.45"	"0"	"3.56"	"BDBM147745"	"N#C[C@H]1C[C@@H](N2CCC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(OC(F)(F)F)cc2)n1"	"IC50"	"'='"	"23.0"	"nM"	"7.64"	""	"285679"	"UO_0000065"	"17.03"	"0.33"	"4.08"	"6.99"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703063"	""	"0"	"502.54"	"1"	"4.04"	"BDBM147773"	"N#C[C@H]1C[C@H](N2CC3(CCC3)C2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc([C@@H](O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"27.0"	"nM"	"7.57"	""	"285707"	"UO_0000065"	"15.06"	"0.29"	"3.53"	"6.30"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651058"	""	"0"	"355.40"	"0"	"4.19"	"BDBM153235"	"COc1ccccc1-c1c[nH]c2ncnc(-c3ccc4cn(C)nc4c3)c12"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294183"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699459"	""	"0"	"295.35"	"0"	"2.59"	"BDBM147474"	"N#C[C@H]1CCC[C@@H]1n1cc(C(N)=O)c(Nc2ccccc2)n1"	"IC50"	"'='"	"101.0"	"nM"	"7.00"	""	"285399"	"UO_0000065"	"23.69"	"0.43"	"4.41"	"7.23"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3622958"	""	"0"	"417.52"	"0"	"3.00"	"16h"	"Cc1nn(-c2ccnc(Nc3ccc4c(c3)c(C)c(C)n4C)n2)cc1CN1CC(O)C1"	"IC50"	"'='"	"138200.0"	"nM"	""	"Outside typical range"	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3627021"	"Inhibition of human JAK2 pre-incubated for 30 mins at room temperature before substrate addition and measured 1 hr after substrate addition by cell free kinase assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621069"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL1834657"	"INFIGRATINIB PHOSPHATE"	"4"	"658.48"	"2"	"5.35"	"1h, NVP-BGJ398"	"CCN1CCN(c2ccc(Nc3cc(N(C)C(=O)Nc4c(Cl)c(OC)cc(OC)c4Cl)ncn3)cc2)CC1.O=P(O)(O)O"	"IC50"	"'='"	"2882.0"	"nM"	"5.54"	""	""	"UO_0000065"	"9.88"	"0.20"	"0.19"	"5.83"	"False"	"CHEMBL1839965"	"Inhibition of JAK2-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833940"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3307634"	""
"CHEMBL3622956"	""	"0"	"437.94"	"0"	"3.34"	"16f"	"Cc1nn(-c2ccnc(Nc3ccc4c(c3)c(Cl)c(C)n4C)n2)cc1CN1CC(O)C1"	"IC50"	"'='"	"111900.0"	"nM"	""	"Outside typical range"	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3627021"	"Inhibition of human JAK2 pre-incubated for 30 mins at room temperature before substrate addition and measured 1 hr after substrate addition by cell free kinase assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621069"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3642317"	""	"0"	"476.61"	"0"	"3.29"	"BDBM99589"	"CN1CCN(Cc2ccc(Nc3nc4cccc(-c5cccc(S(C)(=O)=O)c5)n4n3)cc2)CC1"	"IC50"	"'='"	"11.7"	"nM"	"7.93"	""	"216279"	"UO_0000065"	"16.64"	"0.32"	"4.64"	"9.57"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652381"	""	"0"	"441.56"	"0"	"2.17"	"BDBM113192"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC(c3ncccn3)C2)CC1"	"IC50"	"'='"	"22.6"	"nM"	"7.65"	""	"234635"	"UO_0000065"	"17.32"	"0.34"	"5.48"	"7.08"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3665123"	""	"0"	"336.40"	"0"	"2.44"	"BDBM112510"	"CC(=O)N1CCC[C@@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.0228"	"nM"	"10.64"	""	"233749"	"UO_0000065"	"31.64"	"0.58"	"8.20"	"12.26"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3702968"	""	"0"	"397.45"	"0"	"3.52"	"BDBM147675"	"N#C[C@@H]1C[C@@H](OCC2CC2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"102.0"	"nM"	"6.99"	""	"285607"	"UO_0000065"	"17.59"	"0.33"	"3.47"	"6.60"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703019"	""	"0"	"372.86"	"0"	"2.83"	"BDBM147729"	"CN[C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	"285663"	"UO_0000065"	"20.91"	"0.41"	"4.97"	"7.17"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3689517"	""	"0"	"346.34"	"0"	"1.69"	"BDBM109867"	"N#CCC(=O)N1CC(F)(F)C12CCCN(c1ncnc3[nH]ccc13)C2"	"IC50"	"'='"	"1.9"	"nM"	"8.72"	""	"230597"	"UO_0000065"	"25.18"	"0.48"	"7.03"	"9.81"	"False"	"CHEMBL3705639"	"Inhibition Assay: In the kinase reactions, fused proteins (6His tag-fused hJAK2 kinase domain (aa808-end)) which were coexpressed in Sf21 cells and purified by Ni2+/NTA agarose were used."	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638515"	"37"	"BindingDB Database"	""	"2013"	"CHEMBL4106362"	""
"CHEMBL3593779"	""	"0"	"375.44"	"0"	"2.26"	"19"	"C[C@H]1CN(c2ccc(C#N)cn2)CC[C@H]1Nc1c(C(N)=O)cnc2[nH]ccc12"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	""	"UO_0000065"	"20.92"	"0.38"	"5.59"	"6.35"	"False"	"CHEMBL3594790"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593212"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3593778"	""	"0"	"379.40"	"0"	"1.96"	"35"	"N#Cc1ccc(N2CC[C@H](Nc3c(C(N)=O)cnc4[nH]ccc34)[C@H](F)C2)nc1"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	""	"UO_0000065"	"20.48"	"0.38"	"5.81"	"6.28"	"False"	"CHEMBL3594790"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593212"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3703083"	""	"0"	"407.40"	"0"	"2.35"	"BDBM147796"	"N#C[C@H]1C[C@@H](NCC(F)F)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccnc(F)c2)n1"	"IC50"	"'='"	"33.0"	"nM"	"7.48"	""	"285730"	"UO_0000065"	"18.36"	"0.35"	"5.13"	"6.15"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4553196"	""	"0"	"319.33"	"0"	"1.85"	"6"	"O=C(Nc1ccc2[nH]ncc2c1)c1cccc(Cn2cnnn2)c1"	"IC50"	"'='"	"15200.0"	"nM"	"4.82"	""	""	"UO_0000065"	"15.09"	"0.27"	"2.97"	"4.75"	"False"	"CHEMBL4481929"	"Inhibition of JAK2 (unknown origin) after 1 hr FRET-based Z'-Lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480435"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4593750"	""	"0"	"329.33"	"0"	"1.79"	"10"	"c1ccc(-n2cnnn2)c(-c2cn(-c3ccc4[nH]ncc4c3)nn2)c1"	"IC50"	"'='"	"9530.0"	"nM"	"5.02"	""	""	"UO_0000065"	"15.25"	"0.27"	"3.23"	"4.88"	"False"	"CHEMBL4481929"	"Inhibition of JAK2 (unknown origin) after 1 hr FRET-based Z'-Lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480435"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL1595400"	""	"0"	"237.26"	"0"	"2.82"	"28a"	"O=C(Nc1ccc2[nH]ncc2c1)c1ccccc1"	"IC50"	"'='"	"13800.0"	"nM"	"4.86"	""	""	"UO_0000065"	"20.48"	"0.37"	"2.04"	"8.41"	"False"	"CHEMBL4481929"	"Inhibition of JAK2 (unknown origin) after 1 hr FRET-based Z'-Lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480435"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL1305321"	""	"0"	"271.71"	"0"	"3.47"	"28b"	"O=C(Nc1ccc2[nH]ncc2c1)c1ccccc1Cl"	"IC50"	"'='"	"453.0"	"nM"	"6.34"	""	""	"UO_0000065"	"23.35"	"0.46"	"2.87"	"10.98"	"False"	"CHEMBL4481929"	"Inhibition of JAK2 (unknown origin) after 1 hr FRET-based Z'-Lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480435"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4552462"	""	"0"	"321.17"	"0"	"3.70"	"35c"	"Nc1n[nH]c2ccc(C(=O)Nc3cc(Cl)ccc3Cl)cc12"	"IC50"	"'='"	"38.0"	"nM"	"7.42"	""	""	"UO_0000065"	"23.10"	"0.48"	"3.72"	"8.85"	"False"	"CHEMBL4481929"	"Inhibition of JAK2 (unknown origin) after 1 hr FRET-based Z'-Lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480435"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL3125667"	""	"0"	"539.64"	"1"	"4.59"	"22e"	"NS(=O)(=O)OCCn1cnc2c(Nc3ccc(F)cc3)nc(NCc3ccc(C4CCCCC4)cc3)nc21"	"IC50"	"'='"	"16600.0"	"nM"	"4.78"	""	""	"UO_0000065"	"8.86"	"0.17"	"0.19"	"3.49"	"False"	"CHEMBL3131078"	"Inhibition of JAK2 (unknown origin) after 20 mins"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3124828"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2013"	"None"	""
"CHEMBL1630788"	""	"0"	"391.42"	"0"	"2.00"	"17a"	"C[C@@H]1CCN(S(=O)(=O)CC(F)(F)F)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"790.0"	"nM"	"6.10"	""	""	"UO_0000065"	"15.59"	"0.32"	"4.10"	"7.42"	"False"	"CHEMBL1641117"	"Inhibition of GST-tagged human JAK2 catalytic domain expressed in Sf9 cells by ELISA"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1629452"	"1"	"Scientific Literature"	"J. Med. Chem."	"2010"	"CHEMBL3308860"	""
"CHEMBL4555943"	""	"0"	"321.17"	"0"	"3.70"	"35d"	"Nc1n[nH]c2ccc(C(=O)Nc3c(Cl)cccc3Cl)cc12"	"IC50"	"'='"	"28.0"	"nM"	"7.55"	""	""	"UO_0000065"	"23.52"	"0.49"	"3.85"	"9.01"	"False"	"CHEMBL4481929"	"Inhibition of JAK2 (unknown origin) after 1 hr FRET-based Z'-Lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480435"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4526032"	""	"0"	"410.40"	"0"	"1.88"	"21"	"Cn1cc(Nc2nccc(N3C[C@H]4CC[C@H](C3)N4C(=O)NCC(F)(F)F)n2)cn1"	"IC50"	"'='"	"1160.0"	"nM"	"5.94"	""	""	"UO_0000065"	"14.46"	"0.28"	"4.06"	"6.51"	"False"	"CHEMBL4411592"	"Inhibition of JAK2 homodimer signaling pathway in human spiked CD34 +ve cells of whole blood assessed as reduction in EPO induced STAT5 phosphorylation preincubated for 45 mins followed by EPO addition and measured measured after 15 mins by FACS assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4411260"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4554881"	""	"0"	"406.49"	"0"	"2.17"	"11"	"CCNC(=O)c1ccc(Nc2nccc(N3C[C@@H]4C[C@H]3CN4C(=O)C3CC3)n2)cc1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4411595"	"Inhibition of human JAK2 using fluorescence labeled peptide as substrate and using 1 mM ATP by microfluidic based mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4411260"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4593760"	""	"0"	"329.32"	"0"	"2.86"	"13"	"c1ccc(-n2cnnn2)c(-c2cc(-c3ccc4[nH]ncc4c3)on2)c1"	"IC50"	"'='"	"2000.0"	"nM"	"5.70"	""	""	"UO_0000065"	"17.31"	"0.31"	"2.84"	"5.80"	"False"	"CHEMBL4481929"	"Inhibition of JAK2 (unknown origin) after 1 hr FRET-based Z'-Lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480435"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4579262"	""	"0"	"379.84"	"0"	"3.98"	"16b"	"Clc1cccc(-n2cnnn2)c1-c1nc(-c2ccc3[nH]ncc3c2)cs1"	"IC50"	"'='"	"1680.0"	"nM"	"5.78"	""	""	"UO_0000065"	"15.20"	"0.30"	"1.79"	"6.78"	"False"	"CHEMBL4481929"	"Inhibition of JAK2 (unknown origin) after 1 hr FRET-based Z'-Lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480435"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4474752"	""	"0"	"413.49"	"0"	"3.27"	"14a"	"N#Cc1ccc(N2CCC(Nc3cc(Nc4ccccc4)ncc3C(N)=O)CC2)nc1"	"IC50"	"'='"	"190.0"	"nM"	"6.72"	""	""	"UO_0000065"	"16.25"	"0.30"	"3.45"	"5.60"	"False"	"CHEMBL4429528"	"Inhibition of human JAK2 assessed as reduction in phosphorylation of Biotin-Lyn-Substrate-2 after 1 hr in presence of ATP by ELISA"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4428070"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2016"	"None"	""
"CHEMBL4065693"	""	"0"	"387.44"	"0"	"3.66"	"9a"	"C=CC(=O)Nc1cccc(CNc2cc(Nc3ccccc3)ncc2C(N)=O)c1"	"IC50"	"'='"	"11000.0"	"nM"	"4.96"	""	""	"UO_0000065"	"12.80"	"0.23"	"1.30"	"4.54"	"False"	"CHEMBL4047236"	"Inhibition of JAK2 in human TF1 cells assessed as reduction in EPO-induced STAT5A phosphorylation pretreated for 30 mins followed by EPO addition measured after 10 mins by ELISA"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4043231"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL475817"	""	"0"	"469.25"	"1"	"5.49"	"39"	"Nc1ncc(NC(=O)c2cc(NC(=O)c3cccc(C(F)(F)F)c3)ccc2Cl)cc1Cl"	"IC50"	"'='"	"29000.0"	"nM"	"4.54"	""	""	"UO_0000065"	"9.67"	"0.20"	"-0.95"	"4.67"	"False"	"CHEMBL947777"	"Inhibition of Jak2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1143270"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL4640314"	""	"0"	"401.45"	"0"	"1.14"	"8"	"O=C(C1CC1)N1C2CCC1CN(c1nc(Nc3cnn(CCO)c3)ncc1F)C2"	"IC50"	"'='"	"260.0"	"nM"	"6.58"	""	""	"UO_0000065"	"16.40"	"0.31"	"5.45"	"6.62"	"False"	"CHEMBL4620433"	"Inhibition of human recombinant JAK2 assessed as level of phosphorylation in presence of peptide substrate FITC-KGGEEEEYFELVKK and ATP by mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4619733"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2020"	"None"	""
"CHEMBL4240012"	""	"0"	"610.72"	"2"	"6.21"	"13e"	"O=C(CCCCCCC(=O)Nc1ccc(Nc2nc(-c3cnn(CCCCOc4ccccc4)c3)c3cc[nH]c3n2)cc1)NO"	"IC50"	"'='"	"40.0"	"nM"	"7.40"	""	""	"UO_0000065"	"12.11"	"0.22"	"1.19"	"4.65"	"False"	"CHEMBL4233426"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma-33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229421"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2018"	"None"	""
"CHEMBL3589168"	""	"0"	"457.53"	"0"	"4.35"	"5"	"CCCOc1cccc(-c2cc(C(N)=O)c3[nH]c4ccc(C(=O)N5CCOCC5)cc4c3c2)c1"	"IC50"	"'='"	"350.0"	"nM"	"6.46"	""	""	"UO_0000065"	"14.11"	"0.26"	"2.11"	"6.61"	"False"	"CHEMBL3592855"	"Inhibition of JAK2 in human SET2 cells assessed as inhibition of cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3589325"	""	"0"	"384.48"	"0"	"3.84"	"17"	"CN1CCN(c2ccc3c(c2)[nH]c2c(C(N)=O)cc(-c4ccccc4)cc23)CC1"	"IC50"	"'='"	"370.0"	"nM"	"6.43"	""	""	"UO_0000065"	"16.73"	"0.30"	"2.59"	"9.84"	"False"	"CHEMBL3592855"	"Inhibition of JAK2 in human SET2 cells assessed as inhibition of cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL4455068"	""	"0"	"414.47"	"0"	"2.67"	"14b"	"N#Cc1ccc(N2CCC(Nc3cc(Nc4ccccn4)ncc3C(N)=O)CC2)nc1"	"IC50"	"'='"	"4.9"	"nM"	"8.31"	""	""	"UO_0000065"	"20.05"	"0.37"	"5.64"	"6.26"	"False"	"CHEMBL4429528"	"Inhibition of human JAK2 assessed as reduction in phosphorylation of Biotin-Lyn-Substrate-2 after 1 hr in presence of ATP by ELISA"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4428070"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2016"	"None"	""
"CHEMBL4529314"	""	"0"	"446.55"	"0"	"3.86"	"29"	"CCc1cc(O)c(F)cc1-c1cc(NS(=O)(=O)CCN2CCCCC2)c2cn[nH]c2c1"	"IC50"	"'='"	"158.49"	"nM"	"6.80"	""	""	"UO_0000065"	"15.23"	"0.30"	"2.94"	"6.92"	"False"	"CHEMBL4478762"	"Inhibition of human His-tagged JAK2 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4477220"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2016"	"None"	""
"CHEMBL4589842"	""	"0"	"351.82"	"0"	"3.35"	"12"	"CCS(=O)(=O)Nc1cc(-c2ccc(O)cc2Cl)cc2[nH]ncc12"	"IC50"	"'='"	"19.95"	"nM"	"7.70"	""	""	"UO_0000065"	"21.89"	"0.46"	"4.35"	"8.10"	"False"	"CHEMBL4478762"	"Inhibition of human His-tagged JAK2 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4477220"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2016"	"None"	""
"CHEMBL4563039"	""	"0"	"412.45"	"0"	"3.83"	"33"	"CCc1cc(O)c(F)cc1-c1cc(NS(=O)(=O)c2cccnc2)c2cn[nH]c2c1"	"IC50"	"'='"	"25.12"	"nM"	"7.60"	""	""	"UO_0000065"	"18.43"	"0.36"	"3.77"	"7.04"	"False"	"CHEMBL4478762"	"Inhibition of human His-tagged JAK2 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4477220"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2016"	"None"	""
"CHEMBL4483364"	""	"0"	"363.41"	"0"	"3.40"	"19"	"CCc1cc(O)c(F)cc1-c1cc(NS(=O)(=O)CC)c2cn[nH]c2c1"	"IC50"	"'='"	"5.012"	"nM"	"8.30"	""	""	"UO_0000065"	"22.84"	"0.45"	"4.90"	"8.73"	"False"	"CHEMBL4478762"	"Inhibition of human His-tagged JAK2 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4477220"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2016"	"None"	""
"CHEMBL4551061"	""	"0"	"345.42"	"0"	"3.26"	"11"	"CCc1cc(O)ccc1-c1cc(NS(=O)(=O)CC)c2cn[nH]c2c1"	"IC50"	"'='"	"19.95"	"nM"	"7.70"	""	""	"UO_0000065"	"22.29"	"0.44"	"4.44"	"8.10"	"False"	"CHEMBL4478762"	"Inhibition of human His-tagged JAK2 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4477220"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2016"	"None"	""
"CHEMBL3354185"	""	"0"	"391.44"	"0"	"2.50"	"4"	"COC1CCN(c2nccc(Nc3cc4[nH]c(-c5cn[nH]c5)nc4cn3)n2)CC1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3375809"	"Inhibition of Jak2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351701"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL3335697"	""	"0"	"458.55"	"0"	"0.82"	"26"	"CS(=O)(=O)N1CCC[C@H](Nc2nc(N3CC[C@@H](O)C3)ncc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"180.0"	"nM"	"6.75"	""	""	"UO_0000065"	"14.71"	"0.29"	"5.92"	"4.81"	"False"	"CHEMBL3374010"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 1 hr in presence of [gamma-33P]ATP by scintillation counting analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351377"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL4553035"	""	"0"	"447.54"	"0"	"2.47"	"11"	"Cc1cnc(NC(=O)C2CC2)nc1-c1c[nH]c2c(NC(=O)CN3CCN(C)CC3)cccc12"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4406243"	"Inhibition of recombinant human N-terminal GST-tagged JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-labeled GEEPLYWSFPAKKK-NH2 peptide as substrate after 10 mins in presence of 5 mM ATP by caliper mobility shift assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402602"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL3891913"	""	"0"	"463.43"	"0"	"4.06"	"BDBM255017"	"O=C1c2cnc3[nH]ccc3c2N([C@H]2CC[C@H](CNCC(F)(F)F)CC2)CN1CC(F)(F)F"	"IC50"	"'='"	"35.0"	"nM"	"7.46"	""	"443873"	"UO_0000065"	"16.09"	"0.32"	"3.40"	"11.60"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3942783"	""	"0"	"434.47"	"0"	"3.36"	"BDBM254994"	"CN(CC#N)C[C@H]1CC[C@H](N2CN(CC(F)(F)F)C(=O)c3cnc4[nH]ccc4c32)CC1"	"IC50"	"'='"	"74.0"	"nM"	"7.13"	""	"443901"	"UO_0000065"	"16.41"	"0.31"	"3.77"	"9.00"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL569091"	""	"0"	"422.54"	"0"	"2.63"	"25"	"CCCN(CCC)C(=O)C1CCCN(c2cc(-c3c(N)nn4cccnc34)ncn2)C1"	"IC50"	"'='"	"1900.0"	"nM"	"5.72"	""	""	"UO_0000065"	"13.54"	"0.25"	"3.09"	"5.42"	"False"	"CHEMBL1044320"	"Inhibition of JAK2-mediated STAT5 phosphorylation in GMCSF-stimulated human TF1 cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"CHEMBL3307972"	""
"CHEMBL570456"	""	"0"	"462.48"	"0"	"2.79"	"28"	"CCN(CCC(F)(F)F)C(=O)C1CCCN(c2cc(-c3c(N)nn4cccnc34)ncn2)C1"	"IC50"	"'='"	"910.0"	"nM"	"6.04"	""	""	"UO_0000065"	"13.06"	"0.25"	"3.25"	"5.72"	"False"	"CHEMBL1044320"	"Inhibition of JAK2-mediated STAT5 phosphorylation in GMCSF-stimulated human TF1 cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"CHEMBL3307972"	""
"CHEMBL568816"	""	"0"	"331.38"	"0"	"2.94"	"37"	"C[C@@H](Nc1cc(-c2c(N)nn3cccnc23)ncn1)c1ccccc1"	"IC50"	"'='"	"4700.0"	"nM"	"5.33"	""	""	"UO_0000065"	"16.08"	"0.29"	"2.39"	"5.67"	"False"	"CHEMBL1044320"	"Inhibition of JAK2-mediated STAT5 phosphorylation in GMCSF-stimulated human TF1 cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"CHEMBL3307972"	""
"CHEMBL3335695"	""	"0"	"389.44"	"0"	"0.54"	"24"	"CS(=O)(=O)N1CCC[C@H](Nc2[nH]c(=O)ncc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"129.0"	"nM"	"6.89"	""	""	"UO_0000065"	"17.69"	"0.35"	"6.35"	"5.04"	"False"	"CHEMBL3374010"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 1 hr in presence of [gamma-33P]ATP by scintillation counting analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351377"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3968326"	""	"0"	"420.44"	"0"	"3.02"	"BDBM255006"	"N#CCNC[C@H]1CC[C@H](N2CN(CC(F)(F)F)C(=O)c3cnc4[nH]ccc4c32)CC1"	"IC50"	"'='"	"44.0"	"nM"	"7.36"	""	"443862"	"UO_0000065"	"17.50"	"0.33"	"4.34"	"8.35"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3589329"	""	"0"	"438.54"	"0"	"3.73"	"21"	"CN1CCN(c2ccc3c(c2)[nH]c2c(C(N)=O)cc(-c4ccc5c(cnn5C)c4)cc23)CC1"	"IC50"	"'='"	"130.0"	"nM"	"6.89"	""	""	"UO_0000065"	"15.70"	"0.28"	"3.16"	"8.28"	"False"	"CHEMBL3592855"	"Inhibition of JAK2 in human SET2 cells assessed as inhibition of cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL569092"	""	"0"	"448.45"	"0"	"2.40"	"26"	"CCN(CC(F)(F)F)C(=O)C1CCCN(c2cc(-c3c(N)nn4cccnc34)ncn2)C1"	"IC50"	"'='"	"1300.0"	"nM"	"5.89"	""	""	"UO_0000065"	"13.13"	"0.25"	"3.49"	"5.58"	"False"	"CHEMBL1044320"	"Inhibition of JAK2-mediated STAT5 phosphorylation in GMCSF-stimulated human TF1 cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"CHEMBL3307972"	""
"CHEMBL569012"	""	"0"	"351.80"	"0"	"3.03"	"35"	"Nc1nn2cccnc2c1-c1cc(NCc2ccc(Cl)cc2)ncn1"	"IC50"	"'='"	"1500.0"	"nM"	"5.82"	""	""	"UO_0000065"	"16.55"	"0.32"	"2.79"	"6.19"	"False"	"CHEMBL1044320"	"Inhibition of JAK2-mediated STAT5 phosphorylation in GMCSF-stimulated human TF1 cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"CHEMBL3307972"	""
"CHEMBL3932070"	""	"0"	"378.48"	"0"	"2.62"	"BDBM255033"	"CN1CN([C@H]2CC[C@H](CNC3(C#N)CC3)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	"443905"	"UO_0000065"	"20.46"	"0.38"	"5.12"	"8.80"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3894490"	""	"0"	"407.47"	"0"	"2.80"	"BDBM255037"	"COCN1CN([C@H]2CC[C@H](CNCC(F)F)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	"443909"	"UO_0000065"	"19.01"	"0.36"	"4.94"	"10.54"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3896236"	""	"0"	"380.50"	"0"	"2.82"	"BDBM255041"	"CCN1CN([C@H]2CC[C@H](CN(C)CC#N)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"260.0"	"nM"	"6.58"	""	"443913"	"UO_0000065"	"17.31"	"0.32"	"3.77"	"8.31"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3957838"	""	"0"	"485.53"	"0"	"2.94"	"BDBM254997"	"O=C1c2cnc3[nH]ccc3c2N([C@H]2CC[C@H](CN3CCCS3(=O)=O)CC2)CN1CC(F)(F)F"	"IC50"	"'='"	"28.0"	"nM"	"7.55"	""	"443918"	"UO_0000065"	"15.56"	"0.31"	"4.61"	"8.43"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL460472"	""	"0"	"539.59"	"1"	"4.71"	"59e, AMG-458"	"COc1ccc2c(Oc3ccc(NC(=O)c4c(C)n(CC(C)(C)O)n(-c5ccccc5)c4=O)nc3)ccnc2c1"	"IC50"	"'='"	"25000.0"	"nM"	"4.60"	""	""	"UO_0000065"	"8.53"	"0.16"	"-0.11"	"3.82"	"False"	"CHEMBL2032473"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2029218"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL3892634"	""	"0"	"309.37"	"0"	"2.64"	"BDBM255000"	"N#CCN1CN(C2CCCCC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"24.0"	"nM"	"7.62"	""	"443856"	"UO_0000065"	"24.63"	"0.45"	"4.98"	"10.02"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3938113"	""	"0"	"407.44"	"0"	"3.31"	"BDBM255010"	"O=C1NCN([C@H]2CC[C@H](CNC3(C(F)(F)F)CC3)CC2)c2c1cnc1[nH]ccc21"	"IC50"	"'='"	"6.4"	"nM"	"8.19"	""	"443866"	"UO_0000065"	"20.11"	"0.39"	"4.88"	"11.22"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3901870"	""	"0"	"466.51"	"0"	"2.58"	"BDBM255025"	"CN(C)C(=O)CN1CN([C@H]2CC[C@H](CNCC(F)(F)F)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	"443881"	"UO_0000065"	"17.06"	"0.33"	"5.38"	"9.41"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL568788"	""	"0"	"338.35"	"0"	"2.83"	"7b"	"Cc1cc(Nc2cnc(C#N)c(NC(C)c3ccc(F)cn3)n2)n[nH]1"	"IC50"	"'<'"	"3.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1043451"	"Inhibition of JAK2 using 2 mM ATP as a substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156131"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL569720"	""	"0"	"353.37"	"0"	"2.53"	"7c"	"Cc1cc(Nc2nc(N[C@@H](C)c3ncc(F)cn3)c(C#N)nc2C)n[nH]1"	"IC50"	"'<'"	"3.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1043451"	"Inhibition of JAK2 using 2 mM ATP as a substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156131"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL571526"	""	"0"	"353.36"	"0"	"3.11"	"7j"	"Cc1cc(Nc2nc(O[C@H](C)c3ccc(F)cn3)c(C#N)nc2C)n[nH]1"	"IC50"	"'='"	"108.0"	"nM"	"6.97"	""	""	"UO_0000065"	"19.72"	"0.37"	"3.86"	"6.20"	"False"	"CHEMBL1043451"	"Inhibition of JAK2 using 2 mM ATP as a substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156131"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL576068"	""	"0"	"327.37"	"0"	"3.27"	"7l"	"Cc1cc(Nc2nc(N[C@@H](C)c3ccc(F)cn3)cnc2C)n[nH]1"	"IC50"	"'<'"	"3.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1043451"	"Inhibition of JAK2 using 2 mM ATP as a substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156131"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL570230"	""	"0"	"352.38"	"0"	"3.14"	"7f"	"Cc1cc(Nc2nc(N[C@H](C)c3ccc(F)cn3)c(C#N)nc2C)n[nH]1"	"IC50"	"'='"	"907.0"	"nM"	"6.04"	""	""	"UO_0000065"	"17.15"	"0.32"	"2.90"	"5.25"	"False"	"CHEMBL1043452"	"Inhibition of JAK2 using 5 mM ATP as a substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156131"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL568789"	""	"0"	"352.38"	"0"	"3.14"	"7g"	"Cc1cc(Nc2nc(NC(C)c3ccc(F)cn3)c(C#N)nc2C)n[nH]1"	"IC50"	"'='"	"47.0"	"nM"	"7.33"	""	""	"UO_0000065"	"20.80"	"0.38"	"4.19"	"6.36"	"False"	"CHEMBL1043452"	"Inhibition of JAK2 using 5 mM ATP as a substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156131"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL570899"	""	"0"	"314.33"	"0"	"2.35"	"7o"	"Cc1cc(Nc2cncc(N[C@@H](C)c3ncc(F)cn3)n2)n[nH]1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"27.11"	"0.51"	"6.17"	"8.17"	"True"	"CHEMBL1043452"	"Inhibition of JAK2 using 5 mM ATP as a substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156131"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL576272"	""	"0"	"338.38"	"0"	"0.47"	"17"	"NC(=O)C1CCN(c2cc(-c3c(N)nn4cccnc34)ncn2)CC1"	"IC50"	"'='"	"190.0"	"nM"	"6.72"	""	""	"UO_0000065"	"19.86"	"0.37"	"6.25"	"5.24"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL569757"	""	"0"	"408.51"	"0"	"2.24"	"24"	"CCCN(CC)C(=O)C1CCCN(c2cc(-c3c(N)nn4cccnc34)ncn2)C1"	"IC50"	"'='"	"3.6"	"nM"	"8.44"	""	""	"UO_0000065"	"20.67"	"0.38"	"6.20"	"8.00"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL569012"	""	"0"	"351.80"	"0"	"3.03"	"35"	"Nc1nn2cccnc2c1-c1cc(NCc2ccc(Cl)cc2)ncn1"	"IC50"	"'='"	"1.4"	"nM"	"8.85"	""	""	"UO_0000065"	"25.17"	"0.48"	"5.82"	"9.42"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL3930342"	""	"0"	"395.43"	"0"	"3.12"	"BDBM254996"	"CN(CC(F)(F)F)C[C@H]1CC[C@H](N2CNC(=O)c3cnc4[nH]ccc4c32)CC1"	"IC50"	"'='"	"4.6"	"nM"	"8.34"	""	"443917"	"UO_0000065"	"21.08"	"0.41"	"5.22"	"12.97"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3964946"	""	"0"	"334.37"	"0"	"3.24"	"BDBM255008"	"CN1CN([C@H]2CC[C@H](C(F)F)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	"443864"	"UO_0000065"	"23.69"	"0.45"	"4.68"	"15.17"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4592912"	""	"0"	"391.79"	"0"	"2.85"	"8t"	"O=C(CCn1cc(Nc2ncc(Cl)c(Nc3ccc(F)cc3)n2)cn1)NO"	"IC50"	"'='"	"22.0"	"nM"	"7.66"	""	""	"UO_0000065"	"19.55"	"0.39"	"4.81"	"6.55"	"False"	"CHEMBL4347596"	"Inhibition of recombinant human JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate measured after 60 mins by LANCE assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4346670"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4540416"	""	"0"	"479.90"	"0"	"4.52"	"8z"	"O=C(/C=C/c1ccc(Cn2cc(Nc3ncc(Cl)c(Nc4ccc(F)cc4)n3)cn2)cc1)NO"	"IC50"	"'='"	"43.0"	"nM"	"7.37"	""	""	"UO_0000065"	"15.35"	"0.30"	"2.85"	"6.30"	"False"	"CHEMBL4347596"	"Inhibition of recombinant human JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate measured after 60 mins by LANCE assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4346670"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL1243326"	""	"0"	"515.55"	"2"	"6.87"	"8b"	"CNc1nccc(-c2cccnc2Oc2ccc(Nc3nnc(-c4ccc(F)cc4)c4ccccc34)cc2)n1"	"IC50"	"'>'"	"25000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1247968"	"Inhibition of Jak2 by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1240487"	"1"	"Scientific Literature"	"J. Med. Chem."	"2010"	"None"	""
"CHEMBL560245"	""	"0"	"387.91"	"1"	"5.80"	"11a"	"Cc1cc2c(c(Cl)n1)-c1[nH]c3ccccc3c1CCN2CCc1ccccc1"	"IC50"	"'='"	"33500.0"	"nM"	"4.47"	""	""	"UO_0000065"	"11.54"	"0.22"	"-1.33"	"14.02"	"False"	"CHEMBL1036442"	"Inhibition of recombinant JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1151875"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2009"	"None"	""
"CHEMBL4466247"	""	"0"	"482.55"	"0"	"4.68"	"8"	"COc1nn(C)cc1Nc1ncc(C)c(-c2c[nH]c3c(C(=O)Nc4ccc(C)nc4C)cccc23)n1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4406243"	"Inhibition of recombinant human N-terminal GST-tagged JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-labeled GEEPLYWSFPAKKK-NH2 peptide as substrate after 10 mins in presence of 5 mM ATP by caliper mobility shift assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402602"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL3645537"	""	"0"	"457.97"	"0"	"4.71"	"BDBM107120"	"O=C(CN1CCN(c2ccc(Cl)cc2)CC1)Nc1cccc(-c2cnc3ccccc3n2)c1"	"IC50"	"'>'"	"20000.0"	"nM"	""	""	"226357"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652392"	""	"0"	"494.63"	"0"	"2.37"	"BDBM113204"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCN(c3ncccc3C#N)CC2)CC1"	"IC50"	"'='"	"17.6"	"nM"	"7.75"	""	"234647"	"UO_0000065"	"15.68"	"0.30"	"5.38"	"6.35"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3642399"	""	"0"	"504.66"	"1"	"4.34"	"BDBM99677"	"CN1CCC(c2ccc(Nc3nc4c(-c5cccc(CN(C)S(C)(=O)=O)c5)cccn4n3)cc2)CC1"	"IC50"	"'='"	"7.21"	"nM"	"8.14"	""	"216367"	"UO_0000065"	"16.13"	"0.31"	"3.80"	"9.83"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703047"	""	"0"	"490.61"	"0"	"3.81"	"BDBM147757"	"CC(C)(C(=O)O)c1ccc(Nc2nn([C@H]3CCC(N4CC5(CCC5)C4)C[C@@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"80.0"	"nM"	"7.10"	""	"285691"	"UO_0000065"	"14.47"	"0.27"	"3.29"	"5.17"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL191003"	"JNJ-7706621"	"0"	"394.36"	"0"	"1.22"	"1; JNJ7706621"	"Nc1nc(Nc2ccc(S(N)(=O)=O)cc2)nn1C(=O)c1c(F)cccc1F"	"IC50"	"'='"	"2960.0"	"nM"	"5.53"	""	""	"UO_0000065"	"14.02"	"0.28"	"4.31"	"3.79"	"False"	"CHEMBL4359666"	"Inhibition of wild type full length human JAK2 (1 to 1132 residues) autophosphorylation expressed in HEK293T cells incubated in buffer with compound for 1 hr followed by treatment with enzyme and [gamma32P]-ATP for 15 mins by immunoprecipitation assay based autoradiography"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4354882"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL3645066"	""	"0"	"502.59"	"1"	"4.56"	"BDBM99834"	"COc1cccc(-c2cccn3nc(Nc4ccc(C5CCN(CC(=O)N(C)C)CC5)cc4)nc23)c1F"	"IC50"	"'='"	"18.73"	"nM"	"7.73"	""	"216507"	"UO_0000065"	"15.38"	"0.29"	"3.17"	"10.30"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647794"	""	"0"	"430.94"	"0"	"2.97"	"BDBM147897"	"CC(C)(O)CN[C@H]1CCC(n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"42.0"	"nM"	"7.38"	""	"285831"	"UO_0000065"	"17.12"	"0.34"	"4.41"	"5.72"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3639465"	""	"0"	"588.63"	"1"	"2.28"	"BDBM147831"	"N#C[C@H]1CC(NCC2CCS(=O)(=O)C2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	"285765"	"UO_0000065"	"13.59"	"0.28"	"5.72"	"4.52"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL1289991"	""	"0"	"328.38"	"0"	"3.60"	"1"	"O=c1[nH]ccc2nc(NCc3ccncc3)c(-c3ccccc3)cc12"	"IC50"	"'='"	"1400.0"	"nM"	"5.85"	""	""	"UO_0000065"	"17.83"	"0.32"	"2.25"	"8.28"	"False"	"CHEMBL1291235"	"Inhibition of JAK2 in cell-free system"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287746"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1289218"	""	"0"	"336.32"	"0"	"3.47"	"41"	"CC(C)[C@@H](Nc1nc2cc[nH]c(=O)c2c2cnccc12)C(F)(F)F"	"IC50"	"'='"	"40.0"	"nM"	"7.40"	""	""	"UO_0000065"	"22.00"	"0.42"	"3.93"	"10.47"	"True"	"CHEMBL1291236"	"Inhibition of JAK2 expressed in human Du-145 cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"DU-145"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287746"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3308034"	""
"CHEMBL4453646"	""	"0"	"321.17"	"0"	"3.99"	"7"	"Clc1cccc(Nc2nc(Nc3cn[nH]c3)ncc2Cl)c1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	""	"UO_0000065"	"27.09"	"0.57"	"4.71"	"11.08"	"False"	"CHEMBL4347596"	"Inhibition of recombinant human JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate measured after 60 mins by LANCE assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4346670"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4441124"	""	"0"	"413.46"	"0"	"3.76"	"8p"	"O=C(CCCCCCn1cc(Nc2nccc(Nc3ccc(F)cc3)n2)cn1)NO"	"IC50"	"'>'"	"100.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4347596"	"Inhibition of recombinant human JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate measured after 60 mins by LANCE assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4346670"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4538220"	""	"0"	"431.45"	"0"	"3.89"	"8q"	"O=C(CCCCCCn1cc(Nc2ncc(F)c(Nc3ccc(F)cc3)n2)cn1)NO"	"IC50"	"'>'"	"100.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4347596"	"Inhibition of recombinant human JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate measured after 60 mins by LANCE assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4346670"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL3702893"	""	"0"	"368.40"	"0"	"2.16"	"BDBM147592"	"COC(=O)c1cncc(Nc2nn([C@H]3CCCC[C@@H]3C#N)cc2C(N)=O)c1"	"IC50"	"'='"	"89.0"	"nM"	"7.05"	""	"285522"	"UO_0000065"	"19.14"	"0.36"	"4.89"	"5.19"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651019"	""	"0"	"380.40"	"0"	"2.94"	"BDBM153196"	"CCOC(=O)c1c[nH]c2ncnc(-c3cccc(NC(=O)/C=C/COC)c3)c12"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294144"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647932"	""	"0"	"457.43"	"0"	"2.24"	"BDBM148052"	"N#C[C@@H]1C[C@@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"285445"	"UO_0000065"	"18.15"	"0.37"	"6.06"	"5.49"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702922"	""	"0"	"378.36"	"0"	"3.39"	"BDBM147621"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)nc2)n1"	"IC50"	"'='"	"260.0"	"nM"	"6.58"	""	"285559"	"UO_0000065"	"17.40"	"0.33"	"3.20"	"6.01"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642326"	""	"0"	"354.37"	"0"	"2.09"	"BDBM99598"	"O=[N+]([O-])c1cccc(CNc2cccn3nc(N4CCOCC4)nc23)c1"	"IC50"	"'='"	"9999.0"	"nM"	"5.00"	""	"216288"	"UO_0000065"	"14.11"	"0.26"	"2.91"	"5.11"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3699531"	""	"0"	"449.48"	"0"	"4.18"	"BDBM147549"	"CC(C)(c1ccc(Nc2nn([C@@H]3CCCC[C@H]3C#N)cc2C(N)=O)cc1)[C@@H](O)C(F)(F)F"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"285479"	"UO_0000065"	"20.02"	"0.38"	"4.82"	"7.69"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702984"	""	"0"	"364.45"	"0"	"2.66"	"BDBM147694"	"N#C[C@H]1C[C@@H](N2CCC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccccc2)n1"	"IC50"	"'='"	"39.0"	"nM"	"7.41"	""	"285628"	"UO_0000065"	"20.33"	"0.37"	"4.75"	"7.41"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645008"	""	"0"	"354.37"	"0"	"3.38"	"BDBM99760"	"O=c1[nH]cccc1-c1cccn2nc(Nc3ccc4ncccc4c3)nc12"	"IC50"	"'='"	"224.04"	"nM"	"6.65"	""	"216448"	"UO_0000065"	"18.76"	"0.34"	"3.27"	"7.56"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3645018"	""	"0"	"486.58"	"0"	"3.21"	"BDBM99770"	"COc1cnc(-c2cccn3nc(Nc4ccc(C5CCN(CC(=O)N(C)C)CC5)cc4)nc23)cn1"	"IC50"	"'='"	"134.39"	"nM"	"6.87"	""	"216457"	"UO_0000065"	"14.12"	"0.26"	"3.66"	"6.82"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3665216"	""	"0"	"510.63"	"1"	"1.14"	"BDBM112616"	"C[C@H]1C[C@H](Nc2nc(N3CCN(C)CC3)ncc2-c2cnc3[nH]ccc3n2)CN(S(=O)(=O)CC#N)C1"	"IC50"	"'='"	"0.0782"	"nM"	"10.11"	""	"233853"	"UO_0000065"	"19.79"	"0.38"	"8.97"	"6.87"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3699520"	""	"0"	"328.35"	"0"	"2.51"	"BDBM147538"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(F)nc2)n1"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	"285468"	"UO_0000065"	"23.59"	"0.44"	"5.23"	"7.07"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647828"	""	"0"	"446.48"	"0"	"4.12"	"BDBM147934"	"N#C[C@@H]1C[C@@H](NC2CCC2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"136.0"	"nM"	"6.87"	""	"285868"	"UO_0000065"	"15.38"	"0.29"	"2.75"	"6.31"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642425"	""	"0"	"490.59"	"0"	"3.21"	"BDBM99703"	"CCN1CCN(c2cccc(Nc3nc4c(-c5ccc(S(C)(=O)=O)cc5)cccn4n3)c2)C(=O)C1"	"IC50"	"'='"	"1.88"	"nM"	"8.73"	""	"216393"	"UO_0000065"	"17.79"	"0.34"	"5.52"	"8.73"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL2062788"	""	"0"	"211.23"	"0"	"1.37"	"13"	"Nc1nc2c(-c3cccnc3)cccn2n1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2067611"	"Inhibition of human JAK2 expressed in baculovirus using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate preincubated for 1 hr measured after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL3658111"	""	"0"	"644.70"	"2"	"5.58"	"BDBM148419"	"Cc1ccc(NC(=O)c2cccc(C(F)(F)F)c2)cc1N1CCc2nc(Nc3ccc(C(=O)NC4CCN(C)CC4)nc3)ncc2C1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"286797"	"UO_0000065"	"12.88"	"0.24"	"2.72"	"7.19"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL2062789"	""	"0"	"241.25"	"0"	"1.38"	"14"	"COc1ccc(-c2cccn3nc(N)nc23)cn1"	"IC50"	"'='"	"2874.0"	"nM"	"5.54"	""	""	"UO_0000065"	"22.97"	"0.42"	"4.16"	"7.07"	"False"	"CHEMBL2067611"	"Inhibition of human JAK2 expressed in baculovirus using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate preincubated for 1 hr measured after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2062796"	""	"0"	"364.43"	"0"	"3.54"	"21"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4ccccc4)nc23)cc1"	"IC50"	"'='"	"385.0"	"nM"	"6.42"	""	""	"UO_0000065"	"17.60"	"0.34"	"2.87"	"8.40"	"False"	"CHEMBL2067179"	"Inhibition of JAK2 in human TF-1 cells using GM-CSF pretreated for 1 hr prior to GM-CSF addition measured after 5 hrs by FRET based GeneBLAzer assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"CHEMBL3307972"	""
"CHEMBL2062803"	""	"0"	"449.54"	"0"	"3.38"	"28"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4ccc(N5CCOCC5)cc4)nc23)cc1"	"IC50"	"'='"	"0.9"	"nM"	"9.05"	""	""	"UO_0000065"	"20.12"	"0.39"	"5.67"	"10.18"	"True"	"CHEMBL2067611"	"Inhibition of human JAK2 expressed in baculovirus using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate preincubated for 1 hr measured after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2062802"	""	"0"	"449.54"	"0"	"3.38"	"27"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4cccc(N5CCOCC5)c4)nc23)cc1"	"IC50"	"'='"	"110.0"	"nM"	"6.96"	""	""	"UO_0000065"	"15.48"	"0.30"	"3.58"	"7.83"	"False"	"CHEMBL2067179"	"Inhibition of JAK2 in human TF-1 cells using GM-CSF pretreated for 1 hr prior to GM-CSF addition measured after 5 hrs by FRET based GeneBLAzer assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"CHEMBL3307972"	""
"CHEMBL3703005"	""	"0"	"421.43"	"0"	"2.93"	"BDBM147715"	"CN(C)[C@@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(C(F)(F)F)nc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"155.0"	"nM"	"6.81"	""	"285649"	"UO_0000065"	"16.16"	"0.31"	"3.88"	"6.03"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642375"	""	"0"	"492.61"	"0"	"2.66"	"BDBM99651"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4cccc(N5CCN(CCO)CC5)c4)nc23)cc1"	"IC50"	"'='"	"2.37"	"nM"	"8.62"	""	"216341"	"UO_0000065"	"17.51"	"0.34"	"5.97"	"8.37"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647793"	""	"0"	"414.90"	"0"	"2.68"	"BDBM147896"	"N#C[C@H]1C[C@H](NC2(O)CC2)CCC1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"30.0"	"nM"	"7.52"	""	"285830"	"UO_0000065"	"18.13"	"0.35"	"4.84"	"5.83"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647778"	""	"0"	"412.93"	"0"	"3.75"	"BDBM147881"	"CC1(N[C@H]2CCC(n3cc(C(N)=O)c(Nc4ccc(Cl)cc4)n3)[C@@H](C#N)C2)CC1"	"IC50"	"'='"	"21.0"	"nM"	"7.68"	""	"285815"	"UO_0000065"	"18.59"	"0.36"	"3.93"	"7.06"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699462"	""	"0"	"373.44"	"0"	"1.99"	"BDBM147477"	"CS(=O)(=O)c1ccc(Nc2nn([C@H]3CCC[C@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"82.0"	"nM"	"7.09"	""	"285402"	"UO_0000065"	"18.98"	"0.37"	"5.10"	"5.41"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699550"	""	"0"	"378.26"	"0"	"4.29"	"BDBM147568"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)c(Cl)c2)n1"	"IC50"	"'='"	"93.0"	"nM"	"7.03"	""	"285498"	"UO_0000065"	"18.59"	"0.38"	"2.74"	"7.27"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647807"	""	"0"	"458.99"	"0"	"3.97"	"BDBM147910"	"COCC(C)(C)N(C)[C@H]1CCC(n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"63.0"	"nM"	"7.20"	""	"285844"	"UO_0000065"	"15.69"	"0.31"	"3.23"	"6.59"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3650981"	""	"0"	"306.33"	"0"	"3.28"	"BDBM153155"	"CCOC(=O)c1c[nH]c2ncnc(-c3ccc4cc[nH]c4c3)c12"	"IC50"	"'='"	"137.0"	"nM"	"6.86"	""	"294103"	"UO_0000065"	"22.40"	"0.41"	"3.58"	"8.20"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651052"	""	"0"	"355.40"	"0"	"4.20"	"BDBM153229"	"C=C(C)C(=O)Nc1cccc(-c2ncnc3[nH]cc(-c4cccnc4)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294177"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702970"	""	"0"	"484.50"	"0"	"2.81"	"BDBM147683"	"CN(C)[C@H]1CCC(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"285616"	"UO_0000065"	"16.61"	"0.33"	"5.24"	"6.00"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702928"	""	"0"	"357.39"	"0"	"2.48"	"BDBM147630"	"C[C@]1(C#N)CC[C@H](O)C[C@@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"22.0"	"nM"	"7.66"	""	"285560"	"UO_0000065"	"21.43"	"0.40"	"5.18"	"6.55"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3650677"	""	"0"	"420.47"	"0"	"1.65"	"BDBM148059"	"CS(=O)(=O)N[C@@H]1CCC(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@H](C#N)C1"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	"285962"	"UO_0000065"	"18.84"	"0.37"	"6.27"	"5.54"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3655103"	""	"0"	"430.54"	"0"	"1.36"	"BDBM159770"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)N2CCC(c3cc[nH]n3)CC2)C1"	"IC50"	"'='"	"52.0"	"nM"	"7.28"	""	"302580"	"UO_0000065"	"16.92"	"0.33"	"5.92"	"5.93"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652315"	""	"0"	"435.59"	"0"	"2.64"	"BDBM113125"	"COCC1CCN(S(=O)(=O)C[C@H]2CC[C@H](N(C)c3ncnc4[nH]ccc34)CC2)CC1"	"IC50"	"'='"	"71.0"	"nM"	"7.15"	""	"234568"	"UO_0000065"	"16.41"	"0.33"	"4.51"	"7.82"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL2062804"	""	"0"	"462.58"	"0"	"3.30"	"BDBM99537"	"CN1CCN(c2cccc(Nc3nc4c(-c5ccc(S(C)(=O)=O)cc5)cccn4n3)c2)CC1"	"IC50"	"'='"	"1.3"	"nM"	"8.89"	""	"216229"	"UO_0000065"	"19.21"	"0.37"	"5.59"	"10.73"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL2062797"	""	"0"	"394.46"	"0"	"3.55"	"BDBM99527"	"COc1ccccc1Nc1nc2c(-c3ccc(S(C)(=O)=O)cc3)cccn2n1"	"IC50"	"'='"	"1321.1"	"nM"	"5.88"	""	"216219"	"UO_0000065"	"14.90"	"0.29"	"2.33"	"6.87"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3665148"	""	"0"	"400.51"	"0"	"2.55"	"BDBM112538"	"CCS(=O)(=O)N1CCCC(Nc2nc(C)ccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.1612"	"nM"	"9.79"	""	"233777"	"UO_0000065"	"24.45"	"0.48"	"7.24"	"9.43"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647840"	""	"0"	"373.84"	"0"	"2.99"	"BDBM147949"	"C[C@]1(O)CC[C@H](n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"285883"	"UO_0000065"	"21.52"	"0.42"	"5.06"	"6.88"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699504"	""	"0"	"541.55"	"1"	"3.84"	"BDBM147521"	"CC(C)(C)OC(=O)C1CCC(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)(F)F)cc3)n2)C(C#N)C1"	"IC50"	"'='"	"436.0"	"nM"	"6.36"	""	"285451"	"UO_0000065"	"11.75"	"0.23"	"2.52"	"4.05"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651029"	""	"0"	"435.48"	"0"	"2.63"	"BDBM153206"	"C=C(CN1CCOCC1)C(=O)Nc1cccc(-c2ncnc3[nH]cc(C(=O)OCC)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294154"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651045"	""	"0"	"372.40"	"0"	"4.95"	"BDBM153222"	"C=C(C)C(=O)Nc1cccc(-c2ncnc3[nH]cc(-c4ccccc4F)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294170"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645057"	""	"0"	"534.61"	"2"	"5.35"	"BDBM99825"	"COc1cc(C(F)F)ccc1-c1cccn2nc(Nc3ccc(C4CCN(CC(=O)N(C)C)CC4)cc3)nc12"	"IC50"	"'='"	"33.69"	"nM"	"7.47"	""	"216498"	"UO_0000065"	"13.98"	"0.26"	"2.12"	"9.96"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3651002"	""	"0"	"374.40"	"0"	"3.97"	"BDBM153178"	"C=C(C)C(=O)n1ccc2ccc(-c3ncnc4[nH]cc(C(=O)OCC)c34)cc21"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294126"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647862"	""	"0"	"365.44"	"0"	"2.83"	"BDBM147973"	"N#C[C@H]1C[C@@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C3CC3)cc2)n1"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	"285907"	"UO_0000065"	"21.89"	"0.40"	"5.17"	"6.84"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642401"	""	"0"	"547.68"	"2"	"5.66"	"BDBM99679"	"CC(C)(C)OC(=O)N1CCC(c2cccc(Nc3nc4c(-c5ccc(S(C)(=O)=O)cc5)cccn4n3)c2)CC1"	"IC50"	"'='"	"1.9"	"nM"	"8.72"	""	"216369"	"UO_0000065"	"15.92"	"0.31"	"3.06"	"8.24"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3694587"	""	"0"	"352.83"	"0"	"4.94"	"BDBM125908"	"C[C@@H]1Nc2nc(ncc2Cl)Nc2cccc(c2)COc2cccc1c2"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"255681"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707544"	"In Vitro Kinase Assay: One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Biochemistry 1999, 269, 94-104. The catalytic domains of human JAK1 (a.a. 837-1142), JAK2 (a.a. 828-1132) and JAK3 (a.a. 781-1124) with an N-terminal His tag were expressed using baculovirus in insect cells and purified. The catalytic activity of JAK1, JAK2 or JAK3 was assayed by measuring the phosphorylation of a biotinylated peptide. The phosphorylated peptide was detected by homogenous time resolved fluorescence (HTRF). IC50s of compounds were measured for each kinase in the reactions that contain the enzyme, ATP and 500 nM peptide in 50 mM Tris (pH 7.8) buffer with 100 mM NaCl, 5 mM DTT, and 0.1 mg/mL (0.01%) BSA. The ATP concentration in the reactions was 90 uM for JAK1, 30 uM for JAK2 and 3 uM for JAK3. Reactions were carried out at room temperature for 1 hr and then stopped with 20 uL 45 mM EDTA."	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639093"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3652390"	""	"0"	"469.62"	"0"	"2.50"	"BDBM113202"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCN(c3ccccn3)CC2)CC1"	"IC50"	"'='"	"22.3"	"nM"	"7.65"	""	"234645"	"UO_0000065"	"16.29"	"0.32"	"5.15"	"7.78"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3699461"	""	"0"	"373.44"	"0"	"1.99"	"BDBM147476"	"CS(=O)(=O)c1ccc(Nc2nn([C@H]3CCC[C@@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	"285401"	"UO_0000065"	"21.31"	"0.42"	"5.97"	"6.08"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3658094"	""	"0"	"561.57"	"2"	"5.12"	"BDBM148358"	"CNC(=O)c1ccc(Nc2ncc3c(n2)CCN(c2cc(NC(=O)c4cccc(C(F)(F)F)c4)ccc2C)C3)cn1"	"IC50"	"'='"	"32.0"	"nM"	"7.50"	""	"286779"	"UO_0000065"	"13.35"	"0.25"	"2.37"	"6.68"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665217"	""	"0"	"485.62"	"0"	"1.25"	"BDBM112617"	"C[C@H]1C[C@H](Nc2nc(N3CCN(C)CC3)ncc2-c2cnc3[nH]ccc3n2)CN(S(C)(=O)=O)C1"	"IC50"	"'='"	"0.2168"	"nM"	"9.66"	""	"233854"	"UO_0000065"	"19.90"	"0.39"	"8.41"	"7.84"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703023"	""	"0"	"490.53"	"0"	"3.90"	"BDBM147733"	"CC1(C)CN([C@@H]2CC[C@H](n3cc(C(N)=O)c(Nc4ccc([C@H](O)C(F)(F)F)cc4)n3)[C@@H](C#N)C2)C1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	"285667"	"UO_0000065"	"16.22"	"0.31"	"4.06"	"6.62"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3639983"	""	"0"	"366.43"	"0"	"2.34"	"BDBM147523"	"CNC(=O)c1ccc(Nc2nn([C@H]3CCCC[C@@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"285453"	"UO_0000065"	"22.26"	"0.41"	"5.81"	"6.48"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652336"	""	"0"	"421.57"	"0"	"2.13"	"BDBM113147"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCC[C@@](C)(O)C2)CC1"	"IC50"	"'='"	"40.9"	"nM"	"7.39"	""	"234590"	"UO_0000065"	"17.53"	"0.35"	"5.26"	"7.21"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3702894"	""	"0"	"324.39"	"0"	"2.68"	"BDBM147593"	"Cc1cncc(Nc2nn([C@H]3CCCC[C@@H]3C#N)cc2C(N)=O)c1"	"IC50"	"'='"	"37.0"	"nM"	"7.43"	""	"285523"	"UO_0000065"	"22.91"	"0.42"	"4.75"	"6.78"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699509"	""	"0"	"405.46"	"0"	"2.52"	"BDBM147527"	"CS(=O)(=O)c1ccc(Nc2nn(C3CCCC[C@@H]3C#N)cc2C(N)=O)cc1F"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	"285457"	"UO_0000065"	"19.73"	"0.39"	"5.48"	"6.11"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3648428"	""	"0"	"363.42"	"0"	"2.58"	"BDBM103731"	"O=C(Nc1nc2cccc(-c3ccc(N4CCOCC4)cc3)n2n1)C1CC1"	"IC50"	"'='"	"1760.0"	"nM"	"5.75"	""	"221716"	"UO_0000065"	"15.83"	"0.29"	"3.17"	"8.02"	"False"	"CHEMBL3707887"	"Inhibition Assay: In vitro inhibition assay using various enzyme."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638964"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3953929"	""	"0"	"308.39"	"0"	"3.86"	"BDBM197716"	"CCCCCC(CC#N)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"0.26"	"nM"	"9.59"	""	"351114"	"UO_0000065"	"31.08"	"0.57"	"5.73"	"11.52"	"False"	"CHEMBL3887743"	"Kinase Assay: The compounds of the invention were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Biochemistry 1999, 269, 94-104. The catalytic domains of human JAK1 (a.a. 837-1142), JAK2 (a.a. 828-1132) and JAK3 (a.a. 781-1124) with an N-terminal His tag were expressed using baculovirus in insect cells and purified. The catalytic activity of JAK1, JAK2 or JAK3 was assayed by measuring the phosphorylation of a biotinylated peptide. The phosphorylated peptide was detected by homogenous time resolved fluorescence (HTRF). IC50 was measured for each kinase in the 40 uL reactions that contain the enzyme, ATP and 500 nM peptide in 50 mM Tris (pH 7.8) buffer with 100 mM NaCl, 5 mM DTT, and 0.1 mg/mL (0.01%) BSA. The ATP concentration in the reactions was 90 uM for Jak1, 30 uM for Jak2 and 3 uM for Jak3. Reactions were carried out at room temperature for 1 hr and then stopped with 20 uL 45 mM EDTA."	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886433"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3919101"	""	"0"	"294.36"	"0"	"3.47"	"BDBM197717"	"CCCCC(CC#N)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"1.4"	"nM"	"8.85"	""	"351116"	"UO_0000065"	"30.08"	"0.55"	"5.38"	"10.64"	"False"	"CHEMBL3887743"	"Kinase Assay: The compounds of the invention were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Biochemistry 1999, 269, 94-104. The catalytic domains of human JAK1 (a.a. 837-1142), JAK2 (a.a. 828-1132) and JAK3 (a.a. 781-1124) with an N-terminal His tag were expressed using baculovirus in insect cells and purified. The catalytic activity of JAK1, JAK2 or JAK3 was assayed by measuring the phosphorylation of a biotinylated peptide. The phosphorylated peptide was detected by homogenous time resolved fluorescence (HTRF). IC50 was measured for each kinase in the 40 uL reactions that contain the enzyme, ATP and 500 nM peptide in 50 mM Tris (pH 7.8) buffer with 100 mM NaCl, 5 mM DTT, and 0.1 mg/mL (0.01%) BSA. The ATP concentration in the reactions was 90 uM for Jak1, 30 uM for Jak2 and 3 uM for Jak3. Reactions were carried out at room temperature for 1 hr and then stopped with 20 uL 45 mM EDTA."	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886433"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4649397"	""	"0"	"418.22"	"None"	"None"	"14p"	"C=CC(=O)Nc1cccc(Oc2nc(Nc3ccc4c(c3)COB4O)ncc2OC)c1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4610789"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using Ulight-Poly GT as substrate incubated for 2 hrs by Lanthascreen TR-FRET assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610007"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2020"	"None"	""
"CHEMBL3703064"	""	"0"	"490.53"	"0"	"3.90"	"BDBM147774"	"CC1(C)CN([C@H]2CC[C@H](n3cc(C(N)=O)c(Nc4ccc([C@H](O)C(F)(F)F)cc4)n3)[C@@H](C#N)C2)C1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"285708"	"UO_0000065"	"16.92"	"0.32"	"4.40"	"6.91"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703073"	""	"0"	"418.45"	"0"	"3.12"	"BDBM147785"	"CN(C)[C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(OC(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	"285719"	"UO_0000065"	"18.85"	"0.36"	"4.77"	"7.22"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL2062811"	""	"0"	"452.48"	"0"	"4.91"	"BDBM99567"	"CN1CCN(c2cccc(Nc3nc4c(-c5ccc(C(F)(F)F)cc5)cccn4n3)c2)CC1"	"IC50"	"'='"	"3.7"	"nM"	"8.43"	""	"216257"	"UO_0000065"	"18.63"	"0.35"	"3.52"	"17.31"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652305"	""	"0"	"416.55"	"0"	"2.52"	"BDBM113114"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC[C@H](CC#N)C2)CC1"	"IC50"	"'='"	"27.3"	"nM"	"7.56"	""	"234558"	"UO_0000065"	"18.16"	"0.36"	"5.04"	"7.14"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3652380"	""	"0"	"363.49"	"0"	"1.99"	"BDBM113191"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCC2)CC1"	"IC50"	"'='"	"39.4"	"nM"	"7.41"	""	"234634"	"UO_0000065"	"20.37"	"0.40"	"5.41"	"9.01"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3650682"	""	"0"	"367.41"	"0"	"2.33"	"BDBM148066"	"N#C[C@H]1CCC2(C[C@H]1n1cc(C(N)=O)c(Nc3ccccc3)n1)OCCO2"	"IC50"	"'='"	"308.0"	"nM"	"6.51"	""	"285988"	"UO_0000065"	"17.72"	"0.33"	"4.18"	"5.65"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647861"	""	"0"	"465.48"	"0"	"3.15"	"BDBM147971"	"CC(C)(c1ccc(Nc2nn([C@H]3CC[C@H](O)C[C@@H]3C#N)cc2C(N)=O)cc1)C(O)C(F)(F)F"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"285905"	"UO_0000065"	"18.69"	"0.36"	"5.55"	"6.34"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702974"	""	"0"	"470.48"	"0"	"2.47"	"BDBM147684"	"CN[C@H]1CCC(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"51.0"	"nM"	"7.29"	""	"285617"	"UO_0000065"	"15.50"	"0.31"	"4.82"	"5.10"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4577281"	""	"0"	"365.24"	"0"	"1.60"	"10l"	"C=CC(=O)N1CCC(Cn2nc(Br)c3c(N)ncnc32)CC1"	"IC50"	"'='"	"90.1"	"nM"	"7.04"	""	""	"UO_0000065"	"19.29"	"0.44"	"5.45"	"7.83"	"False"	"CHEMBL4402146"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-biotin as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4400567"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL3650999"	""	"0"	"368.37"	"0"	"3.46"	"BDBM153175"	"C=C(C)C(=O)Nc1cc(F)cc(-c2ncnc3[nH]cc(C(=O)OCC)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294123"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3658865"	""	"0"	"373.48"	"0"	"2.28"	"BDBM159784"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](CS(=O)(=O)[C@@H]2CC[C@@H](C#N)C2)C1"	"IC50"	"'='"	"801.0"	"nM"	"6.10"	""	"302594"	"UO_0000065"	"16.32"	"0.32"	"3.82"	"5.93"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3658099"	""	"0"	"600.64"	"2"	"6.60"	"BDBM148374"	"Cc1ccc(NC(=O)c2cccc(C(F)(F)F)c2)cc1N1CCc2nc(Nc3ccc(C(=O)N4CCCC4)cc3)ncc2C1"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	"286785"	"UO_0000065"	"13.08"	"0.24"	"1.25"	"8.68"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703021"	""	"0"	"372.86"	"0"	"2.83"	"BDBM147731"	"CN[C@@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"36.0"	"nM"	"7.44"	""	"285665"	"UO_0000065"	"19.96"	"0.39"	"4.61"	"6.84"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645097"	""	"0"	"443.56"	"0"	"3.85"	"BDBM99871"	"COc1cccc(CNc2cccn3nc(Nc4ccc(N5CCN(C)CC5)cc4)nc23)c1"	"IC50"	"'='"	"1339.32"	"nM"	"5.87"	""	"216539"	"UO_0000065"	"13.24"	"0.24"	"2.02"	"8.39"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647745"	""	"0"	"510.54"	"1"	"3.25"	"BDBM147848"	"N#C[C@H]1C[C@@H](NCC2CC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	"285782"	"UO_0000065"	"15.86"	"0.32"	"4.85"	"5.67"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3301607"	"FILGOTINIB"	"4"	"425.51"	"0"	"1.98"	"Filgotinib"	"O=C(Nc1nc2cccc(-c3ccc(CN4CCS(=O)(=O)CC4)cc3)n2n1)C1CC1"	"IC50"	"'='"	"167.34"	"nM"	"6.78"	""	"221712"	"UO_0000065"	"15.93"	"0.31"	"4.80"	"7.01"	"False"	"CHEMBL3707887"	"Inhibition Assay: In vitro inhibition assay using various enzyme."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638964"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642270"	""	"0"	"449.54"	"0"	"3.38"	"BDBM99531"	"CS(=O)(=O)c1cccc(-c2cccn3nc(Nc4cccc(N5CCOCC5)c4)nc23)c1"	"IC50"	"'='"	"5.6"	"nM"	"8.25"	""	"216223"	"UO_0000065"	"18.36"	"0.35"	"4.87"	"9.29"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL1439384"	""	"0"	"328.73"	"0"	"2.48"	"SID26727034"	"COc1ccc([N+](=O)[O-])c(S(=O)(=O)c2ccc(Cl)cc2)n1"	"IC50"	"'='"	"3261.0"	"nM"	"5.49"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1420155"	""	"0"	"389.46"	"0"	"3.57"	"SID862597"	"COc1cc2c(cc1OC)-c1cc(N3CCCc4ccccc43)nc(=O)n1CC2"	"IC50"	"'='"	"35640.0"	"nM"	"4.45"	""	"Not Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL53898"	""	"0"	"322.36"	"0"	"2.75"	"SID855540"	"N#C/C(=C\c1ccc(O)c(O)c1)C(=O)NCCCc1ccccc1"	"IC50"	"'='"	"6007.0"	"nM"	"5.22"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL3647777"	""	"0"	"448.49"	"0"	"4.37"	"BDBM147880"	"CC(C)(C)N[C@H]1CCC(n2cc(C(N)=O)c(Nc3ccc(C(F)(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"26.0"	"nM"	"7.58"	""	"285814"	"UO_0000065"	"16.91"	"0.32"	"3.22"	"6.97"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651000"	""	"0"	"362.39"	"0"	"2.88"	"BDBM153176"	"C=CC(=O)N1CCc2ccc(-c3ncnc4[nH]cc(C(=O)OCC)c34)cc21"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294124"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702903"	""	"0"	"470.60"	"0"	"3.59"	"BDBM147602"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)NC3CCCCC3)cc2)n1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"285532"	"UO_0000065"	"19.12"	"0.37"	"5.41"	"6.30"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645542"	""	"0"	"370.41"	"0"	"4.95"	"BDBM107126"	"COc1ccc(NC(=O)Nc2cccc(-c3cnc4ccccc4n3)c2)cc1"	"IC50"	"'>'"	"50000.0"	"nM"	""	""	"226363"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL1795071"	"RUXOLITINIB PHOSPHATE"	"4"	"404.37"	"0"	"3.47"	"GLPG0634"	"N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1.O=P(O)(O)O"	"IC50"	"'='"	"28.0"	"nM"	"7.55"	""	""	"UO_0000065"	"24.65"	"0.45"	"4.08"	"9.08"	"False"	"CHEMBL2155759"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2150873"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1382022"	""	"0"	"353.46"	"0"	"3.77"	"SID14721235"	"CCCOc1ccc(C(=O)C(CN2CCOCC2)c2ccccc2)cc1"	"IC50"	"'='"	"2460.0"	"nM"	"5.61"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1557820"	""	"0"	"346.83"	"0"	"3.47"	"SID3712447"	"Clc1ccc(-n2nnnc2Sc2ncnc3sccc23)cc1"	"IC50"	"'='"	"2906.0"	"nM"	"5.54"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1440303"	""	"0"	"301.78"	"0"	"1.72"	"SID24817132"	"CNC(=O)c1nnsc1[S+]([O-])c1ccc(Cl)cc1"	"IC50"	"'='"	"2259.0"	"nM"	"5.65"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1973122"	""	"0"	"316.81"	"0"	"3.42"	"SID24835936"	"O=C(CCl)/N=c1\sccn1Cc1cccc2ccccc12"	"IC50"	"'='"	"1036.0"	"nM"	"5.99"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1597039"	""	"0"	"305.83"	"0"	"4.63"	"SID22404308"	"Cc1ccc(C)c(Sc2ccc(NC(=O)CCl)cc2)c1"	"IC50"	"'='"	"7255.0"	"nM"	"5.14"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL3193887"	""	"0"	"409.31"	"0"	"3.72"	"SID14746711"	"Cc1cc(SCC(=O)N/N=C/c2ccc(O)c(O)c2)c(C)cc1Br"	"IC50"	"'='"	"10670.0"	"nM"	"4.97"	""	"Not Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1305275"	""	"0"	"270.76"	"0"	"2.02"	"SID22402056"	"O=C(CCl)NC(=O)NC12CC3CC(CC(C3)C1)C2"	"IC50"	"'='"	"4373.0"	"nM"	"5.36"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1454438"	""	"0"	"339.44"	"0"	"3.23"	"SID4264510"	"COc1ccc(OC)c(NS(=O)(=O)c2ccc(SC)cc2)c1"	"IC50"	"'='"	"12440.0"	"nM"	"4.91"	""	"Not Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1599132"	""	"0"	"311.36"	"0"	"4.01"	"SID17413899"	"Cc1nc(O)c(C(=O)/C=C/c2ccccc2F)c2c1CCCC2"	"IC50"	"'='"	"5185.0"	"nM"	"5.29"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1482285"	""	"0"	"275.31"	"0"	"2.99"	"SID22413683"	"COc1ccc(-c2cnc3c(c2)CCC3(C#N)C#N)cc1"	"IC50"	"'='"	"2067.0"	"nM"	"5.68"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1306583"	""	"0"	"473.23"	"0"	"4.43"	"SID24817911"	"Br.CCCCn1c(=N)n(CC(=O)c2ccc(Br)s2)c2ccccc21"	"IC50"	"'='"	"4365.0"	"nM"	"5.36"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1443757"	""	"0"	"355.44"	"0"	"1.48"	"SID849452"	"CCCn1c(CN(C)Cc2ccccc2)nc2c1c(=O)n(C)c(=O)n2C"	"IC50"	"'='"	"8174.0"	"nM"	"5.09"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1505902"	""	"0"	"240.65"	"0"	"-0.01"	"SID22413972"	"Cc1nc2c(=O)n(C)c(=O)n(C)c2nc1Cl"	"IC50"	"'='"	"4555.0"	"nM"	"5.34"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1613090"	""	"0"	"271.32"	"0"	"3.03"	"SID4259495"	"Cc1cccc(OCC(=O)Nc2cc(C)ccc2O)c1"	"IC50"	"'>'"	"40000.0"	"nM"	""	""	"Not Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL3647744"	""	"0"	"566.53"	"1"	"4.14"	"BDBM147847"	"CN(CCC(F)(F)F)[C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"31.0"	"nM"	"7.51"	""	"285781"	"UO_0000065"	"13.25"	"0.27"	"3.37"	"5.60"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3622149"	""	"0"	"432.53"	"0"	"3.50"	"13"	"CCn1c(C(=O)N(C2CC2)C2CC2)cc2c3c(ncn3C)c(Nc3cc(C)nn3C)nc21"	"IC50"	"'='"	"230.0"	"nM"	"6.64"	""	""	"UO_0000065"	"15.35"	"0.28"	"3.14"	"7.74"	"False"	"CHEMBL3625512"	"Inhibition of recombinant JAK2 (unknown origin) using 5-FAM-KKKKEEIYFFFG-OH substrate and ATP incubated for 180 mins by scintillation counting method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621135"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3622143"	""	"0"	"492.61"	"0"	"3.58"	"5"	"CCn1c(C(=O)N(C2CC2)C2CC2)cc2c3c(ncn3C)c(Nc3nc(C)c(C(=O)NC)s3)nc21"	"IC50"	"'='"	"0.9"	"nM"	"9.05"	""	""	"UO_0000065"	"18.36"	"0.35"	"5.47"	"8.23"	"False"	"CHEMBL3625512"	"Inhibition of recombinant JAK2 (unknown origin) using 5-FAM-KKKKEEIYFFFG-OH substrate and ATP incubated for 180 mins by scintillation counting method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621135"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3745885"	""	"0"	"467.46"	"0"	"3.66"	"7ao; ON1231320"	"Cn1c(=O)c(S(=O)(=O)c2ccc(F)cc2F)cc2cnc(Nc3ccc4[nH]ccc4c3)nc21"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3748225"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3745707"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2016"	"None"	""
"CHEMBL3642250"	""	"0"	"509.61"	"2"	"5.36"	"BDBM2013"	"Cn1ncc2c(-c3cccn4nc(Nc5ccc6c(c5)CCN(C(=O)OC(C)(C)C)CC6)nc34)cccc21"	"IC50"	"'='"	"16.51"	"nM"	"7.78"	""	"3039"	"UO_0000065"	"15.27"	"0.28"	"2.42"	"8.69"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703058"	""	"0"	"462.48"	"0"	"3.26"	"BDBM147768"	"N#C[C@H]1C[C@@H](N2CCC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc([C@@H](O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	"285702"	"UO_0000065"	"17.05"	"0.33"	"4.63"	"6.56"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642281"	""	"0"	"463.56"	"0"	"3.38"	"BDBM99545"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4ccc(CN5CCOCC5)cc4)nc23)cc1"	"IC50"	"'='"	"2.2"	"nM"	"8.66"	""	"216237"	"UO_0000065"	"18.68"	"0.36"	"5.28"	"9.75"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652290"	""	"0"	"511.71"	"1"	"2.82"	"BDBM113099"	"CCCS(=O)(=O)CC1CCCN(S(=O)(=O)C[C@H]2CC[C@H](N(C)c3ncnc4[nH]ccc34)CC2)C1"	"IC50"	"'='"	"54.7"	"nM"	"7.26"	""	"234543"	"UO_0000065"	"14.19"	"0.29"	"4.44"	"6.24"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3658103"	""	"0"	"587.61"	"2"	"5.65"	"BDBM148392"	"Cc1ccc(NC(=O)c2cccc(C(F)(F)F)c2)cc1N1CCc2nc(Nc3ccc(C(=O)NC4CC4)nc3)ncc2C1"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	"286789"	"UO_0000065"	"13.18"	"0.25"	"2.09"	"6.91"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642413"	""	"0"	"515.64"	"1"	"3.02"	"BDBM99691"	"CN1CCN(c2cccc(Nc3nc4c(C#Cc5ccccc5N(C)S(C)(=O)=O)cccn4n3)c2)CC1"	"IC50"	"'='"	"23.89"	"nM"	"7.62"	""	"216380"	"UO_0000065"	"14.78"	"0.28"	"4.60"	"8.85"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642390"	""	"0"	"520.66"	"1"	"3.23"	"BDBM99668"	"CN1CCN(c2ccc(Nc3nc4c(NCc5cccc(N(C)S(C)(=O)=O)c5)cccn4n3)cc2)CC1"	"IC50"	"'='"	"144.8"	"nM"	"6.84"	""	"216358"	"UO_0000065"	"13.14"	"0.25"	"3.61"	"6.97"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3665138"	""	"0"	"350.43"	"0"	"2.83"	"BDBM112525"	"CCCC(=O)N1CC[C@@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.1214"	"nM"	"9.92"	""	"233764"	"UO_0000065"	"28.30"	"0.52"	"7.09"	"11.42"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3658119"	""	"0"	"630.68"	"2"	"5.15"	"BDBM148436"	"Cc1ccc(NC(=O)c2cc(C(F)(F)F)ccn2)cc1N1CCc2nc(Nc3ccc(C(=O)N4CCN(C)CC4)cc3)ncc2C1"	"IC50"	"'='"	"5.3"	"nM"	"8.28"	""	"286803"	"UO_0000065"	"13.12"	"0.25"	"3.13"	"7.76"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642276"	""	"0"	"462.58"	"0"	"3.30"	"BDBM99539"	"CN1CCN(c2ccc(Nc3nc4ccc(-c5ccc(S(C)(=O)=O)cc5)cn4n3)cc2)CC1"	"IC50"	"'='"	"2973.1"	"nM"	"5.53"	""	"216231"	"UO_0000065"	"11.95"	"0.23"	"2.23"	"6.67"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3658088"	""	"0"	"615.66"	"2"	"5.75"	"BDBM148321"	"Cc1ccc(NC(=O)c2cccc(C(F)(F)F)c2)cc1N1CCc2nc(Nc3ccc(N4CCN(C)CC4)cc3)ncc2C1=O"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	"286814"	"UO_0000065"	"12.71"	"0.24"	"2.07"	"8.35"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702919"	""	"0"	"446.53"	"0"	"1.91"	"BDBM147618"	"COCCNS(=O)(=O)c1ccc(Nc2nn([C@H]3CCCC[C@@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"285548"	"UO_0000065"	"20.16"	"0.40"	"7.09"	"5.92"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702944"	""	"0"	"437.42"	"0"	"2.72"	"BDBM147646"	"C[C@](O)(c1ccc(Nc2nn([C@H]3CC[C@@H](O)C[C@@H]3C#N)cc2C(N)=O)cc1)C(F)(F)F"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"285578"	"UO_0000065"	"19.20"	"0.37"	"5.68"	"6.12"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651053"	""	"0"	"360.42"	"0"	"3.94"	"BDBM153230"	"C=C(C)C(=O)Nc1cccc(-c2ncnc3[nH]cc(C4=CCOCC4)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294178"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703088"	""	"0"	"446.48"	"0"	"3.93"	"BDBM147802"	"CC1CN([C@H]2CC[C@H](n3cc(C(N)=O)c(Nc4ccc(C(F)(F)F)cc4)n3)[C@@H](C#N)C2)C1"	"IC50"	"'='"	"61.0"	"nM"	"7.21"	""	"285736"	"UO_0000065"	"16.16"	"0.31"	"3.28"	"7.22"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4635334"	""	"0"	"387.42"	"0"	"0.65"	"11"	"O=C(N[C@]12C[C@H]1CN(c1nc(Nc3cnn(CCO)c3)ncc1F)C2)C1CC1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4620433"	"Inhibition of human recombinant JAK2 assessed as level of phosphorylation in presence of peptide substrate FITC-KGGEEEEYFELVKK and ATP by mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4619733"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2020"	"None"	""
"CHEMBL1431684"	""	"0"	"374.19"	"0"	"3.90"	"SID14737082"	"Cc1nc([N+](=O)[O-])c(Br)n1CC(=O)c1ccc2ccccc2c1"	"IC50"	"'='"	"3676.0"	"nM"	"5.43"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL493657"	""	"0"	"556.46"	"1"	"2.59"	"29"	"O=C1Nc2cc(Br)ccc2/C1=C1/Nc2ccccc2/C1=N\OCCN1CCN(CCOCCO)CC1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4042012"	"Inhibition of recombinant JAK2 (unknown origin) after 120 mins in presence of [33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4041496"	"1"	"Scientific Literature"	"J Nat Prod"	"2016"	"None"	""
"CHEMBL3652287"	""	"0"	"407.54"	"0"	"1.74"	"BDBM113140"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCC[C@H](O)C2)CC1"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	"234583"	"UO_0000065"	"19.00"	"0.38"	"6.00"	"7.56"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3647782"	""	"0"	"440.98"	"0"	"4.39"	"BDBM147885"	"CC(C)(N[C@@H]1CCC(n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@@H](C#N)C1)C1CC1"	"IC50"	"'='"	"208.0"	"nM"	"6.68"	""	"285819"	"UO_0000065"	"15.15"	"0.29"	"2.29"	"6.14"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652277"	""	"0"	"435.59"	"0"	"2.78"	"BDBM113085"	"CCOC1CCCN(S(=O)(=O)CC2CCC(N(C)c3ncnc4[nH]ccc34)CC2)C1"	"IC50"	"'='"	"4.09"	"nM"	"8.39"	""	"234529"	"UO_0000065"	"19.26"	"0.38"	"5.61"	"9.18"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL1537091"	""	"0"	"294.38"	"0"	"3.21"	"BDBM67663"	"CNC(=S)Nc1cccc(-c2cnc3ccccc3n2)c1"	"IC50"	"'='"	"25500.0"	"nM"	"4.59"	""	"226364"	"UO_0000065"	"15.60"	"0.30"	"1.38"	"9.22"	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652350"	""	"0"	"465.62"	"0"	"1.60"	"BDBM113161"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2C[C@@](C)(CO)[C@@](C)(CO)C2)CC1"	"IC50"	"'='"	"55.6"	"nM"	"7.25"	""	"234604"	"UO_0000065"	"15.58"	"0.31"	"5.65"	"5.92"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3655084"	""	"0"	"374.47"	"0"	"1.54"	"BDBM159751"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)[C@H]2C[C@@H](CC#N)C2)C1"	"IC50"	"'='"	"1400.0"	"nM"	"5.85"	""	"302561"	"UO_0000065"	"15.63"	"0.31"	"4.31"	"5.10"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3639439"	""	"0"	"549.62"	"2"	"7.20"	"BDBM99823"	"COc1cc(C(F)F)ccc1-c1cccn2nc(Nc3ccc(C4CCN(C(=O)OC(C)(C)C)CC4)cc3)nc12"	"IC50"	"'='"	"1411.38"	"nM"	"5.85"	""	"216496"	"UO_0000065"	"10.64"	"0.20"	"-1.35"	"7.22"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3648431"	""	"0"	"309.39"	"0"	"3.60"	"BDBM107140"	"CSCC(=O)Nc1cccc(-c2cnc3ccccc3n2)c1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	"226378"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647728"	""	"0"	"512.51"	"1"	"1.93"	"BDBM147830"	"N#C[C@H]1C[C@@H](N2CC(O)C2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"285764"	"UO_0000065"	"17.56"	"0.35"	"7.07"	"5.83"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645013"	""	"0"	"558.71"	"2"	"6.70"	"BDBM99765"	"CC(=O)Nc1ccc(Sc2cccn3nc(Nc4ccc(C5CCN(C(=O)OC(C)(C)C)CC5)cc4)nc23)cc1"	"IC50"	"'='"	"9999.0"	"nM"	"5.00"	""	"216452"	"UO_0000065"	"8.95"	"0.17"	"-1.70"	"4.96"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3676093"	""	"0"	"433.45"	"0"	"2.56"	"BDBM127858"	"Cn1cc(F)cc([C@H]2CCCN2c2ccn3ncc(C(=O)Nc4cccnc4)c3n2)c1=O"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258523"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3665120"	""	"0"	"322.37"	"0"	"2.05"	"BDBM112507"	"CC(=O)N1CC[C@@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.0926"	"nM"	"10.03"	""	"233746"	"UO_0000065"	"31.12"	"0.57"	"7.98"	"11.56"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3675976"	""	"0"	"394.45"	"0"	"3.28"	"BDBM127729"	"CC1(NC(=O)c2cnn3ccc(N4CCCC4c4cncc(F)c4)nc23)CCC1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258403"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675990"	""	"0"	"384.42"	"0"	"1.72"	"BDBM127743"	"C[C@@H](CO)NC(=O)c1cnn2ccc(N3CCCC3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258417"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676006"	""	"0"	"398.44"	"0"	"2.11"	"BDBM127759"	"CC(C)(CO)NC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258433"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676019"	""	"0"	"414.44"	"0"	"1.73"	"BDBM127775"	"COc1ncc(F)cc1[C@H]1CCCN1c1ccn2ncc(C(=O)NCCCO)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258446"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676022"	""	"0"	"428.47"	"0"	"2.12"	"BDBM127778"	"COc1ncc(F)cc1[C@H]1CCCN1c1ccn2ncc(C(=O)NCCCCO)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258449"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676028"	""	"0"	"414.44"	"0"	"1.72"	"BDBM127784"	"COc1ncc(F)cc1[C@H]1CCCN1c1ccn2ncc(C(=O)NC[C@@H](C)O)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258455"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676050"	""	"0"	"394.45"	"0"	"3.06"	"BDBM127809"	"CCc1ncc(F)cc1[C@H]1CCCN1c1ccn2ncc(C(=O)NC3CC3)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258478"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL2062813"	""	"0"	"460.52"	"0"	"4.14"	"BDBM50389203"	"CN1CCN(c2cccc(Nc3nc4c(-c5ccc(P(C)(C)=O)cc5)cccn4n3)c2)CC1"	"IC50"	"'='"	"1.73"	"nM"	"8.76"	""	"216386"	"UO_0000065"	"19.03"	"0.36"	"4.62"	"13.32"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3645081"	""	"0"	"513.57"	"1"	"3.88"	"BDBM99851"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4ccc5c(c4)CCNCC5)nc23)c(OCC(F)F)c1"	"IC50"	"'='"	"61.87"	"nM"	"7.21"	""	"216523"	"UO_0000065"	"14.04"	"0.27"	"3.33"	"7.38"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647918"	""	"0"	"366.43"	"0"	"3.11"	"BDBM148030"	"[C-]#[N+][C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(/C=N/OC)cc2)n1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"285967"	"UO_0000065"	"23.74"	"0.44"	"5.59"	"8.80"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642265"	""	"0"	"316.36"	"0"	"4.15"	"BDBM99524"	"COc1ccccc1Nc1nc2c(-c3ccccc3)cccn2n1"	"IC50"	"'='"	"9999.0"	"nM"	"5.00"	""	"216216"	"UO_0000065"	"15.80"	"0.28"	"0.85"	"9.72"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3694589"	""	"0"	"380.88"	"0"	"4.85"	"BDBM125910"	"Clc1cnc2nc1NCCCc1cccc(c1)OCCc1cccc(c1)N2"	"IC50"	"'='"	"25.0"	"nM"	"7.60"	""	"255683"	"UO_0000065"	"19.96"	"0.38"	"2.75"	"12.87"	"False"	"CHEMBL3707544"	"In Vitro Kinase Assay: One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Biochemistry 1999, 269, 94-104. The catalytic domains of human JAK1 (a.a. 837-1142), JAK2 (a.a. 828-1132) and JAK3 (a.a. 781-1124) with an N-terminal His tag were expressed using baculovirus in insect cells and purified. The catalytic activity of JAK1, JAK2 or JAK3 was assayed by measuring the phosphorylation of a biotinylated peptide. The phosphorylated peptide was detected by homogenous time resolved fluorescence (HTRF). IC50s of compounds were measured for each kinase in the reactions that contain the enzyme, ATP and 500 nM peptide in 50 mM Tris (pH 7.8) buffer with 100 mM NaCl, 5 mM DTT, and 0.1 mg/mL (0.01%) BSA. The ATP concentration in the reactions was 90 uM for JAK1, 30 uM for JAK2 and 3 uM for JAK3. Reactions were carried out at room temperature for 1 hr and then stopped with 20 uL 45 mM EDTA."	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639093"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3647762"	""	"0"	"420.44"	"0"	"3.54"	"BDBM147865"	"CN(C)[C@@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(C(F)(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"21.0"	"nM"	"7.68"	""	"285799"	"UO_0000065"	"18.26"	"0.35"	"4.14"	"7.68"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4087655"	""	"0"	"391.52"	"0"	"3.73"	"8"	"Cc1cccc(-c2cc3c(N[C@@H]4CC[C@](C)(N)C4(C)C)c(C(N)=O)cnn3c2)c1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4054822"	"Inhibition of GST-tagged JAK2 (unknown origin) after 3 hrs by Caliper assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4052645"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4078773"	""	"0"	"407.52"	"0"	"3.43"	"12"	"COc1ccc(-c2cc3c(N[C@@H]4CC[C@](C)(N)C4(C)C)c(C(N)=O)cnn3c2)cc1"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4054822"	"Inhibition of GST-tagged JAK2 (unknown origin) after 3 hrs by Caliper assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4052645"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4076191"	""	"0"	"395.48"	"0"	"3.56"	"13"	"CC1(C)[C@H](Nc2c(C(N)=O)cnn3cc(-c4ccccc4F)cc23)CC[C@]1(C)N"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4054822"	"Inhibition of GST-tagged JAK2 (unknown origin) after 3 hrs by Caliper assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4052645"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4070687"	""	"0"	"402.50"	"0"	"3.29"	"20"	"CC1(C)[C@H](Nc2c(C(N)=O)cnn3cc(-c4cccc(C#N)c4)cc23)CC[C@]1(C)N"	"IC50"	"'='"	"47.0"	"nM"	"7.33"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4054822"	"Inhibition of GST-tagged JAK2 (unknown origin) after 3 hrs by Caliper assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4052645"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4089164"	""	"0"	"379.47"	"0"	"2.21"	"24"	"CC1(C)[C@H](Nc2c(C(N)=O)cnn3cc(-c4cncnc4)cc23)CC[C@]1(C)N"	"IC50"	"'='"	"160.0"	"nM"	"6.80"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4054822"	"Inhibition of GST-tagged JAK2 (unknown origin) after 3 hrs by Caliper assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4052645"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4098840"	""	"0"	"396.47"	"0"	"2.95"	"34"	"CC1(C)[C@H](Nc2c(C(N)=O)cnn3cc(-c4ccc(F)nc4)cc23)CC[C@]1(C)N"	"IC50"	"'='"	"19.0"	"nM"	"7.72"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4054822"	"Inhibition of GST-tagged JAK2 (unknown origin) after 3 hrs by Caliper assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4052645"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4442778"	""	"0"	"380.41"	"0"	"0.97"	"11l"	"C=CC(=O)N1CCCC(n2nc(-c3cc(C=O)n(C)n3)c3c(N)ncnc32)C1"	"IC50"	"'='"	"11.5"	"nM"	"7.94"	""	""	"UO_0000065"	"20.87"	"0.39"	"6.97"	"6.36"	"False"	"CHEMBL4402146"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-biotin as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4400567"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4454392"	""	"0"	"410.48"	"0"	"1.39"	"11g"	"C=CC(=O)N1CCCC(n2nc(-c3cc(C(C)(C)O)n(C)n3)c3c(N)ncnc32)C1"	"IC50"	"'='"	"6.5"	"nM"	"8.19"	""	""	"UO_0000065"	"19.95"	"0.37"	"6.80"	"6.40"	"False"	"CHEMBL4402146"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-biotin as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4400567"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"Tofacitinib"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"4.3"	"nM"	"8.37"	""	""	"UO_0000065"	"26.78"	"0.50"	"6.83"	"9.41"	"False"	"CHEMBL4402146"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-biotin as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4400567"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4062471"	""	"0"	"472.53"	"0"	"3.06"	"13g"	"NC(=O)c1cnn2cccc2c1NCc1cccc(NC(=O)Cn2sc3ccccc3c2=O)c1"	"IC50"	"'='"	"745.0"	"nM"	"6.13"	""	""	"UO_0000065"	"12.97"	"0.25"	"3.07"	"4.96"	"False"	"CHEMBL4047228"	"Inhibition of GST-tagged JAK2 (unknown origin) using fluoresceinated peptide as substrate after 3 hrs by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4043231"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4789639"	""	"0"	"439.47"	"0"	"3.14"	"7; BMS-986202"	"[2H]C([2H])([2H])NC(=O)c1cnc(NC(=O)C2CC2)cc1Nc1cccc(-c2ncc(F)cn2)c1OC"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	""	""	""	""	""	"False"	"CHEMBL4775582"	"Inhibition of JAK2 (unknown origin) by EPO-stimulated cell based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4765480"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	""
"CHEMBL4463215"	""	"0"	"354.35"	"0"	"1.92"	"4"	"O=c1[nH]c2cnc(-c3cnc4ccc(F)cn34)nc2n1C1CCOCC1"	"IC50"	"'='"	"83.0"	"nM"	"7.08"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4574559"	""	"0"	"382.40"	"0"	"2.70"	"14"	"CC1(C)CC(n2c(=O)[nH]c3cnc(-c4cnc5ccc(F)cn45)nc32)CCO1"	"IC50"	"'='"	"4.8"	"nM"	"8.32"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4556988"	""	"0"	"390.40"	"0"	"1.97"	"27"	"O=c1[nH]cccc1Nc1ncc2[nH]c(=O)n([C@@H]3CC[C@@H](O)c4ccccc43)c2n1"	"IC50"	"'='"	"4.3"	"nM"	"8.37"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL3116059"	""	"0"	"394.41"	"0"	"3.22"	"13b, enantiomeric mixture"	"COc1ccc2nc(NC(C)c3ncc(F)cn3)nc(Nc3cn(C)cn3)c2c1"	"IC50"	"'='"	"670.0"	"nM"	"6.17"	""	""	"UO_0000065"	"15.65"	"0.29"	"2.95"	"6.01"	"False"	"CHEMBL3118240"	"Inhibition of Jak2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112447"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL3335696"	""	"0"	"460.56"	"0"	"1.43"	"25"	"CC[C@H](CO)Nc1ncc(-c2cnc3[nH]ccc3n2)c(N[C@H]2CCCN(S(C)(=O)=O)C2)n1"	"IC50"	"'='"	"54.0"	"nM"	"7.27"	""	""	"UO_0000065"	"15.78"	"0.31"	"5.84"	"4.88"	"False"	"CHEMBL3374010"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 1 hr in presence of [gamma-33P]ATP by scintillation counting analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351377"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3301607"	"FILGOTINIB"	"4"	"425.51"	"0"	"1.98"	"65, GLPG0634"	"O=C(Nc1nc2cccc(-c3ccc(CN4CCS(=O)(=O)CC4)cc3)n2n1)C1CC1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3382733"	"Inhibition of JAK2 in EPO-induced human UT7-EPO cells assessed as pSTAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"UT7-EPO"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351789"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"1"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"740.0"	"nM"	"6.13"	""	""	"UO_0000065"	"19.63"	"0.36"	"4.59"	"6.90"	"False"	"CHEMBL3382736"	"Inhibition of JAK2 in human whole blood assessed as inhibition of GM-CSF-induced pSTAT5"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"CHEMBL3638178"	"Blood"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351789"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL4537678"	""	"0"	"380.38"	"0"	"2.56"	"5"	"CNC(=O)c1cnc(Nc2ccc(F)cn2)cc1Nc1ccccc1C(N)=O"	"IC50"	"'>'"	"2000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4414788"	"Inhibition of JAK2 JH1 domain (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414548"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4561663"	""	"0"	"366.36"	"0"	"2.30"	"4"	"NC(=O)c1ccccc1Nc1cc(Nc2ccc(F)cn2)ncc1C(N)=O"	"IC50"	"'='"	"24.0"	"nM"	"7.62"	""	""	"UO_0000065"	"20.80"	"0.39"	"5.32"	"5.60"	"False"	"CHEMBL4414788"	"Inhibition of JAK2 JH1 domain (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414548"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4093813"	""	"0"	"401.47"	"0"	"3.79"	"19"	"CCc1cc(O)ccc1-c1ccc2c(-c3nc4c([nH]3)CN(C(C)=O)CC4)n[nH]c2c1"	"IC50"	"'='"	"3.3"	"nM"	"8.48"	""	""	"UO_0000065"	"21.13"	"0.39"	"4.69"	"8.66"	"False"	"CHEMBL4003453"	"Inhibition of GST tagged human recombinant JAK2 catalytic domain expressed in baculovirus using peptide substrate preincubated for 60 mins followed by substrate addition and measured after 60 mins by microfluidic assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4002590"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL2208023"	""	"0"	"304.35"	"0"	"3.85"	"6c"	"CC(=O)Nc1ccc(-c2ccnc(Nc3ccccc3)n2)cc1"	"IC50"	"'='"	"1971.0"	"nM"	"5.71"	""	""	"UO_0000065"	"18.75"	"0.34"	"1.86"	"8.53"	"False"	"CHEMBL2214784"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT3 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL2207760"	""	"0"	"472.59"	"0"	"4.15"	"10h"	"CCN1CCC[C@@H]1C(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"1431.3"	"nM"	"5.84"	""	""	"UO_0000065"	"12.37"	"0.23"	"1.69"	"7.07"	"False"	"CHEMBL2214785"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT1 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL247468"	""	"0"	"512.66"	"1"	"4.35"	"27"	"c1ccc(-c2c(-c3ccc(OCCN4CCCC4)cc3)oc3ncnc(NCCN4CCNCC4)c23)cc1"	"IC50"	"'>'"	"8333.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL886500"	"Inhibition of Jak2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139142"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2007"	"None"	""
"CHEMBL1650697"	""	"0"	"332.32"	"0"	"2.49"	"9c"	"Cc1cc(Nc2nc(N[C@@H](C)c3ncc(F)cn3)ncc2F)n[nH]1"	"IC50"	"'<'"	"3.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1656588"	"Inhibition of JAK2 using Km ATP concentration"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1650732"	""	"0"	"399.43"	"0"	"2.19"	"16a"	"Cc1cc(Nc2cc(N3CCOCC3)nc(N[C@@H](C)c3ncc(F)cn3)n2)n[nH]1"	"IC50"	"'<'"	"3.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1656588"	"Inhibition of JAK2 using Km ATP concentration"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1650734"	""	"0"	"433.88"	"0"	"2.84"	"16c"	"Cc1cc(Nc2nc(N[C@@H](C)c3ncc(F)cn3)nc(N3CCOCC3)c2Cl)n[nH]1"	"IC50"	"'<'"	"3.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1656588"	"Inhibition of JAK2 using Km ATP concentration"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1650697"	""	"0"	"332.32"	"0"	"2.49"	"9c"	"Cc1cc(Nc2nc(N[C@@H](C)c3ncc(F)cn3)ncc2F)n[nH]1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	""	"UO_0000065"	"24.98"	"0.47"	"5.81"	"7.96"	"False"	"CHEMBL1656589"	"Inhibition of JAK2 using 5 mM of ATP"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1650698"	""	"0"	"358.36"	"0"	"3.06"	"9d"	"C[C@H](Nc1ncc(F)c(Nc2cc(C3CC3)[nH]n2)n1)c1ncc(F)cn1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1656589"	"Inhibition of JAK2 using 5 mM of ATP"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1650729"	""	"0"	"393.22"	"0"	"3.12"	"9j"	"Cc1cc(Nc2nc(N[C@@H](C)c3ncc(F)cn3)ncc2Br)n[nH]1"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	""	"UO_0000065"	"20.34"	"0.46"	"4.88"	"7.67"	"False"	"CHEMBL1656589"	"Inhibition of JAK2 using 5 mM of ATP"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL3797300"	""	"0"	"406.49"	"0"	"2.42"	"15a"	"CC(=O)Nc1ccc(-c2ncnc3c2cc(C(=O)NCCN2CCCC2)n3C)cc1"	"IC50"	"'='"	"4300.0"	"nM"	"5.37"	""	""	"UO_0000065"	"13.20"	"0.24"	"2.95"	"5.82"	"False"	"CHEMBL3802364"	"Inhibition of JAK2 in GMCSF-stimulated human TF1 cells assessed as suppression of STAT5 phosphorylation preincubated for 2 hrs followed by GMCSF stimulation for 50 mins by FACS reader analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"CHEMBL3307972"	""
"CHEMBL3799882"	""	"0"	"448.57"	"0"	"3.45"	"15c"	"Cn1c(C(=O)NCCN2CCCC2)cc2c(-c3ccc(NC(=O)C(C)(C)C)cc3)ncnc21"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	""	"UO_0000065"	"18.05"	"0.34"	"4.65"	"8.79"	"False"	"CHEMBL3802363"	"Inhibition of recombinant human GST-tagged JAK2 expressed in baculovirus expression system using Z'-LYTE Try6 peptide as substrate incubated for 1 hr by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3797514"	""	"0"	"555.64"	"2"	"5.33"	"12e"	"Cn1c(C(=O)OCc2ccccc2)cc2c(-c3ccc(NC(=O)[C@@H]4CCCN4C(=O)OC(C)(C)C)cc3)ncnc21"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3802363"	"Inhibition of recombinant human GST-tagged JAK2 expressed in baculovirus expression system using Z'-LYTE Try6 peptide as substrate incubated for 1 hr by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3800009"	""	"0"	"420.52"	"0"	"2.81"	"15b"	"CCC(=O)Nc1ccc(-c2ncnc3c2cc(C(=O)NCCN2CCCC2)n3C)cc1"	"IC50"	"'='"	"2900.0"	"nM"	"5.54"	""	""	"UO_0000065"	"13.17"	"0.24"	"2.73"	"6.01"	"False"	"CHEMBL3802364"	"Inhibition of JAK2 in GMCSF-stimulated human TF1 cells assessed as suppression of STAT5 phosphorylation preincubated for 2 hrs followed by GMCSF stimulation for 50 mins by FACS reader analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"CHEMBL3307972"	""
"CHEMBL3797831"	""	"0"	"561.69"	"1"	"3.80"	"15e"	"Cn1c(C(=O)NCCN2CCCC2)cc2c(-c3ccc(NC(=O)[C@@H]4CCCN4C(=O)OC(C)(C)C)cc3)ncnc21"	"IC50"	"'='"	"520.0"	"nM"	"6.28"	""	""	"UO_0000065"	"11.19"	"0.21"	"2.48"	"5.16"	"False"	"CHEMBL3802364"	"Inhibition of JAK2 in GMCSF-stimulated human TF1 cells assessed as suppression of STAT5 phosphorylation preincubated for 2 hrs followed by GMCSF stimulation for 50 mins by FACS reader analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"CHEMBL3307972"	""
"CHEMBL3797514"	""	"0"	"555.64"	"2"	"5.33"	"12e"	"Cn1c(C(=O)OCc2ccccc2)cc2c(-c3ccc(NC(=O)[C@@H]4CCCN4C(=O)OC(C)(C)C)cc3)ncnc21"	"IC50"	"'>'"	"20000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3802364"	"Inhibition of JAK2 in GMCSF-stimulated human TF1 cells assessed as suppression of STAT5 phosphorylation preincubated for 2 hrs followed by GMCSF stimulation for 50 mins by FACS reader analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"CHEMBL3307972"	""
"CHEMBL3798740"	""	"0"	"414.47"	"0"	"4.34"	"12b"	"CCC(=O)Nc1ccc(-c2ncnc3c2cc(C(=O)OCc2ccccc2)n3C)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL3802364"	"Inhibition of JAK2 in GMCSF-stimulated human TF1 cells assessed as suppression of STAT5 phosphorylation preincubated for 2 hrs followed by GMCSF stimulation for 50 mins by FACS reader analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"CHEMBL3307972"	""
"CHEMBL3797831"	""	"0"	"561.69"	"1"	"3.80"	"15e"	"Cn1c(C(=O)NCCN2CCCC2)cc2c(-c3ccc(NC(=O)[C@@H]4CCCN4C(=O)OC(C)(C)C)cc3)ncnc21"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	""	"UO_0000065"	"14.32"	"0.27"	"4.25"	"6.61"	"False"	"CHEMBL3802363"	"Inhibition of recombinant human GST-tagged JAK2 expressed in baculovirus expression system using Z'-LYTE Try6 peptide as substrate incubated for 1 hr by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3800186"	""	"0"	"351.41"	"0"	"2.72"	"14c"	"Cn1c(C(N)=O)cc2c(-c3ccc(NC(=O)C(C)(C)C)cc3)ncnc21"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	""	"UO_0000065"	"21.91"	"0.40"	"4.98"	"7.48"	"False"	"CHEMBL3802363"	"Inhibition of recombinant human GST-tagged JAK2 expressed in baculovirus expression system using Z'-LYTE Try6 peptide as substrate incubated for 1 hr by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3800434"	""	"0"	"396.41"	"0"	"2.86"	"14g"	"Cn1c(C(N)=O)cc2c(-c3ccc(NC(=O)c4ccc(C#N)cc4)cc3)ncnc21"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL3802364"	"Inhibition of JAK2 in GMCSF-stimulated human TF1 cells assessed as suppression of STAT5 phosphorylation preincubated for 2 hrs followed by GMCSF stimulation for 50 mins by FACS reader analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"CHEMBL3307972"	""
"CHEMBL3798618"	""	"0"	"591.71"	"1"	"3.43"	"16e"	"Cn1c(C(=O)NCCCN2CCOCC2)cc2c(-c3ccc(NC(=O)[C@@H]4CCCN4C(=O)OC(C)(C)C)cc3)ncnc21"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	""	"UO_0000065"	"13.52"	"0.25"	"4.57"	"6.11"	"False"	"CHEMBL3802363"	"Inhibition of recombinant human GST-tagged JAK2 expressed in baculovirus expression system using Z'-LYTE Try6 peptide as substrate incubated for 1 hr by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL4795804"	""	"0"	"460.97"	"1"	"5.36"	"10i"	"O=C(Nc1c[nH]nc1-c1nc(-c2ccc(CN3CCCCC3)cc2)c[nH]1)c1cccc(Cl)c1"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	""	""	"16.91"	"0.32"	"2.44"	"8.69"	"False"	"CHEMBL4711870"	"Inhibition of JAK2 (unknown origin) incubated for 40 mins in presence of ATP by Kinase-glo luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706620"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2021"	"None"	"TIME = 0.6667 hr"
"CHEMBL4797515"	""	"0"	"264.38"	"0"	"3.45"	"12"	"CNc1nc(C)c(C(=O)/C=C/c2ccsc2)s1"	"IC50"	"'='"	"17.64"	"nM"	"7.75"	""	""	""	"29.33"	"0.62"	"4.30"	"18.47"	"False"	"CHEMBL4732643"	"Inhibition of recombinant human JAK2 JH1 domain expressed in baculovirus infected insect cells using poly-Glu-Tyr (51 to 68 residues) as substrate incubated for 1 hr in presence of ATP by ADP-Glo assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4732032"	"1"	"Scientific Literature"	"RSC Med Chem"	"2021"	"None"	"TIME = 1.0 hr"
"CHEMBL3818247"	""	"0"	"461.48"	"0"	"3.32"	"4d"	"CN1C(=O)COc2c1cnc1ccc(Sc3nnc4c(F)cc(-c5cnn(C)c5)cn34)cc21"	"IC50"	"'='"	"21052.0"	"nM"	"4.68"	""	""	"UO_0000065"	"10.13"	"0.19"	"1.36"	"5.17"	"False"	"CHEMBL3820655"	"Inhibition of JAK2 (unknown origin) incubated for 1 hr by spectrophotometric analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3817824"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2016"	"None"	""
"CHEMBL3702904"	""	"0"	"478.58"	"0"	"3.46"	"BDBM147603"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)NCc3ccccc3)cc2)n1"	"IC50"	"'='"	"0.9"	"nM"	"9.05"	""	"285533"	"UO_0000065"	"18.90"	"0.36"	"5.59"	"6.33"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL1789941"	"RUXOLITINIB"	"4"	"306.37"	"0"	"3.47"	"Ruxolitinib"	"N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"18.06"	"nM"	"7.74"	""	""	""	"25.27"	"0.46"	"4.27"	"9.31"	"False"	"CHEMBL4732643"	"Inhibition of recombinant human JAK2 JH1 domain expressed in baculovirus infected insect cells using poly-Glu-Tyr (51 to 68 residues) as substrate incubated for 1 hr in presence of ATP by ADP-Glo assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4732032"	"1"	"Scientific Literature"	"RSC Med Chem"	"2021"	"None"	"TIME = 1.0 hr"
"CHEMBL4750368"	""	"0"	"274.35"	"0"	"3.09"	"25"	"CNc1nc(C)c(C(=O)/C=C/c2ccc(O)cc2)s1"	"IC50"	"'='"	"33.88"	"nM"	"7.47"	""	""	""	"27.23"	"0.54"	"4.38"	"12.01"	"False"	"CHEMBL4732643"	"Inhibition of recombinant human JAK2 JH1 domain expressed in baculovirus infected insect cells using poly-Glu-Tyr (51 to 68 residues) as substrate incubated for 1 hr in presence of ATP by ADP-Glo assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4732032"	"1"	"Scientific Literature"	"RSC Med Chem"	"2021"	"None"	"TIME = 1.0 hr"
"CHEMBL3335686"	""	"0"	"394.50"	"0"	"1.92"	"13"	"CC(C)(C)CS(=O)(=O)N1CCC[C@H](NC(=O)Nc2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	""	"UO_0000065"	"19.76"	"0.39"	"5.88"	"6.49"	"False"	"CHEMBL3374010"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 1 hr in presence of [gamma-33P]ATP by scintillation counting analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351377"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"1"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	""	"UO_0000065"	"26.88"	"0.50"	"6.86"	"9.45"	"True"	"CHEMBL3374010"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 1 hr in presence of [gamma-33P]ATP by scintillation counting analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351377"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL4467881"	""	"0"	"383.45"	"0"	"2.32"	"16"	"COc1ccc(-c2cc3c(N[C@H](CO)CC(C)C)c(C(N)=O)cnn3c2)cn1"	"IC50"	"'='"	"30.0"	"nM"	"7.52"	""	""	"UO_0000065"	"19.62"	"0.37"	"5.20"	"6.55"	"False"	"CHEMBL4339747"	"Inhibition of GST-tagged JAK2 (unknown origin) using fluoresceinated peptide as substrate measured after 3 hrs by electrophoresis method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4339199"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2019"	"None"	""
"CHEMBL4549451"	""	"0"	"381.44"	"0"	"2.08"	"17"	"COc1ccc(-c2cc3c(N[C@H](CO)CC4CC4)c(C(N)=O)cnn3c2)cn1"	"IC50"	"'='"	"25.0"	"nM"	"7.60"	""	""	"UO_0000065"	"19.93"	"0.37"	"5.52"	"6.62"	"False"	"CHEMBL4339747"	"Inhibition of GST-tagged JAK2 (unknown origin) using fluoresceinated peptide as substrate measured after 3 hrs by electrophoresis method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4339199"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2019"	"None"	""
"CHEMBL4463195"	""	"0"	"340.38"	"0"	"1.25"	"23"	"C[C@H](O)[C@H](CO)Nc1c(C(N)=O)cnn2cc(-c3ccccc3)cc12"	"IC50"	"'='"	"1800.0"	"nM"	"5.75"	""	""	"UO_0000065"	"16.88"	"0.31"	"4.49"	"5.09"	"False"	"CHEMBL4339747"	"Inhibition of GST-tagged JAK2 (unknown origin) using fluoresceinated peptide as substrate measured after 3 hrs by electrophoresis method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4339199"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2019"	"None"	""
"CHEMBL3359922"	""	"0"	"274.32"	"0"	"1.15"	"5a"	"C[C@]1(O)CCC[C@H]1Nc1c(C(N)=O)cnn2cccc12"	"IC50"	"'='"	"150.0"	"nM"	"6.82"	""	""	"UO_0000065"	"24.88"	"0.47"	"5.67"	"7.37"	"False"	"CHEMBL3377596"	"Inhibition of JAK2 (unknown origin) by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352641"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3343040"	""	"0"	"401.43"	"0"	"3.92"	"10"	"COc1cc2c(Nc3ccc(NC(=O)c4ccccc4)cc3)nc(N)nc2cc1O"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3380804"	"Inhibition of human JAK2 incubated for 20 mins prior to MgCl2 addition measured after 90 mins by mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351874"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3359910"	""	"0"	"272.35"	"0"	"2.42"	"3d"	"CC1(C)CCC[C@@H]1Nc1c(C(N)=O)cnn2cccc12"	"IC50"	"'='"	"130.0"	"nM"	"6.89"	""	""	"UO_0000065"	"25.28"	"0.47"	"4.47"	"9.51"	"False"	"CHEMBL3377596"	"Inhibition of JAK2 (unknown origin) by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352641"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3359915"	""	"0"	"302.38"	"0"	"1.78"	"4d"	"CC1(C)[C@H](Nc2c(C(N)=O)cnn3cccc23)CC[C@@]1(C)O"	"IC50"	"'='"	"31.0"	"nM"	"7.51"	""	""	"UO_0000065"	"24.83"	"0.47"	"5.73"	"8.10"	"False"	"CHEMBL3377596"	"Inhibition of JAK2 (unknown origin) by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352641"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3359924"	""	"0"	"288.35"	"0"	"1.40"	"5c"	"C[C@]1(CO)CCC[C@H]1Nc1c(C(N)=O)cnn2cccc12"	"IC50"	"'='"	"110.0"	"nM"	"6.96"	""	""	"UO_0000065"	"24.13"	"0.45"	"5.56"	"7.51"	"False"	"CHEMBL3377596"	"Inhibition of JAK2 (unknown origin) by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352641"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL4112874"	""	"0"	"413.93"	"0"	"3.46"	"BDBM147936"	"C[N+]1(C2CC[C@H](n3cc(C(N)=O)c(Nc4ccc(Cl)cc4)n3)[C@@H](C#N)C2)CCC1"	"IC50"	"'='"	"35.0"	"nM"	"7.46"	""	"285870"	"UO_0000065"	"18.01"	"0.35"	"4.00"	"7.71"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3330110"	""	"0"	"385.86"	"0"	"3.06"	"13"	"COCCNC(=O)c1cc(-c2ccnc(N)n2)[nH]c1-c1cc(Cl)ccc1C"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL3374497"	"Inhibition of JAK2 V617F mutant in human SET2 cells"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330114"	""	"0"	"424.94"	"0"	"3.51"	"17"	"Cc1ccc(Cl)cc1-c1[nH]c(-c2ccnc(N)n2)cc1C(=O)NC1CCN(C)CC1"	"IC50"	"'>'"	"3000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3374497"	"Inhibition of JAK2 V617F mutant in human SET2 cells"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330115"	""	"0"	"341.80"	"0"	"2.79"	"18"	"Cc1ccc(Cl)cc1-c1c(C(N)=O)cc(-c2ccnc(N)n2)n1C"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL3374497"	"Inhibition of JAK2 V617F mutant in human SET2 cells"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330128"	""	"0"	"381.75"	"0"	"3.49"	"31"	"NC(=O)c1cc(-c2ccnc(N)n2)[nH]c1-c1cc(Cl)ccc1C(F)(F)F"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL3374497"	"Inhibition of JAK2 V617F mutant in human SET2 cells"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330129"	""	"0"	"341.80"	"0"	"3.04"	"32"	"CCc1ccc(Cl)cc1-c1[nH]c(-c2ccnc(N)n2)cc1C(N)=O"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"24.94"	"0.48"	"5.48"	"7.70"	"False"	"CHEMBL3374493"	"Inhibition of recombinant human JAK2 (808-1132 residues) using LPLDKDYYVVREPGQ as substrate by radiometric assay in presence of [33P]-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330119"	""	"0"	"447.93"	"0"	"4.82"	"22"	"COc1ccc(CNc2nccc(-c3cc(C(N)=O)c(-c4cc(Cl)ccc4C)[nH]3)n2)cc1"	"IC50"	"'='"	"394.0"	"nM"	"6.41"	""	""	"UO_0000065"	"14.30"	"0.27"	"1.58"	"6.05"	"False"	"CHEMBL3374493"	"Inhibition of recombinant human JAK2 (808-1132 residues) using LPLDKDYYVVREPGQ as substrate by radiometric assay in presence of [33P]-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330117"	""	"0"	"312.76"	"0"	"3.20"	"20"	"Cc1ccc(Cl)cc1-c1[nH]c(-c2ccncn2)cc1C(N)=O"	"IC50"	"'='"	"1235.0"	"nM"	"5.91"	""	""	"UO_0000065"	"18.89"	"0.37"	"2.71"	"6.98"	"False"	"CHEMBL3374493"	"Inhibition of recombinant human JAK2 (808-1132 residues) using LPLDKDYYVVREPGQ as substrate by radiometric assay in presence of [33P]-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330130"	""	"0"	"375.35"	"0"	"3.40"	"33"	"CCc1ccc(C(F)(F)F)cc1-c1[nH]c(-c2ccnc(N)n2)cc1C(N)=O"	"IC50"	"'='"	"320.0"	"nM"	"6.50"	""	""	"UO_0000065"	"17.30"	"0.33"	"3.09"	"5.87"	"False"	"CHEMBL3374497"	"Inhibition of JAK2 V617F mutant in human SET2 cells"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3335689"	""	"0"	"414.54"	"0"	"2.88"	"BDBM112533"	"CC(C)CS(=O)(=O)N1CCC[C@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.1079"	"nM"	"9.97"	""	"233772"	"UO_0000065"	"24.04"	"0.47"	"7.09"	"9.60"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3658123"	""	"0"	"622.10"	"2"	"6.46"	"BDBM148443"	"CN1CCN(c2ccc(Nc3ncc4c(n3)CCN(c3cc(NC(=O)c5cccc(C(F)(F)F)c5)ccc3Cl)C4)cc2)CC1"	"IC50"	"'='"	"8.8"	"nM"	"8.06"	""	"286807"	"UO_0000065"	"12.95"	"0.25"	"1.60"	"10.51"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647854"	""	"0"	"376.37"	"0"	"2.28"	"BDBM147964"	"N#C[C@H]1C[C@@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)F)nc2)n1"	"IC50"	"'='"	"33.0"	"nM"	"7.48"	""	"285898"	"UO_0000065"	"19.88"	"0.38"	"5.20"	"5.76"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4798434"	""	"0"	"265.36"	"0"	"2.85"	"11"	"CNc1nc(C)c(C(=O)/C=C/c2nccs2)s1"	"IC50"	"'='"	"20.32"	"nM"	"7.69"	""	""	""	"28.99"	"0.62"	"4.84"	"14.02"	"False"	"CHEMBL4732643"	"Inhibition of recombinant human JAK2 JH1 domain expressed in baculovirus infected insect cells using poly-Glu-Tyr (51 to 68 residues) as substrate incubated for 1 hr in presence of ATP by ADP-Glo assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4732032"	"1"	"Scientific Literature"	"RSC Med Chem"	"2021"	"None"	"TIME = 1.0 hr"
"CHEMBL4466925"	""	"0"	"450.52"	"0"	"3.29"	"7d"	"Cc1cnc(Nc2ccc(-n3ccnc3)cc2)nc1-c1cc2c(o1)CCN(S(C)(=O)=O)C2"	"IC50"	"'='"	"10.8"	"nM"	"7.97"	""	""	"UO_0000065"	"17.68"	"0.34"	"4.68"	"7.51"	"False"	"CHEMBL4341343"	"Inhibition of JAK2 (unknown origin) using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition and measured by 30 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL3402478"	""	"0"	"285.74"	"0"	"2.87"	"4"	"Cc1ccc(Cl)cc1-n1cc(-c2ccnc(N)n2)cn1"	"IC50"	"'='"	"950.0"	"nM"	"6.02"	""	""	"UO_0000065"	"21.08"	"0.41"	"3.15"	"8.65"	"False"	"CHEMBL3404501"	"Inhibition of recombinant epitope-tagged JAK2 (808 to 1132) (unknown origin) using LPLDKDYYVVREPGQ as substrate by beta-countiing analysis in presence of 33P-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3400063"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3403551"	""	"0"	"327.78"	"0"	"2.78"	"24"	"Cc1ccc(Cl)cc1-c1cc(-c2cc(N)ncn2)[nH]c1C(N)=O"	"IC50"	"'='"	"690.0"	"nM"	"6.16"	""	""	"UO_0000065"	"18.80"	"0.37"	"3.38"	"5.57"	"False"	"CHEMBL3404501"	"Inhibition of recombinant epitope-tagged JAK2 (808 to 1132) (unknown origin) using LPLDKDYYVVREPGQ as substrate by beta-countiing analysis in presence of 33P-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3400063"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3403536"	""	"0"	"341.80"	"0"	"3.04"	"9"	"CNc1cc(-n2cc(C(N)=O)c(-c3cc(Cl)ccc3C)c2)ncn1"	"IC50"	"'='"	"620.0"	"nM"	"6.21"	""	""	"UO_0000065"	"18.16"	"0.35"	"3.17"	"7.23"	"False"	"CHEMBL3404501"	"Inhibition of recombinant epitope-tagged JAK2 (808 to 1132) (unknown origin) using LPLDKDYYVVREPGQ as substrate by beta-countiing analysis in presence of 33P-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3400063"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL1944698"	"ZOTIRACICLIB"	"1"	"372.47"	"0"	"4.66"	"SB1317"	"CN1C/C=C/CCOc2cccc(c2)-c2ccnc(n2)Nc2cccc(c2)C1"	"IC50"	"'='"	"170.0"	"nM"	"6.77"	""	""	"UO_0000065"	"18.17"	"0.33"	"2.11"	"13.46"	"False"	"CHEMBL3419812"	"Inhibition of human recombinant JAK2 using Z'LYTETry6 peptide substrate after 1 hr by microplate reader"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3414525"	"1"	"Scientific Literature"	"Eur. J. Med. Chem."	"2015"	"None"	""
"CHEMBL3417195"	""	"0"	"543.67"	"2"	"5.54"	"41"	"O=C(CCCCCCCC(=O)N1C/C=C/COCc2cccc(c2)-c2ccnc(n2)Nc2cccc(c2)C1)NO"	"IC50"	"'='"	"835.0"	"nM"	"6.08"	""	""	"UO_0000065"	"11.18"	"0.21"	"0.54"	"5.21"	"False"	"CHEMBL3419812"	"Inhibition of human recombinant JAK2 using Z'LYTETry6 peptide substrate after 1 hr by microplate reader"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3414525"	"1"	"Scientific Literature"	"Eur. J. Med. Chem."	"2015"	"None"	""
"CHEMBL3622838"	""	"0"	"282.31"	"0"	"0.55"	"5o"	"NCCn1c(-c2cncnc2)nc2cc(C(N)=O)ccc21"	"IC50"	"'='"	"1600.0"	"nM"	"5.80"	""	""	"UO_0000065"	"20.53"	"0.38"	"5.25"	"5.14"	"False"	"CHEMBL3625898"	"Inhibition of JAK2 (unknown origin) using 35 uM of ATP and Tyr6 peptide by Z'-LYTE kinase assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621116"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL3647859"	""	"0"	"437.42"	"0"	"2.72"	"BDBM147969"	"C[C@@](O)(c1ccc(Nc2nn([C@H]3CC[C@H](O)C[C@@H]3C#N)cc2C(N)=O)cc1)C(F)(F)F"	"IC50"	"'='"	"0.95"	"nM"	"9.02"	""	"285903"	"UO_0000065"	"20.63"	"0.40"	"6.30"	"6.58"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652339"	""	"0"	"407.54"	"0"	"2.00"	"BDBM113150"	"CO[C@@H]1CCN(S(=O)(=O)C[C@H]2CC[C@H](N(C)c3ncnc4[nH]ccc34)CC2)C1"	"IC50"	"'='"	"41.8"	"nM"	"7.38"	""	"234593"	"UO_0000065"	"18.11"	"0.36"	"5.38"	"8.07"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3703493"	""	"0"	"308.34"	"0"	"2.77"	"BDBM153137"	"CCOC(=O)c1c[nH]c2ncnc(-c3ccc4c(c3)NCC4)c12"	"IC50"	"'='"	"91.0"	"nM"	"7.04"	""	"294085"	"UO_0000065"	"22.84"	"0.42"	"4.27"	"8.81"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642351"	""	"0"	"506.63"	"1"	"4.01"	"BDBM99627"	"CN(c1cccc(-c2cccn3nc(Nc4ccc(OCCN5CCCC5)cc4)nc23)c1)S(C)(=O)=O"	"IC50"	"'='"	"33.95"	"nM"	"7.47"	""	"216317"	"UO_0000065"	"14.74"	"0.28"	"3.46"	"8.11"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3622830"	""	"0"	"305.34"	"0"	"1.63"	"5g"	"N#Cc1ccc(-c2nc3cc(C(N)=O)ccc3n2CCN)cc1"	"IC50"	"'='"	"2600.0"	"nM"	"5.58"	""	""	"UO_0000065"	"18.29"	"0.33"	"3.96"	"5.04"	"False"	"CHEMBL3625898"	"Inhibition of JAK2 (unknown origin) using 35 uM of ATP and Tyr6 peptide by Z'-LYTE kinase assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621116"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL4465076"	""	"0"	"411.48"	"0"	"3.74"	"12l"	"COc1ccc(F)cc1C(C)Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"20.71"	"0.39"	"4.78"	"9.77"	"False"	"CHEMBL4341687"	"Inhibition of human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr by Z'-LYTE assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340536"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2019"	"CHEMBL3308860"	""
"CHEMBL3137308"	"PEFICITINIB"	"3"	"326.40"	"0"	"2.01"	"peficitinib"	"NC(=O)c1cnc2[nH]ccc2c1N[C@H]1[C@H]2CC3C[C@@H]1C[C@](O)(C3)C2"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	""	"UO_0000065"	"25.43"	"0.47"	"6.29"	"7.98"	"False"	"CHEMBL3625890"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621116"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL3703087"	""	"0"	"474.49"	"0"	"3.31"	"BDBM147801"	"N#C[C@H]1C[C@@H](N2CC3(COC3)C2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	"285735"	"UO_0000065"	"16.23"	"0.31"	"4.39"	"7.05"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4450347"	""	"0"	"340.38"	"0"	"1.25"	"24"	"C[C@H](O)[C@@H](CO)Nc1c(C(N)=O)cnn2cc(-c3ccccc3)cc12"	"IC50"	"'='"	"370.0"	"nM"	"6.43"	""	""	"UO_0000065"	"18.90"	"0.35"	"5.18"	"5.70"	"False"	"CHEMBL4339747"	"Inhibition of GST-tagged JAK2 (unknown origin) using fluoresceinated peptide as substrate measured after 3 hrs by electrophoresis method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4339199"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2019"	"None"	""
"CHEMBL3310151"	""	"0"	"435.46"	"0"	"2.07"	"17"	"CN1CCN(c2cc(F)c3c(c2)nc(Cc2ccc4c(c2)OCO4)n2nc(N)nc32)CC1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3381081"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352169"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3931371"	""	"0"	"589.71"	"1"	"3.23"	"108"	"Cc1ccc(C#N)c(N2CCC(C(=O)N3CCC(N4CC(CC#N)(n5cc(-c6ncnc7[nH]ccc67)cn5)C4)CC3)CC2)n1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3958200"	""	"0"	"585.65"	"1"	"4.73"	"118"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(-c4ccc(C#N)cc4)c(F)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3922040"	""	"0"	"567.65"	"1"	"4.31"	"121"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(F)c(-c4nccs4)c3)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3944955"	""	"0"	"585.65"	"1"	"4.73"	"125"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(-c4cccc(C#N)c4)c(F)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3947572"	""	"0"	"567.66"	"1"	"4.59"	"126"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(-c4ccc(C#N)cc4)cc3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3977459"	""	"0"	"596.62"	"2"	"5.14"	"127"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(-c4ccc(F)c(F)c4)c(F)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3949720"	""	"0"	"579.56"	"1"	"4.13"	"142"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CC3CCC(C2)N3C(=O)c2ccnc(C(F)(F)F)c2F)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3932974"	""	"0"	"549.56"	"1"	"4.46"	"166"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3cccc(C(F)(F)F)c3)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3906010"	""	"0"	"550.55"	"1"	"3.86"	"188"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3cccc(C(F)(F)F)n3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3910628"	""	"0"	"488.58"	"0"	"2.90"	"190"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3nccs3)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3951065"	""	"0"	"502.61"	"1"	"3.21"	"191"	"Cc1csc(NC(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)n1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3948435"	""	"0"	"516.64"	"1"	"3.52"	"192"	"Cc1nc(NC(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)sc1C"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3958382"	""	"0"	"538.64"	"1"	"3.49"	"209"	"CN(C)c1ccc(CN2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)c(F)c1C#N"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3915507"	""	"0"	"488.55"	"0"	"3.69"	"217"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(Cc3ccc(F)cc3F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3900462"	""	"0"	"611.35"	"1"	"4.33"	"225"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(Cc3cc(Br)nc(Br)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3973675"	""	"0"	"573.00"	"2"	"5.22"	"236"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(Cc3c(C(F)(F)F)ccc(Cl)c3F)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3915302"	""	"0"	"564.67"	"1"	"4.02"	"240"	"CN(C)c1ccc(CN2C3CCC2CC(N2CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C2)C3)c(F)c1C#N"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3945802"	""	"0"	"549.03"	"1"	"4.87"	"241"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CC3CCC(C2)N3Cc2c(F)ccc(F)c2Cl)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3964271"	""	"0"	"506.60"	"1"	"1.33"	"251"	"Cn1ccc(S(=O)(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)n1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3913894"	""	"0"	"466.55"	"0"	"3.05"	"9"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccccc3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3945897"	""	"0"	"496.58"	"0"	"3.06"	"31"	"COc1cccc(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)c1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3907665"	""	"0"	"498.57"	"0"	"3.50"	"64"	"Cc1ccc(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)cc1F"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3966319"	""	"0"	"551.47"	"1"	"3.87"	"75"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccsc3Br)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL2376151"	""	"0"	"484.56"	"0"	"2.91"	"6h"	"C[C@@H](NC(=O)c1c[nH]c2ncc(-c3nn(C)c4cc(C(C)(C)C)ccc34)nc12)C(=O)N1CC(C#N)C1"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	""	"UO_0000065"	"16.27"	"0.30"	"4.98"	"5.95"	"False"	"CHEMBL2378515"	"Inhibition of JAK2 (unknown origin) using [33gammaP]ATP and Biotin-KAIETDKEYYTVKD as substrate incubated for 10 mins prior to substrate addition measured after 30 mins by filtration assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375236"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL1789941"	"RUXOLITINIB"	"4"	"306.37"	"0"	"3.47"	"1b"	"N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"26.0"	"nM"	"7.58"	""	""	"UO_0000065"	"24.76"	"0.45"	"4.12"	"9.12"	"False"	"CHEMBL2378509"	"Inhibition of JAK2 in human monocytes expressing CD14 assessed as inhibition of GM-CSF-stimulated STAT5a phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375236"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2376158"	""	"0"	"450.41"	"0"	"1.65"	"9"	"C[C@@H](NC(=O)c1c[nH]c2ncc(-c3ncn4cc(F)cc(F)c34)nc12)C(=O)N1CC(C#N)C1"	"IC50"	"'='"	"10800.0"	"nM"	"4.97"	""	""	"UO_0000065"	"11.03"	"0.21"	"3.32"	"3.76"	"False"	"CHEMBL2378509"	"Inhibition of JAK2 in human monocytes expressing CD14 assessed as inhibition of GM-CSF-stimulated STAT5a phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375236"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2325895"	""	"0"	"380.45"	"0"	"1.96"	"2a"	"CC(C)(C)[C@@H](NC(=O)c1c[nH]c2ncc(C3CC3)nc12)C(=O)N1CC(C#N)C1"	"IC50"	"'='"	"190.0"	"nM"	"6.72"	""	""	"UO_0000065"	"17.67"	"0.33"	"4.76"	"5.86"	"False"	"CHEMBL2378509"	"Inhibition of JAK2 in human monocytes expressing CD14 assessed as inhibition of GM-CSF-stimulated STAT5a phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375236"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL3907114"	""	"0"	"527.61"	"1"	"2.47"	"249"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(S(=O)(=O)c3ccc(C#N)cc3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3892706"	""	"0"	"494.63"	"0"	"2.48"	"253"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(S(=O)(=O)C3CCCC3)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3979530"	""	"0"	"454.56"	"0"	"1.56"	"255"	"CCS(=O)(=O)N1CCC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3981971"	""	"0"	"500.99"	"1"	"3.70"	"19"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cccc(Cl)c3)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3984184"	""	"0"	"570.60"	"1"	"4.14"	"70"	"COc1cc(C(F)(F)F)sc1C(=O)N1CCC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3926507"	""	"0"	"507.02"	"1"	"3.77"	"77"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(Cl)s3)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3969679"	""	"0"	"575.07"	"2"	"5.06"	"92"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3sc4cccc(F)c4c3Cl)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3973120"	""	"0"	"551.55"	"1"	"4.81"	"266"	"N#CCC1(n2ccc(-c3ncnc4[nH]ccc34)c2)CN(C2CCN(C(=O)c3cc(F)ccc3C(F)(F)F)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3923848"	""	"0"	"551.55"	"1"	"4.81"	"267"	"N#CCC1(n2ccc(-c3ncnc4[nH]ccc34)c2)CN(C2CCN(C(=O)c3ccc(C(F)(F)F)c(F)c3)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3933570"	""	"0"	"533.56"	"1"	"4.67"	"268"	"N#CCC1(n2ccc(-c3ncnc4[nH]ccc34)c2)CN(C2CCN(C(=O)c3cccc(C(F)(F)F)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3983598"	""	"0"	"567.55"	"1"	"4.69"	"269"	"N#CCC1(n2ccc(-c3ncnc4[nH]ccc34)c2)CN(C2CCN(C(=O)c3cc(OC(F)(F)F)ccc3F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3974704"	""	"0"	"535.53"	"1"	"3.46"	"301; 349"	"N#CCC1(n2cc(-c3ccnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cnc(C(F)(F)F)cn3)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3932590"	""	"0"	"516.56"	"1"	"4.33"	"304"	"N#CCC1(n2cc(-c3ccnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3ccc(F)cc3F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3977397"	""	"0"	"523.58"	"1"	"4.06"	"312"	"N#CCC1(n2cc(-c3ccnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3ccc(C#N)cc3F)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3934511"	""	"0"	"526.55"	"1"	"3.81"	"316"	"N#CCC1(n2cc(-c3c(F)cnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc(F)cc(C#N)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3918254"	""	"0"	"533.57"	"1"	"3.54"	"333"	"N#CCC1(n2cc(-c3c(C#N)cnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc(F)cc(C#N)c3)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3920989"	""	"0"	"533.57"	"1"	"3.54"	"334"	"N#CCC1(n2cc(-c3c(C#N)cnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(C#N)c(F)c3)CC2)C1"	"IC50"	"'>'"	"100.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3959944"	""	"0"	"551.56"	"1"	"3.68"	"340"	"N#CCC1(n2cc(-c3c(C#N)cnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3c(F)cc(C#N)cc3F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3915499"	""	"0"	"457.54"	"0"	"1.91"	"355"	"CS(=O)(=O)N1CCC(N2CC(CC#N)(n3cc(-c4c(F)cnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3949497"	""	"0"	"592.63"	"1"	"3.53"	"366"	"CN(C)Cc1cc(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)nc(C(F)(F)F)c1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3917371"	""	"0"	"637.67"	"2"	"2.67"	"385"	"CN(CCCO)Cc1cc(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)nc(C(F)(F)F)n1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3902928"	""	"0"	"496.58"	"0"	"3.55"	"389"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)OCc3ccccc3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3900185"	""	"0"	"462.56"	"0"	"3.00"	"390"	"CC(C)COC(=O)N1CCC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3961888"	""	"0"	"460.54"	"0"	"2.76"	"391"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)OCC3CC3)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3928482"	""	"0"	"532.56"	"1"	"3.83"	"395; 396"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)OCc3cc(F)cc(F)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3958933"	""	"0"	"457.50"	"0"	"2.04"	"16"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ncco3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3900894"	""	"0"	"484.54"	"0"	"3.19"	"25"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cccc(F)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3943519"	""	"0"	"538.51"	"1"	"3.61"	"56"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3c(F)c(F)cc(F)c3F)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3980119"	""	"0"	"484.54"	"0"	"3.19"	"68"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(F)cc3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3896322"	""	"0"	"502.60"	"1"	"3.12"	"72"	"COc1cscc1C(=O)N1CCC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3959500"	""	"0"	"516.99"	"1"	"3.41"	"84"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(O)c(Cl)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3949598"	""	"0"	"583.14"	"2"	"5.36"	"105"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)C3CCC(c4ccc(Cl)cc4)CC3)CC2)C1"	"IC50"	"'>'"	"100.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL4283458"	""	"0"	"392.46"	"0"	"3.31"	"17e"	"COc1cc2c(=O)n(C3CCN(C)CC3)c3c4cc[nH]c4ncc3c2cc1OC"	"IC50"	"'='"	"37.07"	"nM"	"7.43"	""	""	"UO_0000065"	"18.93"	"0.35"	"4.12"	"10.27"	"False"	"CHEMBL4261266"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]-ATP addition measured after 2 hrs by filter-binding method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257589"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4285332"	""	"0"	"409.44"	"0"	"3.39"	"13a"	"COc1cc2c(=O)n(CC(=O)OC(C)(C)C)c3c4cc[nH]c4ncc3c2cc1OC"	"IC50"	"'='"	"14.12"	"nM"	"7.85"	""	""	"UO_0000065"	"19.17"	"0.36"	"4.46"	"8.23"	"False"	"CHEMBL4261266"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]-ATP addition measured after 2 hrs by filter-binding method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257589"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4292011"	""	"0"	"415.42"	"0"	"3.72"	"24"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(C(=O)c2cccc(C(F)(F)F)c2)CC12CC2"	"IC50"	"'='"	"11000.0"	"nM"	"4.96"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4278452"	""	"0"	"401.47"	"0"	"2.39"	"44"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(S(=O)(=O)c2ccc(F)cc2)CC12CC2"	"IC50"	"'='"	"50.0"	"nM"	"7.30"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL551570"	""	"0"	"481.64"	"0"	"4.90"	"15"	"COc1nc(C)cc2c1-c1[nH]c3cc(N4CCN(C)CC4)ccc3c1CCN2CCc1ccccc1"	"IC50"	"'='"	"5100.0"	"nM"	"5.29"	""	""	"UO_0000065"	"10.99"	"0.20"	"0.39"	"11.11"	"False"	"CHEMBL1036442"	"Inhibition of recombinant JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1151875"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2009"	"None"	""
"CHEMBL4287327"	""	"0"	"433.54"	"0"	"3.40"	"54"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(S(=O)(=O)c2ccc3ccccc3c2)CC12CC2"	"IC50"	"'='"	"150.0"	"nM"	"6.82"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4280297"	""	"0"	"368.49"	"0"	"2.90"	"28"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(C(=O)NC2CCCCC2)CC12CC2"	"IC50"	"'='"	"4400.0"	"nM"	"5.36"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL557491"	""	"0"	"560.23"	"2"	"5.91"	"24b"	"Oc1ccc(CCN2CCc3c([nH]c4ccc(Br)cc34)-c3c(I)ccnc32)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1036442"	"Inhibition of recombinant JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1151875"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2009"	"None"	""
"CHEMBL4286370"	""	"0"	"408.49"	"0"	"2.12"	"45"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(S(=O)(=O)c2ccccc2C#N)CC12CC2"	"IC50"	"'='"	"480.0"	"nM"	"6.32"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL549826"	""	"0"	"620.33"	"2"	"7.79"	"25b"	"Brc1ccc2[nH]c3c(c2c1)CCN(CC(c1ccccc1)c1ccccc1)c1nccc(I)c1-3"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1036442"	"Inhibition of recombinant JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1151875"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2009"	"None"	""
"CHEMBL4250122"	""	"0"	"544.66"	"2"	"5.54"	"13d"	"O=C(CCCCCCC(=O)Nc1ccc(Nc2nc(-c3cnn(CC4CCCC4)c3)c3cc[nH]c3n2)cc1)NO"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"15.65"	"0.29"	"2.98"	"5.69"	"False"	"CHEMBL4233426"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma-33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229421"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2018"	"None"	""
"CHEMBL221378"	""	"0"	"400.42"	"0"	"4.78"	"34"	"C[C@H](Nc1cc(-c2ccoc2)nc(-n2cnc3ccncc32)n1)c1ccc(F)cc1"	"IC50"	"'='"	"28.0"	"nM"	"7.55"	""	""	"UO_0000065"	"18.86"	"0.34"	"2.77"	"9.25"	"False"	"CHEMBL908418"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139695"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2006"	"None"	""
"CHEMBL376885"	""	"0"	"420.91"	"0"	"3.36"	"22"	"CN1CCN(c2cc(Nc3ccccc3Cl)nc(-n3cnc4ccncc43)n2)CC1"	"IC50"	"'='"	"113.0"	"nM"	"6.95"	""	""	"UO_0000065"	"16.50"	"0.32"	"3.59"	"9.26"	"False"	"CHEMBL908418"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139695"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2006"	"None"	""
"CHEMBL385114"	""	"0"	"423.43"	"0"	"3.03"	"21"	"CN1CCN(c2cc(Oc3c(F)cccc3F)nc(-n3cnc4ccncc43)n2)CC1"	"IC50"	"'='"	"68.0"	"nM"	"7.17"	""	""	"UO_0000065"	"16.93"	"0.32"	"4.14"	"9.93"	"False"	"CHEMBL908418"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139695"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2006"	"None"	""
"CHEMBL3115324"	""	"0"	"369.45"	"0"	"4.11"	"9"	"CCOc1ccc(Nc2nc(N)c(C(=O)c3cccc(OC)c3)s2)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL3119788"	"Inhibition of JAK2 (unknown origin) by radioactive ATP method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112544"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL1580295"	""	"0"	"373.41"	"0"	"3.26"	"8"	"Cc1cc(/C=C2/C(=O)NN(c3ccccc3)C2=O)c(C)n1-c1cccc(O)c1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL3119788"	"Inhibition of JAK2 (unknown origin) by radioactive ATP method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112544"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL3112617"	""	"0"	"364.79"	"0"	"4.06"	"5"	"O=C1NN(c2ccccc2)C(=O)/C1=C/c1ccc(-c2ccccc2Cl)o1"	"IC50"	"'='"	"6000.0"	"nM"	"5.22"	""	""	"UO_0000065"	"14.31"	"0.27"	"1.16"	"8.35"	"False"	"CHEMBL3119788"	"Inhibition of JAK2 (unknown origin) by radioactive ATP method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112544"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL3974668"	""	"0"	"500.61"	"1"	"2.69"	"146"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CC3CCC(C2)N3C(=O)C2CCOCC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3922382"	""	"0"	"530.04"	"1"	"4.40"	"168"	"Cc1ccc(Cl)cc1NC(=O)N1CCC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3889651"	""	"0"	"565.56"	"1"	"4.34"	"182"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3ccc(OC(F)(F)F)cc3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3939666"	""	"0"	"514.57"	"1"	"3.29"	"200"	"Cc1ccc(NC(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)c(F)n1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3589168"	""	"0"	"457.53"	"0"	"4.35"	"5"	"CCCOc1cccc(-c2cc(C(N)=O)c3[nH]c4ccc(C(=O)N5CCOCC5)cc4c3c2)c1"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	""	"UO_0000065"	"17.70"	"0.33"	"3.75"	"8.29"	"False"	"CHEMBL3592849"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3589164"	""	"0"	"468.34"	"0"	"4.87"	"1"	"NC(=O)c1cc(-c2ccc(Cl)c(Cl)c2)cc2c1[nH]c1ccc(C(=O)N3CCOCC3)cc12"	"IC50"	"'='"	"200.0"	"nM"	"6.70"	""	""	"UO_0000065"	"14.30"	"0.29"	"1.83"	"7.58"	"False"	"CHEMBL3592855"	"Inhibition of JAK2 in human SET2 cells assessed as inhibition of cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3589173"	""	"0"	"472.37"	"0"	"4.20"	"10"	"NC(=O)c1cc(-c2ccc(Cl)c(Cl)c2)cc2c3c([nH]c12)CCC(C(=O)N1CCOCC1)C3"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL3592855"	"Inhibition of JAK2 in human SET2 cells assessed as inhibition of cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3589326"	""	"0"	"418.93"	"0"	"4.49"	"18"	"CN1CCN(c2ccc3c(c2)[nH]c2c(C(N)=O)cc(-c4cccc(Cl)c4)cc23)CC1"	"IC50"	"'='"	"470.0"	"nM"	"6.33"	""	""	"UO_0000065"	"15.10"	"0.29"	"1.84"	"9.68"	"False"	"CHEMBL3592855"	"Inhibition of JAK2 in human SET2 cells assessed as inhibition of cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3782012"	""	"0"	"364.43"	"0"	"1.48"	"1"	"CS(=O)(=O)c1ccc(Nc2nn(C3CCOCC3)cc2C(N)=O)cc1"	"IC50"	"'='"	"150.0"	"nM"	"6.82"	""	""	"UO_0000065"	"18.72"	"0.37"	"5.34"	"5.87"	"False"	"CHEMBL3784139"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3779778"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3890948"	""	"0"	"514.57"	"1"	"3.20"	"5"	"COc1ccc(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)cc1F"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3943415"	""	"0"	"491.56"	"0"	"2.92"	"11"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cccc(C#N)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3892108"	""	"0"	"552.54"	"1"	"4.21"	"23"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc(F)cc(C(F)(F)F)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3934393"	""	"0"	"526.60"	"1"	"3.07"	"33"	"COc1cc(OC)cc(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)c1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3936342"	""	"0"	"503.52"	"1"	"2.72"	"61"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3c(F)cncc3F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3893627"	""	"0"	"556.57"	"1"	"3.84"	"71"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3sc(C(F)(F)F)cc3O)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3890137"	""	"0"	"517.60"	"1"	"3.60"	"89"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc4ncccc4c3)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3983330"	""	"0"	"611.69"	"2"	"5.41"	"131"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(-c4cccc5ccncc45)c(F)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3955708"	""	"0"	"549.56"	"1"	"4.46"	"157"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3ccccc3C(F)(F)F)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3922657"	""	"0"	"535.62"	"1"	"3.33"	"194"	"Cn1c(NC(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)nc2ccccc21"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3971101"	""	"0"	"552.69"	"1"	"3.79"	"235"	"CC(C)(C)C(=O)Nc1ncccc1CN1CCC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3984158"	""	"0"	"547.06"	"1"	"4.08"	"239"	"COc1ccc(CN2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)c(Cl)c1OC"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3956227"	""	"0"	"505.59"	"1"	"3.92"	"287"	"N#CCC1(n2ccc(-c3ncnc4[nH]ccc34)c2)CN(C2CCN(C(=O)Nc3ccccc3C#N)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3974147"	""	"0"	"535.53"	"1"	"3.46"	"345"	"N#CCC1(n2ccc(-c3ncnc4[nH]ccc34)c2)CN(C2CCN(C(=O)c3ccnc(C(F)(F)F)n3)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3948991"	""	"0"	"439.55"	"0"	"1.77"	"351"	"CS(=O)(=O)N1CCC(N2CC(CC#N)(n3cc(-c4ccnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3917805"	""	"0"	"1093.73"	"1"	"3.40"	"377"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc(CN4CC[C@H](F)C4)nc(C(F)(F)F)n3)CC2)C1.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3973560"	""	"0"	"491.56"	"0"	"2.92"	"10"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccccc3C#N)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3981766"	""	"0"	"541.47"	"1"	"4.42"	"30"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc(Cl)sc3Cl)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3398141"	""	"0"	"377.47"	"0"	"3.13"	"7h"	"CCCCN(C)c1ncc(NS(=O)(=O)c2ccccc2C)cc1C(=O)O"	"IC50"	"'='"	"12200.0"	"nM"	"4.91"	""	""	"UO_0000065"	"13.02"	"0.26"	"1.78"	"4.93"	"False"	"CHEMBL3399759"	"Inhibition of IL4-induced JAK2 autophosphorylation in human HT-29 cells by SDS-polyacrylamide gel electrophoresis and Western blot method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HT-29"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3397032"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"CHEMBL3307768"	""
"CHEMBL3917271"	""	"0"	"590.64"	"2"	"5.28"	"95"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc4cccc(C(F)(F)F)c4s3)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3918595"	""	"0"	"567.55"	"1"	"4.60"	"170"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3cccc(C(F)(F)F)c3F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3921362"	""	"0"	"492.59"	"0"	"4.16"	"232"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(Cc3cc4ccccc4o3)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3924462"	""	"0"	"540.59"	"1"	"4.11"	"98"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)C3CCC(C(F)(F)F)CC3)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3920805"	""	"0"	"550.45"	"1"	"4.75"	"160"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3c(Cl)cccc3Cl)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3925297"	""	"0"	"577.55"	"1"	"4.08"	"356"	"N#CCC1(n2cc(-c3c(C#N)cnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc(C(F)(F)F)ncc3F)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3967743"	""	"0"	"499.55"	"0"	"3.50"	"296"	"N#CCC1(n2cc(-c3ccnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(O)c(F)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3946123"	""	"0"	"534.55"	"1"	"4.07"	"22"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cccc(C(F)(F)F)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3948390"	""	"0"	"552.54"	"1"	"4.21"	"45"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3c(F)cccc3C(F)(F)F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3943852"	""	"0"	"516.61"	"1"	"4.20"	"87"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cccc4ccccc34)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3970431"	""	"0"	"509.55"	"1"	"3.06"	"295"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(C#N)cc3F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3984668"	""	"0"	"540.58"	"1"	"4.13"	"350"	"N#CCC1(n2cc(-c3ccnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3nc(C(F)(F)F)cs3)CC2)C1"	"IC50"	"'>'"	"100.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3944722"	""	"0"	"605.63"	"1"	"3.07"	"372"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc(CN4CCC4)nc(C(F)(F)F)n3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3975381"	""	"0"	"434.50"	"0"	"2.37"	"388"	"CCOC(=O)N1CCC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3924438"	""	"0"	"522.44"	"1"	"4.11"	"237"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(Cc3c(Cl)cncc3Cl)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL1470728"	""	"0"	"388.25"	"0"	"3.92"	"SID24782122"	"Cc1cc2[nH]c3c(c[n+](C)c4ccccc34)c2cc1C.[I-]"	"IC50"	"'='"	"3850.0"	"nM"	"5.42"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1393319"	""	"0"	"355.44"	"0"	"4.20"	"SID26663690"	"Cc1nn2c(NCc3ccccn3)c3c(nc2c1-c1ccccc1)CCC3"	"IC50"	"'='"	"4277.0"	"nM"	"5.37"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1981883"	""	"0"	"322.22"	"1"	"5.66"	"SID24783813"	"Oc1ccc(Cl)cc1/N=C/c1sc2ccccc2c1Cl"	"IC50"	"'='"	"5938.0"	"nM"	"5.23"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1587526"	""	"0"	"310.26"	"0"	"2.16"	"SID17512888"	"COC(=O)/C=C/c1ccc(OC(=O)OC)c(OC(=O)OC)c1"	"IC50"	"'='"	"10710.0"	"nM"	"4.97"	""	"Not Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1379604"	""	"0"	"253.77"	"0"	"3.84"	"SID26660329"	"CCCCCCN(C(=O)CCl)c1ccccc1"	"IC50"	"'='"	"2113.0"	"nM"	"5.67"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL3913592"	""	"0"	"501.58"	"1"	"3.41"	"16f"	"CS(=O)(=O)N1CCc2oc(-c3nc(Nc4ccc(OCCN5CCCC5)cc4)ncc3F)cc2C1"	"IC50"	"'='"	"55.4"	"nM"	"7.26"	""	""	"UO_0000065"	"14.47"	"0.28"	"3.85"	"7.20"	"False"	"CHEMBL3868063"	"Inhibition of GST-tagged recombinant human JAK2 expressed in baculovirus using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3867460"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2017"	"None"	""
"CHEMBL103667"	"DORAMAPIMOD"	"2"	"527.67"	"2"	"5.99"	"Birb796"	"Cc1ccc(-n2nc(C(C)(C)C)cc2NC(=O)Nc2ccc(OCCN3CCOCC3)c3ccccc23)cc1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1932879"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1926590"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL3330113"	""	"0"	"403.87"	"0"	"4.94"	"16"	"Cc1ccc(Cl)cc1-c1[nH]c(-c2ccnc(N)n2)cc1C(=O)Nc1ccccc1"	"IC50"	"'='"	"247.0"	"nM"	"6.61"	""	""	"UO_0000065"	"16.36"	"0.31"	"1.67"	"6.83"	"False"	"CHEMBL3374493"	"Inhibition of recombinant human JAK2 (808-1132 residues) using LPLDKDYYVVREPGQ as substrate by radiometric assay in presence of [33P]-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL4584430"	""	"0"	"534.66"	"2"	"5.71"	"4"	"CCC(=O)N1CCC(c2ccc(Nc3cc(NCc4cccc(-c5ccncc5)c4)c(C(N)=O)cn3)cc2)CC1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4482016"	"Inhibition of human GST-tagged JAK2 by fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480445"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL3301607"	"FILGOTINIB"	"4"	"425.51"	"0"	"1.98"	"8"	"O=C(Nc1nc2cccc(-c3ccc(CN4CCS(=O)(=O)CC4)cc3)n2n1)C1CC1"	"IC50"	"'='"	"2400.0"	"nM"	"5.62"	""	""	"UO_0000065"	"13.21"	"0.26"	"3.64"	"5.81"	"True"	"CHEMBL3299201"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3297690"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL3314279"	""	"0"	"562.54"	"2"	"5.76"	"23"	"CCOP(=O)(CCn1cc(-c2ccc(-c3nc(-c4ccc(F)cc4)c(-c4cc[nH]c(=O)c4)[nH]3)cc2)nn1)OCC"	"IC50"	"'='"	"4200.0"	"nM"	"5.38"	""	""	"UO_0000065"	"9.56"	"0.18"	"-0.38"	"4.21"	"False"	"CHEMBL3363474"	"Inhibition of JAK2 (unknown origin) by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352554"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3787614"	""	"0"	"433.56"	"0"	"3.90"	"1"	"Nc1ncnc2c1c(-c1cccc(OC[C@@H]3CCCO3)c1)cn2[C@H]1C[C@@H](CN2CCC2)C1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3789994"	"Inhibition of JAK2 (unknown origin) in presence of [gamma33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3785066"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3647882"	""	"0"	"484.99"	"0"	"3.09"	"BDBM147994"	"CC(C)(O)C1CN(C(=O)[C@H]2CC[C@H](n3cc(C(N)=O)c(Nc4ccc(Cl)cc4)n3)[C@@H](C#N)C2)C1"	"IC50"	"'='"	"315.0"	"nM"	"6.50"	""	"285929"	"UO_0000065"	"13.41"	"0.26"	"3.41"	"4.74"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3640019"	""	"0"	"462.48"	"0"	"3.31"	"BDBM147780"	"COC1CN([C@H]2CC[C@H](n3cc(C(N)=O)c(Nc4ccc(C(F)(F)F)cc4)n3)[C@@H](C#N)C2)C1"	"IC50"	"'='"	"32.0"	"nM"	"7.50"	""	"285714"	"UO_0000065"	"16.21"	"0.31"	"4.18"	"6.86"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651038"	""	"0"	"365.39"	"0"	"2.25"	"BDBM153215"	"C=C(CN)C(=O)Nc1cccc(-c2ncnc3[nH]cc(C(=O)OCC)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294163"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642380"	""	"0"	"534.69"	"1"	"3.23"	"BDBM99656"	"CN1CCN(c2cccc(Nc3nc4c(NCc5ccccc5CN(C)S(C)(=O)=O)cccn4n3)c2)CC1"	"IC50"	"'='"	"219.62"	"nM"	"6.66"	""	"216346"	"UO_0000065"	"12.45"	"0.24"	"3.43"	"6.79"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3645019"	""	"0"	"549.68"	"2"	"6.75"	"BDBM99771"	"Cc1ccc(-n2cc(-c3cccn4nc(Nc5ccc(C6CCN(C(=O)OC(C)(C)C)CC6)cc5)nc34)cn2)cc1"	"IC50"	"'='"	"1690.16"	"nM"	"5.77"	""	"216458"	"UO_0000065"	"10.50"	"0.19"	"-0.98"	"6.44"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642305"	""	"0"	"477.59"	"0"	"4.02"	"BDBM99575"	"CS(=O)(=O)c1ccc(-c2cccc3nc(Nc4ccc(OCCN5CCCC5)cc4)nn23)cc1"	"IC50"	"'='"	"2.1"	"nM"	"8.68"	""	"216265"	"UO_0000065"	"18.17"	"0.35"	"4.66"	"9.77"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3650985"	""	"0"	"350.38"	"0"	"3.32"	"BDBM153159"	"C=C(C)C(=O)Nc1cccc(-c2ncnc3[nH]cc(C(=O)OCC)c23)c1"	"IC50"	"'>'"	"1480.0"	"nM"	""	""	"294107"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699518"	""	"0"	"471.46"	"0"	"2.77"	"BDBM147536"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)c(CO)c2)n1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"285466"	"UO_0000065"	"17.61"	"0.35"	"5.53"	"5.49"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3330109"	""	"0"	"373.82"	"0"	"3.38"	"12"	"Cc1ccc(Cl)cc1-c1[nH]c(-c2ccnc(N)n2)cc1C(=O)NCCF"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL3374497"	"Inhibition of JAK2 V617F mutant in human SET2 cells"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330111"	""	"0"	"383.88"	"0"	"4.07"	"14"	"Cc1ccc(Cl)cc1-c1[nH]c(-c2ccnc(N)n2)cc1C(=O)NCC(C)C"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL3374497"	"Inhibition of JAK2 V617F mutant in human SET2 cells"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330117"	""	"0"	"312.76"	"0"	"3.20"	"20"	"Cc1ccc(Cl)cc1-c1[nH]c(-c2ccncn2)cc1C(N)=O"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL3374497"	"Inhibition of JAK2 V617F mutant in human SET2 cells"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330106"	""	"0"	"355.83"	"0"	"3.38"	"8"	"Cc1ccc(Cl)cc1-c1[nH]c(-c2ccnc(N)n2)cc1C(=O)N(C)C"	"IC50"	"'='"	"3056.0"	"nM"	"5.51"	""	""	"UO_0000065"	"15.50"	"0.30"	"2.13"	"6.27"	"False"	"CHEMBL3374493"	"Inhibition of recombinant human JAK2 (808-1132 residues) using LPLDKDYYVVREPGQ as substrate by radiometric assay in presence of [33P]-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330102"	""	"0"	"313.75"	"0"	"2.47"	"4"	"NC(=O)c1cc(-c2ccnc(N)n2)[nH]c1-c1cccc(Cl)c1"	"IC50"	"'='"	"617.0"	"nM"	"6.21"	""	""	"UO_0000065"	"19.79"	"0.39"	"3.74"	"5.61"	"False"	"CHEMBL3374493"	"Inhibition of recombinant human JAK2 (808-1132 residues) using LPLDKDYYVVREPGQ as substrate by radiometric assay in presence of [33P]-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL1270230"	""	"0"	"279.30"	"0"	"1.82"	"1"	"NC(=O)c1cc(-c2ccnc(N)n2)[nH]c1-c1ccccc1"	"IC50"	"'='"	"3200.0"	"nM"	"5.50"	""	""	"UO_0000065"	"19.67"	"0.36"	"3.67"	"4.96"	"False"	"CHEMBL3374493"	"Inhibition of recombinant human JAK2 (808-1132 residues) using LPLDKDYYVVREPGQ as substrate by radiometric assay in presence of [33P]-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL2178804"	""	"0"	"402.25"	"0"	"3.27"	"7j"	"Cn1cc(NC(=O)c2cnn3ccc(N)nc23)c(-c2cc(Cl)ccc2Cl)n1"	"IC50"	"'='"	"3.9"	"nM"	"8.41"	""	""	"UO_0000065"	"20.90"	"0.43"	"5.14"	"8.15"	"False"	"CHEMBL2186598"	"Inhibition of JAK2 V617F mutant in human SET2 cells assessed as reduction in STAT5 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176876"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL3642355"	""	"0"	"522.64"	"1"	"3.48"	"BDBM99631"	"CN(c1ncccc1Nc1cccn2nc(Nc3ccc(OCCN4CCCC4)cc3)nc12)S(C)(=O)=O"	"IC50"	"'='"	"33.07"	"nM"	"7.48"	""	"216321"	"UO_0000065"	"14.31"	"0.28"	"4.00"	"6.39"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3747542"	""	"0"	"332.79"	"0"	"3.35"	"12"	"COCCNc1c(Cl)cnc2[nH]c(-c3ccc(OC)cc3)nc12"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3751000"	"Inhibition of N-terminal GST-fused recombinant JAK2 (831 to 1132 residues) (unknown origin) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate by microfluidic capillary electrophoresis method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3745697"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3703502"	""	"0"	"281.31"	"0"	"3.11"	"BDBM153146"	"CCOC(=O)c1c[nH]c2ncnc(-c3cccc(C)c3)c12"	"IC50"	"'='"	"143.0"	"nM"	"6.84"	""	"294094"	"UO_0000065"	"24.33"	"0.45"	"3.73"	"10.08"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3746743"	""	"0"	"371.87"	"0"	"3.79"	"13"	"COc1ccc(-c2nc3c(NC4CCN(C)CC4)c(Cl)cnc3[nH]2)cc1"	"IC50"	"'='"	"14900.0"	"nM"	"4.83"	""	""	"UO_0000065"	"12.98"	"0.25"	"1.04"	"7.31"	"False"	"CHEMBL3751000"	"Inhibition of N-terminal GST-fused recombinant JAK2 (831 to 1132 residues) (unknown origin) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate by microfluidic capillary electrophoresis method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3745697"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL2333365"	""	"0"	"455.51"	"0"	"3.22"	"28, XL388"	"Cc1c(C(=O)N2CCOc3ccc(-c4ccc(N)nc4)cc3C2)ccc(S(C)(=O)=O)c1F"	"IC50"	"'>'"	"3500.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2341960"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2331117"	"1"	"Scientific Literature"	"J. Med. Chem."	"2013"	"None"	""
"CHEMBL3746486"	""	"0"	"288.74"	"0"	"3.33"	"10"	"CNc1c(Cl)cnc2[nH]c(-c3ccc(OC)cc3)nc12"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3751000"	"Inhibition of N-terminal GST-fused recombinant JAK2 (831 to 1132 residues) (unknown origin) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate by microfluidic capillary electrophoresis method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3745697"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3702910"	""	"0"	"499.60"	"0"	"1.83"	"BDBM147609"	"CC(=O)N1CCN(S(=O)(=O)c2ccc(Nc3nn([C@H]4CCCC[C@@H]4C#N)cc3C(N)=O)cc2)CC1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"285539"	"UO_0000065"	"18.01"	"0.35"	"7.17"	"5.83"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645093"	""	"0"	"464.56"	"0"	"2.09"	"BDBM99867"	"CN1CCN(c2cncc(Nc3nc4c(-c5ccc(S(C)(=O)=O)cc5)cccn4n3)n2)CC1"	"IC50"	"'='"	"29.92"	"nM"	"7.52"	""	"216535"	"UO_0000065"	"16.20"	"0.31"	"5.43"	"6.93"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642315"	""	"0"	"476.61"	"0"	"3.29"	"BDBM99587"	"CN1CCN(Cc2ccc(Nc3nc4cccc(-c5ccc(S(C)(=O)=O)cc5)n4n3)cc2)CC1"	"IC50"	"'='"	"1.7"	"nM"	"8.77"	""	"216277"	"UO_0000065"	"18.40"	"0.35"	"5.48"	"10.59"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3645043"	""	"0"	"566.63"	"2"	"5.43"	"BDBM99810"	"CC(C)Oc1ccc(C(F)(F)F)cc1-c1cccn2nc(Nc3ccc4c(c3)CCN(CC(=O)N(C)C)CC4)nc12"	"IC50"	"'='"	"1205.98"	"nM"	"5.92"	""	"216483"	"UO_0000065"	"10.45"	"0.20"	"0.49"	"7.89"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL4517645"	""	"0"	"377.44"	"0"	"3.79"	"21"	"CCc1cc(O)c(F)cc1-c1cc(NS(=O)(=O)C(C)C)c2cn[nH]c2c1"	"IC50"	"'='"	"7.943"	"nM"	"8.10"	""	""	"UO_0000065"	"21.46"	"0.43"	"4.31"	"8.52"	"False"	"CHEMBL4478762"	"Inhibition of human His-tagged JAK2 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4477220"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2016"	"None"	""
"CHEMBL4567359"	""	"0"	"303.34"	"0"	"2.31"	"2"	"CS(=O)(=O)Nc1cc(-c2ccc(O)cc2)cc2[nH]ncc12"	"IC50"	"'='"	"19.95"	"nM"	"7.70"	""	""	"UO_0000065"	"25.38"	"0.50"	"5.39"	"8.10"	"False"	"CHEMBL4478762"	"Inhibition of human His-tagged JAK2 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4477220"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2016"	"None"	""
"CHEMBL3814195"	""	"0"	"301.39"	"0"	"0.95"	"3g"	"NCCCn1c(C2CCNCC2)nc2cc(C(N)=O)ccc21"	"IC50"	"'='"	"27300.0"	"nM"	"4.56"	""	""	"UO_0000065"	"15.14"	"0.28"	"3.61"	"4.61"	"False"	"CHEMBL3817413"	"Inhibition of JAK2 (unknown origin) using tyrosine 6 peptide as substrate by z'-lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3813615"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3593587"	""	"0"	"335.39"	"0"	"0.80"	"10a"	"CS(=O)(=O)N1CCC(n2c(=O)[nH]c3cnc4[nH]ccc4c32)CC1"	"IC50"	"'='"	"140.0"	"nM"	"6.85"	""	""	"UO_0000065"	"20.44"	"0.41"	"6.05"	"6.60"	"False"	"CHEMBL3594576"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate and ATP incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593193"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3593429"	""	"0"	"242.28"	"0"	"2.32"	"6b"	"O=c1[nH]c2cnc3[nH]ccc3c2n1C1CCCC1"	"IC50"	"'='"	"97.0"	"nM"	"7.01"	""	""	"UO_0000065"	"28.95"	"0.53"	"4.69"	"10.55"	"False"	"CHEMBL3594576"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate and ATP incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593193"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3699499"	""	"0"	"457.43"	"0"	"2.24"	"BDBM147516"	"N#C[C@H]1C[C@@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"285895"	"UO_0000065"	"19.02"	"0.38"	"6.46"	"5.76"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652407"	""	"0"	"463.65"	"0"	"3.42"	"BDBM113219"	"CC(C)COC1CCCN(S(=O)(=O)C[C@H]2CC[C@H](N(C)c3ncnc4[nH]ccc34)CC2)C1"	"IC50"	"'='"	"0.00767"	"nM"	""	"Outside typical range"	"234662"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL1834657"	"INFIGRATINIB PHOSPHATE"	"4"	"658.48"	"2"	"5.35"	"1h, NVP-BGJ398"	"CCN1CCN(c2ccc(Nc3cc(N(C)C(=O)Nc4c(Cl)c(OC)cc(OC)c4Cl)ncn3)cc2)CC1.O=P(O)(O)O"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1839909"	"Inhibition of recombinant JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833940"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL3647741"	""	"0"	"496.52"	"0"	"2.96"	"BDBM147844"	"N#C[C@H]1C[C@@H](N2CCC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"285778"	"UO_0000065"	"16.91"	"0.34"	"5.44"	"6.26"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3694590"	""	"0"	"445.75"	"1"	"5.57"	"BDBM125911"	"Clc1cnc2nc1NCc1cc(ccc1Br)OCCCc1cccc(c1)N2"	"IC50"	"'='"	"91.0"	"nM"	"7.04"	""	"255684"	"UO_0000065"	"15.80"	"0.36"	"1.47"	"11.92"	"False"	"CHEMBL3707544"	"In Vitro Kinase Assay: One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Biochemistry 1999, 269, 94-104. The catalytic domains of human JAK1 (a.a. 837-1142), JAK2 (a.a. 828-1132) and JAK3 (a.a. 781-1124) with an N-terminal His tag were expressed using baculovirus in insect cells and purified. The catalytic activity of JAK1, JAK2 or JAK3 was assayed by measuring the phosphorylation of a biotinylated peptide. The phosphorylated peptide was detected by homogenous time resolved fluorescence (HTRF). IC50s of compounds were measured for each kinase in the reactions that contain the enzyme, ATP and 500 nM peptide in 50 mM Tris (pH 7.8) buffer with 100 mM NaCl, 5 mM DTT, and 0.1 mg/mL (0.01%) BSA. The ATP concentration in the reactions was 90 uM for JAK1, 30 uM for JAK2 and 3 uM for JAK3. Reactions were carried out at room temperature for 1 hr and then stopped with 20 uL 45 mM EDTA."	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639093"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3703070"	""	"0"	"398.90"	"0"	"3.32"	"BDBM147781"	"N#C[C@H]1C[C@@H](N2CCC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"41.0"	"nM"	"7.39"	""	"285715"	"UO_0000065"	"18.52"	"0.36"	"4.07"	"7.39"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642365"	""	"0"	"506.63"	"1"	"3.05"	"BDBM99641"	"C[C@H](O)CN1CCN(c2cccc(Nc3nc4c(-c5ccc(S(C)(=O)=O)cc5)cccn4n3)c2)CC1"	"IC50"	"'='"	"0.75"	"nM"	"9.12"	""	"216331"	"UO_0000065"	"18.01"	"0.35"	"6.07"	"8.85"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL1835071"	""	"0"	"342.40"	"0"	"1.16"	"20"	"Cc1ccc(Nc2nc(N[C@@H]3CCOC[C@@H]3N)ncc2C(N)=O)cc1"	"IC50"	"'='"	"1584.89"	"nM"	"5.80"	""	""	"UO_0000065"	"16.94"	"0.32"	"4.64"	"4.52"	"False"	"CHEMBL1838267"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833860"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL3910814"	""	"0"	"419.55"	"0"	"2.25"	"BDBM255028"	"CCN1CN([C@H]2CC[C@H](CN(C)S(C)(=O)=O)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"23.0"	"nM"	"7.64"	""	"443884"	"UO_0000065"	"18.21"	"0.36"	"5.39"	"8.52"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3984749"	""	"0"	"417.54"	"0"	"2.01"	"BDBM254982"	"CN1CN([C@H]2CC[C@H](CN3CCCS3(=O)=O)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"0.62"	"nM"	"9.21"	""	"443889"	"UO_0000065"	"22.05"	"0.43"	"7.20"	"10.28"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3593581"	""	"0"	"270.34"	"0"	"2.96"	"6g"	"CC1CCCC(n2c(=O)[nH]c3cnc4[nH]ccc4c32)C1"	"IC50"	"'='"	"23.0"	"nM"	"7.64"	""	""	"UO_0000065"	"28.25"	"0.52"	"4.68"	"11.49"	"False"	"CHEMBL3594576"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate and ATP incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593193"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3647888"	""	"0"	"462.89"	"0"	"3.34"	"BDBM148000"	"N#C[C@@H]1C[C@H](C(=O)N2CC(F)(F)C2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"28.0"	"nM"	"7.55"	""	"285935"	"UO_0000065"	"16.32"	"0.32"	"4.21"	"6.45"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3593582"	""	"0"	"270.34"	"0"	"2.96"	"6h"	"CC1CCC(n2c(=O)[nH]c3cnc4[nH]ccc4c32)CC1"	"IC50"	"'='"	"23.0"	"nM"	"7.64"	""	""	"UO_0000065"	"28.25"	"0.52"	"4.68"	"11.49"	"False"	"CHEMBL3594576"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate and ATP incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593193"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3593772"	""	"0"	"404.40"	"0"	"3.16"	"11c"	"NC(=O)c1cnc2[nH]ccc2c1NC1CCN(c2ccc(C(F)(F)F)cn2)CC1"	"IC50"	"'='"	"370.0"	"nM"	"6.43"	""	""	"UO_0000065"	"15.90"	"0.30"	"3.27"	"6.44"	"False"	"CHEMBL3594790"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593212"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3593765"	""	"0"	"349.44"	"0"	"2.74"	"7b"	"NC(=O)c1cnc2[nH]ccc2c1NC1CCN(Cc2ccccc2)CC1"	"IC50"	"'='"	"84.0"	"nM"	"7.08"	""	""	"UO_0000065"	"20.25"	"0.37"	"4.34"	"8.13"	"True"	"CHEMBL3594790"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593212"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL231925"	""	"0"	"499.55"	"0"	"2.84"	"23"	"CN1CCN(C(=O)c2cc3c(NCc4ccccc4F)nc(-n4cnc5ccncc54)nc3n2C)CC1"	"IC50"	"'='"	"1860.0"	"nM"	"5.73"	""	""	"UO_0000065"	"11.47"	"0.21"	"2.89"	"5.91"	"False"	"CHEMBL897052"	"Inhibition of JAK2 by kinase-Glo luminescent assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1148837"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2007"	"None"	""
"CHEMBL3593767"	""	"0"	"349.44"	"0"	"2.74"	"7d"	"NC(=O)c1cnc2[nH]ccc2c1N[C@H]1CCCN(Cc2ccccc2)C1"	"IC50"	"'='"	"640.0"	"nM"	"6.19"	""	""	"UO_0000065"	"17.72"	"0.33"	"3.45"	"7.12"	"False"	"CHEMBL3594790"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593212"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3665209"	""	"0"	"514.61"	"1"	"1.94"	"BDBM112609"	"CS(=O)(=O)N1CCC[C@H](Nc2nc(N3CCC(CC(=O)O)CC3)ncc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.1131"	"nM"	"9.95"	""	"233846"	"UO_0000065"	"19.33"	"0.38"	"8.01"	"6.32"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647809"	""	"0"	"416.91"	"0"	"2.85"	"BDBM147912"	"COCCN[C@H]1CCC(n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"23.0"	"nM"	"7.64"	""	"285846"	"UO_0000065"	"18.32"	"0.36"	"4.79"	"6.47"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642330"	""	"0"	"530.58"	"1"	"4.31"	"BDBM99602"	"CN1CCN(c2ccc(Nc3nc4c(-c5ccc(S(C)(=O)=O)cc5)cc(C(F)(F)F)cn4n3)cc2)CC1"	"IC50"	"'='"	"9999.0"	"nM"	"5.00"	""	"216292"	"UO_0000065"	"9.42"	"0.18"	"0.69"	"6.04"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3639438"	""	"0"	"488.53"	"0"	"4.06"	"BDBM99706"	"CCN1CCN(c2cccc(Nc3nc4c(-c5ccc(P(C)(C)=O)cc5)cccn4n3)c2)C(=O)C1"	"IC50"	"'='"	"13.19"	"nM"	"7.88"	""	"216396"	"UO_0000065"	"16.13"	"0.31"	"3.82"	"9.51"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3665144"	""	"0"	"414.54"	"0"	"2.88"	"BDBM112532"	"CC(C)S(=O)(=O)N1C[C@@H](C)C[C@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.2226"	"nM"	"9.65"	""	"233771"	"UO_0000065"	"23.28"	"0.45"	"6.77"	"9.29"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647908"	""	"0"	"442.95"	"0"	"3.77"	"BDBM148020"	"CC(C)(C)NC(=O)[C@@H]1CC[C@@H](n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@H](C#N)C1"	"IC50"	"'='"	"425.0"	"nM"	"6.37"	""	"285955"	"UO_0000065"	"14.38"	"0.28"	"2.60"	"5.06"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645054"	""	"0"	"439.44"	"0"	"4.81"	"BDBM99821"	"COc1ccc(C(F)(F)F)cc1-c1cccn2nc(Nc3ccc4c(c3)CCNC4)nc12"	"IC50"	"'='"	"41.87"	"nM"	"7.38"	""	"216494"	"UO_0000065"	"16.79"	"0.31"	"2.57"	"11.62"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647768"	""	"0"	"514.47"	"1"	"4.91"	"BDBM147871"	"N#C[C@H]1C[C@H](N[C@@H](C2CC2)C(F)(F)F)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"375.0"	"nM"	"6.43"	""	"285805"	"UO_0000065"	"12.49"	"0.24"	"1.52"	"5.91"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645540"	""	"0"	"288.31"	"0"	"3.15"	"BDBM107124"	"N#CCC(=O)Nc1cccc(-c2cnc3ccccc3n2)c1"	"IC50"	"'='"	"18100.0"	"nM"	"4.74"	""	"226361"	"UO_0000065"	"16.45"	"0.29"	"1.59"	"6.03"	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642412"	""	"0"	"520.62"	"1"	"2.18"	"BDBM99690"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4cccc([C@@H]5CCN(CC(N)=O)C[C@@H]5O)c4)nc23)cc1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"216379"	"UO_0000065"	"17.79"	"0.34"	"7.08"	"6.48"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3644990"	""	"0"	"513.52"	"1"	"4.88"	"BDBM99742"	"COc1ccc(C(F)(F)F)cc1-c1cccn2nc(Nc3ccc(OCCN4CCOCC4)cc3)nc12"	"IC50"	"'='"	"84.5"	"nM"	"7.07"	""	"216430"	"UO_0000065"	"13.77"	"0.26"	"2.19"	"9.67"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3665137"	""	"0"	"336.40"	"0"	"2.44"	"BDBM112524"	"CCC(=O)N1CC[C@@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.0847"	"nM"	"10.07"	""	"233763"	"UO_0000065"	"29.94"	"0.55"	"7.63"	"11.60"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3650980"	""	"0"	"282.30"	"0"	"2.38"	"BDBM153154"	"CCOC(=O)c1c[nH]c2ncnc(-c3ccc(N)cc3)c12"	"IC50"	"'='"	"53.0"	"nM"	"7.28"	""	"294102"	"UO_0000065"	"25.77"	"0.47"	"4.90"	"7.75"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL246356"	""	"0"	"528.47"	"2"	"5.57"	"5"	"CNc1ncnc(-c2cccnc2Oc2cc(NC(=O)c3cccc(OC(F)(F)C(F)F)c3)ccc2C)n1"	"IC50"	"'='"	"1746.0"	"nM"	"5.76"	""	""	"UO_0000065"	"10.90"	"0.21"	"0.19"	"5.18"	"False"	"CHEMBL887085"	"Inhibition of Jak2 by radioactive filtration assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139197"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2007"	"None"	""
"CHEMBL3647718"	""	"0"	"378.48"	"0"	"2.91"	"BDBM147820"	"CC1CN([C@H]2CC[C@H](n3cc(C(N)=O)c(Nc4ccccc4)n3)[C@@H](C#N)C2)C1"	"IC50"	"'='"	"44.0"	"nM"	"7.36"	""	"285754"	"UO_0000065"	"19.44"	"0.36"	"4.45"	"7.36"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699527"	""	"0"	"388.27"	"0"	"3.74"	"BDBM147545"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Br)cc2)n1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	"285475"	"UO_0000065"	"20.50"	"0.45"	"4.22"	"8.23"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3644967"	""	"0"	"294.24"	"0"	"3.20"	"BDBM99717"	"Oc1cccn2nc(Nc3ccc(C(F)(F)F)cc3)nc12"	"IC50"	"'='"	"2999.0"	"nM"	"5.52"	""	"216407"	"UO_0000065"	"18.77"	"0.36"	"2.32"	"8.84"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3699558"	""	"0"	"476.50"	"0"	"3.94"	"BDBM147577"	"CC(C)(C(=O)NCC(F)(F)F)c1ccc(Nc2nn([C@H]3CCCC[C@@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"0.66"	"nM"	"9.18"	""	"285507"	"UO_0000065"	"19.27"	"0.37"	"5.24"	"7.30"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642377"	""	"0"	"429.53"	"0"	"3.95"	"BDBM99653"	"c1cncc(CNc2cccn3nc(Nc4ccc(OCCN5CCCC5)cc4)nc23)c1"	"IC50"	"'='"	"570.68"	"nM"	"6.24"	""	"216343"	"UO_0000065"	"14.54"	"0.27"	"2.29"	"7.84"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3702566"	""	"0"	"417.47"	"0"	"4.84"	"BDBM139539"	"Cn1c(=O)c(Sc2ccc(F)cc2)cc2cnc(Nc3ccc4[nH]ccc4c3)nc21"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	"273860"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707840"	"Kinase Inhibition Assay: The compound of Example 39, 2-(1H-indol-5-ylamino)-6-(2,4-difluorophenylsulfonyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one, was subjected to a kinase inhibition assay for the kinases. Compounds were tested in 5 dose IC50 mode with 10-fold serial dilution starting at 10 μM. Staurosporine, a known protein kinase inhibitor, was tested in 5-dose IC50 mode with 3-fold serial dilution starting at 20 μM. Reactions were carried out in 10 μM ATP. The results are shown in Table 5. The results show that the compound of Example 39 is a kinase inhibitor highly selective for the kinase Plk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639034"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL231733"	""	"0"	"520.60"	"1"	"3.89"	"15"	"C[C@H](Nc1nc(-n2cnc3ccncc32)nc2c1cc(C(=O)NCCCn1ccnc1)n2C)c1ccccc1"	"IC50"	"'='"	"53.0"	"nM"	"7.28"	""	""	"UO_0000065"	"13.98"	"0.25"	"3.39"	"6.04"	"False"	"CHEMBL897052"	"Inhibition of JAK2 by kinase-Glo luminescent assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1148837"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2007"	"None"	""
"CHEMBL3655080"	""	"0"	"363.37"	"0"	"1.41"	"BDBM159747"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)CC(F)(F)F)C1"	"IC50"	"'='"	"381.0"	"nM"	"6.42"	""	"302557"	"UO_0000065"	"17.67"	"0.37"	"5.01"	"7.06"	"True"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699551"	""	"0"	"408.38"	"0"	"2.97"	"BDBM147569"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc([C@H](O)C(F)(F)F)nc2)n1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"285499"	"UO_0000065"	"21.30"	"0.41"	"5.73"	"6.70"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642296"	""	"0"	"491.62"	"0"	"3.29"	"BDBM99565"	"CN1CCN(c2cccc(Nc3nc4c(-c5ccc(N(C)S(C)(=O)=O)cc5)cccn4n3)c2)CC1"	"IC50"	"'='"	"0.6"	"nM"	"9.22"	""	"216255"	"UO_0000065"	"18.76"	"0.36"	"5.93"	"10.71"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3651023"	""	"0"	"413.44"	"0"	"3.85"	"BDBM153200"	"CCOC(=O)c1c[nH]c2ncnc(-c3cccc(NC(=O)/C=C/c4ccccn4)c3)c12"	"IC50"	"'='"	"452.0"	"nM"	"6.34"	""	"294148"	"UO_0000065"	"15.35"	"0.28"	"2.49"	"5.78"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699495"	""	"0"	"354.39"	"0"	"2.90"	"BDBM147511"	"N#C[C@@H]1CC2(CCC1n1cc(C(N)=O)c(Nc3ccnc(F)c3)n1)CC2"	"IC50"	"'='"	"19.0"	"nM"	"7.72"	""	"285439"	"UO_0000065"	"21.79"	"0.41"	"4.82"	"7.04"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702991"	""	"0"	"433.44"	"0"	"3.08"	"BDBM147701"	"N#C[C@H]1C[C@@H](N2CCC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)nc2)n1"	"IC50"	"'='"	"75.0"	"nM"	"7.12"	""	"285635"	"UO_0000065"	"16.44"	"0.31"	"4.04"	"6.31"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642417"	""	"0"	"517.66"	"1"	"3.79"	"BDBM99695"	"CN1CCN(c2ccc(Nc3nc4c(/C=C/c5ccccc5N(C)S(C)(=O)=O)cccn4n3)cc2)CC1"	"IC50"	"'='"	"32.09"	"nM"	"7.49"	""	"216384"	"UO_0000065"	"14.48"	"0.28"	"3.70"	"8.71"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642297"	""	"0"	"452.48"	"0"	"4.91"	"BDBM99566"	"CN1CCN(c2ccc(Nc3nc4c(-c5ccc(C(F)(F)F)cc5)cccn4n3)cc2)CC1"	"IC50"	"'='"	"3.1"	"nM"	"8.51"	""	"216256"	"UO_0000065"	"18.80"	"0.35"	"3.60"	"17.47"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3699463"	""	"0"	"309.37"	"0"	"3.13"	"BDBM147478"	"[C-]#[N+][C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccccc2)n1"	"IC50"	"'='"	"36.0"	"nM"	"7.44"	""	"285403"	"UO_0000065"	"24.06"	"0.44"	"4.31"	"9.63"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3655101"	""	"0"	"378.46"	"0"	"0.23"	"BDBM159768"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)N2C[C@@H]3C[C@H](C2)O3)C1"	"IC50"	"'='"	"1150.0"	"nM"	"5.94"	""	"302578"	"UO_0000065"	"15.69"	"0.31"	"5.71"	"5.74"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647779"	""	"0"	"412.93"	"0"	"3.75"	"BDBM147882"	"CC1(N[C@@H]2CCC(n3cc(C(N)=O)c(Nc4ccc(Cl)cc4)n3)[C@@H](C#N)C2)CC1"	"IC50"	"'='"	"195.0"	"nM"	"6.71"	""	"285816"	"UO_0000065"	"16.25"	"0.32"	"2.96"	"6.17"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651015"	""	"0"	"354.34"	"0"	"3.22"	"BDBM153191"	"C=C(F)C(=O)Nc1cccc(-c2ncnc3[nH]cc(C(=O)OCC)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294139"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3658095"	""	"0"	"603.77"	"2"	"6.03"	"BDBM148361"	"Cc1ccc(NC(=O)c2cccc(C(C)(C)C)c2)cc1N1CCc2nc(Nc3ccc(N4CCN(C)CC4)cc3)ncc2C1=O"	"IC50"	"'='"	"45.0"	"nM"	"7.35"	""	"286781"	"UO_0000065"	"12.17"	"0.22"	"1.32"	"7.84"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699545"	""	"0"	"344.81"	"0"	"3.03"	"BDBM147563"	"N#C[C@@H]1CCCC[C@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)nc2)n1"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	"285493"	"UO_0000065"	"22.46"	"0.44"	"4.71"	"7.07"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702884"	""	"0"	"397.46"	"0"	"2.74"	"BDBM147583"	"N#C[C@H]1CCCCC1n1cc(C(N)=O)c(Nc2ccc3c(c2)C=CS3(=O)=O)n1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	"285513"	"UO_0000065"	"20.02"	"0.39"	"5.22"	"6.08"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651016"	""	"0"	"348.36"	"0"	"2.76"	"BDBM153193"	"CC#CC(=O)Nc1cccc(-c2ncnc3[nH]cc(C(=O)OCC)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294141"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665212"	""	"0"	"485.62"	"0"	"1.39"	"BDBM112612"	"CCN1CCN(c2ncc(-c3cnc4[nH]ccc4n3)c(N[C@H]3CCCN(S(C)(=O)=O)C3)n2)CC1"	"IC50"	"'='"	"0.2125"	"nM"	"9.67"	""	"233849"	"UO_0000065"	"19.92"	"0.39"	"8.28"	"7.85"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3665181"	""	"0"	"458.59"	"0"	"2.34"	"BDBM112575"	"CC(C)CS(=O)(=O)N1CCC[C@H](Nc2nc(N(C)C)ncc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.0549"	"nM"	"10.26"	""	"233812"	"UO_0000065"	"22.37"	"0.44"	"7.92"	"8.55"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3651063"	""	"0"	"362.43"	"0"	"4.03"	"BDBM47235"	"C=C(C)C(=O)Nc1cccc(-c2ncnc3[nH]cc(C4CCOCC4)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"198769"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3644983"	""	"0"	"484.60"	"0"	"4.03"	"BDBM99734"	"CCOc1ccccc1-c1cccn2nc(Nc3ccc4c(c3)CCN(CC(=O)N(C)C)CC4)nc12"	"IC50"	"'='"	"212.47"	"nM"	"6.67"	""	"216423"	"UO_0000065"	"13.77"	"0.25"	"2.64"	"8.90"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647754"	""	"0"	"536.58"	"1"	"3.88"	"BDBM147857"	"N#C[C@H]1CC(N(C2CC2)C2CC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	"285791"	"UO_0000065"	"14.53"	"0.29"	"3.92"	"5.81"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3644985"	""	"0"	"520.54"	"1"	"3.95"	"BDBM99736"	"CN(C)C(=O)CN1CCc2ccc(Nc3nc4c(-c5cccc6c5OC(F)(F)O6)cccn4n3)cc2CC1"	"IC50"	"'='"	"30.41"	"nM"	"7.52"	""	"216425"	"UO_0000065"	"14.44"	"0.27"	"3.57"	"8.92"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3650683"	""	"0"	"387.47"	"0"	"2.38"	"BDBM47170"	"CS(=O)(=O)c1ccc(Nc2nn([C@@H]3CCCC[C@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"285970"	"UO_0000065"	"22.00"	"0.43"	"6.14"	"6.51"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647902"	""	"0"	"470.96"	"0"	"3.01"	"BDBM148014"	"CC1(CNC(=O)[C@@H]2CC[C@@H](n3cc(C(N)=O)c(Nc4ccc(Cl)cc4)n3)[C@H](C#N)C2)COC1"	"IC50"	"'>'"	"500.0"	"nM"	""	""	"285949"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652311"	""	"0"	"416.55"	"0"	"2.52"	"BDBM113121"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@@H](CS(=O)(=O)N2CCC[C@H](C#N)C2)CC1"	"IC50"	"'='"	"75.4"	"nM"	"7.12"	""	"234564"	"UO_0000065"	"17.10"	"0.34"	"4.60"	"6.72"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3702976"	""	"0"	"538.47"	"1"	"3.40"	"BDBM147686"	"N#C[C@H]1C[C@@H](NCC(F)(F)F)CCC1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"285619"	"UO_0000065"	"15.27"	"0.31"	"4.82"	"5.75"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699473"	""	"0"	"325.37"	"0"	"1.95"	"BDBM147488"	"N#C[C@@H]1C(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCC[C@@H]1O"	"IC50"	"'='"	"49.0"	"nM"	"7.31"	""	"285413"	"UO_0000065"	"22.47"	"0.42"	"5.36"	"6.25"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL2062801"	""	"0"	"442.52"	"0"	"2.95"	"BDBM99611"	"CS(=O)(=O)c1ccc(Nc2nc3c(-c4ccc(S(C)(=O)=O)cc4)cccn3n2)cc1"	"IC50"	"'='"	"1.3"	"nM"	"8.89"	""	"216301"	"UO_0000065"	"20.08"	"0.40"	"5.94"	"8.04"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3650683"	""	"0"	"387.47"	"0"	"2.38"	"BDBM47170"	"CS(=O)(=O)c1ccc(Nc2nn([C@@H]3CCCC[C@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"285973"	"UO_0000065"	"21.05"	"0.41"	"5.77"	"6.23"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665153"	""	"0"	"460.99"	"0"	"3.60"	"BDBM112544"	"Cc1ccc(-c2cnc3[nH]cc(Cl)c3n2)c(NC2CCCN(S(=O)(=O)CC3CC3)C2)n1"	"IC50"	"'='"	"0.1543"	"nM"	"9.81"	""	"233783"	"UO_0000065"	"21.28"	"0.43"	"6.21"	"9.45"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3702923"	""	"0"	"376.37"	"0"	"2.98"	"BDBM147622"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(OC(F)F)nc2)n1"	"IC50"	"'='"	"39.0"	"nM"	"7.41"	""	"285552"	"UO_0000065"	"19.69"	"0.37"	"4.43"	"6.23"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703499"	""	"0"	"285.28"	"0"	"2.94"	"BDBM153143"	"CCOC(=O)c1c[nH]c2ncnc(-c3cccc(F)c3)c12"	"IC50"	"'='"	"121.0"	"nM"	"6.92"	""	"294091"	"UO_0000065"	"24.25"	"0.45"	"3.98"	"10.19"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651065"	""	"0"	"345.36"	"0"	"3.79"	"BDBM47237"	"C=C(C)C(=O)Nc1cccc(-c2ncnc3[nH]cc(-c4cnco4)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"198773"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665145"	""	"0"	"350.43"	"0"	"2.75"	"BDBM112534"	"CC(=O)N1CCCC(Nc2nc(C)ccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.0876"	"nM"	"10.06"	""	"233773"	"UO_0000065"	"28.70"	"0.53"	"7.31"	"11.59"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3645035"	""	"0"	"538.57"	"1"	"4.66"	"BDBM99801"	"COc1ccc(C(F)(F)F)cc1-c1cccn2nc(Nc3ccc4c(c3)CCN(CC(=O)N(C)C)CC4)nc12"	"IC50"	"'='"	"54.48"	"nM"	"7.26"	""	"216475"	"UO_0000065"	"13.49"	"0.25"	"2.60"	"9.69"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647909"	""	"0"	"468.95"	"0"	"2.72"	"BDBM148021"	"N#C[C@@H]1C[C@H](C(=O)N2CC3(COC3)C2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"111.0"	"nM"	"6.96"	""	"285956"	"UO_0000065"	"14.83"	"0.29"	"4.23"	"5.51"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647787"	""	"0"	"406.53"	"0"	"3.74"	"BDBM147890"	"CC(C)(N[C@H]1CCC(n2cc(C(N)=O)c(Nc3ccccc3)n2)[C@@H](C#N)C1)C1CC1"	"IC50"	"'='"	"38.0"	"nM"	"7.42"	""	"285824"	"UO_0000065"	"18.25"	"0.34"	"3.68"	"6.82"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703028"	""	"0"	"415.45"	"0"	"3.00"	"BDBM147738"	"N#C[C@H]1C[C@H](N2CCC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)F)nc2)n1"	"IC50"	"'='"	"47.0"	"nM"	"7.33"	""	"285672"	"UO_0000065"	"17.64"	"0.33"	"4.33"	"6.49"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3694579"	""	"0"	"387.85"	"0"	"3.60"	"BDBM125900"	"O=S1(=O)Nc2cccc(c2)CNc2nc(ncc2Cl)Nc2cccc1c2"	"IC50"	"'='"	"589.0"	"nM"	"6.23"	""	"255673"	"UO_0000065"	"16.06"	"0.33"	"2.63"	"6.49"	"False"	"CHEMBL3707544"	"In Vitro Kinase Assay: One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Biochemistry 1999, 269, 94-104. The catalytic domains of human JAK1 (a.a. 837-1142), JAK2 (a.a. 828-1132) and JAK3 (a.a. 781-1124) with an N-terminal His tag were expressed using baculovirus in insect cells and purified. The catalytic activity of JAK1, JAK2 or JAK3 was assayed by measuring the phosphorylation of a biotinylated peptide. The phosphorylated peptide was detected by homogenous time resolved fluorescence (HTRF). IC50s of compounds were measured for each kinase in the reactions that contain the enzyme, ATP and 500 nM peptide in 50 mM Tris (pH 7.8) buffer with 100 mM NaCl, 5 mM DTT, and 0.1 mg/mL (0.01%) BSA. The ATP concentration in the reactions was 90 uM for JAK1, 30 uM for JAK2 and 3 uM for JAK3. Reactions were carried out at room temperature for 1 hr and then stopped with 20 uL 45 mM EDTA."	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639093"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3645112"	""	"0"	"360.42"	"0"	"3.80"	"BDBM99886"	"COc1cccc(CNc2cccn3nc(Nc4ccc(C)nc4)nc23)c1"	"IC50"	"'='"	"1018.22"	"nM"	"5.99"	""	"216554"	"UO_0000065"	"16.63"	"0.30"	"2.19"	"7.85"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3702892"	""	"0"	"409.49"	"0"	"2.90"	"BDBM147591"	"CC(C)(C)NC(=O)c1cncc(Nc2nn([C@H]3CCCC[C@@H]3C#N)cc2C(N)=O)c1"	"IC50"	"'='"	"285.0"	"nM"	"6.54"	""	"285521"	"UO_0000065"	"15.98"	"0.30"	"3.65"	"4.72"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665179"	""	"0"	"415.52"	"0"	"2.28"	"BDBM112573"	"CC(C)CS(=O)(=O)N1CCC[C@H](Nc2ncncc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.0581"	"nM"	"10.24"	""	"233810"	"UO_0000065"	"24.63"	"0.48"	"7.96"	"8.77"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642411"	""	"0"	"553.71"	"1"	"3.77"	"BDBM99689"	"CS(=O)(=O)CCN1CCC(c2cccc(Nc3nc4c(-c5ccc(S(C)(=O)=O)cc5)cccn4n3)c2)CC1"	"IC50"	"'='"	"0.46"	"nM"	"9.34"	""	"216378"	"UO_0000065"	"16.86"	"0.34"	"5.57"	"8.21"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642346"	""	"0"	"520.66"	"1"	"3.69"	"BDBM99622"	"CN1CCC(c2ccc(Nc3nc4c(NCc5cccnc5N(C)S(C)(=O)=O)cccn4n3)cc2)CC1"	"IC50"	"'='"	"40.28"	"nM"	"7.39"	""	"216312"	"UO_0000065"	"14.20"	"0.27"	"3.70"	"6.86"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647919"	""	"0"	"380.45"	"0"	"3.50"	"BDBM148031"	"[C-]#[N+][C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(/C(C)=N/OC)cc2)n1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"285968"	"UO_0000065"	"22.86"	"0.42"	"5.20"	"8.80"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645031"	""	"0"	"533.08"	"2"	"5.07"	"BDBM99792"	"CCCOc1ccc(Cl)cc1-c1cccn2nc(Nc3ccc4c(c3)CCN(CC(=O)N(C)C)CC4)nc12"	"IC50"	"'='"	"365.41"	"nM"	"6.44"	""	"216471"	"UO_0000065"	"12.08"	"0.23"	"1.37"	"8.58"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3699501"	""	"0"	"344.35"	"0"	"1.49"	"BDBM147518"	"N#C[C@H]1C[C@H](O)CCC1n1cc(C(N)=O)c(Nc2ccnc(F)c2)n1"	"IC50"	"'='"	"46.0"	"nM"	"7.34"	""	"285448"	"UO_0000065"	"21.31"	"0.40"	"5.85"	"5.65"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665221"	""	"0"	"403.49"	"0"	"2.82"	"BDBM112621"	"C[C@H]1C[C@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)CN(C2(CC#N)COC2)C1"	"IC50"	"'='"	"0.5116"	"nM"	"9.29"	""	"233858"	"UO_0000065"	"23.03"	"0.42"	"6.47"	"9.04"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3694581"	""	"0"	"366.85"	"0"	"4.81"	"BDBM125902"	"Clc1cnc2nc1NCc1cccc(c1)OCCCc1cccc(c1)N2"	"IC50"	"'='"	"1.9"	"nM"	"8.72"	""	"255675"	"UO_0000065"	"23.77"	"0.46"	"3.91"	"14.76"	"False"	"CHEMBL3707544"	"In Vitro Kinase Assay: One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Biochemistry 1999, 269, 94-104. The catalytic domains of human JAK1 (a.a. 837-1142), JAK2 (a.a. 828-1132) and JAK3 (a.a. 781-1124) with an N-terminal His tag were expressed using baculovirus in insect cells and purified. The catalytic activity of JAK1, JAK2 or JAK3 was assayed by measuring the phosphorylation of a biotinylated peptide. The phosphorylated peptide was detected by homogenous time resolved fluorescence (HTRF). IC50s of compounds were measured for each kinase in the reactions that contain the enzyme, ATP and 500 nM peptide in 50 mM Tris (pH 7.8) buffer with 100 mM NaCl, 5 mM DTT, and 0.1 mg/mL (0.01%) BSA. The ATP concentration in the reactions was 90 uM for JAK1, 30 uM for JAK2 and 3 uM for JAK3. Reactions were carried out at room temperature for 1 hr and then stopped with 20 uL 45 mM EDTA."	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639093"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3702942"	""	"0"	"393.37"	"0"	"2.97"	"BDBM147644"	"N#C[C@H]1C[C@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	"285576"	"UO_0000065"	"20.34"	"0.39"	"5.03"	"6.84"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665195"	""	"0"	"460.56"	"0"	"1.43"	"BDBM112593"	"CC(C)(O)CNc1ncc(-c2cnc3[nH]ccc3n2)c(N[C@H]2CCCN(S(C)(=O)=O)C2)n1"	"IC50"	"'='"	"0.1769"	"nM"	"9.75"	""	"233830"	"UO_0000065"	"21.17"	"0.42"	"8.32"	"6.54"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642344"	""	"0"	"511.63"	"1"	"2.77"	"BDBM99620"	"CS(=O)(=O)c1ccc(-c2cccc3nc(Nc4cccc(CN5CCS(=O)(=O)CC5)c4)nn23)cc1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"216310"	"UO_0000065"	"18.10"	"0.36"	"6.49"	"8.14"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3956439"	""	"0"	"421.47"	"0"	"3.66"	"BDBM255023"	"O=C1c2cnc3[nH]ccc3c2N([C@H]2CC[C@H](CNCC(F)(F)F)CC2)CN1C1CC1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	"443879"	"UO_0000065"	"18.88"	"0.36"	"4.30"	"12.39"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3645111"	""	"0"	"360.42"	"0"	"3.80"	"BDBM99885"	"COc1ccccc1CNc1cccn2nc(Nc3ccnc(C)c3)nc12"	"IC50"	"'='"	"24.7"	"nM"	"7.61"	""	"216553"	"UO_0000065"	"21.11"	"0.38"	"3.81"	"9.96"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647773"	""	"0"	"516.45"	"1"	"3.59"	"BDBM147876"	"N#C[C@H]1C[C@@H](N2CC(O)(C(F)(F)F)C2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"23.0"	"nM"	"7.64"	""	"285810"	"UO_0000065"	"14.79"	"0.29"	"4.05"	"6.35"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647757"	""	"0"	"524.57"	"1"	"3.64"	"BDBM147860"	"C[C@H](N[C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)(F)F)cc3)n2)[C@@H](C#N)C1)C1CC1"	"IC50"	"'='"	"23.0"	"nM"	"7.64"	""	"285794"	"UO_0000065"	"14.56"	"0.29"	"4.00"	"5.35"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665183"	""	"0"	"461.62"	"0"	"3.00"	"BDBM112577"	"CSc1ncc(-c2cnc3[nH]ccc3n2)c(N[C@H]2CCCN(S(=O)(=O)CC(C)C)C2)n1"	"IC50"	"'='"	"0.0764"	"nM"	"10.12"	""	"233814"	"UO_0000065"	"21.92"	"0.45"	"7.12"	"8.66"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3648442"	""	"0"	"356.41"	"0"	"1.91"	"BDBM107151"	"NS(=O)(=O)CCC(=O)Nc1cccc(-c2cnc3ccccc3n2)c1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	"226389"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3665160"	""	"0"	"414.54"	"0"	"2.65"	"BDBM112553"	"CCCS(=O)(=O)N1CCC[C@H](Nc2ncccc2-c2cnc3ccn(C)c3n2)C1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"233791"	"UO_0000065"	"21.71"	"0.42"	"6.35"	"9.68"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647738"	""	"0"	"520.48"	"1"	"3.11"	"BDBM147841"	"N#C[C@H]1C[C@@H](NCC(F)F)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"285775"	"UO_0000065"	"16.13"	"0.33"	"5.29"	"5.88"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651025"	""	"0"	"451.49"	"0"	"4.93"	"BDBM153202"	"CCOC(=O)c1c[nH]c2ncnc(-c3cccc(NC(=O)/C=C/c4c[nH]c5ccccc45)c3)c12"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294150"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652377"	""	"0"	"482.65"	"0"	"3.69"	"BDBM113188"	"Cc1cccc(C[C@H]2CCCN2S(=O)(=O)C[C@H]2CC[C@H](N(C)c3ncnc4[nH]ccc34)CC2)n1"	"IC50"	"'='"	"24.3"	"nM"	"7.61"	""	"234631"	"UO_0000065"	"15.78"	"0.31"	"3.92"	"8.01"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3702994"	""	"0"	"419.44"	"0"	"2.52"	"BDBM147704"	"CN(C)[C@@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(OC(F)F)nc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"100.0"	"nM"	"7.00"	""	"285638"	"UO_0000065"	"16.69"	"0.32"	"4.48"	"5.73"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702978"	""	"0"	"526.54"	"1"	"2.58"	"BDBM147688"	"N#C[C@H]1C[C@@H](N2CCOCC2)CCC1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"285621"	"UO_0000065"	"15.61"	"0.31"	"5.64"	"5.74"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647749"	""	"0"	"524.57"	"1"	"3.64"	"BDBM147852"	"CC(N[C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)(F)F)cc3)n2)[C@@H](C#N)C1)C1CC1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	"285786"	"UO_0000065"	"15.17"	"0.30"	"4.32"	"5.57"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645002"	""	"0"	"441.43"	"0"	"4.99"	"BDBM99754"	"Fc1ccc(C(F)(F)F)cc1-c1cccn2nc(Nc3ccc4c(c3)CCNCC4)nc12"	"IC50"	"'='"	"7.64"	"nM"	"8.12"	""	"216442"	"UO_0000065"	"18.39"	"0.35"	"3.13"	"14.96"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3645062"	""	"0"	"399.50"	"0"	"4.62"	"BDBM99830"	"COc1cccc(-c2cccn3nc(Nc4ccc(C5CCNCC5)cc4)nc23)c1"	"IC50"	"'='"	"7.6"	"nM"	"8.12"	""	"216503"	"UO_0000065"	"20.32"	"0.37"	"3.50"	"12.79"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL4449906"	""	"0"	"494.50"	"0"	"3.70"	"7m"	"Cc1cnc(Nc2cc(F)c(N3CCOCC3)c(F)c2)nc1-c1cc2c(o1)CCN(C(=O)CC#N)C2"	"IC50"	"'='"	"4.2"	"nM"	"8.38"	""	""	"UO_0000065"	"16.94"	"0.32"	"4.68"	"7.79"	"False"	"CHEMBL4341343"	"Inhibition of JAK2 (unknown origin) using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition and measured by 30 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4524343"	""	"0"	"471.57"	"0"	"3.34"	"7k"	"Cc1cnc(Nc2ccc(N3CCN(C)CC3)cc2)nc1-c1cc2c(o1)CCN(C(=O)CC#N)C2"	"IC50"	"'='"	"1.6"	"nM"	"8.80"	""	""	"UO_0000065"	"18.65"	"0.34"	"5.46"	"8.66"	"False"	"CHEMBL4341343"	"Inhibition of JAK2 (unknown origin) using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition and measured by 30 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL2105759"	"BARICITINIB"	"4"	"371.43"	"0"	"1.10"	"3"	"CCS(=O)(=O)N1CC(CC#N)(n2cc(-c3ncnc4[nH]ccc34)cn2)C1"	"IC50"	"'='"	"5.7"	"nM"	"8.24"	""	""	"UO_0000065"	"22.20"	"0.43"	"7.14"	"6.84"	"False"	"CHEMBL4341338"	"Inhibition of recombinant epitope tagged JAK2 kinase domain (828 to 1132 residues) (unknown origin) using peptide substrate by fluorescence based assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL3652373"	""	"0"	"469.62"	"0"	"2.64"	"BDBM113184"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC[C@H](Cc3cnccn3)C2)CC1"	"IC50"	"'='"	"28.6"	"nM"	"7.54"	""	"234627"	"UO_0000065"	"16.06"	"0.31"	"4.90"	"6.99"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL4453064"	""	"0"	"384.46"	"0"	"3.11"	"7a"	"Cc1cnc(Nc2ccccc2)nc1-c1cc2c(o1)CCN(S(C)(=O)=O)C2"	"IC50"	"'='"	"2222.0"	"nM"	"5.65"	""	""	"UO_0000065"	"14.70"	"0.29"	"2.54"	"6.40"	"False"	"CHEMBL4341349"	"Inhibition of JAK2 in human TF-1 cells assessed as reduction in GM-CSF-induced cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"CHEMBL3307972"	""
"CHEMBL4456396"	""	"0"	"505.55"	"1"	"3.22"	"7e"	"Cc1cnc(Nc2cc(F)c(N3CCOCC3)c(F)c2)nc1-c1cc2c(o1)CCN(S(C)(=O)=O)C2"	"IC50"	"'='"	"405.4"	"nM"	"6.39"	""	""	"UO_0000065"	"12.64"	"0.25"	"3.17"	"6.34"	"False"	"CHEMBL4341349"	"Inhibition of JAK2 in human TF-1 cells assessed as reduction in GM-CSF-induced cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"CHEMBL3307972"	""
"CHEMBL3703090"	""	"0"	"433.49"	"0"	"3.28"	"BDBM147804"	"N#C[C@H]1C[C@H](NCc2ccccc2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccnc(F)c2)n1"	"IC50"	"'='"	"56.0"	"nM"	"7.25"	""	"285738"	"UO_0000065"	"16.73"	"0.31"	"3.97"	"5.96"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642314"	""	"0"	"463.56"	"0"	"3.38"	"BDBM99586"	"CS(=O)(=O)c1ccc(-c2cccc3nc(Nc4ccc(CN5CCOCC5)cc4)nn23)cc1"	"IC50"	"'='"	"1.1"	"nM"	"8.96"	""	"216276"	"UO_0000065"	"19.33"	"0.37"	"5.58"	"10.09"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647928"	""	"0"	"367.41"	"0"	"2.76"	"BDBM148048"	"[C-]#[N+][C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(CC(=O)O)cc2)n1"	"IC50"	"'='"	"49.0"	"nM"	"7.31"	""	"285419"	"UO_0000065"	"19.90"	"0.37"	"4.55"	"6.38"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645088"	""	"0"	"580.66"	"2"	"5.68"	"BDBM99861"	"CC(C)COc1ccc(C(F)(F)F)cc1-c1cccn2nc(Nc3ccc4c(c3)CCN(CC(=O)N(C)C)CC4)nc12"	"IC50"	"'='"	"2999.0"	"nM"	"5.52"	""	"216530"	"UO_0000065"	"9.51"	"0.18"	"-0.16"	"7.36"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3644968"	""	"0"	"499.62"	"1"	"5.62"	"BDBM99718"	"COCc1ccccc1-c1cccc2nc(Nc3ccc4c(c3)CCN(C(=O)OC(C)(C)C)CC4)nn12"	"IC50"	"'='"	"650.29"	"nM"	"6.19"	""	"216408"	"UO_0000065"	"12.38"	"0.23"	"0.57"	"7.64"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3702988"	""	"0"	"461.49"	"0"	"3.76"	"BDBM147698"	"C[C@H](N[C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(C(F)(F)F)nc3)n2)[C@@H](C#N)C1)C1CC1"	"IC50"	"'='"	"200.0"	"nM"	"6.70"	""	"285632"	"UO_0000065"	"14.52"	"0.28"	"2.94"	"5.51"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645053"	""	"0"	"539.56"	"2"	"6.46"	"BDBM99820"	"COc1ccc(C(F)(F)F)cc1-c1cccn2nc(Nc3ccc4c(c3)CCN(C(=O)OC(C)(C)C)C4)nc12"	"IC50"	"'='"	"1148.54"	"nM"	"5.94"	""	"216493"	"UO_0000065"	"11.01"	"0.21"	"-0.52"	"7.33"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3651010"	""	"0"	"366.38"	"0"	"3.02"	"BDBM153186"	"C=C(C)C(=O)Nc1cc(-c2ncnc3[nH]cc(C(=O)OCC)c23)ccc1O"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294134"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3985528"	""	"0"	"341.39"	"0"	"2.83"	"BDBM254992"	"N#CCN1CN([C@H]2CC[C@H](CF)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"24.0"	"nM"	"7.62"	""	"443899"	"UO_0000065"	"22.32"	"0.42"	"4.79"	"10.02"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3949572"	""	"0"	"405.52"	"0"	"1.91"	"BDBM254993"	"CCN1CN([C@H]2CC[C@H](CNS(C)(=O)=O)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	"443900"	"UO_0000065"	"19.29"	"0.38"	"5.91"	"7.95"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3658112"	""	"0"	"555.73"	"2"	"5.63"	"BDBM148422"	"Cc1ccc(NC(=O)NC2CCCC2)cc1N1CCc2nc(Nc3ccc(OCCN4CCCC4)cc3)ncc2C1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"286817"	"UO_0000065"	"15.11"	"0.28"	"2.77"	"8.87"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703017"	""	"0"	"404.88"	"0"	"3.31"	"BDBM147727"	"CN(C)[C@@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(Cl)c(F)c3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"173.0"	"nM"	"6.76"	""	"285661"	"UO_0000065"	"16.70"	"0.33"	"3.45"	"6.76"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3650678"	""	"0"	"387.47"	"0"	"2.38"	"BDBM148060"	"CS(=O)(=O)c1ccc(Nc2nn([C@H]3CCCC[C@@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"27.0"	"nM"	"7.57"	""	"285971"	"UO_0000065"	"19.53"	"0.38"	"5.19"	"5.78"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702952"	""	"0"	"376.37"	"0"	"2.28"	"BDBM147654"	"N#C[C@H]1C[C@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)F)nc2)n1"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	"285586"	"UO_0000065"	"21.26"	"0.40"	"5.72"	"6.16"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702961"	""	"0"	"398.44"	"0"	"3.07"	"BDBM147668"	"[C-]#[N+][C@@H]1C[C@H](OCC2CC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccnc(F)c2)n1"	"IC50"	"'='"	"150.0"	"nM"	"6.82"	""	"285600"	"UO_0000065"	"17.13"	"0.32"	"3.75"	"6.86"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665176"	""	"0"	"388.45"	"0"	"0.83"	"BDBM112569"	"CS(=O)(=O)N1CC[C@@H](O)[C@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.0201"	"nM"	"10.70"	""	"233806"	"UO_0000065"	"27.54"	"0.54"	"9.87"	"8.62"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652403"	""	"0"	"491.66"	"0"	"3.34"	"BDBM113215"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCC[C@@H](OC(=O)C(C)(C)C)C2)CC1"	"IC50"	"'='"	"0.129"	"nM"	"9.89"	""	"234658"	"UO_0000065"	"20.11"	"0.40"	"6.55"	"9.12"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3647861"	""	"0"	"465.48"	"0"	"3.15"	"BDBM147971"	"CC(C)(c1ccc(Nc2nn([C@H]3CC[C@H](O)C[C@@H]3C#N)cc2C(N)=O)cc1)C(O)C(F)(F)F"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"285906"	"UO_0000065"	"18.31"	"0.35"	"5.37"	"6.21"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3955793"	""	"0"	"342.40"	"0"	"2.72"	"BDBM198205"	"CC(C)(C)OC(=O)N1CCCC(c2nnn3cnc4[nH]ccc4c23)C1"	"IC50"	"'='"	"250.0"	"nM"	"6.60"	""	"352287"	"UO_0000065"	"19.28"	"0.36"	"3.88"	"7.47"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3920352"	""	"0"	"400.41"	"0"	"4.00"	"BDBM198215"	"FC(F)(F)c1ccc(CN2CCCC(c3nnn4cnc5[nH]ccc5c34)C2)cc1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"352297"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3918854"	""	"0"	"416.41"	"0"	"3.88"	"BDBM198229"	"FC(F)(F)Oc1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"41.0"	"nM"	"7.39"	""	"352311"	"UO_0000065"	"17.74"	"0.34"	"3.51"	"10.35"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3975090"	""	"0"	"380.43"	"0"	"3.13"	"BDBM198238"	"COc1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cc1F"	"IC50"	"'='"	"170.0"	"nM"	"6.77"	""	"352320"	"UO_0000065"	"17.79"	"0.33"	"3.64"	"9.49"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3942741"	""	"0"	"273.32"	"0"	"2.85"	"BDBM198266"	"FC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	"352346"	"UO_0000065"	"28.74"	"0.54"	"5.00"	"13.34"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702999"	""	"0"	"461.49"	"0"	"3.76"	"BDBM147709"	"C[C@H](N[C@@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(C(F)(F)F)nc3)n2)[C@@H](C#N)C1)C1CC1"	"IC50"	"'='"	"675.0"	"nM"	"6.17"	""	"285643"	"UO_0000065"	"13.37"	"0.26"	"2.41"	"5.07"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665131"	""	"0"	"386.48"	"0"	"2.25"	"BDBM112518"	"CS(=O)(=O)N1CCCCC(Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.0209"	"nM"	"10.68"	""	"233757"	"UO_0000065"	"27.63"	"0.54"	"8.43"	"10.28"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3655083"	""	"0"	"374.47"	"0"	"1.54"	"BDBM159750"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)[C@H]2C[C@H](CC#N)C2)C1"	"IC50"	"'='"	"607.0"	"nM"	"6.22"	""	"302560"	"UO_0000065"	"16.60"	"0.33"	"4.68"	"5.42"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3658856"	""	"0"	"399.47"	"0"	"2.23"	"BDBM159775"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](CS(=O)(=O)N2CCC(F)(F)CC2)C1"	"IC50"	"'='"	"373.0"	"nM"	"6.43"	""	"302585"	"UO_0000065"	"16.09"	"0.33"	"4.20"	"7.82"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3655099"	""	"0"	"375.46"	"0"	"0.60"	"BDBM159766"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)N2CC[C@H](C#N)C2)C1"	"IC50"	"'='"	"434.0"	"nM"	"6.36"	""	"302576"	"UO_0000065"	"16.95"	"0.33"	"5.76"	"5.39"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642424"	""	"0"	"476.56"	"0"	"2.82"	"BDBM99702"	"CN1CCN(c2cccc(Nc3nc4c(-c5ccc(S(C)(=O)=O)cc5)cccn4n3)c2)C(=O)C1"	"IC50"	"'='"	"1.63"	"nM"	"8.79"	""	"216392"	"UO_0000065"	"18.44"	"0.35"	"5.97"	"8.80"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3665189"	""	"0"	"403.47"	"0"	"1.26"	"BDBM112584"	"COc1ncc(-c2cnc3[nH]ccc3n2)c(N[C@H]2CCCN(S(C)(=O)=O)C2)n1"	"IC50"	"'='"	"0.0717"	"nM"	"10.14"	""	"233821"	"UO_0000065"	"25.14"	"0.49"	"8.88"	"8.05"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3645038"	""	"0"	"552.60"	"2"	"5.05"	"BDBM99805"	"CCOc1ccc(C(F)(F)F)cc1-c1cccn2nc(Nc3ccc4c(c3)CCN(CC(=O)N(C)C)CC4)nc12"	"IC50"	"'='"	"223.03"	"nM"	"6.65"	""	"216478"	"UO_0000065"	"12.04"	"0.23"	"1.60"	"8.87"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642331"	""	"0"	"531.56"	"1"	"3.71"	"BDBM99603"	"CN1CCN(c2ccc(Nc3nc4c(-c5ccc(S(C)(=O)=O)cc5)cc(C(F)(F)F)cn4n3)cn2)CC1"	"IC50"	"'='"	"927.5"	"nM"	"6.03"	""	"216293"	"UO_0000065"	"11.35"	"0.22"	"2.32"	"6.30"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3699541"	""	"0"	"359.82"	"0"	"2.60"	"BDBM147559"	"N#C[C@H]1C[C@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"49.0"	"nM"	"7.31"	""	"285590"	"UO_0000065"	"20.32"	"0.40"	"4.71"	"6.25"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645046"	""	"0"	"588.58"	"2"	"5.29"	"BDBM99813"	"CN(C)C(=O)CN1CCc2ccc(Nc3nc4c(-c5cc(C(F)(F)F)ccc5OCC(F)F)cccn4n3)cc2CC1"	"IC50"	"'='"	"316.51"	"nM"	"6.50"	""	"216486"	"UO_0000065"	"11.04"	"0.21"	"1.21"	"8.67"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL4294092"	""	"0"	"561.69"	"1"	"3.91"	"61"	"CN1CCN(CC(=O)Nc2ccc(-c3ccnc(Nc4cccc(OCCCCCCC(=O)NO)c4)n3)cc2)CC1"	"IC50"	"'='"	"109.0"	"nM"	"6.96"	""	""	"UO_0000065"	"12.40"	"0.23"	"3.05"	"5.28"	"False"	"CHEMBL4268221"	"Inhibition of human JAK2 using poly(Glu:Tyr)(4:1) as substrate preincubated for 20 mins followed by [gamma33P]ATP addition measured after 120 mins by ion exchange filter paper method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4265943"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2018"	"None"	""
"CHEMBL4290831"	""	"0"	"527.03"	"0"	"4.63"	"45d"	"CC(=O)Nc1ccc(-c2ccnc(Nc3ccc(NC(=O)CCCCCCC(=O)NO)cc3)n2)cc1.Cl"	"IC50"	"'='"	"0.9"	"nM"	"9.05"	""	""	"UO_0000065"	"18.44"	"0.34"	"4.42"	"6.22"	"False"	"CHEMBL4268221"	"Inhibition of human JAK2 using poly(Glu:Tyr)(4:1) as substrate preincubated for 20 mins followed by [gamma33P]ATP addition measured after 120 mins by ion exchange filter paper method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4265943"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2018"	"None"	""
"CHEMBL4277267"	""	"0"	"516.65"	"2"	"5.66"	"69d"	"O=C(CCCCCCC(=O)Nc1ccc(-c2ccnc(Nc3cccc(N4CCCCC4)c3)n2)cc1)NO"	"IC50"	"'='"	"6.6"	"nM"	"8.18"	""	""	"UO_0000065"	"15.83"	"0.29"	"2.52"	"6.85"	"False"	"CHEMBL4268221"	"Inhibition of human JAK2 using poly(Glu:Tyr)(4:1) as substrate preincubated for 20 mins followed by [gamma33P]ATP addition measured after 120 mins by ion exchange filter paper method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4265943"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2018"	"None"	""
"CHEMBL3699505"	""	"0"	"378.36"	"0"	"3.39"	"BDBM147522"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccnc(C(F)(F)F)c2)n1"	"IC50"	"'='"	"123.0"	"nM"	"6.91"	""	"285452"	"UO_0000065"	"18.26"	"0.35"	"3.52"	"6.30"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651041"	""	"0"	"366.38"	"0"	"2.29"	"BDBM153218"	"C=C(CO)C(=O)Nc1cccc(-c2ncnc3[nH]cc(C(=O)OCC)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294166"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702965"	""	"0"	"477.49"	"0"	"3.98"	"BDBM147672"	"N#C[C@H]1C[C@H](OCC2CC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc([C@H](O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"285604"	"UO_0000065"	"16.85"	"0.32"	"4.07"	"6.38"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4465262"	""	"0"	"402.42"	"0"	"1.79"	"11j"	"C=CC(=O)Nc1cccc(Cn2nc(-c3cc(C=O)n(C)n3)c3c(N)ncnc32)c1"	"IC50"	"'='"	"194.0"	"nM"	"6.71"	""	""	"UO_0000065"	"16.68"	"0.31"	"4.92"	"5.02"	"False"	"CHEMBL4402146"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-biotin as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4400567"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4457338"	""	"0"	"424.51"	"0"	"1.46"	"11i"	"C=CC(=O)N1CCC(Cn2nc(-c3cc(C(C)(C)O)n(C)n3)c3c(N)ncnc32)CC1"	"IC50"	"'='"	"14.8"	"nM"	"7.83"	""	""	"UO_0000065"	"18.44"	"0.34"	"6.37"	"6.12"	"False"	"CHEMBL4402146"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-biotin as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4400567"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL1789941"	"RUXOLITINIB"	"4"	"306.37"	"0"	"3.47"	"INCB18424"	"N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"0.056"	"nM"	"10.25"	""	""	"UO_0000065"	"33.46"	"0.61"	"6.78"	"12.32"	"True"	"CHEMBL4031305"	"Inhibition of human JAK2 using poly[Glu:Tyr] as substrate in presence of [gamma-33P]-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028864"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4282456"	""	"0"	"527.03"	"0"	"4.63"	"45b"	"CC(=O)Nc1ccc(-c2ccnc(Nc3cccc(NC(=O)CCCCCCC(=O)NO)c3)n2)cc1.Cl"	"IC50"	"'='"	"9.2"	"nM"	"8.04"	""	""	"UO_0000065"	"16.38"	"0.30"	"3.41"	"5.53"	"False"	"CHEMBL4268221"	"Inhibition of human JAK2 using poly(Glu:Tyr)(4:1) as substrate preincubated for 20 mins followed by [gamma33P]ATP addition measured after 120 mins by ion exchange filter paper method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4265943"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2018"	"None"	""
"CHEMBL4281785"	""	"0"	"532.65"	"1"	"4.82"	"74a"	"Cc1cnc(Nc2ccc(N3CCOCC3)cc2)nc1-c1ccc(NC(=O)CCCCCCC(=O)NO)cc1"	"IC50"	"'='"	"1.8"	"nM"	"8.74"	""	""	"UO_0000065"	"16.42"	"0.31"	"3.92"	"6.79"	"False"	"CHEMBL4268221"	"Inhibition of human JAK2 using poly(Glu:Tyr)(4:1) as substrate preincubated for 20 mins followed by [gamma33P]ATP addition measured after 120 mins by ion exchange filter paper method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4265943"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2018"	"None"	""
"CHEMBL4096145"	""	"0"	"377.49"	"0"	"3.42"	"2"	"CC1(C)[C@H](Nc2c(C(N)=O)cnn3cc(-c4ccccc4)cc23)CC[C@]1(C)N"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4054822"	"Inhibition of GST-tagged JAK2 (unknown origin) after 3 hrs by Caliper assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4052645"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4060536"	""	"0"	"391.52"	"0"	"3.73"	"9"	"Cc1ccc(-c2cc3c(N[C@@H]4CC[C@](C)(N)C4(C)C)c(C(N)=O)cnn3c2)cc1"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4054822"	"Inhibition of GST-tagged JAK2 (unknown origin) after 3 hrs by Caliper assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4052645"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4084341"	""	"0"	"392.51"	"0"	"3.12"	"26"	"Cc1cnccc1-c1cc2c(N[C@@H]3CC[C@](C)(N)C3(C)C)c(C(N)=O)cnn2c1"	"IC50"	"'='"	"19.0"	"nM"	"7.72"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4054822"	"Inhibition of GST-tagged JAK2 (unknown origin) after 3 hrs by Caliper assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4052645"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4091096"	""	"0"	"422.53"	"0"	"3.21"	"36"	"CCOc1ccc(-c2cc3c(N[C@@H]4CC[C@](C)(N)C4(C)C)c(C(N)=O)cnn3c2)cn1"	"IC50"	"'='"	"30.0"	"nM"	"7.52"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4054822"	"Inhibition of GST-tagged JAK2 (unknown origin) after 3 hrs by Caliper assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4052645"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4237800"	""	"0"	"506.61"	"1"	"4.82"	"10"	"Cc1c(-c2ccc(C(N)=O)c3[nH]c4c(c23)CCC(C(C)(C)O)C4)cccc1-n1cnc2ccccc2c1=O"	"IC50"	"'='"	"5700.0"	"nM"	"5.24"	""	""	"UO_0000065"	"10.35"	"0.19"	"0.42"	"4.60"	"False"	"CHEMBL4235700"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229517"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2018"	"None"	""
"CHEMBL3398127"	""	"0"	"394.39"	"0"	"4.00"	"1b"	"COc1cccc(NC(=O)c2cnc(Nc3cccc(OC)c3)c([N+](=O)[O-])c2)c1"	"IC50"	"'='"	"8500.0"	"nM"	"5.07"	""	""	"UO_0000065"	"12.86"	"0.24"	"1.07"	"4.39"	"False"	"CHEMBL3399759"	"Inhibition of IL4-induced JAK2 autophosphorylation in human HT-29 cells by SDS-polyacrylamide gel electrophoresis and Western blot method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HT-29"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3397032"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"CHEMBL3307768"	""
"CHEMBL3593761"	""	"0"	"272.35"	"0"	"2.65"	"5"	"C[C@@H]1CCCC[C@@H]1Nc1c(C(N)=O)cnc2[nH]ccc12"	"IC50"	"'='"	"30.0"	"nM"	"7.52"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4236473"	"Inhibition of JAK2 (unknown origin)"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229549"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4241916"	""	"0"	"270.34"	"0"	"2.26"	"7a, rac-exo isomer"	"NC(=O)c1cnc2[nH]ccc2c1N[C@@H]1C[C@H]2CC[C@@H]1C2"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4236469"	"Inhibition of recombinant human N-terminal His-tagged JAK2 catalytic domain (826 to 1132 residues) expressed in baculovirus expression system using Biotin-Lyn-Substrate2 after 1 hr by ELISA"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229549"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL3896341"	""	"0"	"469.52"	"0"	"4.32"	"BDBM228895"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(c2ccnc3ccccc23)CC1"	"IC50"	"'='"	"488.0"	"nM"	"6.31"	""	"400642"	"UO_0000065"	"13.44"	"0.25"	"1.99"	"5.59"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3953419"	""	"0"	"450.49"	"0"	"4.22"	"BDBM228935"	"Cc1cccc(N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)CC2)c1F"	"IC50"	"'='"	"295.0"	"nM"	"6.53"	""	"400682"	"UO_0000065"	"14.50"	"0.27"	"2.31"	"6.53"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4102286"	""	"0"	"503.61"	"1"	"3.07"	"1"	"COc1nn(C)cc1Nc1nccc(-c2c[nH]c3c(NC(=O)[C@@H](C)N4CCN(C)C[C@@H]4C)cccc23)n1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022634"	"Inhibition of N-terminal GST fused recombinant JAK2 (831 to 1132 amino acids) (unknown origin) expressed in insect cells using ATP and peptide substrate (5FAM-GEEPLYWSFPAKKK-NH2"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020810"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2017"	"None"	""
"CHEMBL4276860"	""	"0"	"275.31"	"0"	"2.68"	"13"	"N#CN[C@@H]1CCc2ccc(-c3ncnc4[nH]ccc34)cc21"	"IC50"	"'='"	"1118.0"	"nM"	"5.95"	""	""	"UO_0000065"	"21.62"	"0.39"	"3.27"	"7.69"	"False"	"CHEMBL4265556"	"Inhibition of recombinant human GST-tagged JAK2 using KAIETDKEYYTVKD-NH2 as substrate in presence of 1 mM ATP concentration by coupled PK/LDH assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4261650"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4292320"	""	"0"	"368.42"	"0"	"1.73"	"28"	"CS(=O)(=O)N[C@@H]1C[C@H](NC#N)c2cc(-c3ncnc4[nH]ccc34)ccc21"	"IC50"	"'>'"	"7448.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4265556"	"Inhibition of recombinant human GST-tagged JAK2 using KAIETDKEYYTVKD-NH2 as substrate in presence of 1 mM ATP concentration by coupled PK/LDH assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4261650"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4092337"	""	"0"	"335.37"	"0"	"2.17"	"13a"	"C=CC(=O)Nc1cccc(CNc2c(C(N)=O)cnn3cccc23)c1"	"IC50"	"'>'"	"2000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4047228"	"Inhibition of GST-tagged JAK2 (unknown origin) using fluoresceinated peptide as substrate after 3 hrs by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4043231"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4064366"	""	"0"	"524.03"	"1"	"3.34"	"36"	"COc1nn(C)cc1Nc1ncc(Cl)c(-c2c[nH]c3c(NC(=O)[C@@H](C)N4CCN(C)CC4)cccc23)n1"	"IC50"	"'='"	"1760.0"	"nM"	"5.75"	""	""	"UO_0000065"	"10.98"	"0.21"	"2.41"	"4.95"	"False"	"CHEMBL4022634"	"Inhibition of N-terminal GST fused recombinant JAK2 (831 to 1132 amino acids) (unknown origin) expressed in insect cells using ATP and peptide substrate (5FAM-GEEPLYWSFPAKKK-NH2"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020810"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2017"	"None"	""
"CHEMBL3932352"	""	"0"	"420.45"	"0"	"2.56"	"BDBM228916"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(c2cncnc2)CC1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"400663"	"UO_0000065"	"20.69"	"0.38"	"6.14"	"6.92"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3963918"	""	"0"	"433.49"	"0"	"3.48"	"BDBM228944"	"Cc1ccc(N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)CC2)cn1"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	"400691"	"UO_0000065"	"18.68"	"0.35"	"4.62"	"7.17"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3915689"	""	"0"	"553.62"	"2"	"5.10"	"42"	"O=C(NO)c1ccc(NCCOc2ccc3cc2COC/C=C/COCc2cccc(c2)-c2ccnc(n2)N3)cc1"	"IC50"	"'='"	"1.71"	"nM"	"8.77"	""	""	"UO_0000065"	"15.84"	"0.29"	"3.67"	"6.91"	"False"	"CHEMBL3877344"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]ATP addition measured after 120 mins by Hotspot assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3877241"	"1"	"Scientific Literature"	"J Med Chem"	"2016"	"None"	""
"CHEMBL3924682"	""	"0"	"554.60"	"2"	"5.07"	"44"	"O=C(NO)c1ccc(OCCOc2ccc3cc2COC/C=C/COCc2cccc(c2)-c2ccnc(n2)N3)cc1"	"IC50"	"'='"	"1.27"	"nM"	"8.90"	""	""	"UO_0000065"	"16.04"	"0.30"	"3.83"	"7.17"	"False"	"CHEMBL3877344"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]ATP addition measured after 120 mins by Hotspot assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3877241"	"1"	"Scientific Literature"	"J Med Chem"	"2016"	"None"	""
"CHEMBL4248202"	""	"0"	"365.40"	"0"	"0.89"	"12c"	"Cn1cc(-c2nn(C3CCCN(C(=O)CC#N)C3)c3ncnc(N)c23)cn1"	"IC50"	"'='"	"590.0"	"nM"	"6.23"	""	""	"UO_0000065"	"17.05"	"0.32"	"5.34"	"4.74"	"False"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4288086"	""	"0"	"322.37"	"0"	"2.94"	"7"	"C=CC(=O)Nc1cccc(-c2ncnc3[nH]cc(CCOC)c23)c1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4265556"	"Inhibition of recombinant human GST-tagged JAK2 using KAIETDKEYYTVKD-NH2 as substrate in presence of 1 mM ATP concentration by coupled PK/LDH assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4261650"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4281693"	""	"0"	"291.31"	"0"	"1.65"	"27"	"N#CN[C@@H]1c2cc(-c3ncnc4[nH]ccc34)ccc2C[C@H]1O"	"IC50"	"'='"	"4964.0"	"nM"	"5.30"	""	""	"UO_0000065"	"18.21"	"0.33"	"3.65"	"5.43"	"False"	"CHEMBL4265556"	"Inhibition of recombinant human GST-tagged JAK2 using KAIETDKEYYTVKD-NH2 as substrate in presence of 1 mM ATP concentration by coupled PK/LDH assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4261650"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4287845"	""	"0"	"351.41"	"0"	"4.35"	"34"	"N#CN[C@H]1CCc2ccc(-c3ncnc4[nH]cc(-c5ccccc5)c34)cc21"	"IC50"	"'>'"	"6578.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4265556"	"Inhibition of recombinant human GST-tagged JAK2 using KAIETDKEYYTVKD-NH2 as substrate in presence of 1 mM ATP concentration by coupled PK/LDH assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4261650"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4284499"	""	"0"	"391.47"	"0"	"4.63"	"17b"	"COc1cc2c(=O)n(CC3CCCCC3)c3c4cc[nH]c4ncc3c2cc1OC"	"IC50"	"'='"	"3.57"	"nM"	"8.45"	""	""	"UO_0000065"	"21.58"	"0.40"	"3.82"	"12.22"	"False"	"CHEMBL4261266"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]-ATP addition measured after 2 hrs by filter-binding method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257589"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL221037"	""	"0"	"401.47"	"0"	"2.95"	"24"	"C[C@H](Nc1cc(N2CC[C@@H](O)C2)nc(-n2cnc3ccncc32)n1)c1ccccc1"	"IC50"	"'='"	"59.0"	"nM"	"7.23"	""	""	"UO_0000065"	"18.01"	"0.33"	"4.28"	"7.86"	"False"	"CHEMBL908418"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139695"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2006"	"None"	""
"CHEMBL4476380"	""	"0"	"447.43"	"0"	"0.79"	"10"	"Nc1nc(Nc2ccc(S(N)(=O)=O)cc2)nn1C(=O)Nc1ccc(OCC(=O)O)cc1"	"IC50"	"'='"	"100000.0"	"nM"	"4.00"	""	""	"UO_0000065"	"8.94"	"0.18"	"3.21"	"1.96"	"False"	"CHEMBL4359667"	"Inhibition of full length human C-terminal FLAG-tagged JAK2 V617F mutant (1 to 1132 residues) autophosphorylation expressed in HEK293T cells incubated in buffer with compound for 1 hr followed by treatment with enzyme and [gamma32P]-ATP for 15 mins by immunoprecipitation assay based autoradiography"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4354882"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL2376153"	""	"0"	"476.93"	"0"	"2.66"	"6j"	"CC[C@@H](NC(=O)c1c[nH]c2ncc(-c3nn(C)c4cc(Cl)ccc34)nc12)C(=O)N1CC(C#N)C1"	"IC50"	"'='"	"4.2"	"nM"	"8.38"	""	""	"UO_0000065"	"17.56"	"0.34"	"5.72"	"6.32"	"False"	"CHEMBL2378515"	"Inhibition of JAK2 (unknown origin) using [33gammaP]ATP and Biotin-KAIETDKEYYTVKD as substrate incubated for 10 mins prior to substrate addition measured after 30 mins by filtration assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375236"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2376147"	""	"0"	"446.45"	"0"	"1.75"	"6d"	"C[C@@H](NC(=O)c1c[nH]c2ncc(-c3nn(C)c4cc(F)ccc34)nc12)C(=O)N1CC(C#N)C1"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	""	"UO_0000065"	"17.74"	"0.33"	"6.17"	"5.97"	"False"	"CHEMBL2378515"	"Inhibition of JAK2 (unknown origin) using [33gammaP]ATP and Biotin-KAIETDKEYYTVKD as substrate incubated for 10 mins prior to substrate addition measured after 30 mins by filtration assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375236"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL3892138"	""	"0"	"357.42"	"0"	"2.86"	"BDBM198227"	"N#Cc1cccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)c1"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	"352309"	"UO_0000065"	"21.74"	"0.39"	"4.91"	"9.04"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL1934334"	""	"0"	"486.58"	"0"	"3.82"	"2"	"COc1cc(C2CCN(CC(N)=O)CC2)ccc1Nc1ncc2ccc(-c3ccccc3OC)n2n1"	"IC50"	"'='"	"250.0"	"nM"	"6.60"	""	""	"UO_0000065"	"13.57"	"0.25"	"2.78"	"6.17"	"False"	"CHEMBL1936085"	"Inhibition of human recombinant JAK2 expressed in baculovirus expression system after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL1934337"	""	"0"	"561.71"	"1"	"3.88"	"3c"	"CC(C)(C)NS(=O)(=O)c1cccc(-c2ccc3cnc(Nc4ccc(C5CCN(CC(N)=O)CC5)cc4)nn23)c1"	"IC50"	"'='"	"90.0"	"nM"	"7.05"	""	""	"UO_0000065"	"12.54"	"0.24"	"3.17"	"5.23"	"False"	"CHEMBL1936009"	"Inhibition of JAK2 in GM-CSF-stimulated human TF1 cells preincubated for 1 hr prior to challenge"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3307972"	""
"CHEMBL1934339"	""	"0"	"519.63"	"1"	"3.18"	"3e"	"CS(=O)(=O)Nc1cccc(-c2ccc3cnc(Nc4ccc(C5CCN(CC(N)=O)CC5)cc4)nn23)c1"	"IC50"	"'='"	"60.0"	"nM"	"7.22"	""	""	"UO_0000065"	"13.90"	"0.27"	"4.04"	"5.36"	"False"	"CHEMBL1936009"	"Inhibition of JAK2 in GM-CSF-stimulated human TF1 cells preincubated for 1 hr prior to challenge"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3307972"	""
"CHEMBL1934343"	""	"0"	"504.62"	"1"	"3.21"	"3i"	"CS(=O)(=O)c1cccc(-c2ccc3cnc(Nc4ccc(C5CCN(CC(N)=O)CC5)cc4)nn23)c1"	"IC50"	"'='"	"58.0"	"nM"	"7.24"	""	""	"UO_0000065"	"14.34"	"0.27"	"4.03"	"5.90"	"False"	"CHEMBL1936009"	"Inhibition of JAK2 in GM-CSF-stimulated human TF1 cells preincubated for 1 hr prior to challenge"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3307972"	""
"CHEMBL3622826"	""	"0"	"287.37"	"0"	"0.56"	"2"	"NCCn1c(C2CCNCC2)nc2cc(C(N)=O)ccc21"	"IC50"	"'='"	"3200.0"	"nM"	"5.50"	""	""	"UO_0000065"	"19.12"	"0.36"	"4.93"	"5.55"	"False"	"CHEMBL3817421"	"Inhibition of FLAG-tagged human JAK2 expressed in insect Sf9 cells using biotin-EQEDEPEGDYFEWLE-NH2 as substrate by HTRF assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3813615"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"CHEMBL3308860"	""
"CHEMBL1938648"	""	"0"	"382.49"	"0"	"3.08"	"13"	"CN(C)C(=O)c1cnc(N)c2cc(-c3ccc(N4CCOCC4)cc3)sc12"	"IC50"	"'='"	"1170.0"	"nM"	"5.93"	""	""	"UO_0000065"	"15.51"	"0.30"	"2.85"	"8.27"	"False"	"CHEMBL1941383"	"Inhibition of human recombinant N-terminal GST-tagged JAK2 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308860"	""
"CHEMBL1938653"	""	"0"	"350.45"	"0"	"3.71"	"18"	"CNC(=O)c1cnc(N)c2cc(-c3ccc(C(C)(C)C#N)cc3)sc12"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	""	"UO_0000065"	"23.96"	"0.46"	"4.69"	"9.15"	"False"	"CHEMBL1941383"	"Inhibition of human recombinant N-terminal GST-tagged JAK2 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308860"	""
"CHEMBL1938657"	""	"0"	"475.64"	"0"	"2.91"	"23"	"CN(C)CCNC(=O)c1cnc(N)c2cc(-c3ccc(S(=O)(=O)NC(C)(C)C)cc3)sc12"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	""	"UO_0000065"	"17.02"	"0.35"	"5.19"	"6.90"	"False"	"CHEMBL1941383"	"Inhibition of human recombinant N-terminal GST-tagged JAK2 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308860"	""
"CHEMBL3763697"	""	"0"	"286.34"	"0"	"1.36"	"11"	"CC(C)Cn1cc(-c2ccn(C)n2)c2[nH]nc(N)c2c1=O"	"IC50"	"'='"	"390.0"	"nM"	"6.41"	""	""	"UO_0000065"	"22.38"	"0.42"	"5.05"	"6.78"	"False"	"CHEMBL3766653"	"Inhibition of JAK2 (unknown origin) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent substrate phosphorylation after 45 mins by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3763089"	"1"	"Scientific Literature"	"J. Med. Chem."	"2016"	"None"	""
"CHEMBL3647739"	""	"0"	"552.50"	"1"	"3.79"	"BDBM147842"	"N#C[C@H]1C[C@@H](NCCC(F)(F)F)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"55.0"	"nM"	"7.26"	""	"285776"	"UO_0000065"	"13.14"	"0.27"	"3.47"	"5.08"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3335698"	""	"0"	"458.55"	"0"	"1.09"	"BDBM112591"	"CS(=O)(=O)N1CCC[C@H](Nc2nc(N3CCOCC3)ncc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.1026"	"nM"	"9.99"	""	"233828"	"UO_0000065"	"21.78"	"0.43"	"8.90"	"7.73"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642311"	""	"0"	"394.46"	"0"	"3.55"	"BDBM99581"	"COc1ccccc1Nc1nc2cccc(-c3cccc(S(C)(=O)=O)c3)n2n1"	"IC50"	"'='"	"1210.9"	"nM"	"5.92"	""	"216271"	"UO_0000065"	"15.00"	"0.29"	"2.37"	"6.91"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3973848"	""	"0"	"367.84"	"0"	"2.90"	"BDBM228720"	"Cc1cc(Cl)nc(N(C)[C@@H]2CCN(c3ncnc4[nH]ccc34)C2)c1C#N"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399640"	"UO_0000065"	"27.89"	"0.54"	"7.36"	"12.11"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3642329"	""	"0"	"530.58"	"1"	"4.31"	"BDBM99601"	"CN1CCN(c2cccc(Nc3nc4c(-c5ccc(S(C)(=O)=O)cc5)cc(C(F)(F)F)cn4n3)c2)CC1"	"IC50"	"'='"	"9999.0"	"nM"	"5.00"	""	"216291"	"UO_0000065"	"9.42"	"0.18"	"0.69"	"6.04"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL2062806"	""	"0"	"476.61"	"0"	"3.29"	"BDBM99615"	"CN1CCN(Cc2cccc(Nc3nc4c(-c5ccc(S(C)(=O)=O)cc5)cccn4n3)c2)CC1"	"IC50"	"'='"	"3.07"	"nM"	"8.51"	""	"216305"	"UO_0000065"	"17.86"	"0.34"	"5.22"	"10.28"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3655094"	""	"0"	"371.41"	"0"	"1.64"	"BDBM159761"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)C2CC(F)(F)C2)C1"	"IC50"	"'='"	"177.0"	"nM"	"6.75"	""	"302571"	"UO_0000065"	"18.18"	"0.37"	"5.11"	"7.42"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699489"	""	"0"	"356.41"	"0"	"2.30"	"BDBM147504"	"N#C[C@@H]1CC(CN)CCC1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"247.0"	"nM"	"6.61"	""	"285431"	"UO_0000065"	"18.54"	"0.35"	"4.31"	"5.38"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699478"	""	"0"	"367.41"	"0"	"2.76"	"BDBM147493"	"[C-]#[N+][C@@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(CC(=O)O)cc2)n1"	"IC50"	"'='"	"109.0"	"nM"	"6.96"	""	"285418"	"UO_0000065"	"18.95"	"0.35"	"4.20"	"6.08"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703020"	""	"0"	"404.88"	"0"	"3.31"	"BDBM147730"	"CN(C)[C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(Cl)c(F)c3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"58.0"	"nM"	"7.24"	""	"285664"	"UO_0000065"	"17.87"	"0.35"	"3.93"	"7.24"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645548"	""	"0"	"311.77"	"0"	"3.86"	"BDBM107134"	"O=C(CCCl)Nc1cccc(-c2cnc3ccccc3n2)c1"	"IC50"	"'>'"	"50000.0"	"nM"	""	""	"226372"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3644965"	""	"0"	"467.56"	"0"	"2.96"	"BDBM99715"	"CS(=O)(=O)c1ccc(Oc2cccn3nc(Nc4cnn(CCN5CCCC5)c4)nc23)cc1"	"IC50"	"'='"	"2999.0"	"nM"	"5.52"	""	"216405"	"UO_0000065"	"11.81"	"0.23"	"2.56"	"5.18"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3982307"	""	"0"	"368.44"	"0"	"3.70"	"BDBM228733"	"CN(c1ccc(C#N)c2ccccc12)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399655"	"UO_0000065"	"27.85"	"0.50"	"6.56"	"14.28"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3932349"	""	"0"	"330.40"	"0"	"2.47"	"BDBM228711"	"N#Cc1ccc2c(c1)CCN2[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399629"	"UO_0000065"	"31.05"	"0.56"	"7.79"	"14.28"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3702907"	""	"0"	"479.57"	"0"	"2.85"	"BDBM147606"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)NCc3ccncc3)cc2)n1"	"IC50"	"'='"	"0.95"	"nM"	"9.02"	""	"285536"	"UO_0000065"	"18.81"	"0.36"	"6.17"	"5.79"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4062946"	""	"0"	"271.32"	"0"	"1.55"	"4"	"C=CC(=O)N1CCC[C@@H](Nc2ncnc3[nH]ccc23)C1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4005719"	"Inhibition of recombinant human GST-tagged cytoplasmic JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by microfluidic assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4004825"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL1945051"	""	"0"	"406.92"	"1"	"5.31"	"27b"	"CN1C/C=C/CCOc2cccc(c2)-c2ccnc(n2)Nc2ccc(Cl)c(c2)C1"	"IC50"	"'='"	"82.0"	"nM"	"7.09"	""	""	"UO_0000065"	"17.41"	"0.33"	"1.78"	"14.09"	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1945566"	""	"0"	"464.59"	"0"	"4.45"	"27e"	"CCS(=O)(=O)c1ccc2cc1CN(C)C/C=C/CCOc1cccc(c1)-c1ccnc(n1)N2"	"IC50"	"'='"	"100.0"	"nM"	"7.00"	""	""	"UO_0000065"	"15.07"	"0.29"	"2.55"	"8.29"	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1945568"	""	"0"	"499.62"	"0"	"4.66"	"27h"	"CN1C/C=C/CCOc2cccc(c2)-c2ccnc(n2)Nc2ccc(OCC(=O)N3CCCC3)c(c2)C1"	"IC50"	"'='"	"140.0"	"nM"	"6.85"	""	""	"UO_0000065"	"13.72"	"0.25"	"2.19"	"8.59"	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1945569"	""	"0"	"457.58"	"0"	"4.49"	"27i"	"CN1C/C=C/CCOc2cccc(c2)-c2ccnc(n2)Nc2ccc(N3CCOCC3)c(c2)C1"	"IC50"	"'='"	"49.0"	"nM"	"7.31"	""	""	"UO_0000065"	"15.97"	"0.29"	"2.82"	"11.65"	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1938650"	""	"0"	"297.38"	"0"	"3.21"	"15"	"CNC(=O)c1cnc(N)c2cc(-c3ccc(C)cc3)sc12"	"IC50"	"'='"	"12600.0"	"nM"	"4.90"	""	""	"UO_0000065"	"16.48"	"0.32"	"1.69"	"7.20"	"False"	"CHEMBL1941390"	"Inhibition of TEL-fused JAK2 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3307634"	""
"CHEMBL1938654"	""	"0"	"418.54"	"0"	"2.98"	"19"	"CNC(=O)c1cnc(N)c2cc(-c3ccc(S(=O)(=O)NC(C)(C)C)cc3)sc12"	"IC50"	"'='"	"1010.0"	"nM"	"6.00"	""	""	"UO_0000065"	"14.33"	"0.29"	"3.02"	"5.25"	"False"	"CHEMBL1941390"	"Inhibition of TEL-fused JAK2 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3307634"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"20, CP-690550"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"265.0"	"nM"	"6.58"	""	""	"UO_0000065"	"21.05"	"0.39"	"5.04"	"7.40"	"True"	"CHEMBL1941390"	"Inhibition of TEL-fused JAK2 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3307634"	""
"CHEMBL4280180"	""	"0"	"364.41"	"0"	"2.73"	"8"	"C=CC(=O)N1CCOc2ccc(-c3ncnc4[nH]cc(CCOC)c34)cc21"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4265556"	"Inhibition of recombinant human GST-tagged JAK2 using KAIETDKEYYTVKD-NH2 as substrate in presence of 1 mM ATP concentration by coupled PK/LDH assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4261650"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4294868"	""	"0"	"291.31"	"0"	"2.17"	"25"	"N#CN[C@H]1C[C@@H](O)c2ccc(-c3ncnc4[nH]ccc34)cc21"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4265556"	"Inhibition of recombinant human GST-tagged JAK2 using KAIETDKEYYTVKD-NH2 as substrate in presence of 1 mM ATP concentration by coupled PK/LDH assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4261650"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4286963"	""	"0"	"291.31"	"0"	"2.17"	"26"	"N#CN[C@H]1C[C@H](O)c2ccc(-c3ncnc4[nH]ccc34)cc21"	"IC50"	"'='"	"2455.0"	"nM"	"5.61"	""	""	"UO_0000065"	"19.26"	"0.35"	"3.44"	"5.75"	"False"	"CHEMBL4265556"	"Inhibition of recombinant human GST-tagged JAK2 using KAIETDKEYYTVKD-NH2 as substrate in presence of 1 mM ATP concentration by coupled PK/LDH assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4261650"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4281035"	""	"0"	"434.49"	"0"	"1.89"	"30"	"Cn1nccc1S(=O)(=O)N[C@@H]1C[C@H](NC#N)c2cc(-c3ncnc4[nH]ccc34)ccc21"	"IC50"	"'>'"	"7646.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4265556"	"Inhibition of recombinant human GST-tagged JAK2 using KAIETDKEYYTVKD-NH2 as substrate in presence of 1 mM ATP concentration by coupled PK/LDH assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4261650"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4292612"	""	"0"	"335.37"	"0"	"2.49"	"9"	"COCCc1c[nH]c2ncnc(-c3ccc4c(c3)N(C#N)CCO4)c12"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4265556"	"Inhibition of recombinant human GST-tagged JAK2 using KAIETDKEYYTVKD-NH2 as substrate in presence of 1 mM ATP concentration by coupled PK/LDH assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4261650"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4292010"	""	"0"	"275.31"	"0"	"2.68"	"11"	"N#CNC1CCc2ccc(-c3ncnc4[nH]ccc34)cc21"	"IC50"	"'='"	"1544.0"	"nM"	"5.81"	""	""	"UO_0000065"	"21.11"	"0.38"	"3.13"	"7.51"	"False"	"CHEMBL4265556"	"Inhibition of recombinant human GST-tagged JAK2 using KAIETDKEYYTVKD-NH2 as substrate in presence of 1 mM ATP concentration by coupled PK/LDH assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4261650"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL1789941"	"RUXOLITINIB"	"4"	"306.37"	"0"	"3.47"	"3"	"N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'<'"	"1.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4222523"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma33P]-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219149"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2018"	"None"	""
"CHEMBL4228240"	""	"0"	"398.50"	"0"	"2.44"	"1"	"CCN(CCO)Cc1cc(Nc2nc(C)cn3c(-c4cn[nH]c4)cnc23)sn1"	"IC50"	"'>'"	"500.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4222462"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219148"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2018"	"None"	""
"CHEMBL1650723"	""	"0"	"364.77"	"0"	"2.71"	"75"	"COc1cc(Nc2nc(N[C@@H](C)c3ncc(F)cn3)ncc2Cl)n[nH]1"	"IC50"	"'='"	"3.9"	"nM"	"8.41"	""	""	"UO_0000065"	"23.05"	"0.46"	"5.70"	"7.41"	"False"	"CHEMBL4349471"	"Inhibition of recombinant C-terminal His6-tagged human JAK2 (808 to end residues) expressed in baculovirus infected SF21 insect cells using Tyr 1054/1055 biotinylated peptide as substrate after 60 mins by Alphascreen assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4346723"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2019"	"CHEMBL4106362"	""
"CHEMBL3892860"	""	"0"	"489.57"	"1"	"5.51"	"39"	"O=C(O)CCCCCOc1ccc2cc1COC/C=C/COCc1cccc(c1)-c1ccnc(n1)N2"	"IC50"	"'<'"	"39.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3877345"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3877241"	"1"	"Scientific Literature"	"J Med Chem"	"2016"	"None"	""
"CHEMBL3972157"	""	"0"	"680.81"	"2"	"6.77"	"47"	"O=C(CCCCCCC(=O)Nc1ccc(NCCOc2ccc3cc2COC/C=C/COCc2cccc(c2)-c2ccnc(n2)N3)cc1)NO"	"IC50"	"'='"	"30.0"	"nM"	"7.52"	""	""	"UO_0000065"	"11.05"	"0.21"	"0.75"	"4.82"	"False"	"CHEMBL3877344"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]ATP addition measured after 120 mins by Hotspot assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3877241"	"1"	"Scientific Literature"	"J Med Chem"	"2016"	"None"	""
"CHEMBL3962918"	""	"0"	"539.59"	"2"	"5.65"	"33"	"O=C(O)c1ccc(OCCOc2ccc3cc2COC/C=C/COCc2cccc(c2)-c2ccnc(n2)N3)cc1"	"IC50"	"'<'"	"39.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3877345"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3877241"	"1"	"Scientific Literature"	"J Med Chem"	"2016"	"None"	""
"CHEMBL4535276"	""	"0"	"401.45"	"0"	"1.14"	"16"	"O=C(C1CC1)N1[C@@H]2CC[C@@H]1CN(c1nc(Nc3cnn(CCO)c3)ncc1F)C2"	"IC50"	"'='"	"2596.0"	"nM"	"5.59"	""	""	"UO_0000065"	"13.91"	"0.26"	"4.45"	"5.62"	"False"	"CHEMBL4411592"	"Inhibition of JAK2 homodimer signaling pathway in human spiked CD34 +ve cells of whole blood assessed as reduction in EPO induced STAT5 phosphorylation preincubated for 45 mins followed by EPO addition and measured measured after 15 mins by FACS assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4411260"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4517702"	""	"0"	"356.43"	"0"	"1.34"	"22"	"CCNC(=O)N1[C@@H]2CC[C@@H]1CN(c1ccnc(Nc3cnn(C)c3)n1)C2"	"IC50"	"'='"	"2866.0"	"nM"	"5.54"	""	""	"UO_0000065"	"15.55"	"0.29"	"4.20"	"6.08"	"False"	"CHEMBL4411592"	"Inhibition of JAK2 homodimer signaling pathway in human spiked CD34 +ve cells of whole blood assessed as reduction in EPO induced STAT5 phosphorylation preincubated for 45 mins followed by EPO addition and measured measured after 15 mins by FACS assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4411260"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4562564"	""	"0"	"353.43"	"0"	"1.54"	"24"	"Cn1cc(Nc2nccc(N3C[C@H]4CC[C@H](C3)N4C(=O)C3CC3)n2)cn1"	"IC50"	"'='"	"3737.0"	"nM"	"5.43"	""	""	"UO_0000065"	"15.36"	"0.29"	"3.89"	"6.85"	"False"	"CHEMBL4411592"	"Inhibition of JAK2 homodimer signaling pathway in human spiked CD34 +ve cells of whole blood assessed as reduction in EPO induced STAT5 phosphorylation preincubated for 45 mins followed by EPO addition and measured measured after 15 mins by FACS assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4411260"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4471304"	""	"0"	"389.41"	"0"	"1.79"	"25"	"Cn1cc(Nc2nccc(N3C[C@H]4CC[C@H](C3)N4C(=O)[C@H]3CC3(F)F)n2)cn1"	"IC50"	"'='"	"3148.0"	"nM"	"5.50"	""	""	"UO_0000065"	"14.13"	"0.27"	"3.71"	"6.95"	"False"	"CHEMBL4411595"	"Inhibition of human JAK2 using fluorescence labeled peptide as substrate and using 1 mM ATP by microfluidic based mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4411260"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4519857"	""	"0"	"405.46"	"0"	"1.67"	"8"	"CCNC(=O)c1ccc(Nc2nccc(N3C[C@@H]4C[C@H]3CN4C(=O)CC#N)n2)cc1"	"IC50"	"'='"	"366.0"	"nM"	"6.44"	""	""	"UO_0000065"	"15.87"	"0.29"	"4.77"	"5.63"	"False"	"CHEMBL4411532"	"Inhibition of human JAK2 using fluorescence labeled peptide as substrate and using ATP at its Km level by microfluidic based mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4411260"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4453646"	""	"0"	"321.17"	"0"	"3.99"	"3f"	"Clc1cccc(Nc2nc(Nc3cn[nH]c3)ncc2Cl)c1"	"IC50"	"'='"	"2.2"	"nM"	"8.66"	""	""	"UO_0000065"	"26.96"	"0.56"	"4.67"	"11.03"	"False"	"CHEMBL4431266"	"Inhibition of human recombinant JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate by LANCE assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4428138"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2016"	"None"	""
"CHEMBL1232805"	""	"0"	"174.09"	"0"	"-1.10"	"SID26665898"	"O=C(O)c1[nH]c(=O)[nH]c(=O)c1F"	"IC50"	"'='"	"6871.0"	"nM"	"5.16"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1472103"	""	"0"	"285.13"	"0"	"2.85"	"SID24824536"	"O=C(CCl)NCc1cc(-c2ccc(Cl)cc2)no1"	"IC50"	"'='"	"8352.0"	"nM"	"5.08"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL4474208"	""	"0"	"283.74"	"0"	"2.17"	"7"	"CS(=O)(=O)Nc1cc(-c2ccncc2)cnc1Cl"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4385137"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4382269"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL1938656"	""	"0"	"462.60"	"0"	"3.00"	"22"	"COCCNC(=O)c1cnc(N)c2cc(-c3ccc(S(=O)(=O)NC(C)(C)C)cc3)sc12"	"IC50"	"'='"	"135.0"	"nM"	"6.87"	""	""	"UO_0000065"	"14.85"	"0.30"	"3.87"	"5.57"	"False"	"CHEMBL1941458"	"Inhibition of JAK2 in human PBMC assessed as inhibition of TPO-stimulated STAT5 phosphorylation preincubated for 30 mins prior to TPO challenge measured after 15 mins by intracellular phosflow staining"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1938659"	""	"0"	"517.68"	"1"	"2.68"	"25"	"CC(C)(C)NS(=O)(=O)c1ccc(-c2cc3c(N)ncc(C(=O)NCCN4CCOCC4)c3s2)cc1"	"IC50"	"'='"	"2190.0"	"nM"	"5.66"	""	""	"UO_0000065"	"10.93"	"0.22"	"2.98"	"4.47"	"False"	"CHEMBL1941461"	"Inhibition of JAK2 in human whole blood assessed as inhibition of TPO-stimulated STAT5 phosphorylation preincubated for 30 mins prior to TPO challenge measured after 15 mins by intracellular phosflow staining"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"CHEMBL3638178"	"Blood"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL98"	"VORINOSTAT"	"4"	"264.32"	"0"	"2.47"	"2; SAHA"	"O=C(CCCCCCC(=O)Nc1ccccc1)NO"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4150584"	"Inhibition of JAK2 (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition and measured after 25 mins in presence of ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4145634"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4289532"	""	"0"	"462.43"	"0"	"3.68"	"21"	"CC[C@@H](C(=O)NCC(F)(F)F)n1c(=O)c2cc(OC)c(OC)cc2c2cnc3[nH]ccc3c21"	"IC50"	"'='"	"109.95"	"nM"	"6.96"	""	""	"UO_0000065"	"15.05"	"0.29"	"3.28"	"7.08"	"False"	"CHEMBL4261266"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]-ATP addition measured after 2 hrs by filter-binding method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257589"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL1170485"	""	"0"	"200.24"	"0"	"2.57"	"SID22405485"	"O=C1C=CCC(/C=C/c2ccccc2)O1"	"IC50"	"'='"	"8516.0"	"nM"	"5.07"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1459746"	""	"0"	"395.46"	"0"	"3.49"	"SID24836573"	"CCN1C/C(=C/c2ccc(OC)c(O)c2)C(=O)/C(=C/c2ccc(OC)c(O)c2)C1"	"IC50"	"'='"	"1500.0"	"nM"	"5.82"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1933343"	""	"0"	"386.50"	"0"	"4.97"	"1"	"Cc1cnc2nc1-c1cccc(c1)OCC/C=C/CN(C)Cc1cccc(c1)N2"	"IC50"	"'='"	"180.0"	"nM"	"6.75"	""	""	"UO_0000065"	"17.45"	"0.32"	"1.77"	"13.41"	"False"	"CHEMBL1937386"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1933054"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL1933346"	""	"0"	"419.45"	"0"	"2.68"	"4"	"COc1ccc(-c2nc(Nc3cccc(NC(=O)CN)c3)nc3[nH]cnc23)cc1OC"	"IC50"	"'='"	"330.0"	"nM"	"6.48"	""	""	"UO_0000065"	"15.45"	"0.29"	"3.80"	"4.63"	"False"	"CHEMBL1937386"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1933054"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL1449794"	""	"0"	"457.55"	"0"	"4.16"	"SID14741112"	"Cc1ccccc1CS(=O)(=O)c1nnc([C@H](Cc2ccccc2)NC(=O)OC(C)(C)C)o1"	"IC50"	"'='"	"5328.0"	"nM"	"5.27"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1325021"	""	"0"	"356.81"	"0"	"4.21"	"SID26659838"	"COc1ccccc1N(C(=O)CCl)c1cn(C(C)=O)c2ccccc12"	"IC50"	"'='"	"4605.0"	"nM"	"5.34"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1307636"	""	"0"	"373.66"	"0"	"3.25"	"SID26667304"	"O=S(=O)(c1cnc(Cl)c(Br)c1)N1CCc2ccccc21"	"IC50"	"'='"	"5308.0"	"nM"	"5.28"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1417496"	""	"0"	"346.65"	"0"	"4.03"	"SID14727382"	"Cc1nn(Cc2ccc(Cl)cc2Cl)c(C)c1NC(=O)CCl"	"IC50"	"'='"	"11410.0"	"nM"	"4.94"	""	"Not Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1562235"	""	"0"	"401.96"	"0"	"4.95"	"SID24781295"	"CC1CCN(CCCNC(=O)c2cc3c(Cl)nc4ccccc4c3s2)CC1"	"IC50"	"'='"	"4387.0"	"nM"	"5.36"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL4563864"	""	"0"	"406.45"	"0"	"2.53"	"14c"	"COCCn1cc(Nc2cc(NCc3cccc(NC(=O)CC#N)c3)ncn2)cn1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4482009"	"Inhibition of human JAK2 using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and further incubated for 30 mins and subsequently measured after 1 hr by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480445"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL1081975"	""	"0"	"427.46"	"1"	"5.81"	"6"	"COc1cc(Nc2nc3cccc(-c4ccc5ncccc5c4)c3o2)cc(OC)c1OC"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	""	"UO_0000065"	"18.94"	"0.35"	"2.29"	"10.30"	"False"	"CHEMBL1102770"	"Inhibition of GST-tagged JAK2 assessed as inhibition of biotinylated JAK3tide peptide phosphorylation after 60 mins by caliper mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154949"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1081976"	""	"0"	"469.52"	"0"	"4.64"	"7"	"COc1cc(Nc2nc3cccc(-c4cccc(NS(C)(=O)=O)c4)c3o2)cc(OC)c1OC"	"IC50"	"'='"	"150.0"	"nM"	"6.82"	""	""	"UO_0000065"	"14.53"	"0.28"	"2.18"	"6.10"	"False"	"CHEMBL1102770"	"Inhibition of GST-tagged JAK2 assessed as inhibition of biotinylated JAK3tide peptide phosphorylation after 60 mins by caliper mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154949"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL595397"	""	"0"	"293.33"	"0"	"3.26"	"13e"	"COC(=O)CC1Nc2ccccc2-c2ccnc3[nH]cc1c23"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL601303"	""	"0"	"315.35"	"0"	"4.88"	"13n"	"Fc1cccc(C2Nc3ccccc3-c3ccnc4[nH]cc2c34)c1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL592033"	""	"0"	"392.26"	"1"	"5.21"	"13z"	"Oc1ccc(C2Nc3ccccc3-c3ccnc4[nH]cc2c34)cc1Br"	"IC50"	"'='"	"5000.0"	"nM"	"5.30"	""	""	"UO_0000065"	"13.51"	"0.29"	"0.09"	"8.70"	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL3903955"	""	"0"	"498.51"	"1"	"5.86"	"5e"	"Cc1cnc(Nc2ccc(N3CCOCC3)cc2)nc1-c1cc2cc(COCC(F)(F)F)ccc2o1"	"IC50"	"'='"	"25.7"	"nM"	"7.59"	""	""	"UO_0000065"	"15.23"	"0.29"	"1.73"	"10.45"	"False"	"CHEMBL3868063"	"Inhibition of GST-tagged recombinant human JAK2 expressed in baculovirus using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3867460"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2017"	"None"	""
"CHEMBL3940537"	""	"0"	"469.57"	"0"	"2.94"	"16h"	"Cc1cnc(Nc2ccc(N3CCOCC3)cc2)nc1-c1cc2c(o1)CCN(S(C)(=O)=O)C2"	"IC50"	"'='"	"1254.0"	"nM"	"5.90"	""	""	"UO_0000065"	"12.57"	"0.24"	"2.96"	"5.85"	"False"	"CHEMBL3868067"	"Inhibition of JAK2 V617F mutant in human HEL cells after 1 hr"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3867460"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2017"	"CHEMBL3308090"	""
"CHEMBL3703045"	""	"0"	"444.94"	"0"	"4.14"	"BDBM147755"	"C[C@H](N[C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(Cl)c(F)c3)n2)[C@@H](C#N)C1)C1CC1"	"IC50"	"'='"	"97.0"	"nM"	"7.01"	""	"285689"	"UO_0000065"	"15.76"	"0.31"	"2.87"	"6.45"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647927"	""	"0"	"295.35"	"0"	"2.59"	"BDBM148047"	"N#C[C@@H]1CCC[C@@H]1n1cc(C(N)=O)c(Nc2ccccc2)n1"	"IC50"	"'='"	"696.0"	"nM"	"6.16"	""	"285398"	"UO_0000065"	"20.85"	"0.38"	"3.57"	"6.37"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647781"	""	"0"	"440.98"	"0"	"4.39"	"BDBM147884"	"CC(C)(NC1CCC(n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@@H](C#N)C1)C1CC1"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	"285818"	"UO_0000065"	"17.62"	"0.34"	"3.38"	"7.14"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702960"	""	"0"	"398.44"	"0"	"3.07"	"BDBM147667"	"[C-]#[N+][C@H]1C[C@H](OCC2CC2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccnc(F)c2)n1"	"IC50"	"'='"	"76.0"	"nM"	"7.12"	""	"285599"	"UO_0000065"	"17.87"	"0.34"	"4.05"	"7.16"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665122"	""	"0"	"358.43"	"0"	"1.47"	"BDBM112509"	"CS(=O)(=O)N1CC[C@@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.0296"	"nM"	"10.53"	""	"233748"	"UO_0000065"	"29.37"	"0.58"	"9.06"	"10.14"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652402"	""	"0"	"421.57"	"0"	"1.84"	"BDBM113214"	"C[C@@H]1C[C@@H](CS(=O)(=O)N2CC[C@H](CO)C2)CC[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"0.0199"	"nM"	"10.70"	""	"234657"	"UO_0000065"	"25.38"	"0.50"	"8.86"	"10.45"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3645543"	""	"0"	"367.46"	"0"	"4.16"	"BDBM107128"	"O=S(=O)(Nc1cccc(-c2cnc3ccccc3n2)c1)c1cccs1"	"IC50"	"'='"	"55500.0"	"nM"	"4.26"	""	"226366"	"UO_0000065"	"11.58"	"0.23"	"0.10"	"5.91"	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3655091"	""	"0"	"335.43"	"0"	"1.25"	"BDBM159758"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@H](NS(=O)(=O)CC2CC2)C1"	"IC50"	"'='"	"7180.0"	"nM"	"5.14"	""	"302568"	"UO_0000065"	"15.34"	"0.31"	"3.89"	"5.65"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3648436"	""	"0"	"337.40"	"0"	"3.52"	"BDBM107145"	"CC(=O)SCC(=O)Nc1cccc(-c2cnc3ccccc3n2)c1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	"226383"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3335699"	""	"0"	"471.59"	"0"	"1.00"	"BDBM112586"	"CN1CCN(c2ncc(-c3cnc4[nH]ccc4n3)c(N[C@H]3CCCN(S(C)(=O)=O)C3)n2)CC1"	"IC50"	"'='"	"0.0603"	"nM"	"10.22"	""	"233823"	"UO_0000065"	"21.67"	"0.42"	"9.22"	"8.29"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647755"	""	"0"	"524.57"	"1"	"3.64"	"BDBM147858"	"C[C@@H](N[C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)(F)F)cc3)n2)[C@@H](C#N)C1)C1CC1"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	"285792"	"UO_0000065"	"15.10"	"0.30"	"4.28"	"5.54"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642261"	""	"0"	"449.54"	"0"	"3.38"	"BDBM99519"	"CS(=O)(=O)c1cccc(-c2cccn3nc(Nc4ccc(N5CCOCC5)cc4)nc23)c1"	"IC50"	"'='"	"8.5"	"nM"	"8.07"	""	"216211"	"UO_0000065"	"17.95"	"0.34"	"4.69"	"9.09"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3645070"	""	"0"	"494.60"	"1"	"6.13"	"BDBM99838"	"CC(C)(C)OC(=O)N1CCC(c2ccc(Nc3nc4c(-c5ccc(C#N)cc5)cccn4n3)cc2)CC1"	"IC50"	"'='"	"61.59"	"nM"	"7.21"	""	"216511"	"UO_0000065"	"14.58"	"0.27"	"1.08"	"7.55"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3650680"	""	"0"	"441.44"	"0"	"3.27"	"BDBM148063"	"N#C[C@@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"285975"	"UO_0000065"	"18.23"	"0.37"	"4.78"	"6.15"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642268"	""	"0"	"493.59"	"0"	"3.25"	"BDBM99528"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4ccc(OCCN5CCOCC5)cc4)nc23)cc1"	"IC50"	"'='"	"1.3"	"nM"	"8.89"	""	"216220"	"UO_0000065"	"18.00"	"0.35"	"5.64"	"9.06"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3699533"	""	"0"	"467.47"	"0"	"4.32"	"BDBM147551"	"CC(C)(c1ccc(Nc2nn([C@H]3CCCC[C@@H]3C#N)cc2C(N)=O)cc1F)[C@H](O)C(F)(F)F"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	"285481"	"UO_0000065"	"17.02"	"0.33"	"3.64"	"6.80"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665164"	""	"0"	"337.39"	"0"	"1.84"	"BDBM112557"	"CC(=O)N1CCC[C@H](Nc2ncccc2-c2cnc3[nH]ncc3n2)C1"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	"233795"	"UO_0000065"	"23.71"	"0.44"	"6.16"	"8.02"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652280"	""	"0"	"459.54"	"0"	"3.56"	"BDBM113088"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCCC(C(F)(F)F)C2)CC1"	"IC50"	"'='"	"54.3"	"nM"	"7.26"	""	"234532"	"UO_0000065"	"15.81"	"0.32"	"3.71"	"8.84"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3655098"	""	"0"	"375.46"	"0"	"0.60"	"BDBM159765"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)N2CC[C@@H](C#N)C2)C1"	"IC50"	"'='"	"308.0"	"nM"	"6.51"	""	"302575"	"UO_0000065"	"17.34"	"0.34"	"5.91"	"5.52"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702997"	""	"0"	"472.52"	"0"	"4.46"	"BDBM147707"	"N#C[C@H]1C[C@@H](N2CC3(CCC3)C2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"121.0"	"nM"	"6.92"	""	"285641"	"UO_0000065"	"14.64"	"0.28"	"2.46"	"6.92"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647819"	""	"0"	"448.49"	"0"	"4.22"	"BDBM147924"	"CC(C)CN[C@H]1CC[C@@H](n2cc(C(N)=O)c(Nc3ccc(C(F)(F)F)cc3)n2)[C@H](C#N)C1"	"IC50"	"'='"	"420.0"	"nM"	"6.38"	""	"285858"	"UO_0000065"	"14.22"	"0.27"	"2.16"	"5.86"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645034"	""	"0"	"491.62"	"0"	"3.59"	"BDBM99798"	"COc1ccccc1-c1cccn2nc(Nc3ccc4c(c3)CCN(CCS(C)(=O)=O)CC4)nc12"	"IC50"	"'='"	"17.76"	"nM"	"7.75"	""	"216474"	"UO_0000065"	"15.77"	"0.30"	"4.16"	"8.73"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652291"	""	"0"	"473.60"	"0"	"2.85"	"BDBM113100"	"Cc1nnc(C2CCCN(S(=O)(=O)C[C@H]3CC[C@H](N(C)c4ncnc5[nH]ccc45)CC3)C2)o1"	"IC50"	"'='"	"19.5"	"nM"	"7.71"	""	"234544"	"UO_0000065"	"16.28"	"0.32"	"4.86"	"6.37"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3642376"	""	"0"	"414.52"	"0"	"3.23"	"BDBM99652"	"CN1CCN(c2cccc(Nc3nc4c(NCc5cccnc5)cccn4n3)c2)CC1"	"IC50"	"'='"	"646.78"	"nM"	"6.19"	""	"216342"	"UO_0000065"	"14.93"	"0.27"	"2.96"	"8.41"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703485"	""	"0"	"267.29"	"0"	"2.80"	"BDBM153129"	"CCOC(=O)c1c[nH]c2ncnc(-c3ccccc3)c12"	"IC50"	"'='"	"91.0"	"nM"	"7.04"	""	"294077"	"UO_0000065"	"26.34"	"0.48"	"4.24"	"10.37"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3644987"	""	"0"	"482.51"	"0"	"4.92"	"BDBM99739"	"COc1ccc(C(F)(F)F)cc1-c1cccn2nc(Nc3cccc(N4CCN(C)CC4)c3)nc12"	"IC50"	"'='"	"158.3"	"nM"	"6.80"	""	"216427"	"UO_0000065"	"14.09"	"0.27"	"1.88"	"11.74"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647814"	""	"0"	"462.48"	"0"	"3.46"	"BDBM147919"	"[C-]#[N+][C@@H]1C[C@@H](N(C)C2COC2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"106.0"	"nM"	"6.97"	""	"285853"	"UO_0000065"	"15.08"	"0.29"	"3.51"	"7.77"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3644964"	""	"0"	"441.46"	"0"	"4.45"	"BDBM99714"	"FC(F)(F)c1ccc(-c2cccn3nc(Nc4cnn(CCN5CCCC5)c4)nc23)cc1"	"IC50"	"'='"	"9.1"	"nM"	"8.04"	""	"216404"	"UO_0000065"	"18.21"	"0.34"	"3.59"	"12.71"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL4445037"	""	"0"	"267.30"	"0"	"1.83"	"49"	"Cc1nn(CCCC#N)nc1-c1ncnc2[nH]ccc12"	"IC50"	"'='"	"73.5"	"nM"	"7.13"	""	""	"UO_0000065"	"26.69"	"0.49"	"5.30"	"7.43"	"False"	"CHEMBL4429697"	"Inhibition of recombinant human C-terminal 6His-tagged JAK2 (808 to end amino acids) expressed in Sf21 cells measured after 1 hr in presence of ATP by TR-FRET assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4428074"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2016"	"CHEMBL4106362"	""
"CHEMBL4466236"	""	"0"	"447.48"	"0"	"2.32"	"27"	"Cc1nccc(Nc2cc(N[C@@H]3CCN(c4ccc(C#N)cn4)C[C@@H]3F)c(C(N)=O)cn2)n1"	"IC50"	"'='"	"1.1"	"nM"	"8.96"	""	""	"UO_0000065"	"20.02"	"0.37"	"6.64"	"6.15"	"False"	"CHEMBL4429528"	"Inhibition of human JAK2 assessed as reduction in phosphorylation of Biotin-Lyn-Substrate-2 after 1 hr in presence of ATP by ELISA"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4428070"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2016"	"None"	""
"CHEMBL3642415"	""	"0"	"519.68"	"1"	"3.41"	"BDBM99693"	"CN1CCN(c2ccc(Nc3nc4c(CCc5ccccc5N(C)S(C)(=O)=O)cccn4n3)cc2)CC1"	"IC50"	"'='"	"218.02"	"nM"	"6.66"	""	"216382"	"UO_0000065"	"12.82"	"0.25"	"3.25"	"7.74"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652395"	""	"0"	"433.62"	"0"	"3.84"	"BDBM113207"	"CC[C@H]1CCCCC1NS(=O)(=O)C[C@H]1CC[C@H](N(C)c2ncnc3[nH]ccc23)CC1"	"IC50"	"'='"	"59.3"	"nM"	"7.23"	""	"234650"	"UO_0000065"	"16.67"	"0.33"	"3.39"	"7.94"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3665184"	""	"0"	"500.63"	"1"	"2.11"	"BDBM112578"	"CC(C)CS(=O)(=O)N1CCC[C@H](Nc2nc(N3CCOCC3)ncc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.049"	"nM"	"10.31"	""	"233815"	"UO_0000065"	"20.59"	"0.40"	"8.20"	"7.98"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL2062810"	""	"0"	"490.63"	"0"	"4.07"	"BDBM99555"	"CC(C)S(=O)(=O)c1ccc(-c2cccn3nc(Nc4cccc(N5CCN(C)CC5)c4)nc23)cc1"	"IC50"	"'='"	"1.3"	"nM"	"8.89"	""	"216246"	"UO_0000065"	"18.11"	"0.35"	"4.82"	"10.73"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3699474"	""	"0"	"325.37"	"0"	"1.95"	"BDBM147489"	"N#C[C@H]1CC[C@H](O)CC1n1cc(C(N)=O)c(Nc2ccccc2)n1"	"IC50"	"'='"	"79.0"	"nM"	"7.10"	""	"285414"	"UO_0000065"	"21.83"	"0.40"	"5.15"	"6.07"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702943"	""	"0"	"394.26"	"0"	"3.26"	"BDBM147645"	"N#C[C@H]1C[C@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)c(Cl)c2)n1"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	"285577"	"UO_0000065"	"19.53"	"0.40"	"4.44"	"6.58"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652391"	""	"0"	"552.71"	"1"	"2.39"	"BDBM113203"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCN(c3ncccc3C(=O)NC3CC3)CC2)CC1"	"IC50"	"'='"	"43.1"	"nM"	"7.37"	""	"234646"	"UO_0000065"	"13.33"	"0.26"	"4.98"	"5.78"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3647922"	""	"0"	"423.45"	"0"	"2.98"	"BDBM148037"	"N#C[C@@H]1CCCC[C@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)F)cc2)n1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"285979"	"UO_0000065"	"20.54"	"0.41"	"5.72"	"6.65"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703069"	""	"0"	"426.95"	"0"	"4.00"	"BDBM147779"	"C[C@H](N[C@@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@@H](C#N)C1)C1CC1"	"IC50"	"'='"	"216.0"	"nM"	"6.67"	""	"285713"	"UO_0000065"	"15.61"	"0.30"	"2.67"	"6.13"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703031"	""	"0"	"446.48"	"0"	"3.77"	"BDBM147741"	"N#C[C@H]1C[C@H](N2CCC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(CC(F)(F)F)cc2)n1"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	"285675"	"UO_0000065"	"18.13"	"0.35"	"4.33"	"8.10"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4777969"	""	"0"	"383.42"	"0"	"2.54"	"27, cis isomer"	"Cn1ccc(-c2cn3nccc3c(-c3cnn([C@]4(CC#N)C[C@H](C#N)C4)c3)n2)n1"	"IC50"	"'='"	"45.0"	"nM"	"7.35"	""	""	""	""	""	""	""	"False"	"CHEMBL4675813"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using FITC-KGGEEEEYFELVKK as substrate in presence of ATP at Km by microfluidic assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4673239"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4459585"	"ROPSACITINIB"	"2"	"383.42"	"0"	"2.54"	"22, PF-06826647"	"Cn1cc(-c2cn3nccc3c(-c3cnn([C@]4(CC#N)C[C@@H](C#N)C4)c3)n2)cn1"	"IC50"	"'='"	"74.0"	"nM"	"7.13"	""	""	""	""	""	""	""	"False"	"CHEMBL4675813"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using FITC-KGGEEEEYFELVKK as substrate in presence of ATP at Km by microfluidic assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4673239"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4740298"	""	"0"	"383.42"	"0"	"2.54"	"21, cis isomer"	"Cn1cc(-c2cn3nccc3c(-c3cnn([C@]4(CC#N)C[C@H](C#N)C4)c3)n2)cn1"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	""	""	""	""	""	""	"False"	"CHEMBL4675813"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using FITC-KGGEEEEYFELVKK as substrate in presence of ATP at Km by microfluidic assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4673239"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4781973"	""	"0"	"397.45"	"0"	"2.93"	"20, trans isomer"	"Cn1cc(-c2cn3nccc3c(-c3cnn([C@]4(CC#N)C[C@@H](CC#N)C4)c3)n2)cn1"	"IC50"	"'='"	"159.0"	"nM"	"6.80"	""	""	""	""	""	""	""	"False"	"CHEMBL4675813"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using FITC-KGGEEEEYFELVKK as substrate in presence of ATP at Km by microfluidic assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4673239"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4517702"	""	"0"	"356.43"	"0"	"1.34"	"22"	"CCNC(=O)N1[C@@H]2CC[C@@H]1CN(c1ccnc(Nc3cnn(C)c3)n1)C2"	"IC50"	"'='"	"538.0"	"nM"	"6.27"	""	""	"UO_0000065"	"17.59"	"0.33"	"4.93"	"6.87"	"False"	"CHEMBL4411595"	"Inhibition of human JAK2 using fluorescence labeled peptide as substrate and using 1 mM ATP by microfluidic based mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4411260"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3414599"	""	"0"	"501.63"	"2"	"5.23"	"38"	"O=C(CCCCCCN1C/C=C/COCc2cccc(c2)-c2ccnc(n2)Nc2cccc(c2)C1)NO"	"IC50"	"'='"	"613.0"	"nM"	"6.21"	""	""	"UO_0000065"	"12.38"	"0.23"	"0.98"	"6.24"	"False"	"CHEMBL3419812"	"Inhibition of human recombinant JAK2 using Z'LYTETry6 peptide substrate after 1 hr by microplate reader"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3414525"	"1"	"Scientific Literature"	"Eur. J. Med. Chem."	"2015"	"None"	""
"CHEMBL3417189"	""	"0"	"529.64"	"2"	"5.40"	"34"	"O=C(CCCCCCC(=O)N1C/C=C/CCOc2cccc(c2)-c2ccnc(n2)Nc2cccc(c2)C1)NO"	"IC50"	"'='"	"558.0"	"nM"	"6.25"	""	""	"UO_0000065"	"11.81"	"0.22"	"0.85"	"5.36"	"False"	"CHEMBL3419812"	"Inhibition of human recombinant JAK2 using Z'LYTETry6 peptide substrate after 1 hr by microplate reader"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3414525"	"1"	"Scientific Literature"	"Eur. J. Med. Chem."	"2015"	"None"	""
"CHEMBL1682365"	""	"0"	"419.51"	"0"	"2.82"	"5"	"O=C(Cc1ccccc1)N1CCN(c2nc(Nc3nccs3)c3cccn3n2)CC1"	"IC50"	"'='"	"59.0"	"nM"	"7.23"	""	""	"UO_0000065"	"17.23"	"0.33"	"4.41"	"9.19"	"False"	"CHEMBL1685409"	"Inhibition of JAK2 after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1681645"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL4238926"	""	"0"	"326.40"	"0"	"2.01"	"4"	"NC(=O)c1cnc2[nH]ccc2c1NC1C2CC3CC1CC(O)(C3)C2"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	""	"UO_0000065"	""	""	""	""	"True"	"CHEMBL4377456"	"Inhibition of JAK2 (unknown origin) in presence of Km ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4376812"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4476770"	""	"0"	"444.85"	"0"	"3.45"	"SAR-20347"	"NC(=O)c1nc(-c2c(F)cccc2Cl)oc1Nc1ccc(C(=O)N2CCOCC2)cc1"	"IC50"	"'='"	"26.0"	"nM"	"7.58"	""	""	"UO_0000065"	"17.05"	"0.33"	"4.14"	"6.85"	"False"	"CHEMBL4331753"	"Inhibition of JAK2 in human Jurkat cells assessed as reduction in IFN-alpha stimulated JAK2 phosphorylation by caspase3/7 reagent-based Western blot analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Jurkat"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4330088"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2019"	"CHEMBL3307526"	""
"CHEMBL4246788"	""	"0"	"340.43"	"0"	"2.67"	"17d"	"COC12CC3CC(C1)C(Nc1c(C(N)=O)cnc4[nH]ccc14)C(C3)C2"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4236469"	"Inhibition of recombinant human N-terminal His-tagged JAK2 catalytic domain (826 to 1132 residues) expressed in baculovirus expression system using Biotin-Lyn-Substrate2 after 1 hr by ELISA"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229549"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4239361"	""	"0"	"310.40"	"0"	"3.04"	"7c"	"NC(=O)c1cnc2[nH]ccc2c1NC12CC3CC(CC(C3)C1)C2"	"IC50"	"'='"	"120.0"	"nM"	"6.92"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4236469"	"Inhibition of recombinant human N-terminal His-tagged JAK2 catalytic domain (826 to 1132 residues) expressed in baculovirus expression system using Biotin-Lyn-Substrate2 after 1 hr by ELISA"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229549"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4447470"	""	"0"	"462.36"	"0"	"4.72"	"12f"	"CC(Oc1cc(-c2cncc(N3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl"	"IC50"	"'='"	"119.0"	"nM"	"6.92"	""	""	"UO_0000065"	"14.98"	"0.31"	"2.20"	"9.08"	"False"	"CHEMBL4341687"	"Inhibition of human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr by Z'-LYTE assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340536"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2019"	"CHEMBL3308860"	""
"CHEMBL4460084"	""	"0"	"425.94"	"1"	"5.73"	"12u"	"CC(Oc1cc(-c2cccc(C3CCNCC3)c2)cnc1N)c1cc(F)ccc1Cl"	"IC50"	"'='"	"35.0"	"nM"	"7.46"	""	""	"UO_0000065"	"17.50"	"0.34"	"1.73"	"12.39"	"False"	"CHEMBL4341687"	"Inhibition of human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr by Z'-LYTE assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340536"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2019"	"CHEMBL3308860"	""
"CHEMBL4550335"	""	"0"	"332.77"	"0"	"3.99"	"12q"	"CC(Oc1cc(-c2cn[nH]c2)cnc1N)c1cc(F)ccc1Cl"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	""	"UO_0000065"	"23.43"	"0.46"	"3.81"	"10.15"	"False"	"CHEMBL4341687"	"Inhibition of human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr by Z'-LYTE assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340536"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2019"	"CHEMBL3308860"	""
"CHEMBL1825137"	""	"0"	"451.33"	"1"	"5.46"	"12e"	"CC(Oc1cc(-c2cnn(C3CCOCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl"	"IC50"	"'='"	"65.0"	"nM"	"7.19"	""	""	"UO_0000065"	"15.92"	"0.33"	"1.73"	"9.56"	"False"	"CHEMBL4341687"	"Inhibition of human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr by Z'-LYTE assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340536"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2019"	"CHEMBL3308860"	""
"CHEMBL4461011"	""	"0"	"322.41"	"0"	"3.56"	"14"	"CC(C)(C)CNc1c(C(N)=O)cnn2cc(-c3ccccc3)cc12"	"IC50"	"'='"	"110.0"	"nM"	"6.96"	""	""	"UO_0000065"	"21.58"	"0.40"	"3.40"	"9.61"	"False"	"CHEMBL4339747"	"Inhibition of GST-tagged JAK2 (unknown origin) using fluoresceinated peptide as substrate measured after 3 hrs by electrophoresis method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4339199"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2019"	"None"	""
"CHEMBL4440767"	""	"0"	"397.44"	"0"	"1.05"	"19"	"COc1ccc(-c2cc3c(NC(CO)[C@H](O)C4CC4)c(C(N)=O)cnn3c2)cn1"	"IC50"	"'='"	"45.0"	"nM"	"7.35"	""	""	"UO_0000065"	"18.49"	"0.35"	"6.30"	"5.44"	"False"	"CHEMBL4339747"	"Inhibition of GST-tagged JAK2 (unknown origin) using fluoresceinated peptide as substrate measured after 3 hrs by electrophoresis method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4339199"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2019"	"None"	""
"CHEMBL4237557"	""	"0"	"347.42"	"0"	"3.98"	"27"	"C=CC(=O)Nc1cccc(-c2ccc(C(N)=O)c3[nH]c(C)c(C)c23)c1C"	"IC50"	"'>'"	"2000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4235700"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229517"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2018"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"Tofacitinib"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"1.4"	"nM"	"8.85"	""	""	"UO_0000065"	"28.34"	"0.53"	"7.31"	"9.96"	"True"	"CHEMBL3784139"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3779778"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL1789941"	"RUXOLITINIB"	"4"	"306.37"	"0"	"3.47"	"Ruxolitinib"	"N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"0.12"	"nM"	"9.92"	""	""	"UO_0000065"	"32.38"	"0.59"	"6.45"	"11.93"	"False"	"CHEMBL3784139"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3779778"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3780091"	""	"0"	"323.40"	"0"	"2.60"	"10"	"N[C@H]1CC[C@@H](Nc2cc[nH]c(=O)c2-c2nc3ccccc3[nH]2)CC1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	""	"UO_0000065"	"25.97"	"0.48"	"5.80"	"8.43"	"False"	"CHEMBL3784139"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3779778"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL4581017"	""	"0"	"481.45"	"0"	"4.77"	"8r"	"O=C(CCCCCCn1cc(Nc2ncc(C(F)(F)F)c(Nc3ccc(F)cc3)n2)cn1)NO"	"IC50"	"'>'"	"100.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4347596"	"Inhibition of recombinant human JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate measured after 60 mins by LANCE assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4346670"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4584008"	""	"0"	"461.93"	"0"	"4.80"	"8x"	"O=C(CCCCCCCn1cc(Nc2ncc(Cl)c(Nc3ccc(F)cc3)n2)cn1)NO"	"IC50"	"'='"	"61.0"	"nM"	"7.21"	""	""	"UO_0000065"	"15.62"	"0.31"	"2.41"	"6.17"	"False"	"CHEMBL4347596"	"Inhibition of recombinant human JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate measured after 60 mins by LANCE assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4346670"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4443462"	""	"0"	"429.91"	"0"	"4.27"	"8d"	"O=C(CCCCCCn1cc(Nc2ncc(Cl)c(Nc3ccccc3)n2)cn1)NO"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	""	"UO_0000065"	"18.42"	"0.36"	"3.65"	"6.77"	"False"	"CHEMBL4347596"	"Inhibition of recombinant human JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate measured after 60 mins by LANCE assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4346670"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4520721"	""	"0"	"447.90"	"0"	"4.41"	"8f"	"O=C(CCCCCCn1cc(Nc2ncc(Cl)c(Nc3ccc(F)cc3)n2)cn1)NO"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	""	"UO_0000065"	"17.47"	"0.34"	"3.41"	"6.69"	"False"	"CHEMBL4347596"	"Inhibition of recombinant human JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate measured after 60 mins by LANCE assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4346670"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4167286"	""	"0"	"609.75"	"1"	"4.05"	"20g"	"CS(=O)(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCC(C(=O)NCCCCCCC(=O)NO)CC4)cc3)n2)cc1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	""	"UO_0000065"	"14.27"	"0.28"	"4.65"	"5.25"	"False"	"CHEMBL4150584"	"Inhibition of JAK2 (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition and measured after 25 mins in presence of ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4145634"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4173676"	""	"0"	"508.98"	"1"	"4.05"	"3"	"CN1CCN(c2cc(Nc3nccc(Nc4ccc(F)c(Cl)c4F)n3)cc(S(C)(=O)=O)c2)CC1"	"IC50"	"'='"	"36.0"	"nM"	"7.44"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4145184"	"Inhibition of recombinant human JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate after 10 mins by caliper assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4138312"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4173429"	""	"0"	"468.58"	"0"	"2.58"	"12"	"Cc1cnc(Nc2cc(N3CCNCC3)cc(S(C)(=O)=O)c2)nc1Nc1cccc(CO)c1"	"IC50"	"'='"	"951.0"	"nM"	"6.02"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4145184"	"Inhibition of recombinant human JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate after 10 mins by caliper assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4138312"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4177188"	""	"0"	"512.64"	"1"	"2.28"	"15"	"Cc1cnc(Nc2cc(N3CCN(CCO)CC3)cc(S(C)(=O)=O)c2)nc1Nc1cccc(CO)c1"	"IC50"	"'='"	"817.0"	"nM"	"6.09"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4145184"	"Inhibition of recombinant human JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate after 10 mins by caliper assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4138312"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL272888"	""	"0"	"589.62"	"2"	"5.80"	"13b"	"Cc1ccc(NC(=O)c2cccc(C(F)(F)F)c2)cc1C(=O)Nc1cnc(Nc2ccc(N3CCN(C)CC3)cc2)nc1"	"IC50"	"'>'"	"1030.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL952061"	"Inhibition of Jak2 by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1144680"	"1"	"Scientific Literature"	"J. Med. Chem."	"2008"	"None"	""
"CHEMBL4092807"	""	"0"	"531.67"	"1"	"3.77"	"62"	"CCOc1nn(C)cc1Nc1ncc(C)c(-c2c[nH]c3c(NC(=O)[C@@H](CC)N4CCN(C)CC4)cccc23)n1"	"IC50"	"'='"	"5010.0"	"nM"	"5.30"	""	""	"UO_0000065"	"9.97"	"0.19"	"1.53"	"4.56"	"False"	"CHEMBL4022634"	"Inhibition of N-terminal GST fused recombinant JAK2 (831 to 1132 amino acids) (unknown origin) expressed in insect cells using ATP and peptide substrate (5FAM-GEEPLYWSFPAKKK-NH2"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020810"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2017"	"None"	""
"CHEMBL4470529"	""	"0"	"588.13"	"1"	"4.61"	"15"	"COc1cc(N2CCN(CCN(C)C)C2=O)ccc1Nc1ncc(Cl)c(Nc2ccccc2S(=O)(=O)C(C)C)n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4348497"	"Inhibition of N-terminal GST-tagged human JAK2 catalytic domain (826 to 1132 residues) expressed in Baculovirus expression system using srctide as substrate incubated for 1 hr by mobility shift assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4346688"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2019"	"None"	""
"CHEMBL4170235"	""	"0"	"468.58"	"0"	"2.61"	"5"	"CN1CCN(c2cc(Nc3nccc(Nc4cccc(CO)c4)n3)cc(S(C)(=O)=O)c2)CC1"	"IC50"	"'='"	"13900.0"	"nM"	"4.86"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4145184"	"Inhibition of recombinant human JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate after 10 mins by caliper assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4138312"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4165344"	""	"0"	"615.72"	"1"	"3.91"	"20c"	"CS(=O)(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCC(C(=O)NCc5ccc(C(=O)NO)cc5)CC4)cc3)n2)cc1"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	""	"UO_0000065"	"12.58"	"0.24"	"3.83"	"4.68"	"False"	"CHEMBL4150584"	"Inhibition of JAK2 (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition and measured after 25 mins in presence of ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4145634"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL2207759"	""	"0"	"458.57"	"0"	"3.76"	"10g"	"CN1CCC[C@@H]1C(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"745.7"	"nM"	"6.13"	""	""	"UO_0000065"	"13.36"	"0.25"	"2.37"	"7.42"	"False"	"CHEMBL2214785"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT1 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL2208035"	""	"0"	"458.52"	"0"	"2.94"	"10e"	"O=C1CC[C@H](C(=O)Nc2ccc(-c3ccnc(Nc4ccc(N5CCOCC5)cc4)n3)cc2)N1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2214785"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT1 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL1614712"	""	"0"	"439.56"	"0"	"4.92"	"NVP-AEW541"	"Nc1ncnc2c1c(-c1cccc(OCc3ccccc3)c1)cn2[C@H]1C[C@@H](CN2CCC2)C1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3789994"	"Inhibition of JAK2 (unknown origin) in presence of [gamma33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3785066"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL2325894"	""	"0"	"338.37"	"0"	"0.94"	"3p"	"C[C@@H](NC(=O)c1c[nH]c2ncc(C3CC3)nc12)C(=O)N1CC(C#N)C1"	"IC50"	"'='"	"36.8"	"nM"	"7.43"	""	""	"UO_0000065"	"21.97"	"0.41"	"6.49"	"6.48"	"False"	"CHEMBL2329570"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 30 mins by scintillation counting analysis in presence of [gamma-33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321829"	"1"	"Scientific Literature"	"J. Med. Chem."	"2013"	"None"	""
"CHEMBL2325901"	""	"0"	"244.30"	"0"	"1.97"	"3a"	"CC(C)NC(=O)c1c[nH]c2ncc(C3CC3)nc12"	"IC50"	"'='"	"106.2"	"nM"	"6.97"	""	""	"UO_0000065"	"28.55"	"0.53"	"5.00"	"9.87"	"False"	"CHEMBL2329570"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 30 mins by scintillation counting analysis in presence of [gamma-33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321829"	"1"	"Scientific Literature"	"J. Med. Chem."	"2013"	"None"	""
"CHEMBL1789941"	"RUXOLITINIB"	"4"	"306.37"	"0"	"3.47"	"1"	"N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	""	"UO_0000065"	"26.26"	"0.48"	"4.58"	"9.67"	"True"	"CHEMBL3803216"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797141"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2016"	"None"	""
"CHEMBL2325910"	""	"0"	"327.39"	"0"	"1.58"	"3l"	"C[C@@H](NC(=O)c1c[nH]c2ncc(C3CC3)nc12)C(=O)N1CCCC1"	"IC50"	"'='"	"121.6"	"nM"	"6.92"	""	""	"UO_0000065"	"21.12"	"0.39"	"5.34"	"7.60"	"False"	"CHEMBL2329570"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 30 mins by scintillation counting analysis in presence of [gamma-33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321829"	"1"	"Scientific Literature"	"J. Med. Chem."	"2013"	"None"	""
"CHEMBL3126344"	""	"0"	"425.20"	"1"	"5.54"	"19"	"O=c1[nH]ccc2c(Nc3c(Cl)cc(C(F)(F)F)cc3Cl)nc3ccncc3c12"	"IC50"	"'='"	"49.0"	"nM"	"7.31"	""	""	"UO_0000065"	"17.19"	"0.36"	"1.77"	"10.34"	"False"	"CHEMBL3131375"	"Inhibition of Jak2 (unknown origin) assessed as inhibition of STAT5 phosphorylation by cell-based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3124786"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3126343"	""	"0"	"441.20"	"1"	"5.42"	"18"	"O=c1[nH]ccc2c(Nc3c(Cl)cc(OC(F)(F)F)cc3Cl)nc3ccncc3c12"	"IC50"	"'='"	"140.0"	"nM"	"6.85"	""	""	"UO_0000065"	"15.53"	"0.32"	"1.43"	"8.58"	"False"	"CHEMBL3131375"	"Inhibition of Jak2 (unknown origin) assessed as inhibition of STAT5 phosphorylation by cell-based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3124786"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3126342"	""	"0"	"358.19"	"0"	"3.92"	"17"	"O=c1[nH]ccc2c(Nc3c(Cl)cncc3Cl)nc3ccncc3c12"	"IC50"	"'='"	"24.0"	"nM"	"7.62"	""	""	"UO_0000065"	"21.27"	"0.43"	"3.70"	"9.12"	"False"	"CHEMBL3131375"	"Inhibition of Jak2 (unknown origin) assessed as inhibition of STAT5 phosphorylation by cell-based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3124786"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3126349"	""	"0"	"437.23"	"0"	"4.82"	"31"	"O=c1[nH]ccc2c(Nc3c(Cl)cc(C(O)C(F)F)cc3Cl)nc3ccncc3c12"	"IC50"	"'='"	"0.2"	"nM"	"9.70"	""	""	"UO_0000065"	"22.18"	"0.46"	"4.88"	"10.67"	"False"	"CHEMBL3131376"	"Inhibition of recombinant Jak2 (unknown origin) using biotinylated synthetic peptide substrate by homogeneous time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3124786"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3126345"	""	"0"	"374.30"	"0"	"4.37"	"20"	"O=c1[nH]ccc2c(Nc3c(F)cccc3C(F)(F)F)nc3ccncc3c12"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	""	"UO_0000065"	"21.50"	"0.41"	"3.68"	"11.38"	"False"	"CHEMBL3131376"	"Inhibition of recombinant Jak2 (unknown origin) using biotinylated synthetic peptide substrate by homogeneous time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3124786"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"CP-690550"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	""	"UO_0000065"	"25.48"	"0.47"	"6.42"	"8.95"	"True"	"CHEMBL908418"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139695"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2006"	"None"	""
"CHEMBL374854"	""	"0"	"302.34"	"0"	"2.82"	"13"	"c1ccc(CNc2ccnc(-n3cnc4ccncc43)n2)cc1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL908418"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139695"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2006"	"None"	""
"CHEMBL218746"	""	"0"	"350.81"	"0"	"4.04"	"11"	"C[C@H](Nc1ccnc(-n2cnc3ccncc32)n1)c1ccc(Cl)cc1"	"IC50"	"'='"	"51.0"	"nM"	"7.29"	""	""	"UO_0000065"	"20.79"	"0.40"	"3.25"	"10.64"	"False"	"CHEMBL908418"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139695"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2006"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"1"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"1.4"	"nM"	"8.85"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4032997"	"Inhibition of GST-tagged recombinant human JAK2 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 as substrate preincubated for 30 mins followed by ATP addition measured after 120 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4104623"	""	"0"	"329.34"	"0"	"1.97"	"15"	"N#C[C@H]1CCOC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4032997"	"Inhibition of GST-tagged recombinant human JAK2 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 as substrate preincubated for 30 mins followed by ATP addition measured after 120 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4066906"	""	"0"	"416.46"	"0"	"1.18"	"23"	"C[C@@H]1NS(=O)(=O)c2ccc(Nc3nn([C@H]4COCC[C@@H]4C#N)cc3C(N)=O)cc21"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4032997"	"Inhibition of GST-tagged recombinant human JAK2 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 as substrate preincubated for 30 mins followed by ATP addition measured after 120 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4104623"	""	"0"	"329.34"	"0"	"1.97"	"15"	"N#C[C@H]1CCOC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"334.0"	"nM"	"6.48"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4033007"	"Inhibition of JAK2 in EPO-stimulated human TF1 cells expressing stably integrated beta-lactamase reporter gene under control of STAT5 response elements in interferon regulatory factor 1 gene promoter by fluorescence assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4102140"	""	"0"	"377.35"	"0"	"2.43"	"17"	"N#C[C@H]1CCOC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(OC(F)F)cc2)n1"	"IC50"	"'='"	"54.0"	"nM"	"7.27"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4033007"	"Inhibition of JAK2 in EPO-stimulated human TF1 cells expressing stably integrated beta-lactamase reporter gene under control of STAT5 response elements in interferon regulatory factor 1 gene promoter by fluorescence assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL2207767"	""	"0"	"423.48"	"1"	"5.10"	"6b"	"CC(=O)Nc1ccc(-c2ccnc(Nc3cccc(NC(=O)c4ccccc4)c3)n2)cc1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2214785"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT1 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL2208028"	""	"0"	"403.49"	"0"	"3.99"	"9c"	"CC(=O)Nc1ccc(-c2nc(Nc3ccc(N4CCOCC4)cc3)ncc2C)cc1"	"IC50"	"'='"	"5.1"	"nM"	"8.29"	""	""	"UO_0000065"	"20.55"	"0.38"	"4.30"	"10.45"	"False"	"CHEMBL2214787"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL2208026"	""	"0"	"389.46"	"0"	"3.68"	"9a"	"CC(=O)Nc1ccc(-c2cc(Nc3ccc(N4CCOCC4)cc3)ncn2)cc1"	"IC50"	"'>'"	"980.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2214787"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL2208025"	""	"0"	"389.46"	"0"	"3.68"	"7b"	"CC(=O)Nc1ccc(-c2ccnc(Nc3cccc(N4CCOCC4)c3)n2)cc1"	"IC50"	"'='"	"4.2"	"nM"	"8.38"	""	""	"UO_0000065"	"21.51"	"0.39"	"4.70"	"10.55"	"False"	"CHEMBL2214787"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL2208024"	""	"0"	"387.49"	"0"	"4.84"	"7a"	"CC(=O)Nc1ccc(-c2ccnc(Nc3cccc(N4CCCCC4)c3)n2)cc1"	"IC50"	"'='"	"6.5"	"nM"	"8.19"	""	""	"UO_0000065"	"21.13"	"0.39"	"3.35"	"11.67"	"False"	"CHEMBL2214787"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL2208027"	""	"0"	"407.45"	"0"	"3.82"	"9b"	"CC(=O)Nc1ccc(-c2nc(Nc3ccc(N4CCOCC4)cc3)ncc2F)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL2214784"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT3 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL2207763"	""	"0"	"470.36"	"0"	"4.59"	"4"	"CC(=O)Nc1ccc(-c2ccnc(NCC3CN(C(=O)c4c(Cl)cccc4Cl)C3)n2)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL2214784"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT3 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL4250891"	""	"0"	"520.59"	"1"	"4.00"	"13c"	"COCCn1cc(-c2nc(Nc3ccc(NC(=O)CCCCCCC(=O)NO)cc3)nc3[nH]ccc23)cn1"	"IC50"	"'='"	"2.3"	"nM"	"8.64"	""	""	"UO_0000065"	"16.59"	"0.31"	"4.64"	"5.43"	"False"	"CHEMBL4233426"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma-33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229421"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2018"	"None"	""
"CHEMBL4102140"	""	"0"	"377.35"	"0"	"2.43"	"17"	"N#C[C@H]1CCOC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(OC(F)F)cc2)n1"	"IC50"	"'='"	"0.8"	"nM"	"9.10"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4032997"	"Inhibition of GST-tagged recombinant human JAK2 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 as substrate preincubated for 30 mins followed by ATP addition measured after 120 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4072848"	""	"0"	"366.38"	"0"	"1.71"	"24"	"COc1cc(Nc2nn([C@H]3COCC[C@@H]3C#N)cc2C(N)=O)ccc1C#N"	"IC50"	"'='"	"3.2"	"nM"	"8.49"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4032997"	"Inhibition of GST-tagged recombinant human JAK2 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 as substrate preincubated for 30 mins followed by ATP addition measured after 120 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL1258913"	""	"0"	"544.68"	"1"	"4.28"	"38"	"O=C(Nc1n[nH]c2cc(C(=O)N[C@H](CN3CCCC3)c3ccccc3)sc12)c1ccc(N2CCOCC2)cc1"	"IC50"	"'='"	"1721.0"	"nM"	"5.76"	""	""	"UO_0000065"	"10.58"	"0.20"	"1.48"	"5.62"	"False"	"CHEMBL1260175"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1255180"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2010"	"None"	""
"CHEMBL4175964"	""	"0"	"567.67"	"1"	"2.88"	"20d"	"CS(=O)(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCC(C(=O)NCCCC(=O)NO)CC4)cc3)n2)cc1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	""	"UO_0000065"	"15.85"	"0.31"	"6.12"	"5.43"	"False"	"CHEMBL4150584"	"Inhibition of JAK2 (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition and measured after 25 mins in presence of ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4145634"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4169802"	""	"0"	"616.68"	"1"	"4.51"	"12a"	"N#CCNC(=O)c1ccc(-c2ccnc(Nc3ccc(N4CCC(C(=O)Nc5ccc(/C=C/C(=O)NO)cc5)CC4)cc3)n2)cc1"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	""	"UO_0000065"	"12.69"	"0.23"	"3.31"	"4.54"	"False"	"CHEMBL4150584"	"Inhibition of JAK2 (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition and measured after 25 mins in presence of ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4145634"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3764277"	""	"0"	"384.48"	"0"	"2.82"	"18"	"CC(C)[C@H](C)n1cc(-c2cc(C3CCOCC3)n(C)n2)c2[nH]nc(N)c2c1=O"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	""	"UO_0000065"	"20.60"	"0.39"	"5.10"	"7.63"	"False"	"CHEMBL3766653"	"Inhibition of JAK2 (unknown origin) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent substrate phosphorylation after 45 mins by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3763089"	"1"	"Scientific Literature"	"J. Med. Chem."	"2016"	"None"	""
"CHEMBL2381116"	""	"0"	"450.52"	"0"	"2.37"	"39"	"COc1ccc2c(c1)C(=O)N(c1nc(C(=O)Nc3cnccc3N3CCNCC3)cs1)C2"	"IC50"	"'='"	"21000.0"	"nM"	"4.68"	""	""	"UO_0000065"	"10.38"	"0.20"	"2.31"	"4.69"	"False"	"CHEMBL2384683"	"Inhibition of human JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2380296"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL1682387"	""	"0"	"452.47"	"0"	"2.67"	"27"	"Cc1cc(Nc2nc(N3CCN(C(=O)Cc4ccc(F)cc4F)CC3)nn3cccc23)n[nH]1"	"IC50"	"'='"	"2.4"	"nM"	"8.62"	""	""	"UO_0000065"	"19.05"	"0.36"	"5.95"	"9.13"	"False"	"CHEMBL1685409"	"Inhibition of JAK2 after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1681645"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL3685796"	"MRL-SYKi"	"0"	"452.58"	"1"	"5.06"	"MRL-SYKi"	"Cc1cc(Nc2nccc(C)n2)cc(-c2cnc([C@@]3(O)CC[C@H](C(=O)O)C(C)(C)C3)s2)c1"	"IC50"	""	"242.0"	"nM"	""	""	"Not Active"	""	""	""	""	""	"False"	"CHEMBL4510261"	"Invitrogen kinase assay (JAK2)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4507285"	"54"	"Donated Chemical Probes - SGC Frankfurt"	""	"2021"	"None"	""
"CHEMBL4454783"	""	"0"	"366.43"	"0"	"1.47"	"11p"	"C=CC(=O)N1CCCC(n2nc(-c3cc(C)n(C)n3)c3c(N)ncnc32)C1"	"IC50"	"'='"	"57.2"	"nM"	"7.24"	""	""	"UO_0000065"	"19.77"	"0.37"	"5.77"	"6.72"	"False"	"CHEMBL4402146"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-biotin as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4400567"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4440612"	""	"0"	"388.44"	"0"	"2.29"	"11n"	"C=CC(=O)Nc1cccc(Cn2nc(-c3cc(C)n(C)n3)c3c(N)ncnc32)c1"	"IC50"	"'='"	"397.4"	"nM"	"6.40"	""	""	"UO_0000065"	"16.48"	"0.30"	"4.11"	"5.49"	"False"	"CHEMBL4402146"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-biotin as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4400567"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4590390"	""	"0"	"423.48"	"0"	"1.11"	"11h"	"Cn1nc(-c2nn(C3CCCN(C(=O)CC#N)C3)c3ncnc(N)c23)cc1C(C)(C)O"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	""	"UO_0000065"	"19.12"	"0.36"	"6.99"	"5.33"	"False"	"CHEMBL4402146"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-biotin as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4400567"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4517080"	""	"0"	"365.24"	"0"	"1.60"	"10h"	"C=CC(=O)N1CCCC(Cn2nc(Br)c3c(N)ncnc32)C1"	"IC50"	"'='"	"72.3"	"nM"	"7.14"	""	""	"UO_0000065"	"19.55"	"0.44"	"5.54"	"7.94"	"False"	"CHEMBL4402146"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-biotin as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4400567"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4228766"	""	"0"	"448.52"	"0"	"4.42"	"8; SB1578"	"C1=C/COc2ccc(o2)-c2ccnc(n2)Nc2ccc(OCCN3CCCC3)c(c2)COC/1"	"IC50"	"'='"	"46.0"	"nM"	"7.34"	""	""	"UO_0000065"	"16.36"	"0.30"	"2.92"	"8.96"	"False"	"CHEMBL4220350"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219057"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4554776"	""	"0"	"398.21"	"0"	"1.36"	"10d"	"C=CC(=O)N1CCCC(n2nc(I)c3c(N)ncnc32)C1"	"IC50"	"'='"	"82.4"	"nM"	"7.08"	""	""	"UO_0000065"	"17.79"	"0.46"	"5.72"	"7.88"	"False"	"CHEMBL4402146"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-biotin as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4400567"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL1630791"	""	"0"	"303.37"	"0"	"0.62"	"17d"	"C[C@@H]1CCN(C(=O)CO)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"480.0"	"nM"	"6.32"	""	""	"UO_0000065"	"20.83"	"0.39"	"5.70"	"7.40"	"False"	"CHEMBL1641117"	"Inhibition of GST-tagged human JAK2 catalytic domain expressed in Sf9 cells by ELISA"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1629452"	"1"	"Scientific Literature"	"J. Med. Chem."	"2010"	"CHEMBL3308860"	""
"CHEMBL1630789"	""	"0"	"385.50"	"0"	"3.10"	"17b"	"Cc1cc(NC(=O)N2CC[C@@H](C)[C@@H](N(C)c3ncnc4[nH]ccc34)C2)sn1"	"IC50"	"'='"	"510.0"	"nM"	"6.29"	""	""	"UO_0000065"	"16.32"	"0.32"	"3.19"	"6.99"	"False"	"CHEMBL1641117"	"Inhibition of GST-tagged human JAK2 catalytic domain expressed in Sf9 cells by ELISA"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1629452"	"1"	"Scientific Literature"	"J. Med. Chem."	"2010"	"CHEMBL3308860"	""
"CHEMBL1630790"	""	"0"	"371.44"	"0"	"3.58"	"17c"	"C[C@@H]1CCN(Cc2cccc(F)c2F)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"1440.0"	"nM"	"5.84"	""	""	"UO_0000065"	"15.73"	"0.30"	"2.26"	"12.16"	"False"	"CHEMBL1641117"	"Inhibition of GST-tagged human JAK2 catalytic domain expressed in Sf9 cells by ELISA"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1629452"	"1"	"Scientific Literature"	"J. Med. Chem."	"2010"	"CHEMBL3308860"	""
"CHEMBL1835014"	""	"0"	"272.28"	"0"	"2.39"	"3"	"CCNc1ncc(C(N)=O)c2[nH]c3ccc(F)cc3c12"	"IC50"	"'='"	"230.0"	"nM"	"6.64"	""	""	"UO_0000065"	"24.38"	"0.45"	"4.25"	"7.92"	"False"	"CHEMBL1840115"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835153"	""	"0"	"441.42"	"0"	"3.61"	"65"	"NC(=O)c1cnc(N[C@H](C2CC2)C(F)(F)F)c2c1[nH]c1cc(-c3cnc(N)nc3)ccc12"	"IC50"	"'='"	"0.4"	"nM"	"9.40"	""	""	"UO_0000065"	"21.29"	"0.40"	"5.79"	"6.93"	"False"	"CHEMBL1840111"	"Inhibition of JAK2 V617F mutant"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835014"	""	"0"	"272.28"	"0"	"2.39"	"3"	"CCNc1ncc(C(N)=O)c2[nH]c3ccc(F)cc3c12"	"IC50"	"'='"	"230.0"	"nM"	"6.64"	""	""	"UO_0000065"	"24.38"	"0.45"	"4.25"	"7.92"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835024"	""	"0"	"326.38"	"0"	"3.70"	"27"	"NC(=O)c1cnc(NC2CCCCC2)c2c1[nH]c1ccc(F)cc12"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	""	"UO_0000065"	"23.81"	"0.44"	"4.07"	"9.27"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835025"	""	"0"	"340.40"	"0"	"4.09"	"28"	"NC(=O)c1cnc(NC2CCCCCC2)c2c1[nH]c1ccc(F)cc12"	"IC50"	"'='"	"19.0"	"nM"	"7.72"	""	""	"UO_0000065"	"22.68"	"0.42"	"3.63"	"9.21"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835033"	""	"0"	"384.48"	"1"	"5.23"	"36"	"NC(=O)c1cnc(NC2CCCCC2)c2c1[nH]c1cc(-c3ccccc3)ccc12"	"IC50"	"'='"	"70.0"	"nM"	"7.16"	""	""	"UO_0000065"	"18.61"	"0.34"	"1.92"	"8.54"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1834948"	""	"0"	"402.50"	"0"	"4.31"	"45"	"C[C@H](Nc1ccc(C(N)=O)c2[nH]c3cc(-c4ccnc(N)n4)ccc3c12)C(C)(C)C"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	""	"UO_0000065"	"19.68"	"0.36"	"3.61"	"6.45"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835151"	""	"0"	"511.51"	"1"	"3.86"	"63"	"NC(=O)c1cnc(N[C@H](C2CC2)C(F)(F)F)c2c1[nH]c1cc(-c3cnc(N4CCOCC4)nc3)ccc12"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	""	"UO_0000065"	"15.83"	"0.30"	"4.24"	"6.63"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL2035187"	"PACRITINIB"	"3"	"472.59"	"0"	"4.96"	"3; SB1518"	"C1=C/COCc2cc(ccc2OCCN2CCCC2)Nc2nccc(n2)-c2cccc(c2)COC/1"	"IC50"	"'='"	"22.0"	"nM"	"7.66"	""	""	"UO_0000065"	"16.20"	"0.30"	"2.70"	"11.14"	"False"	"CHEMBL4360609"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4359824"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2019"	"None"	""
"CHEMBL4469583"	""	"0"	"340.38"	"0"	"1.25"	"25"	"C[C@@H](O)[C@H](CO)Nc1c(C(N)=O)cnn2cc(-c3ccccc3)cc12"	"IC50"	"'='"	"1700.0"	"nM"	"5.77"	""	""	"UO_0000065"	"16.95"	"0.32"	"4.52"	"5.11"	"False"	"CHEMBL4339747"	"Inhibition of GST-tagged JAK2 (unknown origin) using fluoresceinated peptide as substrate measured after 3 hrs by electrophoresis method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4339199"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2019"	"None"	""
"CHEMBL4568896"	""	"0"	"357.37"	"0"	"0.27"	"20"	"COc1ccc(-c2cc3c(NC(CO)CO)c(C(N)=O)cnn3c2)cn1"	"IC50"	"'='"	"240.0"	"nM"	"6.62"	""	""	"UO_0000065"	"18.52"	"0.35"	"6.35"	"4.90"	"False"	"CHEMBL4339747"	"Inhibition of GST-tagged JAK2 (unknown origin) using fluoresceinated peptide as substrate measured after 3 hrs by electrophoresis method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4339199"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2019"	"None"	""
"CHEMBL4075230"	""	"0"	"285.35"	"0"	"1.40"	"8"	"CC(=O)N1CC[C@H]2CCN(c3ncnc4[nH]ccc34)[C@H]2C1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4005719"	"Inhibition of recombinant human GST-tagged cytoplasmic JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by microfluidic assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4004825"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL1682374"	""	"0"	"416.49"	"0"	"2.78"	"14"	"Cc1ccc(C(=O)N2CCN(c3nc(Nc4cc(C)[nH]n4)c4cccn4n3)CC2)cc1"	"IC50"	"'='"	"4.5"	"nM"	"8.35"	""	""	"UO_0000065"	"20.04"	"0.37"	"5.57"	"8.84"	"False"	"CHEMBL1685409"	"Inhibition of JAK2 after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1681645"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1682375"	""	"0"	"427.47"	"0"	"2.34"	"15"	"Cc1cc(Nc2nc(N3CCN(C(=O)c4ccccc4C#N)CC3)nn3cccc23)n[nH]1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	""	"UO_0000065"	"19.23"	"0.35"	"5.88"	"6.95"	"False"	"CHEMBL1685409"	"Inhibition of JAK2 after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1681645"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1682366"	""	"0"	"456.55"	"0"	"3.14"	"6"	"CC1(c2cc(Nc3nc(N4CCN(C(=O)Cc5ccccc5)CC4)nn4cccc34)n[nH]2)CC1"	"IC50"	"'='"	"22.0"	"nM"	"7.66"	""	""	"UO_0000065"	"16.77"	"0.31"	"4.52"	"8.11"	"False"	"CHEMBL1685409"	"Inhibition of JAK2 after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1681645"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL3763310"	""	"0"	"385.84"	"0"	"4.11"	"1"	"O=C(O)Cc1cnc(Nc2n[nH]c3ccc(-c4ncccc4Cl)cc23)s1"	"IC50"	"'='"	"7100.0"	"nM"	"5.15"	""	""	"UO_0000065"	"13.34"	"0.27"	"1.04"	"4.96"	"False"	"CHEMBL3766653"	"Inhibition of JAK2 (unknown origin) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent substrate phosphorylation after 45 mins by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3763089"	"1"	"Scientific Literature"	"J. Med. Chem."	"2016"	"None"	""
"CHEMBL4564021"	""	"0"	"433.88"	"0"	"4.02"	"8w"	"O=C(CCCCCn1cc(Nc2ncc(Cl)c(Nc3ccc(F)cc3)n2)cn1)NO"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	""	"UO_0000065"	"19.13"	"0.38"	"4.28"	"7.10"	"False"	"CHEMBL4347596"	"Inhibition of recombinant human JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate measured after 60 mins by LANCE assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4346670"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL3952338"	""	"0"	"545.02"	"1"	"4.37"	"141"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CC3CCC(C2)N3C(=O)c2ccc(Cl)c(F)c2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3904877"	""	"0"	"551.55"	"1"	"4.81"	"273"	"N#CCC1(n2ccc(-c3ncnc4[nH]ccc34)c2)CN(C2CCN(C(=O)c3cc(C(F)(F)F)ccc3F)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3958893"	""	"0"	"510.60"	"1"	"4.06"	"288"	"COc1ccccc1NC(=O)N1CCC(N2CC(CC#N)(n3ccc(-c4ncnc5[nH]ccc45)c3)C2)CC1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3965794"	""	"0"	"549.56"	"1"	"4.46"	"290"	"N#CCC1(n2ccc(-c3ncnc4[nH]ccc34)c2)CN(C2CCN(C(=O)Nc3ncccc3C(F)(F)F)CC2)C1"	"IC50"	"'>'"	"100.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3972221"	""	"0"	"507.59"	"1"	"4.17"	"302"	"N#CCC1(n2cc(-c3ccnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)C3CCC(F)(F)CC3)CC2)C1"	"IC50"	"'>'"	"100.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3986300"	""	"0"	"502.53"	"1"	"3.33"	"319"	"N#CCC1(n2cc(-c3c(F)cnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(F)cn3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3908463"	""	"0"	"517.54"	"1"	"3.64"	"323"	"N#CCC1(n2cc(-c3c(F)cnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(O)cc3F)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3622826"	""	"0"	"287.37"	"0"	"0.56"	"5c"	"NCCn1c(C2CCNCC2)nc2cc(C(N)=O)ccc21"	"IC50"	"'='"	"3150.0"	"nM"	"5.50"	""	""	"UO_0000065"	"19.14"	"0.36"	"4.94"	"5.56"	"False"	"CHEMBL3625898"	"Inhibition of JAK2 (unknown origin) using 35 uM of ATP and Tyr6 peptide by Z'-LYTE kinase assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621116"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL3940108"	""	"0"	"567.55"	"1"	"4.60"	"330"	"N#CCC1(n2cc(-c3c(F)cnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3cnccc3C(F)(F)F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3622827"	""	"0"	"286.38"	"0"	"2.14"	"5d"	"NCCn1c(C2CCCCC2)nc2cc(C(N)=O)ccc21"	"IC50"	"'='"	"4100.0"	"nM"	"5.39"	""	""	"UO_0000065"	"18.81"	"0.35"	"3.25"	"6.20"	"False"	"CHEMBL3625898"	"Inhibition of JAK2 (unknown origin) using 35 uM of ATP and Tyr6 peptide by Z'-LYTE kinase assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621116"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL3936966"	""	"0"	"583.55"	"1"	"3.23"	"359"	"CO[C@@H]1CN(C(=O)c2ccnc(C(F)(F)F)c2F)CC[C@@H]1N1CC(CC#N)(n2cc(-c3ncnc4[nH]ccc34)cn2)C1"	"IC50"	"'>'"	"100.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3947131"	""	"0"	"558.55"	"1"	"3.60"	"364"	"[2H]C1([2H])CN(C(=O)c2ccnc(C(F)(F)F)c2F)CC([2H])([2H])C1([2H])N1CC(CC#N)(n2cc(-c3ncnc4[nH]ccc34)cn2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3933071"	""	"0"	"447.55"	"0"	"2.33"	"367"	"CC(C)NC(=O)N1CCC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3930370"	""	"0"	"610.62"	"1"	"3.67"	"368"	"CN(C)Cc1cc(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)c(F)c(C(F)(F)F)n1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3947349"	""	"0"	"921.66"	"1"	"2.58"	"371"	"CNCc1cc(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)nc(C(F)(F)F)n1.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3927704"	""	"0"	"573.65"	"1"	"4.05"	"375"	"CN(C)Cc1cc(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)cc(C(F)F)c1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3967417"	""	"0"	"566.55"	"1"	"2.35"	"381"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc(CO)nc(C(F)(F)F)n3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL4581423"	""	"0"	"501.59"	"1"	"3.61"	"14j"	"CC(=O)c1ccc(NC(=O)N2CCN(c3ccnc(Nc4ccc(N5CCOCC5)cc4)n3)CC2)cc1"	"IC50"	"'='"	"27.0"	"nM"	"7.57"	""	""	"UO_0000065"	"15.09"	"0.28"	"3.96"	"7.35"	"False"	"CHEMBL4362531"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain (826 to 1132 resiudes) expressed in baculovirus expression system using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition measured after 1 hr in presence of ATP by mobility shift assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4359878"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2019"	"None"	""
"CHEMBL4438748"	""	"0"	"457.49"	"0"	"4.13"	"12j"	"CN(C)c1ccc(C(=O)Nc2cccc(NC(=O)COc3ccc4c(=O)ccoc4c3)c2)cc1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4379371"	"Inhibition of human recombinant JAK2 (808 to end residues) using KTFCGTPEYLAPE as substrate after 40 mins by [gamma-33ATP] by radiometric scintillation counting analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4376834"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4533614"	""	"0"	"464.36"	"0"	"4.92"	"8c"	"O=C(CCCCCCn1cc(Nc2ncc(Cl)c(Nc3ccccc3Cl)n2)cn1)NO"	"IC50"	"'='"	"46.0"	"nM"	"7.34"	""	""	"UO_0000065"	"15.80"	"0.32"	"2.42"	"6.27"	"False"	"CHEMBL4347596"	"Inhibition of recombinant human JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate measured after 60 mins by LANCE assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4346670"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4224807"	""	"0"	"284.32"	"0"	"0.91"	"6"	"CN(c1ncnc2[nH]ccc12)[C@@H]1CCN(C(=O)CC#N)C1"	"IC50"	"'='"	"240.0"	"nM"	"6.62"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"Tofacitinib"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"9.9"	"nM"	"8.00"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4227047"	""	"0"	"309.40"	"0"	"0.82"	"23"	"CCS(=O)(=O)N1CC[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"2400.0"	"nM"	"5.62"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4226435"	""	"0"	"357.44"	"0"	"1.86"	"27"	"CN(c1ncnc2[nH]ccc12)[C@@H]1CCN(S(=O)(=O)c2ccccc2)C1"	"IC50"	"'='"	"430.0"	"nM"	"6.37"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4227132"	""	"0"	"402.44"	"0"	"1.77"	"35"	"CN(c1ncnc2[nH]ccc12)[C@@H]1CCN(S(=O)(=O)c2ccc([N+](=O)[O-])cc2)C1"	"IC50"	"'='"	"89.0"	"nM"	"7.05"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4229118"	""	"0"	"407.50"	"0"	"3.01"	"40"	"CN(c1ncnc2[nH]ccc12)[C@@H]1CCN(S(=O)(=O)c2ccc3ccccc3c2)C1"	"IC50"	"'='"	"690.0"	"nM"	"6.16"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4228436"	""	"0"	"364.48"	"0"	"1.20"	"41"	"CN(c1ncnc2[nH]ccc12)[C@@H]1CCN(S(=O)(=O)N2CCCCC2)C1"	"IC50"	"'='"	"3900.0"	"nM"	"5.41"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL3975689"	""	"0"	"611.69"	"2"	"5.41"	"115"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(-c4ccc5cnccc5c4)c(F)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3895291"	""	"0"	"611.69"	"2"	"5.41"	"132"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(-c4cccc5cccnc45)c(F)c3)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3981748"	""	"0"	"535.59"	"1"	"3.59"	"140"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CC3CCC(C2)N3C(=O)c2ccc(C#N)c(F)c2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3923756"	""	"0"	"498.57"	"0"	"3.58"	"149, diastereomer 1"	"CC1CC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CCN1C(=O)c1cccc(F)c1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3892276"	""	"0"	"511.59"	"1"	"3.45"	"284"	"COc1ncccc1NC(=O)N1CCC(N2CC(CC#N)(n3ccc(-c4ncnc5[nH]ccc45)c3)C2)CC1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL2208035"	""	"0"	"458.52"	"0"	"2.94"	"10e"	"O=C1CC[C@H](C(=O)Nc2ccc(-c3ccnc(Nc4ccc(N5CCOCC5)cc4)n3)cc2)N1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL2214784"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT3 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL2208031"	""	"0"	"418.50"	"0"	"3.01"	"10a"	"C[C@H](N)C(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"1510.0"	"nM"	"5.82"	""	""	"UO_0000065"	"13.91"	"0.26"	"2.81"	"5.52"	"False"	"CHEMBL2214784"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT3 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL2207758"	""	"0"	"444.54"	"0"	"3.27"	"10f"	"O=C(Nc1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1)[C@H]1CCNC1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL2214784"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT3 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL2208028"	""	"0"	"403.49"	"0"	"3.99"	"9c"	"CC(=O)Nc1ccc(-c2nc(Nc3ccc(N4CCOCC4)cc3)ncc2C)cc1"	"IC50"	"'='"	"447.0"	"nM"	"6.35"	""	""	"UO_0000065"	"15.74"	"0.29"	"2.36"	"8.00"	"False"	"CHEMBL2214784"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT3 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL4249444"	""	"0"	"310.40"	"0"	"2.90"	"7b"	"NC(=O)c1cnc2[nH]ccc2c1NC1C2CC3CC(C2)CC1C3"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4236469"	"Inhibition of recombinant human N-terminal His-tagged JAK2 catalytic domain (826 to 1132 residues) expressed in baculovirus expression system using Biotin-Lyn-Substrate2 after 1 hr by ELISA"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229549"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL2181327"	""	"0"	"459.59"	"0"	"4.49"	"17h, 85:15 trans/cis mixture"	"CN(C)CCN(C)c1ccc2cc1COCC=CCOCc1cccc(c1)-c1ccnc(n1)N2"	"IC50"	"'='"	"77.0"	"nM"	"7.11"	""	""	"UO_0000065"	"15.48"	"0.29"	"2.62"	"11.34"	"False"	"CHEMBL2184201"	"Inhibition of recombinant JAK2 using Poly (Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176955"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL3929735"	""	"0"	"539.52"	"1"	"3.37"	"17"	"Cc1nc(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)c(C(F)(F)F)o1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3968632"	""	"0"	"514.57"	"1"	"3.20"	"39"	"COc1cccc(F)c1C(=O)N1CCC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3977847"	""	"0"	"514.57"	"1"	"3.20"	"40"	"COc1cc(F)ccc1C(=O)N1CCC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3982495"	""	"0"	"569.98"	"1"	"4.12"	"53"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc(Cl)cc(C(F)(F)F)n3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3981886"	""	"0"	"521.59"	"1"	"2.93"	"55"	"COc1ccc(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)cc1C#N"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3925310"	""	"0"	"484.54"	"0"	"3.19"	"67"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccccc3F)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3915630"	""	"0"	"536.52"	"1"	"2.86"	"85"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccnc(C(F)(F)F)n3)CC2)C1"	"IC50"	"'>'"	"100.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3927670"	""	"0"	"590.64"	"2"	"5.28"	"94"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc4ccc(C(F)(F)F)cc4s3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3913887"	""	"0"	"522.66"	"1"	"3.90"	"113"	"Cc1cc(C)c(CC(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)c(C)c1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3935288"	""	"0"	"611.69"	"2"	"5.41"	"129"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(-c4cccc5ncccc45)c(F)c3)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3907920"	""	"0"	"561.57"	"1"	"4.00"	"143"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CC3CCC(C2)N3C(=O)c2ccc(C(F)(F)F)nc2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3896874"	""	"0"	"637.67"	"2"	"2.94"	"384"	"COCCN(C)Cc1cc(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)nc(C(F)(F)F)n1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3911726"	""	"0"	"567.55"	"1"	"4.60"	"154"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3ccc(F)cc3C(F)(F)F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3906336"	""	"0"	"517.54"	"1"	"3.72"	"156"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3c(F)cccc3F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3981303"	""	"0"	"517.54"	"1"	"3.72"	"171"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3ccc(F)cc3F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3927679"	""	"0"	"516.01"	"1"	"4.10"	"184"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3ccc(Cl)cc3)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3929672"	""	"0"	"500.54"	"1"	"2.98"	"202"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3ncccc3F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3896630"	""	"0"	"557.59"	"1"	"3.37"	"208"	"COC(=O)c1ccc(NC(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)c(F)c1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3920589"	""	"0"	"538.55"	"1"	"4.57"	"213"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(Cc3c(F)cccc3C(F)(F)F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3914532"	""	"0"	"521.46"	"1"	"4.72"	"219"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(Cc3cccc(Cl)c3Cl)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3927209"	""	"0"	"477.58"	"0"	"3.28"	"222"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(Cc3ccccc3C#N)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3928974"	""	"0"	"477.58"	"0"	"3.28"	"223"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(Cc3cccc(C#N)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3938515"	""	"0"	"505.00"	"1"	"4.20"	"227"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(Cc3c(F)cccc3Cl)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3931280"	""	"0"	"506.60"	"1"	"1.33"	"246"	"Cn1nccc1S(=O)(=O)N1CCC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3943023"	""	"0"	"472.58"	"0"	"3.11"	"15"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccsc3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3936441"	""	"0"	"550.55"	"1"	"3.95"	"21"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cccc(OC(F)(F)F)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3945016"	""	"0"	"518.98"	"1"	"3.84"	"34"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3958002"	""	"0"	"552.62"	"1"	"3.13"	"51"	"CN(C)c1ccc(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)c(F)c1C#N"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3933201"	""	"0"	"507.02"	"1"	"3.77"	"76"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3sccc3Cl)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3953337"	""	"0"	"517.60"	"1"	"3.60"	"88"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cnc4ccccc4c3)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3950173"	""	"0"	"548.70"	"1"	"4.71"	"104"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)C3CCC(c4ccccc4)CC3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3964472"	""	"0"	"611.69"	"2"	"5.41"	"133"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(-c4ccc5ccncc5c4)c(F)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL1650730"	""	"0"	"377.82"	"0"	"2.76"	"9k"	"C[C@H](Nc1ncc(Cl)c(Nc2cc(N(C)C)[nH]n2)n1)c1ncc(F)cn1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	""	"UO_0000065"	"21.30"	"0.42"	"5.29"	"7.48"	"False"	"CHEMBL1656588"	"Inhibition of JAK2 using Km ATP concentration"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1650726"	""	"0"	"349.76"	"0"	"2.97"	"9g"	"Cc1cc(Nc2nc(O[C@@H](C)c3ncc(F)cn3)ncc2Cl)n[nH]1"	"IC50"	"'<'"	"3.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1656588"	"Inhibition of JAK2 using Km ATP concentration"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1650724"	""	"0"	"374.81"	"0"	"3.58"	"9b"	"C[C@H](Nc1ncc(Cl)c(Nc2cc(C3CC3)[nH]n2)n1)c1ncc(F)cn1"	"IC50"	"'<'"	"3.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1656588"	"Inhibition of JAK2 using Km ATP concentration"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1650737"	""	"0"	"449.88"	"0"	"2.54"	"16f"	"COc1cc(Nc2nc(N[C@@H](C)c3ncc(F)cn3)nc(N3CCOCC3)c2Cl)n[nH]1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	""	"UO_0000065"	"18.67"	"0.37"	"5.86"	"6.67"	"False"	"CHEMBL1656588"	"Inhibition of JAK2 using Km ATP concentration"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1650726"	""	"0"	"349.76"	"0"	"2.97"	"9g"	"Cc1cc(Nc2nc(O[C@@H](C)c3ncc(F)cn3)ncc2Cl)n[nH]1"	"IC50"	"'='"	"21.0"	"nM"	"7.68"	""	""	"UO_0000065"	"21.95"	"0.44"	"4.71"	"7.56"	"False"	"CHEMBL1656589"	"Inhibition of JAK2 using 5 mM of ATP"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1650731"	""	"0"	"361.36"	"0"	"2.25"	"9l"	"C[C@H](Nc1ncc(F)c(Nc2cc(N(C)C)[nH]n2)n1)c1ncc(F)cn1"	"IC50"	"'='"	"815.0"	"nM"	"6.09"	""	""	"UO_0000065"	"16.85"	"0.32"	"3.84"	"5.66"	"False"	"CHEMBL1656589"	"Inhibition of JAK2 using 5 mM of ATP"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1650736"	""	"0"	"433.42"	"0"	"2.03"	"16e"	"COc1cc(Nc2nc(N[C@@H](C)c3ncc(F)cn3)nc(N3CCOCC3)c2F)n[nH]1"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	""	"UO_0000065"	"18.68"	"0.36"	"6.07"	"6.43"	"False"	"CHEMBL1656589"	"Inhibition of JAK2 using 5 mM of ATP"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL2062790"	""	"0"	"211.23"	"0"	"1.37"	"15"	"Nc1nc2c(-c3ccncc3)cccn2n1"	"IC50"	"'='"	"1406.0"	"nM"	"5.85"	""	""	"UO_0000065"	"27.70"	"0.50"	"4.48"	"8.47"	"False"	"CHEMBL2067611"	"Inhibition of human JAK2 expressed in baculovirus using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate preincubated for 1 hr measured after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL4797744"	""	"0"	"460.97"	"1"	"5.36"	"10h"	"O=C(Nc1c[nH]nc1-c1nc(-c2ccc(CN3CCCCC3)cc2)c[nH]1)c1ccc(Cl)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4711870"	"Inhibition of JAK2 (unknown origin) incubated for 40 mins in presence of ATP by Kinase-glo luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706620"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2021"	"None"	"TIME = 0.6667 hr"
"CHEMBL495727"	"AT-9283"	"2"	"381.44"	"0"	"2.07"	"AT9283"	"O=C(Nc1c[nH]nc1-c1nc2ccc(CN3CCOCC3)cc2[nH]1)NC1CC1"	"IC50"	"'='"	"2.2"	"nM"	"8.66"	""	""	""	"22.70"	"0.42"	"6.59"	"7.80"	"False"	"CHEMBL4711870"	"Inhibition of JAK2 (unknown origin) incubated for 40 mins in presence of ATP by Kinase-glo luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706620"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2021"	"None"	"TIME = 0.6667 hr"
"CHEMBL3689516"	""	"0"	"332.31"	"0"	"1.30"	"BDBM109866"	"N#CCC(=O)N1CC(F)(F)C12CCN(c1ncnc3[nH]ccc13)C2"	"IC50"	"'='"	"1.7"	"nM"	"8.77"	""	"230596"	"UO_0000065"	"26.39"	"0.50"	"7.47"	"9.86"	"False"	"CHEMBL3705639"	"Inhibition Assay: In the kinase reactions, fused proteins (6His tag-fused hJAK2 kinase domain (aa808-end)) which were coexpressed in Sf21 cells and purified by Ni2+/NTA agarose were used."	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638515"	"37"	"BindingDB Database"	""	"2013"	"CHEMBL4106362"	""
"CHEMBL4763560"	""	"0"	"448.57"	"0"	"4.28"	"13y"	"COC(=O)CCCN1CCc2cc(Nc3ncc(C)c(-c4cnn(C(C)C)c4)n3)ccc2C1"	"IC50"	"'='"	"1040.0"	"nM"	"5.98"	""	""	""	"13.34"	"0.25"	"1.70"	"7.02"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL4760274"	""	"0"	"432.53"	"0"	"3.97"	"13ae"	"Cc1cnc(Nc2ccc3c(c2)CCN(C/C=C/C(=O)O)C3)nc1-c1cnn(C(C)C)c1"	"IC50"	"'='"	"334.0"	"nM"	"6.48"	""	""	""	"14.97"	"0.28"	"2.51"	"6.73"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL2207764"	""	"0"	"492.37"	"1"	"6.40"	"5"	"CC(=O)Nc1ccc(-c2ccnc(Nc3cccc(NC(=O)c4c(Cl)cccc4Cl)c3)n2)cc1"	"IC50"	"'='"	"505.0"	"nM"	"6.30"	""	""	"UO_0000065"	"12.79"	"0.25"	"-0.10"	"6.56"	"False"	"CHEMBL2214784"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT3 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL3651854"	""	"0"	"591.78"	"2"	"6.24"	"20b"	"Cc1cc(Nc2nc(Nc3ccccc3S(=O)(=O)C(C)C)c3c(C)[nH]nc3n2)c(OC(C)C)cc1C1CCN(C)CC1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	""	""	""	""	""	"False"	"CHEMBL4716842"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715698"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2016"	"None"	""
"CHEMBL1774056"	""	"0"	"355.35"	"0"	"3.57"	"1d"	"Cc1cc(Nc2nc(N[C@@H](C)c3ccc(F)cn3)c(C#N)cc2F)n[nH]1"	"IC50"	"'<'"	"3.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1776838"	"Inhibition of JAK2 after 60 min"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1772962"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL2208025"	""	"0"	"389.46"	"0"	"3.68"	"64b"	"CC(=O)Nc1ccc(-c2ccnc(Nc3cccc(N4CCOCC4)c3)n2)cc1"	"IC50"	"'='"	"19.6"	"nM"	"7.71"	""	""	"UO_0000065"	"19.79"	"0.36"	"4.03"	"9.71"	"False"	"CHEMBL4268221"	"Inhibition of human JAK2 using poly(Glu:Tyr)(4:1) as substrate preincubated for 20 mins followed by [gamma33P]ATP addition measured after 120 mins by ion exchange filter paper method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4265943"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2018"	"None"	""
"CHEMBL4292020"	""	"0"	"420.46"	"0"	"4.63"	"15"	"CN1CCN(c2ccc(-c3c(-c4cc(F)c(O)c(F)c4)cnc4[nH]ccc34)cc2)CC1"	"IC50"	"'<'"	"1000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4266996"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4265896"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2018"	"None"	""
"CHEMBL3764167"	""	"0"	"286.34"	"0"	"1.68"	"10"	"CCC(C)n1cc(-c2ccn(C)n2)c2[nH]nc(N)c2c1=O"	"IC50"	"'='"	"180.0"	"nM"	"6.75"	""	""	"UO_0000065"	"23.55"	"0.44"	"5.06"	"7.14"	"False"	"CHEMBL3766653"	"Inhibition of JAK2 (unknown origin) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent substrate phosphorylation after 45 mins by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3763089"	"1"	"Scientific Literature"	"J. Med. Chem."	"2016"	"None"	""
"CHEMBL4282471"	""	"0"	"576.53"	"0"	"3.85"	"45c"	"CC(=O)Nc1ccc(-c2ccnc(Nc3ccc(NC(=O)CCCCC(=O)NO)cc3)n2)cc1.O=C(O)C(F)(F)F"	"IC50"	"'='"	"58.3"	"nM"	"7.23"	""	""	"UO_0000065"	"15.64"	"0.29"	"3.38"	"4.98"	"False"	"CHEMBL4268221"	"Inhibition of human JAK2 using poly(Glu:Tyr)(4:1) as substrate preincubated for 20 mins followed by [gamma33P]ATP addition measured after 120 mins by ion exchange filter paper method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4265943"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2018"	"None"	""
"CHEMBL4434658"	""	"0"	"502.58"	"1"	"2.51"	"14l"	"NC(=O)c1ccc(NC(=O)N2CCN(c3ccnc(Nc4ccc(N5CCOCC5)cc4)n3)CC2)cc1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	""	"UO_0000065"	"15.84"	"0.29"	"5.45"	"6.17"	"False"	"CHEMBL4362531"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain (826 to 1132 resiudes) expressed in baculovirus expression system using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition measured after 1 hr in presence of ATP by mobility shift assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4359878"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2019"	"None"	""
"CHEMBL2178247"	""	"0"	"381.83"	"0"	"3.17"	"7b"	"CNc1ccn2ncc(C(=O)Nc3cc(C)nn3-c3cccc(Cl)c3)c2n1"	"IC50"	"'='"	"259.0"	"nM"	"6.59"	""	""	"UO_0000065"	"17.25"	"0.33"	"3.42"	"7.39"	"False"	"CHEMBL2186598"	"Inhibition of JAK2 V617F mutant in human SET2 cells assessed as reduction in STAT5 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176876"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL4758753"	""	"0"	"388.44"	"0"	"2.41"	"18, trans isomer"	"CO[C@H]1C[C@](CC#N)(n2cc(-c3nc(-c4cnn(C)c4)cn4nccc34)cn2)C1"	"IC50"	"'='"	"1100.0"	"nM"	"5.96"	""	""	""	""	""	""	""	"False"	"CHEMBL4675820"	"Inhibition of JAK2 homodimer signaling pathway in human whole blood spiked with CD34 +ve cells assessed as reduction in EPO induced STAT5 phosphorylation preincubated for 45 mins followed by EPO addition and measured measured after 15 mins by immunostaining based FACS assay"	"A"	"BAO_0000221"	"tissue-based format"	"Homo sapiens"	"None"	"Blood"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4673239"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 1.0 hr"
"CHEMBL2178253"	""	"0"	"338.76"	"0"	"3.03"	"13b"	"O=C(Nc1c[nH]nc1-c1cccc(Cl)c1)c1cnn2cccnc12"	"IC50"	"'='"	"143.0"	"nM"	"6.84"	""	""	"UO_0000065"	"20.21"	"0.39"	"3.81"	"7.78"	"False"	"CHEMBL2186598"	"Inhibition of JAK2 V617F mutant in human SET2 cells assessed as reduction in STAT5 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176876"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2063926"	""	"0"	"505.70"	"1"	"3.58"	"17"	"CSc1ccccc1Nc1nc(N2CCN(C3CCNCC3)CC2)nc2c(NCC3CC3)ncnc12"	"IC50"	"'<'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2065150"	"Inhibition of JAK2 by FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062359"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL4239990"	""	"0"	"441.54"	"0"	"0.72"	"9f"	"COCCn1cc(-c2nn(CC3CCCN(C(=O)CN(C)C)C3)c3ncnc(N)c23)cn1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4238190"	""	"0"	"409.45"	"0"	"1.00"	"12d"	"COCCn1cc(-c2nn(C3CCCN(C(=O)CC#N)C3)c3ncnc(N)c23)cn1"	"IC50"	"'='"	"696.8"	"nM"	"6.16"	""	""	"UO_0000065"	"15.04"	"0.28"	"5.16"	"4.37"	"False"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4225902"	""	"0"	"371.47"	"0"	"2.17"	"36"	"Cc1cccc(S(=O)(=O)N2CC[C@@H](N(C)c3ncnc4[nH]ccc34)C2)c1"	"IC50"	"'='"	"730.0"	"nM"	"6.14"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL1650735"	""	"0"	"415.43"	"0"	"1.89"	"16d"	"COc1cc(Nc2cc(N3CCOCC3)nc(N[C@@H](C)c3ncc(F)cn3)n2)n[nH]1"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	""	"UO_0000065"	"19.26"	"0.36"	"6.11"	"6.35"	"False"	"CHEMBL1656588"	"Inhibition of JAK2 using Km ATP concentration"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL4225197"	""	"0"	"273.38"	"0"	"2.27"	"16"	"CCCCN1CC[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"27000.0"	"nM"	"4.57"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4225674"	""	"0"	"361.43"	"0"	"0.59"	"26"	"CN(c1ncnc2[nH]ccc12)[C@@H]1CCN(S(=O)(=O)c2cn(C)cn2)C1"	"IC50"	"'='"	"19000.0"	"nM"	"4.72"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4225595"	""	"0"	"368.42"	"0"	"1.70"	"11"	"N#Cc1cccc(S(=O)(=O)N2CC[C@@H](Nc3ncnc4[nH]ccc34)C2)c1"	"IC50"	"'='"	"1900.0"	"nM"	"5.72"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4225201"	""	"0"	"270.34"	"0"	"1.38"	"15"	"CN(c1ncnc2[nH]ccc12)[C@@H]1CCN(CCC#N)C1"	"IC50"	"'='"	"1900.0"	"nM"	"5.72"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4225947"	""	"0"	"323.42"	"0"	"1.21"	"24"	"CC(C)S(=O)(=O)N1CC[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"4800.0"	"nM"	"5.32"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL1299997"	""	"0"	"206.25"	"0"	"2.39"	"SID17413703"	"C/C(=C\c1ccc(N(C)C)cc1)[N+](=O)[O-]"	"IC50"	"'='"	"3498.0"	"nM"	"5.46"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1478382"	""	"0"	"262.70"	"0"	"2.68"	"SID26660752"	"Cn1c(Cl)cnc1/C=C/C(=O)c1ccccc1O"	"IC50"	"'='"	"6561.0"	"nM"	"5.18"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1518085"	""	"0"	"326.40"	"0"	"4.35"	"SID26665472"	"c1ccc(CCNc2nc(-c3ccccn3)nc3ccccc23)cc1"	"IC50"	"'='"	"3020.0"	"nM"	"5.52"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL560919"	""	"0"	"282.30"	"0"	"3.10"	"SID24786554"	"Cc1c(Cc2ccccc2)c(=O)oc2c(O)c(O)ccc12"	"IC50"	"'='"	"8616.0"	"nM"	"5.07"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1525669"	""	"0"	"291.78"	"0"	"3.35"	"SID24832657"	"CC(C)(C)c1cc(NC(=O)CCl)n(-c2ccccc2)n1"	"IC50"	"'='"	"3759.0"	"nM"	"5.42"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1450393"	""	"0"	"312.38"	"0"	"1.57"	"SID26659002"	"CCCC(=O)N(C1CC(C)C(C#N)(C#N)C1(C#N)C#N)N(C)C"	"IC50"	"'='"	"4768.0"	"nM"	"5.32"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1588408"	""	"0"	"264.28"	"0"	"3.76"	"SID844120"	"O=C(Oc1cccc2c(O)cccc12)c1ccccc1"	"IC50"	"'='"	"6512.0"	"nM"	"5.19"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL3211859"	""	"0"	"479.49"	"0"	"2.59"	"SID17386562"	"COc1cccc(/C=N/NC(=O)c2[nH]c(C)c(C(=O)N/N=C/c3cccc(OC)c3O)c2C)c1O"	"IC50"	"'='"	"6662.0"	"nM"	"5.18"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL254255"	""	"0"	"358.38"	"0"	"2.06"	"SID4260677"	"COc1ccc(-n2nnnc2SCC(=O)c2ccc(O)c(O)c2)cc1"	"IC50"	"'='"	"3336.0"	"nM"	"5.48"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1511663"	""	"0"	"401.48"	"0"	"3.56"	"SID22411280"	"O=C(/C=C/c1ccc(O)c(O)c1)c1ccc(S(=O)(=O)N2CCCCCC2)cc1"	"IC50"	"'='"	"7505.0"	"nM"	"5.12"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1466500"	""	"0"	"279.73"	"0"	"2.33"	"SID26666159"	"CCOc1ccc(Nc2nc(N)nc(CCl)n2)cc1"	"IC50"	"'='"	"1924.0"	"nM"	"5.72"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1597766"	""	"0"	"250.37"	"0"	"2.47"	"SID4247660"	"C#CCSc1nsc(SCC#C)c1C#N"	"IC50"	"'='"	"2833.0"	"nM"	"5.55"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1561655"	""	"0"	"358.47"	"0"	"3.70"	"SID14743139"	"COc1ccc(C2=Nn3c(nnc3C3CCCCC3)SC2)cc1OC"	"IC50"	"'='"	"7519.0"	"nM"	"5.12"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL4471707"	""	"0"	"429.49"	"0"	"2.37"	"14f"	"Cc1cnc(Nc2cc(NC3CCN(c4ccc(C#N)cn4)CC3)c(C(N)=O)cn2)cn1"	"IC50"	"'='"	"5.3"	"nM"	"8.28"	""	""	"UO_0000065"	"19.27"	"0.35"	"5.91"	"5.68"	"False"	"CHEMBL4429528"	"Inhibition of human JAK2 assessed as reduction in phosphorylation of Biotin-Lyn-Substrate-2 after 1 hr in presence of ATP by ELISA"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4428070"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2016"	"None"	""
"CHEMBL1447125"	""	"0"	"263.73"	"0"	"2.55"	"SID26671644"	"Cc1cccc(Nc2nc(N)nc(CCl)n2)c1C"	"IC50"	"'='"	"2072.0"	"nM"	"5.68"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1318943"	""	"0"	"293.37"	"0"	"2.71"	"SID856169"	"[O-][N+]1=c2ccc(Nc3ccccc3)cc2=NC12CCCCC2"	"IC50"	"'='"	"5197.0"	"nM"	"5.28"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1575649"	""	"0"	"344.42"	"0"	"3.33"	"SID24781164"	"O=C1/C(=C/c2ccc(O)c(O)c2)SC(=S)N1Nc1ccccc1"	"IC50"	"'='"	"10990.0"	"nM"	"4.96"	""	"Not Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1498517"	""	"0"	"246.74"	"0"	"1.88"	"SID22409904"	"CC1CCCC(NC(=O)NC(=O)CCl)C1C"	"IC50"	"'='"	"10610.0"	"nM"	"4.97"	""	"Not Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL3191989"	""	"0"	"335.64"	"0"	"3.57"	"SID24825651"	"O=C(CCl)/N=c1\sccn1Cc1ccc(Cl)cc1Cl"	"IC50"	"'='"	"653.0"	"nM"	"6.18"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1332689"	""	"0"	"519.58"	"1"	"4.06"	"SID26670262"	"CCN(CC)S(=O)(=O)c1cccc(N2C(=O)/C(=C\Nc3ccccc3C(=O)O)c3ccccc3C2=O)c1"	"IC50"	"'>'"	"40000.0"	"nM"	""	""	"Not Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL3196363"	""	"0"	"385.47"	"0"	"3.82"	"SID26658457"	"Oc1ccc(/C=N/N2CCN(C3c4ccccc4-c4ccccc43)CC2)cc1O"	"IC50"	"'='"	"5677.0"	"nM"	"5.25"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1481030"	""	"0"	"311.78"	"0"	"3.66"	"SID26666804"	"Nc1nc(CCl)nc(N(c2ccccc2)c2ccccc2)n1"	"IC50"	"'='"	"1263.0"	"nM"	"5.90"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1599994"	""	"0"	"357.35"	"0"	"3.75"	"SID24822486"	"O=C(Nc1cccc(NC(=O)c2cccs2)c1)c1ccc([N+](=O)[O-])o1"	"IC50"	"'='"	"3699.0"	"nM"	"5.43"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL3193428"	""	"0"	"344.37"	"0"	"3.80"	"SID22406436"	"O=C(/C(=N/N=C/c1ccc(O)c(O)c1)c1ccccc1)c1ccccc1"	"IC50"	"'='"	"1666.0"	"nM"	"5.78"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1311354"	""	"0"	"289.67"	"0"	"3.49"	"SID26726005"	"O=c1oc2ccc(Cl)cc2nc1/C=C(\O)c1ccco1"	"IC50"	"'='"	"8349.0"	"nM"	"5.08"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL4637587"	""	"0"	"418.46"	"0"	"1.75"	"21"	"N#C[C@]1(C2CC2)C(=O)N2C[C@H]1COCC(=O)NCc1cccc(n1)Nc1cc2ccn1"	"IC50"	"'='"	"1000.0"	"nM"	"6.00"	""	""	"UO_0000065"	"14.34"	"0.26"	"4.25"	"4.99"	"False"	"CHEMBL4627620"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4627255"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL4638122"	""	"0"	"383.81"	"0"	"4.31"	"16l"	"CC(Oc1cc(-c2ccc3ncnn3c2)cnc1N)c1cc(F)ccc1Cl"	"IC50"	"'='"	"71.0"	"nM"	"7.15"	""	""	"UO_0000065"	"18.63"	"0.36"	"2.84"	"9.13"	"False"	"CHEMBL4628503"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4627317"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL3645074"	""	"0"	"417.49"	"0"	"4.75"	"BDBM99842"	"COc1ccc(-c2cccn3nc(Nc4ccc(C5CCNCC5)cc4)nc23)c(F)c1"	"IC50"	"'='"	"9.04"	"nM"	"8.04"	""	"216515"	"UO_0000065"	"19.27"	"0.35"	"3.29"	"12.67"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL2062795"	""	"0"	"364.43"	"0"	"3.54"	"20"	"CS(=O)(=O)c1cccc(-c2cccn3nc(Nc4ccccc4)nc23)c1"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	""	"UO_0000065"	"22.22"	"0.43"	"4.56"	"10.60"	"False"	"CHEMBL2067611"	"Inhibition of human JAK2 expressed in baculovirus using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate preincubated for 1 hr measured after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2062795"	""	"0"	"364.43"	"0"	"3.54"	"20"	"CS(=O)(=O)c1cccc(-c2cccn3nc(Nc4ccccc4)nc23)c1"	"IC50"	"'='"	"1071.0"	"nM"	"5.97"	""	""	"UO_0000065"	"16.38"	"0.31"	"2.43"	"7.82"	"False"	"CHEMBL2067179"	"Inhibition of JAK2 in human TF-1 cells using GM-CSF pretreated for 1 hr prior to GM-CSF addition measured after 5 hrs by FRET based GeneBLAzer assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"CHEMBL3307972"	""
"CHEMBL2062804"	""	"0"	"462.58"	"0"	"3.30"	"29, CEP-33779"	"CN1CCN(c2cccc(Nc3nc4c(-c5ccc(S(C)(=O)=O)cc5)cccn4n3)c2)CC1"	"IC50"	"'='"	"1.8"	"nM"	"8.74"	""	""	"UO_0000065"	"18.90"	"0.36"	"5.44"	"10.56"	"False"	"CHEMBL2067611"	"Inhibition of human JAK2 expressed in baculovirus using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate preincubated for 1 hr measured after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2062798"	""	"0"	"394.46"	"0"	"3.55"	"23"	"COc1cccc(Nc2nc3c(-c4ccc(S(C)(=O)=O)cc4)cccn3n2)c1"	"IC50"	"'='"	"176.0"	"nM"	"6.75"	""	""	"UO_0000065"	"17.12"	"0.33"	"3.20"	"7.89"	"False"	"CHEMBL2067179"	"Inhibition of JAK2 in human TF-1 cells using GM-CSF pretreated for 1 hr prior to GM-CSF addition measured after 5 hrs by FRET based GeneBLAzer assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"CHEMBL3307972"	""
"CHEMBL2062799"	""	"0"	"394.46"	"0"	"3.55"	"24"	"COc1ccc(Nc2nc3c(-c4ccc(S(C)(=O)=O)cc4)cccn3n2)cc1"	"IC50"	"'='"	"209.0"	"nM"	"6.68"	""	""	"UO_0000065"	"16.93"	"0.33"	"3.13"	"7.80"	"False"	"CHEMBL2067179"	"Inhibition of JAK2 in human TF-1 cells using GM-CSF pretreated for 1 hr prior to GM-CSF addition measured after 5 hrs by FRET based GeneBLAzer assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"CHEMBL3307972"	""
"CHEMBL2062805"	""	"0"	"462.58"	"0"	"3.30"	"30"	"CN1CCN(c2ccc(Nc3nc4c(-c5ccc(S(C)(=O)=O)cc5)cccn4n3)cc2)CC1"	"IC50"	"'='"	"64.0"	"nM"	"7.19"	""	""	"UO_0000065"	"15.55"	"0.30"	"3.89"	"8.68"	"False"	"CHEMBL2067179"	"Inhibition of JAK2 in human TF-1 cells using GM-CSF pretreated for 1 hr prior to GM-CSF addition measured after 5 hrs by FRET based GeneBLAzer assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"CHEMBL3307972"	""
"CHEMBL4297507"	"DELGOCITINIB"	"3"	"310.36"	"0"	"1.30"	"ent-60, JTE-052"	"C[C@H]1CN(C(=O)CC#N)[C@]12CCN(c1ncnc3[nH]ccc13)C2"	"IC50"	"'='"	"300.0"	"nM"	"6.52"	""	""	"UO_0000065"	"21.02"	"0.39"	"5.22"	"7.34"	"False"	"CHEMBL4630022"	"Inhibition of JAK2 in human PBMC assessed as reduction in GM-CSF-induced Stat5 phosphorylation in CD3- CD4+ cells preincubated for 30 mins followed by GM-CSF stimulation and measured after 15 mins"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"PBMC"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4627398"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3308021"	""
"CHEMBL1549175"	""	"0"	"461.52"	"0"	"3.99"	"SID864316"	"CC(C)(C)OC(=O)N[C@@H](Cc1ccccc1)c1nnc(S(=O)(=O)Cc2cccc(F)c2)o1"	"IC50"	"'='"	"3741.0"	"nM"	"5.43"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1424355"	""	"0"	"280.33"	"0"	"3.77"	"SID24801814"	"COc1ccc(-c2cc(-c3cc(C)ccc3O)[nH]n2)cc1"	"IC50"	"'='"	"8759.0"	"nM"	"5.06"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1304902"	""	"0"	"442.97"	"0"	"4.43"	"SID17509716"	"COc1cccc(N(C(=O)CCl)C(C(=O)NCCc2ccccc2)c2cccs2)c1"	"IC50"	"'='"	"1342.0"	"nM"	"5.87"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1364913"	""	"0"	"249.71"	"0"	"2.24"	"SID26662766"	"Cc1ccc(Nc2nc(N)nc(CCl)n2)cc1"	"IC50"	"'='"	"1421.0"	"nM"	"5.85"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1574219"	""	"0"	"323.37"	"0"	"2.60"	"SID17387987"	"CCCn1c(CC)nc([N+](=O)[O-])c1S(=O)(=O)c1ccccc1"	"IC50"	"'='"	"5896.0"	"nM"	"5.23"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1980982"	""	"0"	"280.78"	"0"	"2.57"	"SID24825554"	"Cc1ccc(Cn2ccs/c2=N\C(=O)CCl)cc1"	"IC50"	"'='"	"7757.0"	"nM"	"5.11"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL2062793"	""	"0"	"278.24"	"0"	"3.00"	"18"	"Nc1nc2c(-c3ccc(C(F)(F)F)cc3)cccn2n1"	"IC50"	"'='"	"193.0"	"nM"	"6.71"	""	""	"UO_0000065"	"24.13"	"0.46"	"3.71"	"11.95"	"False"	"CHEMBL2067611"	"Inhibition of human JAK2 expressed in baculovirus using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate preincubated for 1 hr measured after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2062803"	""	"0"	"449.54"	"0"	"3.38"	"28"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4ccc(N5CCOCC5)cc4)nc23)cc1"	"IC50"	"'='"	"61.0"	"nM"	"7.21"	""	""	"UO_0000065"	"16.05"	"0.31"	"3.83"	"8.12"	"False"	"CHEMBL2067179"	"Inhibition of JAK2 in human TF-1 cells using GM-CSF pretreated for 1 hr prior to GM-CSF addition measured after 5 hrs by FRET based GeneBLAzer assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"CHEMBL3307972"	""
"CHEMBL2443026"	""	"0"	"578.67"	"1"	"4.49"	"38"	"CN(C)c1ccc(Oc2cc(O)cc(O)c2-c2cc(C(=O)NC3CCN(C4CCC5(CC4)OCCO5)CC3)no2)cc1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2443999"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2439976"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2013"	"None"	""
"CHEMBL3114763"	""	"0"	"467.50"	"0"	"4.18"	"11g"	"O=C1NC(=O)C(c2c[nH]c3ccccc23)=C1Nc1cccc(C2CCN(c3ccnc(F)c3)C2)c1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3118993"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112442"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3116056"	""	"0"	"384.44"	"0"	"3.58"	"23b"	"Cc1csc2c(Nc3cn(C)cn3)nc(N[C@@H](C)c3ncc(F)cn3)nc12"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	""	"UO_0000065"	"21.84"	"0.42"	"4.82"	"8.99"	"False"	"CHEMBL3118240"	"Inhibition of Jak2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112447"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL3116054"	""	"0"	"368.38"	"0"	"1.94"	"19e"	"C[C@H](Nc1nc(Nc2cn(C)cn2)c2cnn(C)c2n1)c1ncc(F)cn1"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	""	"UO_0000065"	"21.24"	"0.40"	"5.88"	"7.03"	"False"	"CHEMBL3118240"	"Inhibition of Jak2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112447"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL3116052"	""	"0"	"393.43"	"0"	"3.35"	"19c"	"C[C@H](Nc1nc(Nc2cn(C)cn2)c2ccn(C3CC3)c2n1)c1ncc(F)cn1"	"IC50"	"'='"	"27.0"	"nM"	"7.57"	""	""	"UO_0000065"	"19.24"	"0.36"	"4.22"	"7.69"	"False"	"CHEMBL3118240"	"Inhibition of Jak2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112447"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL2414553"	""	"0"	"331.38"	"0"	"3.85"	"23"	"COc1ccc(-c2cccc3nc(Nc4ccnc(C)c4)nn23)cc1"	"IC50"	"'='"	"174.0"	"nM"	"6.76"	""	""	"UO_0000065"	"20.40"	"0.37"	"2.91"	"10.51"	"False"	"CHEMBL2415128"	"Inhibition of JAK2 in human SET2 cells assessed as reduction of phosphorylated STAT5 level"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2412966"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2414546"	""	"0"	"414.51"	"0"	"3.90"	"11"	"COc1cccc(-c2cccc3nc(Nc4ccc(N5CCN(C)CC5)cc4)nn23)c1"	"IC50"	"'='"	"53.6"	"nM"	"7.27"	""	""	"UO_0000065"	"17.54"	"0.32"	"3.37"	"12.55"	"False"	"CHEMBL2415128"	"Inhibition of JAK2 in human SET2 cells assessed as reduction of phosphorylated STAT5 level"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2412966"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL3116050"	""	"0"	"353.37"	"0"	"2.54"	"19a"	"C[C@H](Nc1nc(Nc2cn(C)cn2)c2cc[nH]c2n1)c1ncc(F)cn1"	"IC50"	"'='"	"30.0"	"nM"	"7.52"	""	""	"UO_0000065"	"21.29"	"0.40"	"4.98"	"6.89"	"False"	"CHEMBL3116827"	"Inhibition of Jak2 V617F mutant in human SET2 cells assessed as inhibition of STAT5 phosphorylation after 1 hr by Western blotting analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112447"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL1650733"	""	"0"	"417.42"	"0"	"2.33"	"16b"	"Cc1cc(Nc2nc(N[C@@H](C)c3ncc(F)cn3)nc(N3CCOCC3)c2F)n[nH]1"	"IC50"	"'<'"	"3.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1656589"	"Inhibition of JAK2 using 5 mM of ATP"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1946153"	""	"0"	"441.58"	"1"	"5.26"	"28b"	"CN1C/C=C/CCOc2cccc(c2)-c2cc(N3CCCC3)nc(n2)Nc2cccc(c2)C1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1945046"	""	"0"	"416.53"	"0"	"4.67"	"26p"	"COCCN1C/C=C/CCOc2cccc(c2)-c2ccnc(n2)Nc2cccc(c2)C1"	"IC50"	"'='"	"1600.0"	"nM"	"5.80"	""	""	"UO_0000065"	"13.91"	"0.26"	"1.13"	"9.74"	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1945565"	""	"0"	"446.55"	"0"	"4.68"	"27d"	"COCCOc1ccc2cc1CN(C)C/C=C/CCOc1cccc(c1)-c1ccnc(n1)N2"	"IC50"	"'='"	"62.0"	"nM"	"7.21"	""	""	"UO_0000065"	"16.14"	"0.30"	"2.53"	"10.49"	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL495727"	"AT-9283"	"2"	"381.44"	"0"	"2.07"	"16, AT9283"	"O=C(Nc1c[nH]nc1-c1nc2ccc(CN3CCOCC3)cc2[nH]1)NC1CC1"	"IC50"	"'='"	"1.2"	"nM"	"8.92"	""	""	"UO_0000065"	"23.39"	"0.44"	"6.85"	"8.04"	"False"	"CHEMBL1009897"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139387"	"1"	"Scientific Literature"	"J. Med. Chem."	"2009"	"None"	""
"CHEMBL480411"	""	"0"	"344.44"	"0"	"2.89"	"13"	"CC(C)(C)NS(=O)(=O)c1ccc(-c2ccc3[nH]nc(N)c3c2)cc1"	"IC50"	"'='"	"78.0"	"nM"	"7.11"	""	""	"UO_0000065"	"20.64"	"0.40"	"4.22"	"7.05"	"False"	"CHEMBL1011746"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139271"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL447670"	""	"0"	"308.39"	"0"	"3.34"	"14"	"CC(C)(C)NC(=O)c1ccc(-c2ccc3[nH]nc(N)c3c2)cc1"	"IC50"	"'='"	"1950.0"	"nM"	"5.71"	""	""	"UO_0000065"	"18.52"	"0.34"	"2.37"	"6.81"	"False"	"CHEMBL1011746"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139271"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL482189"	""	"0"	"378.89"	"0"	"3.54"	"22"	"CC(C)(C)NS(=O)(=O)c1ccc(-c2ccc3[nH]nc(N)c3c2)c(Cl)c1"	"IC50"	"'='"	"39.0"	"nM"	"7.41"	""	""	"UO_0000065"	"19.55"	"0.40"	"3.87"	"7.35"	"False"	"CHEMBL1011746"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139271"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL3647824"	""	"0"	"518.49"	"2"	"5.05"	"BDBM147929"	"N#C[C@H]1C[C@H](NCc2c(F)cccc2F)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"500.0"	"nM"	"6.30"	""	"285863"	"UO_0000065"	"12.15"	"0.23"	"1.25"	"5.79"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3658090"	""	"0"	"626.56"	"2"	"5.50"	"BDBM148334"	"Cc1ccc(NC(=O)c2cccc(Br)c2)cc1N1CCc2nc(Nc3ccc(N4CCN(C)CC4)cc3)ncc2C1=O"	"IC50"	"'='"	"44.0"	"nM"	"7.36"	""	"286816"	"UO_0000065"	"11.74"	"0.24"	"1.86"	"7.85"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703089"	""	"0"	"502.49"	"1"	"2.81"	"BDBM147803"	"N#C[C@H]1CC(NCC(F)F)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)F)cc2)n1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"285737"	"UO_0000065"	"16.36"	"0.33"	"5.41"	"5.75"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647920"	""	"0"	"451.41"	"0"	"2.66"	"BDBM148032"	"[C-]#[N+][C@H]1C[C@H](OC(C)=O)[C@@H](O)C[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"184.0"	"nM"	"6.74"	""	"285969"	"UO_0000065"	"14.92"	"0.29"	"4.08"	"5.44"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703015"	""	"0"	"416.89"	"0"	"3.46"	"BDBM147725"	"N#C[C@H]1C[C@@H](N2CCC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)c(F)c2)n1"	"IC50"	"'='"	"84.0"	"nM"	"7.08"	""	"285659"	"UO_0000065"	"16.97"	"0.33"	"3.62"	"7.08"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703091"	""	"0"	"474.49"	"0"	"3.31"	"BDBM147805"	"N#C[C@H]1C[C@H](N2CC3(COC3)C2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"23.0"	"nM"	"7.64"	""	"285739"	"UO_0000065"	"16.10"	"0.31"	"4.33"	"6.99"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652282"	""	"0"	"474.68"	"0"	"3.09"	"BDBM113090"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCCC(CN3CCCC3)C2)CC1"	"IC50"	"'='"	"125.0"	"nM"	"6.90"	""	"234534"	"UO_0000065"	"14.54"	"0.29"	"3.81"	"8.08"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3703036"	""	"0"	"502.54"	"1"	"4.04"	"BDBM147746"	"N#C[C@H]1C[C@@H](N2CC3(CCC3)C2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc([C@@H](O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"285680"	"UO_0000065"	"16.01"	"0.31"	"4.01"	"6.69"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3648437"	""	"0"	"331.38"	"0"	"3.93"	"BDBM107146"	"C/C(Nc1cccc(-c2cnc3ccccc3n2)c1)=C1/CCOC1=O"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	"226384"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703016"	""	"0"	"416.89"	"0"	"3.46"	"BDBM147726"	"N#C[C@H]1C[C@H](N2CCC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)c(F)c2)n1"	"IC50"	"'='"	"120.0"	"nM"	"6.92"	""	"285660"	"UO_0000065"	"16.60"	"0.33"	"3.46"	"6.92"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL1923581"	""	"0"	"509.61"	"1"	"3.43"	"21"	"CN1CCN(c2ccc(Nc3ncc4ccc(-c5ccccc5N(C)S(C)(=O)=O)n4n3)cc2F)CC1"	"IC50"	"'='"	"3.7"	"nM"	"8.43"	""	""	"UO_0000065"	"16.55"	"0.32"	"5.00"	"9.80"	"False"	"CHEMBL1926252"	"Inhibition of human recombinant JAK2 using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate after 20 mins by fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1921765"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1822515"	""	"0"	"414.51"	"0"	"3.90"	"23"	"COc1ccccc1-c1ccc2cnc(Nc3ccc(N4CCN(C)CC4)cc3)nn12"	"IC50"	"'='"	"0.17"	"nM"	"9.77"	""	""	"UO_0000065"	"23.57"	"0.43"	"5.87"	"16.86"	"False"	"CHEMBL1926252"	"Inhibition of human recombinant JAK2 using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate after 20 mins by fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1921765"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1923583"	""	"0"	"432.50"	"0"	"4.04"	"24"	"COc1ccccc1-c1ccc2cnc(Nc3ccc(N4CCN(C)CC4)c(F)c3)nn12"	"IC50"	"'='"	"0.35"	"nM"	"9.46"	""	""	"UO_0000065"	"21.86"	"0.40"	"5.42"	"16.32"	"False"	"CHEMBL1926252"	"Inhibition of human recombinant JAK2 using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate after 20 mins by fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1921765"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1923586"	""	"0"	"537.67"	"1"	"4.11"	"27"	"CN1CCN(c2ccc(Nc3ncc4ccc(-c5cccc(S(=O)(=O)NC(C)(C)C)c5)n4n3)cc2F)CC1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	""	"UO_0000065"	"16.74"	"0.32"	"4.89"	"9.49"	"False"	"CHEMBL1926252"	"Inhibition of human recombinant JAK2 using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate after 20 mins by fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1921765"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1923594"	""	"0"	"458.57"	"0"	"4.10"	"36"	"COc1ccc(-c2ccc3cnc(Nc4ccc(C5CCN(C[C@H](C)O)CC5)cc4)nn23)cn1"	"IC50"	"'='"	"0.5"	"nM"	"9.30"	""	""	"UO_0000065"	"20.28"	"0.37"	"5.20"	"10.59"	"False"	"CHEMBL1926252"	"Inhibition of human recombinant JAK2 using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate after 20 mins by fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1921765"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL3703032"	""	"0"	"436.44"	"0"	"3.42"	"BDBM147742"	"CN(C)[C@@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(OC(F)(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"92.0"	"nM"	"7.04"	""	"285676"	"UO_0000065"	"16.12"	"0.31"	"3.62"	"6.44"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3644972"	""	"0"	"505.64"	"1"	"3.73"	"BDBM99722"	"COCc1ccccc1-c1cccc2nc(Nc3ccc4c(c3)CCN(CCS(C)(=O)=O)CC4)nn12"	"IC50"	"'='"	"27.55"	"nM"	"7.56"	""	"216412"	"UO_0000065"	"14.95"	"0.29"	"3.83"	"8.51"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647771"	""	"0"	"462.48"	"0"	"3.04"	"BDBM147874"	"CC1(O)CN([C@H]2CC[C@H](n3cc(C(N)=O)c(Nc4ccc(C(F)(F)F)cc4)n3)[C@@H](C#N)C2)C1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"285808"	"UO_0000065"	"18.43"	"0.35"	"5.48"	"7.09"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665215"	""	"0"	"527.70"	"1"	"2.27"	"BDBM112615"	"CC(C)CS(=O)(=O)N1C[C@@H](C)C[C@H](Nc2nc(N3CCN(C)CC3)ncc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.0838"	"nM"	"10.08"	""	"233852"	"UO_0000065"	"19.10"	"0.37"	"7.81"	"8.18"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642280"	""	"0"	"384.42"	"0"	"2.15"	"BDBM99544"	"COc1ccc(Nc2nc3c(-c4cnn(S(C)(=O)=O)c4)cccn3n2)cc1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"216236"	"UO_0000065"	"22.17"	"0.43"	"6.37"	"8.24"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3702932"	""	"0"	"390.45"	"0"	"2.78"	"BDBM147634"	"Cn1cc(-c2ccc(Nc3nn(C4CCCC[C@@H]4C#N)cc3C(N)=O)cn2)cn1"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	"285565"	"UO_0000065"	"20.04"	"0.37"	"5.04"	"6.14"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665166"	""	"0"	"350.43"	"0"	"2.45"	"BDBM112559"	"CC(=O)N1CCC[C@H](Nc2ncccc2-c2cnc3ccn(C)c3n2)C1"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	"233797"	"UO_0000065"	"22.83"	"0.42"	"5.55"	"10.53"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642266"	""	"0"	"373.42"	"0"	"3.51"	"BDBM99525"	"CNC(=O)c1cccc(-c2cccn3nc(Nc4ccccc4OC)nc23)c1"	"IC50"	"'='"	"9999.0"	"nM"	"5.00"	""	"216217"	"UO_0000065"	"13.39"	"0.24"	"1.49"	"6.21"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3335693"	""	"0"	"373.44"	"0"	"1.25"	"BDBM112572"	"CS(=O)(=O)N1CCC[C@H](Nc2ncncc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.1806"	"nM"	"9.74"	""	"233809"	"UO_0000065"	"26.09"	"0.51"	"8.49"	"8.34"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703097"	""	"0"	"432.45"	"0"	"3.68"	"BDBM147812"	"N#C[C@H]1C[C@H](N2CCC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"51.0"	"nM"	"7.29"	""	"285746"	"UO_0000065"	"16.86"	"0.32"	"3.61"	"7.29"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699498"	""	"0"	"409.49"	"0"	"3.55"	"BDBM147515"	"CC(C)(C)OC(=O)C1CC[C@H](C#N)C(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"50.0"	"nM"	"7.30"	""	"285443"	"UO_0000065"	"17.83"	"0.33"	"3.75"	"5.93"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3650997"	""	"0"	"380.40"	"0"	"3.32"	"BDBM153173"	"C=C(C)C(=O)Nc1cc(-c2ncnc3[nH]cc(C(=O)OCC)c23)ccc1OC"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294121"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699561"	""	"0"	"394.87"	"0"	"4.18"	"BDBM147580"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2cnc3ccc(Cl)cc3c2)n1"	"IC50"	"'='"	"23.0"	"nM"	"7.64"	""	"285510"	"UO_0000065"	"19.34"	"0.37"	"3.46"	"6.97"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3658868"	""	"0"	"382.45"	"0"	"1.91"	"BDBM159787"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](CS(=O)(=O)c2cc(C#N)ccn2)C1"	"IC50"	"'='"	"569.0"	"nM"	"6.25"	""	"302597"	"UO_0000065"	"16.33"	"0.32"	"4.33"	"5.40"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL1822525"	""	"0"	"565.70"	"1"	"3.05"	"2"	"COc1cc(N2CCN(C[C@H](C)O)CC2)ccc1Nc1ncc2ccc(-c3ccccc3N(C)S(C)(=O)=O)n2n1"	"IC50"	"'='"	"379.0"	"nM"	"6.42"	""	""	"UO_0000065"	"11.35"	"0.22"	"3.37"	"5.56"	"False"	"CHEMBL1926252"	"Inhibition of human recombinant JAK2 using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate after 20 mins by fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1921765"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1923576"	""	"0"	"414.51"	"0"	"3.90"	"15"	"COc1ccccc1-c1ccc2cnc(Nc3cccc(N4CCN(C)CC4)c3)nn12"	"IC50"	"'='"	"0.8"	"nM"	"9.10"	""	""	"UO_0000065"	"21.95"	"0.40"	"5.20"	"15.70"	"False"	"CHEMBL1926252"	"Inhibition of human recombinant JAK2 using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate after 20 mins by fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1921765"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL2403108"	"CERITINIB"	"4"	"558.15"	"2"	"6.36"	"15b, LDK378"	"Cc1cc(Nc2ncc(Cl)c(Nc3ccccc3S(=O)(=O)C(C)C)n2)c(OC(C)C)cc1C1CCNCC1"	"IC50"	"'='"	"2160.0"	"nM"	"5.67"	""	""	"UO_0000065"	"10.15"	"0.20"	"-0.69"	"5.38"	"False"	"CHEMBL2406312"	"Inhibition of TEL-fused JAK2 (unknown origin) by cell-based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2401692"	"1"	"Scientific Literature"	"J. Med. Chem."	"2013"	"None"	""
"CHEMBL1923571"	""	"0"	"429.48"	"0"	"3.62"	"9"	"COc1ccccc1-c1ccc2cnc(Nc3ccc(C(=O)N4CCOCC4)cc3)nn12"	"IC50"	"'='"	"0.17"	"nM"	"9.77"	""	""	"UO_0000065"	"22.75"	"0.42"	"6.15"	"12.06"	"False"	"CHEMBL1926252"	"Inhibition of human recombinant JAK2 using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate after 20 mins by fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1921765"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1923575"	""	"0"	"401.47"	"0"	"3.99"	"14"	"COc1ccccc1-c1ccc2cnc(Nc3cccc(N4CCOCC4)c3)nn12"	"IC50"	"'='"	"0.35"	"nM"	"9.46"	""	""	"UO_0000065"	"23.55"	"0.43"	"5.47"	"14.79"	"False"	"CHEMBL1926252"	"Inhibition of human recombinant JAK2 using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate after 20 mins by fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1921765"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1923579"	""	"0"	"476.56"	"0"	"3.79"	"18"	"COc1ccccc1-c1ccc2cnc(Nc3ccc(N4CCN(C[C@H](C)O)CC4)c(F)c3)nn12"	"IC50"	"'='"	"0.5"	"nM"	"9.30"	""	""	"UO_0000065"	"19.52"	"0.36"	"5.51"	"11.90"	"False"	"CHEMBL1926252"	"Inhibition of human recombinant JAK2 using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate after 20 mins by fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1921765"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL3644999"	""	"0"	"421.48"	"0"	"3.50"	"BDBM99751"	"CC(=O)Nc1cccc(Nc2nc3c(-c4ccc(S(C)(=O)=O)cc4)cccn3n2)c1"	"IC50"	"'='"	"3.43"	"nM"	"8.46"	""	"216439"	"UO_0000065"	"20.08"	"0.39"	"4.96"	"8.03"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3969771"	""	"0"	"448.64"	"0"	"2.60"	"BDBM113109"	"CCN[C@@H](C)[C@@H]1CCN(S(=O)(=O)CC2CCC(N(C)c3ncnc4[nH]ccc34)CC2)C1"	"IC50"	"'='"	"62.5"	"nM"	"7.20"	""	"234553"	"UO_0000065"	"16.06"	"0.32"	"4.60"	"7.65"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3645535"	""	"0"	"306.37"	"0"	"2.80"	"BDBM107118"	"CN(C)CC(=O)Nc1cccc(-c2cnc3ccccc3n2)c1"	"IC50"	"'>'"	"50000.0"	"nM"	""	""	"226355"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647756"	""	"0"	"524.57"	"1"	"3.64"	"BDBM147859"	"C[C@@H](N[C@@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)(F)F)cc3)n2)[C@@H](C#N)C1)C1CC1"	"IC50"	"'='"	"61.0"	"nM"	"7.21"	""	"285793"	"UO_0000065"	"13.75"	"0.27"	"3.57"	"5.05"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3658107"	""	"0"	"553.63"	"2"	"5.12"	"BDBM148405"	"Cc1ccc(NC(=O)CCC(F)(F)F)cc1N1CCc2nc(Nc3ccc(N4CCN(C)CC4)cc3)ncc2C1"	"IC50"	"'='"	"40.0"	"nM"	"7.40"	""	"286793"	"UO_0000065"	"13.36"	"0.25"	"2.28"	"9.65"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699513"	""	"0"	"455.46"	"0"	"3.32"	"BDBM147531"	"N#C[C@H]1CCCCC1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)CC(F)(F)F)cc2)n1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"285461"	"UO_0000065"	"18.23"	"0.37"	"4.98"	"6.34"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL1933345"	""	"0"	"337.77"	"0"	"4.12"	"3"	"Oc1ccc(-c2nc(Nc3cccc(Cl)c3)nc3[nH]cnc23)cc1"	"IC50"	"'='"	"830.0"	"nM"	"6.08"	""	""	"UO_0000065"	"18.00"	"0.35"	"1.96"	"7.01"	"False"	"CHEMBL1937386"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1933054"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL1774055"	""	"0"	"354.36"	"0"	"4.18"	"1c, AZ960"	"Cc1cc(Nc2nc(N[C@@H](C)c3ccc(F)cc3)c(C#N)cc2F)n[nH]1"	"IC50"	"'<'"	"3.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1776838"	"Inhibition of JAK2 after 60 min"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1772962"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1835020"	""	"0"	"328.39"	"0"	"3.80"	"23"	"C[C@H](Nc1ncc(C(N)=O)c2[nH]c3ccc(F)cc3c12)C(C)(C)C"	"IC50"	"'='"	"52.0"	"nM"	"7.28"	""	""	"UO_0000065"	"22.18"	"0.41"	"3.48"	"8.69"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835021"	""	"0"	"328.39"	"0"	"3.80"	"24"	"C[C@@H](Nc1ncc(C(N)=O)c2[nH]c3ccc(F)cc3c12)C(C)(C)C"	"IC50"	"'='"	"210.0"	"nM"	"6.68"	""	""	"UO_0000065"	"20.33"	"0.38"	"2.88"	"7.97"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835026"	""	"0"	"328.35"	"0"	"2.54"	"29"	"NC(=O)c1cnc(NC2CCOCC2)c2c1[nH]c1ccc(F)cc12"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	""	"UO_0000065"	"23.59"	"0.44"	"5.20"	"8.32"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835036"	""	"0"	"388.48"	"0"	"3.96"	"39"	"Cn1cc(-c2ccc3[nH]c4c(C(N)=O)cnc(NC5CCCCC5)c4c3c2)cn1"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	""	"UO_0000065"	"20.30"	"0.37"	"3.93"	"7.76"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835139"	""	"0"	"388.48"	"0"	"3.82"	"50"	"CCC(Nc1ncc(C(N)=O)c2[nH]c3cc(-c4cnn(C)c4)ccc3c12)C1CC1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	""	"UO_0000065"	"22.39"	"0.41"	"4.88"	"8.56"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL576475"	""	"0"	"318.34"	"0"	"1.78"	"32"	"Nc1nn2cccnc2c1-c1cc(NCc2ccccn2)ncn1"	"IC50"	"'='"	"22.0"	"nM"	"7.66"	""	""	"UO_0000065"	"24.05"	"0.44"	"5.88"	"7.16"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL576862"	""	"0"	"331.38"	"0"	"2.94"	"38"	"C[C@H](Nc1cc(-c2c(N)nn3cccnc23)ncn1)c1ccccc1"	"IC50"	"'='"	"21.0"	"nM"	"7.68"	""	""	"UO_0000065"	"23.17"	"0.42"	"4.74"	"8.17"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL583895"	""	"0"	"349.37"	"0"	"3.08"	"40"	"C[C@@H](Nc1cc(-c2c(N)nn3cccnc23)ncn1)c1ccc(F)cc1"	"IC50"	"'='"	"160.0"	"nM"	"6.80"	""	""	"UO_0000065"	"19.45"	"0.36"	"3.72"	"7.23"	"False"	"CHEMBL1044320"	"Inhibition of JAK2-mediated STAT5 phosphorylation in GMCSF-stimulated human TF1 cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"CHEMBL3307972"	""
"CHEMBL576286"	""	"0"	"357.39"	"0"	"3.44"	"7m"	"CC(C)Oc1cc(Nc2cncc(N[C@@H](C)c3ccc(F)cn3)n2)n[nH]1"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	""	"UO_0000065"	"22.38"	"0.42"	"4.56"	"7.95"	"False"	"CHEMBL1043451"	"Inhibition of JAK2 using 2 mM ATP as a substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156131"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL569738"	""	"0"	"313.34"	"0"	"2.96"	"7n"	"Cc1cc(Nc2cncc(N[C@@H](C)c3ccc(F)cn3)n2)n[nH]1"	"IC50"	"'<'"	"3.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1043451"	"Inhibition of JAK2 using 2 mM ATP as a substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156131"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL570899"	""	"0"	"314.33"	"0"	"2.35"	"7o"	"Cc1cc(Nc2cncc(N[C@@H](C)c3ncc(F)cn3)n2)n[nH]1"	"IC50"	"'<'"	"3.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"True"	"CHEMBL1043451"	"Inhibition of JAK2 using 2 mM ATP as a substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156131"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL576257"	""	"0"	"338.35"	"0"	"2.83"	"7h"	"Cc1cc(Nc2cnc(C#N)c(N[C@@H](C)c3ccc(F)cn3)n2)n[nH]1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"25.19"	"0.47"	"5.69"	"7.40"	"False"	"CHEMBL1043452"	"Inhibition of JAK2 using 5 mM ATP as a substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156131"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL570464"	""	"0"	"329.34"	"0"	"2.66"	"7p"	"COc1cc(Nc2cncc(N[C@@H](C)c3ccc(F)cn3)n2)n[nH]1"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	""	"UO_0000065"	"24.59"	"0.46"	"5.44"	"8.05"	"False"	"CHEMBL1043452"	"Inhibition of JAK2 using 5 mM ATP as a substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156131"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL570668"	""	"0"	"295.35"	"0"	"1.76"	"10"	"Nc1nn2cccnc2c1-c1cc(N2CCCCC2)ncn1"	"IC50"	"'='"	"44.0"	"nM"	"7.36"	""	""	"UO_0000065"	"24.91"	"0.46"	"5.60"	"8.63"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL568866"	""	"0"	"408.51"	"0"	"2.16"	"13"	"CCN(CC)C(=O)C1CCCN(c2cc(-c3c(N)nn4cc(C)cnc34)ncn2)C1"	"IC50"	"'='"	"260.0"	"nM"	"6.58"	""	""	"UO_0000065"	"16.12"	"0.30"	"4.43"	"6.24"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL569737"	""	"0"	"366.43"	"0"	"1.07"	"23"	"CN(C)C(=O)C1CCCN(c2cc(-c3c(N)nn4cccnc34)ncn2)C1"	"IC50"	"'='"	"200.0"	"nM"	"6.70"	""	""	"UO_0000065"	"18.28"	"0.34"	"5.63"	"6.35"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL570686"	""	"0"	"335.35"	"0"	"2.52"	"34"	"Nc1nn2cccnc2c1-c1cc(NCc2ccc(F)cc2)ncn1"	"IC50"	"'='"	"1.5"	"nM"	"8.82"	""	""	"UO_0000065"	"26.31"	"0.48"	"6.30"	"9.39"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1682388"	""	"0"	"486.91"	"0"	"3.33"	"28"	"Cc1cc(Nc2nc(N3CCN(C(=O)Cc4c(F)cc(Cl)cc4F)CC3)nn3cccc23)n[nH]1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	""	"UO_0000065"	"18.48"	"0.36"	"5.67"	"9.53"	"False"	"CHEMBL1685409"	"Inhibition of JAK2 after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1681645"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1682382"	""	"0"	"430.52"	"0"	"2.70"	"22"	"Cc1ccc(CC(=O)N2CCN(c3nc(Nc4cc(C)[nH]n4)c4cccn4n3)CC2)cc1"	"IC50"	"'='"	"1.1"	"nM"	"8.96"	""	""	"UO_0000065"	"20.81"	"0.38"	"6.26"	"9.49"	"False"	"CHEMBL1685409"	"Inhibition of JAK2 after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1681645"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1682377"	""	"0"	"432.49"	"0"	"2.48"	"17"	"COc1ccccc1C(=O)N1CCN(c2nc(Nc3cc(C)[nH]n3)c3cccn3n2)CC1"	"IC50"	"'='"	"3.5"	"nM"	"8.46"	""	""	"UO_0000065"	"19.55"	"0.36"	"5.98"	"8.16"	"False"	"CHEMBL1685409"	"Inhibition of JAK2 after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1681645"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1682370"	""	"0"	"369.43"	"0"	"1.31"	"10"	"Cc1cc(Nc2nc(N3CCN(C(=O)N(C)C)CC3)nn3cccc23)n[nH]1"	"IC50"	"'='"	"9.3"	"nM"	"8.03"	""	""	"UO_0000065"	"21.74"	"0.41"	"6.72"	"8.22"	"False"	"CHEMBL1685409"	"Inhibition of JAK2 after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1681645"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1682363"	""	"0"	"413.49"	"0"	"2.76"	"3"	"O=C(Cc1ccccc1)N1CCN(c2nc(Nc3ccccn3)c3cccn3n2)CC1"	"IC50"	"'='"	"190.0"	"nM"	"6.72"	""	""	"UO_0000065"	"16.25"	"0.30"	"3.96"	"8.54"	"False"	"CHEMBL1685409"	"Inhibition of JAK2 after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1681645"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1448"	"NICLOSAMIDE"	"4"	"327.12"	"0"	"3.86"	"5"	"O=C(Nc1ccc([N+](=O)[O-])cc1Cl)c1cc(Cl)ccc1O"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1697118"	"Inhibition of JAK2 after 60 mins by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1687697"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1081291"	""	"0"	"410.86"	"1"	"5.92"	"4"	"COc1cc(Nc2nc3cccc(-c4cccc(Cl)c4)c3o2)cc(OC)c1OC"	"IC50"	"'='"	"440.0"	"nM"	"6.36"	""	""	"UO_0000065"	"15.47"	"0.30"	"0.44"	"9.67"	"False"	"CHEMBL1102770"	"Inhibition of GST-tagged JAK2 assessed as inhibition of biotinylated JAK3tide peptide phosphorylation after 60 mins by caliper mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154949"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1081977"	""	"0"	"469.52"	"0"	"4.64"	"8"	"COc1cc(Nc2nc3cccc(-c4ccc(NS(C)(=O)=O)cc4)c3o2)cc(OC)c1OC"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	""	"UO_0000065"	"17.68"	"0.34"	"3.66"	"7.42"	"False"	"CHEMBL1102770"	"Inhibition of GST-tagged JAK2 assessed as inhibition of biotinylated JAK3tide peptide phosphorylation after 60 mins by caliper mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154949"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1081484"	""	"0"	"507.52"	"1"	"4.88"	"10"	"COc1cc(Nc2nc3cccc(-c4ccc(C(=O)N5CCOCC5)c(F)c4)c3o2)cc(OC)c1OC"	"IC50"	"'<'"	"3.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1102770"	"Inhibition of GST-tagged JAK2 assessed as inhibition of biotinylated JAK3tide peptide phosphorylation after 60 mins by caliper mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154949"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1082022"	""	"0"	"492.53"	"1"	"5.02"	"15"	"CNC(=O)c1ccc(Nc2nc3cccc(-c4cc(F)c(CN5CCOCC5)c(F)c4)c3o2)cc1C"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	""	"UO_0000065"	"16.85"	"0.31"	"3.28"	"10.42"	"False"	"CHEMBL1102770"	"Inhibition of GST-tagged JAK2 assessed as inhibition of biotinylated JAK3tide peptide phosphorylation after 60 mins by caliper mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154949"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1078178"	"MOMELOTINIB"	"3"	"414.47"	"0"	"2.98"	"28"	"N#CCNC(=O)c1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	""	"UO_0000065"	"19.20"	"0.35"	"4.98"	"7.71"	"False"	"CHEMBL1108564"	"Inhibition of JAK2 V617F mutant (JH1-JH2)"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1289992"	""	"0"	"325.39"	"0"	"4.19"	"7"	"CC(C)(C)CNc1nc2cc[nH]c(=O)c2cc1-c1ccc(F)cc1"	"IC50"	"'='"	"29000.0"	"nM"	"4.54"	""	""	"UO_0000065"	"13.95"	"0.26"	"0.35"	"7.85"	"False"	"CHEMBL1291235"	"Inhibition of JAK2 in cell-free system"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287746"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1290309"	""	"0"	"313.38"	"0"	"4.06"	"24"	"CC(Nc1nc2cc[nH]c(=O)c2c2cc(F)ccc12)C(C)(C)C"	"IC50"	"'='"	"26.0"	"nM"	"7.58"	""	""	"UO_0000065"	"24.20"	"0.45"	"3.53"	"13.13"	"False"	"CHEMBL1291235"	"Inhibition of JAK2 in cell-free system"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287746"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1290310"	""	"0"	"314.36"	"0"	"2.61"	"25"	"CC(C)(CN)CNc1nc2cc[nH]c(=O)c2c2cc(F)ccc12"	"IC50"	"'='"	"3157.0"	"nM"	"5.50"	""	""	"UO_0000065"	"17.50"	"0.33"	"2.89"	"6.56"	"False"	"CHEMBL1291235"	"Inhibition of JAK2 in cell-free system"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287746"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1290424"	""	"0"	"320.33"	"0"	"3.22"	"27"	"O=c1[nH]ccc2nc(NCc3ccccn3)c3ccc(F)cc3c12"	"IC50"	"'='"	"1115.0"	"nM"	"5.95"	""	""	"UO_0000065"	"18.58"	"0.34"	"2.73"	"8.42"	"False"	"CHEMBL1291235"	"Inhibition of JAK2 in cell-free system"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287746"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1290534"	""	"0"	"366.44"	"0"	"3.28"	"29"	"CN1CCC(N(c2nc3cc[nH]c(=O)c3c3cc(F)ccc23)C2CC2)CC1"	"IC50"	"'='"	"540.0"	"nM"	"6.27"	""	""	"UO_0000065"	"17.10"	"0.32"	"2.99"	"12.00"	"False"	"CHEMBL1291235"	"Inhibition of JAK2 in cell-free system"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287746"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1289097"	""	"0"	"353.32"	"0"	"4.21"	"38"	"CC(C)[C@@H](Nc1nc2cc[nH]c(=O)c2c2cc(F)ccc12)C(F)(F)F"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	""	"UO_0000065"	"25.47"	"0.49"	"4.79"	"15.58"	"False"	"CHEMBL1291235"	"Inhibition of JAK2 in cell-free system"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287746"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1289218"	""	"0"	"336.32"	"0"	"3.47"	"41"	"CC(C)[C@@H](Nc1nc2cc[nH]c(=O)c2c2cnccc12)C(F)(F)F"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	""	"UO_0000065"	"26.76"	"0.51"	"5.53"	"12.74"	"True"	"CHEMBL1291235"	"Inhibition of JAK2 in cell-free system"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287746"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1289097"	""	"0"	"353.32"	"0"	"4.21"	"38"	"CC(C)[C@@H](Nc1nc2cc[nH]c(=O)c2c2cc(F)ccc12)C(F)(F)F"	"IC50"	"'='"	"50.0"	"nM"	"7.30"	""	""	"UO_0000065"	"20.66"	"0.40"	"3.09"	"12.64"	"False"	"CHEMBL1291236"	"Inhibition of JAK2 expressed in human Du-145 cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"DU-145"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287746"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3308034"	""
"CHEMBL1087235"	""	"0"	"336.36"	"0"	"1.81"	"5a"	"O=c1[nH]c2cnc(-n3cnc4ccccc43)nc2n1C1CCOCC1"	"IC50"	"'='"	"3250.0"	"nM"	"5.49"	""	""	"UO_0000065"	"16.32"	"0.30"	"3.68"	"6.06"	"False"	"CHEMBL1102456"	"Inhibition of human JAK2 (532-1132) by time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154364"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1773082"	""	"0"	"371.81"	"0"	"4.09"	"1e"	"Cc1cc(Nc2nc(N[C@@H](C)c3ccc(F)cn3)c(C#N)cc2Cl)n[nH]1"	"IC50"	"'<'"	"3.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1776838"	"Inhibition of JAK2 after 60 min"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1772962"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1080322"	""	"0"	"370.80"	"0"	"2.46"	"5e"	"O=c1[nH]c2cnc(-n3cnc4ccc(Cl)cc43)nc2n1C1CCOCC1"	"IC50"	"'='"	"393.0"	"nM"	"6.41"	""	""	"UO_0000065"	"17.28"	"0.34"	"3.95"	"7.07"	"False"	"CHEMBL1102456"	"Inhibition of human JAK2 (532-1132) by time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154364"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1079523"	""	"0"	"403.35"	"0"	"2.66"	"6j"	"N#Cc1ccc2ncn(-c3ncc4[nH]c(=O)n(Cc5c(F)cccc5F)c4n3)c2c1"	"IC50"	"'='"	"28.0"	"nM"	"7.55"	""	""	"UO_0000065"	"18.73"	"0.34"	"4.89"	"7.18"	"False"	"CHEMBL1102456"	"Inhibition of human JAK2 (532-1132) by time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154364"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1079526"	""	"0"	"402.39"	"0"	"2.97"	"21b"	"O=c1[nH]c2cnc(-n3cnc4ccccc43)nc2n1C1CCOc2cccc(F)c21"	"IC50"	"'='"	"97.0"	"nM"	"7.01"	""	""	"UO_0000065"	"17.43"	"0.32"	"4.04"	"7.74"	"False"	"CHEMBL1102456"	"Inhibition of human JAK2 (532-1132) by time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154364"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1079594"	""	"0"	"427.40"	"0"	"2.84"	"25"	"N#Cc1ccc2ncn(-c3ncc4[nH]c(=O)n([C@@H]5CCOc6c(F)cccc65)c4n3)c2c1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	""	"UO_0000065"	"19.42"	"0.35"	"5.46"	"7.26"	"False"	"CHEMBL1102456"	"Inhibition of human JAK2 (532-1132) by time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154364"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1092588"	""	"0"	"471.56"	"0"	"4.82"	"14"	"COc1cc(-c2cnc3cccc(-c4ccc(CN5CCOCC5)cc4)c3n2)cc(OC)c1OC"	"IC50"	"'='"	"120.0"	"nM"	"6.92"	""	""	"UO_0000065"	"14.68"	"0.27"	"2.10"	"10.50"	"False"	"CHEMBL1116984"	"Inhibition of recombinant GST tagged JAK2 protein after 60 mins using FITC-GGEEEEYFELVKKKK-NH2 substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156975"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1092063"	""	"0"	"569.73"	"1"	"3.89"	"20"	"Cc1cc(-c2cnc3cccc(-c4ccc(CN5CCS(=O)(=O)CC5)cc4)c3n2)ccc1C(=O)N1CCN(C)CC1"	"IC50"	"'='"	"7.1"	"nM"	"8.15"	""	""	"UO_0000065"	"14.30"	"0.27"	"4.26"	"9.40"	"False"	"CHEMBL1116984"	"Inhibition of recombinant GST tagged JAK2 protein after 60 mins using FITC-GGEEEEYFELVKKKK-NH2 substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156975"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1092925"	""	"0"	"564.66"	"1"	"3.62"	"25"	"CN1CCN(c2ccc(-c3cnc4cccc(-c5cc(F)c(CN6CCS(=O)(=O)CC6)c(F)c5)c4n3)cn2)CC1"	"IC50"	"'='"	"6.8"	"nM"	"8.17"	""	""	"UO_0000065"	"14.46"	"0.28"	"4.55"	"9.90"	"False"	"CHEMBL1116984"	"Inhibition of recombinant GST tagged JAK2 protein after 60 mins using FITC-GGEEEEYFELVKKKK-NH2 substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156975"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL595305"	""	"0"	"221.26"	"0"	"3.16"	"13f"	"c1ccc2c(c1)NCc1c[nH]c3nccc-2c13"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL595626"	""	"0"	"341.41"	"0"	"4.91"	"13h"	"c1ccc(COCC2Nc3ccccc3-c3ccnc4[nH]cc2c34)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL601718"	""	"0"	"333.34"	"1"	"5.02"	"13p"	"Fc1cccc(F)c1C1Nc2ccccc2-c2ccnc3[nH]cc1c23"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL592270"	""	"0"	"316.34"	"0"	"4.28"	"14d"	"Fc1cccc(C2Nc3ccccc3-c3ncnc4[nH]cc2c34)c1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL604038"	""	"0"	"332.34"	"0"	"3.98"	"14e"	"Oc1ccc(C2Nc3ccccc3-c3ncnc4[nH]cc2c34)c(F)c1"	"IC50"	"'='"	"200.0"	"nM"	"6.70"	""	""	"UO_0000065"	"20.16"	"0.37"	"2.72"	"9.07"	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL1946151"	""	"0"	"500.60"	"1"	"4.52"	"27u"	"CN1C/C=C/CCOc2cccc(c2)-c2ccnc(n2)Nc2cc(cc(NC(=O)N3CCOCC3)c2)C1"	"IC50"	"'='"	"44.0"	"nM"	"7.36"	""	""	"UO_0000065"	"14.70"	"0.27"	"2.84"	"8.01"	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1938643"	""	"0"	"368.46"	"0"	"2.74"	"8"	"CNC(=O)c1cnc(N)c2cc(-c3ccc(N4CCOCC4)cc3)sc12"	"IC50"	"'='"	"3940.0"	"nM"	"5.41"	""	""	"UO_0000065"	"14.67"	"0.28"	"2.66"	"6.72"	"False"	"CHEMBL1941390"	"Inhibition of TEL-fused JAK2 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3307634"	""
"CHEMBL1088857"	""	"0"	"489.55"	"0"	"4.96"	"17"	"COc1cc(-c2cnc3cccc(-c4ccc(CN5CCOCC5)c(F)c4)c3n2)cc(OC)c1OC"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	""	"UO_0000065"	"15.73"	"0.29"	"2.74"	"11.68"	"False"	"CHEMBL1116984"	"Inhibition of recombinant GST tagged JAK2 protein after 60 mins using FITC-GGEEEEYFELVKKKK-NH2 substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156975"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1093119"	""	"0"	"544.60"	"1"	"4.86"	"23"	"Cc1cc(-c2cnc3cccc(-c4cc(F)c(CN5CCOCC5)c(F)c4)c3n2)ccc1C(=O)N1CCOCC1"	"IC50"	"'='"	"3.1"	"nM"	"8.51"	""	""	"UO_0000065"	"15.62"	"0.29"	"3.65"	"12.55"	"False"	"CHEMBL1116984"	"Inhibition of recombinant GST tagged JAK2 protein after 60 mins using FITC-GGEEEEYFELVKKKK-NH2 substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156975"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL585927"	""	"0"	"523.55"	"1"	"4.88"	"1"	"CNc1ccn(-c2ccccc2)c(=O)c1C(=O)Nc1ccc(Oc2ccnc3cc(OC)c(OC)cc23)cn1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1038361"	"Inhibition of Jak2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1155349"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1085511"	""	"0"	"499.62"	"0"	"4.60"	"4c"	"CC(C)COC(=O)Nc1ccc(-c2cnc3c(-c4ccc(N5CCN(C)CC5)cc4)cnn3c2N)cc1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1120244"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1158604"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL592035"	""	"0"	"341.37"	"0"	"4.44"	"13ae"	"O=C(O)c1ccc(C2Nc3ccccc3-c3ccnc4[nH]cc2c34)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL602788"	""	"0"	"298.35"	"0"	"4.14"	"13ag"	"c1ccc2c(c1)NC(c1ccncc1)c1c[nH]c3nccc-2c13"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL602842"	""	"0"	"290.25"	"0"	"3.65"	"14a"	"FC(F)(F)C1Nc2ccccc2-c2ncnc3[nH]cc1c23"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL604037"	""	"0"	"298.35"	"0"	"4.14"	"14c"	"c1ccc(C2Nc3ccccc3-c3ncnc4[nH]cc2c34)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL589387"	""	"0"	"389.39"	"0"	"3.92"	"22b"	"COC(=O)C1(c2ccc(O)c(F)c2)Nc2ccccc2-c2ccnc3[nH]cc1c23"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL590854"	""	"0"	"333.34"	"1"	"5.02"	"13q"	"Fc1ccc(C2Nc3ccccc3-c3ccnc4[nH]cc2c34)c(F)c1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL591096"	""	"0"	"331.35"	"0"	"4.59"	"13v"	"Oc1ccc(C2Nc3ccccc3-c3ccnc4[nH]cc2c34)cc1F"	"IC50"	"'='"	"860.0"	"nM"	"6.07"	""	""	"UO_0000065"	"18.31"	"0.33"	"1.48"	"9.95"	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL604245"	""	"0"	"327.39"	"0"	"4.75"	"13aa"	"COc1ccc(C2Nc3ccccc3-c3ccnc4[nH]cc2c34)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL1835138"	""	"0"	"374.45"	"0"	"3.43"	"49"	"C[C@@H](Nc1ncc(C(N)=O)c2[nH]c3cc(-c4cnn(C)c4)ccc3c12)C1CC1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	""	"UO_0000065"	"21.25"	"0.39"	"4.53"	"7.83"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835137"	""	"0"	"374.45"	"0"	"3.43"	"48"	"C[C@H](Nc1ncc(C(N)=O)c2[nH]c3cc(-c4cnn(C)c4)ccc3c12)C1CC1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	""	"UO_0000065"	"24.04"	"0.44"	"5.57"	"8.86"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835149"	""	"0"	"414.39"	"0"	"3.96"	"61"	"NC(=O)c1cnc(N[C@H](C2CC2)C(F)(F)F)c2c1[nH]c1cc(-c3cn[nH]c3)ccc12"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	""	"UO_0000065"	"21.72"	"0.41"	"5.04"	"8.00"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL570899"	""	"0"	"314.33"	"0"	"2.35"	"4"	"Cc1cc(Nc2cncc(N[C@@H](C)c3ncc(F)cn3)n2)n[nH]1"	"IC50"	"'<'"	"3.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1103122"	"Inhibition of recombinant JAK2 kinase in presence of ATP"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154970"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL228043"	""	"0"	"360.01"	"0"	"3.51"	"LFM-A13"	"C/C(O)=C(\C#N)C(=O)Nc1cc(Br)ccc1Br"	"IC50"	"'>'"	"500000.0"	"nM"	""	"Outside typical range"	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL920666"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1144565"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2007"	"None"	""
"CHEMBL1650734"	""	"0"	"433.88"	"0"	"2.84"	"16c"	"Cc1cc(Nc2nc(N[C@@H](C)c3ncc(F)cn3)nc(N3CCOCC3)c2Cl)n[nH]1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	""	"UO_0000065"	"18.54"	"0.37"	"5.21"	"6.89"	"False"	"CHEMBL1656589"	"Inhibition of JAK2 using 5 mM of ATP"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1650727"	""	"0"	"349.76"	"0"	"2.97"	"9h"	"Cc1cc(Nc2nc(O[C@H](C)c3ncc(F)cn3)ncc2Cl)n[nH]1"	"IC50"	"'='"	"346.0"	"nM"	"6.46"	""	""	"UO_0000065"	"18.47"	"0.37"	"3.49"	"6.37"	"False"	"CHEMBL1656588"	"Inhibition of JAK2 using Km ATP concentration"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1650728"	""	"0"	"409.22"	"0"	"2.82"	"9i"	"COc1cc(Nc2nc(N[C@@H](C)c3ncc(F)cn3)ncc2Br)n[nH]1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	""	"UO_0000065"	"20.52"	"0.46"	"5.58"	"7.40"	"False"	"CHEMBL1656588"	"Inhibition of JAK2 using Km ATP concentration"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1650732"	""	"0"	"399.43"	"0"	"2.19"	"16a"	"Cc1cc(Nc2cc(N3CCOCC3)nc(N[C@@H](C)c3ncc(F)cn3)n2)n[nH]1"	"IC50"	"'<'"	"3.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1656589"	"Inhibition of JAK2 using 5 mM of ATP"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL603432"	""	"0"	"263.34"	"0"	"4.35"	"13c"	"CC(C)C1Nc2ccccc2-c2ccnc3[nH]cc1c23"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL604481"	""	"0"	"303.41"	"1"	"5.28"	"13g"	"c1ccc2c(c1)NC(C1CCCCC1)c1c[nH]c3nccc-2c13"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL606355"	""	"0"	"315.35"	"0"	"4.88"	"13m"	"Fc1ccccc1C1Nc2ccccc2-c2ccnc3[nH]cc1c23"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL601925"	""	"0"	"315.35"	"0"	"4.88"	"13o"	"Fc1ccc(C2Nc3ccccc3-c3ccnc4[nH]cc2c34)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL592034"	""	"0"	"327.39"	"0"	"4.24"	"13ab"	"OCc1ccc(C2Nc3ccccc3-c3ccnc4[nH]cc2c34)cc1"	"IC50"	"'='"	"1100.0"	"nM"	"5.96"	""	""	"UO_0000065"	"18.20"	"0.33"	"1.72"	"9.78"	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL589869"	""	"0"	"332.34"	"0"	"3.98"	"14f"	"Oc1ccc(C2Nc3ccccc3-c3ncnc4[nH]cc2c34)cc1F"	"IC50"	"'='"	"140.0"	"nM"	"6.85"	""	""	"UO_0000065"	"20.62"	"0.37"	"2.87"	"9.28"	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL1087269"	""	"0"	"415.50"	"0"	"3.53"	"7b"	"Cc1cnc(Nc2cc(N3CCOCC3)nc(N[C@@H](C)c3ccc(F)cn3)n2)s1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	""	"UO_0000065"	"19.98"	"0.39"	"4.77"	"9.42"	"False"	"CHEMBL1103123"	"Inhibition of recombinant JAK2 kinase in presence of 5 mM ATP"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154970"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL4160833"	""	"0"	"595.73"	"1"	"3.66"	"20f"	"CS(=O)(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCC(C(=O)NCCCCCC(=O)NO)CC4)cc3)n2)cc1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"14.31"	"0.28"	"4.86"	"5.15"	"False"	"CHEMBL4150584"	"Inhibition of JAK2 (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition and measured after 25 mins in presence of ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4145634"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4168767"	""	"0"	"466.55"	"0"	"4.56"	"26"	"Nc1ccccc1NC(=O)c1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"110.0"	"nM"	"6.96"	""	""	"UO_0000065"	"14.92"	"0.27"	"2.40"	"6.60"	"False"	"CHEMBL4150584"	"Inhibition of JAK2 (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition and measured after 25 mins in presence of ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4145634"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL205098"	""	"0"	"377.40"	"0"	"3.58"	"1"	"COc1cc(Nc2ncc3ccn(-c4ccccn4)c3n2)cc(OC)c1OC"	"IC50"	"'='"	"5.9"	"nM"	"8.23"	""	""	"UO_0000065"	"21.80"	"0.40"	"4.65"	"9.88"	"False"	"CHEMBL1107850"	"Inhibition of recombinant GST tagged JAK2 after 60 mins by Caliper mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1155411"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1088424"	""	"0"	"354.35"	"0"	"1.95"	"5d"	"O=c1[nH]c2cnc(-n3cnc4ccc(F)cc43)nc2n1C1CCOCC1"	"IC50"	"'='"	"3400.0"	"nM"	"5.47"	""	""	"UO_0000065"	"15.43"	"0.29"	"3.52"	"6.03"	"False"	"CHEMBL1102456"	"Inhibition of human JAK2 (532-1132) by time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154364"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1079525"	""	"0"	"384.40"	"0"	"2.83"	"21a"	"O=c1[nH]c2cnc(-n3cnc4ccccc43)nc2n1C1CCOc2ccccc21"	"IC50"	"'='"	"170.0"	"nM"	"6.77"	""	""	"UO_0000065"	"17.61"	"0.32"	"3.94"	"7.47"	"False"	"CHEMBL1102456"	"Inhibition of human JAK2 (532-1132) by time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154364"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1290089"	""	"0"	"345.32"	"0"	"3.57"	"8"	"O=c1[nH]ccc2nc(N3CCC(F)(F)C3)c(-c3ccc(F)cc3)cc12"	"IC50"	"'='"	"11800.0"	"nM"	"4.93"	""	""	"UO_0000065"	"14.27"	"0.27"	"1.36"	"10.06"	"False"	"CHEMBL1291235"	"Inhibition of JAK2 in cell-free system"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287746"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1290197"	""	"0"	"389.46"	"0"	"4.49"	"13"	"CC(Nc1nc2cc[nH]c(=O)c2cc1-c1nc(-c2ccccc2)no1)C(C)(C)C"	"IC50"	"'='"	"11500.0"	"nM"	"4.94"	""	""	"UO_0000065"	"12.68"	"0.23"	"0.45"	"5.11"	"False"	"CHEMBL1291235"	"Inhibition of JAK2 in cell-free system"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287746"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1290533"	""	"0"	"388.23"	"1"	"5.13"	"28"	"O=c1[nH]ccc2nc(NCc3c(Cl)cccc3Cl)c3ccc(F)cc3c12"	"IC50"	"'='"	"53.0"	"nM"	"7.28"	""	""	"UO_0000065"	"18.74"	"0.38"	"2.15"	"12.59"	"False"	"CHEMBL1291235"	"Inhibition of JAK2 in cell-free system"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287746"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1290769"	""	"0"	"283.31"	"0"	"3.18"	"34"	"O=c1[nH]ccc2nc(NC3CCC3)c3ccc(F)cc3c12"	"IC50"	"'='"	"75.0"	"nM"	"7.12"	""	""	"UO_0000065"	"25.15"	"0.46"	"3.94"	"12.33"	"False"	"CHEMBL1291235"	"Inhibition of JAK2 in cell-free system"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287746"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1204012"	""	"0"	"430.94"	"0"	"1.85"	"22"	"CCN(CC)C(=O)C1CCCN(c2cc(-c3c(N)nn4cccnc34)ncn2)C1.Cl"	"IC50"	"'>'"	"20000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1044320"	"Inhibition of JAK2-mediated STAT5 phosphorylation in GMCSF-stimulated human TF1 cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"CHEMBL3307972"	""
"CHEMBL568815"	""	"0"	"336.33"	"0"	"2.49"	"36"	"Nc1nn2cccnc2c1-c1cc(OCc2ccc(F)cc2)ncn1"	"IC50"	"'>'"	"20000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1044320"	"Inhibition of JAK2-mediated STAT5 phosphorylation in GMCSF-stimulated human TF1 cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"CHEMBL3307972"	""
"CHEMBL1289096"	""	"0"	"319.29"	"0"	"3.43"	"37"	"O=c1[nH]ccc2nc(NC3CC(F)(F)C3)c3ccc(F)cc3c12"	"IC50"	"'='"	"750.0"	"nM"	"6.12"	""	""	"UO_0000065"	"19.18"	"0.36"	"2.69"	"10.60"	"False"	"CHEMBL1291235"	"Inhibition of JAK2 in cell-free system"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287746"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL569721"	""	"0"	"353.37"	"0"	"2.53"	"7d"	"Cc1cc(Nc2nc(N[C@H](C)c3ncc(F)cn3)c(C#N)nc2C)n[nH]1"	"IC50"	"'='"	"50.0"	"nM"	"7.30"	""	""	"UO_0000065"	"20.66"	"0.38"	"4.77"	"5.70"	"False"	"CHEMBL1043451"	"Inhibition of JAK2 using 2 mM ATP as a substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156131"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL570230"	""	"0"	"352.38"	"0"	"3.14"	"7f"	"Cc1cc(Nc2nc(N[C@H](C)c3ccc(F)cn3)c(C#N)nc2C)n[nH]1"	"IC50"	"'='"	"75.0"	"nM"	"7.12"	""	""	"UO_0000065"	"20.22"	"0.37"	"3.98"	"6.18"	"False"	"CHEMBL1043451"	"Inhibition of JAK2 using 2 mM ATP as a substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156131"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL570002"	""	"0"	"339.34"	"0"	"2.23"	"7a"	"Cc1cc(Nc2cnc(C#N)c(N[C@@H](C)c3ncc(F)cn3)n2)n[nH]1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	""	"UO_0000065"	"24.23"	"0.45"	"5.99"	"6.42"	"False"	"CHEMBL1043452"	"Inhibition of JAK2 using 5 mM ATP as a substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156131"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL571526"	""	"0"	"353.36"	"0"	"3.11"	"7j"	"Cc1cc(Nc2nc(O[C@H](C)c3ccc(F)cn3)c(C#N)nc2C)n[nH]1"	"IC50"	"'='"	"4666.0"	"nM"	"5.33"	""	""	"UO_0000065"	"15.09"	"0.28"	"2.22"	"4.74"	"False"	"CHEMBL1043452"	"Inhibition of JAK2 using 5 mM ATP as a substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156131"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL578194"	""	"0"	"364.39"	"0"	"3.40"	"7k"	"C[C@H](Nc1nc(Nc2cc(C3CC3)[nH]n2)cnc1C#N)c1ccc(F)cn1"	"IC50"	"'='"	"25.0"	"nM"	"7.60"	""	""	"UO_0000065"	"20.86"	"0.38"	"4.20"	"6.60"	"False"	"CHEMBL1043452"	"Inhibition of JAK2 using 5 mM ATP as a substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156131"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL576068"	""	"0"	"327.37"	"0"	"3.27"	"7l"	"Cc1cc(Nc2nc(N[C@@H](C)c3ccc(F)cn3)cnc2C)n[nH]1"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	""	"UO_0000065"	"23.66"	"0.44"	"4.47"	"8.47"	"False"	"CHEMBL1043452"	"Inhibition of JAK2 using 5 mM ATP as a substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156131"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL569738"	""	"0"	"313.34"	"0"	"2.96"	"7n"	"Cc1cc(Nc2cncc(N[C@@H](C)c3ccc(F)cn3)n2)n[nH]1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"27.20"	"0.51"	"5.56"	"9.32"	"False"	"CHEMBL1043452"	"Inhibition of JAK2 using 5 mM ATP as a substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156131"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL576486"	""	"0"	"297.32"	"0"	"0.61"	"14"	"Nc1nn2cccnc2c1-c1cc(N2CCOCC2)ncn1"	"IC50"	"'='"	"210.0"	"nM"	"6.68"	""	""	"UO_0000065"	"22.46"	"0.41"	"6.07"	"7.07"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL585527"	""	"0"	"324.39"	"0"	"0.91"	"15"	"CN(C)C1CCN(c2cc(-c3c(N)nn4cccnc34)ncn2)C1"	"IC50"	"'='"	"880.0"	"nM"	"6.06"	""	""	"UO_0000065"	"18.67"	"0.34"	"5.15"	"6.84"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL571119"	""	"0"	"367.41"	"0"	"1.55"	"20"	"CCOC(=O)C1CCCN(c2cc(-c3c(N)nn4cccnc34)ncn2)C1"	"IC50"	"'='"	"130.0"	"nM"	"6.89"	""	""	"UO_0000065"	"18.74"	"0.35"	"5.34"	"6.17"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL568816"	""	"0"	"331.38"	"0"	"2.94"	"37"	"C[C@@H](Nc1cc(-c2c(N)nn3cccnc23)ncn1)c1ccccc1"	"IC50"	"'='"	"1.4"	"nM"	"8.85"	""	""	"UO_0000065"	"26.72"	"0.48"	"5.91"	"9.42"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL576476"	""	"0"	"343.39"	"0"	"2.87"	"41"	"Nc1nn2cccnc2c1-c1cc(N[C@H]2CCc3ccccc32)ncn1"	"IC50"	"'='"	"52.0"	"nM"	"7.28"	""	""	"UO_0000065"	"21.21"	"0.38"	"4.41"	"7.75"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL582808"	""	"0"	"375.41"	"0"	"3.25"	"43"	"Nc1nn2cccnc2c1-c1cc(N2CCCC2c2ccc(F)cc2)ncn1"	"IC50"	"'='"	"3.4"	"nM"	"8.47"	""	""	"UO_0000065"	"22.56"	"0.41"	"5.22"	"9.94"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL578201"	""	"0"	"352.38"	"0"	"3.14"	"7e"	"Cc1cc(Nc2nc(N[C@@H](C)c3ccc(F)cn3)c(C#N)nc2C)n[nH]1"	"IC50"	"'<'"	"3.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1043451"	"Inhibition of JAK2 using 2 mM ATP as a substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156131"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL578194"	""	"0"	"364.39"	"0"	"3.40"	"7k"	"C[C@H](Nc1nc(Nc2cc(C3CC3)[nH]n2)cnc1C#N)c1ccc(F)cn1"	"IC50"	"'<'"	"3.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1043451"	"Inhibition of JAK2 using 2 mM ATP as a substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156131"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL568788"	""	"0"	"338.35"	"0"	"2.83"	"7b"	"Cc1cc(Nc2cnc(C#N)c(NC(C)c3ccc(F)cn3)n2)n[nH]1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	""	"UO_0000065"	"24.53"	"0.45"	"5.47"	"7.21"	"False"	"CHEMBL1043452"	"Inhibition of JAK2 using 5 mM ATP as a substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156131"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL576286"	""	"0"	"357.39"	"0"	"3.44"	"7m"	"CC(C)Oc1cc(Nc2cncc(N[C@@H](C)c3ccc(F)cn3)n2)n[nH]1"	"IC50"	"'='"	"421.0"	"nM"	"6.38"	""	""	"UO_0000065"	"17.84"	"0.33"	"2.94"	"6.34"	"False"	"CHEMBL1043452"	"Inhibition of JAK2 using 5 mM ATP as a substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156131"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1082023"	""	"0"	"511.63"	"1"	"4.77"	"16"	"Cc1cc(-c2cccc3nc(Nc4ccc(N5CCN(C)CC5)cc4)oc23)ccc1C(=O)N1CCOCC1"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	""	"UO_0000065"	"15.83"	"0.29"	"3.33"	"10.93"	"False"	"CHEMBL1102770"	"Inhibition of GST-tagged JAK2 assessed as inhibition of biotinylated JAK3tide peptide phosphorylation after 60 mins by caliper mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154949"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL583895"	""	"0"	"349.37"	"0"	"3.08"	"40"	"C[C@@H](Nc1cc(-c2c(N)nn3cccnc23)ncn1)c1ccc(F)cc1"	"IC50"	"'='"	"0.2"	"nM"	"9.70"	""	""	"UO_0000065"	"27.76"	"0.51"	"6.62"	"10.32"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL570229"	""	"0"	"343.39"	"0"	"2.87"	"42"	"Nc1nn2cccnc2c1-c1cc(N[C@@H]2CCc3ccccc32)ncn1"	"IC50"	"'='"	"19000.0"	"nM"	"4.72"	""	""	"UO_0000065"	"13.75"	"0.25"	"1.85"	"5.02"	"False"	"CHEMBL1044320"	"Inhibition of JAK2-mediated STAT5 phosphorylation in GMCSF-stimulated human TF1 cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"CHEMBL3307972"	""
"CHEMBL1835144"	""	"0"	"430.43"	"0"	"4.21"	"55"	"CC(C)[C@@H](Nc1ncc(C(N)=O)c2[nH]c3cc(-c4cnn(C)c4)ccc3c12)C(F)(F)F"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1840130"	"Inhibition of JAK2-mediated STAT5 phosphorylation in human HEL 92.1.7 irf1-bla cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308090"	""
"CHEMBL1835149"	""	"0"	"414.39"	"0"	"3.96"	"61"	"NC(=O)c1cnc(N[C@H](C2CC2)C(F)(F)F)c2c1[nH]c1cc(-c3cn[nH]c3)ccc12"	"IC50"	"'='"	"32.0"	"nM"	"7.50"	""	""	"UO_0000065"	"18.09"	"0.34"	"3.53"	"6.66"	"False"	"CHEMBL1840130"	"Inhibition of JAK2-mediated STAT5 phosphorylation in human HEL 92.1.7 irf1-bla cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308090"	""
"CHEMBL1833986"	""	"0"	"413.49"	"0"	"3.45"	"60"	"NC(=O)c1cnc(NC(C2CC2)C2CC2)c2c1[nH]c1cc(-c3cnc(N)nc3)ccc12"	"IC50"	"'='"	"29.0"	"nM"	"7.54"	""	""	"UO_0000065"	"18.23"	"0.33"	"4.09"	"5.56"	"False"	"CHEMBL1840130"	"Inhibition of JAK2-mediated STAT5 phosphorylation in human HEL 92.1.7 irf1-bla cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308090"	""
"CHEMBL1835148"	""	"0"	"413.49"	"0"	"3.45"	"59"	"NC(=O)c1cnc(NC(C2CC2)C2CC2)c2c1[nH]c1cc(-c3cnc(N)cn3)ccc12"	"IC50"	"'='"	"100.0"	"nM"	"7.00"	""	""	"UO_0000065"	"16.93"	"0.31"	"3.55"	"5.16"	"False"	"CHEMBL1840130"	"Inhibition of JAK2-mediated STAT5 phosphorylation in human HEL 92.1.7 irf1-bla cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308090"	""
"CHEMBL1835143"	""	"0"	"428.42"	"0"	"3.97"	"54"	"Cn1cc(-c2ccc3c(c2)[nH]c2c(C(N)=O)cnc(N[C@@H](C4CC4)C(F)(F)F)c23)cn1"	"IC50"	"'='"	"530.0"	"nM"	"6.28"	""	""	"UO_0000065"	"14.65"	"0.28"	"2.31"	"6.18"	"False"	"CHEMBL1840130"	"Inhibition of JAK2-mediated STAT5 phosphorylation in human HEL 92.1.7 irf1-bla cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308090"	""
"CHEMBL1835141"	""	"0"	"400.49"	"0"	"3.82"	"52"	"Cn1cc(-c2ccc3c(c2)[nH]c2c(C(N)=O)cnc(NC(C4CC4)C4CC4)c23)cn1"	"IC50"	"'='"	"130.0"	"nM"	"6.89"	""	""	"UO_0000065"	"17.19"	"0.31"	"3.07"	"6.78"	"False"	"CHEMBL1840130"	"Inhibition of JAK2-mediated STAT5 phosphorylation in human HEL 92.1.7 irf1-bla cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308090"	""
"CHEMBL1078984"	""	"0"	"357.42"	"0"	"3.60"	"1"	"N#Cc1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"533.0"	"nM"	"6.27"	""	""	"UO_0000065"	"17.55"	"0.32"	"2.67"	"8.47"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1079689"	""	"0"	"347.42"	"0"	"3.31"	"4"	"Nc1cccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)c1"	"IC50"	"'='"	"322.0"	"nM"	"6.49"	""	""	"UO_0000065"	"18.69"	"0.34"	"3.18"	"8.51"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1080954"	""	"0"	"411.49"	"0"	"2.37"	"7"	"NS(=O)(=O)c1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"83.0"	"nM"	"7.08"	""	""	"UO_0000065"	"17.21"	"0.33"	"4.71"	"6.41"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1078767"	""	"0"	"453.57"	"0"	"3.22"	"18"	"CS(=O)(=O)Nc1ccc(-c2ccnc(Nc3ccc(CN4CCC(O)CC4)cc3)n2)cc1"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	""	"UO_0000065"	"17.19"	"0.33"	"4.58"	"7.26"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1078971"	""	"0"	"452.58"	"0"	"3.01"	"20"	"CN1CCN(Cc2ccc(Nc3nccc(-c4ccc(NS(C)(=O)=O)cc4)n3)cc2)CC1"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	""	"UO_0000065"	"17.11"	"0.33"	"4.73"	"8.56"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1078370"	""	"0"	"428.50"	"0"	"3.32"	"32"	"CN(CC#N)C(=O)c1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"298.0"	"nM"	"6.53"	""	""	"UO_0000065"	"15.23"	"0.28"	"3.21"	"6.91"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1078721"	""	"0"	"428.50"	"0"	"2.97"	"37"	"N#CCNC(=O)c1ccc(-c2ccnc(Nc3ccc(CN4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"163.0"	"nM"	"6.79"	""	""	"UO_0000065"	"15.84"	"0.29"	"3.82"	"6.58"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1835137"	""	"0"	"374.45"	"0"	"3.43"	"48"	"C[C@H](Nc1ncc(C(N)=O)c2[nH]c3cc(-c4cnn(C)c4)ccc3c12)C1CC1"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	""	"UO_0000065"	"20.97"	"0.38"	"4.42"	"7.73"	"False"	"CHEMBL1840130"	"Inhibition of JAK2-mediated STAT5 phosphorylation in human HEL 92.1.7 irf1-bla cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308090"	""
"CHEMBL1834949"	""	"0"	"278.29"	"0"	"3.61"	"2"	"O=c1[nH]ccc2c1c1cc(F)ccc1n2-c1ccccc1"	"IC50"	"'='"	"1100.0"	"nM"	"5.96"	""	""	"UO_0000065"	"21.41"	"0.39"	"2.35"	"15.77"	"False"	"CHEMBL1840115"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1081443"	""	"0"	"377.40"	"0"	"4.66"	"2"	"COc1cc(Nc2nc3cccc(-c4ccccn4)c3o2)cc(OC)c1OC"	"IC50"	"'='"	"110.0"	"nM"	"6.96"	""	""	"UO_0000065"	"18.44"	"0.34"	"2.30"	"8.85"	"False"	"CHEMBL1102770"	"Inhibition of GST-tagged JAK2 assessed as inhibition of biotinylated JAK3tide peptide phosphorylation after 60 mins by caliper mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154949"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL460702"	"BMS-777607"	"2"	"512.90"	"2"	"5.19"	"10, BMS-777607"	"CCOc1ccn(-c2ccc(F)cc2)c(=O)c1C(=O)Nc1ccc(Oc2ccnc(N)c2Cl)c(F)c1"	"IC50"	"'>'"	"2000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL957083"	"Inhibition of Jak2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1140952"	"1"	"Scientific Literature"	"J. Med. Chem."	"2009"	"None"	""
"CHEMBL1290650"	""	"0"	"323.30"	"0"	"4.10"	"30"	"O=c1[nH]ccc2nc(Nc3cccc(F)c3)c3ccc(F)cc3c12"	"IC50"	"'='"	"4100.0"	"nM"	"5.39"	""	""	"UO_0000065"	"16.66"	"0.31"	"1.29"	"9.32"	"False"	"CHEMBL1291235"	"Inhibition of JAK2 in cell-free system"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287746"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL4789894"	""	"0"	"320.36"	"0"	"2.75"	"1"	"C=CC(=O)Nc1cccc(-c2cc(Nc3cnn(C)c3)ncn2)c1"	"IC50"	"'='"	"2237.0"	"nM"	"5.65"	""	""	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL4777645"	""	"0"	"377.41"	"0"	"1.95"	"5"	"C=CC(=O)Nc1cccc(-c2cc(Nc3cnn(CC(=O)NC)c3)ncn2)c1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL4778584"	""	"0"	"350.38"	"0"	"2.20"	"6"	"C=CC(=O)Nc1cccc(-c2cc(Nc3cnn(CCO)c3)ncn2)c1"	"IC50"	"'='"	"2588.0"	"nM"	"5.59"	""	""	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL4753620"	""	"0"	"333.36"	"0"	"2.47"	"14"	"Cn1cc(Nc2cc(-c3cccc(NC(=O)CC#N)c3)ncn2)cn1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL4778274"	""	"0"	"414.47"	"0"	"3.58"	"18"	"N#CCC(=O)Nc1cccc(-c2cc(Nc3ccc(N4CCOCC4)cc3)ncn2)c1"	"IC50"	"'='"	"734.0"	"nM"	"6.13"	""	""	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL4793519"	""	"0"	"364.41"	"0"	"2.85"	"2"	"C=CC(=O)Nc1cccc(-c2cc(Nc3cnn(CCOC)c3)ncn2)c1"	"IC50"	"'='"	"2852.0"	"nM"	"5.54"	""	""	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL4780984"	""	"0"	"364.41"	"0"	"2.85"	"11"	"C=CC(=O)Nc1ccc(-c2ccnc(Nc3cnn(CCOC)c3)n2)cc1"	"IC50"	"'='"	"1079.0"	"nM"	"5.97"	""	""	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL4754061"	""	"0"	"391.44"	"0"	"2.34"	"20"	"C/C=C/C(=O)Nc1cccc(-c2cc(Nc3cnn(CC(=O)NC)c3)ncn2)c1"	"IC50"	"'='"	"1109.0"	"nM"	"5.96"	""	""	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL1077575"	""	"0"	"414.47"	"0"	"3.58"	"31"	"N#CCC(=O)Nc1cccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)c1"	"IC50"	"'='"	"216.0"	"nM"	"6.67"	""	""	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL1938643"	""	"0"	"368.46"	"0"	"2.74"	"8"	"CNC(=O)c1cnc(N)c2cc(-c3ccc(N4CCOCC4)cc3)sc12"	"IC50"	"'='"	"31.0"	"nM"	"7.51"	""	""	"UO_0000065"	"20.38"	"0.39"	"4.77"	"9.33"	"False"	"CHEMBL1941383"	"Inhibition of human recombinant N-terminal GST-tagged JAK2 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308860"	""
"CHEMBL1938646"	""	"0"	"444.56"	"0"	"4.31"	"11"	"Nc1ncc(C(=O)NCc2ccccc2)c2sc(-c3ccc(N4CCOCC4)cc3)cc12"	"IC50"	"'='"	"100.0"	"nM"	"7.00"	""	""	"UO_0000065"	"15.75"	"0.30"	"2.69"	"8.70"	"False"	"CHEMBL1941383"	"Inhibition of human recombinant N-terminal GST-tagged JAK2 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308860"	""
"CHEMBL1938654"	""	"0"	"418.54"	"0"	"2.98"	"19"	"CNC(=O)c1cnc(N)c2cc(-c3ccc(S(=O)(=O)NC(C)(C)C)cc3)sc12"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	""	"UO_0000065"	"21.50"	"0.44"	"6.02"	"7.88"	"False"	"CHEMBL1941383"	"Inhibition of human recombinant N-terminal GST-tagged JAK2 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308860"	""
"CHEMBL1945052"	""	"0"	"456.47"	"1"	"5.56"	"27c"	"CN1C/C=C/CCOc2cccc(c2)-c2ccnc(n2)Nc2ccc(OC(F)(F)F)c(c2)C1"	"IC50"	"'='"	"150.0"	"nM"	"6.82"	""	""	"UO_0000065"	"14.95"	"0.28"	"1.26"	"11.47"	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL569721"	""	"0"	"353.37"	"0"	"2.53"	"7d"	"Cc1cc(Nc2nc(N[C@H](C)c3ncc(F)cn3)c(C#N)nc2C)n[nH]1"	"IC50"	"'='"	"10420.0"	"nM"	"4.98"	""	""	"UO_0000065"	"14.10"	"0.26"	"2.45"	"3.89"	"False"	"CHEMBL1043452"	"Inhibition of JAK2 using 5 mM ATP as a substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156131"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL569966"	""	"0"	"363.40"	"0"	"3.47"	"44"	"CC[C@@H](Nc1cc(-c2c(N)nn3cccnc23)ncn1)c1ccc(F)cc1"	"IC50"	"'='"	"0.6"	"nM"	"9.22"	""	""	"UO_0000065"	"25.38"	"0.47"	"5.75"	"9.81"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL4758753"	""	"0"	"388.44"	"0"	"2.41"	"18, trans isomer"	"CO[C@H]1C[C@](CC#N)(n2cc(-c3nc(-c4cnn(C)c4)cn4nccc34)cn2)C1"	"IC50"	"'='"	"228.0"	"nM"	"6.64"	""	""	""	""	""	""	""	"False"	"CHEMBL4675813"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using FITC-KGGEEEEYFELVKK as substrate in presence of ATP at Km by microfluidic assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4673239"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4740088"	""	"0"	"387.45"	"0"	"1.94"	"12"	"CCN1CC(CC#N)(n2cc(-c3nc(-c4cnn(C)c4)cn4nccc34)cn2)C1"	"IC50"	"'='"	"346.0"	"nM"	"6.46"	""	""	""	""	""	""	""	"False"	"CHEMBL4675813"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using FITC-KGGEEEEYFELVKK as substrate in presence of ATP at Km by microfluidic assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4673239"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL1230607"	"PHA-793887"	"1"	"361.49"	"0"	"2.31"	"31"	"CC(C)CC(=O)Nc1n[nH]c2c1CN(C(=O)C1CCN(C)CC1)C2(C)C"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1064437"	"Inhibition of JAK2 by scintillation proximity assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1157586"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2010"	"None"	""
"CHEMBL604712"	""	"0"	"376.41"	"0"	"3.56"	"1"	"CC(C)(C)C(=O)N1Cc2c(NC(=O)c3cc(F)cc(F)c3)n[nH]c2C1(C)C"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1064437"	"Inhibition of JAK2 by scintillation proximity assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1157586"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2010"	"None"	""
"CHEMBL570002"	""	"0"	"339.34"	"0"	"2.23"	"7a"	"Cc1cc(Nc2cnc(C#N)c(N[C@@H](C)c3ncc(F)cn3)n2)n[nH]1"	"IC50"	"'<'"	"3.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1043451"	"Inhibition of JAK2 using 2 mM ATP as a substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156131"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL569720"	""	"0"	"353.37"	"0"	"2.53"	"7c"	"Cc1cc(Nc2nc(N[C@@H](C)c3ncc(F)cn3)c(C#N)nc2C)n[nH]1"	"IC50"	"'='"	"87.0"	"nM"	"7.06"	""	""	"UO_0000065"	"19.98"	"0.37"	"4.53"	"5.51"	"False"	"CHEMBL1043452"	"Inhibition of JAK2 using 5 mM ATP as a substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156131"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL578201"	""	"0"	"352.38"	"0"	"3.14"	"7e"	"Cc1cc(Nc2nc(N[C@@H](C)c3ccc(F)cn3)c(C#N)nc2C)n[nH]1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	""	"UO_0000065"	"22.59"	"0.42"	"4.82"	"6.91"	"False"	"CHEMBL1043452"	"Inhibition of JAK2 using 5 mM ATP as a substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156131"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL568790"	""	"0"	"269.31"	"0"	"1.59"	"9"	"CC(C)Nc1cc(-c2c(N)nn3cccnc23)ncn1"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	""	"UO_0000065"	"28.59"	"0.53"	"6.11"	"8.19"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL577944"	""	"0"	"338.38"	"0"	"0.47"	"11"	"NC(=O)C1CCCN(c2cc(-c3c(N)nn4cccnc34)ncn2)C1"	"IC50"	"'='"	"84.0"	"nM"	"7.08"	""	""	"UO_0000065"	"20.91"	"0.39"	"6.61"	"5.51"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL569948"	""	"0"	"311.39"	"0"	"2.39"	"18"	"CCCN(CCC)c1cc(-c2c(N)nn3cccnc23)ncn1"	"IC50"	"'='"	"25.0"	"nM"	"7.60"	""	""	"UO_0000065"	"24.41"	"0.45"	"5.21"	"8.92"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL569092"	""	"0"	"448.45"	"0"	"2.40"	"26"	"CCN(CC(F)(F)F)C(=O)C1CCCN(c2cc(-c3c(N)nn4cccnc34)ncn2)C1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	""	"UO_0000065"	"18.73"	"0.36"	"6.00"	"7.96"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL570456"	""	"0"	"462.48"	"0"	"2.79"	"28"	"CCN(CCC(F)(F)F)C(=O)C1CCCN(c2cc(-c3c(N)nn4cccnc34)ncn2)C1"	"IC50"	"'='"	"4.6"	"nM"	"8.34"	""	""	"UO_0000065"	"18.03"	"0.35"	"5.55"	"7.90"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL568815"	""	"0"	"336.33"	"0"	"2.49"	"36"	"Nc1nn2cccnc2c1-c1cc(OCc2ccc(F)cc2)ncn1"	"IC50"	"'='"	"7.8"	"nM"	"8.11"	""	""	"UO_0000065"	"24.11"	"0.44"	"5.62"	"8.89"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL4756422"	""	"0"	"459.60"	"0"	"3.98"	"13am"	"Cc1cnc(Nc2ccc3c(c2)CN(C(=O)/C=C/CN(C)C)CC3)nc1-c1cnn(C(C)C)c1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	""	""	"17.51"	"0.32"	"4.07"	"10.16"	"False"	"CHEMBL4723820"	"Inhibition of recombinant human JAK2 (808 to end residues) KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate measured after 40 mins in presence of [gamm33P]ATP by scintillation counting method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 0.6667 hr"
"CHEMBL4748354"	""	"0"	"506.61"	"2"	"5.30"	"13z"	"Cc1cnc(Nc2ccc3c(c2)CCN(C(=O)/C=C/C(=O)c2ccccc2)C3)nc1-c1cnn(C(C)C)c1"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	""	""	"15.79"	"0.29"	"2.70"	"8.60"	"False"	"CHEMBL4723820"	"Inhibition of recombinant human JAK2 (808 to end residues) KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate measured after 40 mins in presence of [gamm33P]ATP by scintillation counting method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 0.6667 hr"
"CHEMBL4798378"	""	"0"	"387.49"	"0"	"3.85"	"13t"	"Cc1cnc(Nc2ccc3c(c2)CCN(CC#N)C3)nc1-c1cnn(C(C)C)c1"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	""	""	"21.05"	"0.38"	"4.30"	"9.87"	"False"	"CHEMBL4723820"	"Inhibition of recombinant human JAK2 (808 to end residues) KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate measured after 40 mins in presence of [gamm33P]ATP by scintillation counting method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 0.6667 hr"
"CHEMBL4778029"	""	"0"	"419.53"	"0"	"4.06"	"13h"	"CCNC(=O)N1CCc2cc(Nc3ncc(C)c(-c4cnn(C(C)C)c4)n3)ccc2C1"	"IC50"	"'='"	"2350.0"	"nM"	"5.63"	""	""	""	"13.42"	"0.25"	"1.57"	"6.40"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL4754686"	""	"0"	"420.56"	"0"	"4.10"	"13o"	"Cc1cnc(Nc2ccc3c(c2)CCN(CCCCO)C3)nc1-c1cnn(C(C)C)c1"	"IC50"	"'='"	"268.0"	"nM"	"6.57"	""	""	""	"15.63"	"0.29"	"2.47"	"8.31"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL4739994"	""	"0"	"404.56"	"1"	"5.13"	"13r"	"CCCCN1CCc2cc(Nc3ncc(C)c(-c4cnn(C(C)C)c4)n3)ccc2C1"	"IC50"	"'='"	"592.0"	"nM"	"6.23"	""	""	""	"15.39"	"0.28"	"1.10"	"10.58"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL4798378"	""	"0"	"387.49"	"0"	"3.85"	"13t"	"Cc1cnc(Nc2ccc3c(c2)CCN(CC#N)C3)nc1-c1cnn(C(C)C)c1"	"IC50"	"'='"	"73.2"	"nM"	"7.13"	""	""	""	"18.41"	"0.34"	"3.29"	"8.63"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL4795467"	""	"0"	"386.50"	"0"	"3.96"	"13v"	"C#CCN1CCc2cc(Nc3ncc(C)c(-c4cnn(C(C)C)c4)n3)ccc2C1"	"IC50"	"'='"	"382.0"	"nM"	"6.42"	""	""	""	"16.61"	"0.30"	"2.46"	"10.90"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL4759953"	""	"0"	"520.64"	"2"	"5.61"	"13aa"	"Cc1ccc(C(=O)/C=C/C(=O)N2CCc3cc(Nc4ncc(C)c(-c5cnn(C(C)C)c5)n4)ccc3C2)cc1"	"IC50"	"'='"	"14.7"	"nM"	"7.83"	""	""	""	"15.04"	"0.27"	"2.22"	"8.42"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL1835034"	""	"0"	"384.48"	"1"	"5.23"	"37"	"NC(=O)c1cnc(NC2CCCCC2)c2c1[nH]c1ccc(-c3ccccc3)cc12"	"IC50"	"'='"	"180.0"	"nM"	"6.75"	""	""	"UO_0000065"	"17.54"	"0.32"	"1.51"	"8.05"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835041"	""	"0"	"402.50"	"0"	"4.31"	"44"	"C[C@H](Nc1ccc(C(N)=O)c2[nH]c3cc(-c4cnc(N)nc4)ccc3c12)C(C)(C)C"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	""	"UO_0000065"	"19.68"	"0.36"	"3.61"	"6.45"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL557844"	""	"0"	"386.84"	"0"	"2.92"	"35"	"COC[C@H](C)Nc1cc(-c2ccoc2)nc(-n2cnc3ccncc32)n1.Cl"	"IC50"	"'='"	"141.0"	"nM"	"6.85"	""	""	"UO_0000065"	"19.55"	"0.36"	"3.93"	"7.54"	"False"	"CHEMBL908418"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139695"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2006"	"None"	""
"CHEMBL375205"	""	"0"	"406.45"	"1"	"5.12"	"33"	"C[C@H](Nc1cc(-c2ccoc2)nc(-n2cnc3ccc(C#N)cc32)n1)c1ccccc1"	"IC50"	"'='"	"29.0"	"nM"	"7.54"	""	""	"UO_0000065"	"18.54"	"0.33"	"2.42"	"8.14"	"False"	"CHEMBL908418"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139695"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2006"	"None"	""
"CHEMBL218439"	""	"0"	"421.89"	"0"	"3.41"	"20"	"CN1CCN(c2cc(Oc3ccccc3Cl)nc(-n3cnc4ccncc43)n2)CC1"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	""	"UO_0000065"	"18.42"	"0.35"	"4.36"	"10.76"	"False"	"CHEMBL908418"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139695"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2006"	"None"	""
"CHEMBL375076"	""	"0"	"316.37"	"0"	"3.38"	"8"	"C[C@@H](Nc1nccc(-n2cnc3ccncc32)n1)c1ccccc1"	"IC50"	"'='"	"49.0"	"nM"	"7.31"	""	""	"UO_0000065"	"23.11"	"0.42"	"3.93"	"10.67"	"False"	"CHEMBL908418"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139695"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2006"	"None"	""
"CHEMBL220585"	""	"0"	"316.37"	"0"	"3.38"	"5"	"C[C@H](Nc1ccnc(-n2cnc3cnccc32)n1)c1ccccc1"	"IC50"	"'='"	"51.0"	"nM"	"7.29"	""	""	"UO_0000065"	"23.05"	"0.41"	"3.91"	"10.64"	"False"	"CHEMBL908418"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139695"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2006"	"None"	""
"CHEMBL221038"	""	"0"	"342.41"	"0"	"3.70"	"14"	"c1ccc2c(c1)CCC[C@@H]2Nc1ccnc(-n2cnc3ccncc32)n1"	"IC50"	"'='"	"7218.0"	"nM"	"5.14"	""	""	"UO_0000065"	"15.02"	"0.27"	"1.44"	"7.50"	"False"	"CHEMBL908418"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139695"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2006"	"None"	""
"CHEMBL1835146"	""	"0"	"386.46"	"0"	"3.81"	"57"	"NC(=O)c1cnc(NC(C2CC2)C2CC2)c2c1[nH]c1cc(-c3cn[nH]c3)ccc12"	"IC50"	"'='"	"40.0"	"nM"	"7.40"	""	""	"UO_0000065"	"19.14"	"0.35"	"3.59"	"6.58"	"False"	"CHEMBL1840130"	"Inhibition of JAK2-mediated STAT5 phosphorylation in human HEL 92.1.7 irf1-bla cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308090"	""
"CHEMBL4742766"	""	"0"	"411.48"	"0"	"2.96"	"32b"	"CNC(=O)c1cnc2[nH]ccc2c1N[C@@H]1CCN(Cc2cccc(OC)c2)C[C@H]1F"	"IC50"	"'='"	"319.0"	"nM"	"6.50"	""	""	""	"15.79"	"0.30"	"3.54"	"7.90"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL21156"	""	"0"	"309.34"	"0"	"3.99"	"1"	"CC(C)(C)c1nc2c3ccc(F)cc3c3c(=O)[nH]ccc3c2[nH]1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	""	"UO_0000065"	"29.09"	"0.53"	"5.01"	"14.62"	"True"	"CHEMBL987116"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1142524"	"1"	"Scientific Literature"	"J. Med. Chem."	"2008"	"None"	""
"CHEMBL1835143"	""	"0"	"428.42"	"0"	"3.97"	"54"	"Cn1cc(-c2ccc3c(c2)[nH]c2c(C(N)=O)cnc(N[C@@H](C4CC4)C(F)(F)F)c23)cn1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	""	"UO_0000065"	"18.78"	"0.35"	"4.08"	"7.92"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835153"	""	"0"	"441.42"	"0"	"3.61"	"65"	"NC(=O)c1cnc(N[C@H](C2CC2)C(F)(F)F)c2c1[nH]c1cc(-c3cnc(N)nc3)ccc12"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	""	"UO_0000065"	"18.03"	"0.34"	"4.35"	"5.87"	"False"	"CHEMBL1840112"	"Inhibition of JAK2 V617F mutant-mediated STAT5 phosphorylation in mouse BAF3 cells"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3307634"	""
"CHEMBL1835029"	""	"0"	"354.43"	"0"	"4.11"	"32"	"CCN(c1ncc(C(N)=O)c2[nH]c3ccc(F)cc3c12)C1CCCCC1"	"IC50"	"'='"	"2700.0"	"nM"	"5.57"	""	""	"UO_0000065"	"15.71"	"0.29"	"1.46"	"7.42"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL461139"	""	"0"	"413.48"	"0"	"3.32"	"16"	"O=c1[nH]cnc2[nH]c(-c3ccnc(/C=C/c4ccc(CN5CCOCC5)cc4)c3)cc12"	"IC50"	"'='"	"1300.0"	"nM"	"5.89"	""	""	"UO_0000065"	"14.24"	"0.26"	"2.57"	"6.77"	"False"	"CHEMBL955790"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1152141"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2008"	"None"	""
"CHEMBL406845"	""	"0"	"301.78"	"0"	"3.48"	"K00048, AG-1879"	"CC(C)(C)n1nc(-c2ccc(Cl)cc2)c2c(N)ncnc21"	"IC50"	"'>'"	"50000000.0"	"nM"	""	"Outside typical range"	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL937065"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1145498"	"1"	"Scientific Literature"	"Proc. Natl. Acad. Sci. U.S.A."	"2007"	"None"	""
"CHEMBL405130"	"WHI-P131"	"1"	"297.31"	"0"	"3.10"	"WHI-P131"	"COc1cc2ncnc(Nc3ccc(O)cc3)c2cc1OC"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1016953"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1152817"	"1"	"Scientific Literature"	"Science"	"2003"	"None"	""
"CHEMBL1288001"	""	"0"	"358.35"	"0"	"2.64"	"19"	"CN(C)c1cccc(Nc2nc(N)n(C(=O)c3c(F)cccc3F)n2)c1"	"IC50"	"'='"	"5000.0"	"nM"	"5.30"	""	""	"UO_0000065"	"14.79"	"0.28"	"2.66"	"5.95"	"False"	"CHEMBL1292866"	"Inhibition of human recombinant JAK2 by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287810"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1287812"	""	"0"	"387.35"	"0"	"2.75"	"12"	"CCOC(=O)c1cccc(Nc2nc(N)n(C(=O)c3c(F)cccc3F)n2)c1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1292866"	"Inhibition of human recombinant JAK2 by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287810"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1934350"	""	"0"	"545.67"	"1"	"3.08"	"3p"	"CS(=O)(=O)N1Cc2cccc(-c3ccc4cnc(Nc5ccc(C6CCN(CC(N)=O)CC6)cc5)nn34)c2C1"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	""	"UO_0000065"	"14.29"	"0.27"	"4.72"	"6.19"	"False"	"CHEMBL1936085"	"Inhibition of human recombinant JAK2 expressed in baculovirus expression system after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL1945049"	""	"0"	"457.58"	"0"	"4.55"	"26r"	"CC(C)NCC(=O)N1C/C=C/CCOc2cccc(c2)-c2ccnc(n2)Nc2cccc(c2)C1"	"IC50"	"'='"	"120.0"	"nM"	"6.92"	""	""	"UO_0000065"	"15.12"	"0.28"	"2.37"	"8.72"	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL221376"	""	"0"	"396.46"	"0"	"3.78"	"29"	"C[C@H](Nc1cc(-c2cnn(C)c2)nc(-n2cnc3ccncc32)n1)c1ccccc1"	"IC50"	"'='"	"77.0"	"nM"	"7.11"	""	""	"UO_0000065"	"17.94"	"0.32"	"3.33"	"8.24"	"False"	"CHEMBL908418"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139695"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2006"	"None"	""
"CHEMBL220483"	""	"0"	"452.52"	"1"	"5.07"	"28"	"COc1ccc(-c2cc(N[C@@H](C)c3ccccc3)nc(-n3cnc4ccncc43)n2)cc1OC"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	""	"UO_0000065"	"17.50"	"0.32"	"2.85"	"9.11"	"False"	"CHEMBL908418"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139695"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2006"	"None"	""
"CHEMBL222028"	""	"0"	"315.38"	"0"	"3.99"	"15"	"C[C@H](Nc1ccnc(-n2ccc3ccncc32)n1)c1ccccc1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL908418"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139695"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2006"	"None"	""
"CHEMBL220484"	""	"0"	"350.38"	"0"	"2.92"	"32"	"COC[C@H](C)Nc1cc(-c2ccoc2)nc(-n2cnc3ccncc32)n1"	"IC50"	"'='"	"446.0"	"nM"	"6.35"	""	""	"UO_0000065"	"18.13"	"0.33"	"3.43"	"6.99"	"False"	"CHEMBL908418"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139695"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2006"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"1"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"1.6"	"nM"	"8.80"	""	""	"UO_0000065"	"28.16"	"0.52"	"7.26"	"9.89"	"False"	"CHEMBL1641122"	"Inhibition of JAK2 by solution phase kinase assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1629452"	"1"	"Scientific Literature"	"J. Med. Chem."	"2010"	"None"	""
"CHEMBL319556"	""	"0"	"488.37"	"1"	"6.77"	"14b"	"O=C1NCc2c(-c3ccc(F)cc3F)cc(C3CCNCC3)cc2N1c1c(Cl)cccc1Cl"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL704111"	"Inhibition of Janus kinase 2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1136271"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2003"	"None"	""
"CHEMBL1088423"	""	"0"	"404.35"	"0"	"2.83"	"5c"	"O=c1[nH]c2cnc(-n3cnc4ccc(C(F)(F)F)cc43)nc2n1C1CCOCC1"	"IC50"	"'='"	"560.0"	"nM"	"6.25"	""	""	"UO_0000065"	"15.46"	"0.29"	"3.42"	"6.90"	"False"	"CHEMBL1102456"	"Inhibition of human JAK2 (532-1132) by time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154364"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1080111"	""	"0"	"402.39"	"0"	"2.97"	"21f"	"O=c1[nH]c2cnc(-n3cnc4ccccc43)nc2n1C1CCOc2c(F)cccc21"	"IC50"	"'='"	"285.0"	"nM"	"6.54"	""	""	"UO_0000065"	"16.27"	"0.30"	"3.58"	"7.22"	"False"	"CHEMBL1102456"	"Inhibition of human JAK2 (532-1132) by time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154364"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"Xelianz"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"77.0"	"nM"	"7.11"	""	""	"UO_0000065"	"22.77"	"0.42"	"5.57"	"8.00"	"True"	"CHEMBL3803216"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797141"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2016"	"None"	""
"CHEMBL3909103"	""	"0"	"434.54"	"0"	"3.54"	"BDBM229266"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)C2CCCCC2)CC1"	"IC50"	"'='"	"44.0"	"nM"	"7.36"	""	"401005"	"UO_0000065"	"16.93"	"0.31"	"3.82"	"6.29"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4108859"	""	"0"	"443.51"	"0"	"3.50"	"BDBM229360"	"Cc1cc(C)cc(NC(=O)N2CC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)C2)c1"	"IC50"	"'='"	"326.0"	"nM"	"6.49"	""	"401099"	"UO_0000065"	"14.63"	"0.27"	"2.99"	"5.03"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4107428"	""	"0"	"457.49"	"0"	"3.08"	"BDBM229372"	"CC(=O)c1cccc(NC(=O)N2CC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)C2)c1"	"IC50"	"'='"	"86.0"	"nM"	"7.07"	""	"401111"	"UO_0000065"	"15.44"	"0.28"	"3.99"	"4.83"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3951300"	""	"0"	"467.94"	"0"	"4.58"	"BDBM229401"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(Nc2ccccc2Cl)CC1"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"401140"	"UO_0000065"	"17.43"	"0.34"	"3.57"	"6.70"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3960177"	""	"0"	"459.53"	"0"	"3.87"	"BDBM229415"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(N2CCc3ccccc32)CC1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"401159"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3909143"	""	"0"	"439.54"	"0"	"3.73"	"BDBM228228"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(NC2CCCCC2)CC1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"401180"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3896010"	""	"0"	"450.49"	"0"	"4.67"	"BDBM228237"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(Nc2ccccc2F)CC1"	"IC50"	"'='"	"758.0"	"nM"	"6.12"	""	"401189"	"UO_0000065"	"13.59"	"0.25"	"1.45"	"5.63"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3923655"	""	"0"	"438.43"	"0"	"3.57"	"BDBM229468"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(NCC(F)(F)F)CC1"	"IC50"	"'='"	"31.0"	"nM"	"7.51"	""	"401226"	"UO_0000065"	"17.13"	"0.33"	"3.94"	"6.90"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3935618"	""	"0"	"436.50"	"0"	"2.67"	"BDBM237832"	"CCn1ccnc1CN1CC[C@@H](C#N)[C@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)C1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	"414936"	"UO_0000065"	"18.23"	"0.34"	"5.29"	"6.76"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4114100"	""	"0"	"409.43"	"0"	"2.44"	"BDBM237842"	"N#C[C@@H]1CN(Cc2ncco2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"47.0"	"nM"	"7.33"	""	"414946"	"UO_0000065"	"17.90"	"0.33"	"4.89"	"5.82"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3903353"	""	"0"	"356.43"	"0"	"3.16"	"BDBM198252"	"CC(C)(C)OC(=O)N[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"180.0"	"nM"	"6.75"	""	"352334"	"UO_0000065"	"18.92"	"0.35"	"3.58"	"6.94"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3954894"	""	"0"	"289.77"	"0"	"3.12"	"BDBM198268"	"ClC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"352348"	"UO_0000065"	"31.06"	"0.61"	"5.88"	"15.29"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3978777"	""	"0"	"361.45"	"0"	"2.86"	"BDBM198315"	"c1cc(CCNC2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)ccn1"	"IC50"	"'='"	"470.0"	"nM"	"6.33"	""	"352393"	"UO_0000065"	"17.51"	"0.32"	"3.47"	"7.55"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3913397"	""	"0"	"371.45"	"0"	"3.92"	"BDBM198325"	"Cc1cc(C#N)ccc1NC1CCC(c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"34.0"	"nM"	"7.47"	""	"352403"	"UO_0000065"	"20.11"	"0.36"	"3.55"	"7.89"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3945964"	""	"0"	"350.40"	"0"	"3.12"	"BDBM198341"	"Fc1ccccc1CN1CCC(c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	"352419"	"UO_0000065"	"22.41"	"0.41"	"4.73"	"12.65"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3923513"	""	"0"	"448.27"	"0"	"3.18"	"BDBM198346"	"Ic1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)o1"	"IC50"	"'='"	"4.9"	"nM"	"8.31"	""	"352424"	"UO_0000065"	"18.54"	"0.45"	"5.13"	"11.04"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3951230"	""	"0"	"338.44"	"0"	"3.05"	"BDBM198347"	"c1csc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)c1"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	"352425"	"UO_0000065"	"23.64"	"0.46"	"4.95"	"12.88"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3979340"	""	"0"	"401.27"	"0"	"3.34"	"BDBM198348"	"Brc1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)o1"	"IC50"	"'='"	"2.8"	"nM"	"8.55"	""	"352426"	"UO_0000065"	"21.31"	"0.47"	"5.21"	"11.37"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3926817"	""	"0"	"408.94"	"0"	"4.37"	"BDBM198377"	"Clc1ccc(CCNC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"24.0"	"nM"	"7.62"	""	"352455"	"UO_0000065"	"18.63"	"0.36"	"3.25"	"10.75"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3973302"	""	"0"	"376.47"	"0"	"2.77"	"BDBM198382"	"Cc1cnc(CNC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cn1"	"IC50"	"'='"	"55.0"	"nM"	"7.26"	""	"352460"	"UO_0000065"	"19.28"	"0.35"	"4.49"	"7.51"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4064018"	""	"0"	"297.36"	"0"	"1.57"	"7"	"C=CC(=O)N1CC[C@H]2CCN(c3ncnc4[nH]ccc34)[C@H]2C1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4005719"	"Inhibition of recombinant human GST-tagged cytoplasmic JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by microfluidic assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4004825"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL3948605"	""	"0"	"240.31"	"0"	"3.26"	"BDBM198194"	"c1cc2c(ncn3cnc(C4CCCCC4)c23)[nH]1"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	"351816"	"UO_0000065"	"32.33"	"0.59"	"4.51"	"16.90"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3936356"	""	"0"	"255.32"	"0"	"2.90"	"BDBM198199"	"CC1CCCCC1c1nnn2cnc3[nH]ccc3c12"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	"351821"	"UO_0000065"	"31.02"	"0.57"	"5.02"	"13.45"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL1290767"	""	"0"	"374.20"	"1"	"5.27"	"32"	"O=c1[nH]ccc2nc(Nc3c(Cl)cccc3Cl)c3ccc(F)cc3c12"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	""	"UO_0000065"	"20.99"	"0.43"	"2.58"	"13.59"	"False"	"CHEMBL1291235"	"Inhibition of JAK2 in cell-free system"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287746"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1290768"	""	"0"	"365.45"	"0"	"4.84"	"33"	"CC1(C)C2CCCC1(C)[C@@H]2Nc1nc2cc[nH]c(=O)c2c2cc(F)ccc12"	"IC50"	"'='"	"200.0"	"nM"	"6.70"	""	""	"UO_0000065"	"18.33"	"0.34"	"1.86"	"11.59"	"False"	"CHEMBL1291235"	"Inhibition of JAK2 in cell-free system"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287746"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1289217"	""	"0"	"315.35"	"0"	"2.65"	"40"	"CC(C)(CO)CNc1nc2cc[nH]c(=O)c2c2cc(F)ccc12"	"IC50"	"'='"	"274.0"	"nM"	"6.56"	""	""	"UO_0000065"	"20.81"	"0.39"	"3.91"	"8.41"	"False"	"CHEMBL1291235"	"Inhibition of JAK2 in cell-free system"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287746"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL3955861"	""	"0"	"476.51"	"0"	"3.91"	"BDBM229205"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)OCc2cccc(F)c2)CC1"	"IC50"	"'='"	"88.0"	"nM"	"7.06"	""	"400942"	"UO_0000065"	"14.81"	"0.28"	"3.15"	"5.59"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3903224"	""	"0"	"494.60"	"0"	"1.81"	"BDBM229216"	"CN1CCN(CCOC(=O)N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)CC2)CC1"	"IC50"	"'='"	"318.0"	"nM"	"6.50"	""	"400953"	"UO_0000065"	"13.14"	"0.25"	"4.69"	"4.89"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3951407"	""	"0"	"444.47"	"0"	"2.35"	"BDBM228005"	"COCCOC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CC1"	"IC50"	"'='"	"71.0"	"nM"	"7.15"	""	"400958"	"UO_0000065"	"16.08"	"0.31"	"4.80"	"5.28"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4110362"	""	"0"	"451.49"	"0"	"1.41"	"BDBM229235"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CN(C(=O)OCCN2CCCC2=O)C1"	"IC50"	"'='"	"1481.0"	"nM"	"5.83"	""	"400974"	"UO_0000065"	"12.91"	"0.24"	"4.42"	"3.98"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3973093"	""	"0"	"507.58"	"1"	"2.59"	"BDBM229381"	"Cc1ccc(NC(=O)N2CC(CC#N)(n3cc(C(N)=O)c(Nc4ccc(S(C)(=O)=O)cc4)n3)C2)cc1"	"IC50"	"'='"	"175.0"	"nM"	"6.76"	""	"401120"	"UO_0000065"	"13.31"	"0.26"	"4.17"	"4.14"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3947490"	""	"0"	"473.52"	"0"	"3.04"	"BDBM229130"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2nc3ccccc3[nH]2)CC1"	"IC50"	"'='"	"641.0"	"nM"	"6.19"	""	"400866"	"UO_0000065"	"13.08"	"0.24"	"3.15"	"4.38"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3890379"	""	"0"	"414.90"	"0"	"2.56"	"BDBM239958"	"Cn1cc(Nc2ncc(Cl)c(NC3CCC4CN(C(=O)CC#N)CC4C3)n2)cn1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"418578"	"UO_0000065"	"19.82"	"0.39"	"5.66"	"7.36"	"False"	"CHEMBL3888834"	"Kinase Assay: JAK2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 100 μM KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC, 10 mM MgAcetate and [γ-33P-ATP](specific activity approx. 500 cpm/pmol, concentration as required). The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of 3% phosphoric acid solution. 10 μL of the reaction is then spotted onto a P30 filtermat and washed three times for 5 minutes in 75 mM phosphoric acid and once in methanol prior to drying and scintillation counting."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886854"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3953702"	""	"0"	"471.92"	"0"	"4.13"	"BDBM239965"	"Cn1cc(Nc2ncc(Cl)c(NC3CCC4(CC3)CCN(C(=O)C(F)(F)F)CC4)n2)cn1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"418585"	"UO_0000065"	"17.59"	"0.35"	"4.17"	"9.44"	"False"	"CHEMBL3888834"	"Kinase Assay: JAK2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 100 μM KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC, 10 mM MgAcetate and [γ-33P-ATP](specific activity approx. 500 cpm/pmol, concentration as required). The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of 3% phosphoric acid solution. 10 μL of the reaction is then spotted onto a P30 filtermat and washed three times for 5 minutes in 75 mM phosphoric acid and once in methanol prior to drying and scintillation counting."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886854"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4111034"	""	"0"	"457.47"	"0"	"1.89"	"BDBM229516"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(C(=O)O[C@@H]2CCOC2)CC1"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	"401280"	"UO_0000065"	"16.83"	"0.32"	"5.81"	"5.19"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3980102"	""	"0"	"457.47"	"0"	"1.89"	"BDBM229523"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(C(=O)O[C@H]2CCOC2)CC1"	"IC50"	"'='"	"22.0"	"nM"	"7.66"	""	"401281"	"UO_0000065"	"16.74"	"0.32"	"5.77"	"5.16"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3958399"	""	"0"	"432.50"	"0"	"3.77"	"BDBM229096"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(Cc2ccccc2)CC1"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	"400832"	"UO_0000065"	"18.23"	"0.34"	"4.12"	"7.89"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4115501"	""	"0"	"423.45"	"0"	"2.75"	"BDBM237846"	"Cc1cc(CN2CC[C@@H](n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)[C@H](C#N)C2)no1"	"IC50"	"'='"	"92.0"	"nM"	"7.04"	""	"414950"	"UO_0000065"	"16.62"	"0.31"	"4.29"	"5.58"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4112701"	""	"0"	"437.45"	"0"	"2.99"	"BDBM237849"	"N#C[C@@H]1CN(Cc2cccc(F)n2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"24.0"	"nM"	"7.62"	""	"414953"	"UO_0000065"	"17.42"	"0.33"	"4.63"	"6.75"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3932038"	""	"0"	"363.37"	"0"	"0.97"	"BDBM237860"	"N#C[C@H]1CS(=O)(=O)C[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"32.0"	"nM"	"7.50"	""	"414964"	"UO_0000065"	"20.63"	"0.41"	"6.52"	"5.73"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4111885"	""	"0"	"363.37"	"0"	"0.97"	"BDBM237861"	"N#C[C@@H]1CS(=O)(=O)C[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"24.0"	"nM"	"7.62"	""	"414965"	"UO_0000065"	"20.97"	"0.42"	"6.65"	"5.82"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4067915"	""	"0"	"330.32"	"0"	"1.36"	"BDBM237866"	"N#C[C@H]1CCOC[C@@H]1n1cc(C(N)=O)c(Nc2ccnc(F)c2)n1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"414968"	"UO_0000065"	"26.33"	"0.50"	"7.34"	"7.32"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3923812"	""	"0"	"380.24"	"0"	"3.13"	"BDBM237876"	"N#C[C@@H]1CCOC[C@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)c(Cl)c2)n1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"414978"	"UO_0000065"	"21.83"	"0.45"	"5.17"	"7.83"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3913755"	""	"0"	"363.78"	"0"	"2.62"	"BDBM237878"	"N#C[C@@H]1CCOC[C@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)c(F)c2)n1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"414980"	"UO_0000065"	"23.09"	"0.46"	"5.78"	"7.93"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4109202"	""	"0"	"396.84"	"0"	"3.03"	"BDBM237887"	"N#C[C@H]1CCOC[C@@H]1n1cc(C(N)=O)c(Nc2cnc3cc(Cl)ccc3c2)n1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"414989"	"UO_0000065"	"20.92"	"0.40"	"5.27"	"6.98"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3928267"	""	"0"	"330.32"	"0"	"1.36"	"BDBM237896"	"N#C[C@@H]1CCOC[C@H]1n1cc(C(N)=O)c(Nc2cncc(F)c2)n1"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"414998"	"UO_0000065"	"24.69"	"0.46"	"6.79"	"6.86"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3934877"	""	"0"	"362.34"	"0"	"2.16"	"BDBM237898"	"N#C[C@@H]1CCOC[C@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)F)nc2)n1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"415000"	"UO_0000065"	"23.52"	"0.45"	"6.36"	"7.17"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4100288"	""	"0"	"311.35"	"0"	"1.83"	"BDBM237902"	"N#C[C@H]1CCOC[C@@H]1n1cc(C(N)=O)c(Nc2ccccc2)n1"	"IC50"	"'='"	"67.0"	"nM"	"7.17"	""	"415004"	"UO_0000065"	"23.04"	"0.43"	"5.34"	"6.77"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4108691"	""	"0"	"377.40"	"0"	"1.36"	"BDBM60977"	"C[C@]1(C#N)CS(=O)(=O)C[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"292.0"	"nM"	"6.54"	""	"415018"	"UO_0000065"	"17.31"	"0.34"	"5.17"	"4.99"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3911829"	""	"0"	"451.48"	"0"	"3.30"	"BDBM229138"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(Cc2cncc(F)c2)CC1"	"IC50"	"'='"	"29.0"	"nM"	"7.54"	""	"400874"	"UO_0000065"	"16.70"	"0.31"	"4.24"	"6.68"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3927968"	""	"0"	"507.49"	"1"	"3.47"	"BDBM229304"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(C(=O)C(C2CCC2)C(F)(F)F)CC1"	"IC50"	"'='"	"37.0"	"nM"	"7.43"	""	"401043"	"UO_0000065"	"14.64"	"0.28"	"3.96"	"5.72"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4107691"	""	"0"	"374.43"	"0"	"0.61"	"BDBM229336"	"CS(=O)(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"366.0"	"nM"	"6.44"	""	"401075"	"UO_0000065"	"17.19"	"0.34"	"5.83"	"4.80"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4109661"	""	"0"	"381.44"	"0"	"1.77"	"BDBM229343"	"CC(C)NC(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"185.0"	"nM"	"6.73"	""	"401082"	"UO_0000065"	"17.65"	"0.33"	"4.96"	"5.22"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4108922"	""	"0"	"443.51"	"0"	"3.50"	"BDBM229359"	"Cc1ccc(NC(=O)N2CC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)C2)c(C)c1"	"IC50"	"'='"	"334.0"	"nM"	"6.48"	""	"401098"	"UO_0000065"	"14.60"	"0.27"	"2.98"	"5.02"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3938195"	""	"0"	"464.47"	"0"	"3.95"	"BDBM229391"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(C(F)(F)F)cc3)n2)CCC(N2CC(F)C2)CC1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"401128"	"UO_0000065"	"18.35"	"0.35"	"4.57"	"8.53"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3911515"	""	"0"	"536.61"	"1"	"3.04"	"BDBM229411"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)F)cc3)n2)CCC(NC2CCOCC2)CC1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"401155"	"UO_0000065"	"15.47"	"0.31"	"5.26"	"5.46"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3890345"	""	"0"	"438.55"	"0"	"4.34"	"BDBM229518"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(NC2CCCCC2)CC1"	"IC50"	"'='"	"48.0"	"nM"	"7.32"	""	"401130"	"UO_0000065"	"16.69"	"0.31"	"2.98"	"6.73"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3984597"	""	"0"	"396.47"	"0"	"3.12"	"BDBM229448"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(N2CCC2)CC1"	"IC50"	"'='"	"325.0"	"nM"	"6.49"	""	"401209"	"UO_0000065"	"16.36"	"0.31"	"3.37"	"6.49"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3947540"	""	"0"	"534.51"	"1"	"3.43"	"BDBM229457"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)F)cc3)n2)CCC(NCC(F)(F)F)CC1"	"IC50"	"'='"	"466.0"	"nM"	"6.33"	""	"401217"	"UO_0000065"	"11.85"	"0.24"	"2.90"	"4.43"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3950882"	""	"0"	"458.54"	"0"	"4.43"	"BDBM229458"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(N2Cc3ccccc3C2)CC1"	"IC50"	"'='"	"84.0"	"nM"	"7.08"	""	"401218"	"UO_0000065"	"15.43"	"0.28"	"2.65"	"7.08"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3969967"	""	"0"	"414.46"	"0"	"3.07"	"BDBM229467"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(N2CC(F)C2)CC1"	"IC50"	"'='"	"216.0"	"nM"	"6.67"	""	"401228"	"UO_0000065"	"16.08"	"0.30"	"3.60"	"6.67"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3917223"	""	"0"	"448.45"	"0"	"3.20"	"BDBM229522"	"N#CC[C@]1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CC[C@H](C(=O)NCC(F)(F)F)CC1"	"IC50"	"'='"	"1481.0"	"nM"	"5.83"	""	"401274"	"UO_0000065"	"13.00"	"0.25"	"2.63"	"4.63"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3977718"	""	"0"	"400.87"	"0"	"2.17"	"BDBM239953"	"Cn1cc(Nc2ncc(Cl)c(NC3CC4CN(C(=O)CC#N)CC4C3)n2)cn1"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	"418572"	"UO_0000065"	"19.32"	"0.38"	"5.57"	"6.93"	"False"	"CHEMBL3888834"	"Kinase Assay: JAK2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 100 μM KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC, 10 mM MgAcetate and [γ-33P-ATP](specific activity approx. 500 cpm/pmol, concentration as required). The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of 3% phosphoric acid solution. 10 μL of the reaction is then spotted onto a P30 filtermat and washed three times for 5 minutes in 75 mM phosphoric acid and once in methanol prior to drying and scintillation counting."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886854"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3944988"	""	"0"	"375.86"	"0"	"2.28"	"BDBM239967"	"CC(=O)N1CC2CC(Nc3nc(Nc4cnn(C)c4)ncc3Cl)CC2C1"	"IC50"	"'='"	"37.0"	"nM"	"7.43"	""	"418587"	"UO_0000065"	"19.77"	"0.39"	"5.15"	"8.45"	"False"	"CHEMBL3888834"	"Kinase Assay: JAK2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 100 μM KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC, 10 mM MgAcetate and [γ-33P-ATP](specific activity approx. 500 cpm/pmol, concentration as required). The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of 3% phosphoric acid solution. 10 μL of the reaction is then spotted onto a P30 filtermat and washed three times for 5 minutes in 75 mM phosphoric acid and once in methanol prior to drying and scintillation counting."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886854"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3986584"	""	"0"	"460.52"	"0"	"1.60"	"BDBM229169"	"COC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(S(C)(=O)=O)cc3)n2)CC1"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	"400905"	"UO_0000065"	"16.93"	"0.33"	"6.20"	"4.86"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3942553"	""	"0"	"440.48"	"0"	"3.26"	"BDBM229177"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(C(=O)OC2CCC2)CC1"	"IC50"	"'='"	"33.0"	"nM"	"7.48"	""	"400914"	"UO_0000065"	"16.98"	"0.32"	"4.22"	"5.92"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4113401"	""	"0"	"459.51"	"0"	"2.81"	"BDBM229239"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CN(C(=O)OCCCc2cccnc2)C1"	"IC50"	"'='"	"445.0"	"nM"	"6.35"	""	"400978"	"UO_0000065"	"13.82"	"0.26"	"3.54"	"4.56"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4108923"	""	"0"	"460.49"	"0"	"3.00"	"BDBM229240"	"COc1ccccc1COC(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"671.0"	"nM"	"6.17"	""	"400979"	"UO_0000065"	"13.41"	"0.25"	"3.17"	"4.56"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3936839"	""	"0"	"392.46"	"0"	"2.53"	"BDBM229253"	"C/C=C/C(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)CC1"	"IC50"	"'='"	"64.0"	"nM"	"7.19"	""	"400992"	"UO_0000065"	"18.33"	"0.34"	"4.66"	"6.15"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3930514"	""	"0"	"429.48"	"0"	"2.67"	"BDBM229262"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)c2ccccn2)CC1"	"IC50"	"'='"	"372.0"	"nM"	"6.43"	""	"401001"	"UO_0000065"	"14.97"	"0.27"	"3.76"	"4.95"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3948843"	""	"0"	"455.52"	"0"	"3.07"	"BDBM229270"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)/C=C/c2cccnc2)CC1"	"IC50"	"'='"	"158.0"	"nM"	"6.80"	""	"401009"	"UO_0000065"	"14.93"	"0.27"	"3.73"	"5.23"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3957574"	""	"0"	"443.48"	"0"	"1.51"	"BDBM229300"	"CC(C)[C@H](O)C(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CC1"	"IC50"	"'='"	"79.0"	"nM"	"7.10"	""	"401039"	"UO_0000065"	"16.02"	"0.30"	"5.59"	"4.73"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3958613"	""	"0"	"473.56"	"0"	"1.56"	"BDBM229383"	"CCCCNC(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(S(C)(=O)=O)cc3)n2)C1"	"IC50"	"'='"	"322.0"	"nM"	"6.49"	""	"401122"	"UO_0000065"	"13.71"	"0.27"	"4.93"	"3.98"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3983303"	""	"0"	"371.45"	"0"	"3.86"	"BDBM198285"	"N#Cc1ccc(NC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"352363"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3920570"	""	"0"	"481.96"	"0"	"4.25"	"BDBM229483"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(NCc2ccc(Cl)cc2)CC1"	"IC50"	"'='"	"440.0"	"nM"	"6.36"	""	"401246"	"UO_0000065"	"13.19"	"0.26"	"2.11"	"5.23"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3979560"	""	"0"	"463.52"	"0"	"3.31"	"BDBM229494"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(NCc2ccc(O)cc2)CC1"	"IC50"	"'='"	"759.0"	"nM"	"6.12"	""	"401263"	"UO_0000065"	"13.20"	"0.25"	"2.81"	"4.31"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3953692"	""	"0"	"472.55"	"0"	"3.42"	"BDBM229089"	"COC(=O)c1ccccc1CN1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)CC1"	"IC50"	"'='"	"400.0"	"nM"	"6.40"	""	"400825"	"UO_0000065"	"13.54"	"0.25"	"2.98"	"5.07"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3968639"	""	"0"	"424.44"	"0"	"2.15"	"BDBM229115"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2cocn2)CC1"	"IC50"	"'='"	"117.0"	"nM"	"6.93"	""	"400851"	"UO_0000065"	"16.33"	"0.31"	"4.78"	"4.99"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4108858"	""	"0"	"463.93"	"0"	"3.84"	"BDBM229353"	"Cc1ccc(NC(=O)N2CC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)C2)cc1Cl"	"IC50"	"'='"	"339.0"	"nM"	"6.47"	""	"401092"	"UO_0000065"	"13.95"	"0.27"	"2.63"	"5.01"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4106590"	""	"0"	"459.51"	"0"	"3.20"	"BDBM229365"	"COc1ccc(C)cc1NC(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"168.0"	"nM"	"6.78"	""	"401104"	"UO_0000065"	"14.74"	"0.27"	"3.57"	"4.90"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3892967"	""	"0"	"459.51"	"0"	"3.28"	"BDBM229370"	"CCOc1ccccc1NC(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"507.0"	"nM"	"6.29"	""	"401109"	"UO_0000065"	"13.70"	"0.25"	"3.01"	"4.55"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4113403"	""	"0"	"447.47"	"0"	"3.33"	"BDBM229378"	"Cc1ccc(F)cc1NC(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"183.0"	"nM"	"6.74"	""	"401117"	"UO_0000065"	"15.06"	"0.28"	"3.41"	"5.22"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3892313"	""	"0"	"434.48"	"0"	"3.32"	"BDBM228183"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(Nc2ccccn2)CC1"	"IC50"	"'='"	"365.0"	"nM"	"6.44"	""	"401135"	"UO_0000065"	"14.82"	"0.27"	"3.12"	"4.78"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3906978"	""	"0"	"480.45"	"0"	"2.33"	"BDBM229184"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(C(=O)OCC(F)(F)CO)CC1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	"400921"	"UO_0000065"	"16.56"	"0.32"	"5.63"	"5.43"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3977586"	""	"0"	"454.51"	"0"	"3.50"	"BDBM229185"	"CC(OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CC1)C1CC1"	"IC50"	"'='"	"71.0"	"nM"	"7.15"	""	"400922"	"UO_0000065"	"15.73"	"0.30"	"3.65"	"5.66"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3926489"	""	"0"	"472.55"	"0"	"3.21"	"BDBM229277"	"COc1ccc(CC(=O)N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)CC2)cc1"	"IC50"	"'='"	"84.0"	"nM"	"7.08"	""	"401016"	"UO_0000065"	"14.97"	"0.28"	"3.87"	"5.60"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3909805"	""	"0"	"481.56"	"0"	"3.76"	"BDBM229279"	"Cn1c(C(=O)N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)CC2)cc2ccccc21"	"IC50"	"'='"	"238.0"	"nM"	"6.62"	""	"401018"	"UO_0000065"	"13.75"	"0.25"	"2.86"	"5.43"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3964474"	""	"0"	"518.62"	"1"	"4.79"	"BDBM229286"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)C(c2ccccc2)c2ccccc2)CC1"	"IC50"	"'='"	"711.0"	"nM"	"6.15"	""	"401025"	"UO_0000065"	"11.85"	"0.22"	"1.36"	"5.25"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4107620"	""	"0"	"401.43"	"0"	"1.89"	"BDBM229291"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CN(C(=O)c2ccccn2)C1"	"IC50"	"'='"	"542.0"	"nM"	"6.27"	""	"401030"	"UO_0000065"	"15.61"	"0.29"	"4.38"	"4.82"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3915901"	""	"0"	"469.53"	"0"	"1.27"	"BDBM229320"	"CS(=O)(=O)c1ccc(Nc2nn(C3(CC#N)CCN(C(=O)CC#N)CC3)cc2C(N)=O)cc1"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	"401059"	"UO_0000065"	"17.04"	"0.33"	"6.73"	"4.57"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3923655"	""	"0"	"438.43"	"0"	"3.57"	"BDBM229468"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(NCC(F)(F)F)CC1"	"IC50"	"'='"	"276.0"	"nM"	"6.56"	""	"401229"	"UO_0000065"	"14.96"	"0.29"	"2.99"	"6.03"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3968173"	""	"0"	"422.47"	"0"	"2.18"	"BDBM237818"	"Cn1ccc(CN2CC[C@@H](C#N)[C@H](n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)C2)n1"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	"414922"	"UO_0000065"	"18.59"	"0.35"	"5.67"	"6.67"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3970415"	""	"0"	"361.88"	"0"	"2.94"	"BDBM239954"	"Cn1cc(Nc2ncc(Cl)c(NC3CCC4(CCNC4)CC3)n2)cn1"	"IC50"	"'='"	"55.0"	"nM"	"7.26"	""	"418573"	"UO_0000065"	"20.06"	"0.40"	"4.32"	"9.11"	"False"	"CHEMBL3888834"	"Kinase Assay: JAK2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 100 μM KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC, 10 mM MgAcetate and [γ-33P-ATP](specific activity approx. 500 cpm/pmol, concentration as required). The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of 3% phosphoric acid solution. 10 μL of the reaction is then spotted onto a P30 filtermat and washed three times for 5 minutes in 75 mM phosphoric acid and once in methanol prior to drying and scintillation counting."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886854"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3920484"	""	"0"	"328.81"	"0"	"2.72"	"BDBM228669"	"CN(c1ccc(Cl)cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399638"	"UO_0000065"	"31.20"	"0.61"	"7.54"	"16.84"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3961850"	""	"0"	"319.37"	"0"	"1.94"	"BDBM228725"	"CN(c1cccc(C#N)n1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399646"	"UO_0000065"	"32.12"	"0.58"	"8.32"	"12.11"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3896481"	""	"0"	"319.37"	"0"	"1.94"	"BDBM228719"	"CN(c1ccc(C#N)cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399647"	"UO_0000065"	"32.12"	"0.58"	"8.32"	"12.11"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3977509"	""	"0"	"319.37"	"0"	"1.94"	"BDBM228731"	"CN(c1ccc(C#N)cn1)[C@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399652"	"UO_0000065"	"32.12"	"0.58"	"8.32"	"12.11"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3905748"	""	"0"	"342.41"	"0"	"2.55"	"BDBM228737"	"C#CCN(c1ccc(C#N)cc1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399665"	"UO_0000065"	"29.96"	"0.54"	"7.71"	"14.28"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3909092"	""	"0"	"333.40"	"0"	"2.25"	"BDBM228685"	"Cc1nc(N(C)[C@@H]2CCN(c3ncnc4[nH]ccc34)C2)ccc1C#N"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399668"	"UO_0000065"	"30.77"	"0.56"	"8.01"	"12.11"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3934942"	""	"0"	"334.39"	"0"	"1.94"	"BDBM228744"	"CN(c1ccc2nc[nH]c2n1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399674"	"UO_0000065"	"30.68"	"0.56"	"8.32"	"11.45"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3944101"	""	"0"	"571.01"	"2"	"5.18"	"BDBM230152"	"Cc1c(-c2c(Cl)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)cc2c(F)cccn2c1=O"	"IC50"	"'='"	"800.0"	"nM"	"6.10"	""	"402046"	"UO_0000065"	"10.68"	"0.20"	"0.92"	"4.97"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3931086"	""	"0"	"564.62"	"2"	"5.07"	"BDBM230105"	"Cc1cc(C(N)=O)c2[nH]c3cc(C(C)(C)O)ccc3c2c1-c1cccc(-n2c(=O)c3cccc(F)c3n(C)c2=O)c1C"	"IC50"	"'='"	"790.0"	"nM"	"6.10"	""	"402040"	"UO_0000065"	"10.81"	"0.20"	"1.03"	"4.96"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3924304"	""	"0"	"473.52"	"0"	"2.81"	"BDBM229123"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2cc3ccccn3n2)CC1"	"IC50"	"'='"	"163.0"	"nM"	"6.79"	""	"400859"	"UO_0000065"	"14.33"	"0.26"	"3.98"	"5.21"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3898832"	""	"0"	"396.47"	"0"	"2.98"	"BDBM229164"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(CC2CC2)CC1"	"IC50"	"'='"	"917.0"	"nM"	"6.04"	""	"400900"	"UO_0000065"	"15.23"	"0.28"	"3.06"	"6.04"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3889909"	""	"0"	"420.45"	"0"	"2.56"	"BDBM229166"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(c2ccncn2)CC1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"400902"	"UO_0000065"	"19.74"	"0.37"	"5.74"	"6.60"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3939808"	""	"0"	"451.48"	"0"	"3.30"	"BDBM229139"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(Cc2cc(F)ccn2)CC1"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	"400875"	"UO_0000065"	"17.27"	"0.32"	"4.50"	"6.91"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3936358"	""	"0"	"316.38"	"0"	"2.94"	"BDBM255009"	"CN1CN([C@H]2CC[C@H](CF)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"8.1"	"nM"	"8.09"	""	"443865"	"UO_0000065"	"25.58"	"0.48"	"5.15"	"15.49"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3943509"	""	"0"	"366.47"	"0"	"2.43"	"BDBM255012"	"CN(CC#N)C[C@H]1CC[C@H](N2CN(C)C(=O)c3cnc4[nH]ccc4c32)CC1"	"IC50"	"'='"	"21.0"	"nM"	"7.68"	""	"443868"	"UO_0000065"	"20.95"	"0.39"	"5.25"	"9.69"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3924902"	""	"0"	"327.43"	"0"	"2.19"	"BDBM254983"	"CN(C)C[C@H]1CC[C@H](N2CNC(=O)c3cnc4[nH]ccc4c32)CC1"	"IC50"	"'='"	"69.0"	"nM"	"7.16"	""	"443890"	"UO_0000065"	"21.87"	"0.41"	"4.97"	"11.14"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3955398"	""	"0"	"467.94"	"0"	"3.82"	"BDBM229148"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2ccccc2Cl)CC1"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"400884"	"UO_0000065"	"17.43"	"0.34"	"4.33"	"7.23"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL2178256"	""	"0"	"354.76"	"0"	"2.87"	"7e"	"Nc1ccn2ncc(C(=O)Nc3cnoc3-c3cccc(Cl)c3)c2n1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL2186598"	"Inhibition of JAK2 V617F mutant in human SET2 cells assessed as reduction in STAT5 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176876"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2178251"	""	"0"	"352.79"	"0"	"3.04"	"12"	"Cn1cc(-c2cccc(Cl)c2)c(NC(=O)c2cnn3cccnc23)n1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL2186598"	"Inhibition of JAK2 V617F mutant in human SET2 cells assessed as reduction in STAT5 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176876"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1946442"	""	"0"	"390.46"	"0"	"4.80"	"28d"	"CN1C/C=C/CCOc2cc(F)cc(c2)-c2ccnc(n2)Nc2cccc(c2)C1"	"IC50"	"'='"	"160.0"	"nM"	"6.80"	""	""	"UO_0000065"	"17.40"	"0.32"	"2.00"	"13.52"	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL4519857"	""	"0"	"405.46"	"0"	"1.67"	"8"	"CCNC(=O)c1ccc(Nc2nccc(N3C[C@@H]4C[C@H]3CN4C(=O)CC#N)n2)cc1"	"IC50"	"'>'"	"9972.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4411595"	"Inhibition of human JAK2 using fluorescence labeled peptide as substrate and using 1 mM ATP by microfluidic based mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4411260"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4587406"	""	"0"	"420.52"	"0"	"2.56"	"14"	"CCNC(=O)c1ccc(Nc2nccc(N3C[C@H]4CC[C@H](C3)N4C(=O)C3CC3)n2)cc1"	"IC50"	"'='"	"329.0"	"nM"	"6.48"	""	""	"UO_0000065"	"15.42"	"0.29"	"3.92"	"7.17"	"False"	"CHEMBL4411595"	"Inhibition of human JAK2 using fluorescence labeled peptide as substrate and using 1 mM ATP by microfluidic based mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4411260"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4535276"	""	"0"	"401.45"	"0"	"1.14"	"16"	"O=C(C1CC1)N1[C@@H]2CC[C@@H]1CN(c1nc(Nc3cnn(CCO)c3)ncc1F)C2"	"IC50"	"'='"	"260.0"	"nM"	"6.58"	""	""	"UO_0000065"	"16.40"	"0.31"	"5.45"	"6.62"	"False"	"CHEMBL4411595"	"Inhibition of human JAK2 using fluorescence labeled peptide as substrate and using 1 mM ATP by microfluidic based mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4411260"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4445892"	""	"0"	"453.52"	"0"	"2.40"	"18"	"CCNC(=O)c1ncc(Nc2ncc(F)c(N3C[C@H]4CC[C@H](C3)N4C(=O)C3CC3)n2)cc1C"	"IC50"	"'='"	"692.0"	"nM"	"6.16"	""	""	"UO_0000065"	"13.58"	"0.25"	"3.76"	"5.96"	"False"	"CHEMBL4411595"	"Inhibition of human JAK2 using fluorescence labeled peptide as substrate and using 1 mM ATP by microfluidic based mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4411260"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4448796"	""	"0"	"439.50"	"0"	"2.09"	"19"	"CCNC(=O)c1ccc(Nc2ncc(F)c(N3C[C@H]4CC[C@H](C3)N4C(=O)C3CC3)n2)nc1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4411595"	"Inhibition of human JAK2 using fluorescence labeled peptide as substrate and using 1 mM ATP by microfluidic based mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4411260"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4520790"	""	"0"	"367.42"	"0"	"0.84"	"20"	"Cn1cc(Nc2nccc(N3C[C@H]4CC[C@H](C3)N4C(=O)NCC#N)n2)cn1"	"IC50"	"'='"	"67.0"	"nM"	"7.17"	""	""	"UO_0000065"	"19.53"	"0.36"	"6.33"	"6.24"	"False"	"CHEMBL4411595"	"Inhibition of human JAK2 using fluorescence labeled peptide as substrate and using 1 mM ATP by microfluidic based mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4411260"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL1933576"	""	"0"	"475.48"	"0"	"2.98"	"13"	"CN1CCN(c2ccc(OC(F)(F)F)c(Nc3nccc(-c4cc(C(N)=O)cn4C)n3)c2)CC1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1936520"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1933058"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL2178807"	""	"0"	"367.80"	"0"	"2.71"	"7a"	"Cc1cc(NC(=O)c2cnn3ccc(N)nc23)n(-c2cccc(Cl)c2)n1"	"IC50"	"'='"	"131.0"	"nM"	"6.88"	""	""	"UO_0000065"	"18.71"	"0.36"	"4.17"	"6.67"	"False"	"CHEMBL2186598"	"Inhibition of JAK2 V617F mutant in human SET2 cells assessed as reduction in STAT5 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176876"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2177122"	""	"0"	"387.23"	"0"	"3.69"	"13g"	"Cn1cc(NC(=O)c2cnn3cccnc23)c(-c2c(Cl)cccc2Cl)n1"	"IC50"	"'='"	"242.0"	"nM"	"6.62"	""	""	"UO_0000065"	"17.09"	"0.35"	"2.93"	"8.58"	"False"	"CHEMBL2186603"	"Inhibition of JAK2 in human TF1 cells assessed as reduction in STAT5 phosphorylation incubated for 30 mins in presence of human recombinant EPO"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176876"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"CHEMBL3307972"	""
"CHEMBL2414548"	""	"0"	"343.43"	"0"	"4.97"	"18"	"Cc1cc(Nc2nc3cccc(-c4cccc(C(C)C)c4)n3n2)ccn1"	"IC50"	"'='"	"190.0"	"nM"	"6.72"	""	""	"UO_0000065"	"19.57"	"0.35"	"1.75"	"12.20"	"False"	"CHEMBL2415128"	"Inhibition of JAK2 in human SET2 cells assessed as reduction of phosphorylated STAT5 level"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2412966"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL1081190"	""	"0"	"402.39"	"0"	"2.97"	"21c"	"O=c1[nH]c2cnc(-n3cnc4ccccc43)nc2n1C1CCOc2ccc(F)cc21"	"IC50"	"'='"	"83.0"	"nM"	"7.08"	""	""	"UO_0000065"	"17.60"	"0.32"	"4.11"	"7.81"	"False"	"CHEMBL1102456"	"Inhibition of human JAK2 (532-1132) by time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154364"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1080110"	""	"0"	"402.39"	"0"	"2.97"	"21e"	"O=c1[nH]c2cnc(-n3cnc4ccccc43)nc2n1C1CCOc2cc(F)ccc21"	"IC50"	"'='"	"95.0"	"nM"	"7.02"	""	""	"UO_0000065"	"17.45"	"0.32"	"4.05"	"7.75"	"False"	"CHEMBL1102456"	"Inhibition of human JAK2 (532-1132) by time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154364"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1081377"	""	"0"	"402.39"	"0"	"2.97"	"(R)-21f"	"O=c1[nH]c2cnc(-n3cnc4ccccc43)nc2n1[C@@H]1CCOc2c(F)cccc21"	"IC50"	"'='"	"333.0"	"nM"	"6.48"	""	""	"UO_0000065"	"16.10"	"0.29"	"3.51"	"7.15"	"False"	"CHEMBL1102456"	"Inhibition of human JAK2 (532-1132) by time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154364"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1081378"	""	"0"	"402.39"	"0"	"2.97"	"(S)-21f"	"O=c1[nH]c2cnc(-n3cnc4ccccc43)nc2n1[C@H]1CCOc2c(F)cccc21"	"IC50"	"'='"	"7000.0"	"nM"	"5.16"	""	""	"UO_0000065"	"12.81"	"0.23"	"2.18"	"5.69"	"False"	"CHEMBL1102456"	"Inhibition of human JAK2 (532-1132) by time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154364"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1081379"	""	"0"	"436.83"	"0"	"3.62"	"23"	"O=c1[nH]c2cnc(-n3cnc4ccc(Cl)cc43)nc2n1[C@@H]1CCOc2c(F)cccc21"	"IC50"	"'='"	"56.0"	"nM"	"7.25"	""	""	"UO_0000065"	"16.60"	"0.32"	"3.63"	"8.00"	"False"	"CHEMBL1102456"	"Inhibition of human JAK2 (532-1132) by time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154364"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1079593"	"VS-5584"	"1"	"420.38"	"0"	"3.11"	"24"	"O=c1[nH]c2cnc(-n3cnc4ccc(F)cc43)nc2n1[C@@H]1CCOc2c(F)cccc21"	"IC50"	"'='"	"26.0"	"nM"	"7.58"	""	""	"UO_0000065"	"18.04"	"0.33"	"4.48"	"8.37"	"False"	"CHEMBL1102456"	"Inhibition of human JAK2 (532-1132) by time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154364"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL569957"	""	"0"	"462.48"	"0"	"2.79"	"27"	"CCCN(CC(F)(F)F)C(=O)C1CCCN(c2cc(-c3c(N)nn4cccnc34)ncn2)C1"	"IC50"	"'='"	"1100.0"	"nM"	"5.96"	""	""	"UO_0000065"	"12.88"	"0.25"	"3.17"	"5.65"	"False"	"CHEMBL1044320"	"Inhibition of JAK2-mediated STAT5 phosphorylation in GMCSF-stimulated human TF1 cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"CHEMBL3307972"	""
"CHEMBL570686"	""	"0"	"335.35"	"0"	"2.52"	"34"	"Nc1nn2cccnc2c1-c1cc(NCc2ccc(F)cc2)ncn1"	"IC50"	"'='"	"3000.0"	"nM"	"5.52"	""	""	"UO_0000065"	"16.47"	"0.30"	"3.00"	"5.87"	"False"	"CHEMBL1044320"	"Inhibition of JAK2-mediated STAT5 phosphorylation in GMCSF-stimulated human TF1 cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"CHEMBL3307972"	""
"CHEMBL569966"	""	"0"	"363.40"	"0"	"3.47"	"44"	"CC[C@@H](Nc1cc(-c2c(N)nn3cccnc23)ncn1)c1ccc(F)cc1"	"IC50"	"'='"	"270.0"	"nM"	"6.57"	""	""	"UO_0000065"	"18.08"	"0.33"	"3.10"	"6.99"	"False"	"CHEMBL1044320"	"Inhibition of JAK2-mediated STAT5 phosphorylation in GMCSF-stimulated human TF1 cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"CHEMBL3307972"	""
"CHEMBL4550702"	""	"0"	"406.39"	"0"	"3.15"	"9"	"Cn1cc(-c2cnc3c(-c4csc(C(=O)NCC(F)(F)F)c4)cnn3c2)cn1"	"IC50"	"'='"	"1200.0"	"nM"	"5.92"	""	""	"UO_0000065"	"14.57"	"0.29"	"2.77"	"7.68"	"False"	"CHEMBL4479735"	"Inhibition of recombinant human GST-tagged cytoplasmic JAK2 (809 to 1153 residues) expressed in baculovirus expression system by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4477252"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2016"	"None"	""
"CHEMBL1934345"	""	"0"	"457.54"	"0"	"3.21"	"3k"	"COc1cccnc1-c1ccc2cnc(Nc3ccc(C4CCN(CC(N)=O)CC4)cc3)nn12"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	""	"UO_0000065"	"17.04"	"0.31"	"4.59"	"7.04"	"False"	"CHEMBL1936085"	"Inhibition of human recombinant JAK2 expressed in baculovirus expression system after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL1934347"	""	"0"	"428.50"	"0"	"2.59"	"3m"	"NC(=O)CN1CCC(c2ccc(Nc3ncc4ccc(-c5cnccn5)n4n3)cc2)CC1"	"IC50"	"'='"	"8.9"	"nM"	"8.05"	""	""	"UO_0000065"	"18.79"	"0.34"	"5.46"	"7.04"	"False"	"CHEMBL1936085"	"Inhibition of human recombinant JAK2 expressed in baculovirus expression system after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL1934348"	""	"0"	"506.51"	"1"	"4.13"	"3n"	"NC(=O)CN1CCC(c2ccc(Nc3ncc4ccc(-c5cccc6c5OC(F)(F)O6)n4n3)cc2)CC1"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	""	"UO_0000065"	"15.57"	"0.29"	"3.76"	"7.37"	"False"	"CHEMBL1936085"	"Inhibition of human recombinant JAK2 expressed in baculovirus expression system after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL1934349"	""	"0"	"483.62"	"0"	"3.87"	"3o"	"CN(C)Cc1ccc(-c2ccc3cnc(Nc4ccc(C5CCN(CC(N)=O)CC5)cc4)nn23)cc1"	"IC50"	"'='"	"2900.0"	"nM"	"5.54"	""	""	"UO_0000065"	"11.45"	"0.21"	"1.67"	"6.03"	"False"	"CHEMBL1936085"	"Inhibition of human recombinant JAK2 expressed in baculovirus expression system after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL1938653"	""	"0"	"350.45"	"0"	"3.71"	"18"	"CNC(=O)c1cnc(N)c2cc(-c3ccc(C(C)(C)C#N)cc3)sc12"	"IC50"	"'='"	"1370.0"	"nM"	"5.86"	""	""	"UO_0000065"	"16.73"	"0.32"	"2.15"	"6.39"	"False"	"CHEMBL1941390"	"Inhibition of TEL-fused JAK2 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3307634"	""
"CHEMBL1946152"	""	"0"	"386.50"	"0"	"4.97"	"28a"	"Cc1cc2nc(n1)Nc1cccc(c1)CN(C)C/C=C/CCOc1cccc-2c1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1934335"	""	"0"	"456.55"	"0"	"3.81"	"3a"	"COc1ccccc1-c1ccc2cnc(Nc3ccc(C4CCN(CC(N)=O)CC4)cc3)nn12"	"IC50"	"'='"	"41.0"	"nM"	"7.39"	""	""	"UO_0000065"	"16.18"	"0.30"	"3.58"	"7.55"	"False"	"CHEMBL1936009"	"Inhibition of JAK2 in GM-CSF-stimulated human TF1 cells preincubated for 1 hr prior to challenge"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3307972"	""
"CHEMBL1934340"	""	"0"	"533.66"	"1"	"3.20"	"3f"	"CN(c1cccc(-c2ccc3cnc(Nc4ccc(C5CCN(CC(N)=O)CC5)cc4)nn23)c1)S(C)(=O)=O"	"IC50"	"'='"	"45.0"	"nM"	"7.35"	""	""	"UO_0000065"	"13.77"	"0.26"	"4.15"	"5.83"	"False"	"CHEMBL1936009"	"Inhibition of JAK2 in GM-CSF-stimulated human TF1 cells preincubated for 1 hr prior to challenge"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3307972"	""
"CHEMBL1934346"	""	"0"	"428.50"	"0"	"2.59"	"3l"	"NC(=O)CN1CCC(c2ccc(Nc3ncc4ccc(-c5ncccn5)n4n3)cc2)CC1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1936009"	"Inhibition of JAK2 in GM-CSF-stimulated human TF1 cells preincubated for 1 hr prior to challenge"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3307972"	""
"CHEMBL1934349"	""	"0"	"483.62"	"0"	"3.87"	"3o"	"CN(C)Cc1ccc(-c2ccc3cnc(Nc4ccc(C5CCN(CC(N)=O)CC5)cc4)nn23)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1936009"	"Inhibition of JAK2 in GM-CSF-stimulated human TF1 cells preincubated for 1 hr prior to challenge"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3307972"	""
"CHEMBL4594048"	""	"0"	"305.30"	"0"	"1.79"	"5"	"O=C(Nc1ccc2[nH]ncc2c1)c1cccc(-n2cnnn2)c1"	"IC50"	"'='"	"718.0"	"nM"	"6.14"	""	""	"UO_0000065"	"20.12"	"0.36"	"4.35"	"6.06"	"False"	"CHEMBL4481929"	"Inhibition of JAK2 (unknown origin) after 1 hr FRET-based Z'-Lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480435"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4572055"	""	"0"	"360.41"	"0"	"2.91"	"17"	"Nc1n[nH]c2ccc(-c3cnc(-c4ccccc4-n4cnnn4)s3)cc12"	"IC50"	"'='"	"3250.0"	"nM"	"5.49"	""	""	"UO_0000065"	"15.23"	"0.29"	"2.58"	"4.94"	"False"	"CHEMBL4481929"	"Inhibition of JAK2 (unknown origin) after 1 hr FRET-based Z'-Lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480435"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL576475"	""	"0"	"318.34"	"0"	"1.78"	"32"	"Nc1nn2cccnc2c1-c1cc(NCc2ccccn2)ncn1"	"IC50"	"'>'"	"20000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1044320"	"Inhibition of JAK2-mediated STAT5 phosphorylation in GMCSF-stimulated human TF1 cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"CHEMBL3307972"	""
"CHEMBL570206"	""	"0"	"365.83"	"0"	"3.60"	"39"	"C[C@@H](Nc1cc(-c2c(N)nn3cccnc23)ncn1)c1ccc(Cl)cc1"	"IC50"	"'='"	"6900.0"	"nM"	"5.16"	""	""	"UO_0000065"	"14.11"	"0.27"	"1.56"	"5.49"	"False"	"CHEMBL1044320"	"Inhibition of JAK2-mediated STAT5 phosphorylation in GMCSF-stimulated human TF1 cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"CHEMBL3307972"	""
"CHEMBL1835151"	""	"0"	"511.51"	"1"	"3.86"	"63"	"NC(=O)c1cnc(N[C@H](C2CC2)C(F)(F)F)c2c1[nH]c1cc(-c3cnc(N4CCOCC4)nc3)ccc12"	"IC50"	"'='"	"530.0"	"nM"	"6.28"	""	""	"UO_0000065"	"12.27"	"0.23"	"2.42"	"5.14"	"False"	"CHEMBL1840130"	"Inhibition of JAK2-mediated STAT5 phosphorylation in human HEL 92.1.7 irf1-bla cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308090"	""
"CHEMBL1835150"	""	"0"	"440.43"	"0"	"4.21"	"62"	"NC(=O)c1cnc(N[C@H](C2CC2)C(F)(F)F)c2c1[nH]c1cc(-c3ccc(N)nc3)ccc12"	"IC50"	"'='"	"61.0"	"nM"	"7.21"	""	""	"UO_0000065"	"16.38"	"0.31"	"3.00"	"5.88"	"False"	"CHEMBL1840130"	"Inhibition of JAK2-mediated STAT5 phosphorylation in human HEL 92.1.7 irf1-bla cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308090"	""
"CHEMBL1089833"	""	"0"	"519.62"	"1"	"4.22"	"10"	"COc1cc(-c2cnc3cccc(-c4ccc(CN5CCS(=O)(=O)CC5)cc4)c3n2)cc(OC)c1OC"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	""	"UO_0000065"	"15.11"	"0.29"	"3.63"	"8.64"	"False"	"CHEMBL1116984"	"Inhibition of recombinant GST tagged JAK2 protein after 60 mins using FITC-GGEEEEYFELVKKKK-NH2 substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156975"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL570217"	""	"0"	"377.43"	"0"	"3.72"	"46"	"CC(C)[C@@H](Nc1cc(-c2c(N)nn3cccnc23)ncn1)c1ccc(F)cc1"	"IC50"	"'='"	"0.6"	"nM"	"9.22"	""	""	"UO_0000065"	"24.43"	"0.45"	"5.50"	"9.81"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL4785910"	""	"0"	"414.51"	"0"	"3.40"	"20f"	"CNC(=O)c1cnc2[nH]ccc2c1NC1CC2CCC(C1)N2Cc1ccc(C#N)cc1"	"IC50"	"'='"	"86.6"	"nM"	"7.06"	""	""	""	"17.04"	"0.31"	"3.66"	"7.29"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL453737"	""	"0"	"629.66"	"2"	"5.92"	"51"	"COc1cc2c(Oc3ccc(-c4cnc(Nc5ccc(F)cc5)n(C)c4=O)cc3F)ccnc2cc1OCCCN1CCOCC1"	"IC50"	"'='"	"3400.0"	"nM"	"5.47"	""	""	"UO_0000065"	"8.68"	"0.16"	"-0.45"	"5.47"	"False"	"CHEMBL971828"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1140082"	"1"	"Scientific Literature"	"J. Med. Chem."	"2008"	"None"	""
"CHEMBL447602"	""	"0"	"612.66"	"3"	"5.18"	"62"	"COc1cc2c(Oc3ccc(-c4cnc(Nc5ccc(F)cc5)n(C)c4=O)nc3)ccnc2cc1OCCCN1CCOCC1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL971828"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1140082"	"1"	"Scientific Literature"	"J. Med. Chem."	"2008"	"None"	""
"CHEMBL1243200"	""	"0"	"488.55"	"1"	"6.37"	"6j"	"CNc1nccc(-c2cccnc2Oc2ccc(NC(=O)c3ccccc3Nc3ccccc3)cc2)n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1247968"	"Inhibition of Jak2 by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1240487"	"1"	"Scientific Literature"	"J. Med. Chem."	"2010"	"None"	""
"CHEMBL1093191"	""	"0"	"499.57"	"0"	"4.39"	"8"	"COc1cc(-c2cnc3cccc(-c4ccc(CC(=O)N5CCOCC5)cc4)c3n2)cc(OC)c1OC"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	""	"UO_0000065"	"15.79"	"0.29"	"3.50"	"9.50"	"False"	"CHEMBL1116984"	"Inhibition of recombinant GST tagged JAK2 protein after 60 mins using FITC-GGEEEEYFELVKKKK-NH2 substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156975"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1091191"	""	"0"	"517.56"	"1"	"4.53"	"12"	"COc1cc(-c2cnc3cc(F)cc(-c4ccc(CC(=O)N5CCOCC5)cc4)c3n2)cc(OC)c1OC"	"IC50"	"'='"	"101.0"	"nM"	"7.00"	""	""	"UO_0000065"	"13.52"	"0.25"	"2.47"	"8.43"	"False"	"CHEMBL1116984"	"Inhibition of recombinant GST tagged JAK2 protein after 60 mins using FITC-GGEEEEYFELVKKKK-NH2 substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156975"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1092840"	""	"0"	"526.61"	"1"	"4.72"	"22"	"Cc1cc(-c2cnc3cccc(-c4ccc(CN5CCOCC5)c(F)c4)c3n2)ccc1C(=O)N1CCOCC1"	"IC50"	"'='"	"12.5"	"nM"	"7.90"	""	""	"UO_0000065"	"15.01"	"0.28"	"3.18"	"11.66"	"False"	"CHEMBL1116984"	"Inhibition of recombinant GST tagged JAK2 protein after 60 mins using FITC-GGEEEEYFELVKKKK-NH2 substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156975"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1092926"	""	"0"	"490.56"	"0"	"4.20"	"26"	"Fc1cc(-c2cccc3ncc(-c4cnn(C5CCNCC5)c4)nc23)cc(F)c1CN1CCOCC1"	"IC50"	"'='"	"7.3"	"nM"	"8.14"	""	""	"UO_0000065"	"16.59"	"0.31"	"3.94"	"11.95"	"False"	"CHEMBL1116984"	"Inhibition of recombinant GST tagged JAK2 protein after 60 mins using FITC-GGEEEEYFELVKKKK-NH2 substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156975"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL4787224"	""	"0"	"423.52"	"0"	"3.02"	"17g"	"CNC(=O)c1cnc2[nH]ccc2c1NC1CCN(Cc2ccc(OC)c(OC)c2)CC1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	""	""	""	""	""	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL4795901"	""	"0"	"419.53"	"0"	"3.54"	"20d"	"CNC(=O)c1cnc2[nH]ccc2c1NC1CC2CCC(C1)N2Cc1cccc(OC)c1"	"IC50"	"'='"	"89.9"	"nM"	"7.05"	""	""	""	"16.80"	"0.31"	"3.51"	"8.56"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL455428"	""	"0"	"368.42"	"0"	"3.47"	"9b"	"CNC(=O)c1ccc(Nc2nccc(-c3cnc(C)n3C(C)C)n2)cc1F"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1009273"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1152177"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2008"	"None"	""
"CHEMBL1934352"	""	"0"	"547.69"	"1"	"3.51"	"14a"	"Cc1cc(-c2ccccc2N(C)S(C)(=O)=O)n2nc(Nc3ccc(C4CCN(CC(N)=O)CC4)cc3)ncc12"	"IC50"	"'='"	"39.0"	"nM"	"7.41"	""	""	"UO_0000065"	"13.53"	"0.26"	"3.90"	"5.88"	"False"	"CHEMBL1936009"	"Inhibition of JAK2 in GM-CSF-stimulated human TF1 cells preincubated for 1 hr prior to challenge"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3307972"	""
"CHEMBL261849"	"GW632580X"	"0"	"366.42"	"0"	"2.83"	"GW2580"	"COc1ccc(COc2ccc(Cc3cnc(N)nc3N)cc2OC)cc1"	"IC50"	"'>'"	"13000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1959335"	"Inhibition of human JAK2 catalytic domain after by scintillation counting"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1955811"	"1"	"Scientific Literature"	"Proc. Natl. Acad. Sci. U.S.A."	"2005"	"None"	""
"CHEMBL3671149"	""	"0"	"437.45"	"0"	"3.01"	"BDBM127648"	"Cn1cnc(CNC(=O)c2cnn3ccc(N4CCC[C@@H]4c4cc(F)ccc4F)nc23)c1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258322"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675925"	""	"0"	"450.47"	"0"	"1.37"	"BDBM127674"	"NS(=O)(=O)CCNC(=O)c1cnn2ccc(N3CCCC3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258348"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3916880"	""	"0"	"455.51"	"0"	"3.77"	"BDBM127677"	"CC1(O)CCC(NC(=O)c2cnn3ccc(N4CCC[C@@H]4c4cc(F)ccc4F)nc23)CC1"	"IC50"	"'='"	"418.0"	"nM"	"6.38"	""	"258351"	"UO_0000065"	"14.00"	"0.26"	"2.61"	"7.71"	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3671129"	""	"0"	"399.45"	"0"	"3.88"	"BDBM127628"	"CC(C)(C)NC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258302"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL4569508"	""	"0"	"529.59"	"2"	"5.28"	"1"	"O=C(NCC(F)(F)F)c1cc(-c2cnn3cc(-c4ccc(OCCN5CCCCC5)cc4)cnc23)cs1"	"IC50"	"'='"	"2400.0"	"nM"	"5.62"	""	""	"UO_0000065"	"10.61"	"0.21"	"0.34"	"7.83"	"False"	"CHEMBL4479735"	"Inhibition of recombinant human GST-tagged cytoplasmic JAK2 (809 to 1153 residues) expressed in baculovirus expression system by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4477252"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2016"	"None"	""
"CHEMBL4453021"	""	"0"	"426.92"	"0"	"4.67"	"12r"	"CC(Oc1cc(-c2ccc(N3CCNCC3)cc2)cnc1N)c1cc(F)ccc1Cl"	"IC50"	"'='"	"37.0"	"nM"	"7.43"	""	""	"UO_0000065"	"17.41"	"0.34"	"2.76"	"11.72"	"False"	"CHEMBL4341687"	"Inhibition of human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr by Z'-LYTE assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340536"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2019"	"CHEMBL3308860"	""
"CHEMBL4537534"	""	"0"	"363.47"	"0"	"3.59"	"12n"	"CC(Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1ccccc1"	"IC50"	"'='"	"215.0"	"nM"	"6.67"	""	""	"UO_0000065"	"18.34"	"0.34"	"3.08"	"8.55"	"False"	"CHEMBL4341687"	"Inhibition of human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr by Z'-LYTE assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340536"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2019"	"CHEMBL3308860"	""
"CHEMBL4451867"	""	"0"	"378.23"	"1"	"5.31"	"12h"	"CC(Oc1cc(-c2cccnc2)cnc1N)c1c(Cl)ccc(F)c1Cl"	"IC50"	"'='"	"3049.0"	"nM"	"5.52"	""	""	"UO_0000065"	"14.58"	"0.30"	"0.21"	"9.04"	"False"	"CHEMBL4341687"	"Inhibition of human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr by Z'-LYTE assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340536"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2019"	"CHEMBL3308860"	""
"CHEMBL4580439"	""	"0"	"462.36"	"0"	"4.72"	"12g"	"CC(Oc1cc(-c2ccc(N3CCNCC3)nc2)cnc1N)c1c(Cl)ccc(F)c1Cl"	"IC50"	"'='"	"804.0"	"nM"	"6.09"	""	""	"UO_0000065"	"13.18"	"0.27"	"1.37"	"7.99"	"False"	"CHEMBL4341687"	"Inhibition of human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr by Z'-LYTE assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340536"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2019"	"CHEMBL3308860"	""
"CHEMBL4568440"	""	"0"	"464.37"	"1"	"5.43"	"12c"	"CCC(Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl"	"IC50"	"'='"	"100.0"	"nM"	"7.00"	""	""	"UO_0000065"	"15.07"	"0.31"	"1.57"	"8.98"	"False"	"CHEMBL4341687"	"Inhibition of human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr by Z'-LYTE assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340536"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2019"	"CHEMBL3308860"	""
"CHEMBL518323"	""	"0"	"436.32"	"0"	"4.48"	"12b"	"Nc1ncc(-c2cnn(C3CCNCC3)c2)cc1OCc1c(Cl)ccc(F)c1Cl"	"IC50"	"'='"	"572.0"	"nM"	"6.24"	""	""	"UO_0000065"	"14.31"	"0.29"	"1.76"	"8.00"	"False"	"CHEMBL4341687"	"Inhibition of human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr by Z'-LYTE assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340536"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2019"	"CHEMBL3308860"	""
"CHEMBL1933344"	""	"0"	"412.50"	"0"	"4.53"	"2"	"CN1C/C=C/CCOc2cccc(c2)-c2nc(nc3[nH]cnc23)Nc2cccc(c2)C1"	"IC50"	"'='"	"450.0"	"nM"	"6.35"	""	""	"UO_0000065"	"15.39"	"0.28"	"1.82"	"8.04"	"False"	"CHEMBL1937386"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1933054"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL2103874"	"OCLACITINIB"	"0"	"337.45"	"0"	"1.50"	"3"	"CNS(=O)(=O)C[C@H]1CC[C@H](N(C)c2ncnc3[nH]ccc23)CC1"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	""	"UO_0000065"	"22.95"	"0.46"	"6.24"	"8.51"	"False"	"CHEMBL4481925"	"Inhibition of human recombinant JAK2 (808 to 1132 residues) by Z-Lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480435"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL3671140"	""	"0"	"469.49"	"0"	"3.68"	"BDBM127639"	"O=C(O)CC1CCN(C(=O)c2cnn3ccc(N4CCCC4c4cc(F)ccc4F)nc23)CC1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258313"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675910"	""	"0"	"413.43"	"0"	"2.56"	"BDBM127659"	"CC1(O)CN(C(=O)c2cnn3ccc(N4CCC[C@@H]4c4cc(F)ccc4F)nc23)C1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258333"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675916"	""	"0"	"410.43"	"0"	"3.38"	"BDBM127665"	"CC(C)(C#N)NC(=O)c1cnn2ccc(N3CCCC3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258339"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675964"	""	"0"	"399.43"	"0"	"2.33"	"BDBM127716"	"COCCOc1ccc(F)cc1[C@H]1CCCN1c1ccn2ncc(C(N)=O)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258390"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676064"	""	"0"	"424.48"	"0"	"2.56"	"BDBM127824"	"Cc1ncc(F)cc1C1CCCN1c1ccn2ncc(C(=O)N[C@@H]3CCC[C@H]3O)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258493"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676072"	""	"0"	"495.56"	"0"	"3.63"	"BDBM127833"	"CC1(C)OCC(COc2cc(F)cc([C@H]3CCCN3c3ccn4ncc(C(=O)NC5CC5)c4n3)c2)O1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258501"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675977"	""	"0"	"410.45"	"0"	"2.25"	"BDBM127730"	"O=C(N[C@H]1CCC[C@@H]1O)c1cnn2ccc(N3CCCC3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258404"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3955007"	""	"0"	"438.51"	"0"	"2.95"	"BDBM127821"	"Cc1ncc(F)cc1C1CCCN1c1ccn2ncc(C(=O)NC3CCC(O)CC3)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258490"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL1934341"	""	"0"	"456.55"	"0"	"3.30"	"3g"	"NC(=O)CN1CCC(c2ccc(Nc3ncc4ccc(-c5cccc(CO)c5)n4n3)cc2)CC1"	"IC50"	"'='"	"27.0"	"nM"	"7.57"	""	""	"UO_0000065"	"16.58"	"0.30"	"4.27"	"6.96"	"False"	"CHEMBL1936009"	"Inhibition of JAK2 in GM-CSF-stimulated human TF1 cells preincubated for 1 hr prior to challenge"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3307972"	""
"CHEMBL1934350"	""	"0"	"545.67"	"1"	"3.08"	"3p"	"CS(=O)(=O)N1Cc2cccc(-c3ccc4cnc(Nc5ccc(C6CCN(CC(N)=O)CC6)cc5)nn34)c2C1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1936009"	"Inhibition of JAK2 in GM-CSF-stimulated human TF1 cells preincubated for 1 hr prior to challenge"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3307972"	""
"CHEMBL1934335"	""	"0"	"456.55"	"0"	"3.81"	"3a"	"COc1ccccc1-c1ccc2cnc(Nc3ccc(C4CCN(CC(N)=O)CC4)cc3)nn12"	"IC50"	"'='"	"0.6"	"nM"	"9.22"	""	""	"UO_0000065"	"20.20"	"0.37"	"5.41"	"9.43"	"False"	"CHEMBL1936085"	"Inhibition of human recombinant JAK2 expressed in baculovirus expression system after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL1934338"	""	"0"	"457.54"	"0"	"3.21"	"3d"	"COc1ccc(-c2ccc3cnc(Nc4ccc(C5CCN(CC(N)=O)CC5)cc4)nn23)cn1"	"IC50"	"'='"	"0.77"	"nM"	"9.11"	""	""	"UO_0000065"	"19.92"	"0.37"	"5.90"	"8.23"	"False"	"CHEMBL1936085"	"Inhibition of human recombinant JAK2 expressed in baculovirus expression system after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL1934339"	""	"0"	"519.63"	"1"	"3.18"	"3e"	"CS(=O)(=O)Nc1cccc(-c2ccc3cnc(Nc4ccc(C5CCN(CC(N)=O)CC5)cc4)nn23)c1"	"IC50"	"'='"	"0.22"	"nM"	"9.66"	""	""	"UO_0000065"	"18.59"	"0.36"	"6.48"	"7.17"	"False"	"CHEMBL1936085"	"Inhibition of human recombinant JAK2 expressed in baculovirus expression system after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL1934340"	""	"0"	"533.66"	"1"	"3.20"	"3f"	"CN(c1cccc(-c2ccc3cnc(Nc4ccc(C5CCN(CC(N)=O)CC5)cc4)nn23)c1)S(C)(=O)=O"	"IC50"	"'='"	"0.09"	"nM"	"10.05"	""	""	"UO_0000065"	"18.82"	"0.36"	"6.85"	"7.98"	"False"	"CHEMBL1936085"	"Inhibition of human recombinant JAK2 expressed in baculovirus expression system after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL1934352"	""	"0"	"547.69"	"1"	"3.51"	"14a"	"Cc1cc(-c2ccccc2N(C)S(C)(=O)=O)n2nc(Nc3ccc(C4CCN(CC(N)=O)CC4)cc3)ncc12"	"IC50"	"'='"	"3.6"	"nM"	"8.44"	""	""	"UO_0000065"	"15.42"	"0.30"	"4.93"	"6.71"	"False"	"CHEMBL1936085"	"Inhibition of human recombinant JAK2 expressed in baculovirus expression system after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL1934353"	""	"0"	"568.10"	"1"	"3.85"	"14b"	"CN(c1ccccc1-c1cc(Cl)c2cnc(Nc3ccc(C4CCN(CC(N)=O)CC4)cc3)nn12)S(C)(=O)=O"	"IC50"	"'='"	"2.5"	"nM"	"8.60"	""	""	"UO_0000065"	"15.14"	"0.30"	"4.75"	"6.83"	"False"	"CHEMBL1936085"	"Inhibition of human recombinant JAK2 expressed in baculovirus expression system after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL1934336"	""	"0"	"533.66"	"1"	"3.20"	"3b"	"CN(c1ccccc1-c1ccc2cnc(Nc3ccc(C4CCN(CC(N)=O)CC4)cc3)nn12)S(C)(=O)=O"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	""	"UO_0000065"	"14.66"	"0.28"	"4.62"	"6.21"	"False"	"CHEMBL1936009"	"Inhibition of JAK2 in GM-CSF-stimulated human TF1 cells preincubated for 1 hr prior to challenge"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3307972"	""
"CHEMBL3961053"	""	"0"	"545.64"	"1"	"4.09"	"45"	"O=C(NO)C1CCN(CCOc2ccc3cc2COC/C=C/COCc2cccc(c2)-c2ccnc(n2)N3)CC1"	"IC50"	"'='"	"0.97"	"nM"	"9.01"	""	""	"UO_0000065"	"16.52"	"0.31"	"4.92"	"7.63"	"False"	"CHEMBL3877344"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]ATP addition measured after 120 mins by Hotspot assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3877241"	"1"	"Scientific Literature"	"J Med Chem"	"2016"	"None"	""
"CHEMBL1081978"	""	"0"	"489.53"	"0"	"4.74"	"9"	"COc1cc(Nc2nc3cccc(-c4ccc(C(=O)N5CCOCC5)cc4)c3o2)cc(OC)c1OC"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	""	"UO_0000065"	"16.54"	"0.31"	"3.36"	"8.50"	"False"	"CHEMBL1102770"	"Inhibition of GST-tagged JAK2 assessed as inhibition of biotinylated JAK3tide peptide phosphorylation after 60 mins by caliper mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154949"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1081663"	""	"0"	"470.53"	"0"	"4.41"	"12"	"CN(C)C(=O)c1ccc(Nc2nc3cccc(-c4ccc(C(=O)N5CCOCC5)cc4)c3o2)cc1"	"IC50"	"'='"	"39.0"	"nM"	"7.41"	""	""	"UO_0000065"	"15.75"	"0.29"	"3.00"	"8.43"	"False"	"CHEMBL1102770"	"Inhibition of GST-tagged JAK2 assessed as inhibition of biotinylated JAK3tide peptide phosphorylation after 60 mins by caliper mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154949"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL595396"	""	"0"	"277.37"	"0"	"4.74"	"13d"	"CC(C)(C)C1Nc2ccccc2-c2ccnc3[nH]cc1c23"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL600562"	""	"0"	"351.33"	"1"	"5.16"	"13r"	"Fc1ccc(F)c(C2Nc3ccccc3-c3ccnc4[nH]cc2c34)c1F"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL592269"	""	"0"	"354.41"	"0"	"4.10"	"13af"	"CNC(=O)c1ccc(C2Nc3ccccc3-c3ccnc4[nH]cc2c34)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL602100"	""	"0"	"386.41"	"0"	"3.56"	"23"	"CCOC(=O)C1(c2ccc(O)cc2)Nc2ccccc2-c2ncnc3[nH]cc1c23"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL589634"	""	"0"	"355.40"	"0"	"4.07"	"26"	"COc1ccc(C2NC(=O)c3ccccc3-c3ccnc4[nH]cc2c34)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL604695"	""	"0"	"311.39"	"0"	"4.94"	"13i"	"c1ccc(CC2Nc3ccccc3-c3ccnc4[nH]cc2c34)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL594686"	""	"0"	"293.37"	"0"	"3.86"	"13j"	"OCCCCC1Nc2ccccc2-c2ccnc3[nH]cc1c23"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL608999"	""	"0"	"279.34"	"0"	"3.47"	"13k"	"OCCCC1Nc2ccccc2-c2ccnc3[nH]cc1c23"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL1789941"	"RUXOLITINIB"	"4"	"306.37"	"0"	"3.47"	"Ruxolitinib"	"N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	""	"UO_0000065"	"26.43"	"0.48"	"4.63"	"9.73"	"False"	"CHEMBL3784147"	"Inhibition of JAK2 in human CD34+ cells assessed as inhibition of EPO-mediated cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"CD34+ cell"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3779778"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3798894"	""	"0"	"371.40"	"0"	"2.99"	"14f"	"Cn1c(C(N)=O)cc2c(-c3ccc(NC(=O)c4ccccc4)cc3)ncnc21"	"IC50"	"'>'"	"20000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3802364"	"Inhibition of JAK2 in GMCSF-stimulated human TF1 cells assessed as suppression of STAT5 phosphorylation preincubated for 2 hrs followed by GMCSF stimulation for 50 mins by FACS reader analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"CHEMBL3307972"	""
"CHEMBL3298194"	""	"0"	"416.44"	"1"	"5.14"	"27"	"COc1cc(Nc2nc3cccc(-c4cccc5[nH]cnc45)c3o2)cc(OC)c1OC"	"IC50"	"'='"	"460.0"	"nM"	"6.34"	""	""	"UO_0000065"	"15.22"	"0.28"	"1.20"	"6.71"	"False"	"CHEMBL3368761"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3297653"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL2181310"	""	"0"	"490.58"	"1"	"5.10"	"22c, 85:15 trans/cis mixture"	"Fc1cnc2nc1-c1cccc(c1)COCC=CCOCc1cc(ccc1OCCN1CCCC1)N2"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	""	"UO_0000065"	"15.84"	"0.29"	"2.67"	"11.30"	"False"	"CHEMBL2184201"	"Inhibition of recombinant JAK2 using Poly (Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176955"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL2181317"	""	"0"	"389.46"	"0"	"4.75"	"16c, 85:15 trans/cis mixture"	"COc1ccc2cc1COCC=CCCOc1cccc(c1)-c1ccnc(n1)N2"	"IC50"	"'='"	"130.0"	"nM"	"6.89"	""	""	"UO_0000065"	"17.68"	"0.32"	"2.14"	"10.51"	"False"	"CHEMBL2184201"	"Inhibition of recombinant JAK2 using Poly (Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176955"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL4637190"	""	"0"	"426.46"	"0"	"0.65"	"16"	"C[C@@H]1[C@@H]2CN(c3nc(Nc4cnn(CCO)c4)ncc3F)C[C@]12NC(=O)[C@H]1C[C@@H]1C#N"	"IC50"	"'='"	"676.0"	"nM"	"6.17"	""	""	"UO_0000065"	"14.47"	"0.27"	"5.52"	"4.67"	"False"	"CHEMBL4620433"	"Inhibition of human recombinant JAK2 assessed as level of phosphorylation in presence of peptide substrate FITC-KGGEEEEYFELVKK and ATP by mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4619733"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2020"	"None"	""
"CHEMBL4635104"	""	"0"	"407.40"	"0"	"1.69"	"20"	"C[C@@H]1[C@@H]2CN(c3nc(Nc4cnn(C)c4)ncc3F)C[C@]12NC(=O)[C@H]1CC1(F)F"	"IC50"	"'='"	"1132.0"	"nM"	"5.95"	""	""	"UO_0000065"	"14.60"	"0.28"	"4.26"	"6.76"	"False"	"CHEMBL4620433"	"Inhibition of human recombinant JAK2 assessed as level of phosphorylation in presence of peptide substrate FITC-KGGEEEEYFELVKK and ATP by mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4619733"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2020"	"None"	""
"CHEMBL3642308"	""	"0"	"470.58"	"1"	"5.20"	"BDBM99578"	"CC(C)(C)OC(=O)N1CCN(c2ccc(Nc3nc4cccc(-c5ccccc5)n4n3)cc2)CC1"	"IC50"	"'='"	"6.6"	"nM"	"8.18"	""	"216268"	"UO_0000065"	"17.38"	"0.32"	"2.98"	"10.91"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL4638696"	""	"0"	"261.32"	"0"	"2.10"	"17"	"Cc1[nH]nc2[nH]c(=O)c(CO)c(C3CCCCC3)c12"	"IC50"	"'>'"	"40000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"Tofacitinib"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"120.0"	"nM"	"6.92"	""	""	"UO_0000065"	"22.16"	"0.41"	"5.38"	"7.78"	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL4649054"	""	"0"	"314.39"	"0"	"2.11"	"25"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](C(=O)NC4CC4)CC3)c12"	"IC50"	"'>'"	"40000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL4632897"	""	"0"	"342.44"	"0"	"2.89"	"26"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](NC(=O)C4CCCC4)CC3)c12"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL3703022"	""	"0"	"390.85"	"0"	"2.97"	"BDBM147732"	"CN[C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(Cl)c(F)c3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"26.0"	"nM"	"7.58"	""	"285666"	"UO_0000065"	"19.41"	"0.38"	"4.62"	"6.97"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4787731"	""	"0"	"393.49"	"0"	"3.14"	"31l"	"COc1cccc(CN2CC[C@@H](Nc3c(C(N)=O)cnc4[nH]ccc34)C[C@H]2C)c1"	"IC50"	"'='"	"57.6"	"nM"	"7.24"	""	""	""	"18.40"	"0.34"	"4.10"	"7.52"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL4763821"	""	"0"	"393.49"	"0"	"3.01"	"17f"	"CNC(=O)c1cnc2[nH]ccc2c1NC1CCN(Cc2ccc(OC)cc2)CC1"	"IC50"	"'='"	"3540.0"	"nM"	"5.45"	""	""	""	"13.85"	"0.26"	"2.44"	"6.62"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL4787974"	""	"0"	"423.95"	"0"	"4.18"	"20c"	"CNC(=O)c1cnc2[nH]ccc2c1NC1CC2CCC(C1)N2Cc1ccc(Cl)cc1"	"IC50"	"'='"	"2590.0"	"nM"	"5.59"	""	""	""	"13.18"	"0.25"	"1.41"	"7.65"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL4787133"	""	"0"	"407.52"	"0"	"3.40"	"30d"	"CNC(=O)c1cnc2[nH]ccc2c1NC1CCCN(Cc2cccc(OC)c2)CC1"	"IC50"	"'='"	"4.34"	"nM"	"8.36"	""	""	""	"20.52"	"0.38"	"4.96"	"10.16"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL4744772"	""	"0"	"402.50"	"0"	"3.26"	"31j"	"CNC(=O)c1cnc2[nH]ccc2c1N[C@@H]1CCN(Cc2ccc(C#N)cc2)[C@H](C)C1"	"IC50"	"'='"	"4.46"	"nM"	"8.35"	""	""	""	"20.75"	"0.38"	"5.09"	"8.62"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL4746186"	""	"0"	"407.52"	"0"	"3.40"	"31e"	"CNC(=O)c1cnc2[nH]ccc2c1N[C@@H]1CCN(Cc2ccc(OC)cc2)[C@@H](C)C1"	"IC50"	"'='"	"817.0"	"nM"	"6.09"	""	""	""	"14.94"	"0.28"	"2.69"	"7.40"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL3928976"	""	"0"	"587.46"	"2"	"5.69"	"6d; BMS-986143"	"Cc1c(-c2c(Cl)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)cc2c(Cl)cccn2c1=O"	"IC50"	"'='"	"1000.0"	"nM"	"6.00"	""	""	""	""	""	""	""	"False"	"CHEMBL4672879"	"Inhibition of JAK2 (unknown origin)"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4665894"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2020"	"None"	""
"CHEMBL2178806"	""	"0"	"352.79"	"0"	"3.13"	"8"	"Cc1cc(NC(=O)c2cnn3cccnc23)n(-c2cccc(Cl)c2)n1"	"IC50"	"'='"	"1100.0"	"nM"	"5.96"	""	""	"UO_0000065"	"16.89"	"0.33"	"2.83"	"7.73"	"False"	"CHEMBL2186598"	"Inhibition of JAK2 V617F mutant in human SET2 cells assessed as reduction in STAT5 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176876"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL3645108"	""	"0"	"346.39"	"0"	"3.49"	"BDBM99882"	"COc1ccccc1CNc1cccn2nc(Nc3ccncc3)nc12"	"IC50"	"'='"	"54.84"	"nM"	"7.26"	""	"216550"	"UO_0000065"	"20.96"	"0.38"	"3.77"	"9.51"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL2181314"	""	"0"	"490.58"	"1"	"5.10"	"22g, 85:15 trans/cis mixture"	"Fc1ccc2cc1COCC=CCOCc1cc(ccc1OCCN1CCCC1)Nc1nccc-2n1"	"IC50"	"'='"	"25.0"	"nM"	"7.60"	""	""	"UO_0000065"	"15.50"	"0.29"	"2.50"	"11.06"	"False"	"CHEMBL2184201"	"Inhibition of recombinant JAK2 using Poly (Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176955"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL2181085"	""	"0"	"374.44"	"0"	"4.07"	"21k, 85:15 trans/cis mixture"	"Nc1cc2cc(c1)Nc1nccc(n1)-c1cccc(c1)COCC=CCOC2"	"IC50"	"'='"	"35.0"	"nM"	"7.46"	""	""	"UO_0000065"	"19.91"	"0.36"	"3.39"	"9.06"	"False"	"CHEMBL2184201"	"Inhibition of recombinant JAK2 using Poly (Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176955"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1789941"	"RUXOLITINIB"	"4"	"306.37"	"0"	"3.47"	"5"	"N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"8.8"	"nM"	"8.06"	""	""	"UO_0000065"	"26.29"	"0.48"	"4.59"	"9.68"	"False"	"CHEMBL3299201"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3297690"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL1921819"	""	"0"	"562.74"	"1"	"4.78"	"35"	"C[C@H](O)CN1CCC(c2ccc(Nc3ncc4ccc(-c5cccc(S(=O)(=O)NC(C)(C)C)c5)n4n3)cc2)CC1"	"IC50"	"'='"	"1.5"	"nM"	"8.82"	""	""	"UO_0000065"	"15.68"	"0.30"	"4.04"	"7.89"	"False"	"CHEMBL1926252"	"Inhibition of human recombinant JAK2 using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate after 20 mins by fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1921765"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1923572"	""	"0"	"423.50"	"0"	"3.40"	"10"	"COc1ccccc1-c1ccc2cnc(Nc3ccc(S(=O)(=O)N(C)C)cc3)nn12"	"IC50"	"'='"	"2.1"	"nM"	"8.68"	""	""	"UO_0000065"	"20.49"	"0.40"	"5.28"	"9.77"	"False"	"CHEMBL1926252"	"Inhibition of human recombinant JAK2 using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate after 20 mins by fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1921765"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1821735"	""	"0"	"491.62"	"0"	"3.29"	"20"	"CN1CCN(c2ccc(Nc3ncc4ccc(-c5ccccc5N(C)S(C)(=O)=O)n4n3)cc2)CC1"	"IC50"	"'='"	"1.6"	"nM"	"8.80"	""	""	"UO_0000065"	"17.89"	"0.34"	"5.51"	"10.22"	"False"	"CHEMBL1926252"	"Inhibition of human recombinant JAK2 using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate after 20 mins by fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1921765"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1945567"	""	"0"	"508.64"	"1"	"4.47"	"27g"	"CCS(=O)(=O)CCOc1ccc2cc1CN(C)C/C=C/CCOc1cccc(c1)-c1ccnc(n1)N2"	"IC50"	"'='"	"110.0"	"nM"	"6.96"	""	""	"UO_0000065"	"13.68"	"0.26"	"2.49"	"7.43"	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1945706"	""	"0"	"514.67"	"1"	"4.28"	"27o"	"CN1CCN(CCOc2ccc3cc2CN(C)C/C=C/CCOc2cccc(c2)-c2ccnc(n2)N3)CC1"	"IC50"	"'='"	"220.0"	"nM"	"6.66"	""	""	"UO_0000065"	"12.94"	"0.24"	"2.38"	"10.09"	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1938658"	""	"0"	"515.71"	"1"	"3.84"	"24"	"CC(C)(C)NS(=O)(=O)c1ccc(-c2cc3c(N)ncc(C(=O)NCCN4CCCCC4)c3s2)cc1"	"IC50"	"'='"	"2130.0"	"nM"	"5.67"	""	""	"UO_0000065"	"11.00"	"0.22"	"1.83"	"4.83"	"False"	"CHEMBL1941390"	"Inhibition of TEL-fused JAK2 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3307634"	""
"CHEMBL1938645"	""	"0"	"430.53"	"0"	"4.63"	"10"	"Nc1ncc(C(=O)Nc2ccccc2)c2sc(-c3ccc(N4CCOCC4)cc3)cc12"	"IC50"	"'='"	"72.0"	"nM"	"7.14"	""	""	"UO_0000065"	"16.59"	"0.31"	"2.51"	"8.88"	"False"	"CHEMBL1941383"	"Inhibition of human recombinant N-terminal GST-tagged JAK2 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308860"	""
"CHEMBL1938651"	""	"0"	"339.46"	"0"	"4.20"	"16"	"CNC(=O)c1cnc(N)c2cc(-c3ccc(C(C)(C)C)cc3)sc12"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	""	"UO_0000065"	"23.57"	"0.46"	"3.80"	"11.76"	"False"	"CHEMBL1941383"	"Inhibition of human recombinant N-terminal GST-tagged JAK2 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308860"	""
"CHEMBL1938659"	""	"0"	"517.68"	"1"	"2.68"	"25"	"CC(C)(C)NS(=O)(=O)c1ccc(-c2cc3c(N)ncc(C(=O)NCCN4CCOCC4)c3s2)cc1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	""	"UO_0000065"	"16.80"	"0.34"	"6.02"	"6.87"	"False"	"CHEMBL1941383"	"Inhibition of human recombinant N-terminal GST-tagged JAK2 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308860"	""
"CHEMBL1923584"	""	"0"	"448.96"	"0"	"4.55"	"25"	"COc1ccccc1-c1ccc2cnc(Nc3ccc(N4CCN(C)CC4)c(Cl)c3)nn12"	"IC50"	"'='"	"0.5"	"nM"	"9.30"	""	""	"UO_0000065"	"20.72"	"0.40"	"4.75"	"16.06"	"False"	"CHEMBL1926252"	"Inhibition of human recombinant JAK2 using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate after 20 mins by fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1921765"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1789941"	"RUXOLITINIB"	"4"	"306.37"	"0"	"3.47"	"5"	"N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"677.0"	"nM"	"6.17"	""	""	"UO_0000065"	"20.14"	"0.37"	"2.70"	"7.42"	"True"	"CHEMBL3299209"	"Inhibition of JAK2 homodimer in human CD34+ cells spiked into human whole blood assessed as inhibition of EPO-induced STAT-5 phosphorylation preincubated for 45 mins followed by EPO addition measured after 15 mins by FACS analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"CHEMBL3638178"	"Blood"	"CD34+ cell"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3297690"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL1873475"	"IBRUTINIB"	"4"	"440.51"	"0"	"4.22"	"Ibrutinib"	"C=CC(=O)N1CCC[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4610789"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using Ulight-Poly GT as substrate incubated for 2 hrs by Lanthascreen TR-FRET assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610007"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2020"	"None"	""
"CHEMBL481585"	""	"0"	"244.69"	"0"	"2.86"	"10"	"Nc1n[nH]c2ccc(-c3cccc(Cl)n3)cc12"	"IC50"	"'='"	"5800.0"	"nM"	"5.24"	""	""	"UO_0000065"	"21.40"	"0.42"	"2.38"	"7.75"	"False"	"CHEMBL1011746"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139271"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL482188"	""	"0"	"358.47"	"0"	"3.20"	"21"	"Cc1cc(-c2ccc(S(=O)(=O)NC(C)(C)C)cc2)cc2c(N)n[nH]c12"	"IC50"	"'='"	"770.0"	"nM"	"6.11"	""	""	"UO_0000065"	"17.05"	"0.33"	"2.91"	"6.06"	"False"	"CHEMBL1011746"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139271"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL3675936"	""	"0"	"431.44"	"0"	"1.82"	"BDBM127687"	"CC(CO)(CO)NC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258361"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675968"	""	"0"	"368.42"	"0"	"2.74"	"BDBM127720"	"CC(C)NC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258394"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676091"	""	"0"	"447.47"	"0"	"2.86"	"BDBM127856"	"Cc1ccc(NC(=O)c2cnn3ccc(N4CCC[C@@H]4c4cc(F)cn(C)c4=O)nc23)cn1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258521"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676017"	""	"0"	"430.44"	"0"	"0.70"	"BDBM127770"	"COc1ncc(F)cc1[C@H]1CCCN1c1ccn2ncc(C(=O)NC[C@H](O)CO)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258444"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676024"	""	"0"	"370.39"	"0"	"1.97"	"BDBM127780"	"CNC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)cnc3OC)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258451"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676026"	""	"0"	"400.41"	"0"	"1.34"	"BDBM127782"	"COc1ncc(F)cc1[C@H]1CCCN1c1ccn2ncc(C(=O)NCCO)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258453"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676045"	""	"0"	"401.42"	"0"	"2.46"	"BDBM127804"	"C[C@@H](CO)NC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258473"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676058"	""	"0"	"394.45"	"0"	"3.20"	"BDBM127817"	"Cc1ncc(F)cc1C1CCCN1c1ccn2ncc(C(=O)NC3(C)CC3)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258486"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675980"	""	"0"	"380.43"	"0"	"2.74"	"BDBM127733"	"O=C(NCC1CC1)c1cnn2ccc(N3CCCC3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258407"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676008"	""	"0"	"390.37"	"0"	"2.60"	"BDBM127761"	"O=C(NCC(F)F)c1cnn2ccc(N3CCC[C@@H]3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258435"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676010"	""	"0"	"424.48"	"0"	"2.64"	"BDBM127763"	"O=C(N[C@@H]1CCCC[C@H]1O)c1cnn2ccc(N3CCC[C@@H]3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258437"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676023"	""	"0"	"472.52"	"0"	"3.09"	"BDBM127779"	"COc1ncc(F)cc1[C@H]1CCCN1c1ccn2ncc(C(=O)NOCCOC(C)(C)C)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258450"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676031"	""	"0"	"430.44"	"0"	"0.70"	"BDBM127787"	"COc1ncc(F)cc1[C@H]1CCCN1c1ccn2ncc(C(=O)NC(CO)CO)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258458"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3671144"	""	"0"	"413.43"	"0"	"2.60"	"BDBM127643"	"O=C(NC1(CO)CC1)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258317"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675913"	""	"0"	"423.49"	"0"	"3.24"	"BDBM127662"	"O=C(N[C@H]1CC[C@H](O)CC1)c1cnn2ccc(N3CCC[C@@H]3c3cccc(F)c3)nc12"	"IC50"	"'='"	"278.0"	"nM"	"6.56"	""	"258336"	"UO_0000065"	"15.48"	"0.29"	"3.32"	"7.92"	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675929"	""	"0"	"366.40"	"0"	"2.50"	"BDBM127679"	"O=C(NC1CC1)c1cnn2ccc(N3CCC[C@@H]3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258353"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675932"	""	"0"	"429.45"	"0"	"0.79"	"BDBM127682"	"O=C(NCC(O)CO)c1cnn2ccc(N3CCCC3c3cc(F)ccc3CO)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258357"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675942"	""	"0"	"413.43"	"0"	"3.42"	"BDBM127693"	"O=C(NOCC1CC1)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258367"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676047"	""	"0"	"429.47"	"0"	"3.10"	"BDBM127806"	"CC(C)[C@@H](CO)NC(=O)c1cnn2ccc(N3CCCC3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258475"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676068"	""	"0"	"426.50"	"0"	"2.67"	"BDBM127828"	"CCc1ncc(F)cc1C1CCCN1c1ccn2ncc(C(=O)NCC(C)(C)O)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258497"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL1923587"	""	"0"	"554.12"	"1"	"4.62"	"28"	"CN1CCN(c2ccc(Nc3ncc4ccc(-c5cccc(S(=O)(=O)NC(C)(C)C)c5)n4n3)cc2Cl)CC1"	"IC50"	"'='"	"1.2"	"nM"	"8.92"	""	""	"UO_0000065"	"16.10"	"0.32"	"4.30"	"9.40"	"False"	"CHEMBL1926252"	"Inhibition of human recombinant JAK2 using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate after 20 mins by fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1921765"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1934348"	""	"0"	"506.51"	"1"	"4.13"	"3n"	"NC(=O)CN1CCC(c2ccc(Nc3ncc4ccc(-c5cccc6c5OC(F)(F)O6)n4n3)cc2)CC1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1936009"	"Inhibition of JAK2 in GM-CSF-stimulated human TF1 cells preincubated for 1 hr prior to challenge"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3307972"	""
"CHEMBL1944698"	"ZOTIRACICLIB"	"1"	"372.47"	"0"	"4.66"	"26h, SB1317/TG02"	"CN1C/C=C/CCOc2cccc(c2)-c2ccnc(n2)Nc2cccc(c2)C1"	"IC50"	"'='"	"73.0"	"nM"	"7.14"	""	""	"UO_0000065"	"19.16"	"0.35"	"2.48"	"14.19"	"True"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1945045"	""	"0"	"449.56"	"1"	"5.62"	"26o"	"C1=C/CN(Cc2ccccn2)Cc2cccc(c2)Nc2nccc(n2)-c2cccc(c2)OCC/1"	"IC50"	"'='"	"1350.0"	"nM"	"5.87"	""	""	"UO_0000065"	"13.06"	"0.24"	"0.25"	"9.29"	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1087236"	""	"0"	"404.35"	"0"	"2.83"	"5b"	"O=c1[nH]c2cnc(-n3cnc4cc(C(F)(F)F)ccc43)nc2n1C1CCOCC1"	"IC50"	"'='"	"1800.0"	"nM"	"5.75"	""	""	"UO_0000065"	"14.21"	"0.27"	"2.91"	"6.34"	"False"	"CHEMBL1102456"	"Inhibition of human JAK2 (532-1132) by time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154364"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1088856"	""	"0"	"499.57"	"0"	"4.77"	"16"	"COc1cc(-c2cnc3cccc(-c4ccc(C(=O)N5CCOCC5)c(C)c4)c3n2)cc(OC)c1OC"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	""	"UO_0000065"	"15.41"	"0.28"	"2.93"	"9.27"	"False"	"CHEMBL1116984"	"Inhibition of recombinant GST tagged JAK2 protein after 60 mins using FITC-GGEEEEYFELVKKKK-NH2 substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156975"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1089815"	""	"0"	"522.65"	"1"	"4.89"	"21"	"Cc1cc(-c2cccc3ncc(-c4ccc(C(=O)N5CCOCC5)c(C)c4)nc23)ccc1CN1CCOCC1"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	""	"UO_0000065"	"15.09"	"0.28"	"3.00"	"11.63"	"False"	"CHEMBL1116984"	"Inhibition of recombinant GST tagged JAK2 protein after 60 mins using FITC-GGEEEEYFELVKKKK-NH2 substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156975"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1946150"	""	"0"	"493.63"	"0"	"4.46"	"27t"	"CCS(=O)(=O)CNc1cc2cc(c1)Nc1nccc(n1)-c1cccc(c1)OCC/C=C/CN(C)C2"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	""	"UO_0000065"	"15.69"	"0.30"	"3.28"	"8.03"	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1822511"	""	"0"	"376.42"	"0"	"4.17"	"1"	"COc1cc(Nc2ncc3ccc(-c4ccccc4)n3n2)cc(OC)c1OC"	"IC50"	"'='"	"0.2"	"nM"	"9.70"	""	""	"UO_0000065"	"25.77"	"0.47"	"5.53"	"13.87"	"False"	"CHEMBL1936085"	"Inhibition of human recombinant JAK2 expressed in baculovirus expression system after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL4743499"	""	"0"	"480.62"	"1"	"5.68"	"(S)-1"	"N#CC[C@@H](C1CCCC1)n1cc(-c2nc(Nc3ccc(C4CCNCC4)cc3)nc3[nH]ccc23)cn1"	"IC50"	"'='"	"0.099"	"nM"	"10.00"	""	""	""	"20.82"	"0.38"	"4.32"	"9.33"	"False"	"CHEMBL4714135"	"Inhibition of human JAK2 by radiometric assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEK293F"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706688"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	""
"CHEMBL462168"	""	"0"	"522.48"	"2"	"6.20"	"7j"	"COc1cc2nccc(Oc3ccc4c(NC(=O)c5cccc(C(F)(F)F)c5)nn(C)c4c3)c2cc1OC"	"IC50"	"'='"	"25000000.0"	"nM"	""	"Outside typical range"	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL973643"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1157345"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2008"	"None"	""
"CHEMBL3647790"	""	"0"	"442.95"	"0"	"3.24"	"BDBM147893"	"CC1(CN[C@H]2CCC(n3cc(C(N)=O)c(Nc4ccc(Cl)cc4)n3)[C@@H](C#N)C2)COC1"	"IC50"	"'='"	"47.0"	"nM"	"7.33"	""	"285827"	"UO_0000065"	"16.54"	"0.32"	"4.09"	"6.21"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699467"	""	"0"	"325.37"	"0"	"1.95"	"BDBM147482"	"N#C[C@@H]1CCC[C@@H](O)C1n1cc(C(N)=O)c(Nc2ccccc2)n1"	"IC50"	"'>'"	"1500.0"	"nM"	""	""	"285407"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL1090360"	""	"0"	"587.71"	"2"	"6.28"	"26"	"O=C(Cc1ccccc1)Nc1cccc(-c2nc3sccn3c2-c2ccnc(Nc3cccc(N4CCOCC4)c3)n2)c1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1109692"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156213"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL4788363"	""	"0"	"480.62"	"1"	"5.68"	"(rac)-1"	"N#CCC(C1CCCC1)n1cc(-c2nc(Nc3ccc(C4CCNCC4)cc3)nc3[nH]ccc23)cn1"	"IC50"	"'<'"	"0.05"	"nM"	""	""	""	""	""	""	""	""	"False"	"CHEMBL4714135"	"Inhibition of human JAK2 by radiometric assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEK293F"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706688"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	""
"CHEMBL1682385"	""	"0"	"446.52"	"0"	"2.40"	"25"	"COc1ccc(CC(=O)N2CCN(c3nc(Nc4cc(C)[nH]n4)c4cccn4n3)CC2)cc1"	"IC50"	"'='"	"1.2"	"nM"	"8.92"	""	""	"UO_0000065"	"19.98"	"0.37"	"6.52"	"8.60"	"False"	"CHEMBL1685409"	"Inhibition of JAK2 after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1681645"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1682362"	""	"0"	"485.55"	"0"	"1.98"	"2"	"O=C(NC1CC1)c1cc(Nc2nc(N3CCN(C(=O)Cc4ccccc4)CC3)nn3cccc23)n[nH]1"	"IC50"	"'='"	"2700.0"	"nM"	"5.57"	""	""	"UO_0000065"	"11.47"	"0.21"	"3.59"	"4.51"	"False"	"CHEMBL1685409"	"Inhibition of JAK2 after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1681645"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL4793696"	""	"0"	"378.48"	"0"	"3.33"	"13b"	"Cc1cnc(Nc2ccc3c(c2)CCN3CCO)nc1-c1cnn(C(C)C)c1"	"IC50"	"'='"	"3790.0"	"nM"	"5.42"	""	""	""	"14.32"	"0.26"	"2.09"	"6.85"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL4745971"	""	"0"	"424.52"	"0"	"3.93"	"13m"	"CC(C)n1cc(-c2nc(Nc3ccc4c(c3)CCN(CCCCO)C4)ncc2F)cn1"	"IC50"	"'='"	"604.0"	"nM"	"6.22"	""	""	""	"14.65"	"0.27"	"2.29"	"7.86"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL4743195"	""	"0"	"522.65"	"2"	"5.83"	"13ab"	"Cc1ccc(C(=O)CCC(=O)N2CCc3cc(Nc4ncc(C)c(-c5cnn(C(C)C)c5)n4)ccc3C2)cc1"	"IC50"	"'='"	"626.0"	"nM"	"6.20"	""	""	""	"11.87"	"0.22"	"0.37"	"6.67"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL4789556"	""	"0"	"487.65"	"0"	"4.76"	"13ah"	"CCN(CC)C(=O)/C=C/CN1CCc2cc(Nc3ncc(C)c(-c4cnn(C(C)C)c4)n3)ccc2C1"	"IC50"	"'='"	"329.0"	"nM"	"6.48"	""	""	""	"13.29"	"0.25"	"1.72"	"8.19"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL560446"	""	"0"	"544.23"	"2"	"6.72"	"23b"	"C[C@@H](c1ccccc1)N1CCc2c([nH]c3ccc(Br)cc23)-c2c(I)ccnc21"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1036442"	"Inhibition of recombinant JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1151875"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2009"	"None"	""
"CHEMBL551906"	""	"0"	"528.88"	"2"	"7.84"	"25a"	"Clc1nccc2c1-c1[nH]c3ccc(Br)cc3c1CCN2CC(c1ccccc1)c1ccccc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1036442"	"Inhibition of recombinant JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1151875"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2009"	"None"	""
"CHEMBL4634634"	""	"0"	"365.44"	"0"	"1.44"	"29"	"C[C@@H]1C[C@H]1C(=O)N1CCN(c2cnc(C#N)c(-c3cnn(C)c3)n2)C[C@H]1C"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4603510"	"Inhibition of human recombinant GST tagged JAK2 catalytic domain expressed in baculovirus expression system using Tyr6 peptide as substrate measured after 1 hr in presence of ATP by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4602617"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL4745155"	""	"0"	"413.53"	"0"	"4.61"	"3"	"C=CCCn1cc(-c2nc(Nc3ccc(C4CCNCC4)cc3)nc3[nH]ccc23)cn1"	"IC50"	"'='"	"0.26"	"nM"	"9.59"	""	""	""	"23.18"	"0.42"	"4.98"	"11.49"	"False"	"CHEMBL4714135"	"Inhibition of human JAK2 by radiometric assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEK293F"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706688"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	""
"CHEMBL556596"	""	"0"	"452.78"	"1"	"6.77"	"23a"	"C[C@@H](c1ccccc1)N1CCc2c([nH]c3ccc(Br)cc23)-c2c1ccnc2Cl"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1036442"	"Inhibition of recombinant JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1151875"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2009"	"None"	""
"CHEMBL563555"	""	"0"	"383.50"	"1"	"5.15"	"13a"	"COc1nc(C)cc2c1-c1[nH]c3ccccc3c1CCN2CCc1ccccc1"	"IC50"	"'>'"	"40000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1036442"	"Inhibition of recombinant JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1151875"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2009"	"None"	""
"CHEMBL3895530"	""	"0"	"597.07"	"2"	"5.29"	"BDBM230085"	"COc1cccc2c(=O)n(-c3cccc(-c4c(Cl)cc(C(N)=O)c5[nH]c6cc(C(C)(C)O)ccc6c45)c3C)c(=O)n(C)c12"	"IC50"	"'='"	"1600.0"	"nM"	"5.80"	""	"402018"	"UO_0000065"	"9.71"	"0.18"	"0.51"	"4.38"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3944101"	""	"0"	"571.01"	"2"	"5.18"	"BDBM230152"	"Cc1c(-c2c(Cl)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)cc2c(F)cccn2c1=O"	"IC50"	"'='"	"450.0"	"nM"	"6.35"	""	"402047"	"UO_0000065"	"11.12"	"0.21"	"1.17"	"5.18"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3973901"	""	"0"	"517.59"	"2"	"5.03"	"BDBM230145"	"Cc1nc(C(N)=O)c2[nH]c3cc(C(C)(C)O)ccc3c2c1-c1cccc(-n2cnc3ccccc3c2=O)c1C"	"IC50"	"'='"	"200.0"	"nM"	"6.70"	""	"402087"	"UO_0000065"	"12.94"	"0.23"	"1.67"	"5.28"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4112580"	""	"0"	"336.37"	"0"	"2.68"	"BDBM228644"	"CN(c1ccc(C#N)c(F)c1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"48.7"	"nM"	"7.31"	""	"399536"	"UO_0000065"	"21.74"	"0.40"	"4.63"	"10.18"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3936156"	""	"0"	"571.01"	"2"	"5.41"	"BDBM230091"	"Cc1c(-c2c(Cl)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)[nH]c2c(F)cccc2c1=O"	"IC50"	"'='"	"300.0"	"nM"	"6.52"	""	"402025"	"UO_0000065"	"11.42"	"0.22"	"1.11"	"4.87"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3945518"	""	"0"	"554.55"	"1"	"4.89"	"BDBM230122"	"Cc1c(-c2c(F)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)[nH]c2cc(F)ccc2c1=O"	"IC50"	"'>'"	"2000.0"	"nM"	""	""	"402062"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3944859"	""	"0"	"294.36"	"0"	"3.18"	"BDBM198650"	"N#CCC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"4.6"	"nM"	"8.34"	""	"352728"	"UO_0000065"	"28.32"	"0.52"	"5.16"	"10.09"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3917954"	""	"0"	"426.43"	"0"	"4.31"	"BDBM198478"	"FC1(F)Oc2ccc(NC[C@H]3CC[C@H](c4nnn5cnc6[nH]ccc6c45)CC3)cc2O1"	"IC50"	"'='"	"65.0"	"nM"	"7.19"	""	"352556"	"UO_0000065"	"16.85"	"0.32"	"2.88"	"8.04"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3930431"	""	"0"	"310.41"	"0"	"2.59"	"BDBM198489"	"c1cc2c(ncn3nnc([C@H]4CC[C@H](CN5CCC5)CC4)c23)[nH]1"	"IC50"	"'='"	"35.0"	"nM"	"7.46"	""	"352567"	"UO_0000065"	"24.02"	"0.44"	"4.87"	"12.00"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3939232"	""	"0"	"340.43"	"0"	"1.99"	"BDBM198530"	"OCC1(NC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)CC1"	"IC50"	"'='"	"54.0"	"nM"	"7.27"	""	"352608"	"UO_0000065"	"21.35"	"0.40"	"5.28"	"7.97"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3923711"	""	"0"	"298.39"	"0"	"2.49"	"BDBM198533"	"CCNC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"47.0"	"nM"	"7.33"	""	"352611"	"UO_0000065"	"24.56"	"0.45"	"4.84"	"10.34"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3893196"	""	"0"	"431.57"	"0"	"1.85"	"BDBM198548"	"CCS(=O)(=O)N1CCN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)CC1"	"IC50"	"'='"	"200.0"	"nM"	"6.70"	""	"352626"	"UO_0000065"	"15.52"	"0.30"	"4.85"	"6.73"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3904501"	""	"0"	"428.47"	"0"	"3.19"	"BDBM237717"	"CC(C)(C)OC(=O)N1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"367.0"	"nM"	"6.43"	""	"414821"	"UO_0000065"	"15.02"	"0.28"	"3.25"	"5.10"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4106784"	""	"0"	"424.44"	"0"	"2.41"	"BDBM237755"	"C#CCCOC(=O)N1CC[C@@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@H](C#N)C1"	"IC50"	"'='"	"154.0"	"nM"	"6.81"	""	"414859"	"UO_0000065"	"16.05"	"0.30"	"4.40"	"5.40"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4112307"	""	"0"	"494.53"	"0"	"3.02"	"BDBM237774"	"CC(C)(COC(=O)N1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@H](C#N)C1)n1cccn1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"414878"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4109285"	""	"0"	"428.42"	"0"	"1.79"	"BDBM237778"	"N#C[C@@H]1CN(C(=O)OC2COC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"1110.0"	"nM"	"5.96"	""	"414882"	"UO_0000065"	"13.90"	"0.26"	"4.16"	"4.39"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4113736"	""	"0"	"465.49"	"0"	"3.08"	"BDBM237785"	"N#CCC1(COC(=O)N2CC[C@H](n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)[C@H](C#N)C2)CC1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"414889"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4112560"	""	"0"	"436.39"	"0"	"2.65"	"BDBM237786"	"N#C[C@@H]1CN(C(=O)OCC(F)F)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"1084.0"	"nM"	"5.96"	""	"414890"	"UO_0000065"	"13.67"	"0.26"	"3.31"	"4.72"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4446962"	""	"0"	"468.57"	"1"	"5.04"	"7"	"COc1nn(C)cc1Nc1ncc(C)c(-c2c[nH]c3c(NCc4ccc(C)nc4C)cccc23)n1"	"IC50"	"'='"	"560.0"	"nM"	"6.25"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4406243"	"Inhibition of recombinant human N-terminal GST-tagged JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-labeled GEEPLYWSFPAKKK-NH2 peptide as substrate after 10 mins in presence of 5 mM ATP by caliper mobility shift assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402602"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4551327"	""	"0"	"461.57"	"0"	"2.86"	"10"	"Cc1cnc(NC(=O)C2CC2)nc1-c1c[nH]c2c(NC(=O)[C@H](C)N3CCN(C)CC3)cccc12"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4406243"	"Inhibition of recombinant human N-terminal GST-tagged JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-labeled GEEPLYWSFPAKKK-NH2 peptide as substrate after 10 mins in presence of 5 mM ATP by caliper mobility shift assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402602"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4476801"	""	"0"	"434.50"	"0"	"2.55"	"13"	"Cc1cnc(NC(=O)C2CC2)nc1-c1c[nH]c2c(NC(=O)CN3CCOCC3)cccc12"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4406243"	"Inhibition of recombinant human N-terminal GST-tagged JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-labeled GEEPLYWSFPAKKK-NH2 peptide as substrate after 10 mins in presence of 5 mM ATP by caliper mobility shift assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402602"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4064366"	""	"0"	"524.03"	"1"	"3.34"	"18"	"COc1nn(C)cc1Nc1ncc(Cl)c(-c2c[nH]c3c(NC(=O)[C@@H](C)N4CCN(C)CC4)cccc23)n1"	"IC50"	"'='"	"1800.0"	"nM"	"5.75"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4406243"	"Inhibition of recombinant human N-terminal GST-tagged JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-labeled GEEPLYWSFPAKKK-NH2 peptide as substrate after 10 mins in presence of 5 mM ATP by caliper mobility shift assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402602"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4456630"	""	"0"	"489.62"	"0"	"3.42"	"5"	"N#CC[C@H]1CC[C@H](n2c(CC(=O)N3CCC(N4CCOCC4)CC3)nc3cnc4[nH]ccc4c32)CC1"	"IC50"	"'='"	"243.0"	"nM"	"6.61"	""	""	"UO_0000065"	"13.51"	"0.25"	"3.19"	"6.42"	"False"	"CHEMBL4404829"	"Inhibition of JAK2/JAK2 in human PBMC assessed as reduction in GM-CSF-induced STAT5 phosphorylation pre-incubated for 30 mins before GM-CSF stimulation for 30 mins AlphaLISAassay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402578"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"Tofa"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"38.0"	"nM"	"7.42"	""	""	"UO_0000065"	"23.75"	"0.44"	"5.88"	"8.35"	"False"	"CHEMBL4404829"	"Inhibition of JAK2/JAK2 in human PBMC assessed as reduction in GM-CSF-induced STAT5 phosphorylation pre-incubated for 30 mins before GM-CSF stimulation for 30 mins AlphaLISAassay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402578"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL3949257"	""	"0"	"436.39"	"0"	"4.28"	"BDBM198427"	"Fc1cc(C(F)(F)F)cc(F)c1CN1CCC(c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	"352505"	"UO_0000065"	"18.15"	"0.35"	"3.64"	"12.75"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3928091"	""	"0"	"353.43"	"0"	"1.31"	"BDBM198463"	"O=C1CN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)CCN1"	"IC50"	"'='"	"48.0"	"nM"	"7.32"	""	"352541"	"UO_0000065"	"20.71"	"0.38"	"6.01"	"8.02"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3909024"	""	"0"	"417.47"	"0"	"3.32"	"BDBM198476"	"O=C1COc2cc(NC[C@H]3CC[C@H](c4nnn5cnc6[nH]ccc6c45)CC3)ccc2N1"	"IC50"	"'='"	"21.0"	"nM"	"7.68"	""	"352554"	"UO_0000065"	"18.39"	"0.34"	"4.36"	"7.03"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3899587"	""	"0"	"420.56"	"0"	"3.41"	"BDBM198507"	"OC12CC3CC(C1)C(NC[C@H]1CC[C@H](c4nnn5cnc6[nH]ccc6c45)CC1)C(C3)C2"	"IC50"	"'='"	"270.0"	"nM"	"6.57"	""	"352585"	"UO_0000065"	"15.62"	"0.29"	"3.16"	"7.21"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3906776"	""	"0"	"382.51"	"0"	"3.02"	"BDBM198515"	"O[C@H]1CCCC[C@H]1CNC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"45.0"	"nM"	"7.35"	""	"352593"	"UO_0000065"	"19.21"	"0.36"	"4.33"	"8.06"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3889588"	""	"0"	"404.49"	"0"	"4.30"	"BDBM198526"	"Fc1ccc(C2(NC[C@H]3CC[C@H](c4nnn5cnc6[nH]ccc6c45)CC3)CC2)cc1"	"IC50"	"'='"	"34.0"	"nM"	"7.47"	""	"352604"	"UO_0000065"	"18.46"	"0.34"	"3.17"	"10.53"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL1923569"	""	"0"	"535.67"	"1"	"3.04"	"1"	"C[C@H](O)CN1CCN(c2ccc(Nc3ncc4ccc(-c5ccccc5N(C)S(C)(=O)=O)n4n3)cc2)CC1"	"IC50"	"'='"	"1.14"	"nM"	"8.94"	""	""	"UO_0000065"	"16.70"	"0.32"	"5.90"	"8.41"	"False"	"CHEMBL1926252"	"Inhibition of human recombinant JAK2 using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate after 20 mins by fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1921765"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1923590"	""	"0"	"449.95"	"0"	"3.95"	"31"	"COc1ccc(-c2ccc3cnc(Nc4ccc(N5CCN(C)CC5)c(Cl)c4)nn23)cn1"	"IC50"	"'='"	"0.4"	"nM"	"9.40"	""	""	"UO_0000065"	"20.89"	"0.40"	"5.45"	"13.27"	"False"	"CHEMBL1926252"	"Inhibition of human recombinant JAK2 using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate after 20 mins by fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1921765"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1923591"	""	"0"	"526.07"	"1"	"3.94"	"32"	"CN1CCN(c2ccc(Nc3ncc4ccc(-c5ccccc5N(C)S(C)(=O)=O)n4n3)c(Cl)c2)CC1"	"IC50"	"'='"	"480.0"	"nM"	"6.32"	""	""	"UO_0000065"	"12.01"	"0.24"	"2.38"	"7.34"	"False"	"CHEMBL1926252"	"Inhibition of human recombinant JAK2 using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate after 20 mins by fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1921765"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL4635876"	""	"0"	"380.79"	"0"	"2.95"	"Pyrimidine 1"	"OCCn1cc(Nc2ncc(Cl)c(NCc3cc(F)ccc3F)n2)cn1"	"IC50"	"'='"	"0.3162"	"nM"	"9.50"	""	""	"UO_0000065"	"24.95"	"0.50"	"6.55"	"10.81"	"False"	"CHEMBL4627716"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4627263"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2020"	"None"	""
"CHEMBL1835027"	""	"0"	"298.32"	"0"	"2.55"	"30"	"NC(=O)c1cnc(N2CCCC2)c2c1[nH]c1ccc(F)cc12"	"IC50"	"'='"	"230.0"	"nM"	"6.64"	""	""	"UO_0000065"	"22.25"	"0.41"	"4.09"	"8.85"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835142"	""	"0"	"428.42"	"0"	"3.97"	"53"	"Cn1cc(-c2ccc3c(c2)[nH]c2c(C(N)=O)cnc(N[C@H](C4CC4)C(F)(F)F)c23)cn1"	"IC50"	"'='"	"0.4"	"nM"	"9.40"	""	""	"UO_0000065"	"21.94"	"0.41"	"5.43"	"9.25"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835150"	""	"0"	"440.43"	"0"	"4.21"	"62"	"NC(=O)c1cnc(N[C@H](C2CC2)C(F)(F)F)c2c1[nH]c1cc(-c3ccc(N)nc3)ccc12"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	""	"UO_0000065"	"19.75"	"0.37"	"4.49"	"7.09"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835145"	""	"0"	"442.45"	"0"	"4.36"	"56"	"Cn1cc(-c2ccc3c(c2)[nH]c2c(C(N)=O)cnc(N[C@H](C4CCC4)C(F)(F)F)c23)cn1"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	""	"UO_0000065"	"17.90"	"0.34"	"3.56"	"7.79"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1938642"	""	"0"	"354.44"	"0"	"2.48"	"3"	"NC(=O)c1cnc(N)c2cc(-c3ccc(N4CCOCC4)cc3)sc12"	"IC50"	"'>'"	"25000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1941461"	"Inhibition of JAK2 in human whole blood assessed as inhibition of TPO-stimulated STAT5 phosphorylation preincubated for 30 mins prior to TPO challenge measured after 15 mins by intracellular phosflow staining"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"CHEMBL3638178"	"Blood"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1938656"	""	"0"	"462.60"	"0"	"3.00"	"22"	"COCCNC(=O)c1cnc(N)c2cc(-c3ccc(S(=O)(=O)NC(C)(C)C)cc3)sc12"	"IC50"	"'='"	"3950.0"	"nM"	"5.40"	""	""	"UO_0000065"	"11.68"	"0.24"	"2.40"	"4.38"	"False"	"CHEMBL1941461"	"Inhibition of JAK2 in human whole blood assessed as inhibition of TPO-stimulated STAT5 phosphorylation preincubated for 30 mins prior to TPO challenge measured after 15 mins by intracellular phosflow staining"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"CHEMBL3638178"	"Blood"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1938657"	""	"0"	"475.64"	"0"	"2.91"	"23"	"CN(C)CCNC(=O)c1cnc(N)c2cc(-c3ccc(S(=O)(=O)NC(C)(C)C)cc3)sc12"	"IC50"	"'='"	"7830.0"	"nM"	"5.11"	""	""	"UO_0000065"	"10.74"	"0.22"	"2.20"	"4.35"	"False"	"CHEMBL1941461"	"Inhibition of JAK2 in human whole blood assessed as inhibition of TPO-stimulated STAT5 phosphorylation preincubated for 30 mins prior to TPO challenge measured after 15 mins by intracellular phosflow staining"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"CHEMBL3638178"	"Blood"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1650533"	""	"0"	"463.01"	"0"	"3.22"	"1"	"CCN(Cc1cc(Nc2nc(C)cn3c(-c4cn[nH]c4)cnc23)sn1)C(C)(C)CO.Cl"	"IC50"	"'>'"	"100.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1656192"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649074"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL594687"	""	"0"	"297.36"	"0"	"4.74"	"13l"	"c1ccc(C2Nc3ccccc3-c3ccnc4[nH]cc2c34)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL600874"	""	"0"	"351.33"	"1"	"5.16"	"13s"	"Fc1ccc(C2Nc3ccccc3-c3ccnc4[nH]cc2c34)c(F)c1F"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL591095"	""	"0"	"313.36"	"0"	"4.45"	"13t"	"Oc1ccccc1C1Nc2ccccc2-c2ccnc3[nH]cc1c23"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL602183"	""	"0"	"331.35"	"0"	"4.59"	"13w"	"Oc1ccc(C2Nc3ccccc3-c3ccnc4[nH]cc2c34)c(F)c1"	"IC50"	"'='"	"720.0"	"nM"	"6.14"	""	""	"UO_0000065"	"18.54"	"0.34"	"1.55"	"10.08"	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL599911"	""	"0"	"341.18"	"None"	"None"	"13x"	"OB(O)c1ccc(C2Nc3ccccc3-c3ccnc4[nH]cc2c34)cc1"	"IC50"	"'>'"	"20000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL604246"	""	"0"	"390.47"	"0"	"4.12"	"13ad"	"CS(=O)(=O)Nc1ccc(C2Nc3ccccc3-c3ccnc4[nH]cc2c34)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL589145"	""	"0"	"342.40"	"0"	"4.31"	"14b"	"c1ccc(COCC2Nc3ccccc3-c3ncnc4[nH]cc2c34)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL3665206"	""	"0"	"453.53"	"0"	"1.21"	"BDBM112606"	"CS(=O)(=O)N1CCC[C@H](Nc2nc(N3CC(C#N)C3)ncc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.0485"	"nM"	"10.31"	""	"233843"	"UO_0000065"	"22.74"	"0.44"	"9.10"	"7.17"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642379"	""	"0"	"534.69"	"1"	"3.23"	"BDBM99655"	"CN1CCN(c2ccc(Nc3nc4c(NCc5ccccc5CN(C)S(C)(=O)=O)cccn4n3)cc2)CC1"	"IC50"	"'='"	"35.44"	"nM"	"7.45"	""	"216345"	"UO_0000065"	"13.93"	"0.27"	"4.22"	"7.59"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3699506"	""	"0"	"334.38"	"0"	"2.85"	"BDBM147524"	"N#Cc1ccc(Nc2nn([C@H]3CCCC[C@@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"285454"	"UO_0000065"	"24.06"	"0.44"	"5.20"	"6.68"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702925"	""	"0"	"343.82"	"0"	"3.63"	"BDBM147624"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	"285557"	"UO_0000065"	"23.15"	"0.45"	"4.33"	"8.23"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665194"	""	"0"	"408.49"	"0"	"2.45"	"BDBM112592"	"CSc1ncc(-c2cnc3[nH]ccc3n2)c(N[C@H]2CCCN(C(=O)CC#N)C2)n1"	"IC50"	"'='"	"0.223"	"nM"	"9.65"	""	"233829"	"UO_0000065"	"23.63"	"0.45"	"7.20"	"7.82"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3699525"	""	"0"	"328.35"	"0"	"2.51"	"BDBM147543"	"N#C[C@@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(F)nc2)n1"	"IC50"	"'='"	"75.0"	"nM"	"7.12"	""	"285473"	"UO_0000065"	"21.70"	"0.41"	"4.61"	"6.50"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699476"	""	"0"	"387.47"	"0"	"2.38"	"BDBM147491"	"CS(=O)(=O)c1ccc(Nc2nn(C3CCCC[C@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	"285416"	"UO_0000065"	"19.99"	"0.39"	"5.36"	"5.92"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4226201"	""	"0"	"349.34"	"0"	"1.32"	"22"	"CN(c1ncnc2[nH]ccc12)[C@@H]1CCN(S(=O)(=O)C(F)(F)F)C1"	"IC50"	"'='"	"4500.0"	"nM"	"5.35"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4225016"	""	"0"	"402.44"	"0"	"1.77"	"34"	"CN(c1ncnc2[nH]ccc12)[C@@H]1CCN(S(=O)(=O)c2cccc([N+](=O)[O-])c2)C1"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4228745"	""	"0"	"387.47"	"0"	"1.87"	"38"	"COc1ccc(S(=O)(=O)N2CC[C@@H](N(C)c3ncnc4[nH]ccc34)C2)cc1"	"IC50"	"'='"	"1500.0"	"nM"	"5.82"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL1080395"	""	"0"	"375.43"	"0"	"2.82"	"3"	"NC(=O)c1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"326.0"	"nM"	"6.49"	""	""	"UO_0000065"	"17.28"	"0.32"	"3.67"	"6.95"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1079690"	""	"0"	"455.52"	"0"	"4.25"	"5"	"O=C(NCc1ccco1)c1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"202.0"	"nM"	"6.70"	""	""	"UO_0000065"	"14.70"	"0.27"	"2.44"	"7.24"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1078363"	""	"0"	"428.50"	"0"	"3.29"	"29"	"Cc1cc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)ccc1C(=O)NCC#N"	"IC50"	"'='"	"65.0"	"nM"	"7.19"	""	""	"UO_0000065"	"16.77"	"0.31"	"3.90"	"6.97"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1078933"	""	"0"	"455.57"	"0"	"3.28"	"42"	"CCN1CCN(Cc2ccc(Nc3nccc(-c4ccc(C(=O)NCC#N)cc4)n3)cc2)CC1"	"IC50"	"'='"	"47.0"	"nM"	"7.33"	""	""	"UO_0000065"	"16.09"	"0.29"	"4.05"	"7.54"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL4575735"	""	"0"	"353.81"	"0"	"2.18"	"8o"	"CNc1nc(Nc2cnn(CCCCCC(=O)NO)c2)ncc1Cl"	"IC50"	"'='"	"36.0"	"nM"	"7.44"	""	""	"UO_0000065"	"21.04"	"0.42"	"5.26"	"6.36"	"False"	"CHEMBL4347596"	"Inhibition of recombinant human JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate measured after 60 mins by LANCE assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4346670"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL3694578"	""	"0"	"352.83"	"0"	"4.42"	"BDBM125899"	"Clc1cnc2nc1NCc1cccc(c1)OCCc1cccc(c1)N2"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	"255672"	"UO_0000065"	"22.67"	"0.44"	"3.58"	"13.54"	"False"	"CHEMBL3707544"	"In Vitro Kinase Assay: One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Biochemistry 1999, 269, 94-104. The catalytic domains of human JAK1 (a.a. 837-1142), JAK2 (a.a. 828-1132) and JAK3 (a.a. 781-1124) with an N-terminal His tag were expressed using baculovirus in insect cells and purified. The catalytic activity of JAK1, JAK2 or JAK3 was assayed by measuring the phosphorylation of a biotinylated peptide. The phosphorylated peptide was detected by homogenous time resolved fluorescence (HTRF). IC50s of compounds were measured for each kinase in the reactions that contain the enzyme, ATP and 500 nM peptide in 50 mM Tris (pH 7.8) buffer with 100 mM NaCl, 5 mM DTT, and 0.1 mg/mL (0.01%) BSA. The ATP concentration in the reactions was 90 uM for JAK1, 30 uM for JAK2 and 3 uM for JAK3. Reactions were carried out at room temperature for 1 hr and then stopped with 20 uL 45 mM EDTA."	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639093"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3647796"	""	"0"	"428.92"	"0"	"2.73"	"BDBM147899"	"N#C[C@H]1C[C@@H](NC2(CO)CC2)CCC1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	"285833"	"UO_0000065"	"18.31"	"0.36"	"5.12"	"6.09"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647894"	""	"0"	"481.00"	"0"	"4.16"	"BDBM148006"	"N#C[C@H]1C[C@@H](C(=O)NC(C2CC2)C2CC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"500.0"	"nM"	"6.30"	""	"285941"	"UO_0000065"	"13.10"	"0.25"	"2.14"	"5.01"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3658105"	""	"0"	"650.11"	"2"	"6.41"	"BDBM148395"	"Cc1ccc(NC(=O)c2cc(Cl)cc(C(F)(F)F)c2)cc1N1CCc2nc(Nc3ccc(N4CCN(C)CC4)cc3)ncc2C1=O"	"IC50"	"'='"	"36.0"	"nM"	"7.44"	""	"286791"	"UO_0000065"	"11.45"	"0.22"	"1.03"	"7.94"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651006"	""	"0"	"375.39"	"0"	"3.19"	"BDBM153182"	"C=C(C)C(=O)Nc1cc(-c2ncnc3[nH]cc(C(=O)OCC)c23)ccc1C#N"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294130"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665200"	""	"0"	"460.56"	"0"	"1.43"	"BDBM112598"	"CC[C@@H](CO)Nc1ncc(-c2cnc3[nH]ccc3n2)c(N[C@H]2CCCN(S(C)(=O)=O)C2)n1"	"IC50"	"'='"	"0.0432"	"nM"	"10.36"	""	"233835"	"UO_0000065"	"22.50"	"0.44"	"8.93"	"6.96"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3645012"	""	"0"	"553.64"	"2"	"6.58"	"BDBM99764"	"CC(C)(C)OC(=O)N1CCC(c2ccc(Nc3nc4c(-c5cnn(-c6ccc(F)cc6)c5)cccn4n3)cc2)CC1"	"IC50"	"'='"	"1108.85"	"nM"	"5.96"	""	"216451"	"UO_0000065"	"10.76"	"0.20"	"-0.62"	"6.65"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647890"	""	"0"	"466.97"	"0"	"3.87"	"BDBM148002"	"N#C[C@H]1C[C@@H](C(=O)N2CC3(CCC3)C2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"480.0"	"nM"	"6.32"	""	"285937"	"UO_0000065"	"13.53"	"0.26"	"2.45"	"5.40"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642393"	""	"0"	"520.66"	"1"	"3.36"	"BDBM99671"	"CN1CCN(c2cccc(Nc3nc4c(Nc5ccccc5CN(C)S(C)(=O)=O)cccn4n3)c2)CC1"	"IC50"	"'='"	"453.17"	"nM"	"6.34"	""	"216361"	"UO_0000065"	"12.18"	"0.23"	"2.98"	"6.47"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642323"	""	"0"	"442.52"	"0"	"2.95"	"BDBM99595"	"CS(=O)(=O)c1ccc(-c2cccc3nc(Nc4cccc(S(C)(=O)=O)c4)nn23)cc1"	"IC50"	"'='"	"9.3"	"nM"	"8.03"	""	"216285"	"UO_0000065"	"18.15"	"0.37"	"5.08"	"7.27"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL4539805"	""	"0"	"294.36"	"0"	"2.92"	"11"	"CC(C)Nc1c(C(N)=O)cnn2cc(-c3ccccc3)cc12"	"IC50"	"'='"	"190.0"	"nM"	"6.72"	""	""	"UO_0000065"	"22.83"	"0.42"	"3.80"	"9.28"	"False"	"CHEMBL4339747"	"Inhibition of GST-tagged JAK2 (unknown origin) using fluoresceinated peptide as substrate measured after 3 hrs by electrophoresis method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4339199"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2019"	"None"	""
"CHEMBL4471290"	""	"0"	"322.41"	"0"	"3.56"	"13"	"CC(C)CCNc1c(C(N)=O)cnn2cc(-c3ccccc3)cc12"	"IC50"	"'='"	"220.0"	"nM"	"6.66"	""	""	"UO_0000065"	"20.65"	"0.38"	"3.10"	"9.19"	"False"	"CHEMBL4339747"	"Inhibition of GST-tagged JAK2 (unknown origin) using fluoresceinated peptide as substrate measured after 3 hrs by electrophoresis method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4339199"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2019"	"None"	""
"CHEMBL4447360"	""	"0"	"340.38"	"0"	"1.25"	"22"	"C[C@@H](O)[C@@H](CO)Nc1c(C(N)=O)cnn2cc(-c3ccccc3)cc12"	"IC50"	"'='"	"70.0"	"nM"	"7.16"	""	""	"UO_0000065"	"21.02"	"0.39"	"5.90"	"6.34"	"False"	"CHEMBL4339747"	"Inhibition of GST-tagged JAK2 (unknown origin) using fluoresceinated peptide as substrate measured after 3 hrs by electrophoresis method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4339199"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2019"	"None"	""
"CHEMBL1774054"	""	"0"	"398.42"	"0"	"4.66"	"1b"	"CC(C)Oc1cc(Nc2nc(N[C@@H](C)c3ccc(F)cc3)c(C#N)cc2F)n[nH]1"	"IC50"	"'='"	"688.0"	"nM"	"6.16"	""	""	"UO_0000065"	"15.47"	"0.29"	"1.50"	"6.25"	"False"	"CHEMBL1776838"	"Inhibition of JAK2 after 60 min"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1772962"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1774053"	""	"0"	"380.40"	"0"	"4.75"	"1a"	"C[C@H](Nc1nc(Nc2cc(C3CC3)[nH]n2)c(F)cc1C#N)c1ccc(F)cc1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"22.41"	"0.42"	"3.77"	"9.53"	"False"	"CHEMBL1776838"	"Inhibition of JAK2 after 60 min"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1772962"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL3647769"	""	"0"	"460.50"	"0"	"4.46"	"BDBM147872"	"CC1(C)CCN1[C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(C(F)(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"34.0"	"nM"	"7.47"	""	"285806"	"UO_0000065"	"16.22"	"0.31"	"3.01"	"7.47"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703506"	""	"0"	"373.41"	"0"	"4.38"	"BDBM153150"	"CCOC(=O)c1c[nH]c2ncnc(-c3cccc(OCc4ccccc4)c3)c12"	"IC50"	"'='"	"62.0"	"nM"	"7.21"	""	"294098"	"UO_0000065"	"19.30"	"0.35"	"2.83"	"9.35"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642257"	""	"0"	"372.43"	"0"	"3.37"	"BDBM99515"	"c1cc(-c2ccncc2)c2nc(Nc3ccc(N4CCOCC4)cc3)nn2c1"	"IC50"	"'='"	"5.5"	"nM"	"8.26"	""	"216207"	"UO_0000065"	"22.18"	"0.40"	"4.89"	"12.22"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3115325"	""	"0"	"356.39"	"0"	"1.95"	"10"	"COc1ccc(Nc2nc(N3CCOCC3)c3nc[nH]c3n2)cc1OC"	"IC50"	"'='"	"110.0"	"nM"	"6.96"	""	""	"UO_0000065"	"19.53"	"0.37"	"5.01"	"7.14"	"False"	"CHEMBL3119788"	"Inhibition of JAK2 (unknown origin) by radioactive ATP method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112544"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL3647899"	""	"0"	"505.00"	"1"	"2.12"	"BDBM148011"	"CS(=O)(=O)C1CN(C(=O)[C@H]2CC[C@H](n3cc(C(N)=O)c(Nc4ccc(Cl)cc4)n3)[C@@H](C#N)C2)C1"	"IC50"	"'='"	"49.0"	"nM"	"7.31"	""	"285946"	"UO_0000065"	"14.47"	"0.29"	"5.19"	"4.84"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702935"	""	"0"	"327.36"	"0"	"2.93"	"BDBM147637"	"N#C[C@H]1CCCC(F)[C@@H]1n1cc(C(N)=O)c(Nc2ccccc2)n1"	"IC50"	"'='"	"60.0"	"nM"	"7.22"	""	"285569"	"UO_0000065"	"22.06"	"0.41"	"4.29"	"7.47"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665140"	""	"0"	"364.45"	"0"	"3.08"	"BDBM112527"	"CC(C)CC(=O)N1CC[C@@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.1532"	"nM"	"9.81"	""	"233766"	"UO_0000065"	"26.93"	"0.50"	"6.73"	"11.31"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3589171"	""	"0"	"442.52"	"0"	"3.48"	"8"	"COc1cccc(-c2cc(C(N)=O)c3[nH]c4ccc(C(=O)N5CCN(C)CC5)cc4c3c2)c1"	"IC50"	"'='"	"280.0"	"nM"	"6.55"	""	""	"UO_0000065"	"14.81"	"0.27"	"3.07"	"7.15"	"False"	"CHEMBL3592855"	"Inhibition of JAK2 in human SET2 cells assessed as inhibition of cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3589164"	""	"0"	"468.34"	"0"	"4.87"	"1"	"NC(=O)c1cc(-c2ccc(Cl)c(Cl)c2)cc2c1[nH]c1ccc(C(=O)N3CCOCC3)cc12"	"IC50"	"'='"	"2.4"	"nM"	"8.62"	""	""	"UO_0000065"	"18.40"	"0.37"	"3.75"	"9.75"	"True"	"CHEMBL3592849"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3589167"	""	"0"	"468.34"	"0"	"4.87"	"4"	"NC(=O)c1cc(-c2ccc(Cl)cc2Cl)cc2c1[nH]c1ccc(C(=O)N3CCOCC3)cc12"	"IC50"	"'='"	"6.8"	"nM"	"8.17"	""	""	"UO_0000065"	"17.44"	"0.35"	"3.30"	"9.24"	"False"	"CHEMBL3592849"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3589166"	""	"0"	"429.48"	"0"	"3.57"	"3"	"COc1cccc(-c2cc(C(N)=O)c3[nH]c4ccc(C(=O)N5CCOCC5)cc4c3c2)c1"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	""	"UO_0000065"	"18.15"	"0.33"	"4.23"	"7.98"	"False"	"CHEMBL3592855"	"Inhibition of JAK2 in human SET2 cells assessed as inhibition of cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3589179"	""	"0"	"371.44"	"0"	"3.92"	"16"	"NC(=O)c1cc(-c2ccccc2)cc2c1[nH]c1cc(N3CCOCC3)ccc12"	"IC50"	"'='"	"500.0"	"nM"	"6.30"	""	""	"UO_0000065"	"16.96"	"0.31"	"2.38"	"8.83"	"False"	"CHEMBL3592855"	"Inhibition of JAK2 in human SET2 cells assessed as inhibition of cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3699530"	""	"0"	"449.48"	"0"	"4.18"	"BDBM147548"	"CC(C)(c1ccc(Nc2nn([C@H]3CCCC[C@@H]3C#N)cc2C(N)=O)cc1)[C@H](O)C(F)(F)F"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"285478"	"UO_0000065"	"18.96"	"0.36"	"4.34"	"7.29"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3589170"	""	"0"	"495.41"	"1"	"5.17"	"7"	"CN(C)[C@H]1CCN(C(=O)c2ccc3[nH]c4c(C(N)=O)cc(-c5ccc(Cl)c(Cl)c5)cc4c3c2)C1"	"IC50"	"'='"	"140.0"	"nM"	"6.85"	""	""	"UO_0000065"	"13.83"	"0.28"	"1.68"	"8.31"	"False"	"CHEMBL3592855"	"Inhibition of JAK2 in human SET2 cells assessed as inhibition of cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3622821"	"UPADACITINIB"	"4"	"380.37"	"0"	"2.91"	"11"	"CC[C@@H]1CN(C(=O)NCC(F)(F)F)C[C@@H]1c1cnc2cnc3[nH]ccc3n12"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	""	"UO_0000065"	"21.29"	"0.41"	"5.19"	"10.34"	"False"	"CHEMBL4309397"	"Inhibition of recombinant JAK2 (unknown origin) in presence of 0.1 mM ATP by alpha-screen assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4308837"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL1087898"	""	"0"	"331.38"	"0"	"3.09"	"3"	"Cc1cnc(Nc2cncc(N[C@@H](C)c3ncc(F)cn3)n2)s1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	""	"UO_0000065"	"25.34"	"0.50"	"5.31"	"9.49"	"False"	"CHEMBL1103122"	"Inhibition of recombinant JAK2 kinase in presence of ATP"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154970"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1087268"	""	"0"	"428.54"	"0"	"3.44"	"7a"	"Cc1cnc(Nc2cc(N3CCN(C)CC3)nc(N[C@@H](C)c3ccc(F)cn3)n2)s1"	"IC50"	"'<'"	"3.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1103123"	"Inhibition of recombinant JAK2 kinase in presence of 5 mM ATP"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154970"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL3647737"	""	"0"	"550.61"	"1"	"4.03"	"BDBM147840"	"N#C[C@H]1CC(NC(C2CC2)C2CC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"225.0"	"nM"	"6.65"	""	"285774"	"UO_0000065"	"12.07"	"0.24"	"2.62"	"4.65"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647866"	""	"0"	"462.49"	"0"	"4.35"	"BDBM147978"	"N#C[C@H]1C[C@@H](OC(=O)Nc2ccccc2)CCC1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"107.0"	"nM"	"6.97"	""	"285912"	"UO_0000065"	"15.07"	"0.28"	"2.62"	"5.16"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL1088030"	""	"0"	"416.49"	"0"	"2.92"	"6b"	"Cc1cnc(Nc2cc(N3CCOCC3)nc(N[C@@H](C)c3ncc(F)cn3)n2)s1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"20.46"	"0.40"	"5.60"	"8.44"	"False"	"CHEMBL1103123"	"Inhibition of recombinant JAK2 kinase in presence of 5 mM ATP"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154970"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL4648612"	""	"0"	"257.34"	"0"	"2.85"	"13"	"Cc1[nH]nc2[nH]c(=O)cc(C3CC4CCC3CC4)c12"	"IC50"	"'='"	"330.0"	"nM"	"6.48"	""	""	"UO_0000065"	"25.19"	"0.47"	"3.63"	"10.53"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4647966"	""	"0"	"245.33"	"0"	"2.86"	"15"	"CCc1[nH]nc2[nH]c(=O)cc(C3CCCCC3)c12"	"IC50"	"'='"	"2700.0"	"nM"	"5.57"	""	""	"UO_0000065"	"22.70"	"0.42"	"2.71"	"9.05"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4648246"	""	"0"	"257.34"	"0"	"3.18"	"16"	"O=c1cc(C2CCCCC2)c2c(C3CC3)[nH]nc2[nH]1"	"IC50"	"'='"	"1300.0"	"nM"	"5.89"	""	""	"UO_0000065"	"22.87"	"0.42"	"2.71"	"9.56"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4649054"	""	"0"	"314.39"	"0"	"2.11"	"25"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](C(=O)NC4CC4)CC3)c12"	"IC50"	"'='"	"9400.0"	"nM"	"5.03"	""	""	"UO_0000065"	"15.99"	"0.30"	"2.92"	"5.55"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4632766"	""	"0"	"351.35"	"0"	"2.78"	"29"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](OC(=O)[C@@H]4CC4(F)F)CC3)c12"	"IC50"	"'='"	"120.0"	"nM"	"6.92"	""	""	"UO_0000065"	"19.70"	"0.38"	"4.14"	"7.88"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4647506"	""	"0"	"247.30"	"0"	"1.58"	"33"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](O)CC3)c12"	"IC50"	"'='"	"4600.0"	"nM"	"5.34"	""	""	"UO_0000065"	"21.58"	"0.40"	"3.76"	"6.53"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4639606"	""	"0"	"418.54"	"0"	"4.24"	"37"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](CC(=O)N4CCC(c5ccccc5)C4)CC3)c12"	"IC50"	"'='"	"19.0"	"nM"	"7.72"	""	""	"UO_0000065"	"18.45"	"0.34"	"3.48"	"9.43"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL1923578"	""	"0"	"553.66"	"1"	"3.18"	"17"	"C[C@H](O)CN1CCN(c2ccc(Nc3ncc4ccc(-c5ccccc5N(C)S(C)(=O)=O)n4n3)cc2F)CC1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	""	"UO_0000065"	"16.26"	"0.32"	"5.82"	"8.47"	"False"	"CHEMBL1926252"	"Inhibition of human recombinant JAK2 using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate after 20 mins by fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1921765"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1923582"	""	"0"	"526.07"	"1"	"3.94"	"22"	"CN1CCN(c2ccc(Nc3ncc4ccc(-c5ccccc5N(C)S(C)(=O)=O)n4n3)cc2Cl)CC1"	"IC50"	"'='"	"1.1"	"nM"	"8.96"	""	""	"UO_0000065"	"17.03"	"0.34"	"5.02"	"10.41"	"False"	"CHEMBL1926252"	"Inhibition of human recombinant JAK2 using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate after 20 mins by fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1921765"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL582808"	""	"0"	"375.41"	"0"	"3.25"	"43"	"Nc1nn2cccnc2c1-c1cc(N2CCCC2c2ccc(F)cc2)ncn1"	"IC50"	"'>'"	"20000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1044320"	"Inhibition of JAK2-mediated STAT5 phosphorylation in GMCSF-stimulated human TF1 cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"CHEMBL3307972"	""
"CHEMBL3902006"	""	"0"	"447.49"	"0"	"3.98"	"BDBM147935"	"[C-]#[N+][C@H]1C[C@@H]([N+]2(C)CCC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"33.0"	"nM"	"7.48"	""	"285869"	"UO_0000065"	"16.72"	"0.32"	"3.50"	"9.68"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665172"	""	"0"	"386.48"	"0"	"2.16"	"BDBM112565"	"Cc1c[nH]c2ncc(-c3cccnc3N[C@H]3CCCN(S(C)(=O)=O)C3)nc12"	"IC50"	"'='"	"0.0367"	"nM"	"10.44"	""	"233802"	"UO_0000065"	"27.00"	"0.53"	"8.28"	"10.05"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3645121"	""	"0"	"431.52"	"0"	"0.97"	"BDBM100350"	"CS(=O)(=O)N1CCN(c2ccc(Nc3ncc(C(N)=O)c(NC4CC4)n3)cc2)CC1"	"IC50"	"'='"	"3.2"	"nM"	"8.49"	""	"279118"	"UO_0000065"	"19.69"	"0.39"	"7.52"	"6.36"	"False"	"CHEMBL3707618"	"Time-Resolved Fluorescence Resonance Energy Transfer Assay (TR-FRET): SYK tyrosine phosphorylation activity is measured using the LANCE Technology developed by Perkin Elmer Life and Analytical Sciences (Boston, Mass.). LANCE refers to homogeneous time resolved fluorometry applications using techniques such as time-resolved fluorescence resonance energy transfer assay (TR-FRET) (see generally for procedures in Perkin Elmer Application Note How to Optimize a Tyrosine Kinase Assay Using Time Resolved Fluorescence-Based LANCE Detection, wwww.perkinelmer.com/lifesciences). The assay principle involves detection of a phosphorylated substrate using energy transfer from a phosphospecific europium-labeled antibody to streptavidin-allophycocyanin as an acceptor.To test the ability of candidate molecules to inhibit SYK tyrosine phosphorylation activity, molecules are reconstituted in 30% DMSO and serially diluted 1:3 with the final dilution containing DMSO in the absence of the candidate molecule. The final DMSO concentration in the assay is 3%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638708"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699555"	""	"0"	"311.35"	"0"	"1.77"	"BDBM147573"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccnnc2)n1"	"IC50"	"'='"	"28.0"	"nM"	"7.55"	""	"285503"	"UO_0000065"	"24.26"	"0.45"	"5.78"	"6.17"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL576257"	""	"0"	"338.35"	"0"	"2.83"	"7h"	"Cc1cc(Nc2cnc(C#N)c(N[C@@H](C)c3ccc(F)cn3)n2)n[nH]1"	"IC50"	"'<'"	"3.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1043451"	"Inhibition of JAK2 using 2 mM ATP as a substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156131"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL4449906"	""	"0"	"494.50"	"0"	"3.70"	"7m"	"Cc1cnc(Nc2cc(F)c(N3CCOCC3)c(F)c2)nc1-c1cc2c(o1)CCN(C(=O)CC#N)C2"	"IC50"	"'='"	"586.1"	"nM"	"6.23"	""	""	"UO_0000065"	"12.60"	"0.24"	"2.53"	"5.80"	"False"	"CHEMBL4341349"	"Inhibition of JAK2 in human TF-1 cells assessed as reduction in GM-CSF-induced cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"CHEMBL3307972"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"2"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	""	"UO_0000065"	"28.81"	"0.53"	"7.46"	"10.12"	"False"	"CHEMBL4341343"	"Inhibition of JAK2 (unknown origin) using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition and measured by 30 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4456396"	""	"0"	"505.55"	"1"	"3.22"	"7e"	"Cc1cnc(Nc2cc(F)c(N3CCOCC3)c(F)c2)nc1-c1cc2c(o1)CCN(S(C)(=O)=O)C2"	"IC50"	"'='"	"3.7"	"nM"	"8.43"	""	""	"UO_0000065"	"16.68"	"0.33"	"5.21"	"8.36"	"False"	"CHEMBL4341343"	"Inhibition of JAK2 (unknown origin) using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition and measured by 30 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4456396"	""	"0"	"505.55"	"1"	"3.22"	"7e"	"Cc1cnc(Nc2cc(F)c(N3CCOCC3)c(F)c2)nc1-c1cc2c(o1)CCN(S(C)(=O)=O)C2"	"IC50"	"'='"	"1993.0"	"nM"	"5.70"	""	""	"UO_0000065"	"11.28"	"0.22"	"2.48"	"5.66"	"False"	"CHEMBL4341350"	"Inhibition of JAK2 V617F mutant in human HEL cells assessed as reduction in cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"CHEMBL3308090"	""
"CHEMBL1287910"	""	"0"	"359.29"	"0"	"2.27"	"13"	"Nc1nc(Nc2cccc(C(=O)O)c2)nn1C(=O)c1c(F)cccc1F"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1292866"	"Inhibition of human recombinant JAK2 by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287810"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1287941"	""	"0"	"359.29"	"0"	"2.27"	"15"	"Nc1nc(Nc2ccc(C(=O)O)cc2)nn1C(=O)c1c(F)cccc1F"	"IC50"	"'='"	"2110.0"	"nM"	"5.68"	""	""	"UO_0000065"	"15.80"	"0.30"	"3.41"	"4.61"	"False"	"CHEMBL1292866"	"Inhibition of human recombinant JAK2 by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287810"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1288769"	""	"0"	"247.26"	"0"	"1.31"	"17"	"CCOC(=O)c1cccc(Nc2n[nH]c(N)n2)c1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1292866"	"Inhibition of human recombinant JAK2 by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287810"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1287971"	""	"0"	"315.28"	"0"	"2.57"	"18"	"Nc1nc(Nc2ccccc2)nn1C(=O)c1c(F)cccc1F"	"IC50"	"'>='"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1292866"	"Inhibition of human recombinant JAK2 by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287810"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL505896"	""	"0"	"610.69"	"2"	"5.63"	"22"	"COc1cc2c(Oc3ccc(-c4cnc(Cc5ccccc5)n(C)c4=O)cc3F)ccnc2cc1OCCCN1CCOCC1"	"IC50"	"'>'"	"25000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL971828"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1140082"	"1"	"Scientific Literature"	"J. Med. Chem."	"2008"	"None"	""
"CHEMBL1077458"	""	"0"	"389.46"	"0"	"3.68"	"9"	"CC(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"67.0"	"nM"	"7.17"	""	""	"UO_0000065"	"18.42"	"0.34"	"3.49"	"9.04"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1078275"	""	"0"	"423.54"	"0"	"3.85"	"13"	"CS(=O)(=O)Nc1ccc(-c2ccnc(Nc3cccc(CN4CCCC4)c3)n2)cc1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	""	"UO_0000065"	"19.41"	"0.37"	"4.37"	"9.43"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1078889"	""	"0"	"487.61"	"0"	"2.49"	"21"	"CS(=O)(=O)Nc1ccc(-c2ccnc(Nc3ccc(CN4CCS(=O)(=O)CC4)cc3)n2)cc1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	""	"UO_0000065"	"17.84"	"0.36"	"6.21"	"7.17"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1078166"	""	"0"	"414.47"	"0"	"3.58"	"27"	"N#CCC(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	""	"UO_0000065"	"19.30"	"0.35"	"4.42"	"7.75"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1078005"	""	"0"	"428.50"	"0"	"3.29"	"33"	"Cc1cnc(Nc2ccc(N3CCOCC3)cc2)nc1-c1ccc(C(=O)NCC#N)cc1"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	""	"UO_0000065"	"18.90"	"0.35"	"4.81"	"7.85"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1078229"	""	"0"	"414.47"	"0"	"2.98"	"39"	"N#CCNC(=O)c1ccc(-c2ccnc(Nc3cccc(N4CCOCC4)c3)n2)cc1"	"IC50"	"'='"	"113.0"	"nM"	"6.95"	""	""	"UO_0000065"	"16.76"	"0.31"	"3.97"	"6.73"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1077842"	""	"0"	"476.56"	"0"	"2.37"	"41"	"N#CCNC(=O)c1ccc(-c2ccnc(Nc3ccc(CN4CCS(=O)(=O)CC4)cc3)n2)cc1"	"IC50"	"'='"	"52.0"	"nM"	"7.28"	""	""	"UO_0000065"	"15.28"	"0.29"	"4.91"	"5.69"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1078934"	""	"0"	"427.51"	"0"	"2.89"	"43"	"CN1CCN(c2ccc(Nc3nccc(-c4ccc(C(=O)NCC#N)cc4)n3)cc2)CC1"	"IC50"	"'='"	"41.0"	"nM"	"7.39"	""	""	"UO_0000065"	"17.28"	"0.32"	"4.50"	"7.60"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL253292"	""	"0"	"489.41"	"1"	"5.89"	"1"	"CCN(CC)CCOc1ccc(Nc2cc(NC(=O)Nc3c(Cl)cccc3Cl)ncn2)cc1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL928476"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1141507"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2008"	"None"	""
"CHEMBL592520"	""	"0"	"249.32"	"0"	"4.11"	"13a"	"CCC1Nc2ccccc2-c2ccnc3[nH]cc1c23"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL3928468"	""	"0"	"502.53"	"1"	"3.33"	"3"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc(F)cc(F)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3923756"	""	"0"	"498.57"	"0"	"3.58"	"149, diastereomer 1"	"CC1CC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CCN1C(=O)c1cccc(F)c1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3913298"	""	"0"	"510.61"	"1"	"3.45"	"189"	"Cc1ccc(NC(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)c(C)n1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3944405"	""	"0"	"564.58"	"1"	"4.16"	"205"	"Cc1nc(C(F)(F)F)ccc1NC(=O)N1CCC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3890434"	""	"0"	"549.56"	"1"	"4.46"	"307"	"N#CCC1(n2cc(-c3ccnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3ccncc3C(F)(F)F)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3938863"	""	"0"	"550.55"	"1"	"3.48"	"32"	"COc1c(F)c(F)cc(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)c1F"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3930982"	""	"0"	"527.54"	"1"	"3.20"	"83"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3c(F)cc(C#N)cc3F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3894159"	""	"0"	"536.52"	"1"	"2.86"	"86"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cncc(C(F)(F)F)n3)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3927154"	""	"0"	"520.64"	"1"	"3.54"	"97"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)C3CCc4ccccc4C3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3938103"	""	"0"	"506.61"	"1"	"3.47"	"110"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)C3(c4ccccc4)CC3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3933284"	""	"0"	"611.69"	"2"	"5.41"	"130"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(-c4cccc5cnccc45)c(F)c3)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3970818"	""	"0"	"535.53"	"1"	"3.86"	"173"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3cc(F)cc(F)c3F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3961075"	""	"0"	"517.54"	"1"	"3.72"	"174"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3cc(F)ccc3F)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3918195"	""	"0"	"512.58"	"1"	"2.85"	"204"	"COc1ncccc1NC(=O)N1CCC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3945214"	""	"0"	"471.59"	"0"	"3.72"	"271"	"N#CCC1(n2ccc(-c3ncnc4[nH]ccc34)c2)CN(C2CCN(C(=O)c3cccs3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3951864"	""	"0"	"567.55"	"1"	"4.69"	"281"	"N#CCC1(n2ccc(-c3ncnc4[nH]ccc34)c2)CN(C2CCN(C(=O)c3cccc(OC(F)(F)F)c3F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL1087898"	""	"0"	"331.38"	"0"	"3.09"	"3"	"Cc1cnc(Nc2cncc(N[C@@H](C)c3ncc(F)cn3)n2)s1"	"IC50"	"'='"	"49.0"	"nM"	"7.31"	""	""	"UO_0000065"	"22.06"	"0.43"	"4.22"	"8.26"	"False"	"CHEMBL1103123"	"Inhibition of recombinant JAK2 kinase in presence of 5 mM ATP"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154970"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL3908780"	""	"0"	"553.52"	"1"	"3.60"	"353"	"N#CCC1(n2cc(-c3c(F)cnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccnc(C(F)(F)F)n3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL565612"	"SOTRASTAURIN"	"2"	"438.49"	"0"	"2.43"	"1"	"CN1CCN(c2nc(C3=C(c4c[nH]c5ccccc45)C(=O)NC3=O)c3ccccc3n2)CC1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1040939"	"Inhibition of human recombinant JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156112"	"1"	"Scientific Literature"	"J. Med. Chem."	"2009"	"None"	""
"CHEMBL1080394"	""	"0"	"332.41"	"0"	"3.72"	"2"	"c1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"467.0"	"nM"	"6.33"	""	""	"UO_0000065"	"19.04"	"0.35"	"2.61"	"12.59"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1080955"	""	"0"	"426.52"	"0"	"4.28"	"8"	"Cc1nccn1Cc1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"81.0"	"nM"	"7.09"	""	""	"UO_0000065"	"16.63"	"0.30"	"2.81"	"10.41"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1078274"	""	"0"	"378.43"	"0"	"3.44"	"12"	"COc1cc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)ccc1O"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"22.52"	"0.42"	"5.08"	"10.69"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1078277"	""	"0"	"439.54"	"0"	"3.09"	"15"	"CS(=O)(=O)Nc1ccc(-c2ccnc(Nc3cccc(CN4CCOCC4)c3)n2)cc1"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	""	"UO_0000065"	"18.42"	"0.36"	"5.01"	"8.39"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1079121"	""	"0"	"482.47"	"0"	"4.00"	"35"	"N#CCNC(=O)c1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)c(C(F)(F)F)c3)n2)cc1"	"IC50"	"'='"	"374.0"	"nM"	"6.43"	""	""	"UO_0000065"	"13.32"	"0.25"	"2.43"	"6.23"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"CP-690550"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"33.0"	"nM"	"7.48"	""	""	"UO_0000065"	"23.95"	"0.44"	"5.94"	"8.41"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL3647743"	""	"0"	"566.53"	"1"	"4.14"	"BDBM147846"	"CN(CCC(F)(F)F)[C@@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"180.0"	"nM"	"6.75"	""	"285780"	"UO_0000065"	"11.91"	"0.24"	"2.60"	"5.03"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3593428"	""	"0"	"256.31"	"0"	"2.71"	"6a"	"O=c1[nH]c2cnc3[nH]ccc3c2n1C1CCCCC1"	"IC50"	"'='"	"43.0"	"nM"	"7.37"	""	""	"UO_0000065"	"28.74"	"0.53"	"4.66"	"11.08"	"False"	"CHEMBL3594576"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate and ATP incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593193"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL1081290"	""	"0"	"376.41"	"1"	"5.26"	"3"	"COc1cc(Nc2nc3cccc(-c4ccccc4)c3o2)cc(OC)c1OC"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	""	"UO_0000065"	"20.79"	"0.38"	"2.56"	"11.90"	"True"	"CHEMBL1102770"	"Inhibition of GST-tagged JAK2 assessed as inhibition of biotinylated JAK3tide peptide phosphorylation after 60 mins by caliper mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154949"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1080159"	""	"0"	"506.55"	"2"	"5.36"	"14"	"Cc1cc(Nc2nc3cccc(-c4cc(F)c(CN5CCOCC5)c(F)c4)c3o2)ccc1C(=O)N(C)C"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	""	"UO_0000065"	"16.39"	"0.31"	"2.94"	"11.72"	"False"	"CHEMBL1102770"	"Inhibition of GST-tagged JAK2 assessed as inhibition of biotinylated JAK3tide peptide phosphorylation after 60 mins by caliper mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154949"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1080332"	""	"0"	"403.35"	"0"	"2.66"	"6h"	"N#Cc1ccc2ncn(-c3ncc4[nH]c(=O)n(Cc5cccc(F)c5F)c4n3)c2c1"	"IC50"	"'='"	"270.0"	"nM"	"6.57"	""	""	"UO_0000065"	"16.29"	"0.30"	"3.91"	"6.25"	"False"	"CHEMBL1102456"	"Inhibition of human JAK2 (532-1132) by time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154364"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1080333"	""	"0"	"396.33"	"0"	"2.92"	"6i"	"O=c1[nH]c2cnc(-n3cnc4ccc(F)cc43)nc2n1Cc1c(F)cccc1F"	"IC50"	"'='"	"320.0"	"nM"	"6.50"	""	""	"UO_0000065"	"16.39"	"0.31"	"3.57"	"7.98"	"False"	"CHEMBL1102456"	"Inhibition of human JAK2 (532-1132) by time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154364"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1079524"	""	"0"	"436.26"	"0"	"3.69"	"6k"	"N#Cc1ccc2ncn(-c3ncc4[nH]c(=O)n(Cc5c(Cl)cccc5Cl)c4n3)c2c1"	"IC50"	"'='"	"1550.0"	"nM"	"5.81"	""	""	"UO_0000065"	"13.32"	"0.26"	"2.12"	"5.52"	"False"	"CHEMBL1102456"	"Inhibition of human JAK2 (532-1132) by time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154364"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1076221"	""	"0"	"418.84"	"0"	"3.48"	"21d"	"O=c1[nH]c2cnc(-n3cnc4ccccc43)nc2n1C1CCOc2ccc(Cl)cc21"	"IC50"	"'='"	"500.0"	"nM"	"6.30"	""	""	"UO_0000065"	"15.04"	"0.29"	"2.82"	"6.95"	"False"	"CHEMBL1102456"	"Inhibition of human JAK2 (532-1132) by time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154364"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL3658121"	""	"0"	"650.11"	"2"	"6.41"	"BDBM148440"	"Cc1cc(Nc2ncc3c(n2)CCN(c2cc(NC(=O)c4cccc(C(F)(F)F)c4)ccc2Cl)C3=O)ccc1N1CCN(C)CC1"	"IC50"	"'='"	"19.0"	"nM"	"7.72"	""	"286805"	"UO_0000065"	"11.88"	"0.23"	"1.31"	"8.24"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL21156"	""	"0"	"309.34"	"0"	"3.99"	"pyridone-6"	"CC(C)(C)c1nc2c3ccc(F)cc3c3c(=O)[nH]ccc3c2[nH]1"	"IC50"	"'='"	"1400.0"	"nM"	"5.85"	""	""	"UO_0000065"	"18.92"	"0.35"	"1.86"	"9.51"	"False"	"CHEMBL3625905"	"Inhibition of JAK2 (unknown origin) using 1 mM of ATP and Tyr6 peptide by Z'-LYTE kinase assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621116"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL3647784"	""	"0"	"456.98"	"0"	"3.32"	"BDBM147887"	"CC(C)(O)C1CN([C@H]2CCC(n3cc(C(N)=O)c(Nc4ccc(Cl)cc4)n3)[C@@H](C#N)C2)C1"	"IC50"	"'='"	"71.0"	"nM"	"7.15"	""	"285821"	"UO_0000065"	"15.64"	"0.31"	"3.83"	"5.95"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651034"	""	"0"	"354.34"	"0"	"3.07"	"BDBM153211"	"C=C(C)C(=O)Nc1cc(-c2ncnc3[nH]cc(C(=O)OC)c23)ccc1F"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294159"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642405"	""	"0"	"504.62"	"1"	"3.21"	"BDBM99683"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4cccc(C5CCN(CC(N)=O)CC5)c4)nc23)cc1"	"IC50"	"'='"	"0.41"	"nM"	"9.39"	""	"216372"	"UO_0000065"	"18.60"	"0.36"	"6.18"	"7.65"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647826"	""	"0"	"500.57"	"2"	"5.10"	"BDBM147931"	"N#C[C@H]1C[C@H](N(CC2CC2)CC2CC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'>'"	"1500.0"	"nM"	""	""	"285865"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665124"	""	"0"	"352.40"	"0"	"2.66"	"BDBM112511"	"COC(=O)N1CCC(Nc2ncccc2-c2cnc3[nH]ccc3n2)CC1"	"IC50"	"'='"	"0.047"	"nM"	"10.33"	""	"233750"	"UO_0000065"	"29.31"	"0.54"	"7.67"	"10.75"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3699540"	""	"0"	"404.42"	"0"	"2.85"	"BDBM147558"	"C[C@](O)(c1ccc(Nc2nn([C@H]3CCCC[C@@H]3C#N)cc2C(N)=O)cn1)C(F)F"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"285488"	"UO_0000065"	"21.07"	"0.40"	"5.67"	"6.56"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647812"	""	"0"	"444.97"	"0"	"3.58"	"BDBM147916"	"COCC(C)N(C)[C@H]1CCC(n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"28.0"	"nM"	"7.55"	""	"285851"	"UO_0000065"	"16.97"	"0.33"	"3.97"	"6.92"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703081"	""	"0"	"514.51"	"1"	"2.91"	"BDBM147794"	"N#C[C@H]1C[C@@H](N2CC(F)C2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	"285728"	"UO_0000065"	"15.33"	"0.31"	"4.98"	"5.88"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702948"	""	"0"	"360.81"	"0"	"2.00"	"BDBM147650"	"N#C[C@H]1C[C@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)nc2)n1"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	"285582"	"UO_0000065"	"21.34"	"0.42"	"5.70"	"5.93"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652358"	""	"0"	"455.59"	"0"	"2.56"	"BDBM113169"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC[C@H](c3ncccn3)C2)CC1"	"IC50"	"'='"	"5.72"	"nM"	"8.24"	""	"234612"	"UO_0000065"	"18.09"	"0.35"	"5.68"	"7.63"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3652341"	""	"0"	"395.50"	"0"	"2.33"	"BDBM113152"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC[C@H](F)C2)CC1"	"IC50"	"'='"	"36.4"	"nM"	"7.44"	""	"234595"	"UO_0000065"	"18.81"	"0.38"	"5.11"	"9.05"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3645021"	""	"0"	"449.56"	"1"	"5.10"	"BDBM99773"	"Cc1ccc(-n2cc(-c3cccn4nc(Nc5ccc(C6CCNCC6)cc5)nc34)cn2)cc1"	"IC50"	"'='"	"4.04"	"nM"	"8.39"	""	"216460"	"UO_0000065"	"18.67"	"0.34"	"3.29"	"11.65"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3360353"	""	"0"	"377.45"	"0"	"2.58"	"BDBM103728"	"O=C(Nc1nc2cccc(-c3ccc(CN4CCOCC4)cc3)n2n1)C1CC1"	"IC50"	"'='"	"184.7"	"nM"	"6.73"	""	"221715"	"UO_0000065"	"17.84"	"0.33"	"4.15"	"9.38"	"False"	"CHEMBL3707887"	"Inhibition Assay: In vitro inhibition assay using various enzyme."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638964"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703057"	""	"0"	"436.44"	"0"	"3.42"	"BDBM147767"	"CN(C)[C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(OC(F)(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	"285701"	"UO_0000065"	"17.75"	"0.34"	"4.32"	"7.09"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL1290423"	""	"0"	"361.40"	"0"	"2.06"	"26"	"O=c1[nH]ccc2nc(NCC3CCS(=O)(=O)C3)c3ccc(F)cc3c12"	"IC50"	"'='"	"512.0"	"nM"	"6.29"	""	""	"UO_0000065"	"17.41"	"0.34"	"4.23"	"6.84"	"False"	"CHEMBL1291235"	"Inhibition of JAK2 in cell-free system"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287746"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL3647873"	""	"0"	"428.47"	"0"	"3.23"	"BDBM147985"	"CC(C)NC(=O)O[C@H]1CCC(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"94.0"	"nM"	"7.03"	""	"285919"	"UO_0000065"	"16.40"	"0.31"	"3.80"	"5.20"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL1288720"	""	"0"	"271.30"	"0"	"3.04"	"35"	"CC(C)Nc1nc2cc[nH]c(=O)c2c2cc(F)ccc12"	"IC50"	"'='"	"139.0"	"nM"	"6.86"	""	""	"UO_0000065"	"25.27"	"0.47"	"3.82"	"11.87"	"False"	"CHEMBL1291235"	"Inhibition of JAK2 in cell-free system"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287746"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL4575813"	""	"0"	"464.36"	"0"	"4.92"	"8b"	"O=C(CCCCCCn1cc(Nc2ncc(Cl)c(Nc3ccc(Cl)cc3)n2)cn1)NO"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	""	"UO_0000065"	"16.91"	"0.35"	"2.93"	"6.71"	"False"	"CHEMBL4347596"	"Inhibition of recombinant human JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate measured after 60 mins by LANCE assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4346670"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4451298"	""	"0"	"367.84"	"0"	"2.57"	"8k"	"CNc1nc(Nc2cnn(CCCCCCC(=O)NO)c2)ncc1Cl"	"IC50"	"'='"	"36.0"	"nM"	"7.44"	""	""	"UO_0000065"	"20.24"	"0.41"	"4.87"	"6.36"	"False"	"CHEMBL4347596"	"Inhibition of recombinant human JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate measured after 60 mins by LANCE assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4346670"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL3699490"	""	"0"	"384.46"	"0"	"2.91"	"BDBM147505"	"CN(C)CC1CCC(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@H](C#N)C1"	"IC50"	"'='"	"357.0"	"nM"	"6.45"	""	"285432"	"UO_0000065"	"16.77"	"0.31"	"3.54"	"6.45"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3655085"	""	"0"	"390.47"	"0"	"0.77"	"BDBM159752"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)CC2(CC#N)COC2)C1"	"IC50"	"'='"	"313.0"	"nM"	"6.50"	""	"302562"	"UO_0000065"	"16.66"	"0.33"	"5.73"	"5.25"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699547"	""	"0"	"408.38"	"0"	"2.97"	"BDBM147565"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc([C@@H](O)C(F)(F)F)nc2)n1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"285495"	"UO_0000065"	"20.87"	"0.40"	"5.55"	"6.56"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647925"	""	"0"	"442.50"	"0"	"3.62"	"BDBM148043"	"CC(C)(C)OC(=O)N[C@@H]1CC[C@H](C#N)C(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)C1"	"IC50"	"'='"	"990.0"	"nM"	"6.00"	""	"285985"	"UO_0000065"	"13.57"	"0.26"	"2.38"	"4.45"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647822"	""	"0"	"500.57"	"2"	"5.24"	"BDBM147927"	"N#C[C@@H]1C[C@@H](N(CC2CC2)C2CCC2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"610.0"	"nM"	"6.21"	""	"285861"	"UO_0000065"	"12.42"	"0.24"	"0.97"	"6.22"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3644993"	""	"0"	"448.96"	"0"	"4.46"	"BDBM99745"	"CN1CCN(c2cccc(Nc3nc4c(OCc5cccc(Cl)c5)cccn4n3)c2)CC1"	"IC50"	"'='"	"99.52"	"nM"	"7.00"	""	"216433"	"UO_0000065"	"15.60"	"0.30"	"2.54"	"12.09"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3658858"	""	"0"	"374.47"	"0"	"1.35"	"BDBM159777"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](CS(=O)(=O)N2CC[C@@H](C#N)C2)C1"	"IC50"	"'='"	"179.0"	"nM"	"6.75"	""	"302587"	"UO_0000065"	"18.02"	"0.35"	"5.40"	"6.37"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703048"	""	"0"	"476.50"	"0"	"3.43"	"BDBM147758"	"C[C@@](O)(c1ccc(Nc2nn([C@H]3CC[C@@H](N4CCC4)C[C@@H]3C#N)cc2C(N)=O)cc1)C(F)(F)F"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"285692"	"UO_0000065"	"18.26"	"0.35"	"5.27"	"7.24"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702895"	""	"0"	"335.37"	"0"	"2.25"	"BDBM147594"	"N#Cc1cncc(Nc2nn([C@H]3CCCC[C@@H]3C#N)cc2C(N)=O)c1"	"IC50"	"'='"	"49.0"	"nM"	"7.31"	""	"285524"	"UO_0000065"	"21.80"	"0.40"	"5.06"	"5.48"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3694592"	""	"0"	"445.75"	"1"	"5.57"	"BDBM125913"	"Clc1cnc2nc1NCc1cc(Br)cc(c1)OCCCc1cccc(c1)N2"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"255686"	"UO_0000065"	"18.62"	"0.42"	"2.73"	"14.05"	"False"	"CHEMBL3707544"	"In Vitro Kinase Assay: One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Biochemistry 1999, 269, 94-104. The catalytic domains of human JAK1 (a.a. 837-1142), JAK2 (a.a. 828-1132) and JAK3 (a.a. 781-1124) with an N-terminal His tag were expressed using baculovirus in insect cells and purified. The catalytic activity of JAK1, JAK2 or JAK3 was assayed by measuring the phosphorylation of a biotinylated peptide. The phosphorylated peptide was detected by homogenous time resolved fluorescence (HTRF). IC50s of compounds were measured for each kinase in the reactions that contain the enzyme, ATP and 500 nM peptide in 50 mM Tris (pH 7.8) buffer with 100 mM NaCl, 5 mM DTT, and 0.1 mg/mL (0.01%) BSA. The ATP concentration in the reactions was 90 uM for JAK1, 30 uM for JAK2 and 3 uM for JAK3. Reactions were carried out at room temperature for 1 hr and then stopped with 20 uL 45 mM EDTA."	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639093"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3642322"	""	"0"	"442.52"	"0"	"2.95"	"BDBM99594"	"CS(=O)(=O)c1ccc(Nc2nc3cccc(-c4ccc(S(C)(=O)=O)cc4)n3n2)cc1"	"IC50"	"'='"	"1.4"	"nM"	"8.85"	""	"216284"	"UO_0000065"	"20.01"	"0.40"	"5.90"	"8.01"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647805"	""	"0"	"442.95"	"0"	"3.33"	"BDBM147908"	"CN([C@H]1CCC(n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@@H](C#N)C1)C1(C)COC1"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"285842"	"UO_0000065"	"18.41"	"0.36"	"4.82"	"7.47"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3644957"	""	"0"	"382.45"	"0"	"2.76"	"BDBM99707"	"CCn1cc(Nc2nc3c(-c4ccc(S(C)(=O)=O)cc4)cccn3n2)cn1"	"IC50"	"'='"	"1.88"	"nM"	"8.73"	""	"216397"	"UO_0000065"	"22.82"	"0.44"	"5.97"	"9.27"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3335696"	""	"0"	"460.56"	"0"	"1.43"	"BDBM112599"	"CC[C@H](CO)Nc1ncc(-c2cnc3[nH]ccc3n2)c(N[C@H]2CCCN(S(C)(=O)=O)C2)n1"	"IC50"	"'='"	"0.054"	"nM"	"10.27"	"Potential transcription error"	"233836"	"UO_0000065"	""	""	""	""	"True"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3651030"	""	"0"	"380.40"	"0"	"2.94"	"BDBM153207"	"C=C(COC)C(=O)Nc1cccc(-c2ncnc3[nH]cc(C(=O)OCC)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294155"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647905"	""	"0"	"476.92"	"0"	"3.73"	"BDBM148017"	"N#C[C@@H]1C[C@H](C(=O)N2CCC(F)(F)C2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"60.0"	"nM"	"7.22"	""	"285952"	"UO_0000065"	"15.14"	"0.30"	"3.49"	"6.17"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647795"	""	"0"	"444.97"	"0"	"3.63"	"BDBM147898"	"COCC(C)(C)N[C@H]1CCC(n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"43.0"	"nM"	"7.37"	""	"285832"	"UO_0000065"	"16.56"	"0.32"	"3.74"	"6.24"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4089286"	""	"0"	"323.42"	"0"	"1.11"	"21"	"CCNS(=O)(=O)C[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"377.0"	"nM"	"6.42"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4059894"	""	"0"	"337.45"	"0"	"1.50"	"22"	"CCCNS(=O)(=O)C[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"326.0"	"nM"	"6.49"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4104105"	""	"0"	"349.46"	"0"	"1.60"	"43"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](CS(=O)(=O)N2CCCC2)C1"	"IC50"	"'='"	"1970.0"	"nM"	"5.71"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3973234"	""	"0"	"579.62"	"1"	"4.39"	"116"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3c(F)cc(-c4cccnc4)cc3F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3902174"	""	"0"	"552.66"	"1"	"3.88"	"243, diastereomer 2"	"CC1CC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CCN1Cc1ccc(N(C)C)c(C#N)c1F"	"IC50"	"'>'"	"100.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL4446102"	""	"0"	"326.40"	"0"	"1.87"	"2"	"NC(=O)c1cnc2[nH]ccc2c1NC1C2CC3CC1CC(C2)C3O"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	""	"UO_0000065"	"25.43"	"0.47"	"6.43"	"7.98"	"False"	"CHEMBL4309402"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate incubated for 1 hr by ELISA"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4308837"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3893843"	""	"0"	"535.53"	"1"	"3.46"	"57"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccnc(C(F)(F)F)c3)CC2)C1"	"IC50"	"'>'"	"100.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL584052"	""	"0"	"341.37"	"0"	"4.02"	"9"	"O=C1Nc2ccccc2-c2ccnc3[nH]cc(c23)C1c1ccc(O)cc1"	"IC50"	"'='"	"270.0"	"nM"	"6.57"	""	""	"UO_0000065"	"19.24"	"0.35"	"2.55"	"8.42"	"False"	"CHEMBL1042393"	"Inhibition of JAK2 in human TF1 cells assessed as inhibition of GMCSF-induced STAT5 phosphorylation by flow cytometry"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154754"	"1"	"Scientific Literature"	"J. Med. Chem."	"2009"	"CHEMBL3307972"	""
"CHEMBL599912"	""	"0"	"312.38"	"0"	"4.33"	"13ac"	"Nc1ccc(C2Nc3ccccc3-c3ccnc4[nH]cc2c34)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL604578"	""	"0"	"292.34"	"0"	"3.22"	"18"	"OCCCCC1=Nc2ccccc2-c2ncnc3[nH]cc1c23"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL601268"	""	"0"	"324.34"	"0"	"3.69"	"20c"	"O=C1c2ccccc2C2c3c[nH]c4ncnc(c34)-c3ccccc3N12"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL589632"	""	"0"	"371.40"	"0"	"3.78"	"22c"	"COC(=O)C1(c2ccc(O)cc2)Nc2ccccc2-c2ccnc3[nH]cc1c23"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL589633"	""	"0"	"359.36"	"0"	"3.91"	"25"	"O=C1NC(c2ccc(O)cc2F)c2c[nH]c3nccc(c23)-c2ccccc21"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL3895868"	""	"0"	"573.58"	"1"	"4.94"	"311"	"N#CCC1(n2cc(-c3ccnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3ccc(C#N)cc3C(F)(F)F)CC2)C1"	"IC50"	"'>'"	"100.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3954167"	""	"0"	"586.98"	"1"	"4.86"	"326"	"N#CCC1(n2cc(-c3c(F)cnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc(C(F)(F)F)ncc3Cl)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL1448"	"NICLOSAMIDE"	"4"	"327.12"	"0"	"3.86"	"5"	"O=C(Nc1ccc([N+](=O)[O-])cc1Cl)c1cc(Cl)ccc1O"	"IC50"	"'='"	"10000.0"	"nM"	"5.00"	""	""	"UO_0000065"	"15.28"	"0.33"	"1.14"	"5.41"	"False"	"CHEMBL1696959"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1687697"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL563080"	""	"0"	"387.91"	"1"	"5.80"	"11b"	"Cc1cc(Cl)c2c(n1)N(CCc1ccccc1)CCc1c-2[nH]c2ccccc12"	"IC50"	"'>'"	"40000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1036442"	"Inhibition of recombinant JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1151875"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2009"	"None"	""
"CHEMBL1789941"	"RUXOLITINIB"	"4"	"306.37"	"0"	"3.47"	"Ruxolitinib"	"N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"1.84"	"nM"	"8.73"	""	""	"UO_0000065"	"28.51"	"0.52"	"5.27"	"10.50"	"False"	"CHEMBL2186598"	"Inhibition of JAK2 V617F mutant in human SET2 cells assessed as reduction in STAT5 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176876"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL3967338"	""	"0"	"570.68"	"1"	"2.54"	"250"	"CN(C)c1ccc(S(=O)(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)cc1C#N"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3966182"	""	"0"	"520.62"	"1"	"1.64"	"259"	"Cc1nc(S(=O)(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)cn1C"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3958544"	""	"0"	"621.67"	"1"	"3.70"	"373"	"CCN(CC)Cc1cc(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)nc(C(F)(F)F)n1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL519279"	""	"0"	"307.40"	"0"	"2.56"	"11"	"CN1CCN(c2ccc(-c3ccc4[nH]nc(N)c4c3)cc2)CC1"	"IC50"	"'='"	"8580.0"	"nM"	"5.07"	""	""	"UO_0000065"	"16.48"	"0.30"	"2.51"	"8.28"	"False"	"CHEMBL1011746"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139271"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL480606"	""	"0"	"322.37"	"0"	"2.28"	"16"	"Nc1n[nH]c2ccc(-c3ccc(C(=O)N4CCOCC4)cc3)cc12"	"IC50"	"'='"	"1570.0"	"nM"	"5.80"	""	""	"UO_0000065"	"18.00"	"0.33"	"3.52"	"6.89"	"False"	"CHEMBL1011746"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139271"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL501406"	""	"0"	"212.05"	"0"	"1.91"	"Page 279, R16C2"	"Nc1n[nH]c2cc(Br)ccc12"	"IC50"	"'='"	"131000.0"	"nM"	"3.88"	""	""	"UO_0000065"	"18.31"	"0.48"	"1.97"	"7.10"	"False"	"CHEMBL1011746"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139271"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL4444782"	""	"0"	"304.36"	"0"	"3.41"	"3"	"Cc1cnc(Nc2cnn(C)c2)nc1-c1c[nH]c2ccccc12"	"IC50"	"'='"	"380.0"	"nM"	"6.42"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4406243"	"Inhibition of recombinant human N-terminal GST-tagged JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-labeled GEEPLYWSFPAKKK-NH2 peptide as substrate after 10 mins in presence of 5 mM ATP by caliper mobility shift assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402602"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL481985"	""	"0"	"301.37"	"0"	"2.61"	"18"	"CCS(=O)(=O)c1ccc(-c2ccc3[nH]nc(N)c3c2)cc1"	"IC50"	"'='"	"790.0"	"nM"	"6.10"	""	""	"UO_0000065"	"20.25"	"0.40"	"3.49"	"6.87"	"False"	"CHEMBL1011746"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139271"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL480998"	""	"0"	"344.44"	"0"	"2.89"	"12"	"CC(C)(C)NS(=O)(=O)c1cccc(-c2ccc3[nH]nc(N)c3c2)c1"	"IC50"	"'='"	"3550.0"	"nM"	"5.45"	""	""	"UO_0000065"	"15.82"	"0.31"	"2.56"	"5.40"	"False"	"CHEMBL1011746"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139271"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL520947"	""	"0"	"358.42"	"0"	"1.83"	"19"	"Nc1n[nH]c2ccc(-c3ccc(S(=O)(=O)N4CCOCC4)cc3)cc12"	"IC50"	"'='"	"330.0"	"nM"	"6.48"	""	""	"UO_0000065"	"18.08"	"0.35"	"4.65"	"6.40"	"False"	"CHEMBL1011746"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139271"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL4536860"	""	"0"	"452.52"	"0"	"4.67"	"4"	"Cc1ccc(C(=O)Nc2cccc3c(-c4nc(Nc5cnn(C)c5)ncc4C)c[nH]c23)c(C)n1"	"IC50"	"'='"	"200.0"	"nM"	"6.70"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4406243"	"Inhibition of recombinant human N-terminal GST-tagged JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-labeled GEEPLYWSFPAKKK-NH2 peptide as substrate after 10 mins in presence of 5 mM ATP by caliper mobility shift assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402602"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL3234894"	""	"0"	"295.37"	"0"	"3.65"	"2"	"NC(=O)c1cc(-c2ccccc2)sc1Nc1ccccn1"	"IC50"	"'='"	"65.0"	"nM"	"7.19"	""	""	"UO_0000065"	"24.33"	"0.47"	"3.54"	"10.57"	"False"	"CHEMBL3239499"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3232939"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3234889"	""	"0"	"309.39"	"0"	"3.96"	"7"	"Cc1ccnc(Nc2sc(-c3ccccc3)cc2C(N)=O)c1"	"IC50"	"'='"	"398.0"	"nM"	"6.40"	""	""	"UO_0000065"	"20.69"	"0.40"	"2.44"	"9.41"	"False"	"CHEMBL3239499"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3232939"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL1270399"	""	"0"	"438.56"	"0"	"3.80"	"25"	"Cc1cn2c(-c3cn[nH]c3)cnc2c(Nc2cc([C@@H](C)N3C[C@H](C)O[C@H](C)C3)ns2)n1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1272516"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1268847"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL272424"	""	"0"	"381.77"	"1"	"5.16"	"2a"	"O=c1[nH]ccc2c3[nH]c(-c4c(F)cccc4Cl)nc3c3ccc(F)cc3c12"	"IC50"	"'='"	"0.2"	"nM"	"9.70"	""	""	"UO_0000065"	"25.41"	"0.49"	"4.54"	"15.76"	"False"	"CHEMBL945937"	"Inhibition of human JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1142217"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2007"	"None"	""
"CHEMBL270347"	""	"0"	"346.79"	"1"	"6.33"	"4"	"Fc1cccc(Cl)c1-c1nc2c3ccccc3c3ccccc3c2[nH]1"	"IC50"	"'='"	"900.0"	"nM"	"6.05"	""	""	"UO_0000065"	"17.43"	"0.33"	"-0.28"	"21.08"	"False"	"CHEMBL945937"	"Inhibition of human JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1142217"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2007"	"None"	""
"CHEMBL1171837"	"PONATINIB"	"4"	"532.57"	"1"	"4.46"	"AP-24534"	"Cc1ccc(C(=O)Nc2ccc(CN3CCN(C)CC3)c(C(F)(F)F)c2)cc1C#Cc1cnc2cccnn12"	"IC50"	"'='"	"169.0"	"nM"	"6.77"	""	""	""	"12.72"	"0.24"	"2.31"	"10.30"	"False"	"CHEMBL4721774"	"Binding affinity to human JAK2 using poly[Glu:Tyr] (4:1) as substrate by radiometric hotspot kinase assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715823"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2018"	"None"	""
"CHEMBL1682381"	""	"0"	"430.52"	"0"	"2.70"	"21"	"Cc1cc(Nc2nc(N3CCN(C(=O)Cc4ccccc4C)CC3)nn3cccc23)n[nH]1"	"IC50"	"'='"	"5.3"	"nM"	"8.28"	""	""	"UO_0000065"	"19.22"	"0.35"	"5.58"	"8.76"	"False"	"CHEMBL1685409"	"Inhibition of JAK2 after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1681645"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1682369"	""	"0"	"354.42"	"0"	"1.56"	"9"	"CCC(=O)N1CCN(c2nc(Nc3cc(C)[nH]n3)c3cccn3n2)CC1"	"IC50"	"'='"	"22.0"	"nM"	"7.66"	""	""	"UO_0000065"	"21.61"	"0.40"	"6.10"	"8.11"	"False"	"CHEMBL1685409"	"Inhibition of JAK2 after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1681645"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1682361"	""	"0"	"434.53"	"0"	"2.52"	"1"	"Cc1nnc(Nc2nc(N3CCN(C(=O)Cc4ccccc4)CC3)nn3cccc23)s1"	"IC50"	"'='"	"14000.0"	"nM"	"4.85"	""	""	"UO_0000065"	"11.17"	"0.21"	"2.33"	"5.30"	"False"	"CHEMBL1685409"	"Inhibition of JAK2 after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1681645"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1682380"	""	"0"	"480.55"	"0"	"1.87"	"20"	"Cc1cc(Nc2nc(N3CCN(C(=O)c4ccccc4S(C)(=O)=O)CC3)nn3cccc23)n[nH]1"	"IC50"	"'='"	"1.1"	"nM"	"8.96"	""	""	"UO_0000065"	"18.64"	"0.36"	"7.09"	"6.97"	"False"	"CHEMBL1685409"	"Inhibition of JAK2 after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1681645"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1682378"	""	"0"	"436.91"	"0"	"3.12"	"18"	"Cc1cc(Nc2nc(N3CCN(C(=O)c4ccccc4Cl)CC3)nn3cccc23)n[nH]1"	"IC50"	"'='"	"7.3"	"nM"	"8.14"	""	""	"UO_0000065"	"18.62"	"0.36"	"5.02"	"8.61"	"False"	"CHEMBL1685409"	"Inhibition of JAK2 after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1681645"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1630770"	""	"0"	"230.31"	"0"	"2.73"	"S13"	"CN(c1ncnc2[nH]ccc12)C1CCCCC1"	"IC50"	"'='"	"45000.0"	"nM"	"4.35"	""	""	"UO_0000065"	"18.87"	"0.35"	"1.62"	"9.70"	"False"	"CHEMBL4031305"	"Inhibition of human JAK2 using poly[Glu:Tyr] as substrate in presence of [gamma-33P]-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028864"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4091233"	""	"0"	"489.58"	"0"	"4.24"	"36"	"O=C(CCCCCCC(=O)Nc1ccc(CCCn2cc(-c3ncnc4[nH]ccc34)cn2)cc1)NO"	"IC50"	"'='"	"865.0"	"nM"	"6.06"	""	""	"UO_0000065"	"12.38"	"0.23"	"1.82"	"4.40"	"False"	"CHEMBL4031305"	"Inhibition of human JAK2 using poly[Glu:Tyr] as substrate in presence of [gamma-33P]-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028864"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4070306"	""	"0"	"384.48"	"0"	"3.84"	"26"	"O=C(CCCCCCCCCCn1cc(-c2ncnc3[nH]ccc23)cn1)NO"	"IC50"	"'='"	"43.0"	"nM"	"7.37"	""	""	"UO_0000065"	"19.16"	"0.36"	"3.53"	"6.78"	"False"	"CHEMBL4031305"	"Inhibition of human JAK2 using poly[Glu:Tyr] as substrate in presence of [gamma-33P]-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028864"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL446576"	""	"0"	"209.25"	"0"	"2.81"	"3"	"Nc1n[nH]c2cc(-c3ccccc3)ccc12"	"IC50"	"'='"	"145300.0"	"nM"	"3.84"	""	""	"UO_0000065"	"18.34"	"0.33"	"1.03"	"7.02"	"False"	"CHEMBL1011746"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139271"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL553"	"ERLOTINIB"	"4"	"393.44"	"0"	"3.41"	"1, erlotinib"	"C#Cc1cccc(Nc2ncnc3cc(OCCOC)c(OCCOC)cc23)c1"	"IC50"	"'='"	"4000.0"	"nM"	"5.40"	""	""	"UO_0000065"	"13.72"	"0.25"	"1.99"	"7.22"	"False"	"CHEMBL1007370"	"Inhibition of human JAK2 V617F mutant expressed in COS7 cells"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"COS-7"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156429"	"1"	"Scientific Literature"	"J. Biol. Chem."	"2007"	"CHEMBL3307648"	""
"CHEMBL4068856"	""	"0"	"391.52"	"0"	"3.73"	"7"	"Cc1ccccc1-c1cc2c(N[C@@H]3CC[C@](C)(N)C3(C)C)c(C(N)=O)cnn2c1"	"IC50"	"'='"	"49.0"	"nM"	"7.31"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4054822"	"Inhibition of GST-tagged JAK2 (unknown origin) after 3 hrs by Caliper assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4052645"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4063870"	""	"0"	"378.48"	"0"	"2.81"	"23"	"CC1(C)[C@H](Nc2c(C(N)=O)cnn3cc(-c4ccncc4)cc23)CC[C@]1(C)N"	"IC50"	"'='"	"80.0"	"nM"	"7.10"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4054822"	"Inhibition of GST-tagged JAK2 (unknown origin) after 3 hrs by Caliper assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4052645"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4060984"	""	"0"	"367.46"	"0"	"2.14"	"25"	"CC1(C)[C@H](Nc2c(C(N)=O)cnn3cc(-c4cc[nH]n4)cc23)CC[C@]1(C)N"	"IC50"	"'='"	"21.0"	"nM"	"7.68"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4054822"	"Inhibition of GST-tagged JAK2 (unknown origin) after 3 hrs by Caliper assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4052645"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4104127"	""	"0"	"396.47"	"0"	"2.95"	"29"	"CC1(C)[C@H](Nc2c(C(N)=O)cnn3cc(-c4ccnc(F)c4)cc23)CC[C@]1(C)N"	"IC50"	"'='"	"38.0"	"nM"	"7.42"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4054822"	"Inhibition of GST-tagged JAK2 (unknown origin) after 3 hrs by Caliper assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4052645"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL2181318"	""	"0"	"375.43"	"0"	"4.36"	"16d, 85:15 trans/cis mixture"	"COc1ccc2cc1COCC=CCOc1cccc(c1)-c1ccnc(n1)N2"	"IC50"	"'='"	"260.0"	"nM"	"6.58"	""	""	"UO_0000065"	"17.54"	"0.32"	"2.23"	"10.05"	"False"	"CHEMBL2184201"	"Inhibition of recombinant JAK2 using Poly (Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176955"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL2181312"	""	"0"	"490.58"	"1"	"5.10"	"22e, 85:15 trans/cis mixture"	"Fc1cc2cc(c1)-c1ccnc(n1)Nc1ccc(OCCN3CCCC3)c(c1)COCC=CCOC2"	"IC50"	"'='"	"24.0"	"nM"	"7.62"	""	""	"UO_0000065"	"15.53"	"0.29"	"2.52"	"11.08"	"False"	"CHEMBL2184201"	"Inhibition of recombinant JAK2 using Poly (Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176955"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL4561692"	""	"0"	"462.53"	"0"	"1.43"	"3"	"COc1ncc(-c2cc3c(c(NC(=O)CN4CCOCC4)c2)COC3)cc1NS(C)(=O)=O"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4479370"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4477235"	"1"	"Scientific Literature"	"J Med Chem"	"2016"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"1, CP-690550"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	""	"UO_0000065"	"24.65"	"0.46"	"6.16"	"8.66"	"False"	"CHEMBL1019775"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1151738"	"1"	"Scientific Literature"	"J. Med. Chem."	"2008"	"None"	""
"CHEMBL2181082"	""	"0"	"486.57"	"0"	"4.14"	"21f, 85:15 trans/cis mixture"	"O=C1CCN(CCOc2ccc3cc2COCC=CCOCc2cccc(c2)-c2ccnc(n2)N3)C1"	"IC50"	"'='"	"22.0"	"nM"	"7.66"	""	""	"UO_0000065"	"15.74"	"0.29"	"3.52"	"8.92"	"False"	"CHEMBL2184201"	"Inhibition of recombinant JAK2 using Poly (Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176955"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL2181322"	""	"0"	"443.55"	"0"	"3.90"	"17c, 85:15 trans/cis mixture"	"C1=CCOCc2cc(ccc2N2CCNCC2)Nc2nccc(n2)-c2cccc(c2)COC1"	"IC50"	"'='"	"83.0"	"nM"	"7.08"	""	""	"UO_0000065"	"15.96"	"0.29"	"3.18"	"9.90"	"False"	"CHEMBL2184201"	"Inhibition of recombinant JAK2 using Poly (Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176955"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL4287529"	""	"0"	"299.42"	"0"	"2.66"	"8"	"CCCCN1C[C@H](N(C)c2ncnc3[nH]ccc23)C2(CC2)C1"	"IC50"	"'='"	"15000.0"	"nM"	"4.82"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4285473"	""	"0"	"349.46"	"0"	"1.60"	"40"	"CCCS(=O)(=O)N1C[C@H](N(C)c2ncnc3[nH]ccc23)C2(CC2)C1"	"IC50"	"'='"	"36.0"	"nM"	"7.44"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4282998"	""	"0"	"408.49"	"0"	"2.12"	"47"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(S(=O)(=O)c2ccc(C#N)cc2)CC12CC2"	"IC50"	"'='"	"1100.0"	"nM"	"5.96"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL1077431"	""	"0"	"376.46"	"0"	"4.05"	"6"	"Cc1cc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc(C)c1O"	"IC50"	"'='"	"88.0"	"nM"	"7.06"	""	""	"UO_0000065"	"18.74"	"0.34"	"3.01"	"10.01"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1078689"	""	"0"	"439.54"	"0"	"3.09"	"17"	"CS(=O)(=O)Nc1ccc(-c2ccnc(Nc3ccc(CN4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	""	"UO_0000065"	"18.30"	"0.35"	"4.96"	"8.34"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1078159"	""	"0"	"414.47"	"0"	"2.98"	"24"	"N#CCNC(=O)c1cccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)c1"	"IC50"	"'='"	"545.0"	"nM"	"6.26"	""	""	"UO_0000065"	"15.11"	"0.28"	"3.28"	"6.07"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL3938282"	""	"0"	"520.52"	"1"	"3.47"	"4"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc(F)c(F)c(F)c3)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3952888"	""	"0"	"502.62"	"1"	"2.94"	"103"	"COC1CCCC(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3959533"	""	"0"	"603.64"	"1"	"4.87"	"119"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(-c4ccc(C#N)c(F)c4)c(F)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL374321"	""	"0"	"417.48"	"0"	"4.92"	"30"	"C[C@H](Nc1cc(-c2ccc(C#N)cc2)nc(-n2cnc3ccncc32)n1)c1ccccc1"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	""	"UO_0000065"	"18.55"	"0.33"	"2.82"	"8.39"	"False"	"CHEMBL908418"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139695"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2006"	"None"	""
"CHEMBL373523"	""	"0"	"435.54"	"1"	"5.12"	"27"	"C[C@H](Nc1cc(-c2cccc(N(C)C)c2)nc(-n2cnc3ccncc32)n1)c1ccccc1"	"IC50"	"'='"	"167.0"	"nM"	"6.78"	""	""	"UO_0000065"	"15.56"	"0.28"	"1.66"	"9.44"	"False"	"CHEMBL908418"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139695"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2006"	"None"	""
"CHEMBL218579"	""	"0"	"359.44"	"0"	"3.45"	"18"	"C[C@H](Nc1cc(N(C)C)nc(-n2cnc3ccncc32)n1)c1ccccc1"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	""	"UO_0000065"	"22.69"	"0.41"	"4.70"	"11.36"	"False"	"CHEMBL908418"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139695"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2006"	"None"	""
"CHEMBL3924980"	""	"0"	"516.01"	"1"	"4.10"	"183"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3cccc(Cl)c3)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL590109"	""	"0"	"425.52"	"0"	"4.40"	"31a"	"NCCn1cc(-c2cc(-c3cc4ccccc4s3)c3[nH]ncc3c2)c2nc(N)ncc21"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1073305"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153138"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1076700"	""	"0"	"563.65"	"2"	"5.34"	"17"	"Cc1cc(Nc2nc3cccc(-c4cc(F)c(CN5CCOCC5)c(F)c4)c3o2)ccc1C(=O)NCCCN(C)C"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	""	"UO_0000065"	"14.73"	"0.28"	"2.96"	"10.02"	"False"	"CHEMBL1102770"	"Inhibition of GST-tagged JAK2 assessed as inhibition of biotinylated JAK3tide peptide phosphorylation after 60 mins by caliper mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154949"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL2181323"	""	"0"	"457.58"	"0"	"4.24"	"17d, 85:15 trans/cis mixture"	"CN1CCN(c2ccc3cc2COCC=CCOCc2cccc(c2)-c2ccnc(n2)N3)CC1"	"IC50"	"'='"	"41.0"	"nM"	"7.39"	""	""	"UO_0000065"	"16.14"	"0.30"	"3.15"	"11.77"	"False"	"CHEMBL2184201"	"Inhibition of recombinant JAK2 using Poly (Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176955"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL4100048"	""	"0"	"308.41"	"0"	"1.61"	"16"	"CCS(=O)(=O)C[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"5437.0"	"nM"	"5.26"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4100431"	""	"0"	"295.37"	"0"	"0.47"	"5"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(C)(=O)=O)C1"	"IC50"	"'='"	"11900.0"	"nM"	"4.92"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4078655"	""	"0"	"336.42"	"0"	"0.51"	"13"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)NC2CC2)C1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3655097"	""	"0"	"350.45"	"0"	"0.76"	"14"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)NCC2CC2)C1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4059667"	""	"0"	"321.41"	"0"	"1.01"	"28"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)C2CC2)C1"	"IC50"	"'='"	"1990.0"	"nM"	"5.70"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4103435"	""	"0"	"377.39"	"0"	"1.80"	"31"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)CCC(F)(F)F)C1"	"IC50"	"'='"	"6110.0"	"nM"	"5.21"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3655086"	""	"0"	"351.43"	"0"	"0.49"	"36"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)CC2COC2)C1"	"IC50"	"'='"	"6810.0"	"nM"	"5.17"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4063642"	""	"0"	"350.45"	"0"	"0.85"	"38"	"CN(C1CC1)S(=O)(=O)N[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"4670.0"	"nM"	"5.33"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL500779"	""	"0"	"209.25"	"0"	"2.81"	"2"	"Nc1n[nH]c2ccc(-c3ccccc3)cc12"	"IC50"	"'='"	"1600.0"	"nM"	"5.80"	""	""	"UO_0000065"	"27.70"	"0.49"	"2.99"	"10.60"	"False"	"CHEMBL1011746"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139271"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL2181331"	""	"0"	"486.62"	"1"	"5.35"	"21d, 85:15 trans/cis mixture"	"C1=CCOCc2cc(ccc2OCCN2CCCCC2)Nc2nccc(n2)-c2cccc(c2)COC1"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	""	"UO_0000065"	"16.08"	"0.30"	"2.47"	"11.38"	"False"	"CHEMBL2184201"	"Inhibition of recombinant JAK2 using Poly (Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176955"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL3652307"	""	"0"	"395.50"	"0"	"2.33"	"BDBM113116"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC[C@@H](F)C2)CC1"	"IC50"	"'='"	"16.7"	"nM"	"7.78"	""	"234560"	"UO_0000065"	"19.66"	"0.39"	"5.45"	"9.46"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3647785"	""	"0"	"456.98"	"0"	"3.32"	"BDBM147888"	"CC(C)(O)C1CN([C@@H]2CCC(n3cc(C(N)=O)c(Nc4ccc(Cl)cc4)n3)[C@@H](C#N)C2)C1"	"IC50"	"'='"	"36.0"	"nM"	"7.44"	""	"285822"	"UO_0000065"	"16.29"	"0.32"	"4.12"	"6.19"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665197"	""	"0"	"486.60"	"0"	"1.87"	"BDBM112595"	"COC1CCN(c2ncc(-c3cnc4[nH]ccc4n3)c(N[C@H]3CCCN(S(C)(=O)=O)C3)n2)CC1"	"IC50"	"'='"	"0.1067"	"nM"	"9.97"	""	"233832"	"UO_0000065"	"20.49"	"0.40"	"8.10"	"7.72"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647930"	""	"0"	"337.43"	"0"	"3.62"	"BDBM148050"	"CC1(C)CC[C@H](C#N)[C@@H](n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"50.0"	"nM"	"7.30"	""	"285434"	"UO_0000065"	"21.64"	"0.40"	"3.68"	"7.55"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645121"	""	"0"	"431.52"	"0"	"0.97"	"BDBM100350"	"CS(=O)(=O)N1CCN(c2ccc(Nc3ncc(C(N)=O)c(NC4CC4)n3)cc2)CC1"	"IC50"	"'='"	"3.2"	"nM"	"8.49"	""	"217552"	"UO_0000065"	"19.69"	"0.39"	"7.52"	"6.36"	"True"	"CHEMBL3707560"	"Binding Assay: ATP-site dependent competition binding assay using Ambit KinomeScan Screening kit."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638944"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL2376156"	""	"0"	"448.87"	"0"	"2.05"	"7"	"C[C@@H](NC(=O)c1c[nH]c2ncc(-n3ncc4cc(Cl)ccc43)nc12)C(=O)N1CC(C#N)C1"	"IC50"	"'='"	"83.0"	"nM"	"7.08"	""	""	"UO_0000065"	"15.77"	"0.30"	"5.03"	"5.34"	"False"	"CHEMBL2378515"	"Inhibition of JAK2 (unknown origin) using [33gammaP]ATP and Biotin-KAIETDKEYYTVKD as substrate incubated for 10 mins prior to substrate addition measured after 30 mins by filtration assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375236"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL3642392"	""	"0"	"520.66"	"1"	"3.36"	"BDBM99670"	"CN1CCN(c2ccc(Nc3nc4c(Nc5ccccc5CN(C)S(C)(=O)=O)cccn4n3)cc2)CC1"	"IC50"	"'='"	"70.8"	"nM"	"7.15"	""	"216360"	"UO_0000065"	"13.73"	"0.26"	"3.79"	"7.29"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647884"	""	"0"	"440.94"	"0"	"3.53"	"BDBM147996"	"N#C[C@@H]1C[C@H](C(=O)NC2CCC2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"78.0"	"nM"	"7.11"	""	"285931"	"UO_0000065"	"16.12"	"0.31"	"3.58"	"5.65"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL2376158"	""	"0"	"450.41"	"0"	"1.65"	"9"	"C[C@@H](NC(=O)c1c[nH]c2ncc(-c3ncn4cc(F)cc(F)c34)nc12)C(=O)N1CC(C#N)C1"	"IC50"	"'='"	"37.0"	"nM"	"7.43"	""	""	"UO_0000065"	"16.50"	"0.31"	"5.78"	"5.63"	"False"	"CHEMBL2378515"	"Inhibition of JAK2 (unknown origin) using [33gammaP]ATP and Biotin-KAIETDKEYYTVKD as substrate incubated for 10 mins prior to substrate addition measured after 30 mins by filtration assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375236"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2376146"	""	"0"	"428.46"	"0"	"1.61"	"6c"	"C[C@@H](NC(=O)c1c[nH]c2ncc(-c3nn(C)c4ccccc34)nc12)C(=O)N1CC(C#N)C1"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	""	"UO_0000065"	"17.97"	"0.33"	"6.09"	"5.81"	"False"	"CHEMBL2378515"	"Inhibition of JAK2 (unknown origin) using [33gammaP]ATP and Biotin-KAIETDKEYYTVKD as substrate incubated for 10 mins prior to substrate addition measured after 30 mins by filtration assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375236"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL3335688"	""	"0"	"372.45"	"0"	"1.86"	"BDBM112505"	"CS(=O)(=O)N1CCC[C@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.0822"	"nM"	"10.09"	""	"233744"	"UO_0000065"	"27.08"	"0.53"	"8.23"	"9.71"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652313"	""	"0"	"421.57"	"0"	"2.39"	"BDBM113123"	"COC1CCN(S(=O)(=O)C[C@H]2CC[C@H](N(C)c3ncnc4[nH]ccc34)CC2)CC1"	"IC50"	"'='"	"107.0"	"nM"	"6.97"	""	"234566"	"UO_0000065"	"16.53"	"0.33"	"4.58"	"7.62"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3699548"	""	"0"	"344.81"	"0"	"3.03"	"BDBM147566"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2cncc(Cl)c2)n1"	"IC50"	"'='"	"39.0"	"nM"	"7.41"	""	"285496"	"UO_0000065"	"21.49"	"0.42"	"4.38"	"6.76"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702925"	""	"0"	"343.82"	"0"	"3.63"	"BDBM147624"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"120.0"	"nM"	"6.92"	""	"285558"	"UO_0000065"	"20.13"	"0.39"	"3.29"	"7.15"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645024"	""	"0"	"427.55"	"0"	"4.86"	"BDBM99778"	"CC(C)COc1cccc(-c2cccn3nc(Nc4ccc5c(c4)CCNCC5)nc23)c1"	"IC50"	"'='"	"32.64"	"nM"	"7.49"	""	"216463"	"UO_0000065"	"17.51"	"0.32"	"2.63"	"11.79"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3639467"	""	"0"	"399.48"	"0"	"2.31"	"BDBM148045"	"N#C[C@@H]1CCCC[C@H]1n1cc(C(N)=O)c(Nc2ccc3c(c2)CCS3(=O)=O)n1"	"IC50"	"'='"	"32.0"	"nM"	"7.50"	""	"285990"	"UO_0000065"	"18.76"	"0.37"	"5.18"	"5.73"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665132"	""	"0"	"400.51"	"0"	"2.63"	"BDBM112519"	"CC(C)S(=O)(=O)N1CCC[C@@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.7285"	"nM"	"9.14"	""	"233758"	"UO_0000065"	"22.81"	"0.45"	"6.51"	"8.80"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703026"	""	"0"	"444.94"	"0"	"4.14"	"BDBM147736"	"C[C@H](N[C@@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(Cl)c(F)c3)n2)[C@@H](C#N)C1)C1CC1"	"IC50"	"'='"	"215.0"	"nM"	"6.67"	""	"285670"	"UO_0000065"	"14.99"	"0.29"	"2.53"	"6.13"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652369"	""	"0"	"504.66"	"1"	"2.00"	"BDBM113180"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC[C@H](OCC(=O)N3CCCC3)C2)CC1"	"IC50"	"'='"	"29.6"	"nM"	"7.53"	""	"234623"	"UO_0000065"	"14.92"	"0.29"	"5.53"	"6.74"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3651054"	""	"0"	"375.46"	"0"	"4.57"	"BDBM153231"	"C=C(C)C(=O)Nc1cccc(-c2ncnc3[nH]cc(-c4cnc(C)s4)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294179"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL2177736"	""	"0"	"393.45"	"0"	"1.58"	"1, BIIB-057"	"NC(=O)c1cnc(N[C@@H]2CCCC[C@@H]2N)nc1Nc1cccc(-n2nccn2)c1"	"IC50"	"'='"	"1750.0"	"nM"	"5.76"	""	""	"UO_0000065"	"14.63"	"0.27"	"4.18"	"3.85"	"False"	"CHEMBL3268711"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3259804"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3262617"	""	"0"	"391.44"	"0"	"2.07"	"3g"	"N[C@H]1COCC[C@H]1Nc1cc2nc[nH]c(=O)c2c(Nc2cccc3cc[nH]c23)n1"	"IC50"	"'='"	"290.0"	"nM"	"6.54"	""	""	"UO_0000065"	"16.70"	"0.31"	"4.47"	"4.89"	"False"	"CHEMBL3268711"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3259804"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3262620"	""	"0"	"405.46"	"0"	"2.38"	"3j"	"Cc1c[nH]c2c(Nc3nc(N[C@@H]4CCOC[C@@H]4N)cc4nc[nH]c(=O)c34)cccc12"	"IC50"	"'='"	"184.0"	"nM"	"6.74"	""	""	"UO_0000065"	"16.61"	"0.31"	"4.36"	"5.04"	"False"	"CHEMBL3268711"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3259804"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL1650956"	""	"0"	"441.41"	"0"	"3.59"	"10"	"O=C1NC(=O)C(c2c[nH]c3ccccc23)=C1c1cc(N2CCOCC2)ccc1C(F)(F)F"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1657171"	"Inhibition of GST-tagged Jak2 expressed in insect cells using 20 uM ATP"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649080"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL3652295"	""	"0"	"423.54"	"0"	"0.71"	"BDBM113104"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC[C@H](O)[C@H](O)C2)CC1"	"IC50"	"'='"	"32.5"	"nM"	"7.49"	""	"234548"	"UO_0000065"	"17.68"	"0.35"	"6.78"	"6.11"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3647869"	""	"0"	"428.47"	"0"	"3.23"	"BDBM147981"	"CC(C)NC(=O)O[C@@H]1CCC(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"19.0"	"nM"	"7.72"	""	"285915"	"UO_0000065"	"18.02"	"0.34"	"4.49"	"5.72"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652379"	""	"0"	"460.65"	"0"	"2.84"	"BDBM113190"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCC[C@H]2CN2CCCC2)CC1"	"IC50"	"'='"	"40.6"	"nM"	"7.39"	""	"234633"	"UO_0000065"	"16.05"	"0.32"	"4.55"	"8.65"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3647900"	""	"0"	"456.93"	"0"	"2.45"	"BDBM148012"	"CC1(O)CN(C(=O)[C@@H]2CC[C@@H](n3cc(C(N)=O)c(Nc4ccc(Cl)cc4)n3)[C@H](C#N)C2)C1"	"IC50"	"'='"	"35.0"	"nM"	"7.46"	""	"285947"	"UO_0000065"	"16.32"	"0.32"	"5.01"	"5.43"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL2376436"	""	"0"	"419.49"	"0"	"3.40"	"12a"	"CC(=O)N[C@@H]1CCc2ccc(Oc3cnc4[nH]cc(C(=O)N[C@@H](C)C5CC5)c4n3)cc21"	"IC50"	"'='"	"3610.0"	"nM"	"5.44"	""	""	"UO_0000065"	"12.97"	"0.24"	"2.04"	"4.99"	"False"	"CHEMBL2378973"	"Inhibition of JAK2 in human PBMC expressing CD14 assessed as inhibition of GM-CSF-induced STAT5a phosphorylation"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375291"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2376338"	""	"0"	"336.40"	"0"	"3.38"	"1i"	"CC(C)NC(=O)c1c[nH]c2ncc(Oc3ccc4c(c3)CCC4)nc12"	"IC50"	"'='"	"580.0"	"nM"	"6.24"	""	""	"UO_0000065"	"18.54"	"0.34"	"2.86"	"7.81"	"False"	"CHEMBL2378977"	"Inhibition of JAK2 (unknown origin) expressed in SF21 cells using Biotin-KAIETDKEYYTVKD as substrate and [33Pgamma]ATP incubated for 10 mins prior to substrate addition measured after 30 mins by Topcount analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375291"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"CHEMBL4106362"	""
"CHEMBL2376330"	""	"0"	"296.33"	"0"	"2.89"	"1a"	"CC(C)NC(=O)c1c[nH]c2ncc(Oc3ccccc3)nc12"	"IC50"	"'='"	"250.0"	"nM"	"6.60"	""	""	"UO_0000065"	"22.28"	"0.41"	"3.71"	"8.26"	"False"	"CHEMBL2378977"	"Inhibition of JAK2 (unknown origin) expressed in SF21 cells using Biotin-KAIETDKEYYTVKD as substrate and [33Pgamma]ATP incubated for 10 mins prior to substrate addition measured after 30 mins by Topcount analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375291"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"CHEMBL4106362"	""
"CHEMBL3651048"	""	"0"	"368.44"	"1"	"5.11"	"BDBM153225"	"C=C(C)C(=O)Nc1cccc(-c2ncnc3[nH]cc(-c4ccccc4C)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294173"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665154"	""	"0"	"386.48"	"0"	"1.87"	"BDBM112547"	"Cn1ccc2ncc(-c3cccnc3N[C@H]3CCCN(S(C)(=O)=O)C3)nc21"	"IC50"	"'='"	"1.96"	"nM"	"8.71"	""	"233786"	"UO_0000065"	"22.53"	"0.44"	"6.84"	"9.36"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3650988"	""	"0"	"336.35"	"0"	"2.93"	"BDBM153163"	"C=CC(=O)Nc1cccc(-c2ncnc3[nH]cc(C(=O)OCC)c23)c1"	"IC50"	"'='"	"790.0"	"nM"	"6.10"	""	"294111"	"UO_0000065"	"18.14"	"0.33"	"3.17"	"6.29"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642356"	""	"0"	"506.64"	"1"	"3.82"	"BDBM99632"	"CN1CCC(c2ccc(Nc3nc4c(Nc5cccnc5N(C)S(C)(=O)=O)cccn4n3)cc2)CC1"	"IC50"	"'='"	"17.42"	"nM"	"7.76"	""	"216322"	"UO_0000065"	"15.31"	"0.29"	"3.94"	"7.20"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642408"	""	"0"	"508.62"	"1"	"4.03"	"BDBM99686"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4cccc(N5CCN(CCCF)CC5)c4)nc23)cc1"	"IC50"	"'='"	"4.93"	"nM"	"8.31"	""	"216375"	"UO_0000065"	"16.33"	"0.32"	"4.28"	"10.03"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3651004"	""	"0"	"380.40"	"0"	"2.81"	"BDBM153180"	"C=C(C)C(=O)Nc1cc(-c2ncnc3[nH]cc(C(=O)OCC)c23)ccc1CO"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294128"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3650994"	""	"0"	"350.38"	"0"	"3.23"	"BDBM153169"	"C=CC(=O)Nc1cccc(-c2ncnc3[nH]cc(C(=O)OCC)c23)c1C"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294117"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665180"	""	"0"	"430.54"	"0"	"1.86"	"BDBM112574"	"CC(C)CS(=O)(=O)N1CCC[C@H](Nc2nc(N)ncc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.0196"	"nM"	"10.71"	""	"233811"	"UO_0000065"	"24.87"	"0.49"	"8.85"	"7.50"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL461140"	""	"0"	"401.47"	"0"	"3.42"	"17"	"CN(C)CCOc1ccc(/C=C/c2cc(-c3cc4c(=O)[nH]cnc4[nH]3)ccn2)cc1"	"IC50"	"'='"	"3600.0"	"nM"	"5.44"	""	""	"UO_0000065"	"13.56"	"0.25"	"2.02"	"6.26"	"False"	"CHEMBL955790"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1152141"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2008"	"None"	""
"CHEMBL3651057"	""	"0"	"301.35"	"0"	"4.30"	"BDBM153234"	"COc1ccccc1-c1c[nH]c2ncnc(-c3ccccc3)c12"	"IC50"	"'='"	"183.0"	"nM"	"6.74"	""	"294182"	"UO_0000065"	"22.36"	"0.40"	"2.44"	"13.26"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL1221633"	""	"0"	"433.89"	"1"	"5.82"	"15"	"O=C(CCc1cn(Cc2ccc(Cl)cc2)c2ccccc12)Nc1ccc([N+](=O)[O-])cc1"	"IC50"	"'='"	"106700.0"	"nM"	""	"Outside typical range"	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1227372"	"Inhibition of recombinant JAK2 after 1 hr"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1221237"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL3928976"	""	"0"	"587.46"	"2"	"5.69"	"6c"	"Cc1c(-c2c(Cl)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)cc2c(Cl)cccn2c1=O"	"IC50"	"'='"	"1000.0"	"nM"	"6.00"	""	""	""	""	""	""	""	"False"	"CHEMBL4672879"	"Inhibition of JAK2 (unknown origin)"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4665894"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2020"	"None"	""
"CHEMBL1091565"	""	"0"	"485.54"	"0"	"4.46"	"13"	"COc1cc(-c2cnc3cccc(-c4ccc(C(=O)N5CCOCC5)cc4)c3n2)cc(OC)c1OC"	"IC50"	"'='"	"72.0"	"nM"	"7.14"	""	""	"UO_0000065"	"14.71"	"0.27"	"2.68"	"8.60"	"False"	"CHEMBL1116984"	"Inhibition of recombinant GST tagged JAK2 protein after 60 mins using FITC-GGEEEEYFELVKKKK-NH2 substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156975"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL3642364"	""	"0"	"506.63"	"1"	"3.96"	"BDBM99640"	"CS(=O)(=O)c1ccccc1CNc1cccn2nc(Nc3ccc(OCCN4CCCC4)cc3)nc12"	"IC50"	"'='"	"15.09"	"nM"	"7.82"	""	"216330"	"UO_0000065"	"15.44"	"0.30"	"3.86"	"7.75"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642282"	""	"0"	"476.61"	"0"	"3.29"	"BDBM99546"	"CN1CCN(Cc2ccc(Nc3nc4c(-c5ccc(S(C)(=O)=O)cc5)cccn4n3)cc2)CC1"	"IC50"	"'='"	"2.4"	"nM"	"8.62"	""	"216238"	"UO_0000065"	"18.09"	"0.35"	"5.33"	"10.41"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642303"	""	"0"	"531.69"	"1"	"3.12"	"BDBM99573"	"CN1CCN(c2cccc(Nc3nc4cccc(-c5ccc(CN6CCS(=O)(=O)CC6)cc5)n4n3)c2)CC1"	"IC50"	"'='"	"0.8"	"nM"	"9.10"	""	"216263"	"UO_0000065"	"17.11"	"0.33"	"5.98"	"10.57"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3665202"	""	"0"	"541.73"	"1"	"2.81"	"BDBM112601"	"CN1CCN(c2ncc(-c3cnc4[nH]ccc4n3)c(N[C@H]3CCCN(S(=O)(=O)CCC(C)(C)C)C3)n2)CC1"	"IC50"	"'='"	"0.0172"	"nM"	"10.76"	""	"233838"	"UO_0000065"	"19.87"	"0.39"	"7.95"	"8.73"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703038"	""	"0"	"504.56"	"1"	"4.07"	"BDBM147748"	"CC1(C)CN([C@@H]2CC[C@H](n3cc(C(N)=O)c(Nc4ccc([C@@](C)(O)C(F)(F)F)cc4)n3)[C@@H](C#N)C2)C1"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	"285682"	"UO_0000065"	"15.70"	"0.30"	"3.85"	"6.59"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3658120"	""	"0"	"644.66"	"1"	"4.79"	"BDBM148439"	"Cc1ccc(NC(=O)c2cc(C(F)(F)F)ccn2)cc1N1CCc2nc(Nc3ccc(C(=O)N4CCN(C)CC4)cc3)ncc2C1=O"	"IC50"	"'='"	"70.0"	"nM"	"7.16"	""	"286804"	"UO_0000065"	"11.10"	"0.21"	"2.36"	"5.79"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL2376149"	""	"0"	"458.48"	"0"	"1.62"	"6f"	"COc1ccc2c(-c3cnc4[nH]cc(C(=O)N[C@H](C)C(=O)N5CC(C#N)C5)c4n3)nn(C)c2c1"	"IC50"	"'='"	"880.0"	"nM"	"6.06"	""	""	"UO_0000065"	"13.21"	"0.24"	"4.44"	"4.27"	"False"	"CHEMBL2378509"	"Inhibition of JAK2 in human monocytes expressing CD14 assessed as inhibition of GM-CSF-stimulated STAT5a phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375236"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL3642324"	""	"0"	"463.56"	"0"	"3.38"	"BDBM99596"	"COc1ccc(Nc2nc3cccc(-c4ccc(CN5CCS(=O)(=O)CC5)cc4)n3n2)cc1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"216286"	"UO_0000065"	"19.41"	"0.37"	"5.62"	"10.13"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL2443044"	""	"0"	"454.44"	"0"	"3.28"	"18, NMS-E973"	"CN1CCC(NC(=O)c2cc(-c3c(O)cc(O)cc3Oc3ccc([N+](=O)[O-])cc3)on2)CC1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2443999"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2439976"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2013"	"None"	""
"CHEMBL559626"	""	"0"	"438.66"	"1"	"6.51"	"G6, NSC-33994"	"CC/C(=C(/CC)c1ccc(O)c(CN(CC)CC)c1)c1ccc(O)c(CN(CC)CC)c1"	"IC50"	"'='"	"60.0"	"nM"	"7.22"	""	""	"UO_0000065"	"16.46"	"0.31"	"0.71"	"15.39"	"False"	"CHEMBL1033558"	"Inhibition of recombinant JAK2-Val617Phe kinase activity after 30 mins by luminometry"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1158435"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1789941"	"RUXOLITINIB"	"4"	"306.37"	"0"	"3.47"	"3, INCB-018424"	"N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"27.82"	"0.51"	"5.05"	"10.25"	"True"	"CHEMBL1292866"	"Inhibition of human recombinant JAK2 by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287810"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL392371"	""	"0"	"495.59"	"0"	"3.26"	"22"	"C[C@@H](Nc1nc(-n2cnc3ccncc32)nc2c1cc(C(=O)N1CCN(C)CC1)n2C)c1ccccc1"	"IC50"	"'='"	"298.0"	"nM"	"6.53"	""	""	"UO_0000065"	"13.17"	"0.24"	"3.27"	"6.73"	"False"	"CHEMBL897052"	"Inhibition of JAK2 by kinase-Glo luminescent assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1148837"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2007"	"None"	""
"CHEMBL392998"	""	"0"	"552.62"	"1"	"3.99"	"20"	"C[C@H](Nc1nc(-n2cnc3ccncc32)nc2c1cc(C(=O)NS(=O)(=O)c1ccccc1)n2C)c1ccccc1"	"IC50"	"'='"	"359.0"	"nM"	"6.45"	""	""	"UO_0000065"	"11.66"	"0.22"	"2.45"	"4.71"	"False"	"CHEMBL897052"	"Inhibition of JAK2 by kinase-Glo luminescent assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1148837"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2007"	"None"	""
"CHEMBL391096"	""	"0"	"482.55"	"0"	"3.35"	"14"	"C[C@H](Nc1nc(-n2cnc3ccncc32)nc2c1cc(C(=O)N1CCOCC1)n2C)c1ccccc1"	"IC50"	"'='"	"21.0"	"nM"	"7.68"	""	""	"UO_0000065"	"15.91"	"0.29"	"4.33"	"7.45"	"False"	"CHEMBL897052"	"Inhibition of JAK2 by kinase-Glo luminescent assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1148837"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2007"	"None"	""
"CHEMBL233555"	""	"0"	"483.58"	"0"	"3.17"	"11"	"C[C@H](Nc1nc(-n2cnc3ccncc32)nc2c1cc(C(=O)NCCN(C)C)n2C)c1ccccc1"	"IC50"	"'='"	"19.0"	"nM"	"7.72"	""	""	"UO_0000065"	"15.97"	"0.29"	"4.55"	"7.30"	"False"	"CHEMBL897052"	"Inhibition of JAK2 by kinase-Glo luminescent assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1148837"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2007"	"None"	""
"CHEMBL1287853"	"FEDRATINIB"	"4"	"524.69"	"1"	"4.82"	"2, TG101348"	"Cc1cnc(Nc2ccc(OCCN3CCCC3)cc2)nc1Nc1cccc(S(=O)(=O)NC(C)(C)C)c1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"16.24"	"0.31"	"3.70"	"7.86"	"True"	"CHEMBL1292866"	"Inhibition of human recombinant JAK2 by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287810"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1287940"	""	"0"	"373.32"	"0"	"2.36"	"14"	"COC(=O)c1ccc(Nc2nc(N)n(C(=O)c3c(F)cccc3F)n2)cc1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1292866"	"Inhibition of human recombinant JAK2 by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287810"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL4541350"	""	"0"	"295.35"	"0"	"2.83"	"26"	"CCNc1ccccc1C(=O)Nc1ccc2[nH]nc(N)c2c1"	"IC50"	"'='"	"1970.0"	"nM"	"5.71"	""	""	"UO_0000065"	"19.32"	"0.35"	"2.88"	"5.95"	"False"	"CHEMBL4481929"	"Inhibition of JAK2 (unknown origin) after 1 hr FRET-based Z'-Lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480435"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4559204"	""	"0"	"321.17"	"0"	"3.70"	"30e"	"Nc1n[nH]c2ccc(NC(=O)c3cc(Cl)ccc3Cl)cc12"	"IC50"	"'='"	"23.0"	"nM"	"7.64"	""	""	"UO_0000065"	"23.78"	"0.50"	"3.94"	"9.11"	"False"	"CHEMBL4481929"	"Inhibition of JAK2 (unknown origin) after 1 hr FRET-based Z'-Lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480435"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4226840"	""	"0"	"382.45"	"0"	"1.73"	"12"	"CN(c1ncnc2[nH]ccc12)[C@@H]1CCN(S(=O)(=O)c2cccc(C#N)c2)C1"	"IC50"	"'='"	"57.0"	"nM"	"7.24"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4225530"	""	"0"	"301.39"	"0"	"2.04"	"18"	"CC(C)CC(=O)N1CC[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"3900.0"	"nM"	"5.41"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4229278"	""	"0"	"317.39"	"0"	"2.26"	"19"	"CC(C)COC(=O)N1CC[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"4300.0"	"nM"	"5.37"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4227709"	""	"0"	"375.43"	"0"	"2.00"	"30"	"CN(c1ncnc2[nH]ccc12)[C@@H]1CCN(S(=O)(=O)c2ccc(F)cc2)C1"	"IC50"	"'='"	"110.0"	"nM"	"6.96"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL564679"	""	"0"	"468.78"	"1"	"5.96"	"24a"	"Oc1ccc(CCN2CCc3c([nH]c4ccc(Br)cc34)-c3c2ccnc3Cl)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1036442"	"Inhibition of recombinant JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1151875"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2009"	"None"	""
"CHEMBL1302460"	""	"0"	"442.52"	"1"	"5.28"	"SID24836171"	"Cc1ccc(NC(=O)C(=Cc2ccc(C(=O)O)cc2)C(=O)Nc2ccc(C)cc2C)c(C)c1"	"IC50"	"'='"	"5462.0"	"nM"	"5.26"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1530569"	""	"0"	"382.41"	"0"	"4.01"	"SID26660517"	"Oc1ccccc1OCCOc1ccccc1OCCOc1ccccc1O"	"IC50"	"'='"	"7122.0"	"nM"	"5.15"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1330242"	""	"0"	"327.81"	"0"	"2.60"	"SID4258362"	"O=C(NC1C=CS(=O)(=O)C1)c1sc2ccccc2c1Cl"	"IC50"	"'='"	"13770.0"	"nM"	"4.86"	""	"Not Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL120563"	"THIRAM"	"0"	"240.44"	"0"	"2.06"	"SID11532980"	"CN(C)C(=S)SSC(=S)N(C)C"	"IC50"	"'='"	"223.0"	"nM"	"6.65"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1520801"	""	"0"	"365.01"	"0"	"4.22"	"SID24812398"	"Cc1nc([N+](=O)[O-])c(Br)n1Cc1ccc(Cl)c(Cl)c1"	"IC50"	"'='"	"8441.0"	"nM"	"5.07"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1481601"	""	"0"	"279.72"	"0"	"3.79"	"SID26669556"	"CC(C)(C)/C(O)=C/c1nc2cc(Cl)ccc2oc1=O"	"IC50"	"'='"	"9549.0"	"nM"	"5.02"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1411125"	""	"0"	"368.39"	"0"	"3.18"	"SID26731158"	"COc1cc(/C=C2\COC/C(=C\c3ccc(O)c(OC)c3)C2=O)ccc1O"	"IC50"	"'='"	"3615.0"	"nM"	"5.44"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1386220"	""	"0"	"278.23"	"0"	"3.82"	"SID14718839"	"O=C(Nc1cccc2c1[nH]c1ccccc12)C(F)(F)F"	"IC50"	"'='"	"13710.0"	"nM"	"4.86"	""	"Not Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1976304"	""	"0"	"362.81"	"0"	"2.99"	"SID14727518"	"COC1(OC)C(/C=C/c2ccc(Cl)cc2)C(C#N)(C#N)C1(OC)OC"	"IC50"	"'='"	"7832.0"	"nM"	"5.11"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1543839"	""	"0"	"333.56"	"0"	"3.02"	"SID17402821"	"O=C(OCn1ncc(Cl)c(Cl)c1=O)c1ccccc1Cl"	"IC50"	"'='"	"1199.0"	"nM"	"5.92"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1466593"	""	"0"	"352.32"	"0"	"0.22"	"SID26729567"	"COc1cccc(F)c1C(C[N+](=O)[O-])c1c(N)n(C)c(=O)n(C)c1=O"	"IC50"	"'='"	"4217.0"	"nM"	"5.38"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1427637"	""	"0"	"323.40"	"0"	"2.72"	"SID7974352"	"COc1ccc(Nc2ccc3c(c2)=NC2(CCCCC2)[N+]=3[O-])cc1"	"IC50"	"'='"	"1711.0"	"nM"	"5.77"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL564201"	"6-AZAURIDINE"	"0"	"245.19"	"0"	"-3.46"	"SID8139884"	"O=c1cnn([C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)c(=O)[nH]1"	"IC50"	"'='"	"6798.0"	"nM"	"5.17"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL4781984"	""	"0"	"369.39"	"0"	"2.53"	"23, cis isomer"	"N#CC[C@]1(n2cc(-c3nc(-c4cn[nH]c4)cn4nccc34)cn2)C[C@@H](C#N)C1"	"IC50"	"'='"	"22.0"	"nM"	"7.66"	""	""	""	""	""	""	""	"False"	"CHEMBL4675813"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using FITC-KGGEEEEYFELVKK as substrate in presence of ATP at Km by microfluidic assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4673239"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4780288"	""	"0"	"397.45"	"0"	"2.93"	"19, cis isomer"	"Cn1cc(-c2cn3nccc3c(-c3cnn([C@]4(CC#N)C[C@H](CC#N)C4)c3)n2)cn1"	"IC50"	"'='"	"38.0"	"nM"	"7.42"	""	""	""	""	""	""	""	"False"	"CHEMBL4675813"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using FITC-KGGEEEEYFELVKK as substrate in presence of ATP at Km by microfluidic assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4673239"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL1290196"	""	"0"	"322.41"	"0"	"3.83"	"12"	"CC(Nc1nc2cc[nH]c(=O)c2cc1-c1ccccn1)C(C)(C)C"	"IC50"	"'='"	"630.0"	"nM"	"6.20"	""	""	"UO_0000065"	"19.23"	"0.35"	"2.37"	"8.77"	"False"	"CHEMBL1291235"	"Inhibition of JAK2 in cell-free system"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287746"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL386637"	""	"0"	"526.54"	"1"	"4.40"	"6l"	"CN(C)[C@H]1CCCN(c2ccc(C(F)(F)F)cc2NC(=O)c2cc(C#Cc3cnc(N)nc3)ccc2F)C1"	"IC50"	"'='"	"550.0"	"nM"	"6.26"	""	""	"UO_0000065"	"11.89"	"0.22"	"1.86"	"7.16"	"False"	"CHEMBL910182"	"Inhibition of Jak2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1141381"	"1"	"Scientific Literature"	"J. Med. Chem."	"2007"	"None"	""
"CHEMBL232149"	""	"0"	"447.55"	"0"	"2.30"	"21"	"CN1CCN(C(=O)c2cc3c(NC(C)(C)C)nc(-n4cnc5ccncc54)nc3n2C)CC1"	"IC50"	"'='"	"323.0"	"nM"	"6.49"	""	""	"UO_0000065"	"14.50"	"0.27"	"4.19"	"6.69"	"False"	"CHEMBL897052"	"Inhibition of JAK2 by kinase-Glo luminescent assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1148837"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2007"	"None"	""
"CHEMBL232147"	""	"0"	"477.57"	"0"	"1.66"	"19"	"C[C@H](Nc1nc(-n2cnc3ccncc32)nc2c1cc(C(=O)N1CCN(C)CC1)n2C)C(C)(C)O"	"IC50"	"'='"	"209.0"	"nM"	"6.68"	""	""	"UO_0000065"	"13.99"	"0.26"	"5.02"	"5.70"	"False"	"CHEMBL897052"	"Inhibition of JAK2 by kinase-Glo luminescent assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1148837"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2007"	"None"	""
"CHEMBL393375"	""	"0"	"532.01"	"1"	"3.50"	"18"	"COc1ccc(Cl)c(Nc2nc(-n3cnc4ccncc43)nc3c2cc(C(=O)N2CCN(C)CC2)n3C)c1"	"IC50"	"'='"	"132.0"	"nM"	"6.88"	""	""	"UO_0000065"	"12.93"	"0.25"	"3.38"	"6.48"	"False"	"CHEMBL897052"	"Inhibition of JAK2 by kinase-Glo luminescent assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1148837"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2007"	"None"	""
"CHEMBL231949"	""	"0"	"463.55"	"0"	"1.54"	"17"	"COC[C@H](C)Nc1nc(-n2cnc3ccncc32)nc2c1cc(C(=O)N1CCN(C)CC1)n2C"	"IC50"	"'='"	"222.0"	"nM"	"6.65"	""	""	"UO_0000065"	"14.35"	"0.27"	"5.11"	"6.26"	"False"	"CHEMBL897052"	"Inhibition of JAK2 by kinase-Glo luminescent assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1148837"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2007"	"None"	""
"CHEMBL2376147"	""	"0"	"446.45"	"0"	"1.75"	"6d"	"C[C@@H](NC(=O)c1c[nH]c2ncc(-c3nn(C)c4cc(F)ccc34)nc12)C(=O)N1CC(C#N)C1"	"IC50"	"'='"	"740.0"	"nM"	"6.13"	""	""	"UO_0000065"	"13.73"	"0.25"	"4.38"	"4.62"	"False"	"CHEMBL2378509"	"Inhibition of JAK2 in human monocytes expressing CD14 assessed as inhibition of GM-CSF-stimulated STAT5a phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375236"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2376155"	""	"0"	"504.98"	"1"	"3.29"	"6l"	"Cn1nc(-c2cnc3[nH]cc(C(=O)N[C@@H](C(=O)N4CC(C#N)C4)C(C)(C)C)c3n2)c2ccc(Cl)cc21"	"IC50"	"'='"	"1.3"	"nM"	"8.89"	""	""	"UO_0000065"	"17.60"	"0.34"	"5.60"	"6.70"	"False"	"CHEMBL2378515"	"Inhibition of JAK2 (unknown origin) using [33gammaP]ATP and Biotin-KAIETDKEYYTVKD as substrate incubated for 10 mins prior to substrate addition measured after 30 mins by filtration assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375236"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2381983"	""	"0"	"434.43"	"0"	"3.07"	"9"	"Cc1cc(Nc2nc(N[C@@H](C)c3ncc(F)cc3F)c(F)c(N3CCOCC3)n2)n[nH]1"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	""	"UO_0000065"	"18.77"	"0.36"	"5.08"	"7.85"	"False"	"CHEMBL2383798"	"Inhibition of JAK2 TEL domain (unknown origin) transfected in mouse Ba/F3 cells"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2380256"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"CHEMBL3307634"	""
"CHEMBL1288002"	""	"0"	"358.35"	"0"	"2.64"	"20"	"CN(C)c1ccc(Nc2nc(N)n(C(=O)c3c(F)cccc3F)n2)cc1"	"IC50"	"'='"	"2500.0"	"nM"	"5.60"	""	""	"UO_0000065"	"15.63"	"0.29"	"2.96"	"6.29"	"False"	"CHEMBL1292866"	"Inhibition of human recombinant JAK2 by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287810"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1288032"	""	"0"	"316.27"	"0"	"1.97"	"21"	"Nc1nc(Nc2cccnc2)nn1C(=O)c1c(F)cccc1F"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1292866"	"Inhibition of human recombinant JAK2 by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1287810"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL2380329"	""	"0"	"432.89"	"0"	"3.45"	"12"	"Cc1cc(Nc2nc(N[C@@H](C)c3ccc(F)cn3)c(Cl)c(N3CCOCC3)n2)n[nH]1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	""	"UO_0000065"	"18.99"	"0.37"	"4.77"	"7.91"	"False"	"CHEMBL2383938"	"Inhibition of JAK2 (unknown origin) using biotinylated TYK2 peptide as substrate after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2380256"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2381976"	""	"0"	"415.45"	"0"	"2.51"	"13, table2"	"Cc1cc(Nc2nc(N[C@@H](C)c3ccc(F)cn3)c(F)c(N3CCNCC3)n2)n[nH]1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	""	"UO_0000065"	"20.21"	"0.38"	"5.89"	"7.87"	"False"	"CHEMBL2383938"	"Inhibition of JAK2 (unknown origin) using biotinylated TYK2 peptide as substrate after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2380256"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL479619"	""	"0"	"199.22"	"0"	"1.54"	"4"	"Nc1n[nH]c2ccc(-c3cc[nH]n3)cc12"	"IC50"	"'='"	"9300.0"	"nM"	"5.03"	""	""	"UO_0000065"	"25.26"	"0.46"	"3.49"	"6.03"	"False"	"CHEMBL1011746"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139271"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL479830"	""	"0"	"308.39"	"0"	"2.64"	"17"	"Nc1n[nH]c2ccc(-c3ccc(CN4CCOCC4)cc3)cc12"	"IC50"	"'='"	"1110.0"	"nM"	"5.96"	""	""	"UO_0000065"	"19.31"	"0.35"	"3.31"	"8.87"	"False"	"CHEMBL1011746"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139271"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL465091"	""	"0"	"212.05"	"0"	"1.91"	"1"	"Nc1n[nH]c2ccc(Br)cc12"	"IC50"	"'='"	"40900.0"	"nM"	"4.39"	""	""	"UO_0000065"	"20.69"	"0.54"	"2.48"	"8.02"	"False"	"CHEMBL1011746"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139271"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL480411"	""	"0"	"344.44"	"0"	"2.89"	"13"	"CC(C)(C)NS(=O)(=O)c1ccc(-c2ccc3[nH]nc(N)c3c2)cc1"	"IC50"	"'='"	"206.0"	"nM"	"6.69"	""	""	"UO_0000065"	"19.41"	"0.38"	"3.80"	"6.63"	"False"	"CHEMBL1011748"	"Inhibition of JAK2 V617F mutant"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139271"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL509032"	"TAE-684"	"0"	"614.22"	"2"	"5.02"	"TAE-684"	"COc1cc(N2CCC(N3CCN(C)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2S(=O)(=O)C(C)C)n1"	"IC50"	"'='"	"1505.0"	"nM"	"5.82"	""	""	"UO_0000065"	"9.48"	"0.19"	"0.80"	"5.66"	"False"	"CHEMBL1006340"	"Inhibition of Tel-fused JAK2 kinase-mediated mouse BaF3 cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156430"	"1"	"Scientific Literature"	"Proc. Natl. Acad. Sci. U.S.A."	"2007"	"CHEMBL3307634"	""
"CHEMBL1650729"	""	"0"	"393.22"	"0"	"3.12"	"9j"	"Cc1cc(Nc2nc(N[C@@H](C)c3ncc(F)cn3)ncc2Br)n[nH]1"	"IC50"	"'<'"	"3.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1656588"	"Inhibition of JAK2 using Km ATP concentration"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1650724"	""	"0"	"374.81"	"0"	"3.58"	"9b"	"C[C@H](Nc1ncc(Cl)c(Nc2cc(C3CC3)[nH]n2)n1)c1ncc(F)cn1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1656589"	"Inhibition of JAK2 using 5 mM of ATP"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1650730"	""	"0"	"377.82"	"0"	"2.76"	"9k"	"C[C@H](Nc1ncc(Cl)c(Nc2cc(N(C)C)[nH]n2)n1)c1ncc(F)cn1"	"IC50"	"'='"	"488.0"	"nM"	"6.31"	""	""	"UO_0000065"	"16.71"	"0.33"	"3.55"	"5.87"	"False"	"CHEMBL1656589"	"Inhibition of JAK2 using 5 mM of ATP"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1789941"	"RUXOLITINIB"	"4"	"306.37"	"0"	"3.47"	"1b"	"N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'<'"	"0.3"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2378515"	"Inhibition of JAK2 (unknown origin) using [33gammaP]ATP and Biotin-KAIETDKEYYTVKD as substrate incubated for 10 mins prior to substrate addition measured after 30 mins by filtration assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375236"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL1650723"	""	"0"	"364.77"	"0"	"2.71"	"9a"	"COc1cc(Nc2nc(N[C@@H](C)c3ncc(F)cn3)ncc2Cl)n[nH]1"	"IC50"	"'='"	"108.0"	"nM"	"6.97"	""	""	"UO_0000065"	"19.10"	"0.38"	"4.26"	"6.14"	"False"	"CHEMBL1656589"	"Inhibition of JAK2 using 5 mM of ATP"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1231124"	"AZD-1480"	"2"	"348.77"	"0"	"3.01"	"9e"	"Cc1cc(Nc2nc(N[C@@H](C)c3ncc(F)cn3)ncc2Cl)[nH]n1"	"IC50"	"'='"	"58.0"	"nM"	"7.24"	""	""	"UO_0000065"	"20.75"	"0.41"	"4.23"	"6.94"	"False"	"CHEMBL1656589"	"Inhibition of JAK2 using 5 mM of ATP"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL3116058"	""	"0"	"364.39"	"0"	"3.21"	"13a"	"C[C@H](Nc1nc(Nc2cn(C)cn2)c2ccccc2n1)c1ncc(F)cn1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"23.39"	"0.43"	"5.31"	"9.12"	"False"	"CHEMBL3118240"	"Inhibition of Jak2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112447"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL3916210"	""	"0"	"418.40"	"0"	"2.36"	"BDBM237800"	"N#C[C@@H]1CCN(C(=O)OCCF)C[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"56.0"	"nM"	"7.25"	""	"414904"	"UO_0000065"	"17.33"	"0.33"	"4.89"	"5.74"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3973945"	""	"0"	"485.52"	"0"	"1.72"	"BDBM237808"	"N#C[C@@H]1CCN(C(=O)OCCN2CCOCC2)C[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"85.0"	"nM"	"7.07"	""	"414912"	"UO_0000065"	"14.56"	"0.28"	"5.35"	"5.10"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3968880"	""	"0"	"409.43"	"0"	"2.44"	"BDBM237821"	"N#C[C@@H]1CCN(Cc2ncco2)C[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"22.0"	"nM"	"7.66"	""	"414925"	"UO_0000065"	"18.70"	"0.35"	"5.22"	"6.08"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3981489"	""	"0"	"396.47"	"0"	"3.05"	"BDBM237825"	"N#C[C@@H]1CCN(CC2CCC2)C[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"33.0"	"nM"	"7.48"	""	"414929"	"UO_0000065"	"18.87"	"0.35"	"4.43"	"7.48"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3892314"	""	"0"	"422.47"	"0"	"2.18"	"BDBM237826"	"Cn1nccc1CN1CC[C@@H](C#N)[C@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)C1"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	"414930"	"UO_0000065"	"18.22"	"0.34"	"5.52"	"6.54"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4110650"	""	"0"	"383.45"	"0"	"2.71"	"BDBM237888"	"COC(C)(C)c1ccc(Nc2nn([C@H]3COCC[C@@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	"414990"	"UO_0000065"	"20.26"	"0.38"	"5.06"	"6.74"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4115665"	""	"0"	"498.56"	"0"	"1.64"	"BDBM237745"	"CN1CCN(CCOC(=O)N2CC[C@@H](n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)[C@H](C#N)C2)CC1"	"IC50"	"'='"	"1070.0"	"nM"	"5.97"	""	"414849"	"UO_0000065"	"11.98"	"0.23"	"4.33"	"4.50"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4112066"	""	"0"	"328.35"	"0"	"1.54"	"BDBM237719"	"N#C[C@@H]1CNCC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"81.0"	"nM"	"7.09"	""	"414823"	"UO_0000065"	"21.60"	"0.40"	"5.55"	"6.52"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4114241"	""	"0"	"483.55"	"0"	"2.73"	"BDBM237728"	"CN1CCC(COC(=O)N2CC[C@@H](n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)[C@H](C#N)C2)CC1"	"IC50"	"'='"	"1089.0"	"nM"	"5.96"	""	"414832"	"UO_0000065"	"12.33"	"0.23"	"3.23"	"4.60"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4107008"	""	"0"	"440.48"	"0"	"3.33"	"BDBM237732"	"N#C[C@@H]1CN(C(=O)OC2CCCC2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"756.0"	"nM"	"6.12"	""	"414836"	"UO_0000065"	"13.90"	"0.26"	"2.79"	"4.85"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4114652"	""	"0"	"466.42"	"0"	"2.02"	"BDBM237741"	"N#C[C@@H]1CN(C(=O)OCC(F)(F)CO)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"106.0"	"nM"	"6.97"	""	"414845"	"UO_0000065"	"14.95"	"0.29"	"4.95"	"4.76"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4107667"	""	"0"	"442.45"	"0"	"2.18"	"BDBM237746"	"N#C[C@@H]1CN(C(=O)OC2CCOC2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"255.0"	"nM"	"6.59"	""	"414850"	"UO_0000065"	"14.90"	"0.28"	"4.41"	"4.87"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4109536"	""	"0"	"444.47"	"0"	"2.42"	"BDBM237784"	"COCCCOC(=O)N1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@H](C#N)C1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"414888"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3983426"	""	"0"	"454.38"	"0"	"2.95"	"BDBM237799"	"N#C[C@@H]1CCN(C(=O)OCC(F)(F)F)C[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"61.0"	"nM"	"7.21"	""	"414903"	"UO_0000065"	"15.88"	"0.31"	"4.26"	"5.71"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"CP690, 550"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	""	"UO_0000065"	"26.88"	"0.50"	"6.86"	"9.45"	"True"	"CHEMBL2378977"	"Inhibition of JAK2 (unknown origin) expressed in SF21 cells using Biotin-KAIETDKEYYTVKD as substrate and [33Pgamma]ATP incubated for 10 mins prior to substrate addition measured after 30 mins by Topcount analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375291"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"CHEMBL4106362"	""
"CHEMBL2376436"	""	"0"	"419.49"	"0"	"3.40"	"12a"	"CC(=O)N[C@@H]1CCc2ccc(Oc3cnc4[nH]cc(C(=O)N[C@@H](C)C5CC5)c4n3)cc21"	"IC50"	"'='"	"84.0"	"nM"	"7.08"	""	""	"UO_0000065"	"16.87"	"0.31"	"3.68"	"6.49"	"False"	"CHEMBL2378977"	"Inhibition of JAK2 (unknown origin) expressed in SF21 cells using Biotin-KAIETDKEYYTVKD as substrate and [33Pgamma]ATP incubated for 10 mins prior to substrate addition measured after 30 mins by Topcount analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375291"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"CHEMBL4106362"	""
"CHEMBL2376337"	""	"0"	"322.37"	"0"	"3.28"	"1h"	"CC(NC(=O)c1c[nH]c2ncc(Oc3ccccc3)nc12)C1CC1"	"IC50"	"'='"	"70.0"	"nM"	"7.16"	""	""	"UO_0000065"	"22.19"	"0.41"	"3.87"	"8.95"	"False"	"CHEMBL2378977"	"Inhibition of JAK2 (unknown origin) expressed in SF21 cells using Biotin-KAIETDKEYYTVKD as substrate and [33Pgamma]ATP incubated for 10 mins prior to substrate addition measured after 30 mins by Topcount analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375291"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"CHEMBL4106362"	""
"CHEMBL2376336"	""	"0"	"310.36"	"0"	"3.20"	"1g"	"Cc1ccccc1Oc1cnc2[nH]cc(C(=O)NC(C)C)c2n1"	"IC50"	"'='"	"2320.0"	"nM"	"5.63"	""	""	"UO_0000065"	"18.15"	"0.33"	"2.43"	"7.05"	"False"	"CHEMBL2378977"	"Inhibition of JAK2 (unknown origin) expressed in SF21 cells using Biotin-KAIETDKEYYTVKD as substrate and [33Pgamma]ATP incubated for 10 mins prior to substrate addition measured after 30 mins by Topcount analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375291"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"CHEMBL4106362"	""
"CHEMBL2376334"	""	"0"	"321.34"	"0"	"2.76"	"1e"	"CC(C)NC(=O)c1c[nH]c2ncc(Oc3cccc(C#N)c3)nc12"	"IC50"	"'='"	"1250.0"	"nM"	"5.90"	""	""	"UO_0000065"	"18.37"	"0.34"	"3.14"	"5.69"	"False"	"CHEMBL2378977"	"Inhibition of JAK2 (unknown origin) expressed in SF21 cells using Biotin-KAIETDKEYYTVKD as substrate and [33Pgamma]ATP incubated for 10 mins prior to substrate addition measured after 30 mins by Topcount analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375291"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"CHEMBL4106362"	""
"CHEMBL1789941"	"RUXOLITINIB"	"4"	"306.37"	"0"	"3.47"	"Ruxolitinib"	"N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"6.85"	"nM"	"8.16"	""	""	"UO_0000065"	"26.65"	"0.48"	"4.69"	"9.82"	"False"	"CHEMBL2186603"	"Inhibition of JAK2 in human TF1 cells assessed as reduction in STAT5 phosphorylation incubated for 30 mins in presence of human recombinant EPO"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176876"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"CHEMBL3307972"	""
"CHEMBL4111745"	""	"0"	"439.52"	"0"	"3.22"	"BDBM237850"	"Cc1ncc(CN2CC[C@@H](n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)[C@H](C#N)C2)s1"	"IC50"	"'='"	"104.0"	"nM"	"6.98"	""	"414954"	"UO_0000065"	"15.89"	"0.31"	"3.76"	"6.19"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4106905"	""	"0"	"425.47"	"0"	"2.42"	"BDBM237852"	"CC1=NOC(CN2CC[C@@H](n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)[C@H](C#N)C2)C1"	"IC50"	"'='"	"37.0"	"nM"	"7.43"	""	"414956"	"UO_0000065"	"17.47"	"0.33"	"5.01"	"6.11"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4114032"	""	"0"	"396.47"	"0"	"3.05"	"BDBM237853"	"N#C[C@@H]1CN(CC2CCC2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"66.0"	"nM"	"7.18"	""	"414957"	"UO_0000065"	"18.11"	"0.34"	"4.13"	"7.18"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3914858"	""	"0"	"330.32"	"0"	"1.36"	"BDBM237914"	"N#C[C@@H]1CCOC[C@H]1n1cc(C(N)=O)c(Nc2ccnc(F)c2)n1"	"IC50"	"'='"	"111.0"	"nM"	"6.96"	""	"414969"	"UO_0000065"	"21.05"	"0.40"	"5.59"	"5.85"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3953929"	""	"0"	"308.39"	"0"	"3.86"	"BDBM197716"	"CCCCCC(CC#N)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"0.29"	"nM"	"9.54"	""	"351115"	"UO_0000065"	"30.93"	"0.57"	"5.68"	"11.47"	"False"	"CHEMBL3887743"	"Kinase Assay: The compounds of the invention were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Biochemistry 1999, 269, 94-104. The catalytic domains of human JAK1 (a.a. 837-1142), JAK2 (a.a. 828-1132) and JAK3 (a.a. 781-1124) with an N-terminal His tag were expressed using baculovirus in insect cells and purified. The catalytic activity of JAK1, JAK2 or JAK3 was assayed by measuring the phosphorylation of a biotinylated peptide. The phosphorylated peptide was detected by homogenous time resolved fluorescence (HTRF). IC50 was measured for each kinase in the 40 uL reactions that contain the enzyme, ATP and 500 nM peptide in 50 mM Tris (pH 7.8) buffer with 100 mM NaCl, 5 mM DTT, and 0.1 mg/mL (0.01%) BSA. The ATP concentration in the reactions was 90 uM for Jak1, 30 uM for Jak2 and 3 uM for Jak3. Reactions were carried out at room temperature for 1 hr and then stopped with 20 uL 45 mM EDTA."	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886433"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3900232"	""	"0"	"442.95"	"0"	"3.12"	"BDBM239948"	"CN(c1nc(Nc2cnn(C)c2)ncc1Cl)C1CCC2(CC1)CCN(C(=O)CC#N)C2"	"IC50"	"'='"	"83.0"	"nM"	"7.08"	""	"418569"	"UO_0000065"	"15.99"	"0.31"	"3.96"	"6.88"	"False"	"CHEMBL3888834"	"Kinase Assay: JAK2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 100 μM KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC, 10 mM MgAcetate and [γ-33P-ATP](specific activity approx. 500 cpm/pmol, concentration as required). The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of 3% phosphoric acid solution. 10 μL of the reaction is then spotted onto a P30 filtermat and washed three times for 5 minutes in 75 mM phosphoric acid and once in methanol prior to drying and scintillation counting."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886854"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3944322"	""	"0"	"428.93"	"0"	"3.09"	"BDBM239955"	"Cn1cc(Nc2ncc(Cl)c(NC3CCC4(CC3)CCN(C(=O)CC#N)C4)n2)cn1"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	"418576"	"UO_0000065"	"18.24"	"0.36"	"4.73"	"7.00"	"False"	"CHEMBL3888834"	"Kinase Assay: JAK2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 100 μM KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC, 10 mM MgAcetate and [γ-33P-ATP](specific activity approx. 500 cpm/pmol, concentration as required). The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of 3% phosphoric acid solution. 10 μL of the reaction is then spotted onto a P30 filtermat and washed three times for 5 minutes in 75 mM phosphoric acid and once in methanol prior to drying and scintillation counting."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886854"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4108714"	""	"0"	"458.45"	"0"	"1.95"	"BDBM237780"	"CCOC(=O)COC(=O)N1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@H](C#N)C1"	"IC50"	"'='"	"1395.0"	"nM"	"5.86"	""	"414884"	"UO_0000065"	"12.77"	"0.24"	"3.91"	"3.84"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4112932"	""	"0"	"440.48"	"0"	"3.19"	"BDBM237783"	"CC1(COC(=O)N2CC[C@H](n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)[C@H](C#N)C2)CC1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"414887"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4113009"	""	"0"	"488.52"	"0"	"3.56"	"BDBM237763"	"N#C[C@@H]1CN(C(=O)OC2Cc3ccccc3C2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"414867"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3944822"	""	"0"	"467.53"	"0"	"3.01"	"BDBM228762"	"CN(c1ccc(NS(=O)(=O)c2ccc(F)cc2)cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399693"	"UO_0000065"	"21.94"	"0.42"	"7.25"	"9.58"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3646828"	""	"0"	"348.36"	"0"	"2.85"	"BDBM130274"	"COc1ccc(-c2cc(C(N)=O)c3nc4[nH]c(OC)ccc-4c3n2)cc1"	"IC50"	"'='"	"110.0"	"nM"	"6.96"	""	"262060"	"UO_0000065"	"19.98"	"0.37"	"4.11"	"6.75"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3894399"	""	"0"	"465.56"	"0"	"2.66"	"BDBM229215"	"CN1CCC(OC(=O)N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)CC2)CC1"	"IC50"	"'='"	"798.0"	"nM"	"6.10"	""	"400952"	"UO_0000065"	"13.10"	"0.24"	"3.44"	"4.71"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3911044"	""	"0"	"456.48"	"0"	"2.49"	"BDBM229219"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(C(=O)OC2CCOC2)CC1"	"IC50"	"'='"	"37.0"	"nM"	"7.43"	""	"400956"	"UO_0000065"	"16.28"	"0.31"	"4.94"	"5.48"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4112555"	""	"0"	"466.55"	"0"	"1.03"	"BDBM229243"	"CN1CCN(CCOC(=O)N2CC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)C2)CC1"	"IC50"	"'='"	"1186.0"	"nM"	"5.93"	""	"400982"	"UO_0000065"	"12.70"	"0.24"	"4.90"	"4.46"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3918038"	""	"0"	"428.50"	"0"	"3.27"	"BDBM229260"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)c2ccccc2)CC1"	"IC50"	"'='"	"94.0"	"nM"	"7.03"	""	"400999"	"UO_0000065"	"16.40"	"0.30"	"3.76"	"6.00"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3903567"	""	"0"	"430.47"	"0"	"2.06"	"BDBM229264"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)c2cnccn2)CC1"	"IC50"	"'='"	"283.0"	"nM"	"6.55"	""	"401003"	"UO_0000065"	"15.21"	"0.28"	"4.49"	"4.58"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3931559"	""	"0"	"433.47"	"0"	"2.57"	"BDBM229265"	"Cc1cc(C(=O)N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)CC2)no1"	"IC50"	"'='"	"195.0"	"nM"	"6.71"	""	"401004"	"UO_0000065"	"15.48"	"0.29"	"4.14"	"4.69"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3953465"	""	"0"	"434.53"	"0"	"3.33"	"BDBM229269"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)c2ccsc2)CC1"	"IC50"	"'='"	"35.0"	"nM"	"7.46"	""	"401008"	"UO_0000065"	"17.16"	"0.33"	"4.13"	"6.37"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3954129"	""	"0"	"471.57"	"0"	"3.34"	"BDBM229276"	"CN(C)c1ccc(C(=O)N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)CC2)cc1"	"IC50"	"'='"	"230.0"	"nM"	"6.64"	""	"401015"	"UO_0000065"	"14.08"	"0.26"	"3.30"	"5.52"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3935066"	""	"0"	"488.55"	"0"	"3.29"	"BDBM229280"	"COc1ccc(C(=O)N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)CC2)cc1OC"	"IC50"	"'='"	"448.0"	"nM"	"6.35"	""	"401019"	"UO_0000065"	"13.00"	"0.24"	"3.06"	"4.69"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3927869"	""	"0"	"415.43"	"0"	"1.14"	"BDBM229295"	"COCC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CC1"	"IC50"	"'='"	"96.0"	"nM"	"7.02"	""	"401034"	"UO_0000065"	"16.89"	"0.32"	"5.88"	"5.04"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3905407"	""	"0"	"443.48"	"0"	"1.65"	"BDBM229303"	"CC(C)(O)CC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CC1"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	"401042"	"UO_0000065"	"18.26"	"0.35"	"6.45"	"5.39"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3911822"	""	"0"	"463.50"	"0"	"0.54"	"BDBM229311"	"CS(=O)(=O)CC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CC1"	"IC50"	"'='"	"22.0"	"nM"	"7.66"	""	"401050"	"UO_0000065"	"16.52"	"0.33"	"7.12"	"4.67"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3899110"	""	"0"	"453.40"	"0"	"2.44"	"BDBM229317"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(C(=O)CC(F)(F)F)CC1"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	"401056"	"UO_0000065"	"17.64"	"0.34"	"5.56"	"6.16"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3917637"	""	"0"	"499.00"	"0"	"3.47"	"BDBM229331"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(S(=O)(=O)c2cccc(Cl)c2)CC1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"401070"	"UO_0000065"	"17.43"	"0.35"	"5.23"	"6.49"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4114140"	""	"0"	"436.50"	"0"	"2.04"	"BDBM229339"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CN(S(=O)(=O)c2ccccc2)C1"	"IC50"	"'='"	"463.0"	"nM"	"6.33"	""	"401078"	"UO_0000065"	"14.51"	"0.28"	"4.29"	"4.72"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4113178"	""	"0"	"457.54"	"0"	"4.01"	"BDBM229348"	"CC(C)c1ccccc1NC(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"428.0"	"nM"	"6.37"	""	"401087"	"UO_0000065"	"13.92"	"0.26"	"2.36"	"4.93"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3960898"	""	"0"	"381.44"	"0"	"1.77"	"BDBM229358"	"CCCNC(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"106.0"	"nM"	"6.97"	""	"401097"	"UO_0000065"	"18.29"	"0.34"	"5.20"	"5.40"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4110698"	""	"0"	"451.44"	"0"	"3.16"	"BDBM229368"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CN(C(=O)Nc2ccc(F)cc2F)C1"	"IC50"	"'='"	"79.0"	"nM"	"7.10"	""	"401107"	"UO_0000065"	"15.73"	"0.29"	"3.94"	"5.50"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3927483"	""	"0"	"450.49"	"0"	"4.67"	"BDBM228193"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(Nc2cccc(F)c2)CC1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"401132"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3946481"	""	"0"	"529.57"	"1"	"3.78"	"BDBM229399"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)F)cc3)n2)CCC(Nc2cccnc2)CC1"	"IC50"	"'='"	"352.0"	"nM"	"6.45"	""	"401138"	"UO_0000065"	"12.19"	"0.24"	"2.67"	"4.14"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3898987"	""	"0"	"469.47"	"0"	"4.20"	"BDBM229400"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(Nc2cc(F)ccc2F)CC1"	"IC50"	"'='"	"355.0"	"nM"	"6.45"	""	"401139"	"UO_0000065"	"13.74"	"0.26"	"2.25"	"5.30"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3890238"	""	"0"	"440.52"	"0"	"2.44"	"BDBM229420"	"N#CCC1(C2C=C(C(N)=O)C(Nc3ccnc(F)c3)=N2)CCC(NC2CCOCC2)CC1"	"IC50"	"'='"	"103.0"	"nM"	"6.99"	""	"401167"	"UO_0000065"	"15.86"	"0.30"	"4.55"	"5.57"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3950370"	""	"0"	"466.95"	"1"	"5.18"	"BDBM228230"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(Nc2ccc(Cl)cc2)CC1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"401182"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3896010"	""	"0"	"450.49"	"0"	"4.67"	"BDBM229433"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(Nc2ccccc2F)CC1"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"401187"	"UO_0000065"	"18.10"	"0.34"	"3.48"	"7.50"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3115323"	""	"0"	"404.85"	"0"	"4.38"	"6"	"O=C1NN(c2ccccc2)C(=O)/C1=C\c1cc(Cl)ccc1OCc1ccccc1"	"IC50"	"'='"	"15000.0"	"nM"	"4.82"	""	""	"UO_0000065"	"11.92"	"0.23"	"0.44"	"8.23"	"False"	"CHEMBL3119788"	"Inhibition of JAK2 (unknown origin) by radioactive ATP method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112544"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL3115320"	""	"0"	"328.33"	"0"	"3.75"	"2"	"O=C1Nc2ccc3c(oc4ccccc43)c2/C1=N/Nc1ccncc1"	"IC50"	"'='"	"11000.0"	"nM"	"4.96"	""	""	"UO_0000065"	"15.10"	"0.27"	"1.21"	"6.24"	"False"	"CHEMBL3119788"	"Inhibition of JAK2 (unknown origin) by radioactive ATP method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112544"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL3908733"	""	"0"	"471.54"	"0"	"4.25"	"BDBM229145"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(Cc2ccc3cc[nH]c3c2)CC1"	"IC50"	"'='"	"46.0"	"nM"	"7.34"	""	"400881"	"UO_0000065"	"15.56"	"0.29"	"3.09"	"6.34"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3914006"	""	"0"	"463.52"	"0"	"3.17"	"BDBM229155"	"COc1ccccc1CN1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CC1"	"IC50"	"'='"	"82.0"	"nM"	"7.09"	""	"400891"	"UO_0000065"	"15.29"	"0.28"	"3.92"	"5.80"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3950247"	""	"0"	"458.50"	"0"	"3.04"	"BDBM229161"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2ccccc2C#N)CC1"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	"400897"	"UO_0000065"	"17.20"	"0.32"	"4.85"	"5.77"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3943646"	""	"0"	"471.49"	"0"	"2.28"	"BDBM229190"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(C(=O)OC2CCOCC2)CC1"	"IC50"	"'='"	"96.0"	"nM"	"7.02"	""	"400927"	"UO_0000065"	"14.88"	"0.28"	"4.74"	"4.73"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3914703"	""	"0"	"433.49"	"0"	"3.92"	"BDBM228252"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(Nc2cccnc2)CC1"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"401204"	"UO_0000065"	"18.81"	"0.35"	"4.23"	"6.70"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3940414"	""	"0"	"516.52"	"1"	"3.13"	"BDBM229452"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)F)cc3)n2)CCC(NCC(F)F)CC1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"401212"	"UO_0000065"	"16.50"	"0.33"	"5.39"	"5.96"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3950965"	""	"0"	"432.50"	"0"	"4.53"	"BDBM229463"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(Nc2ccccc2)CC1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"401224"	"UO_0000065"	"20.11"	"0.37"	"4.17"	"8.00"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3946403"	""	"0"	"452.49"	"0"	"2.23"	"BDBM229476"	"N#CC[C@]1(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)F)cc3)n2)CC[C@H](N)CC1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"401239"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3897977"	""	"0"	"481.96"	"0"	"4.25"	"BDBM228302"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(NCc2ccccc2Cl)CC1"	"IC50"	"'='"	"912.0"	"nM"	"6.04"	""	"401253"	"UO_0000065"	"12.53"	"0.24"	"1.79"	"4.97"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3975369"	""	"0"	"448.51"	"0"	"3.00"	"BDBM229489"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(NCc2ccccn2)CC1"	"IC50"	"'='"	"1392.0"	"nM"	"5.86"	""	"401254"	"UO_0000065"	"13.06"	"0.24"	"2.86"	"4.35"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4114903"	""	"0"	"453.40"	"0"	"2.09"	"BDBM229520"	"CC(F)(F)C(=O)N1CC[C@@](CC#N)(n2cc(C(N)=O)c(Nc3ccc(F)nc3)n2)[C@H](F)C1"	"IC50"	"'='"	"67.0"	"nM"	"7.17"	""	"401268"	"UO_0000065"	"15.82"	"0.31"	"5.08"	"5.52"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4108087"	""	"0"	"453.40"	"0"	"2.09"	"BDBM229501"	"CC(F)(F)C(=O)N1CC[C@](CC#N)(n2cc(C(N)=O)c(Nc3ccc(F)nc3)n2)[C@H](F)C1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"401269"	"UO_0000065"	"18.31"	"0.35"	"6.21"	"6.39"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3956972"	""	"0"	"448.51"	"0"	"3.76"	"BDBM229503"	"N#CC[C@]1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CC[C@H](n2cc(C3CC3)nn2)CC1"	"IC50"	"'='"	"1481.0"	"nM"	"5.83"	""	"401271"	"UO_0000065"	"13.00"	"0.24"	"2.07"	"4.57"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3983711"	""	"0"	"448.45"	"0"	"3.20"	"BDBM229506"	"N#CC[C@]1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CC[C@@H](C(=O)NCC(F)(F)F)CC1"	"IC50"	"'='"	"301.0"	"nM"	"6.52"	""	"401273"	"UO_0000065"	"14.54"	"0.28"	"3.32"	"5.18"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3126338"	""	"0"	"269.28"	"0"	"2.79"	"3"	"O=c1[nH]ccc2c(NC3CC3)nc3ccc(F)cc3c12"	"IC50"	"'='"	"200.0"	"nM"	"6.70"	""	""	"UO_0000065"	"24.88"	"0.46"	"3.91"	"11.59"	"False"	"CHEMBL3131376"	"Inhibition of recombinant Jak2 (unknown origin) using biotinylated synthetic peptide substrate by homogeneous time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3124786"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3126352"	""	"0"	"358.74"	"0"	"4.15"	"14"	"O=c1[nH]ccc2c(Nc3c(F)cc(F)cc3Cl)nc3ccncc3c12"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	""	"UO_0000065"	"21.81"	"0.43"	"3.67"	"11.07"	"False"	"CHEMBL3131375"	"Inhibition of Jak2 (unknown origin) assessed as inhibition of STAT5 phosphorylation by cell-based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3124786"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL604274"	""	"0"	"277.37"	"0"	"4.74"	"13b"	"CC(C)CC1Nc2ccccc2-c2ccnc3[nH]cc1c23"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL603048"	""	"0"	"346.78"	"0"	"4.47"	"15a"	"Oc1ccc(C2=Nc3ccccc3-c3ncnc4[nH]cc2c34)c(Cl)c1"	"IC50"	"'='"	"160.0"	"nM"	"6.80"	""	""	"UO_0000065"	"19.60"	"0.37"	"2.33"	"9.16"	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL589146"	""	"0"	"323.36"	"0"	"4.29"	"20a"	"O=C1c2ccccc2C2c3c[nH]c4nccc(c34)-c3ccccc3N12"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL589385"	""	"0"	"383.41"	"0"	"4.31"	"20b"	"COc1cc(OC)c2c(c1)C(=O)N1c3ccccc3-c3ccnc4[nH]cc(c34)C21"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL3952926"	""	"0"	"485.47"	"0"	"3.77"	"BDBM228905"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(c2ccc(OC(F)F)nc2)CC1"	"IC50"	"'='"	"21.0"	"nM"	"7.68"	""	"400652"	"UO_0000065"	"15.82"	"0.30"	"3.91"	"6.29"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3909334"	""	"0"	"477.50"	"0"	"2.96"	"BDBM228927"	"COC(=O)c1cccc(N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)CC2)n1"	"IC50"	"'='"	"280.0"	"nM"	"6.55"	""	"400674"	"UO_0000065"	"13.72"	"0.26"	"3.59"	"4.71"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3977608"	""	"0"	"481.56"	"0"	"2.73"	"BDBM228969"	"CNC(=O)c1ccc(Nc2nn(C3(CC#N)CCN(C(=O)OC(C)(C)C)CC3)cc2C(N)=O)cc1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"400714"	"UO_0000065"	"18.06"	"0.34"	"5.97"	"5.60"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3911418"	""	"0"	"450.49"	"0"	"4.22"	"BDBM228934"	"Cc1cc(N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)CC2)ccc1F"	"IC50"	"'='"	"287.0"	"nM"	"6.54"	""	"400681"	"UO_0000065"	"14.52"	"0.27"	"2.32"	"6.54"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3894383"	""	"0"	"460.49"	"0"	"3.45"	"BDBM228957"	"CC(C)(C)OC(=O)N1CC[C@](CC#N)(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@@H](F)C1"	"IC50"	"'='"	"25.0"	"nM"	"7.60"	""	"400704"	"UO_0000065"	"16.51"	"0.31"	"4.15"	"6.02"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3938455"	""	"0"	"450.50"	"0"	"2.63"	"BDBM228998"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccnc(C#N)c3)n2)CC1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"400743"	"UO_0000065"	"18.25"	"0.34"	"5.59"	"5.05"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3689515"	""	"0"	"310.36"	"0"	"1.44"	"BDBM109865"	"N#CCC(=O)N1CCC12CCCN(c1ncnc3[nH]ccc13)C2"	"IC50"	"'='"	"2.2"	"nM"	"8.66"	""	"230595"	"UO_0000065"	"27.90"	"0.51"	"7.22"	"9.74"	"False"	"CHEMBL3705639"	"Inhibition Assay: In the kinase reactions, fused proteins (6His tag-fused hJAK2 kinase domain (aa808-end)) which were coexpressed in Sf21 cells and purified by Ni2+/NTA agarose were used."	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638515"	"37"	"BindingDB Database"	""	"2013"	"CHEMBL4106362"	""
"CHEMBL4078799"	""	"0"	"391.44"	"0"	"2.23"	"18"	"Cn1cc(-c2ccc(Nc3nn([C@H]4COCC[C@@H]4C#N)cc3C(N)=O)cc2)cn1"	"IC50"	"'='"	"0.5"	"nM"	"9.30"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4032997"	"Inhibition of GST-tagged recombinant human JAK2 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 as substrate preincubated for 30 mins followed by ATP addition measured after 120 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4076473"	""	"0"	"414.83"	"0"	"3.17"	"32"	"N#C[C@H]1CCOC[C@@H]1n1cc(C(N)=O)c(Nc2cc(F)c3nccc(Cl)c3c2)n1"	"IC50"	"'='"	"608.0"	"nM"	"6.22"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4033007"	"Inhibition of JAK2 in EPO-stimulated human TF1 cells expressing stably integrated beta-lactamase reporter gene under control of STAT5 response elements in interferon regulatory factor 1 gene promoter by fluorescence assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4226460"	""	"0"	"336.40"	"0"	"2.70"	"20"	"CN(c1ncnc2[nH]ccc12)[C@@H]1CCN(C(=O)Nc2ccccc2)C1"	"IC50"	"'='"	"550.0"	"nM"	"6.26"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4227368"	""	"0"	"382.45"	"0"	"1.73"	"32"	"CN(c1ncnc2[nH]ccc12)[C@@H]1CCN(S(=O)(=O)c2ccc(C#N)cc2)C1"	"IC50"	"'='"	"1200.0"	"nM"	"5.92"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4227919"	""	"0"	"425.44"	"0"	"2.88"	"39"	"CN(c1ncnc2[nH]ccc12)[C@@H]1CCN(S(=O)(=O)c2ccc(C(F)(F)F)cc2)C1"	"IC50"	"'='"	"3400.0"	"nM"	"5.47"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL3958942"	""	"0"	"514.49"	"1"	"2.49"	"BDBM229167"	"COC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)(F)F)cc3)n2)CC1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"400903"	"UO_0000065"	"16.91"	"0.34"	"6.21"	"5.42"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3920087"	""	"0"	"458.52"	"0"	"3.77"	"BDBM229170"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)OCc2ccccc2)CC1"	"IC50"	"'='"	"85.0"	"nM"	"7.07"	""	"400906"	"UO_0000065"	"15.42"	"0.28"	"3.30"	"5.60"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3982019"	""	"0"	"476.46"	"0"	"3.36"	"BDBM229179"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(C(=O)OCC2CC2(F)F)CC1"	"IC50"	"'='"	"38.0"	"nM"	"7.42"	""	"400916"	"UO_0000065"	"15.57"	"0.30"	"4.06"	"5.88"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3962314"	""	"0"	"454.51"	"0"	"3.51"	"BDBM229181"	"CC1(COC(=O)N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)CC2)CC1"	"IC50"	"'='"	"72.0"	"nM"	"7.14"	""	"400918"	"UO_0000065"	"15.72"	"0.30"	"3.63"	"5.66"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3896725"	""	"0"	"390.49"	"0"	"3.20"	"BDBM198479"	"O[C@@H](CNC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1)c1ccccc1"	"IC50"	"'='"	"49.0"	"nM"	"7.31"	""	"352557"	"UO_0000065"	"18.72"	"0.34"	"4.11"	"8.02"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3978189"	""	"0"	"354.46"	"0"	"2.65"	"BDBM198496"	"COCC1(NC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)CC1"	"IC50"	"'='"	"100.0"	"nM"	"7.00"	""	"352574"	"UO_0000065"	"19.75"	"0.37"	"4.35"	"8.74"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3892562"	""	"0"	"368.49"	"0"	"2.77"	"BDBM198508"	"O[C@H]1CC[C@H](NC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)CC1"	"IC50"	"'='"	"290.0"	"nM"	"6.54"	""	"352586"	"UO_0000065"	"17.74"	"0.33"	"3.77"	"7.17"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3951710"	""	"0"	"396.54"	"0"	"3.36"	"BDBM198514"	"CC(C)(O)C1CCN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)CC1"	"IC50"	"'='"	"160.0"	"nM"	"6.80"	""	"352592"	"UO_0000065"	"17.14"	"0.32"	"3.44"	"8.25"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3931713"	""	"0"	"360.41"	"0"	"3.22"	"BDBM198531"	"FC1(F)CCN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C1"	"IC50"	"'='"	"33.0"	"nM"	"7.48"	""	"352609"	"UO_0000065"	"20.76"	"0.39"	"4.26"	"12.05"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3906986"	""	"0"	"422.92"	"0"	"3.89"	"BDBM198555"	"O=C(NCCc1ccc(Cl)cc1)[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"29.0"	"nM"	"7.54"	""	"352633"	"UO_0000065"	"17.82"	"0.34"	"3.65"	"8.57"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3921442"	""	"0"	"337.39"	"0"	"1.91"	"BDBM198559"	"N#CCCNC(=O)[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"36.0"	"nM"	"7.44"	""	"352637"	"UO_0000065"	"22.06"	"0.41"	"5.53"	"6.66"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3962451"	""	"0"	"323.36"	"0"	"1.97"	"BDBM198422"	"c1cc2c(ncn3nnc(C4CCN(Cc5cocn5)CC4)c23)[nH]1"	"IC50"	"'='"	"81.0"	"nM"	"7.09"	""	"352500"	"UO_0000065"	"21.93"	"0.40"	"5.12"	"8.05"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL2181313"	""	"0"	"502.62"	"1"	"4.97"	"22f, 85:15 trans/cis mixture"	"COc1ccc2cc1COCC=CCOCc1cc(ccc1OCCN1CCCC1)Nc1nccc-2n1"	"IC50"	"'='"	"19.0"	"nM"	"7.72"	""	""	"UO_0000065"	"15.36"	"0.29"	"2.75"	"9.90"	"False"	"CHEMBL2184201"	"Inhibition of recombinant JAK2 using Poly (Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176955"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL2181088"	""	"0"	"486.62"	"1"	"5.27"	"22b, 85:15 trans/cis mixture"	"Cc1cnc2nc1-c1cccc(c1)COCC=CCOCc1cc(ccc1OCCN1CCCC1)N2"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	""	"UO_0000065"	"16.76"	"0.31"	"2.88"	"11.86"	"False"	"CHEMBL2184201"	"Inhibition of recombinant JAK2 using Poly (Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176955"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL2181087"	""	"0"	"502.62"	"1"	"4.97"	"22a, 85:15 trans/cis mixture"	"COc1cc2cc(c1OCCN1CCCC1)COCC=CCOCc1cccc(c1)-c1ccnc(n1)N2"	"IC50"	"'='"	"36.0"	"nM"	"7.44"	""	""	"UO_0000065"	"14.81"	"0.27"	"2.47"	"9.55"	"False"	"CHEMBL2184201"	"Inhibition of recombinant JAK2 using Poly (Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176955"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL2181086"	""	"0"	"501.63"	"2"	"5.16"	"21l, 85:15 trans/cis mixture"	"CCN(CC)CCC(=O)Nc1cc2cc(c1)Nc1nccc(n1)-c1cccc(c1)COCC=CCOC2"	"IC50"	"'='"	"44.0"	"nM"	"7.36"	""	""	"UO_0000065"	"14.67"	"0.27"	"2.20"	"8.30"	"False"	"CHEMBL2184201"	"Inhibition of recombinant JAK2 using Poly (Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176955"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL2181326"	""	"0"	"535.67"	"1"	"3.96"	"17g, 85:15 trans/cis mixture"	"CCS(=O)(=O)N1CCN(c2ccc3cc2COCC=CCOCc2cccc(c2)-c2ccnc(n2)N3)CC1"	"IC50"	"'='"	"150.0"	"nM"	"6.82"	""	""	"UO_0000065"	"12.74"	"0.25"	"2.86"	"7.04"	"False"	"CHEMBL2184201"	"Inhibition of recombinant JAK2 using Poly (Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176955"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL2181321"	""	"0"	"444.54"	"0"	"4.33"	"17a, 85:15 trans/cis mixture"	"C1=CCOCc2cc(ccc2N2CCOCC2)Nc2nccc(n2)-c2cccc(c2)COC1"	"IC50"	"'='"	"60.0"	"nM"	"7.22"	""	""	"UO_0000065"	"16.25"	"0.30"	"2.89"	"10.51"	"False"	"CHEMBL2184201"	"Inhibition of recombinant JAK2 using Poly (Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176955"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL3903493"	""	"0"	"340.43"	"0"	"1.95"	"BDBM198611"	"O[C@H]1CCN(C[C@H]2CC[C@@H](c3nnn4cnc5[nH]ccc5c34)CC2)C1"	"IC50"	"'='"	"350.0"	"nM"	"6.46"	""	"352689"	"UO_0000065"	"18.96"	"0.35"	"4.51"	"7.84"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3956450"	""	"0"	"362.46"	"0"	"1.77"	"BDBM198625"	"CN(C)S(=O)(=O)C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"8.4"	"nM"	"8.08"	""	"352703"	"UO_0000065"	"22.28"	"0.44"	"6.31"	"8.39"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3973343"	""	"0"	"284.32"	"0"	"2.34"	"BDBM198636"	"O/N=C/[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"35.0"	"nM"	"7.46"	""	"352714"	"UO_0000065"	"26.22"	"0.48"	"5.12"	"8.15"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3902333"	""	"0"	"266.31"	"0"	"2.40"	"BDBM198637"	"N#C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"49.0"	"nM"	"7.31"	""	"352715"	"UO_0000065"	"27.45"	"0.50"	"4.91"	"8.84"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3905498"	""	"0"	"333.40"	"0"	"2.38"	"BDBM198442"	"c1cc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)ccn1"	"IC50"	"'='"	"35.0"	"nM"	"7.46"	""	"352520"	"UO_0000065"	"22.36"	"0.41"	"5.08"	"9.94"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3934440"	""	"0"	"382.42"	"0"	"4.27"	"BDBM198452"	"Fc1ccc(NC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1F"	"IC50"	"'='"	"56.0"	"nM"	"7.25"	""	"352530"	"UO_0000065"	"18.96"	"0.35"	"2.98"	"10.23"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3913693"	""	"0"	"385.48"	"0"	"4.06"	"BDBM198467"	"N#CCc1ccc(NC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"32.0"	"nM"	"7.50"	""	"352545"	"UO_0000065"	"19.44"	"0.35"	"3.43"	"7.92"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4114436"	""	"0"	"354.46"	"0"	"2.34"	"BDBM198468"	"OC[C@H]1CCCN1C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"180.0"	"nM"	"6.75"	""	"352546"	"UO_0000065"	"19.03"	"0.35"	"4.40"	"8.19"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4113620"	""	"0"	"340.43"	"0"	"1.95"	"BDBM198470"	"O[C@@H]1CCN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C1"	"IC50"	"'='"	"32.0"	"nM"	"7.50"	""	"352548"	"UO_0000065"	"22.02"	"0.41"	"5.54"	"9.10"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3967880"	""	"0"	"354.41"	"0"	"1.90"	"BDBM198481"	"O=C(O)C1CN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C1"	"IC50"	"'='"	"34.0"	"nM"	"7.47"	""	"352559"	"UO_0000065"	"21.07"	"0.39"	"5.57"	"7.51"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3962117"	""	"0"	"338.46"	"0"	"3.27"	"BDBM198493"	"CC1(C)CC1NC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"39.0"	"nM"	"7.41"	""	"352571"	"UO_0000065"	"21.89"	"0.40"	"4.14"	"10.45"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3934426"	""	"0"	"337.43"	"0"	"2.72"	"BDBM198505"	"CN(CCC#N)C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"29.0"	"nM"	"7.54"	""	"352583"	"UO_0000065"	"22.34"	"0.41"	"4.82"	"8.77"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3941925"	""	"0"	"436.95"	"0"	"4.05"	"BDBM198511"	"Clc1ccc(C2(NC[C@H]3CC[C@H](c4nnn5cnc6[nH]ccc6c45)CC3)COC2)cc1"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	"352589"	"UO_0000065"	"18.13"	"0.35"	"3.87"	"9.88"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3916457"	""	"0"	"420.36"	"0"	"3.96"	"BDBM198520"	"FC(F)(F)C(NC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1)C(F)(F)F"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	"352598"	"UO_0000065"	"18.55"	"0.37"	"3.84"	"11.00"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3908073"	""	"0"	"378.44"	"0"	"3.10"	"BDBM198552"	"Cc1ccc(CNC(=O)[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)o1"	"IC50"	"'='"	"48.0"	"nM"	"7.32"	""	"352630"	"UO_0000065"	"19.34"	"0.36"	"4.22"	"7.24"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4115208"	""	"0"	"404.47"	"0"	"2.73"	"BDBM198556"	"O=C(NC[C@@H](O)c1ccccc1)[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"31.0"	"nM"	"7.51"	""	"352634"	"UO_0000065"	"18.56"	"0.34"	"4.78"	"6.94"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3943928"	""	"0"	"399.24"	"0"	"3.21"	"BDBM198587"	"FC(F)(Br)CN[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"2.8"	"nM"	"8.55"	""	"352665"	"UO_0000065"	"21.42"	"0.49"	"5.34"	"12.06"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3953015"	""	"0"	"342.79"	"0"	"2.23"	"BDBM213746"	"CCc1ccc(Cl)cc1-n1nc(-c2ccnc(N)n2)cc1C(N)=O"	"IC50"	"'<'"	"5000.0"	"nM"	""	""	"375851"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888138"	"JAK2 Enzymatic Assay: The assay has been performed using the commercial available JAK2 kinase domain (Invitrogen, Eugene, Oreg.). The JAK2 kinase domain showed a linear kinetic without prephosphorylation. The JAK2 kinase assay was run with a final enzyme concentration of 1 nM, in the presence of 60 uM ATP, 3 nM 33P-γ-ATP and 64 uM of substrate BioDBn*306 (Aminoacid sequence: LPLDKDYYWREPGQâ¿¿SEQ ID NO: 1). The peptidic substrate was purchased from American Peptide Company (Sunnyvale, Calif.). Specific JAK2, JAK1 or JAK3 peptide substrates are trans-phosphorylated by JAKs kinase in the presence of ATP traced with 33P-γ-ATP. At the end of the phosphorylation reaction, the unreacted ATP, cold and radioactive, is captured by an excess of Dowex ion exchange resin that eventually settles by gravity to the bottom of the reaction plate. The supernatant is subsequently withdrawn and transferred into a counting plate that is then evaluated by 3-counting."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886598"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3972962"	""	"0"	"421.51"	"1"	"5.02"	"BDBM198451"	"N#Cc1ccc(NC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)c2ccccc12"	"IC50"	"'='"	"140.0"	"nM"	"6.85"	""	"352529"	"UO_0000065"	"16.26"	"0.29"	"1.83"	"7.24"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3910680"	""	"0"	"432.43"	"1"	"5.15"	"BDBM198454"	"Fc1ccc(NC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1C(F)(F)F"	"IC50"	"'='"	"200.0"	"nM"	"6.70"	""	"352532"	"UO_0000065"	"15.49"	"0.30"	"1.55"	"9.45"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL1539757"	""	"0"	"345.49"	"0"	"4.54"	"SID22413585"	"O=CO.c1ccc2c(c1)CSc1sccc1C2=C1CCNCC1"	"IC50"	"'='"	"10450.0"	"nM"	"4.98"	""	"Not Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1334315"	""	"0"	"330.39"	"0"	"4.06"	"SID14737384"	"CC(C)C1C(C#N)=C(N)Oc2[nH]nc(-c3ccc4ccccc4c3)c21"	"IC50"	"'='"	"3565.0"	"nM"	"5.45"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1559437"	""	"0"	"324.43"	"0"	"1.96"	"SID26669883"	"O=S(=O)(c1cccs1)N1CCN(c2ccc(O)cc2)CC1"	"IC50"	"'='"	"5658.0"	"nM"	"5.25"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1424118"	""	"0"	"285.74"	"0"	"3.09"	"SID26666773"	"Nc1nc(CCl)nc(Nc2ccc3ccccc3c2)n1"	"IC50"	"'='"	"1081.0"	"nM"	"5.97"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1521348"	""	"0"	"265.70"	"0"	"1.94"	"SID26663568"	"COc1ccc(Nc2nc(N)nc(CCl)n2)cc1"	"IC50"	"'='"	"2656.0"	"nM"	"5.58"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1533676"	""	"0"	"338.46"	"1"	"5.31"	"SID26664277"	"COc1ccc2nc(C)cc(Sc3nc4ccccc4s3)c2c1"	"IC50"	"'='"	"6962.0"	"nM"	"5.16"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1572967"	""	"0"	"317.10"	"0"	"2.50"	"SID17402822"	"O=C(OCn1ncc(Cl)c(Cl)c1=O)c1ccc(F)cc1"	"IC50"	"'='"	"1138.0"	"nM"	"5.94"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1348654"	""	"0"	"246.22"	"0"	"2.75"	"SID24808888"	"Cc1cccc(NC(=O)c2ccc([N+](=O)[O-])o2)c1"	"IC50"	"'='"	"6884.0"	"nM"	"5.16"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1563340"	""	"0"	"289.33"	"0"	"4.14"	"SID24793712"	"Cc1nc2ccccc2c(O)c1C(=O)/C=C/c1ccccc1"	"IC50"	"'='"	"3125.0"	"nM"	"5.50"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1524240"	""	"0"	"264.80"	"0"	"3.54"	"SID24806771"	"Cl.c1ccc2c(CN3CCCCCC3)c[nH]c2c1"	"IC50"	"'='"	"10710.0"	"nM"	"4.97"	""	"Not Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1470321"	""	"0"	"457.55"	"0"	"4.16"	"SID14741113"	"Cc1cccc(CS(=O)(=O)c2nnc([C@H](Cc3ccccc3)NC(=O)OC(C)(C)C)o2)c1"	"IC50"	"'='"	"3644.0"	"nM"	"5.44"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL1489454"	""	"0"	"398.39"	"0"	"2.01"	"SID24815497"	"COC(=O)COc1cccc2c(=O)n(CC(=O)NCc3ccc(F)cc3)ccc12"	"IC50"	"'='"	"3341.0"	"nM"	"5.48"	""	"Active"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1613998"	"PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability. (Class of assay: confirmatory) [Related pubchem assays: 1446 (Primary screen.), 1486 (Counterscreen in triplicate.), 1691 (Dose response.)]"	"F"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1201862"	"7"	"PubChem BioAssays"	""	""	"CHEMBL3307634"	""
"CHEMBL2152252"	""	"0"	"453.86"	"0"	"2.82"	"31"	"CNC(=O)c1nc(-c2ccc(Cl)c(S(=O)(=O)Nc3cccc(F)c3F)c2)cnc1N"	"IC50"	"'>'"	"3600.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2156903"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2150966"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2152253"	""	"0"	"449.90"	"0"	"2.99"	"32"	"CNC(=O)c1nc(-c2ccc(Cl)c(S(=O)(=O)Nc3cccc(F)c3C)c2)cnc1N"	"IC50"	"'>'"	"3600.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2156903"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2150966"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL602648"	""	"0"	"400.39"	"0"	"3.98"	"22a"	"COC(=O)C1(c2ccc([N+](=O)[O-])cc2)Nc2ccccc2-c2ccnc3[nH]cc1c23"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL1049518"	"Inhibition of JAK2 in granulocyte macrophage colony stimulating factor-stimulated human TF1 cells assessed as phosphorylation of STAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1153158"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"CHEMBL3307972"	""
"CHEMBL1682386"	""	"0"	"450.93"	"0"	"3.05"	"26"	"Cc1cc(Nc2nc(N3CCN(C(=O)Cc4ccc(Cl)cc4)CC3)nn3cccc23)n[nH]1"	"IC50"	"'='"	"0.6"	"nM"	"9.22"	""	""	"UO_0000065"	"20.45"	"0.39"	"6.17"	"9.76"	"False"	"CHEMBL1685409"	"Inhibition of JAK2 after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1681645"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1682372"	""	"0"	"430.52"	"0"	"2.79"	"12"	"Cc1cc(Nc2nc(N3CCN(C(=O)CCc4ccccc4)CC3)nn3cccc23)n[nH]1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	""	"UO_0000065"	"20.21"	"0.37"	"5.91"	"9.21"	"False"	"CHEMBL1685409"	"Inhibition of JAK2 after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1681645"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1682367"	""	"0"	"416.49"	"0"	"2.40"	"7"	"Cc1cc(Nc2nc(N3CCN(C(=O)Cc4ccccc4)CC3)nn3cccc23)n[nH]1"	"IC50"	"'='"	"2.8"	"nM"	"8.55"	""	""	"UO_0000065"	"20.54"	"0.38"	"6.15"	"9.06"	"False"	"CHEMBL1685409"	"Inhibition of JAK2 after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1681645"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1682373"	""	"0"	"416.49"	"0"	"2.78"	"13"	"Cc1cc(Nc2nc(N3CCN(C(=O)c4ccccc4C)CC3)nn3cccc23)n[nH]1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"20.46"	"0.38"	"5.74"	"9.02"	"False"	"CHEMBL1685409"	"Inhibition of JAK2 after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1681645"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL3956546"	""	"0"	"472.53"	"0"	"3.65"	"BDBM229110"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2cccc3cc[nH]c23)CC1"	"IC50"	"'='"	"41.0"	"nM"	"7.39"	""	"400846"	"UO_0000065"	"15.63"	"0.29"	"3.74"	"5.74"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3969009"	""	"0"	"298.35"	"0"	"1.30"	"BDBM228765"	"CN(C(=O)CC#N)C1CCCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399699"	"UO_0000065"	"31.04"	"0.57"	"7.96"	"10.41"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3943618"	""	"0"	"396.48"	"0"	"1.47"	"BDBM228775"	"C#CCN(c1ccc(S(C)(=O)=O)cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399711"	"UO_0000065"	"23.35"	"0.45"	"7.79"	"9.74"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3952191"	""	"0"	"339.36"	"0"	"1.98"	"BDBM228776"	"CN(c1ccc([N+](=O)[O-])cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399713"	"UO_0000065"	"27.29"	"0.51"	"7.28"	"8.90"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3977196"	""	"0"	"437.45"	"0"	"3.31"	"BDBM228914"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(c2ccc(F)nc2)CC1"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	"400661"	"UO_0000065"	"18.11"	"0.34"	"4.61"	"7.02"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4470339"	""	"0"	"293.37"	"0"	"3.87"	"1"	"Cc1nc2cnc3[nH]ccc3c2n1[C@H]1CC[C@H](CC#N)CC1"	"IC50"	"'<'"	"0.2"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4404825"	"Inhibition of JAK2-JH1/JH2 domain (532 to 1132 residues) (unknown origin) pre-incubated before NH2-KGGEEEEYFELVKK-CO2 substrate addition and measured after 90 mins by MS analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402578"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL3930305"	""	"0"	"429.51"	"0"	"0.75"	"BDBM228699"	"CN(c1ccc(S(=O)(=O)NC2COC2)cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399696"	"UO_0000065"	"23.89"	"0.47"	"9.51"	"8.82"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3948069"	""	"0"	"444.47"	"0"	"3.04"	"BDBM228913"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(c2cncc(C#N)c2)CC1"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	"400660"	"UO_0000065"	"17.32"	"0.32"	"4.66"	"5.63"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3917536"	""	"0"	"454.46"	"0"	"4.05"	"BDBM228932"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(c2cc(F)cc(F)c2)CC1"	"IC50"	"'='"	"67.0"	"nM"	"7.17"	""	"400679"	"UO_0000065"	"15.79"	"0.30"	"3.12"	"7.18"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3935178"	""	"0"	"538.58"	"1"	"3.36"	"BDBM228981"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)F)cc3)n2)CC1"	"IC50"	"'='"	"0.6"	"nM"	"9.22"	""	"400726"	"UO_0000065"	"17.12"	"0.34"	"5.86"	"5.75"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3908597"	""	"0"	"455.52"	"0"	"2.77"	"BDBM228984"	"COc1cc(Nc2nn(C3(CC#N)CCN(C(=O)OC(C)(C)C)CC3)cc2C(N)=O)ccn1"	"IC50"	"'='"	"146.0"	"nM"	"6.84"	""	"400729"	"UO_0000065"	"15.01"	"0.28"	"4.07"	"4.61"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3971587"	""	"0"	"503.51"	"1"	"3.16"	"BDBM229002"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(OC4CCC4)nc3)n2)CCN(C(=O)OCC(F)F)CC1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"400747"	"UO_0000065"	"16.93"	"0.32"	"5.36"	"5.74"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3891171"	""	"0"	"469.40"	"0"	"2.66"	"BDBM229014"	"N#CCC1(n2cc(C(N)=O)c(Nc3cncc(F)c3)n2)CCN(C(=O)OCC(F)(F)F)CC1"	"IC50"	"'='"	"21.0"	"nM"	"7.68"	""	"400759"	"UO_0000065"	"16.36"	"0.32"	"5.02"	"5.52"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"1"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	""	"UO_0000065"	"26.88"	"0.50"	"6.86"	"9.45"	"True"	"CHEMBL2329570"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 30 mins by scintillation counting analysis in presence of [gamma-33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321829"	"1"	"Scientific Literature"	"J. Med. Chem."	"2013"	"None"	""
"CHEMBL2325911"	""	"0"	"313.36"	"0"	"1.19"	"3m"	"C[C@@H](NC(=O)c1c[nH]c2ncc(C3CC3)nc12)C(=O)N1CCC1"	"IC50"	"'='"	"345.4"	"nM"	"6.46"	""	""	"UO_0000065"	"20.62"	"0.38"	"5.27"	"7.10"	"False"	"CHEMBL2329570"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 30 mins by scintillation counting analysis in presence of [gamma-33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321829"	"1"	"Scientific Literature"	"J. Med. Chem."	"2013"	"None"	""
"CHEMBL2325904"	""	"0"	"288.35"	"0"	"1.72"	"3f"	"C[C@H](NC(=O)c1c[nH]c2ncc(C3CC3)nc12)C(C)(C)O"	"IC50"	"'='"	"76.7"	"nM"	"7.12"	""	""	"UO_0000065"	"24.68"	"0.46"	"5.40"	"7.83"	"False"	"CHEMBL2329570"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 30 mins by scintillation counting analysis in presence of [gamma-33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321829"	"1"	"Scientific Literature"	"J. Med. Chem."	"2013"	"None"	""
"CHEMBL3126339"	""	"0"	"269.28"	"0"	"2.79"	"2"	"O=c1[nH]ccc2nc(NC3CC3)c3ccc(F)cc3c12"	"IC50"	"'='"	"100.0"	"nM"	"7.00"	""	""	"UO_0000065"	"26.00"	"0.48"	"4.21"	"12.11"	"False"	"CHEMBL3131376"	"Inhibition of recombinant Jak2 (unknown origin) using biotinylated synthetic peptide substrate by homogeneous time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3124786"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL388978"	"STAUROSPORINE"	"0"	"466.54"	"0"	"4.35"	"staurosporine"	"CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4c(c5c6ccccc6n2c5c31)C(=O)NC4"	"IC50"	"'='"	"4.7"	"nM"	"8.33"	""	""	"UO_0000065"	"17.85"	"0.32"	"3.98"	"11.99"	"False"	"CHEMBL973444"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1138507"	"1"	"Scientific Literature"	"J. Med. Chem."	"2009"	"None"	""
"CHEMBL2325894"	""	"0"	"338.37"	"0"	"0.94"	"3p"	"C[C@@H](NC(=O)c1c[nH]c2ncc(C3CC3)nc12)C(=O)N1CC(C#N)C1"	"IC50"	"'='"	"8900.0"	"nM"	"5.05"	""	""	"UO_0000065"	"14.93"	"0.28"	"4.11"	"4.40"	"False"	"CHEMBL2329053"	"Inhibition of JAK2 in human PBMC expressing CD14 assessed as inhibition of GM-CSF-stimulated STAT5a phosphorylation after 30 mins by flow cytometric analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321829"	"1"	"Scientific Literature"	"J. Med. Chem."	"2013"	"None"	""
"CHEMBL2325912"	""	"0"	"352.40"	"0"	"1.33"	"3n"	"C[C@@H](NC(=O)c1c[nH]c2ncc(C3CC3)nc12)C(=O)N1CCC(C#N)C1"	"IC50"	"'='"	"2030.0"	"nM"	"5.69"	""	""	"UO_0000065"	"16.15"	"0.30"	"4.36"	"4.96"	"False"	"CHEMBL2329053"	"Inhibition of JAK2 in human PBMC expressing CD14 assessed as inhibition of GM-CSF-stimulated STAT5a phosphorylation after 30 mins by flow cytometric analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321829"	"1"	"Scientific Literature"	"J. Med. Chem."	"2013"	"None"	""
"CHEMBL4279991"	""	"0"	"364.41"	"0"	"2.58"	"17g"	"COc1cc2c(=O)n([C@@H]3CCNC3)c3c4cc[nH]c4ncc3c2cc1OC"	"IC50"	"'='"	"37.91"	"nM"	"7.42"	""	""	"UO_0000065"	"20.37"	"0.38"	"4.84"	"9.14"	"False"	"CHEMBL4261266"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]-ATP addition measured after 2 hrs by filter-binding method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257589"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3650998"	""	"0"	"368.37"	"0"	"3.46"	"BDBM153174"	"C=C(C)C(=O)Nc1ccc(F)c(-c2ncnc3[nH]cc(C(=O)OCC)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294140"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4782355"	""	"0"	"403.45"	"0"	"0.91"	"15"	"Cn1cc(-c2cn3nccc3c(-c3cnn(C4(CC#N)CN(CCO)C4)c3)n2)cn1"	"IC50"	"'='"	"1044.0"	"nM"	"5.98"	""	""	""	""	""	""	""	"False"	"CHEMBL4675813"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using FITC-KGGEEEEYFELVKK as substrate in presence of ATP at Km by microfluidic assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4673239"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL1089814"	""	"0"	"489.55"	"0"	"4.96"	"19"	"COc1cc(-c2cnc3cccc(-c4ccc(CN5CCOCC5)cc4F)c3n2)cc(OC)c1OC"	"IC50"	"'='"	"501.0"	"nM"	"6.30"	""	""	"UO_0000065"	"12.87"	"0.24"	"1.34"	"9.55"	"False"	"CHEMBL1116984"	"Inhibition of recombinant GST tagged JAK2 protein after 60 mins using FITC-GGEEEEYFELVKKKK-NH2 substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156975"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1089773"	""	"0"	"515.61"	"1"	"4.83"	"24"	"CN1CCN(c2ccc(-c3cnc4cccc(-c5cc(F)c(CN6CCOCC6)c(F)c5)c4n3)cc2)CC1"	"IC50"	"'='"	"4.3"	"nM"	"8.37"	""	""	"UO_0000065"	"16.23"	"0.30"	"3.54"	"18.70"	"False"	"CHEMBL1116984"	"Inhibition of recombinant GST tagged JAK2 protein after 60 mins using FITC-GGEEEEYFELVKKKK-NH2 substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156975"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL4754005"	""	"0"	"383.42"	"0"	"2.54"	"28, trans isomer"	"Cn1ccc(-c2cn3nccc3c(-c3cnn([C@]4(CC#N)C[C@@H](C#N)C4)c3)n2)n1"	"IC50"	"'='"	"467.0"	"nM"	"6.33"	""	""	""	""	""	""	""	"False"	"CHEMBL4675813"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using FITC-KGGEEEEYFELVKK as substrate in presence of ATP at Km by microfluidic assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4673239"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL1093749"	""	"0"	"465.53"	"0"	"3.90"	"1"	"CNS(=O)(=O)c1ccc(-c2cccc3ncc(-c4cc(OC)c(OC)c(OC)c4)nc23)cc1"	"IC50"	"'='"	"42.0"	"nM"	"7.38"	""	""	"UO_0000065"	"15.85"	"0.31"	"3.48"	"7.40"	"False"	"CHEMBL1116984"	"Inhibition of recombinant GST tagged JAK2 protein after 60 mins using FITC-GGEEEEYFELVKKKK-NH2 substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156975"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1093468"	""	"0"	"547.63"	"1"	"3.79"	"9"	"COc1cc(-c2cnc3cccc(-c4ccc(CC(=O)N5CCS(=O)(=O)CC5)cc4)c3n2)cc(OC)c1OC"	"IC50"	"'='"	"5.1"	"nM"	"8.29"	""	""	"UO_0000065"	"15.14"	"0.29"	"4.50"	"7.68"	"False"	"CHEMBL1116984"	"Inhibition of recombinant GST tagged JAK2 protein after 60 mins using FITC-GGEEEEYFELVKKKK-NH2 substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156975"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1093454"	""	"0"	"485.58"	"1"	"5.13"	"15"	"COc1cc(-c2cnc3cccc(-c4ccc(CN5CCOCC5)c(C)c4)c3n2)cc(OC)c1OC"	"IC50"	"'='"	"195.0"	"nM"	"6.71"	""	""	"UO_0000065"	"13.82"	"0.25"	"1.58"	"10.18"	"False"	"CHEMBL1116984"	"Inhibition of recombinant GST tagged JAK2 protein after 60 mins using FITC-GGEEEEYFELVKKKK-NH2 substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156975"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1089813"	""	"0"	"485.58"	"1"	"5.13"	"18"	"COc1cc(-c2cnc3cccc(-c4ccc(CN5CCOCC5)cc4C)c3n2)cc(OC)c1OC"	"IC50"	"'='"	"685.0"	"nM"	"6.16"	""	""	"UO_0000065"	"12.69"	"0.23"	"1.03"	"9.35"	"False"	"CHEMBL1116984"	"Inhibition of recombinant GST tagged JAK2 protein after 60 mins using FITC-GGEEEEYFELVKKKK-NH2 substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156975"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1784637"	""	"0"	"582.63"	"1"	"2.87"	"8h"	"CNC(=O)c1ncc(C#Cc2cc(C(=O)Nc3ccc(CN4CCN(CCO)CC4)c(C(F)(F)F)c3)ccc2C)n1C"	"IC50"	"'='"	"536.0"	"nM"	"6.27"	""	""	"UO_0000065"	"10.76"	"0.20"	"3.40"	"6.10"	"False"	"CHEMBL1785330"	"Inhibition of human JAK2 using poly[Glu:Tyr] by Hotspot assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1781971"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL3890522"	""	"0"	"449.49"	"0"	"3.18"	"BDBM228898"	"COc1cc(N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)CC2)ccn1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"400645"	"UO_0000065"	"18.47"	"0.34"	"5.12"	"6.80"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3895008"	""	"0"	"432.50"	"0"	"4.08"	"BDBM228931"	"Cc1ccc(N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)CC2)cc1"	"IC50"	"'='"	"117.0"	"nM"	"6.93"	""	"400678"	"UO_0000065"	"16.03"	"0.30"	"2.85"	"6.93"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3911273"	""	"0"	"451.48"	"0"	"3.64"	"BDBM228942"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(c2cccc(CF)n2)CC1"	"IC50"	"'='"	"39.0"	"nM"	"7.41"	""	"400689"	"UO_0000065"	"16.41"	"0.31"	"3.77"	"6.56"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3896338"	""	"0"	"450.50"	"0"	"2.63"	"BDBM228977"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(C#N)nc3)n2)CC1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"400722"	"UO_0000065"	"18.25"	"0.34"	"5.59"	"5.05"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3907923"	""	"0"	"463.52"	"0"	"3.57"	"BDBM228908"	"CCOc1cccc(N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)CC2)n1"	"IC50"	"'='"	"861.0"	"nM"	"6.07"	""	"400655"	"UO_0000065"	"13.08"	"0.24"	"2.49"	"4.97"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3974477"	""	"0"	"520.51"	"1"	"4.11"	"BDBM228976"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(C(=O)C(F)(F)F)cc3)n2)CC1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"400721"	"UO_0000065"	"16.37"	"0.31"	"4.41"	"5.95"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3896424"	""	"0"	"455.52"	"0"	"2.25"	"BDBM228983"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccnc(CO)c3)n2)CC1"	"IC50"	"'='"	"101.0"	"nM"	"7.00"	""	"400728"	"UO_0000065"	"15.36"	"0.29"	"4.75"	"4.39"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3891348"	""	"0"	"473.48"	"0"	"3.10"	"BDBM229005"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(C4CC4)nc3)n2)CCN(C(=O)OCC(F)F)CC1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	"400750"	"UO_0000065"	"16.81"	"0.32"	"4.86"	"5.72"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3974307"	""	"0"	"351.80"	"0"	"0.51"	"BDBM236508"	"Cn1cc(Nc2ncc(Cl)c(NC3COC4C(N)COC34)n2)cn1"	"IC50"	"'='"	"99.0"	"nM"	"7.00"	""	"411892"	"UO_0000065"	"19.91"	"0.40"	"6.49"	"6.25"	"False"	"CHEMBL3888641"	"Kinase Assay: Aurora-A (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 200 μM LRRASLG (Kemptide), 10 mM MgAcetate and [γ-33P-ATP](specific activity approx. 500 cpm/pmol, concentration as required). The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of 3% phosphoric acid solution. 10 μL of the reaction is then spotted onto a P30 filtermat and washed three times for 5 minutes in 75 mM phosphoric acid and once in methanol prior to drying and scintillation counting."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886792"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3939379"	""	"0"	"387.47"	"0"	"1.44"	"BDBM228690"	"CN(c1ccc(NS(C)(=O)=O)cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399738"	"UO_0000065"	"23.90"	"0.47"	"7.82"	"8.64"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3983040"	""	"0"	"443.53"	"0"	"1.09"	"BDBM228705"	"CN(c1ccc(S(=O)(=O)N2CCOCC2)cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399742"	"UO_0000065"	"20.88"	"0.41"	"8.17"	"8.61"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3930951"	""	"0"	"338.37"	"0"	"1.77"	"BDBM228795"	"CN(c1ccc(C(=O)O)cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399734"	"UO_0000065"	"27.37"	"0.51"	"7.49"	"9.43"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3976446"	""	"0"	"450.49"	"0"	"4.22"	"BDBM228926"	"Cc1ccc(N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)CC2)cc1F"	"IC50"	"'='"	"215.0"	"nM"	"6.67"	""	"400673"	"UO_0000065"	"14.80"	"0.28"	"2.45"	"6.67"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL1270795"	""	"0"	"343.44"	"0"	"3.35"	"10i"	"CSc1cn2c(-c3cn[nH]c3)cnc2c(Nc2cc(C)ns2)n1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1805358"	"Inhibition of Jak2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1799927"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL3974023"	""	"0"	"439.52"	"0"	"3.22"	"BDBM237831"	"Cc1ncc(CN2CC[C@@H](C#N)[C@H](n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)C2)s1"	"IC50"	"'='"	"19.0"	"nM"	"7.72"	""	"414935"	"UO_0000065"	"17.57"	"0.34"	"4.50"	"6.84"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4108565"	""	"0"	"395.34"	"0"	"2.73"	"BDBM237868"	"N#C[C@H]1CCOC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(OC(F)(F)F)cc2)n1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"414970"	"UO_0000065"	"22.77"	"0.44"	"6.27"	"7.81"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4112743"	""	"0"	"405.41"	"0"	"2.30"	"BDBM237882"	"C[C@@](O)(c1ccc(Nc2nn([C@H]3COCC[C@@H]3C#N)cc2C(N)=O)cc1)C(F)F"	"IC50"	"'='"	"0.2"	"nM"	"9.70"	""	"414984"	"UO_0000065"	"23.92"	"0.46"	"7.40"	"7.69"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3959433"	""	"0"	"405.41"	"0"	"2.30"	"BDBM237884"	"C[C@@](O)(c1ccc(Nc2nn([C@@H]3COCC[C@H]3C#N)cc2C(N)=O)cc1)C(F)F"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"414986"	"UO_0000065"	"19.85"	"0.38"	"5.75"	"6.38"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3951700"	""	"0"	"349.40"	"0"	"1.95"	"BDBM228668"	"COc1nc(N(C)[C@@H]2CCN(c3ncnc4[nH]ccc34)C2)ccc1C#N"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399628"	"UO_0000065"	"29.36"	"0.54"	"8.31"	"10.92"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3968548"	""	"0"	"305.35"	"0"	"1.92"	"BDBM228722"	"N#Cc1ccc(NC2CCN(c3ncnc4[nH]ccc34)C2)nc1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399642"	"UO_0000065"	"33.60"	"0.61"	"8.34"	"10.97"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3906885"	""	"0"	"398.27"	"0"	"2.70"	"BDBM228730"	"CN(c1ncc(C#N)cc1Br)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399651"	"UO_0000065"	"25.76"	"0.56"	"7.56"	"12.11"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL2376437"	""	"0"	"419.49"	"0"	"3.40"	"12b"	"CC(=O)N[C@@H]1CCc2ccc(Oc3cnc4[nH]cc(C(=O)N[C@H](C)C5CC5)c4n3)cc21"	"IC50"	"'='"	"194.0"	"nM"	"6.71"	""	""	"UO_0000065"	"16.00"	"0.30"	"3.31"	"6.16"	"False"	"CHEMBL2378977"	"Inhibition of JAK2 (unknown origin) expressed in SF21 cells using Biotin-KAIETDKEYYTVKD as substrate and [33Pgamma]ATP incubated for 10 mins prior to substrate addition measured after 30 mins by Topcount analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375291"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"CHEMBL4106362"	""
"CHEMBL3915857"	""	"0"	"336.37"	"0"	"2.68"	"BDBM228732"	"CN(c1ccc(C#N)cc1F)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399653"	"UO_0000065"	"30.50"	"0.56"	"7.58"	"14.28"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4115639"	""	"0"	"310.38"	"0"	"-0.07"	"BDBM228645"	"CNS(=O)(=O)N(C)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399630"	"UO_0000065"	"33.06"	"0.67"	"10.33"	"10.89"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3925768"	""	"0"	"363.35"	"0"	"2.48"	"BDBM228715"	"CN(c1ccc(C(F)(F)F)nn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399634"	"UO_0000065"	"28.24"	"0.54"	"7.78"	"13.90"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3913220"	""	"0"	"270.34"	"0"	"1.38"	"BDBM228717"	"CN(CCC#N)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399636"	"UO_0000065"	"37.95"	"0.70"	"8.88"	"14.28"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL2376331"	""	"0"	"310.36"	"0"	"3.20"	"1b"	"Cc1cccc(Oc2cnc3[nH]cc(C(=O)NC(C)C)c3n2)c1"	"IC50"	"'='"	"410.0"	"nM"	"6.39"	""	""	"UO_0000065"	"20.58"	"0.38"	"3.19"	"7.99"	"False"	"CHEMBL2378977"	"Inhibition of JAK2 (unknown origin) expressed in SF21 cells using Biotin-KAIETDKEYYTVKD as substrate and [33Pgamma]ATP incubated for 10 mins prior to substrate addition measured after 30 mins by Topcount analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375291"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"CHEMBL4106362"	""
"CHEMBL3671131"	""	"0"	"434.45"	"0"	"4.30"	"BDBM127630"	"Cc1cccnc1NC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258304"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3937419"	""	"0"	"454.51"	"0"	"1.94"	"BDBM127865"	"Cn1cc(F)cc([C@H]2CCCN2c2ccn3ncc(C(=O)NC4CCC(O)CC4)c3n2)c1=O"	"IC50"	"'='"	"499.0"	"nM"	"6.30"	""	"258530"	"UO_0000065"	"13.87"	"0.26"	"4.36"	"6.02"	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL404609"	""	"0"	"261.31"	"0"	"2.00"	"1"	"NC(=O)Nc1sc(-c2ccccc2)cc1C(N)=O"	"IC50"	"'='"	"61.0"	"nM"	"7.21"	""	""	"UO_0000065"	"27.61"	"0.55"	"5.21"	"7.35"	"False"	"CHEMBL3239499"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3232939"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3234887"	""	"0"	"313.36"	"0"	"3.79"	"9"	"NC(=O)c1cc(-c2ccccc2)sc1Nc1ccc(F)cn1"	"IC50"	"'='"	"161.0"	"nM"	"6.79"	""	""	"UO_0000065"	"21.68"	"0.42"	"3.00"	"9.99"	"False"	"CHEMBL3239499"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3232939"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL4089234"	""	"0"	"345.79"	"0"	"2.48"	"14"	"N#C[C@H]1CCOC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"140.0"	"nM"	"6.85"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4033007"	"Inhibition of JAK2 in EPO-stimulated human TF1 cells expressing stably integrated beta-lactamase reporter gene under control of STAT5 response elements in interferon regulatory factor 1 gene promoter by fluorescence assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL3646818"	""	"0"	"447.93"	"0"	"3.52"	"BDBM130264"	"CN1CCN(C(=O)c2ccc3c(c2)[nH]c2c(C(N)=O)cc(-c4ccc(Cl)nc4)cc23)CC1"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"262050"	"UO_0000065"	"18.21"	"0.35"	"4.63"	"8.56"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3646839"	""	"0"	"461.49"	"0"	"3.83"	"BDBM130288"	"COc1ccc(-c2cc(C(N)=O)c3[nH]c4ccc(C(=O)N5CCC[C@H](O)C5)cc4c3c2)cc1F"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"262074"	"UO_0000065"	"18.85"	"0.35"	"4.87"	"8.01"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3589169"	""	"0"	"446.94"	"0"	"4.13"	"BDBM130257"	"CN1CCN(C(=O)c2ccc3[nH]c4c(C(N)=O)cc(-c5ccc(Cl)cc5)cc4c3c2)CC1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"262043"	"UO_0000065"	"20.14"	"0.38"	"4.87"	"10.92"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3646843"	""	"0"	"317.35"	"0"	"3.49"	"BDBM130292"	"COc1cccc(-c2cc(C(N)=O)c3[nH]c4ccncc4c3c2)c1"	"IC50"	"'='"	"34.0"	"nM"	"7.47"	""	"262078"	"UO_0000065"	"23.53"	"0.42"	"3.98"	"9.22"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649619"	""	"0"	"506.01"	"1"	"4.10"	"BDBM130313"	"NC(=O)c1cc(-c2ccc(OC3CCNCC3)c(Cl)c2)nc2c1[nH]c1cc(N3CCOCC3)ccc12"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"262099"	"UO_0000065"	"16.12"	"0.31"	"4.05"	"7.73"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649645"	""	"0"	"420.90"	"0"	"4.28"	"BDBM130340"	"Cc1cc(-c2cc(C(N)=O)c3[nH]c4cc(N5CCOCC5)ccc4c3n2)ccc1Cl"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"262126"	"UO_0000065"	"19.37"	"0.37"	"3.87"	"9.68"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3646816"	""	"0"	"469.37"	"0"	"4.69"	"BDBM130261"	"CN(C)CCNC(=O)c1ccc2[nH]c3c(C(N)=O)cc(-c4ccc(Cl)c(Cl)c4)cc3c2c1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"262047"	"UO_0000065"	"17.52"	"0.35"	"3.53"	"9.01"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3646848"	""	"0"	"434.88"	"0"	"3.61"	"BDBM130297"	"NC(=O)c1cc(-c2ccc(Cl)cc2)nc2c1[nH]c1cc(C(=O)N3CCOCC3)ccc12"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"262083"	"UO_0000065"	"20.00"	"0.38"	"5.09"	"8.59"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649644"	""	"0"	"403.44"	"0"	"2.21"	"BDBM130339"	"NC(=O)c1cc(-c2ccc(CO)nc2)nc2c1[nH]c1cc(N3CCOCC3)ccc12"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"262125"	"UO_0000065"	"20.38"	"0.37"	"6.01"	"7.01"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL1938655"	""	"0"	"448.57"	"0"	"2.34"	"21"	"CC(C)(C)NS(=O)(=O)c1ccc(-c2cc3c(N)ncc(C(=O)NCCO)c3s2)cc1"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	""	"UO_0000065"	"18.05"	"0.37"	"5.76"	"6.02"	"False"	"CHEMBL1941383"	"Inhibition of human recombinant N-terminal GST-tagged JAK2 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308860"	""
"CHEMBL3963555"	""	"0"	"382.45"	"0"	"2.78"	"BDBM198213"	"Cc1cc(NC(=O)N2CCCC(c3nnn4cnc5[nH]ccc5c34)C2)sn1"	"IC50"	"'='"	"110.0"	"nM"	"6.96"	""	"352295"	"UO_0000065"	"18.19"	"0.35"	"4.18"	"6.68"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3981443"	""	"0"	"339.43"	"0"	"2.44"	"BDBM198240"	"c1csc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)n1"	"IC50"	"'='"	"54.0"	"nM"	"7.27"	""	"352322"	"UO_0000065"	"21.41"	"0.41"	"4.83"	"9.69"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3899634"	""	"0"	"375.41"	"0"	"3.00"	"BDBM198232"	"N#Cc1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)c(F)c1"	"IC50"	"'='"	"6.4"	"nM"	"8.19"	""	"352314"	"UO_0000065"	"21.83"	"0.40"	"5.19"	"9.54"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3897798"	""	"0"	"401.40"	"0"	"3.40"	"BDBM198244"	"FC(F)(F)c1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cn1"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	"352326"	"UO_0000065"	"19.29"	"0.36"	"4.34"	"10.33"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4163122"	""	"0"	"510.62"	"1"	"2.84"	"14"	"CC(=O)N1CCN(c2cc(Nc3ncc(C)c(Nc4cccc(CO)c4)n3)cc(S(C)(=O)=O)c2)CC1"	"IC50"	"'='"	"347.0"	"nM"	"6.46"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4145184"	"Inhibition of recombinant human JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate after 10 mins by caliper assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4138312"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4168613"	""	"0"	"399.52"	"0"	"3.56"	"23"	"CCC(CC)Nc1nc(Nc2cc(N3C[C@@H]4C[C@H]3CN4C)cnc2F)ncc1C"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4145184"	"Inhibition of recombinant human JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate after 10 mins by caliper assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4138312"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL1789941"	"RUXOLITINIB"	"4"	"306.37"	"0"	"3.47"	"Ruxolitinib"	"N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"0.4"	"nM"	"9.40"	""	""	""	"30.68"	"0.56"	"5.93"	"11.30"	"False"	"CHEMBL4714135"	"Inhibition of human JAK2 by radiometric assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEK293F"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706688"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	""
"CHEMBL1287853"	"FEDRATINIB"	"4"	"524.69"	"1"	"4.82"	"Fedratinib"	"Cc1cnc(Nc2ccc(OCCN3CCCC3)cc2)nc1Nc1cccc(S(=O)(=O)NC(C)(C)C)c1"	"IC50"	"'='"	"0.75"	"nM"	"9.12"	""	""	""	"17.39"	"0.34"	"4.30"	"8.41"	"False"	"CHEMBL4714135"	"Inhibition of human JAK2 by radiometric assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEK293F"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706688"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	""
"CHEMBL3601722"	""	"0"	"443.56"	"0"	"3.71"	"11e"	"C=CC(=O)Nc1cccc(CNc2cc(Nc3ccc(N4CCN(C)CC4)cc3)ncn2)c1"	"IC50"	"'='"	"945.0"	"nM"	"6.03"	""	""	"UO_0000065"	"13.58"	"0.25"	"2.31"	"7.05"	"False"	"CHEMBL4482009"	"Inhibition of human JAK2 using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and further incubated for 30 mins and subsequently measured after 1 hr by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480445"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4566777"	""	"0"	"457.58"	"0"	"4.10"	"12e"	"C/C=C/C(=O)Nc1cccc(CNc2cc(Nc3ccc(N4CCN(C)CC4)cc3)ncn2)c1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4482009"	"Inhibition of human JAK2 using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and further incubated for 30 mins and subsequently measured after 1 hr by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480445"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4571470"	""	"0"	"363.43"	"0"	"3.08"	"12a'"	"C/C=C/C(=O)Nc1ccc(CNc2cc(Nc3cnn(C)c3)ncn2)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4482009"	"Inhibition of human JAK2 using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and further incubated for 30 mins and subsequently measured after 1 hr by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480445"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL3940644"	""	"0"	"406.46"	"0"	"4.15"	"BDBM198461"	"FC(F)(F)C1CCN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)CC1"	"IC50"	"'='"	"81.0"	"nM"	"7.09"	""	"352539"	"UO_0000065"	"17.45"	"0.33"	"2.94"	"11.42"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4112919"	""	"0"	"390.49"	"0"	"3.20"	"BDBM198480"	"O[C@H](CNC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1)c1ccccc1"	"IC50"	"'='"	"33.0"	"nM"	"7.48"	""	"352558"	"UO_0000065"	"19.16"	"0.35"	"4.28"	"8.21"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3911362"	""	"0"	"399.50"	"0"	"3.58"	"BDBM198485"	"N#Cc1ccc(CCNC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"70.0"	"nM"	"7.16"	""	"352563"	"UO_0000065"	"17.91"	"0.33"	"3.57"	"7.56"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3957921"	""	"0"	"324.43"	"0"	"2.88"	"BDBM198488"	"c1cc2c(ncn3nnc([C@H]4CC[C@H](CNCC5CC5)CC4)c23)[nH]1"	"IC50"	"'='"	"120.0"	"nM"	"6.92"	""	"352566"	"UO_0000065"	"21.33"	"0.39"	"4.04"	"9.76"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3979623"	""	"0"	"416.43"	"0"	"2.36"	"BDBM198627"	"O=S(=O)(C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1)NCC(F)(F)F"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	"352705"	"UO_0000065"	"18.79"	"0.38"	"5.46"	"7.45"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3902992"	""	"0"	"280.34"	"0"	"2.79"	"BDBM198642"	"N#CC[C@H]1CC[C@@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"21.0"	"nM"	"7.68"	""	"352720"	"UO_0000065"	"27.39"	"0.50"	"4.89"	"9.29"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3912503"	""	"0"	"337.39"	"0"	"1.91"	"BDBM198653"	"N#CCNC(=O)C[C@H]1CC[C@@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"60.0"	"nM"	"7.22"	""	"352731"	"UO_0000065"	"21.41"	"0.39"	"5.31"	"6.46"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL1835140"	""	"0"	"402.50"	"0"	"4.06"	"51"	"CC(C)C(Nc1ncc(C(N)=O)c2[nH]c3cc(-c4cnn(C)c4)ccc3c12)C1CC1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"21.17"	"0.39"	"4.46"	"8.39"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835015"	""	"0"	"258.26"	"0"	"2.00"	"18"	"CNc1ncc(C(N)=O)c2[nH]c3ccc(F)cc3c12"	"IC50"	"'='"	"210.0"	"nM"	"6.68"	""	""	"UO_0000065"	"25.86"	"0.48"	"4.68"	"7.97"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835023"	""	"0"	"312.35"	"0"	"3.31"	"26"	"NC(=O)c1cnc(NC2CCCC2)c2c1[nH]c1ccc(F)cc12"	"IC50"	"'='"	"51.0"	"nM"	"7.29"	""	""	"UO_0000065"	"23.35"	"0.43"	"3.98"	"8.70"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835030"	""	"0"	"308.39"	"0"	"3.56"	"33"	"NC(=O)c1cnc(NC2CCCCC2)c2c1[nH]c1ccccc12"	"IC50"	"'='"	"59.0"	"nM"	"7.23"	""	""	"UO_0000065"	"23.44"	"0.43"	"3.67"	"8.63"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835031"	""	"0"	"342.83"	"0"	"4.21"	"34"	"NC(=O)c1cnc(NC2CCCCC2)c2c1[nH]c1cc(Cl)ccc12"	"IC50"	"'='"	"23.0"	"nM"	"7.64"	""	""	"UO_0000065"	"22.28"	"0.43"	"3.43"	"9.11"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835042"	""	"0"	"421.93"	"1"	"5.38"	"46"	"C[C@H](Nc1ccc(C(N)=O)c2[nH]c3cc(-c4ccc(Cl)nn4)ccc3c12)C(C)(C)C"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	""	"UO_0000065"	"18.61"	"0.36"	"2.47"	"8.12"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835153"	""	"0"	"441.42"	"0"	"3.61"	"65"	"NC(=O)c1cnc(N[C@H](C2CC2)C(F)(F)F)c2c1[nH]c1cc(-c3cnc(N)nc3)ccc12"	"IC50"	"'='"	"0.8"	"nM"	"9.10"	""	""	"UO_0000065"	"20.61"	"0.39"	"5.49"	"6.71"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835147"	""	"0"	"398.47"	"0"	"3.87"	"58"	"NC(=O)c1cnc(NC(C2CC2)C2CC2)c2c1[nH]c1cc(-c3cccnn3)ccc12"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	""	"UO_0000065"	"21.83"	"0.40"	"4.83"	"7.94"	"False"	"CHEMBL1840262"	"Inhibition of JAK2 using biotin-EQEDEPEGDYFEWLE- NH2 as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL3977496"	""	"0"	"242.29"	"0"	"1.07"	"BDBM198207"	"c1cc2c(ncn3nnc(C4CCCNC4)c23)[nH]1"	"IC50"	"'='"	"2500.0"	"nM"	"5.60"	""	"352289"	"UO_0000065"	"23.12"	"0.43"	"4.53"	"7.90"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3896215"	""	"0"	"369.41"	"0"	"1.87"	"BDBM198212"	"O=C(Nc1nncs1)N1CCCC(c2nnn3cnc4[nH]ccc4c23)C1"	"IC50"	"'='"	"32.0"	"nM"	"7.50"	""	"352294"	"UO_0000065"	"20.29"	"0.39"	"5.62"	"6.41"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3902447"	""	"0"	"357.42"	"0"	"2.86"	"BDBM198214"	"N#Cc1ccc(CN2CCCC(c3nnn4cnc5[nH]ccc5c34)C2)cc1"	"IC50"	"'='"	"560.0"	"nM"	"6.25"	""	"352296"	"UO_0000065"	"17.49"	"0.32"	"3.39"	"7.28"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3890660"	""	"0"	"414.44"	"0"	"4.05"	"BDBM198234"	"FC(F)(F)c1ccc(CCN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"410.0"	"nM"	"6.39"	""	"352316"	"UO_0000065"	"15.41"	"0.29"	"2.34"	"10.28"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3936877"	""	"0"	"402.29"	"0"	"3.69"	"BDBM198434"	"Clc1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)c(Cl)n1"	"IC50"	"'='"	"23.0"	"nM"	"7.64"	""	"352512"	"UO_0000065"	"18.99"	"0.39"	"3.95"	"10.18"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3938277"	""	"0"	"346.44"	"0"	"3.55"	"BDBM198448"	"CC(c1ccccc1)N1CCC(c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"62.0"	"nM"	"7.21"	""	"352526"	"UO_0000065"	"20.80"	"0.38"	"3.66"	"11.60"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3935532"	""	"0"	"366.39"	"0"	"3.42"	"BDBM198459"	"FC(F)(F)CCNC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"62.0"	"nM"	"7.21"	""	"352537"	"UO_0000065"	"19.67"	"0.38"	"3.79"	"10.17"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4112922"	""	"0"	"381.48"	"0"	"2.09"	"BDBM198521"	"CC(=O)N[C@@H]1CCN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C1"	"IC50"	"'='"	"57.0"	"nM"	"7.24"	""	"352599"	"UO_0000065"	"18.99"	"0.35"	"5.15"	"7.94"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3955124"	""	"0"	"349.40"	"0"	"1.86"	"BDBM198566"	"N#CC1CN(C(=O)[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C1"	"IC50"	"'='"	"290.0"	"nM"	"6.54"	""	"352644"	"UO_0000065"	"18.71"	"0.34"	"4.68"	"6.35"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL1081292"	""	"0"	"406.44"	"1"	"5.27"	"5"	"COc1ccc(-c2cccc3nc(Nc4cc(OC)c(OC)c(OC)c4)oc23)cc1"	"IC50"	"'='"	"840.0"	"nM"	"6.08"	""	""	"UO_0000065"	"14.95"	"0.28"	"0.81"	"8.10"	"False"	"CHEMBL1102770"	"Inhibition of GST-tagged JAK2 assessed as inhibition of biotinylated JAK3tide peptide phosphorylation after 60 mins by caliper mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154949"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1081485"	""	"0"	"475.55"	"1"	"5.10"	"11"	"COc1cc(Nc2nc3cccc(-c4ccc(CN5CCOCC5)cc4)c3o2)cc(OC)c1OC"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	""	"UO_0000065"	"16.52"	"0.31"	"2.75"	"10.04"	"False"	"CHEMBL1102770"	"Inhibition of GST-tagged JAK2 assessed as inhibition of biotinylated JAK3tide peptide phosphorylation after 60 mins by caliper mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154949"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1081664"	""	"0"	"484.56"	"0"	"4.72"	"13"	"Cc1cc(Nc2nc3cccc(-c4ccc(C(=O)N5CCOCC5)cc4)c3o2)ccc1C(=O)N(C)C"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	""	"UO_0000065"	"16.71"	"0.31"	"3.38"	"9.21"	"False"	"CHEMBL1102770"	"Inhibition of GST-tagged JAK2 assessed as inhibition of biotinylated JAK3tide peptide phosphorylation after 60 mins by caliper mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154949"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2010"	"None"	""
"CHEMBL1079078"	""	"0"	"439.54"	"0"	"3.22"	"23"	"CS(=O)(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCC(O)CC4)cc3)n2)cc1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	""	"UO_0000065"	"18.71"	"0.36"	"5.00"	"7.65"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1078364"	""	"0"	"444.50"	"0"	"2.99"	"30"	"COc1cc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)ccc1C(=O)NCC#N"	"IC50"	"'='"	"30.0"	"nM"	"7.52"	""	""	"UO_0000065"	"16.92"	"0.31"	"4.53"	"6.69"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1078453"	""	"0"	"442.52"	"0"	"3.76"	"31"	"CC(C)(C#N)NC(=O)c1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"549.0"	"nM"	"6.26"	""	""	"UO_0000065"	"14.15"	"0.26"	"2.50"	"6.07"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1079120"	""	"0"	"444.50"	"0"	"2.99"	"34"	"COc1cnc(Nc2ccc(N3CCOCC3)cc2)nc1-c1ccc(C(=O)NCC#N)cc1"	"IC50"	"'='"	"186.0"	"nM"	"6.73"	""	""	"UO_0000065"	"15.14"	"0.28"	"3.74"	"5.99"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1077841"	""	"0"	"430.54"	"0"	"3.69"	"40"	"N#CCNC(=O)c1ccc(-c2ccnc(Nc3ccc(N4CCSCC4)cc3)n2)cc1"	"IC50"	"'='"	"69.0"	"nM"	"7.16"	""	""	"UO_0000065"	"16.63"	"0.32"	"3.47"	"7.62"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL3652410"	""	"0"	"487.52"	"0"	"1.86"	"BDBM113222"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCC[C@@H](OP(=O)(O)O)C2)CC1"	"IC50"	"'='"	"0.106"	"nM"	"9.97"	""	"234665"	"UO_0000065"	"20.46"	"0.43"	"8.11"	"6.70"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3699464"	""	"0"	"325.37"	"0"	"1.95"	"BDBM147479"	"N#C[C@H]1C[C@H](O)CCC1n1cc(C(N)=O)c(Nc2ccccc2)n1"	"IC50"	"'='"	"70.0"	"nM"	"7.16"	""	"285404"	"UO_0000065"	"21.99"	"0.41"	"5.20"	"6.12"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645003"	""	"0"	"500.60"	"2"	"5.66"	"BDBM99755"	"COc1ncccc1-c1cccn2nc(Nc3ccc(C4CCN(C(=O)OC(C)(C)C)CC4)cc3)nc12"	"IC50"	"'='"	"674.8"	"nM"	"6.17"	""	"216443"	"UO_0000065"	"12.33"	"0.23"	"0.51"	"6.57"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647838"	""	"0"	"451.45"	"0"	"3.11"	"BDBM147947"	"C[C@]1(O)CC[C@H](n2cc(C(N)=O)c(Nc3ccc([C@](C)(O)C(F)(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"285881"	"UO_0000065"	"18.60"	"0.36"	"5.29"	"6.12"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3929066"	""	"0"	"465.62"	"0"	"2.41"	"BDBM113110"	"CCOCCO[C@@H]1CCN(S(=O)(=O)CC2CCC(N(C)c3ncnc4[nH]ccc34)CC2)C1"	"IC50"	"'='"	"16.8"	"nM"	"7.78"	""	"234554"	"UO_0000065"	"16.70"	"0.33"	"5.36"	"7.72"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL1947159"	""	"0"	"385.47"	"0"	"4.22"	"26b"	"CN1C/C=C/CC(=O)Nc2cccc(c2)-c2ccnc(n2)Nc2cccc(c2)C1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1944872"	""	"0"	"428.58"	"1"	"6.07"	"26n"	"CC(C)(C)CN1C/C=C/CCOc2cccc(c2)-c2ccnc(n2)Nc2cccc(c2)C1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1945050"	""	"0"	"402.50"	"0"	"4.67"	"27a"	"COc1ccc2cc1CN(C)C/C=C/CCOc1cccc(c1)-c1ccnc(n1)N2"	"IC50"	"'='"	"280.0"	"nM"	"6.55"	""	""	"UO_0000065"	"16.28"	"0.30"	"1.88"	"11.01"	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1945704"	""	"0"	"485.63"	"1"	"5.13"	"27k"	"CN1C/C=C/CCOc2cccc(c2)-c2ccnc(n2)Nc2ccc(OCCN3CCCC3)c(c2)C1"	"IC50"	"'='"	"56.0"	"nM"	"7.25"	""	""	"UO_0000065"	"14.93"	"0.28"	"2.12"	"11.56"	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1945707"	""	"0"	"499.66"	"1"	"5.52"	"27p"	"CN1C/C=C/CCOc2cccc(c2)-c2ccnc(n2)Nc2ccc(OCCN3CCCCC3)c(c2)C1"	"IC50"	"'='"	"62.0"	"nM"	"7.21"	""	""	"UO_0000065"	"14.43"	"0.27"	"1.69"	"11.49"	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL3903817"	""	"0"	"421.47"	"0"	"3.66"	"BDBM255034"	"CN1CN([C@H]2CC[C@H](CNC3(C(F)(F)F)CC3)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"443906"	"UO_0000065"	"19.51"	"0.37"	"4.56"	"12.79"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3922146"	""	"0"	"392.51"	"0"	"2.96"	"BDBM255040"	"CN(CC#N)C[C@H]1CC[C@H](N2CN(C3CC3)C(=O)c3cnc4[nH]ccc4c32)CC1"	"IC50"	"'='"	"100.0"	"nM"	"7.00"	""	"443912"	"UO_0000065"	"17.83"	"0.33"	"4.04"	"8.83"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3960523"	""	"0"	"342.42"	"0"	"3.47"	"BDBM255043"	"O=C1c2cnc3[nH]ccc3c2N([C@H]2CC[C@H](CF)CC2)CN1C1CC1"	"IC50"	"'='"	"33.0"	"nM"	"7.48"	""	"443915"	"UO_0000065"	"21.85"	"0.41"	"4.01"	"14.32"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL1938642"	""	"0"	"354.44"	"0"	"2.48"	"3"	"NC(=O)c1cnc(N)c2cc(-c3ccc(N4CCOCC4)cc3)sc12"	"IC50"	"'>'"	"25000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1941390"	"Inhibition of TEL-fused JAK2 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3307634"	""
"CHEMBL1938656"	""	"0"	"462.60"	"0"	"3.00"	"22"	"COCCNC(=O)c1cnc(N)c2cc(-c3ccc(S(=O)(=O)NC(C)(C)C)cc3)sc12"	"IC50"	"'='"	"959.0"	"nM"	"6.02"	""	""	"UO_0000065"	"13.01"	"0.27"	"3.02"	"4.88"	"False"	"CHEMBL1941390"	"Inhibition of TEL-fused JAK2 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3307634"	""
"CHEMBL3644979"	""	"0"	"399.50"	"0"	"4.23"	"BDBM99730"	"CCOc1ccccc1-c1cccn2nc(Nc3ccc4c(c3)CCNCC4)nc12"	"IC50"	"'='"	"130.71"	"nM"	"6.88"	""	"216419"	"UO_0000065"	"17.23"	"0.31"	"2.65"	"10.84"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703067"	""	"0"	"412.93"	"0"	"3.56"	"BDBM147777"	"CC1CN([C@H]2CC[C@H](n3cc(C(N)=O)c(Nc4ccc(Cl)cc4)n3)[C@@H](C#N)C2)C1"	"IC50"	"'='"	"85.0"	"nM"	"7.07"	""	"285711"	"UO_0000065"	"17.12"	"0.33"	"3.51"	"7.07"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3891030"	""	"0"	"322.37"	"0"	"2.58"	"BDBM198345"	"c1coc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)c1"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	"352423"	"UO_0000065"	"23.88"	"0.44"	"5.12"	"10.23"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3912553"	""	"0"	"373.87"	"0"	"3.10"	"BDBM198349"	"Clc1ncc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)s1"	"IC50"	"'='"	"22.0"	"nM"	"7.66"	""	"352427"	"UO_0000065"	"20.48"	"0.42"	"4.56"	"10.21"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3894161"	""	"0"	"340.42"	"0"	"1.84"	"BDBM198351"	"c1cc2c(ncn3nnc(C4CCN(Cc5csnn5)CC4)c23)[nH]1"	"IC50"	"'='"	"3.7"	"nM"	"8.43"	""	"352429"	"UO_0000065"	"24.77"	"0.48"	"6.59"	"9.59"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3939331"	""	"0"	"380.88"	"0"	"4.64"	"BDBM198375"	"Clc1ccc(NC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"190.0"	"nM"	"6.72"	""	"352453"	"UO_0000065"	"17.65"	"0.34"	"2.08"	"9.48"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3902287"	""	"0"	"328.42"	"0"	"1.85"	"BDBM198383"	"C[C@H](O)CNC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"42.0"	"nM"	"7.38"	""	"352461"	"UO_0000065"	"22.46"	"0.42"	"5.53"	"8.09"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3922606"	""	"0"	"485.56"	"0"	"2.98"	"BDBM237796"	"CN(C)CC(C)(C)COC(=O)N1CC[C@@H](C#N)[C@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)C1"	"IC50"	"'='"	"444.0"	"nM"	"6.35"	""	"414900"	"UO_0000065"	"13.08"	"0.25"	"3.37"	"4.91"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3652367"	""	"0"	"498.65"	"0"	"3.22"	"BDBM113178"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC[C@H](COCc3cccnc3)C2)CC1"	"IC50"	"'='"	"32.1"	"nM"	"7.49"	""	"234621"	"UO_0000065"	"15.03"	"0.29"	"4.27"	"7.18"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3981393"	""	"0"	"337.39"	"0"	"1.91"	"BDBM198575"	"N#CCC(=O)NC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	"352653"	"UO_0000065"	"23.11"	"0.43"	"5.89"	"6.98"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3927682"	""	"0"	"452.87"	"0"	"3.71"	"BDBM198577"	"Cc1c(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)c(Cl)nn1CC(F)(F)F"	"IC50"	"'='"	"180.0"	"nM"	"6.75"	""	"352655"	"UO_0000065"	"14.89"	"0.30"	"3.03"	"8.44"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3889789"	""	"0"	"388.48"	"0"	"2.88"	"BDBM198581"	"O[C@H]1Cc2ccccc2[C@H]1NC1CCC(c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"71.0"	"nM"	"7.15"	""	"352659"	"UO_0000065"	"18.40"	"0.34"	"4.27"	"7.84"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4111878"	""	"0"	"388.48"	"0"	"2.88"	"BDBM198582"	"O[C@@H]1Cc2ccccc2[C@@H]1NC1CCC(c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"110.0"	"nM"	"6.96"	""	"352660"	"UO_0000065"	"17.91"	"0.33"	"4.08"	"7.64"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3965030"	""	"0"	"395.39"	"0"	"1.90"	"BDBM198591"	"O=C(CN[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1)NCC(F)(F)F"	"IC50"	"'='"	"80.0"	"nM"	"7.10"	""	"352669"	"UO_0000065"	"17.95"	"0.35"	"5.20"	"7.10"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3958508"	""	"0"	"385.48"	"0"	"3.34"	"BDBM198598"	"N#Cc1ccc(CCN[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"390.0"	"nM"	"6.41"	""	"352676"	"UO_0000065"	"16.63"	"0.30"	"3.07"	"6.77"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3941598"	""	"0"	"296.38"	"0"	"2.38"	"BDBM198599"	"c1cc2c(ncn3nnc([C@H]4CC[C@H](NC5CC5)CC4)c23)[nH]1"	"IC50"	"'='"	"80.0"	"nM"	"7.10"	""	"352677"	"UO_0000065"	"23.95"	"0.44"	"4.72"	"10.01"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3902570"	""	"0"	"271.32"	"0"	"1.87"	"BDBM198608"	"OC[C@H]1CC[C@@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"36.0"	"nM"	"7.44"	""	"352686"	"UO_0000065"	"27.44"	"0.51"	"5.57"	"9.41"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3890993"	""	"0"	"326.40"	"0"	"1.56"	"BDBM198610"	"OC1CN(C[C@H]2CC[C@@H](c3nnn4cnc5[nH]ccc5c34)CC2)C1"	"IC50"	"'='"	"300.0"	"nM"	"6.52"	""	"352688"	"UO_0000065"	"19.98"	"0.37"	"4.96"	"7.92"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3972067"	""	"0"	"392.43"	"0"	"3.91"	"BDBM198620"	"FC(F)(F)CN(CC1CC1)[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"31.0"	"nM"	"7.51"	""	"352698"	"UO_0000065"	"19.13"	"0.37"	"3.60"	"12.09"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3947782"	""	"0"	"335.39"	"0"	"1.77"	"BDBM198623"	"O=S(=O)(O)C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"47.0"	"nM"	"7.33"	""	"352701"	"UO_0000065"	"21.85"	"0.44"	"5.56"	"6.47"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3898818"	""	"0"	"317.36"	"0"	"2.85"	"BDBM198638"	"N#CC(C#N)=C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	"352716"	"UO_0000065"	"24.85"	"0.45"	"5.04"	"7.41"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3945676"	""	"0"	"352.47"	"0"	"3.36"	"BDBM198439"	"Cc1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)s1"	"IC50"	"'='"	"52.0"	"nM"	"7.28"	""	"352517"	"UO_0000065"	"20.67"	"0.40"	"3.92"	"11.73"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3985243"	""	"0"	"413.27"	"0"	"3.46"	"BDBM198472"	"FC(F)(Br)CNC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	"352550"	"UO_0000065"	"19.17"	"0.43"	"4.46"	"11.17"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3956966"	""	"0"	"533.00"	"2"	"5.54"	"BDBM198512"	"OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)CC1"	"IC50"	"'='"	"97.0"	"nM"	"7.01"	""	"352590"	"UO_0000065"	"13.16"	"0.26"	"1.47"	"8.52"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3973072"	""	"0"	"392.51"	"0"	"2.41"	"BDBM198517"	"N#CCCN1CCN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)CC1"	"IC50"	"'='"	"190.0"	"nM"	"6.72"	""	"352595"	"UO_0000065"	"17.12"	"0.32"	"4.31"	"7.54"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3983856"	""	"0"	"324.39"	"0"	"2.16"	"BDBM198562"	"O=C(NC1CC1)[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"220.0"	"nM"	"6.66"	""	"352640"	"UO_0000065"	"20.52"	"0.38"	"4.50"	"7.57"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4090883"	""	"0"	"285.35"	"0"	"1.57"	"5"	"C=CC(=O)N1CCC[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4005719"	"Inhibition of recombinant human GST-tagged cytoplasmic JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by microfluidic assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4004825"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL3647857"	""	"0"	"423.40"	"0"	"2.55"	"BDBM147967"	"N#C[C@H]1C[C@@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc([C@@H](O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"285901"	"UO_0000065"	"20.13"	"0.39"	"5.97"	"6.21"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3655082"	""	"0"	"337.45"	"0"	"1.50"	"BDBM159749"	"CC(C)CS(=O)(=O)N[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"542.0"	"nM"	"6.27"	""	"302559"	"UO_0000065"	"18.57"	"0.37"	"4.77"	"6.89"	"True"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651039"	""	"0"	"407.43"	"0"	"2.43"	"BDBM153216"	"C=C(CNC(C)=O)C(=O)Nc1cccc(-c2ncnc3[nH]cc(C(=O)OCC)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294164"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3965485"	""	"0"	"340.39"	"0"	"1.08"	"BDBM198564"	"O=C([C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1)N1CC(O)C1"	"IC50"	"'='"	"250.0"	"nM"	"6.60"	""	"352642"	"UO_0000065"	"19.40"	"0.36"	"5.52"	"6.64"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3930389"	""	"0"	"319.37"	"0"	"2.93"	"BDBM198639"	"N#CC(C#N)C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"8.8"	"nM"	"8.06"	""	"352717"	"UO_0000065"	"25.22"	"0.46"	"5.13"	"7.57"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3900105"	""	"0"	"280.34"	"0"	"2.79"	"BDBM198643"	"N#CC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"2.5"	"nM"	"8.60"	""	"352721"	"UO_0000065"	"30.68"	"0.56"	"5.81"	"10.41"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3945399"	""	"0"	"294.36"	"0"	"3.04"	"BDBM198648"	"CC(C#N)[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"6.7"	"nM"	"8.17"	""	"352726"	"UO_0000065"	"27.77"	"0.51"	"5.13"	"9.89"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3896766"	""	"0"	"326.45"	"0"	"3.27"	"BDBM198535"	"CC(C)(C)NC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"45.0"	"nM"	"7.35"	""	"352613"	"UO_0000065"	"22.51"	"0.42"	"4.08"	"10.36"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4106545"	""	"0"	"367.50"	"0"	"2.52"	"BDBM198543"	"CN(C)[C@@H]1CCN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C1"	"IC50"	"'='"	"230.0"	"nM"	"6.64"	""	"352621"	"UO_0000065"	"18.06"	"0.34"	"4.12"	"10.16"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3972353"	""	"0"	"402.37"	"0"	"3.67"	"BDBM198545"	"FC(F)(F)C(F)(F)CNC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"34.0"	"nM"	"7.47"	""	"352623"	"UO_0000065"	"18.56"	"0.36"	"3.80"	"10.53"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3931435"	""	"0"	"399.46"	"0"	"3.26"	"BDBM198554"	"N#CC(NC(=O)[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1)c1ccccc1"	"IC50"	"'='"	"89.0"	"nM"	"7.05"	""	"352632"	"UO_0000065"	"17.65"	"0.32"	"3.79"	"6.31"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3956311"	""	"0"	"392.43"	"0"	"3.91"	"BDBM198248"	"FC(F)(F)C1CCC(N2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)CC1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"352330"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3973060"	""	"0"	"375.43"	"0"	"3.73"	"BDBM198277"	"O=C(OCc1ccccc1)N1CCC(c2ncn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"89.0"	"nM"	"7.05"	""	"352356"	"UO_0000065"	"18.78"	"0.34"	"3.32"	"9.34"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3922488"	""	"0"	"363.47"	"0"	"3.11"	"BDBM198282"	"N#CC1CCN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)CC1"	"IC50"	"'='"	"200.0"	"nM"	"6.70"	""	"352360"	"UO_0000065"	"18.43"	"0.34"	"3.59"	"7.80"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3900746"	""	"0"	"428.46"	"0"	"4.69"	"BDBM198291"	"FC(F)(F)c1ccc(CNC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"70.0"	"nM"	"7.16"	""	"352369"	"UO_0000065"	"16.70"	"0.32"	"2.46"	"10.09"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3962689"	""	"0"	"464.88"	"1"	"5.54"	"BDBM198308"	"FC(F)(F)Oc1ccc(NC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)c(Cl)c1"	"IC50"	"'='"	"400.0"	"nM"	"6.40"	""	"352386"	"UO_0000065"	"13.76"	"0.27"	"0.86"	"7.98"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3926748"	""	"0"	"326.40"	"0"	"1.96"	"BDBM198317"	"c1cc2c(ncn3nnc(C4CCC(N5CCOCC5)CC4)c23)[nH]1"	"IC50"	"'='"	"230.0"	"nM"	"6.64"	""	"352395"	"UO_0000065"	"20.34"	"0.38"	"4.68"	"9.31"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3906857"	""	"0"	"357.42"	"0"	"3.62"	"BDBM198328"	"N#Cc1ccc(N[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"24.0"	"nM"	"7.62"	""	"352406"	"UO_0000065"	"21.32"	"0.39"	"4.00"	"8.05"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3897300"	""	"0"	"374.49"	"0"	"3.85"	"BDBM198332"	"c1ccc(CCCN[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"290.0"	"nM"	"6.54"	""	"352410"	"UO_0000065"	"17.46"	"0.32"	"2.69"	"9.22"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3980979"	""	"0"	"414.44"	"0"	"4.44"	"BDBM198336"	"FC(F)(F)c1ccc(CN[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"43.0"	"nM"	"7.37"	""	"352414"	"UO_0000065"	"17.77"	"0.34"	"2.93"	"10.39"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3956418"	""	"0"	"364.46"	"0"	"2.43"	"BDBM198391"	"c1nc(CCNC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)c[nH]1"	"IC50"	"'='"	"38.0"	"nM"	"7.42"	""	"352469"	"UO_0000065"	"20.36"	"0.38"	"4.99"	"7.45"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3985363"	""	"0"	"346.44"	"0"	"3.42"	"BDBM198394"	"c1ccc(CN[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"46.0"	"nM"	"7.34"	""	"352472"	"UO_0000065"	"21.18"	"0.39"	"3.92"	"10.35"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3980095"	""	"0"	"364.43"	"0"	"3.56"	"BDBM198396"	"Fc1ccc(CN[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"42.0"	"nM"	"7.38"	""	"352474"	"UO_0000065"	"20.24"	"0.37"	"3.82"	"10.40"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3972033"	""	"0"	"406.46"	"0"	"3.38"	"BDBM198411"	"O=C(NCCc1ccc(F)cc1)[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"33.0"	"nM"	"7.48"	""	"352489"	"UO_0000065"	"18.41"	"0.34"	"4.10"	"8.50"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3933458"	""	"0"	"356.41"	"0"	"2.45"	"BDBM198412"	"O=C([C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1)N1CC[C@H](F)C1"	"IC50"	"'='"	"420.0"	"nM"	"6.38"	""	"352490"	"UO_0000065"	"17.89"	"0.33"	"3.93"	"8.05"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3905358"	""	"0"	"348.41"	"0"	"3.09"	"BDBM198418"	"C(=C/c1ccco1)\CN1CCC(c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"250.0"	"nM"	"6.60"	""	"352496"	"UO_0000065"	"18.95"	"0.35"	"3.51"	"8.77"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3897131"	""	"0"	"414.39"	"0"	"3.64"	"BDBM198251"	"O=C(c1ccc(C(F)(F)F)cc1)N1CCC(c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"820.0"	"nM"	"6.09"	""	"352333"	"UO_0000065"	"14.69"	"0.28"	"2.45"	"7.69"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3927827"	""	"0"	"390.45"	"0"	"3.56"	"BDBM198253"	"O=C(N[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1)OCc1ccccc1"	"IC50"	"'='"	"32.0"	"nM"	"7.50"	""	"352335"	"UO_0000065"	"19.20"	"0.35"	"3.93"	"7.71"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3931093"	""	"0"	"418.32"	"0"	"3.20"	"BDBM198352"	"Brc1ncc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)s1"	"IC50"	"'='"	"2.3"	"nM"	"8.64"	""	"352430"	"UO_0000065"	"20.65"	"0.47"	"5.44"	"11.52"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3969811"	""	"0"	"351.39"	"0"	"2.52"	"BDBM198361"	"Fc1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)nc1"	"IC50"	"'='"	"200.0"	"nM"	"6.70"	""	"352439"	"UO_0000065"	"19.06"	"0.35"	"4.18"	"8.93"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3917860"	""	"0"	"458.49"	"0"	"3.92"	"BDBM198371"	"OC(CNC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1)(c1ccccc1)C(F)(F)F"	"IC50"	"'='"	"93.0"	"nM"	"7.03"	""	"352449"	"UO_0000065"	"15.34"	"0.29"	"3.11"	"7.72"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3965670"	""	"0"	"454.46"	"0"	"4.89"	"BDBM198374"	"FC(F)(F)c1nc2cc(NC[C@H]3CC[C@H](c4nnn5cnc6[nH]ccc6c45)CC3)ccc2[nH]1"	"IC50"	"'='"	"7.4"	"nM"	"8.13"	""	"352452"	"UO_0000065"	"17.89"	"0.34"	"3.24"	"8.17"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3972475"	""	"0"	"393.40"	"0"	"3.14"	"BDBM198245"	"N#Cc1cc(F)c(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)c(F)c1"	"IC50"	"'='"	"1.5"	"nM"	"8.82"	""	"352327"	"UO_0000065"	"22.43"	"0.42"	"5.68"	"10.27"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647748"	""	"0"	"498.53"	"0"	"3.25"	"BDBM147851"	"CC(C)N[C@@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"19.0"	"nM"	"7.72"	""	"285785"	"UO_0000065"	"15.49"	"0.31"	"4.47"	"5.40"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652298"	""	"0"	"393.51"	"0"	"1.35"	"BDBM113107"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC[C@H](O)C2)CC1"	"IC50"	"'='"	"44.7"	"nM"	"7.35"	""	"234551"	"UO_0000065"	"18.68"	"0.37"	"6.00"	"7.18"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3699484"	""	"0"	"356.41"	"0"	"2.32"	"BDBM147499"	"CN[C@H]1CC[C@H](C#N)[C@@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)C1"	"IC50"	"'>'"	"1500.0"	"nM"	""	""	"285426"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702920"	""	"0"	"458.54"	"0"	"2.00"	"BDBM147619"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)N3CCOCC3)cc2)n1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"285549"	"UO_0000065"	"19.63"	"0.38"	"7.00"	"6.28"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645115"	""	"0"	"379.45"	"0"	"2.81"	"BDBM99889"	"CS(=O)(=O)c1ccc(-c2cccn3nc(NCc4cccnc4)nc23)cc1"	"IC50"	"'='"	"2757.82"	"nM"	"5.56"	""	"216557"	"UO_0000065"	"14.65"	"0.28"	"2.75"	"6.23"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703061"	""	"0"	"440.86"	"0"	"3.61"	"BDBM147771"	"N#C[C@H]1C[C@@H](NCC(F)F)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)c(F)c2)n1"	"IC50"	"'='"	"35.0"	"nM"	"7.46"	""	"285705"	"UO_0000065"	"16.91"	"0.34"	"3.85"	"6.86"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645005"	""	"0"	"485.59"	"0"	"3.81"	"BDBM99757"	"COc1ncccc1-c1cccn2nc(Nc3ccc(C4CCN(CC(=O)N(C)C)CC4)cc3)nc12"	"IC50"	"'='"	"251.31"	"nM"	"6.60"	""	"216445"	"UO_0000065"	"13.59"	"0.25"	"2.79"	"7.51"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642256"	""	"0"	"477.59"	"0"	"4.02"	"BDBM99514"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4ccc(OCCN5CCCC5)cc4)nc23)cc1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"216206"	"UO_0000065"	"18.84"	"0.36"	"4.98"	"10.13"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647833"	""	"0"	"417.87"	"0"	"3.67"	"BDBM147940"	"[C-]#[N+][C@H]1C[C@@](O)(C2CC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)c(F)c2)n1"	"IC50"	"'='"	"59.0"	"nM"	"7.23"	""	"285874"	"UO_0000065"	"17.30"	"0.34"	"3.56"	"7.41"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3644994"	""	"0"	"439.52"	"0"	"3.68"	"BDBM99746"	"CN1CCN(c2ccc(Nc3nc4c(OCc5ccccc5C#N)cccn4n3)cc2)CC1"	"IC50"	"'='"	"15.1"	"nM"	"7.82"	""	"216434"	"UO_0000065"	"17.79"	"0.32"	"4.14"	"9.57"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3702992"	""	"0"	"419.44"	"0"	"2.52"	"BDBM147702"	"CN(C)[C@H]1CC[C@@H](n2cc(C(N)=O)c(Nc3ccc(OC(F)F)nc3)n2)[C@H](C#N)C1"	"IC50"	"'>'"	"1500.0"	"nM"	""	""	"285636"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645078"	""	"0"	"497.65"	"0"	"4.47"	"BDBM99846"	"CN(C)C(=O)CN1CCC(c2ccc(Nc3nc4c(-c5cccc(N(C)C)c5)cccn4n3)cc2)CC1"	"IC50"	"'='"	"4.99"	"nM"	"8.30"	""	"216519"	"UO_0000065"	"16.68"	"0.31"	"3.83"	"12.03"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL4531121"	""	"0"	"317.37"	"0"	"2.70"	"9"	"CCS(=O)(=O)Nc1cc(-c2ccc(O)cc2)cc2[nH]ncc12"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	""	"UO_0000065"	"25.21"	"0.50"	"5.30"	"8.41"	"False"	"CHEMBL4478762"	"Inhibition of human His-tagged JAK2 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4477220"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2016"	"None"	""
"CHEMBL3699532"	""	"0"	"449.48"	"0"	"4.18"	"BDBM147550"	"CC(C)(c1ccc(Nc2nn([C@H]3CCCC[C@@H]3C#N)cc2C(N)=O)cc1)[C@@H](O)C(F)(F)F"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	"285480"	"UO_0000065"	"17.80"	"0.34"	"3.82"	"6.84"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645539"	""	"0"	"330.35"	"0"	"2.53"	"BDBM107123"	"O=C(Cn1cncn1)Nc1cccc(-c2cnc3ccccc3n2)c1"	"IC50"	"'>'"	"50000.0"	"nM"	""	""	"226360"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3973276"	""	"0"	"354.41"	"0"	"1.47"	"BDBM198561"	"O=C([C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1)N1CC[C@H](O)C1"	"IC50"	"'='"	"910.0"	"nM"	"6.04"	""	"352639"	"UO_0000065"	"17.05"	"0.32"	"4.57"	"6.08"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3931001"	""	"0"	"350.40"	"0"	"3.88"	"BDBM198584"	"Fc1ccc(N[C@H]2CC[C@@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"220.0"	"nM"	"6.66"	""	"352662"	"UO_0000065"	"19.00"	"0.35"	"2.78"	"9.39"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3949248"	""	"0"	"504.51"	"1"	"3.69"	"BDBM198597"	"COc1ccc(C(O)(CN[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C(F)(F)F)cc1OC"	"IC50"	"'='"	"89.0"	"nM"	"7.05"	""	"352675"	"UO_0000065"	"13.98"	"0.27"	"3.36"	"6.43"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652393"	""	"0"	"483.64"	"0"	"2.50"	"BDBM113205"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCN(Cc3ccccn3)CC2)CC1"	"IC50"	"'='"	"49.8"	"nM"	"7.30"	""	"234648"	"UO_0000065"	"15.10"	"0.29"	"4.80"	"7.43"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3665219"	""	"0"	"482.53"	"0"	"3.67"	"BDBM112619"	"CC(C)CS(=O)(=O)N1C[C@@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C[C@H](C(F)(F)F)C1"	"IC50"	"'='"	"0.4635"	"nM"	"9.33"	""	"233856"	"UO_0000065"	"19.34"	"0.39"	"5.66"	"8.99"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703002"	""	"0"	"421.43"	"0"	"2.93"	"BDBM147712"	"CN(C)[C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(C(F)(F)F)nc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"145.0"	"nM"	"6.84"	""	"285646"	"UO_0000065"	"16.23"	"0.31"	"3.91"	"6.06"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3900631"	""	"0"	"324.43"	"0"	"2.98"	"BDBM198490"	"c1cc2c(ncn3nnc([C@H]4CC[C@H](CN5CCCC5)CC4)c23)[nH]1"	"IC50"	"'='"	"77.0"	"nM"	"7.11"	""	"352568"	"UO_0000065"	"21.93"	"0.40"	"4.13"	"11.45"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3907648"	""	"0"	"326.40"	"0"	"1.87"	"BDBM198497"	"c1cc2c(ncn3nnc([C@H]4CC[C@H](CNC5COC5)CC4)c23)[nH]1"	"IC50"	"'='"	"120.0"	"nM"	"6.92"	""	"352575"	"UO_0000065"	"21.20"	"0.39"	"5.05"	"8.64"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3959692"	""	"0"	"418.52"	"0"	"4.69"	"BDBM198527"	"Fc1ccc(C2(NC[C@H]3CC[C@H](c4nnn5cnc6[nH]ccc6c45)CC3)CCC2)cc1"	"IC50"	"'='"	"34.0"	"nM"	"7.47"	""	"352605"	"UO_0000065"	"17.85"	"0.33"	"2.78"	"10.53"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652398"	""	"0"	"421.57"	"0"	"1.99"	"BDBM113210"	"C[C@@H]1C[C@@H](CS(=O)(=O)N2CCC[C@@H](O)C2)CC[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"6.89"	"nM"	"8.16"	""	"234653"	"UO_0000065"	"19.36"	"0.38"	"6.17"	"7.97"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3647848"	""	"0"	"409.37"	"0"	"2.85"	"BDBM147957"	"N#C[C@H]1C[C@@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(OC(F)(F)F)cc2)n1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"285891"	"UO_0000065"	"20.28"	"0.39"	"5.45"	"6.58"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702898"	""	"0"	"349.40"	"0"	"2.56"	"BDBM147597"	"Cc1cc(Nc2nn([C@H]3CCCC[C@@H]3C#N)cc2C(N)=O)cnc1C#N"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	"285527"	"UO_0000065"	"22.17"	"0.41"	"5.18"	"5.81"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645087"	""	"0"	"495.55"	"1"	"5.88"	"BDBM99860"	"CC(C)COc1ccc(C(F)(F)F)cc1-c1cccn2nc(Nc3ccc4c(c3)CCNCC4)nc12"	"IC50"	"'='"	"1078.21"	"nM"	"5.97"	""	"216529"	"UO_0000065"	"12.04"	"0.23"	"0.09"	"9.40"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3694580"	""	"0"	"351.80"	"0"	"4.05"	"BDBM125901"	"O=C1Nc2cccc(c2)CNc2nc(ncc2Cl)Nc2cccc1c2"	"IC50"	"'='"	"104.0"	"nM"	"6.98"	""	"255674"	"UO_0000065"	"19.85"	"0.38"	"2.93"	"8.85"	"False"	"CHEMBL3707544"	"In Vitro Kinase Assay: One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Biochemistry 1999, 269, 94-104. The catalytic domains of human JAK1 (a.a. 837-1142), JAK2 (a.a. 828-1132) and JAK3 (a.a. 781-1124) with an N-terminal His tag were expressed using baculovirus in insect cells and purified. The catalytic activity of JAK1, JAK2 or JAK3 was assayed by measuring the phosphorylation of a biotinylated peptide. The phosphorylated peptide was detected by homogenous time resolved fluorescence (HTRF). IC50s of compounds were measured for each kinase in the reactions that contain the enzyme, ATP and 500 nM peptide in 50 mM Tris (pH 7.8) buffer with 100 mM NaCl, 5 mM DTT, and 0.1 mg/mL (0.01%) BSA. The ATP concentration in the reactions was 90 uM for JAK1, 30 uM for JAK2 and 3 uM for JAK3. Reactions were carried out at room temperature for 1 hr and then stopped with 20 uL 45 mM EDTA."	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639093"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3647896"	""	"0"	"426.91"	"0"	"3.14"	"BDBM148008"	"N#C[C@H]1C[C@@H](C(=O)NC2CC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"295.0"	"nM"	"6.53"	""	"285943"	"UO_0000065"	"15.30"	"0.30"	"3.39"	"5.19"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3965965"	""	"0"	"351.39"	"0"	"2.52"	"BDBM198344"	"Fc1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cn1"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	"352422"	"UO_0000065"	"22.27"	"0.41"	"5.30"	"10.43"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3937326"	""	"0"	"400.41"	"0"	"4.41"	"BDBM198453"	"Fc1cc(NC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc(F)c1F"	"IC50"	"'='"	"180.0"	"nM"	"6.75"	""	"352531"	"UO_0000065"	"16.84"	"0.32"	"2.33"	"9.51"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3948921"	""	"0"	"284.37"	"0"	"2.10"	"BDBM198532"	"CNC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"29.0"	"nM"	"7.54"	""	"352610"	"UO_0000065"	"26.51"	"0.49"	"5.44"	"10.63"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3959789"	""	"0"	"429.41"	"0"	"4.04"	"BDBM198250"	"O=C(Nc1cccc(C(F)(F)F)c1)N1CCC(c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"352332"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3967397"	""	"0"	"360.46"	"0"	"3.67"	"BDBM198392"	"c1ccc(CNC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"41.0"	"nM"	"7.39"	""	"352470"	"UO_0000065"	"20.49"	"0.37"	"3.72"	"10.42"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3941241"	""	"0"	"346.44"	"0"	"3.42"	"BDBM198393"	"c1ccc(CN[C@H]2CC[C@@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"740.0"	"nM"	"6.13"	""	"352471"	"UO_0000065"	"17.70"	"0.32"	"2.71"	"8.65"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3911096"	""	"0"	"388.34"	"0"	"3.42"	"BDBM198589"	"FC(F)(F)C(F)(F)CN[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	"352667"	"UO_0000065"	"20.31"	"0.40"	"4.47"	"11.12"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3926894"	""	"0"	"445.45"	"0"	"3.07"	"BDBM198657"	"OC(CN[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1)(c1cccnc1)C(F)(F)F"	"IC50"	"'='"	"31.0"	"nM"	"7.51"	""	"352670"	"UO_0000065"	"16.86"	"0.32"	"4.44"	"7.22"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3985391"	""	"0"	"475.48"	"0"	"3.08"	"BDBM198594"	"COc1ccc(C(O)(CN[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C(F)(F)F)cn1"	"IC50"	"'='"	"32.0"	"nM"	"7.50"	""	"352672"	"UO_0000065"	"15.76"	"0.30"	"4.41"	"6.62"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3941431"	""	"0"	"295.35"	"0"	"1.74"	"BDBM198600"	"N#CCN[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"30.0"	"nM"	"7.52"	""	"352678"	"UO_0000065"	"25.47"	"0.47"	"5.78"	"7.94"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL2208023"	""	"0"	"304.35"	"0"	"3.85"	"6"	"CC(=O)Nc1ccc(-c2ccnc(Nc3ccccc3)n2)cc1"	"IC50"	"'='"	"27.4"	"nM"	"7.56"	""	""	"UO_0000065"	"24.85"	"0.45"	"3.71"	"11.30"	"False"	"CHEMBL4268221"	"Inhibition of human JAK2 using poly(Glu:Tyr)(4:1) as substrate preincubated for 20 mins followed by [gamma33P]ATP addition measured after 120 mins by ion exchange filter paper method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4265943"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2018"	"None"	""
"CHEMBL4110067"	""	"0"	"454.38"	"0"	"2.95"	"BDBM237749"	"N#C[C@@H]1CN(C(=O)OCC(F)(F)F)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"268.0"	"nM"	"6.57"	""	"414853"	"UO_0000065"	"14.46"	"0.28"	"3.62"	"5.20"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4111826"	""	"0"	"426.45"	"0"	"2.80"	"BDBM237751"	"N#C[C@@H]1CN(C(=O)OCC2CC2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"286.0"	"nM"	"6.54"	""	"414855"	"UO_0000065"	"15.34"	"0.29"	"3.74"	"5.18"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3330120"	""	"0"	"502.02"	"1"	"4.69"	"23"	"Cc1ccc(Cl)cc1-c1[nH]c(-c2ccnc(Nc3ccc(N4CCN(C)CC4)cc3)n2)cc1C(N)=O"	"IC50"	"'='"	"59.0"	"nM"	"7.23"	""	""	"UO_0000065"	"14.40"	"0.27"	"2.54"	"7.01"	"False"	"CHEMBL3374493"	"Inhibition of recombinant human JAK2 (808-1132 residues) using LPLDKDYYVVREPGQ as substrate by radiometric assay in presence of [33P]-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL4518744"	""	"0"	"351.82"	"0"	"3.35"	"14"	"CCS(=O)(=O)Nc1cc(-c2ccc(O)c(Cl)c2)cc2[nH]ncc12"	"IC50"	"'='"	"19.95"	"nM"	"7.70"	""	""	"UO_0000065"	"21.89"	"0.46"	"4.35"	"8.10"	"False"	"CHEMBL4478762"	"Inhibition of human His-tagged JAK2 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4477220"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2016"	"None"	""
"CHEMBL3330120"	""	"0"	"502.02"	"1"	"4.69"	"23"	"Cc1ccc(Cl)cc1-c1[nH]c(-c2ccnc(Nc3ccc(N4CCN(C)CC4)cc3)n2)cc1C(N)=O"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL3374497"	"Inhibition of JAK2 V617F mutant in human SET2 cells"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330127"	""	"0"	"415.30"	"0"	"3.86"	"30"	"NC(=O)c1cc(-c2ccnc(N)n2)[nH]c1-c1cc(C(F)(F)F)ccc1C(F)(F)F"	"IC50"	"'='"	"3070.0"	"nM"	"5.51"	""	""	"UO_0000065"	"13.27"	"0.26"	"1.65"	"4.98"	"False"	"CHEMBL3374497"	"Inhibition of JAK2 V617F mutant in human SET2 cells"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330110"	""	"0"	"385.86"	"0"	"3.06"	"13"	"COCCNC(=O)c1cc(-c2ccnc(N)n2)[nH]c1-c1cc(Cl)ccc1C"	"IC50"	"'='"	"268.0"	"nM"	"6.57"	""	""	"UO_0000065"	"17.03"	"0.33"	"3.51"	"6.20"	"False"	"CHEMBL3374493"	"Inhibition of recombinant human JAK2 (808-1132 residues) using LPLDKDYYVVREPGQ as substrate by radiometric assay in presence of [33P]-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL4175808"	""	"0"	"399.52"	"0"	"3.41"	"22"	"Cc1cnc(Nc2cc(N3C[C@@H]4C[C@H]3CN4C)cnc2F)nc1N[C@H](C)C(C)C"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4145184"	"Inhibition of recombinant human JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate after 10 mins by caliper assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4138312"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3330125"	""	"0"	"381.75"	"0"	"3.49"	"28"	"NC(=O)c1cc(-c2ccnc(N)n2)[nH]c1-c1cc(C(F)(F)F)ccc1Cl"	"IC50"	"'='"	"480.0"	"nM"	"6.32"	""	""	"UO_0000065"	"16.55"	"0.33"	"2.83"	"5.71"	"False"	"CHEMBL3374497"	"Inhibition of JAK2 V617F mutant in human SET2 cells"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330126"	""	"0"	"397.74"	"0"	"3.37"	"29"	"NC(=O)c1cc(-c2ccnc(N)n2)[nH]c1-c1cc(OC(F)(F)F)ccc1Cl"	"IC50"	"'='"	"1100.0"	"nM"	"5.96"	""	""	"UO_0000065"	"14.98"	"0.30"	"2.59"	"4.97"	"False"	"CHEMBL3374497"	"Inhibition of JAK2 V617F mutant in human SET2 cells"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330114"	""	"0"	"424.94"	"0"	"3.51"	"17"	"Cc1ccc(Cl)cc1-c1[nH]c(-c2ccnc(N)n2)cc1C(=O)NC1CCN(C)CC1"	"IC50"	"'='"	"46.0"	"nM"	"7.34"	""	""	"UO_0000065"	"17.27"	"0.33"	"3.83"	"7.34"	"False"	"CHEMBL3374493"	"Inhibition of recombinant human JAK2 (808-1132 residues) using LPLDKDYYVVREPGQ as substrate by radiometric assay in presence of [33P]-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3954558"	""	"0"	"309.40"	"0"	"0.82"	"BDBM228712"	"CCS(=O)(=O)N(C)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399631"	"UO_0000065"	"33.16"	"0.67"	"9.44"	"12.48"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3949972"	""	"0"	"372.45"	"0"	"1.47"	"BDBM228714"	"CN(c1ccc(S(C)(=O)=O)cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399633"	"UO_0000065"	"27.55"	"0.54"	"8.79"	"10.79"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3897417"	""	"0"	"405.46"	"0"	"2.63"	"BDBM228672"	"COc1cc2ncnc(N(C)[C@@H]3CCN(c4ncnc5[nH]ccc45)C3)c2cc1OC"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399644"	"UO_0000065"	"25.30"	"0.47"	"7.63"	"11.12"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3926766"	""	"0"	"253.31"	"0"	"2.51"	"BDBM198258"	"c1cc2c(ncn3nnc(C4CC5CCC4C5)c23)[nH]1"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	"352340"	"UO_0000065"	"31.13"	"0.57"	"5.38"	"13.40"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3954819"	""	"0"	"376.46"	"0"	"2.96"	"BDBM198405"	"OC(CN[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1)c1ccccc1"	"IC50"	"'='"	"85.0"	"nM"	"7.07"	""	"352483"	"UO_0000065"	"18.78"	"0.34"	"4.11"	"7.76"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3902579"	""	"0"	"387.47"	"0"	"0.98"	"BDBM228697"	"CNS(=O)(=O)c1ccc(N(C)[C@@H]2CCN(c3ncnc4[nH]ccc34)C2)nc1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399740"	"UO_0000065"	"23.90"	"0.47"	"8.28"	"8.64"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3944875"	""	"0"	"429.89"	"0"	"0.10"	"BDBM236509"	"Cn1cc(Nc2ncc(Cl)c(NC3COC4C(NS(C)(=O)=O)COC34)n2)cn1"	"IC50"	"'='"	"51.0"	"nM"	"7.29"	""	"411893"	"UO_0000065"	"16.96"	"0.36"	"7.19"	"5.51"	"False"	"CHEMBL3888641"	"Kinase Assay: Aurora-A (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 200 μM LRRASLG (Kemptide), 10 mM MgAcetate and [γ-33P-ATP](specific activity approx. 500 cpm/pmol, concentration as required). The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of 3% phosphoric acid solution. 10 μL of the reaction is then spotted onto a P30 filtermat and washed three times for 5 minutes in 75 mM phosphoric acid and once in methanol prior to drying and scintillation counting."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886792"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3746882"	""	"0"	"371.87"	"0"	"3.70"	"18"	"COc1ccc(-c2nc3c(NCC4CCCNC4)c(Cl)cnc3[nH]2)cc1"	"IC50"	"'='"	"3040.0"	"nM"	"5.52"	""	""	"UO_0000065"	"14.84"	"0.29"	"1.82"	"7.37"	"False"	"CHEMBL3751000"	"Inhibition of N-terminal GST-fused recombinant JAK2 (831 to 1132 residues) (unknown origin) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate by microfluidic capillary electrophoresis method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3745697"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3746976"	""	"0"	"433.97"	"0"	"3.44"	"6"	"CN1CCC(CNc2c(Cl)cnc3[nH]c(-c4cccc(S(C)(=O)=O)c4)nc23)CC1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3751000"	"Inhibition of N-terminal GST-fused recombinant JAK2 (831 to 1132 residues) (unknown origin) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate by microfluidic capillary electrophoresis method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3745697"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3746045"	""	"0"	"373.86"	"0"	"4.17"	"4"	"CN1CCC(CNc2c(Cl)cnc3[nH]c(-c4cccc(F)c4)nc23)CC1"	"IC50"	"'='"	"16200.0"	"nM"	"4.79"	""	""	"UO_0000065"	"12.81"	"0.25"	"0.62"	"8.43"	"False"	"CHEMBL3751000"	"Inhibition of N-terminal GST-fused recombinant JAK2 (831 to 1132 residues) (unknown origin) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate by microfluidic capillary electrophoresis method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3745697"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3746531"	""	"0"	"385.90"	"0"	"4.04"	"2"	"COc1cccc(-c2nc3c(NCC4CCN(C)CC4)c(Cl)cnc3[nH]2)c1"	"IC50"	"'='"	"16200.0"	"nM"	"4.79"	""	""	"UO_0000065"	"12.41"	"0.24"	"0.75"	"7.25"	"False"	"CHEMBL3751000"	"Inhibition of N-terminal GST-fused recombinant JAK2 (831 to 1132 residues) (unknown origin) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate by microfluidic capillary electrophoresis method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3745697"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3746463"	""	"0"	"419.89"	"0"	"3.85"	"30"	"COc1cc(F)c(-c2nc3c(NCC4CCNCC4)c(Cl)cnc3[nH]2)cc1OC"	"IC50"	"'>'"	"22000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3751000"	"Inhibition of N-terminal GST-fused recombinant JAK2 (831 to 1132 residues) (unknown origin) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate by microfluidic capillary electrophoresis method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3745697"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3642416"	""	"0"	"521.65"	"1"	"3.20"	"BDBM99694"	"CN1CCN(c2ccc(Nc3nc4c(OCc5ccccc5N(C)S(C)(=O)=O)cccn4n3)cc2)CC1"	"IC50"	"'='"	"15.01"	"nM"	"7.82"	""	"216383"	"UO_0000065"	"15.00"	"0.29"	"4.62"	"8.21"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703504"	""	"0"	"311.30"	"0"	"2.53"	"BDBM153148"	"CCOC(=O)c1c[nH]c2ncnc(-c3ccc4c(c3)OCO4)c12"	"IC50"	"'='"	"66.0"	"nM"	"7.18"	""	"294096"	"UO_0000065"	"23.07"	"0.43"	"4.65"	"8.32"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL1938642"	""	"0"	"354.44"	"0"	"2.48"	"3"	"NC(=O)c1cnc(N)c2cc(-c3ccc(N4CCOCC4)cc3)sc12"	"IC50"	"'='"	"19.0"	"nM"	"7.72"	""	""	"UO_0000065"	"21.78"	"0.42"	"5.24"	"8.17"	"False"	"CHEMBL1941383"	"Inhibition of human recombinant N-terminal GST-tagged JAK2 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308860"	""
"CHEMBL1938660"	""	"0"	"531.70"	"1"	"3.07"	"26"	"CC(C)(C)NS(=O)(=O)c1ccc(-c2cc3c(N)ncc(C(=O)NCCCN4CCOCC4)c3s2)cc1"	"IC50"	"'='"	"4720.0"	"nM"	"5.33"	""	""	"UO_0000065"	"10.02"	"0.20"	"2.26"	"4.21"	"False"	"CHEMBL1941390"	"Inhibition of TEL-fused JAK2 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3307634"	""
"CHEMBL1947160"	""	"0"	"385.47"	"0"	"3.62"	"26c"	"CN1C/C=C/CNC(=O)c2cccc(c2)-c2ccnc(n2)Nc2cccc(c2)C1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1945048"	""	"0"	"454.45"	"1"	"5.12"	"26f"	"O=C(N1C/C=C/CCOc2cccc(c2)-c2ccnc(n2)Nc2cccc(c2)C1)C(F)(F)F"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1947158"	""	"0"	"372.43"	"0"	"4.55"	"26a"	"O=C1CC/C=C\COc2cccc(c2)-c2ccnc(n2)Nc2cccc(c2)N1"	"IC50"	"'='"	"1750.0"	"nM"	"5.76"	""	""	"UO_0000065"	"15.46"	"0.28"	"1.21"	"7.56"	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1944871"	""	"0"	"412.54"	"1"	"5.44"	"26m"	"C1=C/CN(CC2CC2)Cc2cccc(c2)Nc2nccc(n2)-c2cccc(c2)OCC/1"	"IC50"	"'='"	"1500.0"	"nM"	"5.82"	""	""	"UO_0000065"	"14.12"	"0.26"	"0.38"	"11.58"	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1945047"	""	"0"	"402.50"	"0"	"4.02"	"26q"	"OCCN1C/C=C/CCOc2cccc(c2)-c2ccnc(n2)Nc2cccc(c2)C1"	"IC50"	"'='"	"720.0"	"nM"	"6.14"	""	""	"UO_0000065"	"15.26"	"0.28"	"2.12"	"8.71"	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1945703"	""	"0"	"487.65"	"1"	"5.38"	"27j"	"CCN(CC)CCOc1ccc2cc1CN(C)C/C=C/CCOc1cccc(c1)-c1ccnc(n1)N2"	"IC50"	"'='"	"48.0"	"nM"	"7.32"	""	""	"UO_0000065"	"15.01"	"0.28"	"1.94"	"11.66"	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL3956611"	""	"0"	"357.42"	"0"	"3.62"	"BDBM198314"	"N#Cc1ccc(NC2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"42.0"	"nM"	"7.38"	""	"352392"	"UO_0000065"	"20.64"	"0.37"	"3.76"	"7.79"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3957421"	""	"0"	"414.44"	"0"	"4.44"	"BDBM198335"	"FC(F)(F)c1ccc(CN[C@H]2CC[C@@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"740.0"	"nM"	"6.13"	""	"352413"	"UO_0000065"	"14.79"	"0.28"	"1.69"	"8.65"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3922180"	""	"0"	"322.38"	"0"	"1.71"	"BDBM198350"	"c1cc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)[nH]n1"	"IC50"	"'='"	"72.0"	"nM"	"7.14"	""	"352428"	"UO_0000065"	"22.16"	"0.41"	"5.43"	"7.87"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3908624"	""	"0"	"410.50"	"0"	"2.39"	"BDBM198355"	"CS(=O)(=O)c1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"42.0"	"nM"	"7.38"	""	"352433"	"UO_0000065"	"17.97"	"0.35"	"4.99"	"7.66"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3957659"	""	"0"	"367.84"	"0"	"3.03"	"BDBM198359"	"Clc1cc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)ccn1"	"IC50"	"'='"	"21.0"	"nM"	"7.68"	""	"352437"	"UO_0000065"	"20.87"	"0.40"	"4.65"	"10.24"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3975439"	""	"0"	"382.47"	"0"	"1.49"	"BDBM198390"	"O=C1NCCN1CCNC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"84.0"	"nM"	"7.08"	""	"352468"	"UO_0000065"	"18.50"	"0.35"	"5.59"	"6.85"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL1835147"	""	"0"	"398.47"	"0"	"3.87"	"58"	"NC(=O)c1cnc(NC(C2CC2)C2CC2)c2c1[nH]c1cc(-c3cccnn3)ccc12"	"IC50"	"'='"	"28.0"	"nM"	"7.55"	""	""	"UO_0000065"	"18.95"	"0.34"	"3.68"	"6.89"	"False"	"CHEMBL1840130"	"Inhibition of JAK2-mediated STAT5 phosphorylation in human HEL 92.1.7 irf1-bla cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308090"	""
"CHEMBL1835142"	""	"0"	"428.42"	"0"	"3.97"	"53"	"Cn1cc(-c2ccc3c(c2)[nH]c2c(C(N)=O)cnc(N[C@H](C4CC4)C(F)(F)F)c23)cn1"	"IC50"	"'='"	"41.0"	"nM"	"7.39"	""	""	"UO_0000065"	"17.24"	"0.33"	"3.42"	"7.27"	"False"	"CHEMBL1840130"	"Inhibition of JAK2-mediated STAT5 phosphorylation in human HEL 92.1.7 irf1-bla cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308090"	""
"CHEMBL4113706"	""	"0"	"373.44"	"0"	"0.72"	"BDBM228640"	"CN(c1ccc(S(N)(=O)=O)cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"41.1"	"nM"	"7.39"	""	"399540"	"UO_0000065"	"19.78"	"0.39"	"6.67"	"6.10"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3956529"	""	"0"	"425.44"	"0"	"2.97"	"BDBM228677"	"CN(c1ccc(S(=O)(=O)C(F)(F)F)cc1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399658"	"UO_0000065"	"24.12"	"0.48"	"7.29"	"12.48"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3934580"	""	"0"	"333.42"	"0"	"1.92"	"BDBM198270"	"CS(=O)(=O)C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"5.4"	"nM"	"8.27"	""	"352350"	"UO_0000065"	"24.80"	"0.49"	"6.35"	"8.89"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3897850"	""	"0"	"430.43"	"0"	"4.95"	"BDBM198326"	"Cc1cc(OC(F)(F)F)ccc1NC1CCC(c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"352404"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3920857"	""	"0"	"455.54"	"0"	"2.63"	"16a"	"CS(=O)(=O)N1CCc2oc(-c3ccnc(Nc4ccc(N5CCOCC5)cc4)n3)cc2C1"	"IC50"	"'='"	"42.9"	"nM"	"7.37"	""	""	"UO_0000065"	"16.17"	"0.31"	"4.74"	"7.31"	"False"	"CHEMBL3868063"	"Inhibition of GST-tagged recombinant human JAK2 expressed in baculovirus using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3867460"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2017"	"None"	""
"CHEMBL3974845"	""	"0"	"386.41"	"0"	"4.46"	"5j"	"Cc1cnc(Nc2ccc(/C=C/C(=O)NO)cc2)nc1-c1cc2ccccc2o1"	"IC50"	"'='"	"226.1"	"nM"	"6.65"	""	""	"UO_0000065"	"17.20"	"0.31"	"2.19"	"6.63"	"False"	"CHEMBL3868063"	"Inhibition of GST-tagged recombinant human JAK2 expressed in baculovirus using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3867460"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2017"	"None"	""
"CHEMBL3934182"	""	"0"	"403.44"	"0"	"4.88"	"5b"	"CCOC(=O)COc1ccc(Nc2ncc(C)c(-c3cc4ccccc4o3)n2)cc1"	"IC50"	"'='"	"324.5"	"nM"	"6.49"	""	""	"UO_0000065"	"16.08"	"0.30"	"1.61"	"7.50"	"False"	"CHEMBL3868063"	"Inhibition of GST-tagged recombinant human JAK2 expressed in baculovirus using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3867460"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2017"	"None"	""
"CHEMBL3651966"	""	"0"	"440.47"	"1"	"5.04"	"8; PIM447"	"C[C@@H]1C[C@H](N)C[C@H](c2ccncc2NC(=O)c2ccc(F)c(-c3c(F)cccc3F)n2)C1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3750404"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3745712"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL1938644"	""	"0"	"382.49"	"0"	"3.13"	"9"	"CCNC(=O)c1cnc(N)c2cc(-c3ccc(N4CCOCC4)cc3)sc12"	"IC50"	"'='"	"48.0"	"nM"	"7.32"	""	""	"UO_0000065"	"19.13"	"0.37"	"4.19"	"9.09"	"False"	"CHEMBL1941383"	"Inhibition of human recombinant N-terminal GST-tagged JAK2 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308860"	""
"CHEMBL3343033"	""	"0"	"386.41"	"0"	"4.34"	"1"	"COc1cc2c(Nc3ccc(NC(=O)c4ccccc4)cc3)ncnc2cc1O"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3380804"	"Inhibition of human JAK2 incubated for 20 mins prior to MgCl2 addition measured after 90 mins by mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351874"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3343037"	""	"0"	"430.46"	"0"	"4.01"	"7a"	"COc1cc2c(Nc3ccc(NC(=O)c4ccccc4)cc3)ncnc2cc1OCCO"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3380804"	"Inhibition of human JAK2 incubated for 20 mins prior to MgCl2 addition measured after 90 mins by mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351874"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3343038"	""	"0"	"444.45"	"0"	"4.10"	"7b"	"COc1cc2c(Nc3ccc(NC(=O)c4ccccc4)cc3)ncnc2cc1OCC(=O)O"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3380804"	"Inhibition of human JAK2 incubated for 20 mins prior to MgCl2 addition measured after 90 mins by mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351874"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3343044"	""	"0"	"363.37"	"0"	"3.30"	"14a"	"COc1cc(C(=O)Nc2ccc(NC(=O)c3ccccn3)cc2)ccc1O"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3380804"	"Inhibition of human JAK2 incubated for 20 mins prior to MgCl2 addition measured after 90 mins by mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351874"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3343055"	""	"0"	"459.46"	"0"	"3.04"	"33"	"COc1cc(C(=O)Nc2ccc(NC(=O)c3ccccn3)cc2)cc(N2CCC(=O)NC2=O)c1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3380804"	"Inhibition of human JAK2 incubated for 20 mins prior to MgCl2 addition measured after 90 mins by mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351874"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL1995703"	""	"0"	"509.68"	"1"	"4.10"	"TG101209"	"Cc1cnc(Nc2ccc(N3CCN(C)CC3)cc2)nc1Nc1cccc(S(=O)(=O)NC(C)(C)C)c1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	""	"UO_0000065"	"16.13"	"0.31"	"4.12"	"8.02"	"True"	"CHEMBL3875841"	"Inhibition of human JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3875172"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2016"	"None"	""
"CHEMBL3986618"	""	"0"	"366.86"	"0"	"3.64"	"BDBM198246"	"Clc1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	"352328"	"UO_0000065"	"21.33"	"0.41"	"4.18"	"12.60"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3932581"	""	"0"	"431.49"	"1"	"5.27"	"BDBM198279"	"FC(F)(F)c1ccc(CN2CCC(c3[nH]c(=S)n4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"170.0"	"nM"	"6.77"	""	"352358"	"UO_0000065"	"15.69"	"0.31"	"1.50"	"12.99"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3894474"	""	"0"	"323.40"	"0"	"2.38"	"BDBM198283"	"N#CCCNC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"26.0"	"nM"	"7.58"	""	"352361"	"UO_0000065"	"23.45"	"0.43"	"5.21"	"8.01"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3915165"	""	"0"	"378.46"	"0"	"4.15"	"BDBM198295"	"CN(C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1)c1ccc(F)cc1"	"IC50"	"'='"	"150.0"	"nM"	"6.82"	""	"352373"	"UO_0000065"	"18.03"	"0.33"	"2.67"	"10.99"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3975123"	""	"0"	"424.53"	"0"	"2.28"	"BDBM198437"	"c1cc2c(ncn3nnc(C4CCN(Cc5cnc(N6CCOCC6)s5)CC4)c23)[nH]1"	"IC50"	"'='"	"880.0"	"nM"	"6.06"	""	"352515"	"UO_0000065"	"14.26"	"0.28"	"3.78"	"6.92"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3950399"	""	"0"	"381.48"	"0"	"2.08"	"BDBM198464"	"NC(=O)C1CCN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)CC1"	"IC50"	"'='"	"91.0"	"nM"	"7.04"	""	"352542"	"UO_0000065"	"18.46"	"0.34"	"4.96"	"6.69"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3039513"	"DECERNOTINIB"	"2"	"392.39"	"0"	"3.28"	"7"	"CC[C@@](C)(Nc1ccnc(-c2c[nH]c3ncccc23)n1)C(=O)NCC(F)(F)F"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3299209"	"Inhibition of JAK2 homodimer in human CD34+ cells spiked into human whole blood assessed as inhibition of EPO-induced STAT-5 phosphorylation preincubated for 45 mins followed by EPO addition measured after 15 mins by FACS analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"CHEMBL3638178"	"Blood"	"CD34+ cell"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3297690"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL3912973"	""	"0"	"375.38"	"0"	"4.41"	"5i"	"Cc1cnc(Nc2ccc(OCC(=O)O)cc2)nc1-c1cc2ccccc2o1"	"IC50"	"'='"	"16.6"	"nM"	"7.78"	""	""	"UO_0000065"	"20.73"	"0.38"	"3.37"	"7.98"	"False"	"CHEMBL3868063"	"Inhibition of GST-tagged recombinant human JAK2 expressed in baculovirus using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3867460"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2017"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"Tofacitinib"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"275.1"	"nM"	"6.56"	""	""	"UO_0000065"	"21.00"	"0.39"	"5.02"	"7.38"	"True"	"CHEMBL3868066"	"Inhibition of JAK2 in human TF1 cells assessed as suppression of cell growth"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3867460"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2017"	"CHEMBL3307972"	""
"CHEMBL3948663"	""	"0"	"444.50"	"0"	"3.12"	"16b"	"N#CCC(=O)N1CCc2oc(-c3ccnc(Nc4ccc(N5CCOCC5)cc4)n3)cc2C1"	"IC50"	"'='"	"5521.0"	"nM"	"5.26"	""	""	"UO_0000065"	"11.83"	"0.22"	"2.14"	"4.89"	"False"	"CHEMBL3868067"	"Inhibition of JAK2 V617F mutant in human HEL cells after 1 hr"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3867460"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2017"	"CHEMBL3308090"	""
"CHEMBL3039513"	"DECERNOTINIB"	"2"	"392.39"	"0"	"3.28"	"7"	"CC[C@@](C)(Nc1ccnc(-c2c[nH]c3ncccc23)n1)C(=O)NCC(F)(F)F"	"IC50"	"'='"	"619.0"	"nM"	"6.21"	""	""	"UO_0000065"	"15.82"	"0.30"	"2.93"	"6.49"	"False"	"CHEMBL3299201"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3297690"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL3298400"	""	"0"	"345.47"	"0"	"3.05"	"1"	"CC(C)(C)CNC(=O)CC1CNC(=O)c2cc(-c3ccsc3)cn21"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3300963"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3297733"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2013"	"None"	""
"CHEMBL2062805"	""	"0"	"462.58"	"0"	"3.30"	"BDBM99534"	"CN1CCN(c2ccc(Nc3nc4c(-c5ccc(S(C)(=O)=O)cc5)cccn4n3)cc2)CC1"	"IC50"	"'='"	"2.4"	"nM"	"8.62"	""	"216226"	"UO_0000065"	"18.63"	"0.36"	"5.32"	"10.41"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3702940"	""	"0"	"377.81"	"0"	"2.74"	"BDBM147642"	"N#C[C@H]1C[C@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)c(F)c2)n1"	"IC50"	"'='"	"26.0"	"nM"	"7.58"	""	"285574"	"UO_0000065"	"20.08"	"0.40"	"4.85"	"6.49"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665218"	""	"0"	"440.45"	"0"	"2.64"	"BDBM112618"	"CS(=O)(=O)N1C[C@@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C[C@H](C(F)(F)F)C1"	"IC50"	"'='"	"0.5559"	"nM"	"9.26"	""	"233855"	"UO_0000065"	"21.01"	"0.42"	"6.62"	"8.91"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3658117"	""	"0"	"622.67"	"2"	"5.80"	"BDBM148434"	"Cc1ccc(NC(=O)c2cccc(C(F)(F)F)c2)cc1N1CCc2nc(Nc3ccc(S(=O)(=O)NC4CC4)cc3)ncc2C1"	"IC50"	"'='"	"54.0"	"nM"	"7.27"	""	"286801"	"UO_0000065"	"11.67"	"0.23"	"1.47"	"6.25"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699549"	""	"0"	"378.41"	"0"	"3.67"	"BDBM147567"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2cnc3ccc(F)cc3c2)n1"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	"285497"	"UO_0000065"	"20.75"	"0.38"	"4.18"	"7.16"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3969473"	""	"0"	"241.30"	"0"	"2.65"	"BDBM198198"	"c1cc2c(ncn3nnc(C4CCCCC4)c23)[nH]1"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	"351820"	"UO_0000065"	"32.83"	"0.60"	"5.27"	"13.45"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3947742"	""	"0"	"444.46"	"0"	"3.67"	"BDBM198397"	"OC(CN[C@H]1CC[C@@H](c2nnn3cnc4[nH]ccc4c23)CC1)(c1ccccc1)C(F)(F)F"	"IC50"	"'='"	"750.0"	"nM"	"6.12"	""	"352475"	"UO_0000065"	"13.78"	"0.26"	"2.45"	"6.72"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3963387"	""	"0"	"342.47"	"0"	"2.58"	"BDBM198547"	"c1cc2c(ncn3nnc([C@H]4CC[C@H](CNC5CSC5)CC4)c23)[nH]1"	"IC50"	"'='"	"68.0"	"nM"	"7.17"	""	"352625"	"UO_0000065"	"20.93"	"0.41"	"4.59"	"10.11"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3981542"	""	"0"	"323.36"	"0"	"1.52"	"BDBM198558"	"N#CCNC(=O)[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"33.0"	"nM"	"7.48"	""	"352636"	"UO_0000065"	"23.14"	"0.43"	"5.96"	"6.69"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3968041"	""	"0"	"387.39"	"0"	"2.81"	"BDBM198571"	"O=S(=O)(C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1)C(F)(F)F"	"IC50"	"'='"	"6.1"	"nM"	"8.21"	""	"352649"	"UO_0000065"	"21.21"	"0.43"	"5.40"	"8.83"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3963480"	""	"0"	"380.46"	"0"	"2.40"	"BDBM198573"	"CC(C)(O)c1cn(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)nn1"	"IC50"	"'='"	"97.0"	"nM"	"7.01"	""	"352651"	"UO_0000065"	"18.43"	"0.34"	"4.61"	"6.39"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3922303"	""	"0"	"404.49"	"0"	"4.16"	"BDBM198596"	"Fc1ccc([C@@H]2C[C@H]2CN[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"140.0"	"nM"	"6.85"	""	"352674"	"UO_0000065"	"16.94"	"0.31"	"2.69"	"9.67"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3910017"	""	"0"	"309.38"	"0"	"2.14"	"BDBM198601"	"N#CCCN[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"90.0"	"nM"	"7.05"	""	"352679"	"UO_0000065"	"22.77"	"0.42"	"4.91"	"7.44"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3985220"	""	"0"	"278.32"	"0"	"2.71"	"BDBM198641"	"N#CC=C1CCC(c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	"352719"	"UO_0000065"	"28.22"	"0.51"	"5.14"	"9.50"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3937822"	""	"0"	"325.37"	"0"	"2.75"	"BDBM198644"	"CCOC(=O)C=C1CCC(c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"170.0"	"nM"	"6.77"	""	"352722"	"UO_0000065"	"20.81"	"0.39"	"4.02"	"7.95"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3963319"	""	"0"	"356.43"	"0"	"2.97"	"BDBM198203"	"CC1CCN(C(=O)OC(C)(C)C)CC1c1nnn2cnc3[nH]ccc3c12"	"IC50"	"'='"	"340.0"	"nM"	"6.47"	""	"352285"	"UO_0000065"	"18.15"	"0.34"	"3.50"	"7.32"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3909793"	""	"0"	"333.40"	"0"	"2.38"	"BDBM198210"	"c1cncc(CN2CCCC(c3nnn4cnc5[nH]ccc5c34)C2)c1"	"IC50"	"'='"	"620.0"	"nM"	"6.21"	""	"352292"	"UO_0000065"	"18.62"	"0.34"	"3.83"	"8.28"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3905627"	""	"0"	"329.43"	"0"	"3.16"	"BDBM198264"	"CC(=O)SC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"2.8"	"nM"	"8.55"	""	"352344"	"UO_0000065"	"25.96"	"0.51"	"5.39"	"11.26"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3967735"	""	"0"	"269.31"	"0"	"2.08"	"BDBM198271"	"O=C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	"352351"	"UO_0000065"	"29.05"	"0.53"	"5.74"	"10.30"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3891947"	""	"0"	"380.52"	"0"	"4.04"	"BDBM198299"	"Cc1ccc(CNC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)s1"	"IC50"	"'='"	"41.0"	"nM"	"7.39"	""	"352377"	"UO_0000065"	"19.41"	"0.37"	"3.35"	"10.42"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3951107"	""	"0"	"376.47"	"0"	"3.01"	"BDBM198379"	"N#CCCN(CCC#N)C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"1.9"	"nM"	"8.72"	""	"352457"	"UO_0000065"	"23.17"	"0.43"	"5.71"	"7.95"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3942304"	""	"0"	"496.23"	"0"	"4.57"	"BDBM198436"	"Brc1cc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)sc1Br"	"IC50"	"'='"	"71.0"	"nM"	"7.15"	""	"352514"	"UO_0000065"	"14.41"	"0.38"	"2.58"	"11.51"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3967749"	""	"0"	"417.34"	"0"	"3.81"	"BDBM198441"	"Brc1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)s1"	"IC50"	"'='"	"4.6"	"nM"	"8.34"	""	"352519"	"UO_0000065"	"19.98"	"0.46"	"4.53"	"13.42"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3941680"	""	"0"	"405.89"	"0"	"4.52"	"BDBM198466"	"N#Cc1cc(NC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)ccc1Cl"	"IC50"	"'='"	"220.0"	"nM"	"6.66"	""	"352544"	"UO_0000065"	"16.40"	"0.31"	"2.14"	"7.03"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3919050"	""	"0"	"390.49"	"0"	"3.68"	"BDBM198473"	"COc1ccc(CNC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"100.0"	"nM"	"7.00"	""	"352551"	"UO_0000065"	"17.93"	"0.33"	"3.32"	"8.74"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3939325"	""	"0"	"335.42"	"0"	"2.33"	"BDBM198484"	"N#CC1CN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C1"	"IC50"	"'='"	"50.0"	"nM"	"7.30"	""	"352562"	"UO_0000065"	"21.77"	"0.40"	"4.97"	"8.50"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3949461"	""	"0"	"324.43"	"0"	"3.02"	"BDBM198486"	"c1cc2c(ncn3nnc([C@H]4CC[C@H](CNC5CCC5)CC4)c23)[nH]1"	"IC50"	"'='"	"110.0"	"nM"	"6.96"	""	"352564"	"UO_0000065"	"21.45"	"0.40"	"3.94"	"9.81"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4106456"	""	"0"	"355.40"	"0"	"0.90"	"BDBM198491"	"O=C1NOC[C@H]1NC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"150.0"	"nM"	"6.82"	""	"352569"	"UO_0000065"	"19.20"	"0.36"	"5.92"	"6.25"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3903941"	""	"0"	"381.48"	"0"	"2.09"	"BDBM198522"	"CC(=O)N[C@H]1CCN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C1"	"IC50"	"'='"	"230.0"	"nM"	"6.64"	""	"352600"	"UO_0000065"	"17.40"	"0.32"	"4.55"	"7.28"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3931935"	""	"0"	"435.45"	"0"	"2.63"	"BDBM198524"	"O=C(N[C@H]1CCN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C1)C(F)(F)F"	"IC50"	"'='"	"210.0"	"nM"	"6.68"	""	"352602"	"UO_0000065"	"15.34"	"0.29"	"4.05"	"7.32"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645068"	""	"0"	"429.52"	"0"	"4.62"	"BDBM99836"	"COc1cccc(-c2cccn3nc(Nc4ccc(C5CCNCC5)cc4)nc23)c1OC"	"IC50"	"'='"	"58.04"	"nM"	"7.24"	""	"216509"	"UO_0000065"	"16.85"	"0.31"	"2.62"	"9.95"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652302"	""	"0"	"469.61"	"0"	"2.74"	"BDBM113111"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2C[C@@H](O)[C@H](c3ccccc3)C2)CC1"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	"234555"	"UO_0000065"	"16.66"	"0.32"	"5.08"	"7.64"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3652372"	""	"0"	"506.67"	"1"	"2.24"	"BDBM113183"	"CCN(CC)C(=O)CO[C@@H]1CCN(S(=O)(=O)C[C@H]2CC[C@H](N(C)c3ncnc4[nH]ccc34)CC2)C1"	"IC50"	"'='"	"35.9"	"nM"	"7.45"	""	"234626"	"UO_0000065"	"14.69"	"0.29"	"5.20"	"6.66"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3642264"	""	"0"	"384.36"	"1"	"5.17"	"BDBM99523"	"COc1ccccc1Nc1nc2c(-c3cccc(C(F)(F)F)c3)cccn2n1"	"IC50"	"'='"	"2999.0"	"nM"	"5.52"	""	"216215"	"UO_0000065"	"14.37"	"0.27"	"0.35"	"10.73"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652312"	""	"0"	"407.54"	"0"	"1.74"	"BDBM113122"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCC[C@@H](O)C2)CC1"	"IC50"	"'='"	"8.04"	"nM"	"8.10"	""	"234565"	"UO_0000065"	"19.86"	"0.39"	"6.35"	"7.90"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3330130"	""	"0"	"375.35"	"0"	"3.40"	"33"	"CCc1ccc(C(F)(F)F)cc1-c1[nH]c(-c2ccnc(N)n2)cc1C(N)=O"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	""	"UO_0000065"	"23.18"	"0.44"	"5.30"	"7.86"	"False"	"CHEMBL3374493"	"Inhibition of recombinant human JAK2 (808-1132 residues) using LPLDKDYYVVREPGQ as substrate by radiometric assay in presence of [33P]-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330123"	""	"0"	"343.77"	"0"	"2.48"	"26"	"COc1ccc(Cl)cc1-c1[nH]c(-c2ccnc(N)n2)cc1C(N)=O"	"IC50"	"'='"	"308.0"	"nM"	"6.51"	""	""	"UO_0000065"	"18.94"	"0.37"	"4.03"	"5.43"	"False"	"CHEMBL3374493"	"Inhibition of recombinant human JAK2 (808-1132 residues) using LPLDKDYYVVREPGQ as substrate by radiometric assay in presence of [33P]-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330108"	""	"0"	"384.87"	"0"	"2.63"	"11"	"CNCCNC(=O)c1cc(-c2ccnc(N)n2)[nH]c1-c1cc(Cl)ccc1C"	"IC50"	"'='"	"44.0"	"nM"	"7.36"	""	""	"UO_0000065"	"19.11"	"0.37"	"4.73"	"6.77"	"False"	"CHEMBL3374493"	"Inhibition of recombinant human JAK2 (808-1132 residues) using LPLDKDYYVVREPGQ as substrate by radiometric assay in presence of [33P]-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3702966"	""	"0"	"477.49"	"0"	"3.98"	"BDBM147673"	"N#C[C@@H]1C[C@H](OCC2CC2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc([C@@H](O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"19.0"	"nM"	"7.72"	""	"285605"	"UO_0000065"	"16.17"	"0.31"	"3.74"	"6.12"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4170168"	""	"0"	"546.64"	"1"	"4.58"	"10"	"N#CCNC(=O)c1ccc(-c2ccnc(Nc3ccc(N4CCC(C(=O)Nc5ccccc5N)CC4)cc3)n2)cc1"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	""	"UO_0000065"	"14.81"	"0.27"	"3.52"	"5.43"	"False"	"CHEMBL4150584"	"Inhibition of JAK2 (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition and measured after 25 mins in presence of ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4145634"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4168763"	""	"0"	"581.70"	"1"	"3.27"	"20e"	"CS(=O)(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCC(C(=O)NCCCCC(=O)NO)CC4)cc3)n2)cc1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	""	"UO_0000065"	"15.47"	"0.30"	"5.73"	"5.43"	"False"	"CHEMBL4150584"	"Inhibition of JAK2 (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition and measured after 25 mins in presence of ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4145634"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4159366"	""	"0"	"623.78"	"1"	"4.44"	"20h"	"CS(=O)(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCC(C(=O)NCCCCCCCC(=O)NO)CC4)cc3)n2)cc1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	""	"UO_0000065"	"13.95"	"0.27"	"4.26"	"5.25"	"False"	"CHEMBL4150584"	"Inhibition of JAK2 (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition and measured after 25 mins in presence of ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4145634"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4160840"	""	"0"	"391.43"	"0"	"2.84"	"24"	"O=C(NO)c1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"85.0"	"nM"	"7.07"	""	""	"UO_0000065"	"18.06"	"0.33"	"4.23"	"7.10"	"False"	"CHEMBL4150584"	"Inhibition of JAK2 (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition and measured after 25 mins in presence of ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4145634"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL1078178"	"MOMELOTINIB"	"3"	"414.47"	"0"	"2.98"	"1; CYT-387"	"N#CCNC(=O)c1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"41.0"	"nM"	"7.39"	""	""	"UO_0000065"	"17.82"	"0.33"	"4.41"	"7.16"	"False"	"CHEMBL4150584"	"Inhibition of JAK2 (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition and measured after 25 mins in presence of ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4145634"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3983127"	""	"0"	"277.28"	"0"	"2.90"	"BDBM198257"	"FC1(F)CCC(c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"120.0"	"nM"	"6.92"	""	"352339"	"UO_0000065"	"24.96"	"0.47"	"4.02"	"11.76"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3984424"	""	"0"	"257.30"	"0"	"1.62"	"BDBM198274"	"O[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"53.0"	"nM"	"7.28"	""	"352353"	"UO_0000065"	"28.28"	"0.52"	"5.66"	"9.20"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3908040"	""	"0"	"385.48"	"0"	"3.54"	"BDBM198286"	"N#Cc1ccc(CNC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"61.0"	"nM"	"7.21"	""	"352364"	"UO_0000065"	"18.72"	"0.34"	"3.67"	"7.62"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3984482"	""	"0"	"341.42"	"0"	"1.47"	"BDBM198338"	"c1cc2c(ncn3nnc([C@H]4CC[C@H](NN5CCOCC5)CC4)c23)[nH]1"	"IC50"	"'='"	"76.0"	"nM"	"7.12"	""	"352416"	"UO_0000065"	"20.85"	"0.39"	"5.65"	"8.54"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3907770"	""	"0"	"368.39"	"0"	"3.26"	"BDBM198363"	"Fc1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)c(F)c1"	"IC50"	"'='"	"30.0"	"nM"	"7.52"	""	"352441"	"UO_0000065"	"20.42"	"0.38"	"4.26"	"12.11"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645059"	""	"0"	"387.46"	"0"	"4.75"	"BDBM99827"	"Fc1ccc(-c2cccn3nc(Nc4ccc(C5CCNCC5)cc4)nc23)cc1"	"IC50"	"'='"	"8.12"	"nM"	"8.09"	""	"216500"	"UO_0000065"	"20.88"	"0.38"	"3.34"	"14.91"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3964008"	""	"0"	"412.40"	"0"	"3.31"	"BDBM198430"	"FC1(F)Oc2ccc(CN3CCC(c4nnn5cnc6[nH]ccc6c45)CC3)cc2O1"	"IC50"	"'='"	"21.0"	"nM"	"7.68"	""	"352508"	"UO_0000065"	"18.62"	"0.35"	"4.37"	"9.53"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3935688"	""	"0"	"298.39"	"0"	"2.44"	"BDBM198499"	"CN(C)C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"65.0"	"nM"	"7.19"	""	"352577"	"UO_0000065"	"24.09"	"0.45"	"4.75"	"11.57"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3644974"	""	"0"	"527.62"	"2"	"5.93"	"BDBM99724"	"COc1ccc(C(F)(F)F)cc1-c1cccc2nc(Nc3ccc4c(c3)CCN(CCSC)CC4)nn12"	"IC50"	"'='"	"26.69"	"nM"	"7.57"	""	"216414"	"UO_0000065"	"14.35"	"0.28"	"1.64"	"13.85"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL4109603"	""	"0"	"376.46"	"0"	"2.96"	"BDBM198406"	"O[C@H](CN[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1)c1ccccc1"	"IC50"	"'='"	"160.0"	"nM"	"6.80"	""	"352484"	"UO_0000065"	"18.05"	"0.33"	"3.84"	"7.46"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645041"	""	"0"	"488.57"	"0"	"3.78"	"BDBM99808"	"COc1cc(F)ccc1-c1cccn2nc(Nc3ccc4c(c3)CCN(CC(=O)N(C)C)CC4)nc12"	"IC50"	"'='"	"46.97"	"nM"	"7.33"	""	"216481"	"UO_0000065"	"15.00"	"0.28"	"3.55"	"9.77"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3648441"	""	"0"	"347.42"	"0"	"2.14"	"BDBM107150"	"O=C(CN1CCNCC1)Nc1cccc(-c2cnc3ccccc3n2)c1"	"IC50"	"'>'"	"20000.0"	"nM"	""	""	"226388"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL4111187"	""	"0"	"440.48"	"0"	"3.19"	"BDBM237789"	"CC(OC(=O)N1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@H](C#N)C1)C1CC1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"414893"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3652368"	""	"0"	"516.69"	"1"	"2.91"	"BDBM113179"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC[C@@](O)(CSc3ccccn3)C2)CC1"	"IC50"	"'='"	"13.1"	"nM"	"7.88"	""	"234622"	"UO_0000065"	"15.26"	"0.31"	"4.97"	"6.84"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3665199"	""	"0"	"513.63"	"1"	"1.34"	"BDBM112597"	"CS(=O)(=O)N1CCC[C@H](Nc2nc(N3CCC(CC(N)=O)CC3)ncc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.0221"	"nM"	"10.66"	""	"233834"	"UO_0000065"	"20.75"	"0.40"	"9.32"	"6.53"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3699501"	""	"0"	"344.35"	"0"	"1.49"	"BDBM147518"	"N#C[C@H]1C[C@H](O)CCC1n1cc(C(N)=O)c(Nc2ccnc(F)c2)n1"	"IC50"	"'='"	"210.0"	"nM"	"6.68"	""	"285593"	"UO_0000065"	"19.39"	"0.36"	"5.19"	"5.14"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4111481"	""	"0"	"476.51"	"0"	"3.63"	"BDBM237769"	"N#C[C@@H]1CN(C(=O)OCCc2ccccc2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"414873"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3940537"	""	"0"	"469.57"	"0"	"2.94"	"16h"	"Cc1cnc(Nc2ccc(N3CCOCC3)cc2)nc1-c1cc2c(o1)CCN(S(C)(=O)=O)C2"	"IC50"	"'='"	"0.7"	"nM"	"9.15"	""	""	"UO_0000065"	"19.50"	"0.38"	"6.21"	"9.08"	"False"	"CHEMBL3868063"	"Inhibition of GST-tagged recombinant human JAK2 expressed in baculovirus using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3867460"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2017"	"None"	""
"CHEMBL3652387"	""	"0"	"436.54"	"0"	"1.32"	"BDBM113199"	"COC(=O)NC1CN(S(=O)(=O)C[C@H]2CC[C@H](N(C)c3ncnc4[nH]ccc34)CC2)C1"	"IC50"	"'='"	"32.4"	"nM"	"7.49"	""	"234642"	"UO_0000065"	"17.16"	"0.34"	"6.17"	"6.21"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3647863"	""	"0"	"395.46"	"0"	"2.24"	"BDBM147974"	"CC1(c2ccc(Nc3nn([C@H]4CC[C@H](O)C[C@@H]4C#N)cc3C(N)=O)cc2)COC1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"285908"	"UO_0000065"	"21.24"	"0.40"	"6.16"	"6.65"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647906"	""	"0"	"444.90"	"0"	"3.04"	"BDBM148018"	"N#C[C@@H]1C[C@H](C(=O)N2CC(F)C2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"200.0"	"nM"	"6.70"	""	"285953"	"UO_0000065"	"15.06"	"0.30"	"3.66"	"5.72"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4112603"	""	"0"	"468.41"	"0"	"3.34"	"BDBM237764"	"CC(OC(=O)N1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@H](C#N)C1)C(F)(F)F"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"414868"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3647865"	""	"0"	"399.47"	"0"	"3.20"	"BDBM147976"	"CC(C)(CF)c1ccc(Nc2nn([C@H]3CC[C@H](O)C[C@@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"285910"	"UO_0000065"	"20.58"	"0.39"	"5.02"	"7.03"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3622924"	""	"0"	"377.49"	"0"	"3.50"	"5"	"Cc1cc(C)cc(Nc2nccc(-n3cc(C)c(CN4CC[C@@H](O)C4)c3)n2)c1"	"IC50"	"'='"	"115300.0"	"nM"	""	"Outside typical range"	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3627021"	"Inhibition of human JAK2 pre-incubated for 30 mins at room temperature before substrate addition and measured 1 hr after substrate addition by cell free kinase assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621069"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3120995"	""	"0"	"440.44"	"0"	"4.23"	"2"	"Cn1c(-c2cn(-c3ccc(C(=O)O)cc3)nn2)nc(-c2ccc(F)cc2)c1-c1ccncc1"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3363474"	"Inhibition of JAK2 (unknown origin) by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352554"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3120983"	""	"0"	"440.44"	"0"	"4.23"	"3"	"Cn1c(-c2cn(-c3cccc(C(=O)O)c3)nn2)nc(-c2ccc(F)cc2)c1-c1ccncc1"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3363474"	"Inhibition of JAK2 (unknown origin) by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352554"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3918568"	""	"0"	"585.04"	"2"	"5.42"	"BDBM230086"	"Cc1c(-c2c(Cl)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)c2cc(F)ccc2n(C)c1=O"	"IC50"	"'>'"	"2000.0"	"nM"	""	""	"402019"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3928976"	""	"0"	"587.46"	"2"	"5.69"	"BDBM230151"	"Cc1c(-c2c(Cl)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)cc2c(Cl)cccn2c1=O"	"IC50"	"'='"	"970.0"	"nM"	"6.01"	""	"402044"	"UO_0000065"	"10.24"	"0.20"	"0.32"	"4.91"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3954590"	""	"0"	"587.46"	"2"	"5.62"	"BDBM230113"	"Cn1c(=O)n(-c2cccc(-c3c(Cl)cc(C(N)=O)c4[nH]c5cc(C(C)(C)O)ccc5c34)c2Cl)c(=O)c2ccccc21"	"IC50"	"'='"	"2000.0"	"nM"	"5.70"	""	"402054"	"UO_0000065"	"9.70"	"0.19"	"0.08"	"4.63"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3908440"	""	"0"	"571.01"	"2"	"5.41"	"BDBM230124"	"Cc1c(-c2c(F)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)[nH]c2c(Cl)cccc2c1=O"	"IC50"	"'='"	"1200.0"	"nM"	"5.92"	""	"402065"	"UO_0000065"	"10.37"	"0.20"	"0.51"	"4.42"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3910427"	""	"0"	"593.03"	"2"	"5.04"	"BDBM230128"	"Cc1c(-c2c(Cl)cc(C(N)=O)c3[nH]c4c(c23)CC[C@H](C(C)(C)O)C4)cccc1-n1c(=O)[nH]c2c(F)cc(F)cc2c1=O"	"IC50"	"'='"	"270.0"	"nM"	"6.57"	""	"402068"	"UO_0000065"	"11.08"	"0.21"	"1.53"	"4.90"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3951540"	""	"0"	"607.06"	"2"	"5.05"	"BDBM230155"	"Cc1c(-c2c(Cl)cc(C(N)=O)c3[nH]c4c(c23)CC[C@H](C(C)(C)O)C4)cccc1-n1c(=O)c2cc(F)cc(F)c2n(C)c1=O"	"IC50"	"'='"	"13000.0"	"nM"	"4.89"	""	"402069"	"UO_0000065"	"8.05"	"0.16"	"-0.16"	"3.97"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3955854"	""	"0"	"575.04"	"1"	"4.90"	"BDBM230132"	"Cc1c(-c2c(F)cc(C(N)=O)c3[nH]c4c(c23)CC[C@H](C(C)(C)O)C4)cccc1-n1c(=O)[nH]c2c(Cl)cccc2c1=O"	"IC50"	"'='"	"11000.0"	"nM"	"4.96"	""	"402074"	"UO_0000065"	"8.62"	"0.17"	"0.06"	"3.70"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3966840"	""	"0"	"326.40"	"0"	"1.56"	"BDBM198460"	"OC1CN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C1"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	"352538"	"UO_0000065"	"23.88"	"0.44"	"6.24"	"9.47"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3913953"	""	"0"	"611.69"	"2"	"5.41"	"2"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(-c4ccc5ncccc5c4)c(F)c3)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3639466"	""	"0"	"448.45"	"0"	"2.97"	"BDBM147933"	"N#C[C@@H]1C[C@@H](NC2COC2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	"285867"	"UO_0000065"	"17.33"	"0.33"	"4.80"	"6.58"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647792"	""	"0"	"456.98"	"0"	"3.58"	"BDBM147895"	"CN(CC1(C)COC1)[C@H]1CCC(n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	"285829"	"UO_0000065"	"17.42"	"0.34"	"4.38"	"7.29"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647727"	""	"0"	"512.51"	"1"	"1.93"	"BDBM147829"	"N#C[C@H]1C[C@H](N2CC(O)C2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"285763"	"UO_0000065"	"16.97"	"0.34"	"6.77"	"5.64"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3892350"	""	"0"	"414.90"	"0"	"2.48"	"BDBM239972"	"Cc1cc(Nc2ncc(Cl)c(NC3CC4CN(C(=O)CC#N)CC4C3)n2)nn1C"	"IC50"	"'='"	"30.0"	"nM"	"7.52"	""	"418592"	"UO_0000065"	"18.13"	"0.35"	"5.04"	"6.73"	"False"	"CHEMBL3888834"	"Kinase Assay: JAK2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 100 μM KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC, 10 mM MgAcetate and [γ-33P-ATP](specific activity approx. 500 cpm/pmol, concentration as required). The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of 3% phosphoric acid solution. 10 μL of the reaction is then spotted onto a P30 filtermat and washed three times for 5 minutes in 75 mM phosphoric acid and once in methanol prior to drying and scintillation counting."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886854"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3906618"	""	"0"	"451.48"	"0"	"3.30"	"BDBM229100"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2ccc(F)cc2)CC1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"400836"	"UO_0000065"	"18.60"	"0.35"	"5.10"	"7.44"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3946078"	""	"0"	"459.51"	"0"	"3.28"	"BDBM229366"	"CCOc1ccc(NC(=O)N2CC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)C2)cc1"	"IC50"	"'='"	"69.0"	"nM"	"7.16"	""	"401105"	"UO_0000065"	"15.58"	"0.29"	"3.88"	"5.18"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3652337"	""	"0"	"484.65"	"0"	"1.28"	"BDBM113148"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCC[C@H](CS(N)(=O)=O)C2)CC1"	"IC50"	"'='"	"22.0"	"nM"	"7.66"	""	"234591"	"UO_0000065"	"15.80"	"0.33"	"6.38"	"5.38"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3703062"	""	"0"	"476.50"	"0"	"4.25"	"BDBM147772"	"C[C@H](N[C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(OC(F)(F)F)cc3)n2)[C@@H](C#N)C1)C1CC1"	"IC50"	"'='"	"65.0"	"nM"	"7.19"	""	"285706"	"UO_0000065"	"15.08"	"0.29"	"2.94"	"6.09"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647835"	""	"0"	"479.50"	"0"	"3.54"	"BDBM147942"	"CC(C)(c1ccc(Nc2nn([C@H]3CC[C@](C)(O)C[C@@H]3C#N)cc2C(N)=O)cc1)C(O)C(F)(F)F"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"285876"	"UO_0000065"	"17.77"	"0.34"	"4.98"	"6.21"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642367"	""	"0"	"520.66"	"1"	"3.44"	"BDBM99643"	"CC(C)(O)CN1CCN(c2cccc(Nc3nc4c(-c5ccc(S(C)(=O)=O)cc5)cccn4n3)c2)CC1"	"IC50"	"'='"	"2.61"	"nM"	"8.58"	""	"216333"	"UO_0000065"	"16.49"	"0.32"	"5.14"	"8.33"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652362"	""	"0"	"469.61"	"0"	"2.88"	"BDBM113173"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC[C@@](O)(c3ccccc3)C2)CC1"	"IC50"	"'='"	"10.8"	"nM"	"7.97"	""	"234616"	"UO_0000065"	"16.96"	"0.33"	"5.09"	"7.78"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3647880"	""	"0"	"442.91"	"0"	"2.37"	"BDBM147992"	"N#C[C@H]1C[C@@H](C(=O)NC2COC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"243.0"	"nM"	"6.61"	""	"285927"	"UO_0000065"	"14.93"	"0.29"	"4.24"	"4.90"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702946"	""	"0"	"394.36"	"0"	"2.37"	"BDBM147648"	"N#C[C@H]1C[C@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)nc2)n1"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	"285580"	"UO_0000065"	"19.70"	"0.38"	"5.40"	"5.98"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642320"	""	"0"	"394.46"	"0"	"3.55"	"BDBM99592"	"COc1ccc(Nc2nc3cccc(-c4ccc(S(C)(=O)=O)cc4)n3n2)cc1"	"IC50"	"'='"	"1.9"	"nM"	"8.72"	""	"216282"	"UO_0000065"	"22.11"	"0.43"	"5.17"	"10.19"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3645107"	""	"0"	"346.39"	"0"	"3.49"	"BDBM99881"	"COc1ccccc1CNc1cccn2nc(Nc3cccnc3)nc12"	"IC50"	"'='"	"32.27"	"nM"	"7.49"	""	"216549"	"UO_0000065"	"21.63"	"0.39"	"4.00"	"9.81"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703084"	""	"0"	"413.43"	"0"	"2.69"	"BDBM147797"	"N#Cc1ccc(Nc2nn([C@H]3CC[C@H](NCC(F)F)C[C@@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"285731"	"UO_0000065"	"19.46"	"0.37"	"5.36"	"6.07"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699481"	""	"0"	"370.43"	"0"	"2.66"	"BDBM147496"	"CN(C)[C@H]1CC[C@H](C#N)[C@@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)C1"	"IC50"	"'>'"	"1500.0"	"nM"	""	""	"285422"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642283"	""	"0"	"662.51"	"2"	"5.68"	"BDBM99547"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4ccc(OS(=O)(=O)C(F)(F)C(F)(F)C(F)(F)C(F)(F)F)cc4)nc23)cc1"	"IC50"	"'='"	"106.1"	"nM"	"6.97"	""	"216239"	"UO_0000065"	"10.53"	"0.22"	"1.29"	"5.83"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703034"	""	"0"	"476.50"	"0"	"3.43"	"BDBM147744"	"C[C@](O)(c1ccc(Nc2nn([C@H]3CC[C@@H](N4CCC4)C[C@@H]3C#N)cc2C(N)=O)cc1)C(F)(F)F"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	"285678"	"UO_0000065"	"16.99"	"0.33"	"4.67"	"6.74"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL570464"	""	"0"	"329.34"	"0"	"2.66"	"7p"	"COc1cc(Nc2cncc(N[C@@H](C)c3ccc(F)cn3)n2)n[nH]1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"25.88"	"0.48"	"5.86"	"8.47"	"False"	"CHEMBL1043451"	"Inhibition of JAK2 using 2 mM ATP as a substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156131"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL3651044"	""	"0"	"372.40"	"0"	"4.95"	"BDBM153221"	"C=C(C)C(=O)Nc1cccc(-c2ncnc3[nH]cc(-c4cccc(F)c4)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294169"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3644963"	""	"0"	"372.35"	"0"	"4.38"	"BDBM99713"	"CCn1cc(Nc2nc3c(-c4ccc(C(F)(F)F)cc4)cccn3n2)cn1"	"IC50"	"'='"	"2.84"	"nM"	"8.55"	""	"216403"	"UO_0000065"	"22.95"	"0.43"	"4.17"	"14.23"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3658863"	""	"0"	"384.45"	"0"	"2.63"	"BDBM159782"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](CS(=O)(=O)CC2CC(F)(F)C2)C1"	"IC50"	"'='"	"161.0"	"nM"	"6.79"	""	"302592"	"UO_0000065"	"17.67"	"0.36"	"4.16"	"8.60"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665133"	""	"0"	"372.45"	"0"	"1.86"	"BDBM112520"	"CCS(=O)(=O)N1CC[C@@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.2469"	"nM"	"9.61"	""	"233759"	"UO_0000065"	"25.80"	"0.50"	"7.75"	"9.25"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3335698"	""	"0"	"458.55"	"0"	"1.09"	"27"	"CS(=O)(=O)N1CCC[C@H](Nc2nc(N3CCOCC3)ncc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"102.0"	"nM"	"6.99"	""	""	"UO_0000065"	"15.25"	"0.30"	"5.90"	"5.41"	"False"	"CHEMBL3374010"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 1 hr in presence of [gamma-33P]ATP by scintillation counting analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351377"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3703101"	""	"0"	"404.52"	"0"	"3.44"	"BDBM147816"	"N#C[C@H]1C[C@@H](N2CC3(CCC3)C2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccccc2)n1"	"IC50"	"'='"	"61.0"	"nM"	"7.21"	""	"285750"	"UO_0000065"	"17.84"	"0.33"	"3.77"	"7.22"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3360356"	""	"0"	"411.46"	"0"	"3.98"	"BDBM103737"	"O=C(Nc1nc2cccc(-c3ccc(CN4CCC(F)(F)CC4)cc3)n2n1)C1CC1"	"IC50"	"'='"	"15.51"	"nM"	"7.81"	""	"221723"	"UO_0000065"	"18.98"	"0.36"	"3.83"	"12.49"	"False"	"CHEMBL3707887"	"Inhibition Assay: In vitro inhibition assay using various enzyme."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638964"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3417186"	""	"0"	"487.60"	"1"	"5.09"	"31"	"O=C(CCCCCN1C/C=C/CCOc2cccc(c2)-c2ccnc(n2)Nc2cccc(c2)C1)NO"	"IC50"	"'='"	"1044.0"	"nM"	"5.98"	""	""	"UO_0000065"	"12.27"	"0.23"	"0.89"	"6.00"	"False"	"CHEMBL3419812"	"Inhibition of human recombinant JAK2 using Z'LYTETry6 peptide substrate after 1 hr by microplate reader"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3414525"	"1"	"Scientific Literature"	"Eur. J. Med. Chem."	"2015"	"None"	""
"CHEMBL3647798"	""	"0"	"440.86"	"0"	"3.76"	"BDBM147901"	"N#C[C@H]1C[C@H](NCC(F)(F)F)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"51.0"	"nM"	"7.29"	""	"285835"	"UO_0000065"	"16.54"	"0.33"	"3.53"	"6.71"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645010"	""	"0"	"468.48"	"1"	"5.03"	"BDBM99762"	"COc1ncc(C(F)(F)F)cc1-c1cccn2nc(Nc3ccc(C4CCNCC4)cc3)nc12"	"IC50"	"'='"	"132.71"	"nM"	"6.88"	""	"216449"	"UO_0000065"	"14.68"	"0.28"	"1.85"	"9.00"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647731"	""	"0"	"512.51"	"1"	"2.24"	"BDBM147834"	"N#C[C@H]1CC(NC2COC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"285768"	"UO_0000065"	"16.63"	"0.33"	"6.28"	"5.60"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651024"	""	"0"	"413.44"	"0"	"3.85"	"BDBM153201"	"CCOC(=O)c1c[nH]c2ncnc(-c3cccc(NC(=O)/C=C/c4ccncc4)c3)c12"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294149"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703092"	""	"0"	"386.89"	"0"	"3.17"	"BDBM147806"	"CN(C)[C@@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"72.0"	"nM"	"7.14"	""	"285740"	"UO_0000065"	"18.46"	"0.36"	"3.97"	"7.14"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3605102"	""	"0"	"398.49"	"1"	"5.74"	"14b"	"Cn1cc(-c2cnc(N)c3c(-c4ccc(Oc5ccccc5)cc4)csc23)cn1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3607493"	"Inhibition of JAK2 (unknown origin) using poly (Glu-Tyr, 4:1) substrate incubated for 60 mins by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3603780"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3403548"	""	"0"	"395.77"	"0"	"3.75"	"21"	"CNc1cc(-c2cc(C(N)=O)n(-c3cc(C(F)(F)F)ccc3Cl)c2)ncn1"	"IC50"	"'='"	"331.0"	"nM"	"6.48"	""	""	"UO_0000065"	"16.37"	"0.33"	"2.73"	"7.55"	"False"	"CHEMBL3404501"	"Inhibition of recombinant epitope-tagged JAK2 (808 to 1132) (unknown origin) using LPLDKDYYVVREPGQ as substrate by beta-countiing analysis in presence of 33P-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3400063"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3403543"	""	"0"	"341.80"	"0"	"2.83"	"16, NMS-P830"	"CCc1ccc(Cl)cc1-n1cc(-c2cc(N)ncn2)cc1C(N)=O"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	""	"UO_0000065"	"23.69"	"0.46"	"5.27"	"8.11"	"False"	"CHEMBL3404501"	"Inhibition of recombinant epitope-tagged JAK2 (808 to 1132) (unknown origin) using LPLDKDYYVVREPGQ as substrate by beta-countiing analysis in presence of 33P-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3400063"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3403542"	""	"0"	"351.80"	"0"	"3.25"	"15"	"Cc1ccc(Cl)cc1-n1cc(-c2ncnn3cccc23)cc1C(N)=O"	"IC50"	"'='"	"68.0"	"nM"	"7.17"	""	""	"UO_0000065"	"20.37"	"0.39"	"3.92"	"9.16"	"False"	"CHEMBL3404501"	"Inhibition of recombinant epitope-tagged JAK2 (808 to 1132) (unknown origin) using LPLDKDYYVVREPGQ as substrate by beta-countiing analysis in presence of 33P-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3400063"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3403538"	""	"0"	"351.80"	"0"	"3.25"	"11"	"Cc1ccc(Cl)cc1-c1cn(-c2ncnn3cccc23)cc1C(N)=O"	"IC50"	"'='"	"2910.0"	"nM"	"5.54"	""	""	"UO_0000065"	"15.74"	"0.30"	"2.29"	"7.08"	"False"	"CHEMBL3404501"	"Inhibition of recombinant epitope-tagged JAK2 (808 to 1132) (unknown origin) using LPLDKDYYVVREPGQ as substrate by beta-countiing analysis in presence of 33P-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3400063"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL1945559"	""	"0"	"363.25"	"0"	"2.96"	"20"	"Cn1c2c(c3ccc(Cl)c(Cl)c31)C(C#N)C1(CCNCC1)NC2=O"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1948127"	"Inhibition of JAK2 using ATP as substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944596"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL3605107"	""	"0"	"455.54"	"0"	"4.95"	"14g"	"CNC(=O)Cn1cc(-c2cnc(N)c3c(-c4ccc(Oc5ccccc5)cc4)csc23)cn1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3607493"	"Inhibition of JAK2 (unknown origin) using poly (Glu-Tyr, 4:1) substrate incubated for 60 mins by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3603780"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL1929238"	""	"0"	"554.54"	"2"	"5.23"	"27"	"CN(C)CCN1CCN(C(=O)c2cc(C(C)(C)C)sc2NC(=O)Nc2cccc(Cl)c2Cl)CCC1=O"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1932879"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1926590"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL3699524"	""	"0"	"328.35"	"0"	"2.51"	"BDBM147542"	"N#C[C@@H]1CCCC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)nc2)n1"	"IC50"	"'='"	"55.0"	"nM"	"7.26"	""	"285472"	"UO_0000065"	"22.11"	"0.41"	"4.75"	"6.62"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3314270"	""	"0"	"482.47"	"1"	"0.52"	"5"	"Cn1c(-c2cn([C@H]3[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]3O)nn2)nc(-c2ccc(F)cc2)c1-c1ccncc1"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3363474"	"Inhibition of JAK2 (unknown origin) by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352554"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3314271"	""	"0"	"352.40"	"0"	"3.30"	"11"	"CSc1nccc(-c2c(-c3ccc(F)cc3)nc3nc(N)ccn23)n1"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3363474"	"Inhibition of JAK2 (unknown origin) by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352554"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3314274"	""	"0"	"568.58"	"3"	"5.24"	"16"	"CCOP(=O)(CCn1cc(-c2ccn3c(-c4ccnc(SC)n4)c(-c4ccc(F)cc4)nc3n2)nn1)OCC"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3363474"	"Inhibition of JAK2 (unknown origin) by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352554"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3314282"	""	"0"	"413.34"	"0"	"3.64"	"27.Na"	"O=C([O-])c1cc(-c2nc(-c3ccc(F)cc3)c(-c3cc[nH]c(=O)c3)[nH]2)ccc1O.[Na+]"	"IC50"	"'='"	"3710.0"	"nM"	"5.43"	""	""	"UO_0000065"	"13.88"	"0.26"	"1.79"	"4.56"	"False"	"CHEMBL3363474"	"Inhibition of JAK2 (unknown origin) by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352554"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3645071"	""	"0"	"394.48"	"0"	"4.48"	"BDBM99839"	"N#Cc1ccc(-c2cccn3nc(Nc4ccc(C5CCNCC5)cc4)nc23)cc1"	"IC50"	"'='"	"5.81"	"nM"	"8.24"	""	"216512"	"UO_0000065"	"20.88"	"0.37"	"3.76"	"10.55"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647751"	""	"0"	"564.63"	"1"	"4.37"	"BDBM147854"	"CN(C(C1CC1)C1CC1)[C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"285788"	"UO_0000065"	"15.41"	"0.30"	"4.33"	"6.49"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642292"	""	"0"	"414.51"	"0"	"3.90"	"BDBM99558"	"COc1ccccc1-c1cccn2nc(Nc3cccc(N4CCN(C)CC4)c3)nc12"	"IC50"	"'='"	"26.8"	"nM"	"7.57"	""	"216249"	"UO_0000065"	"18.27"	"0.33"	"3.67"	"13.07"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL1572928"	""	"0"	"315.33"	"0"	"4.14"	"BDBM107127"	"O=C(Nc1cccc(-c2cnc3ccccc3n2)c1)c1ccco1"	"IC50"	"'='"	"24580.0"	"nM"	"4.61"	""	"226365"	"UO_0000065"	"14.62"	"0.26"	"0.47"	"6.78"	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3645075"	""	"0"	"512.66"	"2"	"6.32"	"BDBM99843"	"CN(C)c1cccc(-c2cccn3nc(Nc4ccc(C5CCN(C(=O)OC(C)(C)C)CC5)cc4)nc23)c1"	"IC50"	"'='"	"193.08"	"nM"	"6.71"	""	"216516"	"UO_0000065"	"13.10"	"0.24"	"0.39"	"8.95"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647844"	""	"0"	"399.88"	"0"	"3.38"	"BDBM147953"	"N#C[C@H]1C[C@@](O)(C2CC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"73.0"	"nM"	"7.14"	""	"285887"	"UO_0000065"	"17.85"	"0.35"	"3.76"	"6.10"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652303"	""	"0"	"407.54"	"0"	"1.60"	"BDBM113112"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC[C@@H](CO)C2)CC1"	"IC50"	"'='"	"8.36"	"nM"	"8.08"	""	"234556"	"UO_0000065"	"19.82"	"0.39"	"6.48"	"7.89"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3335684"	""	"0"	"366.45"	"0"	"1.28"	"11"	"CCCS(=O)(=O)N1CCC[C@H](NC(=O)Nc2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"78.0"	"nM"	"7.11"	""	""	"UO_0000065"	"19.40"	"0.39"	"5.83"	"5.92"	"False"	"CHEMBL3374010"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 1 hr in presence of [gamma-33P]ATP by scintillation counting analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351377"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3335688"	""	"0"	"372.45"	"0"	"1.86"	"16"	"CS(=O)(=O)N1CCC[C@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"82.0"	"nM"	"7.09"	""	""	"UO_0000065"	"19.03"	"0.37"	"5.23"	"6.82"	"False"	"CHEMBL3374010"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 1 hr in presence of [gamma-33P]ATP by scintillation counting analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351377"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3335689"	""	"0"	"414.54"	"0"	"2.88"	"19"	"CC(C)CS(=O)(=O)N1CCC[C@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"108.0"	"nM"	"6.97"	""	""	"UO_0000065"	"16.81"	"0.33"	"4.09"	"6.71"	"False"	"CHEMBL3374010"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 1 hr in presence of [gamma-33P]ATP by scintillation counting analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351377"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3650987"	""	"0"	"381.39"	"0"	"2.72"	"BDBM153162"	"C=C(C)C(=O)Nc1cc(-c2ncnc3[nH]cc(C(=O)OCC)c23)cc(OC)n1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294110"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647802"	""	"0"	"455.01"	"0"	"4.73"	"BDBM147905"	"CN([C@H]1CCC(n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@@H](C#N)C1)C(C)(C)C1CC1"	"IC50"	"'='"	"38.0"	"nM"	"7.42"	""	"285839"	"UO_0000065"	"16.31"	"0.32"	"2.69"	"7.42"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651017"	""	"0"	"415.25"	"0"	"3.65"	"BDBM153194"	"C=C(Br)C(=O)Nc1cccc(-c2ncnc3[nH]cc(C(=O)OCC)c23)c1"	"IC50"	"'='"	"892.0"	"nM"	"6.05"	""	"294142"	"UO_0000065"	"14.57"	"0.32"	"2.40"	"6.24"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652281"	""	"0"	"464.59"	"0"	"1.25"	"BDBM113089"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCCC(OCC(N)=O)C2)CC1"	"IC50"	"'='"	"18.3"	"nM"	"7.74"	""	"234533"	"UO_0000065"	"16.65"	"0.33"	"6.49"	"5.75"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3645014"	""	"0"	"453.53"	"0"	"4.93"	"BDBM99766"	"Fc1ccc(-n2cc(-c3cccn4nc(Nc5ccc(C6CCNCC6)cc5)nc34)cn2)cc1"	"IC50"	"'='"	"2.12"	"nM"	"8.67"	""	"216453"	"UO_0000065"	"19.12"	"0.35"	"3.74"	"12.04"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3650995"	""	"0"	"370.80"	"0"	"3.58"	"BDBM153170"	"C=CC(=O)Nc1cc(-c2ncnc3[nH]cc(C(=O)OCC)c23)ccc1Cl"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294118"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702915"	""	"0"	"515.60"	"1"	"4.33"	"BDBM147614"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)Nc3ccc4cccnc4c3)cc2)n1"	"IC50"	"'='"	"33.0"	"nM"	"7.48"	""	"285544"	"UO_0000065"	"14.51"	"0.28"	"3.15"	"4.80"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703046"	""	"0"	"450.54"	"0"	"3.03"	"BDBM147756"	"CC(C)(C(=O)O)c1ccc(Nc2nn([C@H]3CCC(N4CCC4)C[C@@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"98.0"	"nM"	"7.01"	""	"285690"	"UO_0000065"	"15.56"	"0.29"	"3.98"	"5.11"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665126"	""	"0"	"322.37"	"0"	"2.05"	"BDBM112513"	"CC(=O)N1CC[C@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.0397"	"nM"	"10.40"	""	"233752"	"UO_0000065"	"32.26"	"0.59"	"8.35"	"11.98"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3665141"	""	"0"	"386.48"	"0"	"2.10"	"BDBM112528"	"C[C@H]1C[C@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)CN(S(C)(=O)=O)C1"	"IC50"	"'='"	"0.1401"	"nM"	"9.85"	""	"233767"	"UO_0000065"	"25.50"	"0.50"	"7.75"	"9.49"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3658108"	""	"0"	"630.68"	"2"	"5.15"	"BDBM148406"	"Cc1ccc(NC(=O)c2cccc(C(F)(F)F)c2)cc1N1CCc2nc(Nc3ccc(C(=O)N4CCN(C)CC4)nc3)ncc2C1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"286794"	"UO_0000065"	"13.51"	"0.25"	"3.37"	"8.00"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL388978"	"STAUROSPORINE"	"0"	"466.54"	"0"	"4.35"	"Staurosporine"	"CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4c(c5c6ccccc6n2c5c31)C(=O)NC4"	"IC50"	"'='"	"2.3"	"nM"	"8.64"	""	""	"UO_0000065"	"18.52"	"0.34"	"4.29"	"12.44"	"False"	"CHEMBL3398955"	"Inhibition of N-terminal His-tagged recombinant JAK2 (unknown origin) by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3397021"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3645077"	""	"0"	"412.54"	"0"	"4.67"	"BDBM99845"	"CN(C)c1cccc(-c2cccn3nc(Nc4ccc(C5CCNCC5)cc4)nc23)c1"	"IC50"	"'='"	"3.93"	"nM"	"8.41"	""	"216518"	"UO_0000065"	"20.38"	"0.37"	"3.74"	"14.62"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3640018"	""	"0"	"356.41"	"0"	"2.32"	"BDBM147678"	"CN[C@@H]1CCC(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"25.0"	"nM"	"7.60"	""	"285611"	"UO_0000065"	"21.33"	"0.40"	"5.28"	"6.99"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642293"	""	"0"	"462.58"	"0"	"3.30"	"BDBM99561"	"CN1CCN(c2ccc(Nc3nc4c(-c5cccc(S(C)(=O)=O)c5)cccn4n3)cc2)CC1"	"IC50"	"'='"	"3.3"	"nM"	"8.48"	""	"216251"	"UO_0000065"	"18.34"	"0.35"	"5.18"	"10.24"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642391"	""	"0"	"484.63"	"0"	"2.06"	"BDBM99669"	"CN1CCN(c2ccc(Nc3nc4c(NCC5CCCN5S(C)(=O)=O)cccn4n3)cc2)CC1"	"IC50"	"'='"	"11.63"	"nM"	"7.93"	""	"216359"	"UO_0000065"	"16.37"	"0.32"	"5.87"	"8.09"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3665128"	""	"0"	"358.43"	"0"	"1.47"	"BDBM112515"	"CS(=O)(=O)N1CC[C@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.0108"	"nM"	"10.97"	""	"233754"	"UO_0000065"	"30.60"	"0.60"	"9.50"	"10.56"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL2062798"	""	"0"	"394.46"	"0"	"3.55"	"BDBM99542"	"COc1cccc(Nc2nc3c(-c4ccc(S(C)(=O)=O)cc4)cccn3n2)c1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"216234"	"UO_0000065"	"22.82"	"0.44"	"5.45"	"10.52"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3645052"	""	"0"	"552.60"	"2"	"5.43"	"BDBM99819"	"COc1ccc(C(F)(F)F)cc1-c1cccn2nc(Nc3ccc(C4CCN(CC(=O)N(C)C)CC4)cc3)nc12"	"IC50"	"'='"	"59.74"	"nM"	"7.22"	""	"216492"	"UO_0000065"	"13.07"	"0.25"	"1.79"	"9.63"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3699508"	""	"0"	"344.81"	"0"	"3.03"	"BDBM147526"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccnc(Cl)c2)n1"	"IC50"	"'='"	"31.0"	"nM"	"7.51"	""	"285456"	"UO_0000065"	"21.78"	"0.43"	"4.48"	"6.85"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3639569"	""	"0"	"581.00"	"2"	"6.07"	"BDBM148445"	"CNC(=O)c1ccc(Nc2ncc3c(n2)CCN(c2cc(NC(=O)c4cccc(C(F)(F)F)c4)ccc2Cl)C3)cc1"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	"286808"	"UO_0000065"	"13.47"	"0.26"	"1.75"	"7.88"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL1995703"	""	"0"	"509.68"	"1"	"4.10"	"105"	"Cc1cnc(Nc2ccc(N3CCN(C)CC3)cc2)nc1Nc1cccc(S(=O)(=O)NC(C)(C)C)c1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	""	"UO_0000065"	"16.13"	"0.31"	"4.12"	"8.02"	"True"	"CHEMBL4043457"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4043066"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4109514"	""	"0"	"469.52"	"0"	"2.48"	"BDBM237740"	"N#C[C@@H]1CN(C(=O)OCCN2CCCC2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"1101.0"	"nM"	"5.96"	""	"414844"	"UO_0000065"	"12.69"	"0.24"	"3.48"	"4.60"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4108369"	""	"0"	"485.56"	"0"	"2.98"	"BDBM237742"	"CN(C)CC(C)(C)COC(=O)N1CC[C@@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@H](C#N)C1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"414846"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4111925"	""	"0"	"400.41"	"0"	"2.41"	"BDBM237744"	"CCOC(=O)N1CC[C@@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@H](C#N)C1"	"IC50"	"'='"	"158.0"	"nM"	"6.80"	""	"414848"	"UO_0000065"	"16.99"	"0.32"	"4.39"	"5.39"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3984300"	""	"0"	"549.43"	"1"	"3.12"	"BDBM229009"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(C(O)C(F)(F)F)nc3)n2)CCN(C(=O)OCC(F)(F)F)CC1"	"IC50"	"'='"	"0.6"	"nM"	"9.22"	""	"400754"	"UO_0000065"	"16.78"	"0.33"	"6.10"	"5.79"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3950086"	""	"0"	"447.52"	"0"	"3.79"	"BDBM228906"	"Cc1cc(N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)CC2)cnc1C"	"IC50"	"'='"	"49.0"	"nM"	"7.31"	""	"400653"	"UO_0000065"	"16.33"	"0.30"	"3.52"	"6.48"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3900321"	""	"0"	"433.49"	"0"	"3.48"	"BDBM228925"	"Cc1ccncc1N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CC1"	"IC50"	"'='"	"102.0"	"nM"	"6.99"	""	"400672"	"UO_0000065"	"16.13"	"0.30"	"3.51"	"6.19"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3953347"	""	"0"	"467.51"	"0"	"3.38"	"BDBM228991"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(C#N)c(F)c3)n2)CC1"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"400736"	"UO_0000065"	"17.44"	"0.33"	"4.77"	"5.43"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3901465"	""	"0"	"506.57"	"1"	"3.72"	"BDBM228997"	"Cc1nc(-c2ccc(Nc3nn(C4(CC#N)CCN(C(=O)OC(C)(C)C)CC4)cc3C(N)=O)cc2)no1"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	"400742"	"UO_0000065"	"15.98"	"0.30"	"4.38"	"4.90"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3922799"	""	"0"	"425.49"	"0"	"2.76"	"BDBM228999"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3cccnc3)n2)CC1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"400744"	"UO_0000065"	"19.74"	"0.37"	"5.64"	"6.03"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4106891"	""	"0"	"456.48"	"0"	"2.42"	"BDBM237754"	"CC1(COC(=O)N2CC[C@@H](n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)[C@H](C#N)C2)COC1"	"IC50"	"'='"	"413.0"	"nM"	"6.38"	""	"414858"	"UO_0000065"	"13.99"	"0.26"	"3.96"	"4.71"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3642260"	""	"0"	"400.49"	"0"	"4.01"	"BDBM99518"	"c1cc(-c2ccncc2)c2nc(Nc3ccc(OCCN4CCCC4)cc3)nn2c1"	"IC50"	"'='"	"2999.0"	"nM"	"5.52"	""	"216210"	"UO_0000065"	"13.79"	"0.25"	"1.51"	"8.17"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3933138"	""	"0"	"403.46"	"0"	"1.55"	"BDBM228953"	"CS(=O)(=O)c1ccc(Nc2nn(C3(CC#N)CCOCC3)cc2C(N)=O)cc1"	"IC50"	"'='"	"183.0"	"nM"	"6.74"	""	"400700"	"UO_0000065"	"16.70"	"0.33"	"5.19"	"4.81"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4106834"	""	"0"	"460.49"	"0"	"3.45"	"BDBM228958"	"CC(C)(C)OC(=O)N1CC[C@](CC#N)(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@H](F)C1"	"IC50"	"'='"	"0.2"	"nM"	"9.70"	""	"400705"	"UO_0000065"	"21.06"	"0.40"	"6.25"	"7.68"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3892372"	""	"0"	"359.43"	"0"	"3.00"	"BDBM228962"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCSCC1"	"IC50"	"'='"	"113.0"	"nM"	"6.95"	""	"400709"	"UO_0000065"	"19.33"	"0.38"	"3.95"	"7.18"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3948386"	""	"0"	"442.50"	"0"	"3.50"	"BDBM228968"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CC1"	"IC50"	"'='"	"21.0"	"nM"	"7.68"	""	"400713"	"UO_0000065"	"17.35"	"0.33"	"4.18"	"6.08"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3938918"	""	"0"	"482.59"	"0"	"3.59"	"BDBM228973"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(C(C)(C)O)cc3)n2)CC1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"400718"	"UO_0000065"	"17.66"	"0.33"	"4.93"	"5.82"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3904021"	""	"0"	"495.58"	"0"	"3.07"	"BDBM228987"	"CN(C)C(=O)c1ccc(Nc2nn(C3(CC#N)CCN(C(=O)OC(C)(C)C)CC3)cc2C(N)=O)cc1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"400732"	"UO_0000065"	"17.55"	"0.33"	"5.63"	"5.93"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3967827"	""	"0"	"323.40"	"0"	"3.30"	"BDBM228884"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCCCC1"	"IC50"	"'='"	"92.0"	"nM"	"7.04"	""	"400631"	"UO_0000065"	"21.76"	"0.40"	"3.74"	"7.27"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3955591"	""	"0"	"424.51"	"0"	"3.37"	"BDBM228870"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)CC1"	"IC50"	"'='"	"27.0"	"nM"	"7.57"	""	"400617"	"UO_0000065"	"17.83"	"0.33"	"4.20"	"5.99"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3916994"	""	"0"	"388.45"	"0"	"1.00"	"BDBM228881"	"CCS(=O)(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"404.0"	"nM"	"6.39"	""	"400628"	"UO_0000065"	"16.46"	"0.32"	"5.39"	"4.77"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3939533"	""	"0"	"549.64"	"1"	"-0.13"	"BDBM228882"	"CCS(=O)(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(C(=O)N4CCS(=O)(=O)CC4)cc3)n2)C1"	"IC50"	"'='"	"38.0"	"nM"	"7.42"	""	"400629"	"UO_0000065"	"13.50"	"0.27"	"7.55"	"3.94"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3642370"	""	"0"	"520.66"	"1"	"3.23"	"BDBM99646"	"CN1CCN(c2ccc(Nc3nc4c(NCc5ccccc5N(C)S(C)(=O)=O)cccn4n3)cc2)CC1"	"IC50"	"'='"	"29.1"	"nM"	"7.54"	""	"216336"	"UO_0000065"	"14.47"	"0.28"	"4.31"	"7.68"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL4633694"	""	"0"	"419.41"	"0"	"3.04"	"J-13"	"O=C(Nc1nc2cccc(C3=CCN(C(=O)C4(C(F)(F)F)CC4)CC3)n2n1)C1CC1"	"IC50"	"'='"	"317.0"	"nM"	"6.50"	""	""	"UO_0000065"	"15.50"	"0.30"	"3.46"	"8.16"	"False"	"CHEMBL4624516"	"Inhibition of JAK2 (unknown origin) in presence of ATP at Km concentration by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4622902"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL4113037"	""	"0"	"483.50"	"0"	"2.01"	"BDBM237736"	"N#C[C@@H]1CN(C(=O)OCCN2CCCC2=O)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"411.0"	"nM"	"6.39"	""	"414840"	"UO_0000065"	"13.21"	"0.25"	"4.38"	"4.36"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3911885"	""	"0"	"443.48"	"0"	"2.90"	"BDBM229030"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3cc(F)ccn3)n2)CC1"	"IC50"	"'='"	"903.0"	"nM"	"6.04"	""	"400774"	"UO_0000065"	"13.63"	"0.26"	"3.14"	"4.34"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3934663"	""	"0"	"426.48"	"0"	"2.16"	"BDBM229032"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3cnccn3)n2)CC1"	"IC50"	"'='"	"210.0"	"nM"	"6.68"	""	"400776"	"UO_0000065"	"15.66"	"0.29"	"4.52"	"4.39"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3954311"	""	"0"	"440.51"	"0"	"2.46"	"BDBM229036"	"Cc1cc(Nc2nn(C3(CC#N)CCN(C(=O)OC(C)(C)C)CC3)cc2C(N)=O)ncn1"	"IC50"	"'='"	"126.0"	"nM"	"6.90"	""	"400780"	"UO_0000065"	"15.66"	"0.29"	"4.44"	"4.54"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3968478"	""	"0"	"282.35"	"0"	"1.52"	"BDBM228772"	"N#CCN(C1CC1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399708"	"UO_0000065"	"32.79"	"0.60"	"7.74"	"12.89"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3959770"	""	"0"	"373.26"	"0"	"2.83"	"BDBM228670"	"CN(c1ccc(Br)cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399712"	"UO_0000065"	"24.81"	"0.55"	"6.43"	"15.19"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3960707"	""	"0"	"424.44"	"0"	"2.15"	"BDBM229120"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2ccon2)CC1"	"IC50"	"'='"	"47.0"	"nM"	"7.33"	""	"400856"	"UO_0000065"	"17.26"	"0.32"	"5.18"	"5.28"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3909826"	""	"0"	"441.51"	"0"	"2.39"	"BDBM229126"	"COC1CC(CN2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccnc(F)c4)n3)CC2)C1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"400862"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3936186"	""	"0"	"472.53"	"0"	"3.65"	"BDBM229128"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2cc3ccccc3[nH]2)CC1"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	"400864"	"UO_0000065"	"16.62"	"0.31"	"4.20"	"6.10"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3947600"	""	"0"	"453.40"	"0"	"2.44"	"BDBM229318"	"N#CCC1(n2cc(C(N)=O)c(Nc3cncc(F)c3)n2)CCN(C(=O)CC(F)(F)F)CC1"	"IC50"	"'='"	"35.0"	"nM"	"7.46"	""	"401057"	"UO_0000065"	"16.44"	"0.32"	"5.02"	"5.74"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4108781"	""	"0"	"457.54"	"0"	"4.01"	"BDBM229347"	"CC(C)c1ccc(NC(=O)N2CC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)C2)cc1"	"IC50"	"'='"	"80.0"	"nM"	"7.10"	""	"401086"	"UO_0000065"	"15.51"	"0.29"	"3.09"	"5.50"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4110428"	""	"0"	"429.48"	"0"	"3.19"	"BDBM229351"	"Cc1cccc(NC(=O)N2CC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)C2)c1"	"IC50"	"'='"	"78.0"	"nM"	"7.11"	""	"401090"	"UO_0000065"	"16.55"	"0.30"	"3.92"	"5.51"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4114510"	""	"0"	"443.51"	"0"	"3.50"	"BDBM229356"	"Cc1ccc(C)c(NC(=O)N2CC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)C2)c1"	"IC50"	"'='"	"111.0"	"nM"	"6.96"	""	"401095"	"UO_0000065"	"15.68"	"0.29"	"3.45"	"5.39"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4115634"	""	"0"	"443.51"	"0"	"3.12"	"BDBM229373"	"C[C@@H](NC(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1)c1ccccc1"	"IC50"	"'='"	"265.0"	"nM"	"6.58"	""	"401112"	"UO_0000065"	"14.83"	"0.27"	"3.46"	"5.10"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3699562"	""	"0"	"394.87"	"0"	"4.18"	"BDBM147581"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2cnc3cc(Cl)ccc3c2)n1"	"IC50"	"'='"	"21.0"	"nM"	"7.68"	""	"285511"	"UO_0000065"	"19.44"	"0.37"	"3.50"	"7.00"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703494"	""	"0"	"312.33"	"0"	"1.88"	"BDBM153138"	"CCOC(=O)c1c[nH]c2ncnc(-c3ccc(CO)c(N)c3)c12"	"IC50"	"'='"	"215.0"	"nM"	"6.67"	""	"294086"	"UO_0000065"	"21.35"	"0.40"	"4.79"	"5.84"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652385"	""	"0"	"379.49"	"0"	"0.96"	"BDBM113197"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC(O)C2)CC1"	"IC50"	"'='"	"34.4"	"nM"	"7.46"	""	"234640"	"UO_0000065"	"19.67"	"0.39"	"6.50"	"7.29"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3650979"	""	"0"	"307.31"	"0"	"2.68"	"BDBM153153"	"CCOC(=O)c1c[nH]c2ncnc(-c3ccc4[nH]ncc4c3)c12"	"IC50"	"'='"	"98.0"	"nM"	"7.01"	""	"294101"	"UO_0000065"	"22.81"	"0.42"	"4.33"	"7.26"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703055"	""	"0"	"406.49"	"0"	"2.87"	"BDBM147765"	"CC(=O)c1ccc(Nc2nn([C@H]3CC[C@H](N4CCC4)C[C@@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"285699"	"UO_0000065"	"19.79"	"0.37"	"5.18"	"6.87"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3655087"	""	"0"	"388.50"	"0"	"1.93"	"BDBM159754"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)[C@H]2C[C@@](C)(CC#N)C2)C1"	"IC50"	"'='"	"2020.0"	"nM"	"5.70"	""	"302564"	"UO_0000065"	"14.66"	"0.29"	"3.76"	"4.96"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645015"	""	"0"	"538.63"	"1"	"4.73"	"BDBM99767"	"CN(C)C(=O)CN1CCC(c2ccc(Nc3nc4c(-c5cnn(-c6ccc(F)cc6)c5)cccn4n3)cc2)CC1"	"IC50"	"'='"	"1.06"	"nM"	"8.97"	""	"216454"	"UO_0000065"	"16.66"	"0.31"	"4.24"	"10.74"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3702947"	""	"0"	"397.48"	"0"	"2.83"	"BDBM147649"	"COC(C)(C)c1ccc(Nc2nn([C@H]3CC[C@@H](O)C[C@@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"285581"	"UO_0000065"	"21.89"	"0.41"	"5.87"	"6.89"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702955"	""	"0"	"411.36"	"0"	"3.11"	"BDBM147659"	"N#C[C@H]1C[C@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)c(F)c2)n1"	"IC50"	"'='"	"28.0"	"nM"	"7.55"	""	"285591"	"UO_0000065"	"18.36"	"0.36"	"4.44"	"6.46"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665210"	""	"0"	"465.54"	"0"	"2.39"	"BDBM112610"	"CS(=O)(=O)N1CCC[C@H](Nc2nc(Nc3ccncc3)ncc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.6379"	"nM"	"9.20"	""	"233847"	"UO_0000065"	"19.75"	"0.38"	"6.81"	"6.49"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642420"	""	"0"	"575.74"	"1"	"4.06"	"BDBM99698"	"CN(c1ccccc1CNc1cccn2nc(Nc3ccc4c(c3)CCC(N3CCOCC3)CC4)nc12)S(C)(=O)=O"	"IC50"	"'='"	"134.47"	"nM"	"6.87"	""	"216388"	"UO_0000065"	"11.93"	"0.23"	"2.81"	"6.60"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL2325898"	""	"0"	"378.44"	"0"	"1.72"	"3t"	"N#C[C@H]1CCN(C(=O)[C@H](NC(=O)c2c[nH]c3ncc(C4CC4)nc23)C2CC2)C1"	"IC50"	"'='"	"321.0"	"nM"	"6.49"	""	""	"UO_0000065"	"17.16"	"0.32"	"4.77"	"5.66"	"False"	"CHEMBL2329053"	"Inhibition of JAK2 in human PBMC expressing CD14 assessed as inhibition of GM-CSF-stimulated STAT5a phosphorylation after 30 mins by flow cytometric analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321829"	"1"	"Scientific Literature"	"J. Med. Chem."	"2013"	"None"	""
"CHEMBL1938660"	""	"0"	"531.70"	"1"	"3.07"	"26"	"CC(C)(C)NS(=O)(=O)c1ccc(-c2cc3c(N)ncc(C(=O)NCCCN4CCOCC4)c3s2)cc1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	""	"UO_0000065"	"15.61"	"0.31"	"5.23"	"6.55"	"False"	"CHEMBL1941383"	"Inhibition of human recombinant N-terminal GST-tagged JAK2 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308860"	""
"CHEMBL3330118"	""	"0"	"341.80"	"0"	"3.24"	"21"	"CNc1nccc(-c2cc(C(N)=O)c(-c3cc(Cl)ccc3C)[nH]2)n1"	"IC50"	"'='"	"1010.0"	"nM"	"6.00"	""	""	"UO_0000065"	"17.54"	"0.34"	"2.76"	"6.20"	"False"	"CHEMBL3374497"	"Inhibition of JAK2 V617F mutant in human SET2 cells"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330115"	""	"0"	"341.80"	"0"	"2.79"	"18"	"Cc1ccc(Cl)cc1-c1c(C(N)=O)cc(-c2ccnc(N)n2)n1C"	"IC50"	"'='"	"66.0"	"nM"	"7.18"	""	""	"UO_0000065"	"21.01"	"0.41"	"4.39"	"7.19"	"False"	"CHEMBL3374493"	"Inhibition of recombinant human JAK2 (808-1132 residues) using LPLDKDYYVVREPGQ as substrate by radiometric assay in presence of [33P]-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3126341"	""	"0"	"375.19"	"0"	"4.66"	"16"	"O=c1[nH]ccc2c(Nc3c(Cl)cc(F)cc3Cl)nc3ccncc3c12"	"IC50"	"'='"	"0.8"	"nM"	"9.10"	""	""	"UO_0000065"	"24.25"	"0.50"	"4.44"	"12.87"	"False"	"CHEMBL3131376"	"Inhibition of recombinant Jak2 (unknown origin) using biotinylated synthetic peptide substrate by homogeneous time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3124786"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL1938654"	""	"0"	"418.54"	"0"	"2.98"	"19"	"CNC(=O)c1cnc(N)c2cc(-c3ccc(S(=O)(=O)NC(C)(C)C)cc3)sc12"	"IC50"	"'='"	"48.0"	"nM"	"7.32"	""	""	"UO_0000065"	"17.49"	"0.36"	"4.34"	"6.41"	"False"	"CHEMBL1941458"	"Inhibition of JAK2 in human PBMC assessed as inhibition of TPO-stimulated STAT5 phosphorylation preincubated for 30 mins prior to TPO challenge measured after 15 mins by intracellular phosflow staining"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL3330109"	""	"0"	"373.82"	"0"	"3.38"	"12"	"Cc1ccc(Cl)cc1-c1[nH]c(-c2ccnc(N)n2)cc1C(=O)NCCF"	"IC50"	"'='"	"114.0"	"nM"	"6.94"	""	""	"UO_0000065"	"18.57"	"0.36"	"3.56"	"7.18"	"False"	"CHEMBL3374493"	"Inhibition of recombinant human JAK2 (808-1132 residues) using LPLDKDYYVVREPGQ as substrate by radiometric assay in presence of [33P]-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330105"	""	"0"	"341.80"	"0"	"3.04"	"7"	"CNC(=O)c1cc(-c2ccnc(N)n2)[nH]c1-c1cc(Cl)ccc1C"	"IC50"	"'='"	"35.0"	"nM"	"7.46"	""	""	"UO_0000065"	"21.81"	"0.42"	"4.42"	"7.71"	"False"	"CHEMBL3374493"	"Inhibition of recombinant human JAK2 (808-1132 residues) using LPLDKDYYVVREPGQ as substrate by radiometric assay in presence of [33P]-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330101"	""	"0"	"313.75"	"0"	"2.47"	"3"	"NC(=O)c1cc(-c2ccnc(N)n2)[nH]c1-c1ccccc1Cl"	"IC50"	"'='"	"615.0"	"nM"	"6.21"	""	""	"UO_0000065"	"19.80"	"0.39"	"3.74"	"5.61"	"False"	"CHEMBL3374493"	"Inhibition of recombinant human JAK2 (808-1132 residues) using LPLDKDYYVVREPGQ as substrate by radiometric assay in presence of [33P]-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3116061"	""	"0"	"365.38"	"0"	"2.60"	"13d, enantiomeric mixture"	"CC(Nc1nc(Nc2cn(C)cn2)c2cccnc2n1)c1ncc(F)cn1"	"IC50"	"'='"	"33.0"	"nM"	"7.48"	""	""	"UO_0000065"	"20.48"	"0.38"	"4.88"	"7.04"	"False"	"CHEMBL3118240"	"Inhibition of Jak2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112447"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL3234891"	""	"0"	"295.37"	"0"	"3.65"	"5"	"NC(=O)c1cc(-c2ccccc2)sc1Nc1ccncc1"	"IC50"	"'='"	"175.0"	"nM"	"6.76"	""	""	"UO_0000065"	"22.88"	"0.44"	"3.11"	"9.94"	"False"	"CHEMBL3239499"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3232939"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3234885"	""	"0"	"309.39"	"0"	"3.96"	"11"	"Cc1ccc(Nc2sc(-c3ccccc3)cc2C(N)=O)nc1"	"IC50"	"'='"	"178.0"	"nM"	"6.75"	""	""	"UO_0000065"	"21.82"	"0.42"	"2.79"	"9.92"	"False"	"CHEMBL3239499"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3232939"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3330113"	""	"0"	"403.87"	"0"	"4.94"	"16"	"Cc1ccc(Cl)cc1-c1[nH]c(-c2ccnc(N)n2)cc1C(=O)Nc1ccccc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL3374497"	"Inhibition of JAK2 V617F mutant in human SET2 cells"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3329229"	""	"0"	"371.83"	"0"	"2.40"	"10"	"Cc1ccc(Cl)cc1-c1[nH]c(-c2ccnc(N)n2)cc1C(=O)NCCO"	"IC50"	"'='"	"57.0"	"nM"	"7.24"	""	""	"UO_0000065"	"19.48"	"0.38"	"4.84"	"6.20"	"False"	"CHEMBL3374493"	"Inhibition of recombinant human JAK2 (808-1132 residues) using LPLDKDYYVVREPGQ as substrate by radiometric assay in presence of [33P]-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330104"	""	"0"	"327.78"	"0"	"2.78"	"6"	"Cc1ccc(Cl)cc1-c1[nH]c(-c2ccnc(N)n2)cc1C(N)=O"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	""	"UO_0000065"	"23.49"	"0.46"	"4.92"	"6.96"	"True"	"CHEMBL3374493"	"Inhibition of recombinant human JAK2 (808-1132 residues) using LPLDKDYYVVREPGQ as substrate by radiometric assay in presence of [33P]-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330116"	""	"0"	"355.83"	"0"	"3.27"	"19"	"CCn1c(-c2ccnc(N)n2)cc(C(N)=O)c1-c1cc(Cl)ccc1C"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL3374497"	"Inhibition of JAK2 V617F mutant in human SET2 cells"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330124"	""	"0"	"361.33"	"0"	"3.15"	"27"	"Cc1ccc(C(F)(F)F)cc1-c1[nH]c(-c2ccnc(N)n2)cc1C(N)=O"	"IC50"	"'='"	"760.0"	"nM"	"6.12"	""	""	"UO_0000065"	"16.94"	"0.32"	"2.97"	"5.53"	"False"	"CHEMBL3374497"	"Inhibition of JAK2 V617F mutant in human SET2 cells"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL4784866"	""	"0"	"160.18"	"0"	"1.11"	"MR1"	"Nc1cccc2cc[nH]c(=O)c12"	"IC50"	"'='"	"21400.0"	"nM"	"4.67"	""	""	""	"29.15"	"0.53"	"3.56"	"7.93"	"False"	"CHEMBL4699843"	"Inhibition of JAK2 (unknown origin) using FRET-peptide as substrate incubated for 1 hr by Z-lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4699400"	"1"	"Scientific Literature"	"RSC Med Chem"	"2020"	"None"	"TIME = 1.0 hr"
"CHEMBL2414547"	""	"0"	"462.58"	"0"	"3.30"	"12"	"CN1CCN(c2ccc(Nc3nc4cccc(-c5ccc(S(C)(=O)=O)cc5)n4n3)cc2)CC1"	"IC50"	"'='"	"32.9"	"nM"	"7.48"	""	""	"UO_0000065"	"16.18"	"0.31"	"4.18"	"9.03"	"False"	"CHEMBL2415128"	"Inhibition of JAK2 in human SET2 cells assessed as reduction of phosphorylated STAT5 level"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2412966"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2414544"	""	"0"	"414.51"	"0"	"3.90"	"9"	"COc1ccc(-c2cccc3nc(Nc4ccc(N5CCN(C)CC5)cc4)nn23)cc1"	"IC50"	"'='"	"21.9"	"nM"	"7.66"	""	""	"UO_0000065"	"18.48"	"0.34"	"3.76"	"13.22"	"False"	"CHEMBL2415128"	"Inhibition of JAK2 in human SET2 cells assessed as reduction of phosphorylated STAT5 level"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2412966"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2414533"	""	"0"	"360.37"	"0"	"3.85"	"29"	"COc1ccc(-c2cccn3nc(Nc4ccc(C(=O)O)cc4)nc23)cc1"	"IC50"	"'='"	"212.0"	"nM"	"6.67"	""	""	"UO_0000065"	"18.52"	"0.34"	"2.82"	"7.52"	"False"	"CHEMBL2415128"	"Inhibition of JAK2 in human SET2 cells assessed as reduction of phosphorylated STAT5 level"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2412966"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL1934344"	""	"0"	"534.65"	"1"	"2.60"	"3j"	"CN(c1ncccc1-c1ccc2cnc(Nc3ccc(C4CCN(CC(N)=O)CC4)cc3)nn12)S(C)(=O)=O"	"IC50"	"'='"	"38.0"	"nM"	"7.42"	""	""	"UO_0000065"	"13.88"	"0.27"	"4.82"	"5.35"	"False"	"CHEMBL1936009"	"Inhibition of JAK2 in GM-CSF-stimulated human TF1 cells preincubated for 1 hr prior to challenge"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3307972"	""
"CHEMBL4467200"	""	"0"	"368.37"	"0"	"2.05"	"15"	"O=c1[nH]c2cnc(-c3cnc4ccc(F)cn34)nc2n1[C@H]1CC[C@H](O)CC1"	"IC50"	"'='"	"5.4"	"nM"	"8.27"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4450301"	""	"0"	"374.38"	"0"	"3.18"	"19"	"C[C@H](c1ccccc1)n1c(=O)[nH]c2cnc(-c3cnc4ccc(F)cn34)nc21"	"IC50"	"'='"	"0.7"	"nM"	"9.15"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4443416"	""	"0"	"428.84"	"0"	"1.28"	"32"	"N#CCC(=O)N1CCC[C@H](n2c(=O)[nH]c3cnc(Nc4cc(Cl)c[nH]c4=O)nc32)C1"	"IC50"	"'='"	"2.4"	"nM"	"8.62"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL3899411"	""	"0"	"575.60"	"1"	"4.64"	"BDBM230093"	"Cc1c(-c2c(C#N)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)c2cccc(F)c2n(C)c1=O"	"IC50"	"'='"	"2400.0"	"nM"	"5.62"	""	"402026"	"UO_0000065"	"9.76"	"0.18"	"0.98"	"3.83"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3896019"	""	"0"	"568.58"	"1"	"4.90"	"BDBM230123"	"Cc1c(-c2c(F)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)c2cccc(F)c2n(C)c1=O"	"IC50"	"'='"	"170.0"	"nM"	"6.77"	""	"402028"	"UO_0000065"	"11.91"	"0.22"	"1.87"	"5.50"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3896019"	""	"0"	"568.58"	"1"	"4.90"	"BDBM230123"	"Cc1c(-c2c(F)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)c2cccc(F)c2n(C)c1=O"	"IC50"	"'='"	"2200.0"	"nM"	"5.66"	""	"402029"	"UO_0000065"	"9.95"	"0.18"	"0.76"	"4.60"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3913962"	""	"0"	"597.05"	"2"	"5.72"	"BDBM230099"	"Cc1c(-c2c(Cl)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)ccn(-c2ccc(F)cc2)c1=O"	"IC50"	"'='"	"1800.0"	"nM"	"5.75"	""	"402035"	"UO_0000065"	"9.62"	"0.18"	"0.02"	"4.67"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3914438"	""	"0"	"474.54"	"0"	"3.28"	"BDBM228687"	"CN(c1ccc(C(=O)NC[C@H](O)c2ccccc2)cc1F)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399688"	"UO_0000065"	"21.62"	"0.40"	"6.98"	"10.54"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL1079593"	"VS-5584"	"1"	"420.38"	"0"	"3.11"	"1; PS-020613"	"O=c1[nH]c2cnc(-n3cnc4ccc(F)cc43)nc2n1[C@@H]1CCOc2c(F)cccc21"	"IC50"	"'='"	"1.2"	"nM"	"8.92"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL386760"	""	"0"	"686.81"	"3"	"6.22"	"43"	"COc1ccc(N(C(=O)Oc2c(C)cccc2C)c2ccnc(Nc3cc(OC)c(OCCCN4CCN(C)CC4)c(OC)c3)n2)c(OC)c1"	"IC50"	"'='"	"240.0"	"nM"	"6.62"	""	""	"UO_0000065"	"9.64"	"0.18"	"0.40"	"5.52"	"False"	"CHEMBL870360"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1145338"	"1"	"Scientific Literature"	"J. Med. Chem."	"2006"	"None"	""
"CHEMBL4763483"	""	"0"	"462.94"	"0"	"4.20"	"10d"	"O=C(Nc1c[nH]nc1-c1nc(-c2ccc(CN3CCOCC3)cc2)c[nH]1)c1ccc(Cl)cc1"	"IC50"	"'='"	"94.0"	"nM"	"7.03"	""	""	""	"15.18"	"0.29"	"2.83"	"7.10"	"False"	"CHEMBL4711870"	"Inhibition of JAK2 (unknown origin) incubated for 40 mins in presence of ATP by Kinase-glo luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706620"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2021"	"None"	"TIME = 0.6667 hr"
"CHEMBL3335676"	""	"0"	"259.31"	"0"	"2.41"	"3"	"O=C(Nc1cnc2[nH]ccc2n1)NC1CCCCC1"	"IC50"	"'='"	"47.0"	"nM"	"7.33"	""	""	"UO_0000065"	"28.26"	"0.53"	"4.92"	"8.86"	"False"	"CHEMBL3374010"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 1 hr in presence of [gamma-33P]ATP by scintillation counting analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351377"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3116050"	""	"0"	"353.37"	"0"	"2.54"	"19a"	"C[C@H](Nc1nc(Nc2cn(C)cn2)c2cc[nH]c2n1)c1ncc(F)cn1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	""	"UO_0000065"	"23.49"	"0.44"	"5.76"	"7.60"	"False"	"CHEMBL3116824"	"Inhibition of Jak2 V617F mutant in human UKE1 cells assessed as inhibition of STAT5 phosphorylation after 24 hrs by Western blotting analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"UKE1"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112447"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL4440767"	""	"0"	"397.44"	"0"	"1.05"	"18"	"COc1ccc(-c2cc3c(NC(CO)[C@H](O)C4CC4)c(C(N)=O)cnn3c2)cn1"	"IC50"	"'='"	"1400.0"	"nM"	"5.85"	""	""	"UO_0000065"	"14.73"	"0.28"	"4.80"	"4.34"	"False"	"CHEMBL4339747"	"Inhibition of GST-tagged JAK2 (unknown origin) using fluoresceinated peptide as substrate measured after 3 hrs by electrophoresis method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4339199"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2019"	"None"	""
"CHEMBL1789941"	"RUXOLITINIB"	"4"	"306.37"	"0"	"3.47"	"64"	"N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	""	"UO_0000065"	"26.26"	"0.48"	"4.58"	"9.67"	"False"	"CHEMBL4351042"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4350951"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL1789941"	"RUXOLITINIB"	"4"	"306.37"	"0"	"3.47"	"2"	"N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"0.2"	"nM"	"9.70"	""	""	"UO_0000065"	"31.66"	"0.58"	"6.23"	"11.66"	"False"	"CHEMBL3388144"	"Inhibition of human recombinant JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351789"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL4437903"	""	"0"	"337.36"	"0"	"3.44"	"77"	"Cc1cc(Nc2cnc(C#N)c(N[C@@H](C)c3ccc(F)cc3)n2)n[nH]1"	"IC50"	"'='"	"33.0"	"nM"	"7.48"	""	""	"UO_0000065"	"22.18"	"0.41"	"4.04"	"7.31"	"False"	"CHEMBL4349471"	"Inhibition of recombinant C-terminal His6-tagged human JAK2 (808 to end residues) expressed in baculovirus infected SF21 insect cells using Tyr 1054/1055 biotinylated peptide as substrate after 60 mins by Alphascreen assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4346723"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2019"	"CHEMBL4106362"	""
"CHEMBL4172110"	""	"0"	"482.57"	"0"	"2.98"	"16"	"CS(=O)(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCC(C(=O)NO)CC4)cc3)n2)cc1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	""	"UO_0000065"	"18.65"	"0.36"	"6.02"	"6.59"	"False"	"CHEMBL4150584"	"Inhibition of JAK2 (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition and measured after 25 mins in presence of ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4145634"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3403553"	""	"0"	"365.82"	"0"	"3.93"	"26"	"CCc1ccc(Cl)cc1-c1cc(-c2ncnc3[nH]ccc23)[nH]c1C(N)=O"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"23.30"	"0.45"	"4.59"	"8.48"	"False"	"CHEMBL3404501"	"Inhibition of recombinant epitope-tagged JAK2 (808 to 1132) (unknown origin) using LPLDKDYYVVREPGQ as substrate by beta-countiing analysis in presence of 33P-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3400063"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL4241559"	""	"0"	"418.46"	"0"	"2.59"	"7"	"C=CC(=O)Nc1cccc(Cn2ncc3c(Nc4cnn(CCOC)c4)ncnc32)c1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4244570"	""	"0"	"423.48"	"0"	"1.07"	"9d"	"COCCn1cc(-c2nn(CC3CCCN(C(=O)CC#N)C3)c3ncnc(N)c23)cn1"	"IC50"	"'='"	"696.8"	"nM"	"6.16"	""	""	"UO_0000065"	"14.54"	"0.27"	"5.09"	"4.37"	"False"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL3920230"	""	"0"	"401.44"	"1"	"5.48"	"BDBM195903"	"C=CC(=O)Nc1cccc(-c2cnc3[nH]cc(-c4cc(C)c(F)cc4OC)c3c2)c1"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	"348609"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3887689"	"Biochemical Inhibition Assay: 1H-pyrrolo[2,3-b]pyridine, 1H-pyrazolo[3,4-b]pyridine and 5H-pyrrolo[2,3-b]pyrazine series of compounds exhibited over >100 fold selective against Janus and TEC family of kinases except for the BMX and TXK it had activity of 30 and 45 nM respectively."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886406"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3116065"	""	"0"	"365.38"	"0"	"2.60"	"13h"	"C[C@H](Nc1nc(Nc2cn(C)cn2)c2ccncc2n1)c1ncc(F)cn1"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	""	"UO_0000065"	"21.68"	"0.40"	"5.32"	"7.45"	"False"	"CHEMBL3118240"	"Inhibition of Jak2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112447"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL4636507"	""	"0"	"384.52"	"0"	"3.87"	"38"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](CC(=O)N4CCC(C)(C)CC4)CC3)c12"	"IC50"	"'='"	"32.0"	"nM"	"7.50"	""	""	"UO_0000065"	"19.49"	"0.37"	"3.62"	"9.16"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL3925725"	""	"0"	"480.49"	"1"	"5.38"	"BDBM195901"	"COc1c(F)cc(F)cc1-c1c[nH]c2ncc(-c3cc(NC(=O)/C=C/CN(C)C)ccc3F)cc12"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	"348607"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3887689"	"Biochemical Inhibition Assay: 1H-pyrrolo[2,3-b]pyridine, 1H-pyrazolo[3,4-b]pyridine and 5H-pyrrolo[2,3-b]pyrazine series of compounds exhibited over >100 fold selective against Janus and TEC family of kinases except for the BMX and TXK it had activity of 30 and 45 nM respectively."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886406"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3398129"	""	"0"	"463.49"	"0"	"3.59"	"1d"	"COc1cccc(NC(=O)c2cnc(N3CCN(c4ccccc4OC)CC3)c([N+](=O)[O-])c2)c1"	"IC50"	"'='"	"9500.0"	"nM"	"5.02"	""	""	"UO_0000065"	"10.84"	"0.20"	"1.43"	"4.56"	"False"	"CHEMBL3399759"	"Inhibition of IL4-induced JAK2 autophosphorylation in human HT-29 cells by SDS-polyacrylamide gel electrophoresis and Western blot method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HT-29"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3397032"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"CHEMBL3307768"	""
"CHEMBL3647837"	""	"0"	"391.83"	"0"	"3.13"	"BDBM147946"	"C[C@@]1(O)CC[C@H](n2cc(C(N)=O)c(Nc3ccc(Cl)c(F)c3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"28.0"	"nM"	"7.55"	""	"285880"	"UO_0000065"	"19.28"	"0.38"	"4.42"	"6.46"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642402"	""	"0"	"448.55"	"0"	"2.95"	"BDBM99680"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4cccc(N5CCNCC5)c4)nc23)cc1"	"IC50"	"'='"	"0.97"	"nM"	"9.01"	""	"216370"	"UO_0000065"	"20.09"	"0.38"	"6.06"	"9.84"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703006"	""	"0"	"476.50"	"0"	"3.60"	"BDBM147716"	"CC1(CN[C@H]2CC[C@H](n3cc(C(N)=O)c(Nc4ccc(C(F)(F)F)cc4)n3)[C@@H](C#N)C2)COC1"	"IC50"	"'='"	"35.0"	"nM"	"7.46"	""	"285650"	"UO_0000065"	"15.65"	"0.30"	"3.86"	"6.32"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4526283"	""	"0"	"415.45"	"0"	"2.87"	"23"	"CNC(=O)c1cnc(Nc2ccc(F)cn2)cc1Nc1ccccc1S(C)(=O)=O"	"IC50"	"'>'"	"50000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4414788"	"Inhibition of JAK2 JH1 domain (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414548"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4103980"	""	"0"	"372.40"	"1"	"5.18"	"11"	"CCc1cc(O)c(F)cc1-c1ccc2c(-c3nc4ccccc4[nH]3)n[nH]c2c1"	"IC50"	"'='"	"7.9"	"nM"	"8.10"	""	""	"UO_0000065"	"21.76"	"0.40"	"2.92"	"10.44"	"False"	"CHEMBL4003453"	"Inhibition of GST tagged human recombinant JAK2 catalytic domain expressed in baculovirus using peptide substrate preincubated for 60 mins followed by substrate addition and measured after 60 mins by microfluidic assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4002590"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4086057"	""	"0"	"304.35"	"0"	"3.89"	"12"	"CCc1cc(O)ccc1-c1ccc2c(-c3ncc[nH]3)n[nH]c2c1"	"IC50"	"'='"	"0.8"	"nM"	"9.10"	""	""	"UO_0000065"	"29.89"	"0.54"	"5.21"	"11.72"	"False"	"CHEMBL4003453"	"Inhibition of GST tagged human recombinant JAK2 catalytic domain expressed in baculovirus using peptide substrate preincubated for 60 mins followed by substrate addition and measured after 60 mins by microfluidic assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4002590"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL3642285"	""	"0"	"476.61"	"0"	"3.44"	"BDBM99550"	"CN1CCN(c2ccc(Nc3nc4c(-c5ccc(CS(C)(=O)=O)cc5)cccn4n3)cc2)CC1"	"IC50"	"'='"	"0.7"	"nM"	"9.15"	""	"216242"	"UO_0000065"	"19.21"	"0.37"	"5.71"	"11.05"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647776"	""	"0"	"460.50"	"0"	"4.32"	"BDBM147879"	"CC1(C)CN([C@@H]2CC[C@H](n3cc(C(N)=O)c(Nc4ccc(C(F)(F)F)cc4)n3)[C@@H](C#N)C2)C1"	"IC50"	"'='"	"285.0"	"nM"	"6.54"	""	"285813"	"UO_0000065"	"14.21"	"0.27"	"2.23"	"6.55"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3644966"	""	"0"	"451.56"	"0"	"2.84"	"BDBM99716"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4cnn(CCN5CCCC5)c4)nc23)cc1"	"IC50"	"'='"	"13.9"	"nM"	"7.86"	""	"216406"	"UO_0000065"	"17.40"	"0.34"	"5.02"	"8.07"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642345"	""	"0"	"521.65"	"1"	"2.63"	"BDBM99621"	"CN1CCN(c2ccc(Nc3nc4c(NCc5cccnc5N(C)S(C)(=O)=O)cccn4n3)cc2)CC1"	"IC50"	"'='"	"20.73"	"nM"	"7.68"	""	"216311"	"UO_0000065"	"14.73"	"0.28"	"5.05"	"6.92"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652330"	""	"0"	"434.57"	"0"	"1.48"	"BDBM113141"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCC[C@H](C(N)=O)C2)CC1"	"IC50"	"'='"	"20.6"	"nM"	"7.69"	""	"234584"	"UO_0000065"	"17.69"	"0.35"	"6.21"	"6.14"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3699523"	""	"0"	"390.45"	"0"	"2.78"	"BDBM147541"	"Cn1cc(-c2cc(Nc3nn([C@H]4CCCC[C@@H]4C#N)cc3C(N)=O)ccn2)cn1"	"IC50"	"'='"	"60.0"	"nM"	"7.22"	""	"285471"	"UO_0000065"	"18.50"	"0.34"	"4.44"	"5.67"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652345"	""	"0"	"435.59"	"0"	"2.38"	"BDBM113156"	"CC[C@@]1(CO)CCN(S(=O)(=O)C[C@H]2CC[C@H](N(C)c3ncnc4[nH]ccc34)CC2)C1"	"IC50"	"'='"	"55.2"	"nM"	"7.26"	""	"234599"	"UO_0000065"	"16.66"	"0.33"	"4.88"	"7.09"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3647767"	""	"0"	"514.47"	"1"	"4.91"	"BDBM147870"	"N#C[C@H]1C[C@@H](N[C@@H](C2CC2)C(F)(F)F)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"152.0"	"nM"	"6.82"	""	"285804"	"UO_0000065"	"13.25"	"0.26"	"1.91"	"6.27"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651014"	""	"0"	"351.37"	"0"	"2.71"	"BDBM153190"	"C=C(C)C(=O)Nc1cc(-c2ncnc3[nH]cc(C(=O)OCC)c23)ccn1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294138"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647870"	""	"0"	"468.53"	"0"	"4.16"	"BDBM147982"	"N#C[C@H]1C[C@H](OC(=O)NC2CCCCC2)CCC1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"88.0"	"nM"	"7.06"	""	"285916"	"UO_0000065"	"15.06"	"0.28"	"2.90"	"5.22"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3658867"	""	"0"	"408.89"	"0"	"3.44"	"BDBM159786"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](CS(=O)(=O)c2ccc(F)c(Cl)c2)C1"	"IC50"	"'='"	"85.0"	"nM"	"7.07"	""	"302596"	"UO_0000065"	"17.29"	"0.36"	"3.63"	"8.96"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3798618"	""	"0"	"591.71"	"1"	"3.43"	"16e"	"Cn1c(C(=O)NCCCN2CCOCC2)cc2c(-c3ccc(NC(=O)[C@@H]4CCCN4C(=O)OC(C)(C)C)cc3)ncnc21"	"IC50"	"'='"	"270.0"	"nM"	"6.57"	""	""	"UO_0000065"	"11.10"	"0.21"	"3.14"	"5.02"	"False"	"CHEMBL3802364"	"Inhibition of JAK2 in GMCSF-stimulated human TF1 cells assessed as suppression of STAT5 phosphorylation preincubated for 2 hrs followed by GMCSF stimulation for 50 mins by FACS reader analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"CHEMBL3307972"	""
"CHEMBL4564126"	"TP-008"	"0"	"411.82"	"0"	"2.84"	"18"	"Cc1cnc(-c2cc(Cl)ccc2F)cc1-n1c(=O)n(CC(N)=O)c2cnccc21"	"IC50"	"'>='"	"5000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4427697"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4425174"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2016"	"None"	""
"CHEMBL3896019"	""	"0"	"568.58"	"1"	"4.90"	"BDBM230123"	"Cc1c(-c2c(F)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)c2cccc(F)c2n(C)c1=O"	"IC50"	"'='"	"1100.0"	"nM"	"5.96"	""	"402063"	"UO_0000065"	"10.48"	"0.19"	"1.06"	"4.84"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3894000"	""	"0"	"572.54"	"2"	"5.03"	"BDBM230120"	"Cc1c(-c2c(F)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)[nH]c2c(F)cc(F)cc2c1=O"	"IC50"	"'='"	"580.0"	"nM"	"6.24"	""	"402084"	"UO_0000065"	"10.89"	"0.20"	"1.21"	"4.66"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3797364"	""	"0"	"323.36"	"0"	"2.08"	"14b"	"CCC(=O)Nc1ccc(-c2ncnc3c2cc(C(N)=O)n3C)cc1"	"IC50"	"'='"	"15800.0"	"nM"	"4.80"	""	""	"UO_0000065"	"14.85"	"0.27"	"2.72"	"4.67"	"False"	"CHEMBL3802364"	"Inhibition of JAK2 in GMCSF-stimulated human TF1 cells assessed as suppression of STAT5 phosphorylation preincubated for 2 hrs followed by GMCSF stimulation for 50 mins by FACS reader analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"CHEMBL3307972"	""
"CHEMBL3799168"	""	"0"	"468.56"	"0"	"3.71"	"15f"	"Cn1c(C(=O)NCCN2CCCC2)cc2c(-c3ccc(NC(=O)c4ccccc4)cc3)ncnc21"	"IC50"	"'='"	"78.0"	"nM"	"7.11"	""	""	"UO_0000065"	"15.17"	"0.28"	"3.40"	"7.71"	"False"	"CHEMBL3802363"	"Inhibition of recombinant human GST-tagged JAK2 expressed in baculovirus expression system using Z'-LYTE Try6 peptide as substrate incubated for 1 hr by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3763184"	""	"0"	"314.39"	"0"	"2.31"	"12"	"CCC(C(C)C)n1cc(-c2ccn(C)n2)c2[nH]nc(N)c2c1=O"	"IC50"	"'='"	"830.0"	"nM"	"6.08"	""	""	"UO_0000065"	"19.34"	"0.36"	"3.77"	"6.43"	"False"	"CHEMBL3766653"	"Inhibition of JAK2 (unknown origin) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent substrate phosphorylation after 45 mins by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3763089"	"1"	"Scientific Literature"	"J. Med. Chem."	"2016"	"None"	""
"CHEMBL3314140"	""	"0"	"404.90"	"0"	"4.86"	"13a"	"Clc1ccc(-c2ccc(-c3nccn3-c3ccc(N4CCNCC4)cc3)o2)cc1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3371228"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351352"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL2159198"	""	"0"	"254.34"	"0"	"3.73"	"23"	"Cc1nc2cnc3[nH]ccc3c2n1C1CCCCC1"	"IC50"	"'='"	"6000.0"	"nM"	"5.22"	""	""	"UO_0000065"	"20.53"	"0.38"	"1.49"	"11.23"	"False"	"CHEMBL2327181"	"Inhibition of JAK2 (unknown origin) after 2.5 hrs by time-resolved fluorescence resonance energy transfer assay in presence of 100 uM ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321825"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL3699480"	""	"0"	"343.36"	"0"	"2.09"	"BDBM147495"	"N#C[C@H]1C[C@@H](O)CCC1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	"285421"	"UO_0000065"	"22.97"	"0.43"	"5.80"	"6.74"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651604"	""	"0"	"439.50"	"0"	"1.62"	"BDBM103736"	"O=C(Nc1nc2cccc(-c3ccc(C(=O)N4CCS(=O)(=O)CC4)cc3)n2n1)C1CC1"	"IC50"	"'='"	"65.42"	"nM"	"7.18"	""	"221722"	"UO_0000065"	"16.35"	"0.32"	"5.56"	"6.32"	"False"	"CHEMBL3707887"	"Inhibition Assay: In vitro inhibition assay using various enzyme."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638964"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642410"	""	"0"	"515.64"	"1"	"3.02"	"BDBM99688"	"CN1CCN(c2ccc(Nc3nc4c(C#Cc5ccccc5N(C)S(C)(=O)=O)cccn4n3)cc2)CC1"	"IC50"	"'='"	"2.61"	"nM"	"8.58"	""	"216377"	"UO_0000065"	"16.65"	"0.32"	"5.56"	"9.97"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3651043"	""	"0"	"368.44"	"1"	"5.11"	"BDBM153220"	"C=C(C)C(=O)Nc1cccc(-c2ncnc3[nH]cc(-c4cccc(C)c4)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294168"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3644988"	""	"0"	"567.61"	"2"	"7.28"	"BDBM99740"	"COc1ccc(C(F)(F)F)cc1-c1cccn2nc(Nc3cccc(C4CCN(C(=O)OC(C)(C)C)CC4)c3)nc12"	"IC50"	"'='"	"9999.0"	"nM"	"5.00"	""	"216428"	"UO_0000065"	"8.81"	"0.17"	"-2.28"	"6.17"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL4225923"	""	"0"	"459.58"	"0"	"4.50"	"16"	"Cc1cn2c(-c3cn[nH]c3)cnc2c(Nc2cc(C(NC(C)(C)C)c3ccccn3)ns2)n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4222462"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219148"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2018"	"None"	""
"CHEMBL3645549"	""	"0"	"348.41"	"0"	"2.57"	"BDBM107135"	"O=C(CN1CCOCC1)Nc1cccc(-c2cnc3ccccc3n2)c1"	"IC50"	"'>'"	"50000.0"	"nM"	""	""	"226373"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703039"	""	"0"	"440.86"	"0"	"3.61"	"BDBM147749"	"N#C[C@H]1C[C@@H](NCC(F)F)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(F)c(Cl)c2)n1"	"IC50"	"'='"	"41.0"	"nM"	"7.39"	""	"285683"	"UO_0000065"	"16.76"	"0.34"	"3.78"	"6.79"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702939"	""	"0"	"392.37"	"0"	"1.95"	"BDBM147641"	"N#C[C@H]1C[C@@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(OC(F)F)nc2)n1"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	"285911"	"UO_0000065"	"19.80"	"0.38"	"5.82"	"5.59"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL1835145"	""	"0"	"442.45"	"0"	"4.36"	"56"	"Cn1cc(-c2ccc3c(c2)[nH]c2c(C(N)=O)cnc(N[C@H](C4CCC4)C(F)(F)F)c23)cn1"	"IC50"	"'='"	"350.0"	"nM"	"6.46"	""	""	"UO_0000065"	"14.59"	"0.28"	"2.10"	"6.35"	"False"	"CHEMBL1840130"	"Inhibition of JAK2-mediated STAT5 phosphorylation in human HEL 92.1.7 irf1-bla cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308090"	""
"CHEMBL1835139"	""	"0"	"388.48"	"0"	"3.82"	"50"	"CCC(Nc1ncc(C(N)=O)c2[nH]c3cc(-c4cnn(C)c4)ccc3c12)C1CC1"	"IC50"	"'='"	"45.0"	"nM"	"7.35"	""	""	"UO_0000065"	"18.91"	"0.35"	"3.53"	"7.23"	"False"	"CHEMBL1840130"	"Inhibition of JAK2-mediated STAT5 phosphorylation in human HEL 92.1.7 irf1-bla cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308090"	""
"CHEMBL1835039"	""	"0"	"389.50"	"0"	"4.67"	"42"	"C[C@H](Nc1ccc(C(N)=O)c2[nH]c3cc(-c4cnn(C)c4)ccc3c12)C(C)(C)C"	"IC50"	"'='"	"370.0"	"nM"	"6.43"	""	""	"UO_0000065"	"16.51"	"0.30"	"1.76"	"7.25"	"False"	"CHEMBL1840130"	"Inhibition of JAK2-mediated STAT5 phosphorylation in human HEL 92.1.7 irf1-bla cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308090"	""
"CHEMBL3651007"	""	"0"	"421.46"	"0"	"3.02"	"BDBM153183"	"C=C(C)C(=O)Nc1cc(-c2ncnc3[nH]cc(C(=O)OCC)c23)ccc1C(=O)N(C)C"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294131"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645085"	""	"0"	"469.92"	"1"	"5.13"	"BDBM99858"	"FC(F)COc1ccc(Cl)cc1-c1cccn2nc(Nc3ccc4c(c3)CCNCC4)nc12"	"IC50"	"'='"	"43.97"	"nM"	"7.36"	""	"216527"	"UO_0000065"	"15.66"	"0.30"	"2.23"	"11.59"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703079"	""	"0"	"425.39"	"0"	"2.64"	"BDBM147792"	"N#C[C@H]1C[C@@H](NCC(F)(F)F)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccnc(F)c2)n1"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	"285726"	"UO_0000065"	"18.33"	"0.35"	"5.16"	"6.41"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699468"	""	"0"	"325.37"	"0"	"1.95"	"BDBM147483"	"N#C[C@H]1CCC[C@@H](O)C1n1cc(C(N)=O)c(Nc2ccccc2)n1"	"IC50"	"'='"	"1000.0"	"nM"	"6.00"	""	"285408"	"UO_0000065"	"18.44"	"0.34"	"4.05"	"5.13"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3694577"	""	"0"	"338.80"	"0"	"4.38"	"BDBM125898"	"Clc1cnc2nc1NCc1cccc(c1)OCc1cccc(c1)N2"	"IC50"	"'='"	"49.0"	"nM"	"7.31"	""	"255671"	"UO_0000065"	"21.58"	"0.42"	"2.93"	"12.37"	"False"	"CHEMBL3707544"	"In Vitro Kinase Assay: One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Biochemistry 1999, 269, 94-104. The catalytic domains of human JAK1 (a.a. 837-1142), JAK2 (a.a. 828-1132) and JAK3 (a.a. 781-1124) with an N-terminal His tag were expressed using baculovirus in insect cells and purified. The catalytic activity of JAK1, JAK2 or JAK3 was assayed by measuring the phosphorylation of a biotinylated peptide. The phosphorylated peptide was detected by homogenous time resolved fluorescence (HTRF). IC50s of compounds were measured for each kinase in the reactions that contain the enzyme, ATP and 500 nM peptide in 50 mM Tris (pH 7.8) buffer with 100 mM NaCl, 5 mM DTT, and 0.1 mg/mL (0.01%) BSA. The ATP concentration in the reactions was 90 uM for JAK1, 30 uM for JAK2 and 3 uM for JAK3. Reactions were carried out at room temperature for 1 hr and then stopped with 20 uL 45 mM EDTA."	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639093"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3039513"	"DECERNOTINIB"	"2"	"392.39"	"0"	"3.28"	"7"	"CC[C@@](C)(Nc1ccnc(-c2c[nH]c3ncccc23)n1)C(=O)NCC(F)(F)F"	"IC50"	"'='"	"24.0"	"nM"	"7.62"	""	""	"UO_0000065"	"19.42"	"0.37"	"4.34"	"7.97"	"False"	"CHEMBL3299230"	"Inhibition of JAK2 (unknown origin) using poly(Glu)4Tyr as substrate assessed as 33P incorporation after 20 mins by scintillation counting analysis in presence of radiolabelled ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3297690"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL4225507"	""	"0"	"567.68"	"2"	"5.07"	"18"	"CCNC(=O)c1cc2c(-c3cccc(OCCCCCn4cc(-c5ncnc6[nH]ccc56)cn4)c3)nc(N)nc2s1"	"IC50"	"'='"	"1090.0"	"nM"	"5.96"	""	""	"UO_0000065"	"10.50"	"0.20"	"0.89"	"3.99"	"False"	"CHEMBL4222523"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma33P]-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219149"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2018"	"None"	""
"CHEMBL4227395"	""	"0"	"636.57"	"2"	"6.38"	"26"	"CCNC(=O)c1cc2c(-c3cc(OCCCCCn4cc(-c5ncnc6[nH]ccc56)cn4)c(Cl)cc3Cl)nc(N)nc2s1"	"IC50"	"'='"	"3450.0"	"nM"	"5.46"	""	""	"UO_0000065"	"8.58"	"0.17"	"-0.92"	"3.65"	"False"	"CHEMBL4222523"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma33P]-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219149"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2018"	"None"	""
"CHEMBL4226814"	""	"0"	"927.92"	"4"	"9.30"	"46"	"CCNC(=O)c1cc2c(-c3cc(OCCCCCCn4cc(-c5nc(Nc6ccc(NC(=O)CCCCCCC(=O)NO)cc6)nc6[nH]ccc56)cn4)c(Cl)cc3Cl)nc(N)nc2s1"	"IC50"	"'='"	"14100.0"	"nM"	"4.85"	""	""	"UO_0000065"	"5.23"	"0.10"	"-4.45"	"2.02"	"False"	"CHEMBL4222523"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma33P]-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219149"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2018"	"None"	""
"CHEMBL3645544"	""	"0"	"289.34"	"0"	"3.65"	"BDBM107129"	"O=C(Nc1cccc(-c2cnc3ccccc3n2)c1)C1CC1"	"IC50"	"'='"	"25000.0"	"nM"	"4.60"	""	"226367"	"UO_0000065"	"15.91"	"0.29"	"0.95"	"8.39"	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642382"	""	"0"	"533.70"	"1"	"4.29"	"BDBM99658"	"CN1CCC(c2ccc(Nc3nc4c(NCc5ccccc5CN(C)S(C)(=O)=O)cccn4n3)cc2)CC1"	"IC50"	"'='"	"115.68"	"nM"	"6.94"	""	"216348"	"UO_0000065"	"13.00"	"0.25"	"2.65"	"7.31"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647876"	""	"0"	"484.99"	"0"	"3.09"	"BDBM147988"	"CC(C)(O)C1CN(C(=O)[C@@H]2CC[C@@H](n3cc(C(N)=O)c(Nc4ccc(Cl)cc4)n3)[C@H](C#N)C2)C1"	"IC50"	"'='"	"59.0"	"nM"	"7.23"	""	"285923"	"UO_0000065"	"14.91"	"0.29"	"4.14"	"5.27"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665214"	""	"0"	"513.67"	"1"	"2.03"	"BDBM112614"	"CC(C)CS(=O)(=O)N1CCC[C@H](Nc2nc(N3CCN(C)CC3)ncc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.0585"	"nM"	"10.23"	""	"233851"	"UO_0000065"	"19.92"	"0.39"	"8.20"	"8.30"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL4111738"	""	"0"	"454.00"	"0"	"4.24"	"BDBM147939"	"N#C[C@H]1CC([N+]2(CC3CC3)CCC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"28.0"	"nM"	"7.55"	""	"285873"	"UO_0000065"	"16.64"	"0.32"	"3.31"	"7.81"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642321"	""	"0"	"462.58"	"0"	"3.30"	"BDBM99593"	"CN1CCN(c2cccc(Nc3nc4cccc(-c5ccc(S(C)(=O)=O)cc5)n4n3)c2)CC1"	"IC50"	"'='"	"2.8"	"nM"	"8.55"	""	"216283"	"UO_0000065"	"18.49"	"0.35"	"5.25"	"10.32"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3645116"	""	"0"	"379.45"	"0"	"2.81"	"BDBM99890"	"CS(=O)(=O)c1ccc(-c2cccn3nc(NCc4ccccn4)nc23)cc1"	"IC50"	"'='"	"6499.0"	"nM"	"5.19"	""	"216558"	"UO_0000065"	"13.67"	"0.26"	"2.38"	"5.81"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647864"	""	"0"	"394.26"	"0"	"3.26"	"BDBM147975"	"N#C[C@H]1C[C@@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)c(Cl)c2)n1"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	"285909"	"UO_0000065"	"19.53"	"0.40"	"4.44"	"6.58"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665203"	""	"0"	"499.65"	"0"	"1.78"	"BDBM112602"	"CN(C)C1CCN(c2ncc(-c3cnc4[nH]ccc4n3)c(N[C@H]3CCCN(S(C)(=O)=O)C3)n2)CC1"	"IC50"	"'='"	"0.1373"	"nM"	"9.86"	""	"233839"	"UO_0000065"	"19.74"	"0.38"	"8.08"	"8.00"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647916"	""	"0"	"450.95"	"0"	"2.50"	"BDBM148028"	"CN([C@@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@@H](C#N)C1)S(C)(=O)=O"	"IC50"	"'='"	"46.0"	"nM"	"7.34"	""	"285965"	"UO_0000065"	"16.27"	"0.33"	"4.84"	"5.47"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642418"	""	"0"	"534.69"	"1"	"3.79"	"BDBM99696"	"CC(Nc1cccn2nc(Nc3ccc(N4CCN(C)CC4)cc3)nc12)c1ccccc1N(C)S(C)(=O)=O"	"IC50"	"'='"	"418.16"	"nM"	"6.38"	""	"216385"	"UO_0000065"	"11.93"	"0.23"	"2.59"	"6.50"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3655086"	""	"0"	"351.43"	"0"	"0.49"	"BDBM159753"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)CC2COC2)C1"	"IC50"	"'='"	"933.0"	"nM"	"6.03"	""	"302563"	"UO_0000065"	"17.16"	"0.34"	"5.54"	"6.02"	"True"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3658093"	""	"0"	"657.70"	"2"	"5.32"	"BDBM148351"	"Cc1ccc(NC(=O)c2cccc(C(F)(F)F)c2)cc1N1CCc2nc(Nc3ccc(CC(=O)N4CCN(C)CC4)cc3)ncc2C1=O"	"IC50"	"'='"	"61.0"	"nM"	"7.21"	""	"286780"	"UO_0000065"	"10.97"	"0.21"	"1.89"	"6.51"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642336"	""	"0"	"477.59"	"0"	"3.37"	"BDBM99608"	"CN1CCN(c2ccc(Nc3nc4c(Nc5cccc(S(C)(=O)=O)c5)cccn4n3)cc2)CC1"	"IC50"	"'='"	"326.56"	"nM"	"6.49"	""	"216298"	"UO_0000065"	"13.58"	"0.26"	"3.12"	"6.84"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652344"	""	"0"	"421.57"	"0"	"2.25"	"BDBM113155"	"COC[C@@H]1CCN(S(=O)(=O)C[C@H]2CC[C@H](N(C)c3ncnc4[nH]ccc34)CC2)C1"	"IC50"	"'='"	"22.5"	"nM"	"7.65"	""	"234598"	"UO_0000065"	"18.14"	"0.36"	"5.40"	"8.37"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3645541"	""	"0"	"346.43"	"0"	"3.72"	"BDBM107125"	"O=C(CN1CCCCC1)Nc1cccc(-c2cnc3ccccc3n2)c1"	"IC50"	"'>'"	"20000.0"	"nM"	""	""	"226362"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647907"	""	"0"	"444.90"	"0"	"3.04"	"BDBM148019"	"N#C[C@H]1C[C@@H](C(=O)N2CC(F)C2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"23.0"	"nM"	"7.64"	""	"285954"	"UO_0000065"	"17.17"	"0.34"	"4.60"	"6.53"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647735"	""	"0"	"528.53"	"1"	"3.30"	"BDBM147838"	"N#C[C@H]1CC(N2CC[C@@H](F)C2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	"285772"	"UO_0000065"	"14.65"	"0.29"	"4.44"	"5.77"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702971"	""	"0"	"356.41"	"0"	"2.32"	"BDBM147679"	"CN[C@H]1CCC(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"56.0"	"nM"	"7.25"	""	"285612"	"UO_0000065"	"20.35"	"0.38"	"4.93"	"6.67"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652296"	""	"0"	"421.57"	"0"	"2.13"	"BDBM113105"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCC(C)(O)CC2)CC1"	"IC50"	"'='"	"42.1"	"nM"	"7.38"	""	"234549"	"UO_0000065"	"17.50"	"0.35"	"5.25"	"7.20"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3622376"	""	"0"	"242.24"	"0"	"0.62"	"84"	"c1nc(-c2cn(CC3CO3)nn2)c2cc[nH]c2n1"	"IC50"	"'='"	"2451.0"	"nM"	"5.61"	""	""	"UO_0000065"	"23.16"	"0.43"	"4.99"	"6.62"	"True"	"CHEMBL3626583"	"Inhibition of JAK2 (unknown origin) after 20 mins by radiometric analysis in presence of [gamma33P]-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621113"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL3622141"	""	"0"	"372.43"	"0"	"0.55"	"5"	"CNc1nc2c(cc(C(=O)N(C)C3CC3)n2C[C@H](O)CO)c2c1ncn2C"	"IC50"	"'='"	"450.0"	"nM"	"6.35"	""	""	"UO_0000065"	"17.04"	"0.32"	"5.80"	"5.85"	"False"	"CHEMBL3625473"	"Inhibition of JAK2 (unknown origin) using 5-FAMKKKKEEIYFFFG-OH as substrate after 60 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621098"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3622140"	""	"0"	"388.47"	"0"	"1.19"	"4"	"CCN(C(=O)c1cc2c3c(ncn3C)c(NC)nc2n1C[C@H](O)CO)C(C)C"	"IC50"	"'='"	"43.0"	"nM"	"7.37"	""	""	"UO_0000065"	"18.96"	"0.36"	"6.18"	"6.79"	"False"	"CHEMBL3625473"	"Inhibition of JAK2 (unknown origin) using 5-FAMKKKKEEIYFFFG-OH as substrate after 60 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621098"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3120960"	""	"0"	"320.33"	"0"	"3.07"	"1"	"Cn1c(-c2c[nH]nn2)nc(-c2ccc(F)cc2)c1-c1ccncc1"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3363474"	"Inhibition of JAK2 (unknown origin) by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352554"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3314277"	""	"0"	"442.45"	"0"	"3.49"	"21"	"O=c1cc(-c2[nH]c(-c3ccc(-c4cn(CCO)nn4)cc3)nc2-c2ccc(F)cc2)cc[nH]1"	"IC50"	"'='"	"500.0"	"nM"	"6.30"	""	""	"UO_0000065"	"14.24"	"0.26"	"2.81"	"5.60"	"False"	"CHEMBL3363474"	"Inhibition of JAK2 (unknown origin) by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352554"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL4536858"	""	"0"	"538.63"	"1"	"2.06"	"14q"	"NS(=O)(=O)c1ccc(NC(=O)N2CCN(c3ccnc(Nc4ccc(N5CCOCC5)cc4)n3)CC2)cc1"	"IC50"	"'='"	"9.3"	"nM"	"8.03"	""	""	"UO_0000065"	"14.91"	"0.29"	"5.97"	"5.50"	"False"	"CHEMBL4362531"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain (826 to 1132 resiudes) expressed in baculovirus expression system using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition measured after 1 hr in presence of ATP by mobility shift assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4359878"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2019"	"None"	""
"CHEMBL3647810"	""	"0"	"430.94"	"0"	"3.24"	"BDBM147913"	"COCC(C)N[C@H]1CCC(n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"33.0"	"nM"	"7.48"	""	"285847"	"UO_0000065"	"17.36"	"0.34"	"4.24"	"6.34"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652394"	""	"0"	"395.55"	"0"	"2.29"	"BDBM113206"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCSC2)CC1"	"IC50"	"'='"	"29.5"	"nM"	"7.53"	""	"234649"	"UO_0000065"	"19.04"	"0.40"	"5.24"	"9.16"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3645090"	""	"0"	"541.00"	"2"	"5.52"	"BDBM99863"	"CN(C)C(=O)N1CCc2ccc(Nc3nc4c(-c5cc(Cl)ccc5OCC(F)F)cccn4n3)cc2CC1"	"IC50"	"'='"	"198.22"	"nM"	"6.70"	""	"216532"	"UO_0000065"	"12.39"	"0.24"	"1.18"	"8.94"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3644980"	""	"0"	"535.55"	"2"	"5.80"	"BDBM99731"	"CC(C)(C)OC(=O)N1CCc2ccc(Nc3nc4c(-c5cccc6c5OC(F)(F)O6)cccn4n3)cc2CC1"	"IC50"	"'='"	"2114.62"	"nM"	"5.67"	""	"216420"	"UO_0000065"	"10.60"	"0.20"	"-0.13"	"6.29"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652318"	""	"0"	"483.64"	"0"	"3.03"	"BDBM113128"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCC(Cc3ncccn3)CC2)CC1"	"IC50"	"'='"	"17.7"	"nM"	"7.75"	""	"234571"	"UO_0000065"	"16.03"	"0.31"	"4.72"	"7.18"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3699541"	""	"0"	"359.82"	"0"	"2.60"	"BDBM147559"	"N#C[C@H]1C[C@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	"285595"	"UO_0000065"	"22.12"	"0.43"	"5.36"	"6.80"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645032"	""	"0"	"433.94"	"0"	"4.88"	"BDBM99794"	"CCOc1ccc(Cl)cc1-c1cccn2nc(Nc3ccc4c(c3)CCNCC4)nc12"	"IC50"	"'='"	"33.44"	"nM"	"7.48"	""	"216472"	"UO_0000065"	"17.23"	"0.33"	"2.60"	"11.78"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3665136"	""	"0"	"400.51"	"0"	"2.49"	"BDBM112523"	"CC(C)CS(=O)(=O)N1CC[C@@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.662"	"nM"	"9.18"	""	"233762"	"UO_0000065"	"22.92"	"0.45"	"6.69"	"8.84"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3622131"	""	"0"	"410.52"	"0"	"3.16"	"12"	"CCn1c(C(=O)N(C2CC2)C2CC2)cc2c3c(ncn3C)c(NCCCOC)nc21"	"IC50"	"'='"	"1300.0"	"nM"	"5.89"	""	""	"UO_0000065"	"14.34"	"0.27"	"2.73"	"7.62"	"False"	"CHEMBL3625474"	"Inhibition of JAK2 in human SET2 cells assessed as inhibition of cell proliferation after 72 hrs by [3H]-thymidine incorporation assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621098"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3622136"	""	"0"	"435.56"	"0"	"4.22"	"17"	"CCn1c(C(=O)N(C2CC2)C2CC2)cc2c3c(ncn3C)c(Nc3ncc(C)s3)nc21"	"IC50"	"'='"	"25.0"	"nM"	"7.60"	""	""	"UO_0000065"	"17.45"	"0.33"	"3.38"	"9.40"	"False"	"CHEMBL3625474"	"Inhibition of JAK2 in human SET2 cells assessed as inhibition of cell proliferation after 72 hrs by [3H]-thymidine incorporation assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621098"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3652289"	""	"0"	"435.55"	"0"	"2.08"	"BDBM113098"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCCC(C(=O)O)C2)CC1"	"IC50"	"'='"	"7.71"	"nM"	"8.11"	""	"234542"	"UO_0000065"	"18.63"	"0.37"	"6.03"	"6.79"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3644995"	""	"0"	"439.52"	"0"	"3.68"	"BDBM99747"	"CN1CCN(c2cccc(Nc3nc4c(OCc5ccccc5C#N)cccn4n3)c2)CC1"	"IC50"	"'='"	"26.89"	"nM"	"7.57"	""	"216435"	"UO_0000065"	"17.22"	"0.31"	"3.89"	"9.26"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647761"	""	"0"	"420.44"	"0"	"3.54"	"BDBM147864"	"CN(C)[C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(C(F)(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	"285798"	"UO_0000065"	"18.68"	"0.36"	"4.31"	"7.86"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3649610"	""	"0"	"439.44"	"0"	"3.91"	"BDBM130304"	"NC(=O)c1cc(-c2cccc(C(F)(F)F)c2)nc2c1[nH]c1cc(N3CCNCC3)ccc12"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"262090"	"UO_0000065"	"18.71"	"0.35"	"4.31"	"9.45"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649623"	""	"0"	"378.36"	"0"	"3.93"	"BDBM130317"	"COc1ccc(-c2cc(C(N)=O)c3[nH]c4cc(C(=O)O)ccc4c3c2)cc1F"	"IC50"	"'='"	"111.0"	"nM"	"6.96"	""	"262103"	"UO_0000065"	"18.38"	"0.34"	"3.02"	"6.60"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL1835152"	""	"0"	"559.57"	"1"	"3.26"	"64"	"NC(=O)c1cnc(N[C@H](C2CC2)C(F)(F)F)c2c1[nH]c1cc(-c3ccc(N4CCS(=O)(=O)CC4)nn3)ccc12"	"IC50"	"'='"	"120.0"	"nM"	"6.92"	""	""	"UO_0000065"	"12.37"	"0.24"	"3.66"	"4.71"	"False"	"CHEMBL1840130"	"Inhibition of JAK2-mediated STAT5 phosphorylation in human HEL 92.1.7 irf1-bla cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308090"	""
"CHEMBL4551587"	""	"0"	"406.49"	"0"	"2.17"	"13"	"CCNC(=O)c1ccc(Nc2nccc(N3C[C@@H]4C[C@H](C3)N4C(=O)C3CC3)n2)cc1"	"IC50"	"'='"	"7851.0"	"nM"	"5.11"	""	""	"UO_0000065"	"12.56"	"0.23"	"2.94"	"5.64"	"False"	"CHEMBL4411595"	"Inhibition of human JAK2 using fluorescence labeled peptide as substrate and using 1 mM ATP by microfluidic based mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4411260"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3918943"	""	"0"	"406.33"	"0"	"3.71"	"BDBM198607"	"FC(F)(F)C(N[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1)C(F)(F)F"	"IC50"	"'='"	"190.0"	"nM"	"6.72"	""	"352685"	"UO_0000065"	"16.54"	"0.33"	"3.01"	"9.48"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3927961"	""	"0"	"310.41"	"0"	"2.63"	"BDBM198613"	"c1cc2c(ncn3nnc([C@H]4CC[C@@H](CNC5CC5)CC4)c23)[nH]1"	"IC50"	"'='"	"560.0"	"nM"	"6.25"	""	"352691"	"UO_0000065"	"20.14"	"0.37"	"3.62"	"8.82"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3913565"	""	"0"	"431.50"	"0"	"3.72"	"BDBM198617"	"Cc1ccc(CN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C(=O)CC#N)o1"	"IC50"	"'='"	"40.0"	"nM"	"7.40"	""	"352695"	"UO_0000065"	"17.14"	"0.32"	"3.68"	"6.37"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3924572"	""	"0"	"462.40"	"0"	"4.22"	"BDBM198618"	"O=C(CC(F)(F)F)N(CC(F)(F)F)C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	"352696"	"UO_0000065"	"16.92"	"0.33"	"3.60"	"9.88"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3960109"	""	"0"	"354.41"	"0"	"1.78"	"BDBM198482"	"O=C1OCCC1NC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"44.0"	"nM"	"7.36"	""	"352560"	"UO_0000065"	"20.76"	"0.39"	"5.58"	"7.57"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3959556"	""	"0"	"308.39"	"0"	"2.10"	"BDBM198536"	"C#CCNC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"44.0"	"nM"	"7.36"	""	"352614"	"UO_0000065"	"23.85"	"0.44"	"5.26"	"10.38"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3976356"	""	"0"	"467.62"	"0"	"4.12"	"BDBM198539"	"CC(C)(C)OC(=O)NCC1CCN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)CC1"	"IC50"	"'='"	"370.0"	"nM"	"6.43"	""	"352617"	"UO_0000065"	"13.75"	"0.26"	"2.31"	"6.40"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3949242"	""	"0"	"382.39"	"0"	"2.39"	"BDBM198546"	"OC(CNC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1)C(F)(F)F"	"IC50"	"'='"	"63.0"	"nM"	"7.20"	""	"352624"	"UO_0000065"	"18.83"	"0.36"	"4.81"	"7.90"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647715"	""	"0"	"432.45"	"0"	"3.73"	"BDBM147817"	"N#C[C@H]1C[C@@H](NC2CC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"22.0"	"nM"	"7.66"	""	"285751"	"UO_0000065"	"17.71"	"0.34"	"3.93"	"7.04"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665186"	""	"0"	"416.51"	"0"	"1.32"	"BDBM112580"	"CN(C)c1ncc(-c2cnc3[nH]ccc3n2)c(N[C@H]2CCCN(S(C)(=O)=O)C2)n1"	"IC50"	"'='"	"0.1373"	"nM"	"9.86"	""	"233817"	"UO_0000065"	"23.68"	"0.46"	"8.54"	"8.22"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3702980"	""	"0"	"500.50"	"1"	"1.83"	"BDBM147690"	"N#C[C@H]1CC(NCCO)CCC1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	"285623"	"UO_0000065"	"15.90"	"0.32"	"6.13"	"4.88"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3330127"	""	"0"	"415.30"	"0"	"3.86"	"30"	"NC(=O)c1cc(-c2ccnc(N)n2)[nH]c1-c1cc(C(F)(F)F)ccc1C(F)(F)F"	"IC50"	"'='"	"21.0"	"nM"	"7.68"	""	""	"UO_0000065"	"18.49"	"0.36"	"3.82"	"6.94"	"False"	"CHEMBL3374493"	"Inhibition of recombinant human JAK2 (808-1132 residues) using LPLDKDYYVVREPGQ as substrate by radiometric assay in presence of [33P]-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330112"	""	"0"	"417.90"	"0"	"4.61"	"15"	"Cc1ccc(Cl)cc1-c1[nH]c(-c2ccnc(N)n2)cc1C(=O)NCc1ccccc1"	"IC50"	"'='"	"154.0"	"nM"	"6.81"	""	""	"UO_0000065"	"16.30"	"0.31"	"2.20"	"7.05"	"False"	"CHEMBL3374493"	"Inhibition of recombinant human JAK2 (808-1132 residues) using LPLDKDYYVVREPGQ as substrate by radiometric assay in presence of [33P]-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330111"	""	"0"	"383.88"	"0"	"4.07"	"14"	"Cc1ccc(Cl)cc1-c1[nH]c(-c2ccnc(N)n2)cc1C(=O)NCC(C)C"	"IC50"	"'='"	"384.0"	"nM"	"6.42"	""	""	"UO_0000065"	"16.71"	"0.32"	"2.35"	"6.64"	"False"	"CHEMBL3374493"	"Inhibition of recombinant human JAK2 (808-1132 residues) using LPLDKDYYVVREPGQ as substrate by radiometric assay in presence of [33P]-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3665182"	""	"0"	"493.62"	"0"	"1.68"	"BDBM112576"	"CC(C)CS(=O)(=O)N1CCC[C@H](Nc2nc(S(C)(=O)=O)ncc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.0646"	"nM"	"10.19"	""	"233813"	"UO_0000065"	"20.64"	"0.42"	"8.51"	"6.75"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3354190"	""	"0"	"367.46"	"0"	"3.16"	"9"	"COC1CCN(c2nccc(Nc3cc4c(cn3)ncn4C(C)C)n2)CC1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3375809"	"Inhibition of Jak2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351701"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL3354192"	""	"0"	"367.46"	"0"	"3.23"	"11"	"COC1CCN(c2nccc(Nc3cc4c(C(C)C)n[nH]c4cn3)n2)CC1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3375809"	"Inhibition of Jak2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351701"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL4436287"	""	"0"	"393.45"	"0"	"1.53"	"10"	"CCNC(=O)c1ccc(Nc2nccc(N3CCN(C(=O)CC#N)CC3)n2)cc1"	"IC50"	"'='"	"1083.0"	"nM"	"5.96"	""	""	"UO_0000065"	"15.16"	"0.28"	"4.44"	"5.22"	"False"	"CHEMBL4411532"	"Inhibition of human JAK2 using fluorescence labeled peptide as substrate and using ATP at its Km level by microfluidic based mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4411260"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3330108"	""	"0"	"384.87"	"0"	"2.63"	"11"	"CNCCNC(=O)c1cc(-c2ccnc(N)n2)[nH]c1-c1cc(Cl)ccc1C"	"IC50"	"'>'"	"3000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3374497"	"Inhibition of JAK2 V617F mutant in human SET2 cells"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330123"	""	"0"	"343.77"	"0"	"2.48"	"26"	"COc1ccc(Cl)cc1-c1[nH]c(-c2ccnc(N)n2)cc1C(N)=O"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL3374497"	"Inhibition of JAK2 V617F mutant in human SET2 cells"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330131"	""	"0"	"355.83"	"0"	"3.60"	"34"	"CC(C)c1ccc(Cl)cc1-c1[nH]c(-c2ccnc(N)n2)cc1C(N)=O"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL3374497"	"Inhibition of JAK2 V617F mutant in human SET2 cells"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330131"	""	"0"	"355.83"	"0"	"3.60"	"34"	"CC(C)c1ccc(Cl)cc1-c1[nH]c(-c2ccnc(N)n2)cc1C(N)=O"	"IC50"	"'='"	"150.0"	"nM"	"6.82"	""	""	"UO_0000065"	"19.18"	"0.37"	"3.22"	"6.17"	"False"	"CHEMBL3374493"	"Inhibition of recombinant human JAK2 (808-1132 residues) using LPLDKDYYVVREPGQ as substrate by radiometric assay in presence of [33P]-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330116"	""	"0"	"355.83"	"0"	"3.27"	"19"	"CCn1c(-c2ccnc(N)n2)cc(C(N)=O)c1-c1cc(Cl)ccc1C"	"IC50"	"'='"	"1537.0"	"nM"	"5.81"	""	""	"UO_0000065"	"16.34"	"0.32"	"2.54"	"5.82"	"False"	"CHEMBL3374493"	"Inhibition of recombinant human JAK2 (808-1132 residues) using LPLDKDYYVVREPGQ as substrate by radiometric assay in presence of [33P]-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330100"	""	"0"	"293.33"	"0"	"2.13"	"2"	"Cc1ccccc1-c1[nH]c(-c2ccnc(N)n2)cc1C(N)=O"	"IC50"	"'='"	"695.0"	"nM"	"6.16"	""	""	"UO_0000065"	"20.99"	"0.38"	"4.03"	"5.56"	"False"	"CHEMBL3374493"	"Inhibition of recombinant human JAK2 (808-1132 residues) using LPLDKDYYVVREPGQ as substrate by radiometric assay in presence of [33P]-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL1934341"	""	"0"	"456.55"	"0"	"3.30"	"3g"	"NC(=O)CN1CCC(c2ccc(Nc3ncc4ccc(-c5cccc(CO)c5)n4n3)cc2)CC1"	"IC50"	"'='"	"0.27"	"nM"	"9.57"	""	""	"UO_0000065"	"20.96"	"0.38"	"6.27"	"8.80"	"False"	"CHEMBL1936085"	"Inhibition of human recombinant JAK2 expressed in baculovirus expression system after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL1934342"	""	"0"	"504.62"	"1"	"3.21"	"3h"	"CS(=O)(=O)c1ccc(-c2ccc3cnc(Nc4ccc(C5CCN(CC(N)=O)CC5)cc4)nn23)cc1"	"IC50"	"'='"	"0.22"	"nM"	"9.66"	""	""	"UO_0000065"	"19.14"	"0.37"	"6.45"	"7.87"	"False"	"CHEMBL1936085"	"Inhibition of human recombinant JAK2 expressed in baculovirus expression system after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL1934343"	""	"0"	"504.62"	"1"	"3.21"	"3i"	"CS(=O)(=O)c1cccc(-c2ccc3cnc(Nc4ccc(C5CCN(CC(N)=O)CC5)cc4)nn23)c1"	"IC50"	"'='"	"0.52"	"nM"	"9.28"	""	""	"UO_0000065"	"18.40"	"0.35"	"6.07"	"7.57"	"False"	"CHEMBL1936085"	"Inhibition of human recombinant JAK2 expressed in baculovirus expression system after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL1934344"	""	"0"	"534.65"	"1"	"2.60"	"3j"	"CN(c1ncccc1-c1ccc2cnc(Nc3ccc(C4CCN(CC(N)=O)CC4)cc3)nn12)S(C)(=O)=O"	"IC50"	"'='"	"2.1"	"nM"	"8.68"	""	""	"UO_0000065"	"16.23"	"0.31"	"6.08"	"6.25"	"False"	"CHEMBL1936085"	"Inhibition of human recombinant JAK2 expressed in baculovirus expression system after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL1934346"	""	"0"	"428.50"	"0"	"2.59"	"3l"	"NC(=O)CN1CCC(c2ccc(Nc3ncc4ccc(-c5ncccn5)n4n3)cc2)CC1"	"IC50"	"'='"	"85.0"	"nM"	"7.07"	""	""	"UO_0000065"	"16.50"	"0.30"	"4.48"	"6.18"	"False"	"CHEMBL1936085"	"Inhibition of human recombinant JAK2 expressed in baculovirus expression system after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL1934351"	""	"0"	"477.57"	"0"	"4.35"	"3q"	"NC(=O)CN1CCC(c2ccc(Nc3ncc4ccc(-c5cccc6cccnc56)n4n3)cc2)CC1"	"IC50"	"'='"	"6.3"	"nM"	"8.20"	""	""	"UO_0000065"	"17.17"	"0.31"	"3.85"	"8.08"	"False"	"CHEMBL1936085"	"Inhibition of human recombinant JAK2 expressed in baculovirus expression system after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL1934345"	""	"0"	"457.54"	"0"	"3.21"	"3k"	"COc1cccnc1-c1ccc2cnc(Nc3ccc(C4CCN(CC(N)=O)CC4)cc3)nn12"	"IC50"	"'='"	"1140.0"	"nM"	"5.94"	""	""	"UO_0000065"	"12.99"	"0.24"	"2.73"	"5.37"	"False"	"CHEMBL1936009"	"Inhibition of JAK2 in GM-CSF-stimulated human TF1 cells preincubated for 1 hr prior to challenge"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3307972"	""
"CHEMBL3799882"	""	"0"	"448.57"	"0"	"3.45"	"15c"	"Cn1c(C(=O)NCCN2CCCC2)cc2c(-c3ccc(NC(=O)C(C)(C)C)cc3)ncnc21"	"IC50"	"'='"	"300.0"	"nM"	"6.52"	""	""	"UO_0000065"	"14.54"	"0.27"	"3.07"	"7.08"	"False"	"CHEMBL3802364"	"Inhibition of JAK2 in GMCSF-stimulated human TF1 cells assessed as suppression of STAT5 phosphorylation preincubated for 2 hrs followed by GMCSF stimulation for 50 mins by FACS reader analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"CHEMBL3307972"	""
"CHEMBL3798686"	""	"0"	"436.52"	"0"	"2.05"	"16a"	"CC(=O)Nc1ccc(-c2ncnc3c2cc(C(=O)NCCCN2CCOCC2)n3C)cc1"	"IC50"	"'='"	"9600.0"	"nM"	"5.02"	""	""	"UO_0000065"	"11.49"	"0.21"	"2.97"	"4.95"	"False"	"CHEMBL3802364"	"Inhibition of JAK2 in GMCSF-stimulated human TF1 cells assessed as suppression of STAT5 phosphorylation preincubated for 2 hrs followed by GMCSF stimulation for 50 mins by FACS reader analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"CHEMBL3307972"	""
"CHEMBL4225073"	""	"0"	"324.39"	"0"	"1.69"	"8"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(C(=O)CC#N)CC12CCC2"	"IC50"	"'='"	"450.0"	"nM"	"6.35"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4227865"	""	"0"	"298.35"	"0"	"1.30"	"9"	"CCN(c1ncnc2[nH]ccc12)[C@@H]1CCN(C(=O)CC#N)C1"	"IC50"	"'='"	"1300.0"	"nM"	"5.89"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4225210"	""	"0"	"366.45"	"0"	"0.05"	"42"	"CN(c1ncnc2[nH]ccc12)[C@@H]1CCN(S(=O)(=O)N2CCOCC2)C1"	"IC50"	"'='"	"4400.0"	"nM"	"5.36"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"1"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"77.4"	"nM"	"7.11"	""	""	"UO_0000065"	"22.76"	"0.42"	"5.57"	"8.00"	"False"	"CHEMBL3299201"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3297690"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL4280010"	""	"0"	"348.41"	"0"	"2.09"	"19"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(C(=O)c2cccnc2)CC12CC2"	"IC50"	"'='"	"7800.0"	"nM"	"5.11"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4292627"	""	"0"	"372.43"	"0"	"2.57"	"22"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(C(=O)c2ccc(C#N)cc2)CC12CC2"	"IC50"	"'='"	"4500.0"	"nM"	"5.35"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4281921"	""	"0"	"401.47"	"0"	"2.39"	"42"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(S(=O)(=O)c2ccccc2F)CC12CC2"	"IC50"	"'='"	"97.0"	"nM"	"7.01"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4098975"	""	"0"	"504.60"	"1"	"4.11"	"38"	"O=C(CCCCCCC(=O)Nc1ccc(NCCCn2cc(-c3ncnc4[nH]ccc34)cn2)cc1)NO"	"IC50"	"'='"	"265.0"	"nM"	"6.58"	""	""	"UO_0000065"	"13.03"	"0.24"	"2.47"	"4.39"	"False"	"CHEMBL4031305"	"Inhibition of human JAK2 using poly[Glu:Tyr] as substrate in presence of [gamma-33P]-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028864"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4483484"	""	"0"	"375.38"	"1"	"5.37"	"35"	"CCc1cc(O)c(F)cc1-c1cc(NP(=O)(CC)CC)c2cn[nH]c2c1"	"IC50"	"'='"	"3162.28"	"nM"	"5.50"	""	""	"UO_0000065"	"14.65"	"0.29"	"0.13"	"7.05"	"False"	"CHEMBL4478762"	"Inhibition of human His-tagged JAK2 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4477220"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2016"	"None"	""
"CHEMBL4516561"	""	"0"	"335.36"	"0"	"2.84"	"15"	"CCS(=O)(=O)Nc1cc(-c2ccc(O)c(F)c2)cc2[nH]ncc12"	"IC50"	"'='"	"7.943"	"nM"	"8.10"	""	""	"UO_0000065"	"24.15"	"0.48"	"5.26"	"8.52"	"False"	"CHEMBL4478762"	"Inhibition of human His-tagged JAK2 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4477220"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2016"	"None"	""
"CHEMBL3402479"	""	"0"	"328.76"	"0"	"1.97"	"5"	"Cc1ccc(Cl)cc1-n1nc(-c2ccnc(N)n2)cc1C(N)=O"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3404501"	"Inhibition of recombinant epitope-tagged JAK2 (808 to 1132) (unknown origin) using LPLDKDYYVVREPGQ as substrate by beta-countiing analysis in presence of 33P-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3400063"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3402477"	""	"0"	"285.74"	"0"	"3.08"	"3"	"Cc1ccc(Cl)cc1-c1ncc(-c2ccnc(N)n2)[nH]1"	"IC50"	"'='"	"1068.0"	"nM"	"5.97"	""	""	"UO_0000065"	"20.90"	"0.41"	"2.89"	"7.42"	"False"	"CHEMBL3404501"	"Inhibition of recombinant epitope-tagged JAK2 (808 to 1132) (unknown origin) using LPLDKDYYVVREPGQ as substrate by beta-countiing analysis in presence of 33P-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3400063"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL2208030"	""	"0"	"403.49"	"0"	"3.99"	"9e"	"CC(=O)Nc1ccc(-c2cc(C)nc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL2214784"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT3 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL4567992"	""	"0"	"331.40"	"0"	"3.01"	"10"	"CCS(=O)(=O)Nc1cc(-c2ccc(O)cc2C)cc2[nH]ncc12"	"IC50"	"'='"	"31.62"	"nM"	"7.50"	""	""	"UO_0000065"	"22.63"	"0.45"	"4.49"	"7.89"	"False"	"CHEMBL4478762"	"Inhibition of human His-tagged JAK2 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4477220"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2016"	"None"	""
"CHEMBL4593058"	""	"0"	"393.45"	"0"	"2.80"	"11c'"	"C=CC(=O)Nc1ccc(CNc2cc(Nc3cnn(CCOC)c3)ncn2)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4482009"	"Inhibition of human JAK2 using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and further incubated for 30 mins and subsequently measured after 1 hr by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480445"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4528217"	""	"0"	"432.53"	"0"	"4.02"	"13d"	"CCC(=O)Nc1ccc(CNc2cc(Nc3ccc(N4CCOCC4)cc3)ncn2)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4482009"	"Inhibition of human JAK2 using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and further incubated for 30 mins and subsequently measured after 1 hr by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480445"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL3622831"	""	"0"	"294.36"	"0"	"2.07"	"5h"	"Cc1ccc(-c2nc3cc(C(N)=O)ccc3n2CCN)cc1"	"IC50"	"'='"	"2600.0"	"nM"	"5.58"	""	""	"UO_0000065"	"18.97"	"0.35"	"3.52"	"6.42"	"False"	"CHEMBL3625898"	"Inhibition of JAK2 (unknown origin) using 35 uM of ATP and Tyr6 peptide by Z'-LYTE kinase assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621116"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL3649652"	""	"0"	"442.45"	"0"	"3.57"	"BDBM130347"	"N#Cc1cc(-c2cc(C(N)=O)c3[nH]c4cc(C(=O)N5CCOCC5)ccc4c3c2)ccc1F"	"IC50"	"'='"	"1006.0"	"nM"	"6.00"	""	"262133"	"UO_0000065"	"13.55"	"0.25"	"2.43"	"5.34"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3642361"	""	"0"	"491.62"	"0"	"3.24"	"BDBM99637"	"CN1CCN(c2ccc(Nc3nc4c(NCc5ccccc5S(C)(=O)=O)cccn4n3)cc2)CC1"	"IC50"	"'='"	"13.24"	"nM"	"7.88"	""	"216327"	"UO_0000065"	"16.02"	"0.31"	"4.64"	"8.30"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3655090"	""	"0"	"415.52"	"0"	"2.13"	"BDBM159757"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)c2cccc(C(C)(C)O)c2)C1"	"IC50"	"'='"	"5630.0"	"nM"	"5.25"	""	"302567"	"UO_0000065"	"12.63"	"0.25"	"3.12"	"4.72"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702888"	""	"0"	"465.54"	"0"	"3.18"	"BDBM147587"	"N#C[C@@H]1CCCC[C@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)Nc3ccccn3)cc2)n1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"285517"	"UO_0000065"	"17.28"	"0.33"	"4.87"	"5.16"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665201"	""	"0"	"485.62"	"0"	"1.76"	"BDBM112600"	"CN1CCC(Nc2ncc(-c3cnc4[nH]ccc4n3)c(N[C@H]3CCCN(S(C)(=O)=O)C3)n2)CC1"	"IC50"	"'='"	"0.1084"	"nM"	"9.96"	""	"233837"	"UO_0000065"	"20.52"	"0.40"	"8.20"	"7.55"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647915"	""	"0"	"436.93"	"0"	"2.16"	"BDBM148027"	"CS(=O)(=O)N[C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"285964"	"UO_0000065"	"19.00"	"0.39"	"6.14"	"5.81"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652308"	""	"0"	"416.55"	"0"	"2.52"	"BDBM113117"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC[C@@H](CC#N)C2)CC1"	"IC50"	"'='"	"52.6"	"nM"	"7.28"	""	"234561"	"UO_0000065"	"17.47"	"0.34"	"4.76"	"6.87"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL4104105"	""	"0"	"349.46"	"0"	"1.60"	"43"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](CS(=O)(=O)N2CCCC2)C1"	"IC50"	"'='"	"244.0"	"nM"	"6.61"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4085011"	""	"0"	"371.47"	"0"	"2.04"	"10"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)Cc2ccccc2)C1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL1789941"	"RUXOLITINIB"	"4"	"306.37"	"0"	"3.47"	"3"	"N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	""	"UO_0000065"	""	""	""	""	"True"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3655081"	"ABROCITINIB"	"3"	"323.42"	"0"	"1.25"	"25; PF-04965842"	"CCCS(=O)(=O)N[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"803.0"	"nM"	"6.09"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3746186"	""	"0"	"429.95"	"0"	"4.06"	"17"	"COCCN1CCC(CNc2c(Cl)cnc3[nH]c(-c4ccc(OC)cc4)nc23)CC1"	"IC50"	"'>'"	"22000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3751000"	"Inhibition of N-terminal GST-fused recombinant JAK2 (831 to 1132 residues) (unknown origin) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate by microfluidic capillary electrophoresis method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3745697"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3747111"	""	"0"	"399.88"	"0"	"3.71"	"14"	"COc1ccc(-c2nc3c(NC4CCN(C(C)=O)CC4)c(Cl)cnc3[nH]2)cc1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3751000"	"Inhibition of N-terminal GST-fused recombinant JAK2 (831 to 1132 residues) (unknown origin) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate by microfluidic capillary electrophoresis method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3745697"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3652293"	""	"0"	"462.62"	"0"	"2.13"	"BDBM113102"	"CC(=O)NCC1CCCN(S(=O)(=O)C[C@H]2CC[C@H](N(C)c3ncnc4[nH]ccc34)CC2)C1"	"IC50"	"'='"	"15.2"	"nM"	"7.82"	""	"234546"	"UO_0000065"	"16.90"	"0.33"	"5.69"	"7.03"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL1938649"	""	"0"	"283.36"	"0"	"2.91"	"14"	"CNC(=O)c1cnc(N)c2cc(-c3ccccc3)sc12"	"IC50"	"'='"	"58.0"	"nM"	"7.24"	""	""	"UO_0000065"	"25.54"	"0.49"	"4.33"	"10.64"	"False"	"CHEMBL1941383"	"Inhibition of human recombinant N-terminal GST-tagged JAK2 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308860"	""
"CHEMBL1938650"	""	"0"	"297.38"	"0"	"3.21"	"15"	"CNC(=O)c1cnc(N)c2cc(-c3ccc(C)cc3)sc12"	"IC50"	"'='"	"27.0"	"nM"	"7.57"	""	""	"UO_0000065"	"25.45"	"0.49"	"4.36"	"11.13"	"False"	"CHEMBL1941383"	"Inhibition of human recombinant N-terminal GST-tagged JAK2 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308860"	""
"CHEMBL3417187"	""	"0"	"501.63"	"2"	"5.48"	"32"	"O=C(CCCCCCN1C/C=C/CCOc2cccc(c2)-c2ccnc(n2)Nc2cccc(c2)C1)NO"	"IC50"	"'='"	"686.0"	"nM"	"6.16"	""	""	"UO_0000065"	"12.29"	"0.23"	"0.68"	"6.19"	"False"	"CHEMBL3419812"	"Inhibition of human recombinant JAK2 using Z'LYTETry6 peptide substrate after 1 hr by microplate reader"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3414525"	"1"	"Scientific Literature"	"Eur. J. Med. Chem."	"2015"	"None"	""
"CHEMBL4077886"	""	"0"	"351.41"	"0"	"2.70"	"16"	"N#C[C@H]1CCOC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C3CC3)cc2)n1"	"IC50"	"'='"	"1.9"	"nM"	"8.72"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4032997"	"Inhibition of GST-tagged recombinant human JAK2 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 as substrate preincubated for 30 mins followed by ATP addition measured after 120 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4085737"	""	"0"	"370.80"	"0"	"2.35"	"27"	"N#Cc1ccc(Nc2nn([C@H]3COCC[C@@H]3C#N)cc2C(N)=O)cc1Cl"	"IC50"	"'='"	"2.7"	"nM"	"8.57"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4032997"	"Inhibition of GST-tagged recombinant human JAK2 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 as substrate preincubated for 30 mins followed by ATP addition measured after 120 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4092626"	""	"0"	"373.39"	"0"	"1.43"	"29"	"CN(C)c1cc(Nc2nn([C@H]3COCC[C@@H]3C#N)cc2C(N)=O)cc(F)n1"	"IC50"	"'='"	"3.4"	"nM"	"8.47"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4032997"	"Inhibition of GST-tagged recombinant human JAK2 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 as substrate preincubated for 30 mins followed by ATP addition measured after 120 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4061128"	""	"0"	"336.36"	"0"	"1.70"	"22"	"N#Cc1ccc(Nc2nn([C@H]3COCC[C@@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"89.0"	"nM"	"7.05"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4033007"	"Inhibition of JAK2 in EPO-stimulated human TF1 cells expressing stably integrated beta-lactamase reporter gene under control of STAT5 response elements in interferon regulatory factor 1 gene promoter by fluorescence assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL1287853"	"FEDRATINIB"	"4"	"524.69"	"1"	"4.82"	"5"	"Cc1cnc(Nc2ccc(OCCN3CCCC3)cc2)nc1Nc1cccc(S(=O)(=O)NC(C)(C)C)c1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"16.24"	"0.31"	"3.70"	"7.86"	"False"	"CHEMBL4309406"	"Inhibition of human JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4308837"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3403541"	""	"0"	"351.80"	"0"	"3.48"	"14"	"Cc1ccc(Cl)cc1-n1cc(-c2ncnc3[nH]ccc23)cc1C(N)=O"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	""	"UO_0000065"	"25.58"	"0.49"	"5.52"	"10.05"	"False"	"CHEMBL3404501"	"Inhibition of recombinant epitope-tagged JAK2 (808 to 1132) (unknown origin) using LPLDKDYYVVREPGQ as substrate by beta-countiing analysis in presence of 33P-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3400063"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL2105759"	"BARICITINIB"	"4"	"371.43"	"0"	"1.10"	"baricitinib"	"CCS(=O)(=O)N1CC(CC#N)(n2cc(-c3ncnc4[nH]ccc34)cn2)C1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	""	"UO_0000065"	"22.14"	"0.43"	"7.12"	"6.82"	"False"	"CHEMBL3625890"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621116"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL3622829"	""	"0"	"294.36"	"0"	"1.68"	"5f"	"NCCn1c(Cc2ccccc2)nc2cc(C(N)=O)ccc21"	"IC50"	"'='"	"2700.0"	"nM"	"5.57"	""	""	"UO_0000065"	"18.92"	"0.35"	"3.89"	"6.41"	"False"	"CHEMBL3625898"	"Inhibition of JAK2 (unknown origin) using 35 uM of ATP and Tyr6 peptide by Z'-LYTE kinase assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621116"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL3622833"	""	"0"	"348.33"	"0"	"2.78"	"5j"	"NCCn1c(-c2ccc(C(F)(F)F)cc2)nc2cc(C(N)=O)ccc21"	"IC50"	"'='"	"4800.0"	"nM"	"5.32"	""	""	"UO_0000065"	"15.27"	"0.29"	"2.54"	"6.12"	"False"	"CHEMBL3625898"	"Inhibition of JAK2 (unknown origin) using 35 uM of ATP and Tyr6 peptide by Z'-LYTE kinase assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621116"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL4527179"	""	"0"	"286.72"	"0"	"3.05"	"30c"	"Nc1n[nH]c2ccc(NC(=O)c3cccc(Cl)c3)cc12"	"IC50"	"'='"	"583.0"	"nM"	"6.23"	""	""	"UO_0000065"	"21.74"	"0.43"	"3.18"	"7.44"	"False"	"CHEMBL4481929"	"Inhibition of JAK2 (unknown origin) after 1 hr FRET-based Z'-Lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480435"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4466720"	""	"0"	"406.42"	"0"	"3.09"	"7"	"NC(=O)c1ccccc1Nc1cc(Nc2ccc(F)cn2)ncc1C(=O)NC1CC1"	"IC50"	"'>'"	"2000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4414788"	"Inhibition of JAK2 JH1 domain (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414548"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4438810"	""	"0"	"419.45"	"0"	"1.78"	"8"	"COCCn1c(=O)n(C2CCOCC2)c2nc(-c3cnc4ccc(C#N)cn34)ncc21"	"IC50"	"'='"	"190.0"	"nM"	"6.72"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4446722"	""	"0"	"435.44"	"1"	"0.48"	"9"	"N#Cc1ccc2ncc(-c3ncc4c(n3)n(C3CCOCC3)c(=O)n4C[C@@H](O)CO)n2c1"	"IC50"	"'='"	"81.0"	"nM"	"7.09"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4471599"	""	"0"	"416.42"	"0"	"2.99"	"17"	"O=c1[nH]c2cnc(-c3cnc4ccc(F)cn34)nc2n1[C@@H]1CC[C@@H](O)c2ccccc21"	"IC50"	"'='"	"0.8"	"nM"	"9.10"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4571980"	""	"0"	"374.38"	"0"	"3.18"	"18"	"C[C@@H](c1ccccc1)n1c(=O)[nH]c2cnc(-c3cnc4ccc(F)cn34)nc21"	"IC50"	"'='"	"68.0"	"nM"	"7.17"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4536396"	""	"0"	"393.36"	"0"	"2.72"	"20"	"C[C@H](c1ccc(F)cn1)n1c(=O)[nH]c2cnc(-c3cnc4ccc(F)cn34)nc21"	"IC50"	"'='"	"0.3"	"nM"	"9.52"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4469844"	""	"0"	"394.35"	"0"	"2.11"	"21"	"C[C@H](c1ncc(F)cn1)n1c(=O)[nH]c2cnc(-c3cnc4ccc(F)cn34)nc21"	"IC50"	"'='"	"0.6"	"nM"	"9.22"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4482927"	""	"0"	"428.81"	"0"	"2.72"	"24"	"O=c1[nH]cc(Cl)cc1Nc1ncc2[nH]c(=O)n([C@@H]3CCOc4c(F)cccc43)c2n1"	"IC50"	"'='"	"1.3"	"nM"	"8.89"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4458055"	""	"0"	"367.34"	"0"	"1.69"	"28"	"C[C@H](c1ccc(F)cn1)n1c(=O)[nH]c2cnc(Nc3ccc[nH]c3=O)nc21"	"IC50"	"'='"	"5.3"	"nM"	"8.28"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL3216659"	""	"0"	"541.28"	"0"	"2.86"	"22; MLS-2384"	"Cl.Cl.O=C1Nc2cc(Br)ccc2/C1=C1/Nc2ccccc2/C1=N\OCCN1CCNCC1"	"IC50"	"'='"	"224.0"	"nM"	"6.65"	""	""	"UO_0000065"	"14.20"	"0.30"	"3.79"	"8.53"	"False"	"CHEMBL4042012"	"Inhibition of recombinant JAK2 (unknown origin) after 120 mins in presence of [33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4041496"	"1"	"Scientific Literature"	"J Nat Prod"	"2016"	"None"	""
"CHEMBL493656"	""	"0"	"526.44"	"1"	"3.22"	"27"	"COCCN1CCN(CCO/N=C2C(=C3/C(=O)Nc4cc(Br)ccc43)/Nc3ccccc3/2)CC1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4042012"	"Inhibition of recombinant JAK2 (unknown origin) after 120 mins in presence of [33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4041496"	"1"	"Scientific Literature"	"J Nat Prod"	"2016"	"None"	""
"CHEMBL1938659"	""	"0"	"517.68"	"1"	"2.68"	"25"	"CC(C)(C)NS(=O)(=O)c1ccc(-c2cc3c(N)ncc(C(=O)NCCN4CCOCC4)c3s2)cc1"	"IC50"	"'='"	"1620.0"	"nM"	"5.79"	""	""	"UO_0000065"	"11.19"	"0.23"	"3.11"	"4.57"	"False"	"CHEMBL1941390"	"Inhibition of TEL-fused JAK2 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3307634"	""
"CHEMBL1945823"	""	"0"	"510.64"	"2"	"5.03"	"27m"	"N#CCN1C/C=C/CCOc2cccc(c2)-c2ccnc(n2)Nc2ccc(OCCN3CCCC3)c(c2)C1"	"IC50"	"'='"	"150.0"	"nM"	"6.82"	""	""	"UO_0000065"	"13.36"	"0.25"	"1.79"	"7.89"	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1946006"	""	"0"	"387.49"	"0"	"4.24"	"27s"	"CN1C/C=C/CCOc2cccc(c2)-c2ccnc(n2)Nc2cc(N)cc(c2)C1"	"IC50"	"'='"	"50.0"	"nM"	"7.30"	""	""	"UO_0000065"	"18.84"	"0.34"	"3.06"	"9.57"	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL570890"	""	"0"	"317.36"	"0"	"2.38"	"29"	"Nc1nn2cccnc2c1-c1cc(NCc2ccccc2)ncn1"	"IC50"	"'>'"	"20000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1044320"	"Inhibition of JAK2-mediated STAT5 phosphorylation in GMCSF-stimulated human TF1 cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"CHEMBL3307972"	""
"CHEMBL568789"	""	"0"	"352.38"	"0"	"3.14"	"7g"	"Cc1cc(Nc2nc(NC(C)c3ccc(F)cn3)c(C#N)nc2C)n[nH]1"	"IC50"	"'<'"	"3.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1043451"	"Inhibition of JAK2 using 2 mM ATP as a substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156131"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL570192"	""	"0"	"353.36"	"0"	"3.11"	"7i"	"Cc1cc(Nc2nc(O[C@@H](C)c3ccc(F)cn3)c(C#N)nc2C)n[nH]1"	"IC50"	"'='"	"142.0"	"nM"	"6.85"	""	""	"UO_0000065"	"19.38"	"0.36"	"3.74"	"6.09"	"False"	"CHEMBL1043452"	"Inhibition of JAK2 using 5 mM ATP as a substrate"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156131"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL570462"	""	"0"	"311.35"	"0"	"0.73"	"16"	"Nc1nn2cccnc2c1-c1cc(N2CCCC(O)C2)ncn1"	"IC50"	"'='"	"70.0"	"nM"	"7.16"	""	""	"UO_0000065"	"22.98"	"0.42"	"6.42"	"6.78"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL570231"	""	"0"	"394.48"	"0"	"1.85"	"21"	"CCCN(CC)C(=O)C1CCN(c2cc(-c3c(N)nn4cccnc34)ncn2)C1"	"IC50"	"'='"	"160.0"	"nM"	"6.80"	""	""	"UO_0000065"	"17.23"	"0.32"	"4.95"	"6.44"	"False"	"CHEMBL1044318"	"Inhibition of JAK2 by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL4764176"	""	"0"	"388.44"	"0"	"2.41"	"17, cis isomer"	"CO[C@H]1C[C@@](CC#N)(n2cc(-c3nc(-c4cnn(C)c4)cn4nccc34)cn2)C1"	"IC50"	"'='"	"99.0"	"nM"	"7.00"	""	""	""	""	""	""	""	"False"	"CHEMBL4675813"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using FITC-KGGEEEEYFELVKK as substrate in presence of ATP at Km by microfluidic assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4673239"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4750448"	""	"0"	"369.39"	"0"	"2.53"	"26, trans"	"N#CC[C@]1(n2cc(-c3nc(-c4cc[nH]n4)cn4nccc34)cn2)C[C@H](C#N)C1"	"IC50"	"'='"	"172.0"	"nM"	"6.76"	""	""	""	""	""	""	""	"False"	"CHEMBL4675813"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using FITC-KGGEEEEYFELVKK as substrate in presence of ATP at Km by microfluidic assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4673239"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL3314285"	""	"0"	"378.43"	"0"	"4.77"	"34"	"CSc1nccc(-c2[nH]c(-c3ccc(O)cc3)nc2-c2ccc(F)cc2)n1"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3363474"	"Inhibition of JAK2 (unknown origin) by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352554"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3644986"	""	"0"	"482.51"	"0"	"4.92"	"BDBM99738"	"COc1ccc(C(F)(F)F)cc1-c1cccn2nc(Nc3ccc(N4CCN(C)CC4)cc3)nc12"	"IC50"	"'='"	"31.33"	"nM"	"7.50"	""	"216426"	"UO_0000065"	"15.55"	"0.29"	"2.58"	"12.95"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3301607"	"FILGOTINIB"	"4"	"425.51"	"0"	"1.98"	"BDBM103727"	"O=C(Nc1nc2cccc(-c3ccc(CN4CCS(=O)(=O)CC4)cc3)n2n1)C1CC1"	"IC50"	"'='"	"41.16"	"nM"	"7.39"	""	"221710"	"UO_0000065"	"17.36"	"0.34"	"5.41"	"7.64"	"False"	"CHEMBL3707887"	"Inhibition Assay: In vitro inhibition assay using various enzyme."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638964"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3973113"	""	"0"	"321.41"	"0"	"0.96"	"BDBM228774"	"CN([C@@H]1CCN(c2ncnc3[nH]ccc23)C1)S(=O)(=O)C1CC1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399710"	"UO_0000065"	"28.81"	"0.57"	"8.30"	"11.27"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4163817"	""	"0"	"503.03"	"1"	"3.26"	"8"	"CN1CCN(c2cc(Nc3ncc(Cl)c(Nc4cccc(CO)c4)n3)cc(S(C)(=O)=O)c2)CC1"	"IC50"	"'='"	"722.0"	"nM"	"6.14"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4145184"	"Inhibition of recombinant human JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate after 10 mins by caliper assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4138312"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4166989"	""	"0"	"494.62"	"0"	"3.06"	"17"	"Cc1cnc(Nc2cc(N3C[C@@H]4C[C@H]3CN4C)cc(S(C)(=O)=O)c2)nc1Nc1cccc(CO)c1"	"IC50"	"'='"	"1180.0"	"nM"	"5.93"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4145184"	"Inhibition of recombinant human JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate after 10 mins by caliper assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4138312"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4165365"	""	"0"	"435.51"	"0"	"3.19"	"20"	"Cc1cnc(Nc2cc(N3C[C@@H]4C[C@H]3CN4C)cnc2F)nc1Nc1cccc(CO)c1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4145184"	"Inhibition of recombinant human JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate after 10 mins by caliper assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4138312"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4753959"	""	"0"	"412.50"	"0"	"3.95"	"2"	"N#CCCn1cc(-c2nc(Nc3ccc(C4CCNCC4)cc3)nc3[nH]ccc23)cn1"	"IC50"	"'='"	"0.13"	"nM"	"9.89"	""	""	""	"23.97"	"0.44"	"5.94"	"9.22"	"False"	"CHEMBL4714135"	"Inhibition of human JAK2 by radiometric assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEK293F"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706688"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	""
"CHEMBL4169982"	""	"0"	"469.57"	"0"	"3.00"	"10"	"Cc1cnc(Nc2cc(N3CCOCC3)cc(S(C)(=O)=O)c2)nc1Nc1cccc(CO)c1"	"IC50"	"'='"	"417.0"	"nM"	"6.38"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4145184"	"Inhibition of recombinant human JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate after 10 mins by caliper assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4138312"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3702942"	""	"0"	"393.37"	"0"	"2.97"	"BDBM147644"	"N#C[C@H]1C[C@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	"285592"	"UO_0000065"	"20.58"	"0.39"	"5.13"	"6.92"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702956"	""	"0"	"391.38"	"0"	"2.55"	"BDBM147662"	"N#C[C@H]1C[C@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(OC(F)F)cc2)n1"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	"285594"	"UO_0000065"	"20.69"	"0.39"	"5.55"	"6.42"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703072"	""	"0"	"430.46"	"0"	"3.27"	"BDBM147784"	"N#C[C@H]1C[C@@H](N2CCC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(OC(F)F)cc2)n1"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	"285733"	"UO_0000065"	"18.05"	"0.34"	"4.50"	"7.11"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3644958"	""	"0"	"396.48"	"0"	"2.89"	"BDBM99708"	"Cc1nn(C)c(C)c1Nc1nc2c(-c3ccc(S(C)(=O)=O)cc3)cccn2n1"	"IC50"	"'='"	"2999.0"	"nM"	"5.52"	""	"216398"	"UO_0000065"	"13.93"	"0.27"	"2.63"	"5.86"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3699553"	""	"0"	"361.81"	"0"	"3.77"	"BDBM147571"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)c(F)c2)n1"	"IC50"	"'='"	"26.0"	"nM"	"7.58"	""	"285501"	"UO_0000065"	"20.96"	"0.41"	"3.82"	"7.84"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642279"	""	"0"	"416.51"	"0"	"2.32"	"BDBM99543"	"COc1ccc(Nc2nc3c(NC4CCN(S(C)(=O)=O)CC4)cccn3n2)cc1"	"IC50"	"'='"	"374.9"	"nM"	"6.43"	""	"216235"	"UO_0000065"	"15.43"	"0.30"	"4.11"	"6.37"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3702887"	""	"0"	"442.55"	"0"	"2.67"	"BDBM147586"	"N#C[C@@H]1CCCC[C@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)NCC3CC3)cc2)n1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"285516"	"UO_0000065"	"20.34"	"0.40"	"6.33"	"6.30"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702896"	""	"0"	"335.37"	"0"	"2.25"	"BDBM147595"	"N#Cc1ccc(Nc2nn([C@H]3CCCC[C@@H]3C#N)cc2C(N)=O)cn1"	"IC50"	"'='"	"22.0"	"nM"	"7.66"	""	"285525"	"UO_0000065"	"22.83"	"0.42"	"5.41"	"5.74"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3658086"	""	"0"	"630.67"	"2"	"6.48"	"BDBM148291"	"Cc1ccc(NC(=O)c2cccc(C(F)(F)F)c2)cc1N1CCc2nc(Nc3ccc(OCCN4CCCC4)cc3)ncc2C1=O"	"IC50"	"'='"	"83.0"	"nM"	"7.08"	""	"286812"	"UO_0000065"	"11.23"	"0.21"	"0.60"	"7.10"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699487"	""	"0"	"385.40"	"0"	"2.52"	"BDBM147502"	"COC(=O)[C@H]1CCC(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"101.0"	"nM"	"7.00"	""	"285429"	"UO_0000065"	"18.15"	"0.34"	"4.48"	"5.69"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3658098"	""	"0"	"590.61"	"2"	"5.08"	"BDBM148373"	"Cc1ccc(NC(=O)c2cccc(C(F)(F)F)c2)cc1N1CCc2nc(Nc3ccc(C(=O)NCCO)cc3)ncc2C1"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"286784"	"UO_0000065"	"13.81"	"0.26"	"3.07"	"6.83"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702989"	""	"0"	"460.50"	"0"	"4.46"	"BDBM147699"	"C[C@@H]1C[C@@H](C)N1[C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(C(F)(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"84.0"	"nM"	"7.08"	""	"285633"	"UO_0000065"	"15.37"	"0.29"	"2.62"	"7.08"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647806"	""	"0"	"439.42"	"0"	"2.99"	"BDBM147909"	"CN(CC(F)(F)F)[C@H]1CCC(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"285843"	"UO_0000065"	"18.71"	"0.36"	"5.23"	"7.28"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702939"	""	"0"	"392.37"	"0"	"1.95"	"BDBM147641"	"N#C[C@H]1C[C@@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(OC(F)F)nc2)n1"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	"285573"	"UO_0000065"	"19.80"	"0.38"	"5.82"	"5.59"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3658087"	""	"0"	"629.69"	"2"	"5.75"	"BDBM148297"	"Cc1ccc(NC(=O)c2cccc(C(F)(F)F)c2)cc1N1CCc2nc(Nc3ccc(C(=O)N4CCN(C)CC4)cc3)ncc2C1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"286813"	"UO_0000065"	"13.54"	"0.25"	"2.77"	"9.10"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647726"	""	"0"	"528.56"	"1"	"2.83"	"BDBM147828"	"COCCN(C)[C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	"285762"	"UO_0000065"	"14.70"	"0.29"	"4.94"	"5.42"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645538"	""	"0"	"325.80"	"0"	"4.25"	"BDBM107121"	"O=C(CCCCl)Nc1cccc(-c2cnc3ccccc3n2)c1"	"IC50"	"'>'"	"50000.0"	"nM"	""	""	"226358"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3357978"	""	"0"	"373.44"	"0"	"1.25"	"BDBM112545"	"CS(=O)(=O)N1CCC[C@H](Nc2nccnc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.0359"	"nM"	"10.44"	""	"233784"	"UO_0000065"	"27.97"	"0.55"	"9.19"	"8.95"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647716"	""	"0"	"392.51"	"0"	"3.30"	"BDBM147818"	"CC1(C)CN([C@H]2CC[C@H](n3cc(C(N)=O)c(Nc4ccccc4)n3)[C@@H](C#N)C2)C1"	"IC50"	"'='"	"40.0"	"nM"	"7.40"	""	"285752"	"UO_0000065"	"18.85"	"0.35"	"4.10"	"7.40"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645069"	""	"0"	"514.63"	"1"	"4.42"	"BDBM99837"	"COc1cccc(-c2cccn3nc(Nc4ccc(C5CCN(CC(=O)N(C)C)CC5)cc4)nc23)c1OC"	"IC50"	"'='"	"45.65"	"nM"	"7.34"	""	"216510"	"UO_0000065"	"14.26"	"0.26"	"2.92"	"8.71"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3622145"	""	"0"	"513.65"	"1"	"3.62"	"7"	"CCn1c(C(=O)N(C2CC2)C2CC2)cc2c3c(ncn3C)c(Nc3nc(C)c(S(C)(=O)=O)s3)nc21"	"IC50"	"'='"	"1.4"	"nM"	"8.85"	""	""	"UO_0000065"	"17.24"	"0.35"	"5.23"	"7.70"	"False"	"CHEMBL3625512"	"Inhibition of recombinant JAK2 (unknown origin) using 5-FAM-KKKKEEIYFFFG-OH substrate and ATP incubated for 180 mins by scintillation counting method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621135"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3699537"	""	"0"	"407.40"	"0"	"3.58"	"BDBM147555"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc([C@@H](O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"285485"	"UO_0000065"	"21.35"	"0.41"	"5.12"	"7.44"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642360"	""	"0"	"551.68"	"2"	"2.64"	"BDBM99636"	"COc1cc(N2CCN(C)CC2)ccc1Nc1nc2c(NCc3cccnc3N(C)S(C)(=O)=O)cccn2n1"	"IC50"	"'='"	"2999.0"	"nM"	"5.52"	""	"216326"	"UO_0000065"	"10.01"	"0.19"	"2.88"	"4.59"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL1934347"	""	"0"	"428.50"	"0"	"2.59"	"3m"	"NC(=O)CN1CCC(c2ccc(Nc3ncc4ccc(-c5cnccn5)n4n3)cc2)CC1"	"IC50"	"'='"	"282.0"	"nM"	"6.55"	""	""	"UO_0000065"	"15.29"	"0.28"	"3.96"	"5.73"	"False"	"CHEMBL1936009"	"Inhibition of JAK2 in GM-CSF-stimulated human TF1 cells preincubated for 1 hr prior to challenge"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3307972"	""
"CHEMBL1934351"	""	"0"	"477.57"	"0"	"4.35"	"3q"	"NC(=O)CN1CCC(c2ccc(Nc3ncc4ccc(-c5cccc6cccnc56)n4n3)cc2)CC1"	"IC50"	"'='"	"170.0"	"nM"	"6.77"	""	""	"UO_0000065"	"14.17"	"0.26"	"2.42"	"6.67"	"False"	"CHEMBL1936009"	"Inhibition of JAK2 in GM-CSF-stimulated human TF1 cells preincubated for 1 hr prior to challenge"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1932974"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3307972"	""
"CHEMBL2322135"	""	"0"	"240.31"	"0"	"3.49"	"5"	"c1cc2c(ncc3[nH]nc(C4CCCCC4)c32)[nH]1"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	""	"UO_0000065"	"33.29"	"0.61"	"4.51"	"13.95"	"False"	"CHEMBL2327345"	"Inhibition of JAK2 (unknown origin) after 2.5 hrs by time-resolved fluorescence resonance energy transfer assay in presence of 1 uM ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321825"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL21156"	""	"0"	"309.34"	"0"	"3.99"	"6"	"CC(C)(C)c1nc2c3ccc(F)cc3c3c(=O)[nH]ccc3c2[nH]1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	""	"UO_0000065"	"29.09"	"0.53"	"5.01"	"14.62"	"True"	"CHEMBL704109"	"Inhibition of protein kinase Jak 2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1135866"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2002"	"None"	""
"CHEMBL3329229"	""	"0"	"371.83"	"0"	"2.40"	"10"	"Cc1ccc(Cl)cc1-c1[nH]c(-c2ccnc(N)n2)cc1C(=O)NCCO"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL3374497"	"Inhibition of JAK2 V617F mutant in human SET2 cells"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3309998"	""	"0"	"378.39"	"0"	"1.58"	"12b"	"Nc1nc2c3ccc(NCCO)cc3nc(Cc3ccc4c(c3)OCO4)n2n1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3381081"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352169"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL569757"	""	"0"	"408.51"	"0"	"2.24"	"24"	"CCCN(CC)C(=O)C1CCCN(c2cc(-c3c(N)nn4cccnc34)ncn2)C1"	"IC50"	"'='"	"6500.0"	"nM"	"5.19"	""	""	"UO_0000065"	"12.70"	"0.24"	"2.95"	"4.91"	"False"	"CHEMBL1044320"	"Inhibition of JAK2-mediated STAT5 phosphorylation in GMCSF-stimulated human TF1 cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156132"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"CHEMBL3307972"	""
"CHEMBL3357977"	""	"0"	"352.42"	"0"	"0.53"	"15"	"CN(C(=O)N[C@H]1CCCN(S(C)(=O)=O)C1)c1cnc2[nH]ccc2n1"	"IC50"	"'='"	"4410.0"	"nM"	"5.36"	""	""	"UO_0000065"	"15.20"	"0.30"	"4.83"	"4.81"	"False"	"CHEMBL3374010"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 1 hr in presence of [gamma-33P]ATP by scintillation counting analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351377"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3335677"	""	"0"	"302.34"	"0"	"1.09"	"4"	"CC(=O)N1CCC(NC(=O)Nc2cnc3[nH]ccc3n2)CC1"	"IC50"	"'='"	"226.0"	"nM"	"6.65"	""	""	"UO_0000065"	"21.98"	"0.41"	"5.56"	"6.45"	"False"	"CHEMBL3374010"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 1 hr in presence of [gamma-33P]ATP by scintillation counting analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351377"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL1938658"	""	"0"	"515.71"	"1"	"3.84"	"24"	"CC(C)(C)NS(=O)(=O)c1ccc(-c2cc3c(N)ncc(C(=O)NCCN4CCCCC4)c3s2)cc1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	""	"UO_0000065"	"16.10"	"0.32"	"4.46"	"7.07"	"False"	"CHEMBL1941383"	"Inhibition of human recombinant N-terminal GST-tagged JAK2 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308860"	""
"CHEMBL1946004"	""	"0"	"515.66"	"2"	"5.14"	"27q"	"COc1cc2cc(c1OCCN1CCCC1)CN(C)C/C=C/CCOc1cccc(c1)-c1ccnc(n1)N2"	"IC50"	"'='"	"210.0"	"nM"	"6.68"	""	""	"UO_0000065"	"12.95"	"0.24"	"1.54"	"9.28"	"False"	"CHEMBL1948620"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1944548"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL3702931"	""	"0"	"390.45"	"0"	"2.78"	"BDBM147633"	"Cn1cc(-c2cncc(Nc3nn(C4CCCC[C@@H]4C#N)cc3C(N)=O)c2)cn1"	"IC50"	"'='"	"73.0"	"nM"	"7.14"	""	"285564"	"UO_0000065"	"18.28"	"0.34"	"4.36"	"5.60"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3639511"	""	"0"	"407.54"	"0"	"1.74"	"BDBM113091"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCC(O)CC2)CC1"	"IC50"	"'='"	"34.2"	"nM"	"7.47"	""	"234535"	"UO_0000065"	"18.32"	"0.36"	"5.73"	"7.29"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3263640"	""	"0"	"589.70"	"2"	"6.09"	"20"	"Cc1c(NC(=O)c2ccc(C(C)(C)C)cc2)cccc1-c1nc(Nc2ccc(C(=O)N3CCOCC3)cc2)c2nc[nH]c2n1"	"IC50"	"'='"	"3068.0"	"nM"	"5.51"	""	""	"UO_0000065"	"9.35"	"0.17"	"-0.58"	"4.41"	"False"	"CHEMBL3270967"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3259754"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL4278591"	""	"0"	"514.03"	"1"	"5.07"	"45g"	"CC(=O)Nc1ccc(-c2ccnc(Nc3cccc(OCCCCCCCC(=O)NO)c3)n2)cc1.Cl"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	""	"UO_0000065"	"16.27"	"0.30"	"2.70"	"6.19"	"False"	"CHEMBL4268221"	"Inhibition of human JAK2 using poly(Glu:Tyr)(4:1) as substrate preincubated for 20 mins followed by [gamma33P]ATP addition measured after 120 mins by ion exchange filter paper method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4265943"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2018"	"None"	""
"CHEMBL3330105"	""	"0"	"341.80"	"0"	"3.04"	"7"	"CNC(=O)c1cc(-c2ccnc(N)n2)[nH]c1-c1cc(Cl)ccc1C"	"IC50"	"'='"	"480.0"	"nM"	"6.32"	""	""	"UO_0000065"	"18.49"	"0.36"	"3.28"	"6.54"	"False"	"CHEMBL3374497"	"Inhibition of JAK2 V617F mutant in human SET2 cells"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3360355"	""	"0"	"403.36"	"0"	"2.92"	"62"	"O=C(Nc1nc2cccc(-c3ccc(CNC(=O)C(F)(F)F)cc3)n2n1)C1CC1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3382736"	"Inhibition of JAK2 in human whole blood assessed as inhibition of GM-CSF-induced pSTAT5"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"CHEMBL3638178"	"Blood"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351789"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL3360357"	""	"0"	"425.51"	"0"	"2.02"	"64"	"O=C(Nc1nc2cccc(-c3ccc(CNC4CCS(=O)(=O)C4)cc3)n2n1)C1CC1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3382736"	"Inhibition of JAK2 in human whole blood assessed as inhibition of GM-CSF-induced pSTAT5"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"CHEMBL3638178"	"Blood"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351789"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL510641"	""	"0"	"244.32"	"0"	"2.89"	"7"	"Cc1nc(C)c(-c2ccc3[nH]nc(N)c3c2)s1"	"IC50"	"'='"	"320.0"	"nM"	"6.50"	""	""	"UO_0000065"	"26.58"	"0.52"	"3.60"	"9.61"	"False"	"CHEMBL1011746"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139271"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL498859"	""	"0"	"243.70"	"0"	"3.47"	"8"	"Nc1n[nH]c2ccc(-c3ccccc3Cl)cc12"	"IC50"	"'='"	"370.0"	"nM"	"6.43"	""	""	"UO_0000065"	"26.39"	"0.52"	"2.96"	"11.76"	"False"	"CHEMBL1011746"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139271"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL482187"	""	"0"	"378.89"	"0"	"3.54"	"20"	"CC(C)(C)NS(=O)(=O)c1ccc(-c2cc(Cl)c3[nH]nc(N)c3c2)cc1"	"IC50"	"'='"	"1220.0"	"nM"	"5.91"	""	""	"UO_0000065"	"15.61"	"0.32"	"2.37"	"5.86"	"False"	"CHEMBL1011746"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139271"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL4283513"	""	"0"	"561.69"	"1"	"3.91"	"62"	"CN1CCN(CC(=O)Nc2ccc(-c3ccnc(Nc4ccc(OCCCCCCC(=O)NO)cc4)n3)cc2)CC1"	"IC50"	"'='"	"95.5"	"nM"	"7.02"	""	""	"UO_0000065"	"12.50"	"0.23"	"3.11"	"5.32"	"False"	"CHEMBL4268221"	"Inhibition of human JAK2 using poly(Glu:Tyr)(4:1) as substrate preincubated for 20 mins followed by [gamma33P]ATP addition measured after 120 mins by ion exchange filter paper method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4265943"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2018"	"None"	""
"CHEMBL4291781"	""	"0"	"514.03"	"1"	"5.07"	"45j"	"CC(=O)Nc1ccc(-c2ccnc(Nc3ccc(OCCCCCCCC(=O)NO)cc3)n2)cc1.Cl"	"IC50"	"'='"	"46.0"	"nM"	"7.34"	""	""	"UO_0000065"	"15.36"	"0.29"	"2.27"	"5.85"	"False"	"CHEMBL4268221"	"Inhibition of human JAK2 using poly(Glu:Tyr)(4:1) as substrate preincubated for 20 mins followed by [gamma33P]ATP addition measured after 120 mins by ion exchange filter paper method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4265943"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2018"	"None"	""
"CHEMBL3948029"	""	"0"	"458.54"	"1"	"5.41"	"BDBM195902"	"COc1cc(F)c(C)cc1-c1c[nH]c2ncc(-c3cccc(NC(=O)/C=C/CN(C)C)c3)cc12"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	"348608"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3887689"	"Biochemical Inhibition Assay: 1H-pyrrolo[2,3-b]pyridine, 1H-pyrazolo[3,4-b]pyridine and 5H-pyrrolo[2,3-b]pyrazine series of compounds exhibited over >100 fold selective against Janus and TEC family of kinases except for the BMX and TXK it had activity of 30 and 45 nM respectively."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886406"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3894591"	""	"0"	"400.41"	"0"	"2.41"	"BDBM237797"	"CCOC(=O)N1CC[C@@H](C#N)[C@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)C1"	"IC50"	"'='"	"62.0"	"nM"	"7.21"	""	"414901"	"UO_0000065"	"18.00"	"0.34"	"4.80"	"5.71"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3919101"	""	"0"	"294.36"	"0"	"3.47"	"BDBM197717"	"CCCCC(CC#N)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"0.3"	"nM"	"9.52"	""	"351117"	"UO_0000065"	"32.35"	"0.59"	"6.05"	"11.45"	"False"	"CHEMBL3887743"	"Kinase Assay: The compounds of the invention were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Biochemistry 1999, 269, 94-104. The catalytic domains of human JAK1 (a.a. 837-1142), JAK2 (a.a. 828-1132) and JAK3 (a.a. 781-1124) with an N-terminal His tag were expressed using baculovirus in insect cells and purified. The catalytic activity of JAK1, JAK2 or JAK3 was assayed by measuring the phosphorylation of a biotinylated peptide. The phosphorylated peptide was detected by homogenous time resolved fluorescence (HTRF). IC50 was measured for each kinase in the 40 uL reactions that contain the enzyme, ATP and 500 nM peptide in 50 mM Tris (pH 7.8) buffer with 100 mM NaCl, 5 mM DTT, and 0.1 mg/mL (0.01%) BSA. The ATP concentration in the reactions was 90 uM for Jak1, 30 uM for Jak2 and 3 uM for Jak3. Reactions were carried out at room temperature for 1 hr and then stopped with 20 uL 45 mM EDTA."	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886433"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3908927"	""	"0"	"450.42"	"0"	"2.70"	"BDBM237792"	"N#C[C@@H]1CCN(C(=O)OC(CF)CF)C[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"44.0"	"nM"	"7.36"	""	"414896"	"UO_0000065"	"16.33"	"0.31"	"4.66"	"5.83"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3903415"	""	"0"	"440.48"	"0"	"3.19"	"BDBM237794"	"CC(OC(=O)N1CC[C@@H](C#N)[C@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)C1)C1CC1"	"IC50"	"'='"	"77.0"	"nM"	"7.11"	""	"414898"	"UO_0000065"	"16.15"	"0.30"	"3.92"	"5.63"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL1990583"	""	"0"	"405.39"	"0"	"3.35"	"5g"	"Nc1ncnn2ccc(C(=O)Nc3ccc(NC(=O)Nc4cccc(F)c4)cc3)c12"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2064935"	"Inhibition of Jak2 in presence of 10 uM ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062488"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL3935714"	""	"0"	"272.38"	"0"	"3.92"	"BDBM198200"	"S=c1[nH]c(C2CCCCC2)c2c3cc[nH]c3ncn12"	"IC50"	"'='"	"30.0"	"nM"	"7.52"	""	"351822"	"UO_0000065"	"27.62"	"0.54"	"3.60"	"15.39"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3126347"	""	"0"	"415.28"	"0"	"4.75"	"25"	"CC(C)(O)c1cc(Cl)c(Nc2nc3ccncc3c3c(=O)[nH]ccc23)c(Cl)c1"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	""	"UO_0000065"	"18.65"	"0.38"	"2.99"	"8.52"	"False"	"CHEMBL3131375"	"Inhibition of Jak2 (unknown origin) assessed as inhibition of STAT5 phosphorylation by cell-based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3124786"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3126345"	""	"0"	"374.30"	"0"	"4.37"	"20"	"O=c1[nH]ccc2c(Nc3c(F)cccc3C(F)(F)F)nc3ccncc3c12"	"IC50"	"'='"	"90.0"	"nM"	"7.05"	""	""	"UO_0000065"	"18.82"	"0.36"	"2.68"	"9.97"	"False"	"CHEMBL3131375"	"Inhibition of Jak2 (unknown origin) assessed as inhibition of STAT5 phosphorylation by cell-based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3124786"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3126348"	""	"0"	"423.26"	"0"	"4.91"	"28"	"O=c1[nH]ccc2c(Nc3c(Cl)cc(-c4ccn[nH]4)cc3Cl)nc3ccncc3c12"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	""	"UO_0000065"	"21.26"	"0.42"	"4.09"	"9.06"	"False"	"CHEMBL3131376"	"Inhibition of recombinant Jak2 (unknown origin) using biotinylated synthetic peptide substrate by homogeneous time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3124786"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3126346"	""	"0"	"401.25"	"0"	"4.58"	"24"	"CC(O)c1cc(Cl)c(Nc2nc3ccncc3c3c(=O)[nH]ccc23)c(Cl)c1"	"IC50"	"'='"	"0.6"	"nM"	"9.22"	""	""	"UO_0000065"	"22.98"	"0.47"	"4.64"	"10.15"	"False"	"CHEMBL3131376"	"Inhibition of recombinant Jak2 (unknown origin) using biotinylated synthetic peptide substrate by homogeneous time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3124786"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL1078688"	""	"0"	"453.57"	"0"	"3.22"	"16"	"CS(=O)(=O)Nc1ccc(-c2ccnc(Nc3cccc(CN4CCC(O)CC4)c3)n2)cc1"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	""	"UO_0000065"	"17.46"	"0.34"	"4.70"	"7.37"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1079077"	""	"0"	"425.51"	"0"	"3.10"	"22"	"CS(=O)(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	""	"UO_0000065"	"19.74"	"0.38"	"5.30"	"8.71"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1078178"	"MOMELOTINIB"	"3"	"414.47"	"0"	"2.98"	"28"	"N#CCNC(=O)c1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	""	"UO_0000065"	"18.69"	"0.34"	"4.76"	"7.51"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1078228"	""	"0"	"432.46"	"0"	"3.12"	"38"	"N#CCNC(=O)c1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)c(F)c3)n2)cc1"	"IC50"	"'='"	"116.0"	"nM"	"6.94"	""	""	"UO_0000065"	"16.04"	"0.30"	"3.82"	"6.72"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL3649639"	""	"0"	"474.61"	"1"	"5.72"	"BDBM130333"	"Cc1cccc(-c2cc(C(N)=O)c3[nH]c4cc(N5CCN(Cc6ccccc6)CC5)ccc4c3c2)c1"	"IC50"	"'='"	"123.0"	"nM"	"6.91"	""	"262119"	"UO_0000065"	"14.56"	"0.26"	"1.19"	"10.57"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649643"	""	"0"	"413.48"	"0"	"3.59"	"BDBM130338"	"NC(=O)c1cc(-c2ccc(C3CC3)nc2)nc2c1[nH]c1cc(N3CCOCC3)ccc12"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"262124"	"UO_0000065"	"21.77"	"0.40"	"5.41"	"9.27"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3646847"	""	"0"	"436.42"	"0"	"3.23"	"BDBM130296"	"NC(=O)c1cc(-c2ccc(F)c(F)c2)nc2c1[nH]c1cc(C(=O)N3CCOCC3)ccc12"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"262082"	"UO_0000065"	"18.69"	"0.35"	"4.92"	"8.05"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649627"	""	"0"	"422.49"	"0"	"1.21"	"BDBM130321"	"NC(=O)c1cc(N2CCC(N)CC2)nc2c1[nH]c1cc(C(=O)N3CCOCC3)ccc12"	"IC50"	"'='"	"636.0"	"nM"	"6.20"	""	"262107"	"UO_0000065"	"14.67"	"0.27"	"4.99"	"4.75"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649641"	""	"0"	"582.10"	"2"	"5.47"	"BDBM130335"	"NC(=O)c1cc(-c2ccc(CN3CCOCC3)c(Cl)c2)cc2c1[nH]c1cc(-c3ccc(N4CCOCC4)nc3)ccc12"	"IC50"	"'='"	"917.0"	"nM"	"6.04"	""	"262121"	"UO_0000065"	"10.37"	"0.20"	"0.57"	"6.24"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL1081138"	""	"0"	"371.44"	"0"	"4.21"	"10"	"c1cc(-c2ccc3[nH]ccc3c2)nc(Nc2ccc(N3CCOCC3)cc2)n1"	"IC50"	"'='"	"33.0"	"nM"	"7.48"	""	""	"UO_0000065"	"20.14"	"0.36"	"3.27"	"11.32"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1077575"	""	"0"	"414.47"	"0"	"3.58"	"25"	"N#CCC(=O)Nc1cccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)c1"	"IC50"	"'='"	"303.0"	"nM"	"6.52"	""	""	"UO_0000065"	"15.73"	"0.29"	"2.94"	"6.32"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL1080411"	""	"0"	"377.45"	"0"	"3.31"	"11"	"COc1cc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)ccc1N"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	""	"UO_0000065"	"20.65"	"0.38"	"4.49"	"9.11"	"False"	"CHEMBL1107753"	"Inhibition of GST-tagged JAK2 kinase"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154287"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2009"	"None"	""
"CHEMBL3950301"	""	"0"	"468.58"	"0"	"2.55"	"16c"	"CN1CCN(c2ccc(Nc3nccc(-c4cc5c(o4)CCN(S(C)(=O)=O)C5)n3)cc2)CC1"	"IC50"	"'='"	"37.9"	"nM"	"7.42"	""	""	"UO_0000065"	"15.84"	"0.31"	"4.87"	"7.83"	"False"	"CHEMBL3868063"	"Inhibition of GST-tagged recombinant human JAK2 expressed in baculovirus using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3867460"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2017"	"None"	""
"CHEMBL3907087"	""	"0"	"386.46"	"0"	"4.78"	"5a"	"Cc1cnc(Nc2ccc(N3CCOCC3)cc2)nc1-c1cc2ccccc2o1"	"IC50"	"'='"	"8.9"	"nM"	"8.05"	""	""	"UO_0000065"	"20.83"	"0.38"	"3.27"	"12.69"	"False"	"CHEMBL3868063"	"Inhibition of GST-tagged recombinant human JAK2 expressed in baculovirus using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3867460"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2017"	"None"	""
"CHEMBL3940537"	""	"0"	"469.57"	"0"	"2.94"	"16h"	"Cc1cnc(Nc2ccc(N3CCOCC3)cc2)nc1-c1cc2c(o1)CCN(S(C)(=O)=O)C2"	"IC50"	"'='"	"425.6"	"nM"	"6.37"	""	""	"UO_0000065"	"13.57"	"0.26"	"3.43"	"6.32"	"False"	"CHEMBL3868066"	"Inhibition of JAK2 in human TF1 cells assessed as suppression of cell growth"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3867460"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2017"	"CHEMBL3307972"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"Tofacitinib"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"2.8"	"nM"	"8.55"	""	""	"UO_0000065"	"27.38"	"0.51"	"7.01"	"9.62"	"True"	"CHEMBL3868063"	"Inhibition of GST-tagged recombinant human JAK2 expressed in baculovirus using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3867460"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2017"	"None"	""
"CHEMBL4097778"	"TP-030n"	"0"	"458.54"	"0"	"1.13"	"TP-030n"	"CN1C(=O)[C@@H](N2CCc3cn(CC4CCS(=O)(=O)CC4)nc3C2=O)COc2ccccc21"	"IC50"	""	"1000.0"	"nM"	""	""	""	""	""	""	""	""	"False"	"CHEMBL4513013"	"JAK2(JAK2LGF1) Takeda global kinase panel"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4507327"	"54"	"Donated Chemical Probes - SGC Frankfurt"	""	"2021"	"None"	"Compound concentration None 1.0 µM"
"CHEMBL3948663"	""	"0"	"444.50"	"0"	"3.12"	"16b"	"N#CCC(=O)N1CCc2oc(-c3ccnc(Nc4ccc(N5CCOCC5)cc4)n3)cc2C1"	"IC50"	"'='"	"3125.0"	"nM"	"5.50"	""	""	"UO_0000065"	"12.39"	"0.23"	"2.39"	"5.12"	"False"	"CHEMBL3868066"	"Inhibition of JAK2 in human TF1 cells assessed as suppression of cell growth"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3867460"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2017"	"CHEMBL3307972"	""
"CHEMBL3941571"	""	"0"	"483.59"	"0"	"3.27"	"16e"	"CS(=O)(=O)N1CCc2oc(-c3ccnc(Nc4ccc(OCCN5CCCC5)cc4)n3)cc2C1"	"IC50"	"'='"	"1258.0"	"nM"	"5.90"	""	""	"UO_0000065"	"12.20"	"0.24"	"2.63"	"5.85"	"False"	"CHEMBL3868067"	"Inhibition of JAK2 V617F mutant in human HEL cells after 1 hr"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3867460"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2017"	"CHEMBL3308090"	""
"CHEMBL4761545"	""	"0"	"401.47"	"0"	"3.85"	"3"	"C=CC(=O)Nc1cccc(-c2cc(Nc3ccc(N4CCOCC4)cc3)ncn2)c1"	"IC50"	"'='"	"2043.0"	"nM"	"5.69"	""	""	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL4754557"	""	"0"	"364.41"	"0"	"2.85"	"7"	"C=CC(=O)Nc1cccc(-c2ccnc(Nc3cnn(CCOC)c3)n2)c1"	"IC50"	"'='"	"1286.0"	"nM"	"5.89"	""	""	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL4749364"	""	"0"	"401.47"	"0"	"3.85"	"10"	"C=CC(=O)Nc1ccc(-c2cc(Nc3ccc(N4CCOCC4)cc3)ncn2)cc1"	"IC50"	"'='"	"1569.0"	"nM"	"5.80"	""	""	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"CP-690550"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"1.5"	"nM"	"8.82"	""	""	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL1078166"	""	"0"	"414.47"	"0"	"3.58"	"39"	"N#CCC(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"88.0"	"nM"	"7.06"	""	""	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL3671154"	""	"0"	"417.42"	"0"	"1.43"	"BDBM127653"	"O=C(NC[C@@H](O)CO)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258327"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675920"	""	"0"	"397.45"	"0"	"2.71"	"BDBM127669"	"CC(C)(C)NC(=O)c1cnn2ccc(N3C[C@H](O)C[C@@H]3c3cccc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258343"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676015"	""	"0"	"513.57"	"1"	"3.26"	"BDBM127768"	"COc1ncc(F)cc1[C@H]1CCCN1c1ccn2ncc(C(=O)NCCCNC(=O)OC(C)(C)C)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258442"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676029"	""	"0"	"428.47"	"0"	"2.11"	"BDBM127785"	"COc1ncc(F)cc1[C@H]1CCCN1c1ccn2ncc(C(=O)NCC(C)(C)O)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258456"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676039"	""	"0"	"470.52"	"0"	"2.54"	"BDBM127797"	"O=C(NCCN1CCC(O)CC1)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258466"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676041"	""	"0"	"401.42"	"0"	"2.73"	"BDBM127799"	"COCCNC(=O)c1cnn2ccc(N3CCCC3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258468"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676078"	""	"0"	"452.41"	"0"	"2.65"	"BDBM127839"	"CC(NC(=O)c1cnn2ccc(N3C(CO)CCC3c3cncc(F)c3)nc12)C(F)(F)F"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258508"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL4297507"	"DELGOCITINIB"	"3"	"310.36"	"0"	"1.30"	"ent-60, JTE-052"	"C[C@H]1CN(C(=O)CC#N)[C@]12CCN(c1ncnc3[nH]ccc13)C2"	"IC50"	"'='"	"2.6"	"nM"	"8.59"	""	""	"UO_0000065"	"27.66"	"0.51"	"7.29"	"9.66"	"False"	"CHEMBL4630016"	"Inhibition of N-terminal GST-fused human JAK2 (880 to end residues) expressed in baculovirus infected Sf21 cells using TK-substrate-biotin as substrate incubated for 60 mins in presence of ATP by fluorescence method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4627398"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL4106362"	""
"CHEMBL3911320"	""	"0"	"340.81"	"0"	"3.78"	"13"	"Nc1n[nH]c2ccc(C(=O)N3CCC[C@H]3c3ccc(Cl)cc3)cc12"	"IC50"	"'='"	"286.0"	"nM"	"6.54"	""	""	"UO_0000065"	"19.20"	"0.37"	"2.76"	"8.72"	"False"	"CHEMBL3854810"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3853318"	"1"	"Scientific Literature"	"J Med Chem"	"2016"	"None"	""
"CHEMBL3675946"	""	"0"	"400.43"	"0"	"3.08"	"BDBM127698"	"CC(C)(CF)NC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258372"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675955"	""	"0"	"412.47"	"0"	"2.63"	"BDBM127707"	"CC(C)(C)NC(=O)c1cnn2ccc(N3CCCC3c3cc(F)cnc3CO)nc12"	"IC50"	"'='"	"869.0"	"nM"	"6.06"	""	"258381"	"UO_0000065"	"14.69"	"0.28"	"3.43"	"6.34"	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675958"	""	"0"	"386.39"	"0"	"1.39"	"BDBM127710"	"CONC(=O)c1cnn2ccc(N3CCCC3c3cc(F)cnc3CO)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258384"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675960"	""	"0"	"494.57"	"0"	"2.81"	"BDBM127712"	"O=C(NC1CC1)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)cc(OCCN4CCOCC4)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258386"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675979"	""	"0"	"410.45"	"0"	"2.25"	"BDBM127732"	"O=C(N[C@H]1CC[C@H](O)C1)c1cnn2ccc(N3CCCC3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258406"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675986"	""	"0"	"370.39"	"0"	"1.33"	"BDBM127739"	"O=C(NCCO)c1cnn2ccc(N3CCCC3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258413"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675995"	""	"0"	"412.47"	"0"	"2.35"	"BDBM127748"	"CC(C)[C@@H](CO)NC(=O)c1cnn2ccc(N3CCCC3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258422"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676001"	""	"0"	"396.43"	"0"	"1.67"	"BDBM127754"	"O=C(c1cnn2ccc(N3CCC[C@@H]3c3cncc(F)c3)nc12)N1CC(CO)C1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258428"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676012"	""	"0"	"450.52"	"0"	"2.74"	"BDBM127765"	"O=C(N[C@@H]1C2CC[C@@H](C2)[C@@H]1CO)c1cnn2ccc(N3CCCC3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258439"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676025"	""	"0"	"440.48"	"0"	"2.26"	"BDBM127781"	"COc1ncc(F)cc1[C@H]1CCCN1c1ccn2ncc(C(=O)N[C@H]3CC[C@H](O)C3)c2n1"	"IC50"	"'='"	"524.0"	"nM"	"6.28"	""	"258452"	"UO_0000065"	"14.26"	"0.27"	"4.02"	"5.99"	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676030"	""	"0"	"483.55"	"0"	"1.80"	"BDBM127786"	"COc1ncc(F)cc1[C@H]1CCCN1c1ccn2ncc(C(=O)NC3CCN(CCO)CC3)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258457"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676040"	""	"0"	"469.54"	"0"	"2.33"	"BDBM127798"	"CN1CCN(CCNC(=O)c2cnn3ccc(N4CCCC4c4cc(F)ccc4F)nc23)CC1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258467"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676042"	""	"0"	"417.42"	"0"	"1.43"	"BDBM127800"	"O=C(NC(CO)CO)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258469"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676052"	""	"0"	"382.44"	"0"	"3.05"	"BDBM127811"	"Cc1ncc(F)cc1[C@H]1CCCN1c1ccn2ncc(C(=O)NC(C)C)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258480"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676055"	""	"0"	"340.36"	"0"	"2.01"	"BDBM127814"	"Cc1ncc(F)cc1C1CCCN1c1ccn2ncc(C(N)=O)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258483"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3622129"	""	"0"	"382.47"	"0"	"2.11"	"7"	"CNc1nc2c(cc(C(=O)N(C3CC3)C3CC3)n2C[C@@H](C)O)c2c1ncn2C"	"IC50"	"'='"	"370.0"	"nM"	"6.43"	""	""	"UO_0000065"	"16.82"	"0.31"	"4.32"	"7.29"	"False"	"CHEMBL3625474"	"Inhibition of JAK2 in human SET2 cells assessed as inhibition of cell proliferation after 72 hrs by [3H]-thymidine incorporation assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621098"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3652397"	""	"0"	"460.60"	"0"	"1.88"	"BDBM113209"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCCC3(CNC(=O)C3)C2)CC1"	"IC50"	"'='"	"62.5"	"nM"	"7.20"	""	"234652"	"UO_0000065"	"15.64"	"0.31"	"5.32"	"6.47"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3647717"	""	"0"	"432.45"	"0"	"3.73"	"BDBM147819"	"N#C[C@H]1C[C@H](NC2CC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"113.0"	"nM"	"6.95"	""	"285753"	"UO_0000065"	"16.06"	"0.31"	"3.22"	"6.39"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642328"	""	"0"	"353.43"	"0"	"1.48"	"BDBM99600"	"c1cncc(CNc2cccn3nc(NCCN4CCOCC4)nc23)c1"	"IC50"	"'='"	"9999.0"	"nM"	"5.00"	""	"216290"	"UO_0000065"	"14.15"	"0.26"	"3.52"	"6.28"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL4643392"	""	"0"	"433.51"	"0"	"3.43"	"26"	"N#C[C@]1(C2CC2)C(=O)N2C[C@H]1COCCCCOCc1cccc(n1)Nc1cc2ccn1"	"IC50"	"'='"	"130.0"	"nM"	"6.89"	""	""	"UO_0000065"	"15.88"	"0.29"	"3.46"	"6.86"	"False"	"CHEMBL4627620"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4627255"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL4643183"	""	"0"	"395.87"	"1"	"5.76"	"16d"	"CC(Oc1cc(-c2cn(C)c3ccccc23)cnc1N)c1cc(F)ccc1Cl"	"IC50"	"'='"	"695.0"	"nM"	"6.16"	""	""	"UO_0000065"	"15.56"	"0.30"	"0.40"	"11.60"	"False"	"CHEMBL4628503"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4627317"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL4648097"	""	"0"	"390.85"	"0"	"4.11"	"16r"	"COCCn1cc(-c2cnc(N)c(OC(C)c3cc(F)ccc3Cl)c2)cn1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	""	"UO_0000065"	"20.36"	"0.40"	"3.85"	"10.58"	"False"	"CHEMBL4628503"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4627317"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL3645004"	""	"0"	"400.49"	"0"	"4.01"	"BDBM99756"	"COc1ncccc1-c1cccn2nc(Nc3ccc(C4CCNCC4)cc3)nc12"	"IC50"	"'='"	"377.05"	"nM"	"6.42"	""	"216444"	"UO_0000065"	"16.04"	"0.29"	"2.41"	"8.41"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642332"	""	"0"	"654.82"	"1"	"4.91"	"BDBM99604"	"CN1CCN(c2cccc(N(c3cccc(N4CCN(C)CC4)c3)c3nc4c(-c5ccc(S(C)(=O)=O)cc5)cc(F)cn4n3)c2)CC1"	"IC50"	"'='"	"324.1"	"nM"	"6.49"	""	"216294"	"UO_0000065"	"9.91"	"0.19"	"1.58"	"8.06"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL4642137"	""	"0"	"360.38"	"0"	"2.00"	"J-1"	"N#CCNC(=O)c1ccc(-c2cccc3nc(NC(=O)C4CC4)nn23)cc1"	"IC50"	"'='"	"299.0"	"nM"	"6.52"	""	""	"UO_0000065"	"18.10"	"0.33"	"4.52"	"5.82"	"False"	"CHEMBL4624516"	"Inhibition of JAK2 (unknown origin) in presence of ATP at Km concentration by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4622902"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL4636613"	""	"0"	"397.39"	"0"	"2.84"	"J-3"	"O=C(Nc1nc2cccc(-c3ccc(C(=O)N4CC(F)(F)C4)cc3)n2n1)C1CC1"	"IC50"	"'='"	"139.0"	"nM"	"6.86"	""	""	"UO_0000065"	"17.26"	"0.32"	"4.02"	"8.61"	"False"	"CHEMBL4624516"	"Inhibition of JAK2 (unknown origin) in presence of ATP at Km concentration by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4622902"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL4644662"	""	"0"	"359.39"	"0"	"2.86"	"J-6"	"C=C(C#N)C(O)c1ccc(-c2cccc3nc(NC(=O)C4CC4)nn23)cc1"	"IC50"	"'='"	"55.0"	"nM"	"7.26"	""	""	"UO_0000065"	"20.20"	"0.37"	"4.40"	"7.03"	"False"	"CHEMBL4624516"	"Inhibition of JAK2 (unknown origin) in presence of ATP at Km concentration by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4622902"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL4640450"	""	"0"	"376.42"	"0"	"2.00"	"J-12"	"N#CC1(C(=O)N2CC=C(c3cccc4nc(NC(=O)C5CC5)nn34)CC2)CC1"	"IC50"	"'='"	"441.0"	"nM"	"6.36"	""	""	"UO_0000065"	"16.88"	"0.31"	"4.36"	"6.15"	"False"	"CHEMBL4624516"	"Inhibition of JAK2 (unknown origin) in presence of ATP at Km concentration by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4622902"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL4641716"	""	"0"	"386.42"	"0"	"2.34"	"J-4"	"N#CC1CN(C(=O)c2ccc(-c3cccc4nc(NC(=O)C5CC5)nn34)cc2)C1"	"IC50"	"'='"	"7430.0"	"nM"	"5.13"	""	""	"UO_0000065"	"13.27"	"0.24"	"2.79"	"4.96"	"False"	"CHEMBL4624521"	"Inhibition of JAK2 (unknown origin) expressed in mouse BAF3 cells assessed as antiproliferative activity by cell-based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4622902"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"CHEMBL3307634"	""
"CHEMBL4107397"	""	"0"	"410.48"	"0"	"3.05"	"BDBM237714"	"CC(C)(C)OC(=O)N1CC[C@H](C#N)[C@@H](n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"41.0"	"nM"	"7.39"	""	"414818"	"UO_0000065"	"18.00"	"0.34"	"4.34"	"5.85"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4112478"	""	"0"	"430.44"	"0"	"2.03"	"BDBM237750"	"COCCOC(=O)N1CC[C@@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@H](C#N)C1"	"IC50"	"'='"	"202.0"	"nM"	"6.70"	""	"414854"	"UO_0000065"	"15.55"	"0.29"	"4.66"	"4.94"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3699488"	""	"0"	"357.39"	"0"	"2.34"	"BDBM147503"	"N#C[C@@H]1CC(CO)CCC1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"22.0"	"nM"	"7.66"	""	"285430"	"UO_0000065"	"21.43"	"0.40"	"5.32"	"6.55"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647878"	""	"0"	"481.00"	"0"	"4.16"	"BDBM147990"	"N#C[C@@H]1C[C@H](C(=O)NC(C2CC2)C2CC2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"169.0"	"nM"	"6.77"	""	"285925"	"UO_0000065"	"14.08"	"0.27"	"2.61"	"5.38"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3914049"	""	"0"	"485.85"	"0"	"3.18"	"BDBM229015"	"N#CCC1(n2cc(C(N)=O)c(Nc3cncc(Cl)c3)n2)CCN(C(=O)OCC(F)(F)F)CC1"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	"400760"	"UO_0000065"	"16.10"	"0.32"	"4.64"	"5.62"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3951373"	""	"0"	"425.49"	"0"	"2.76"	"BDBM229028"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccccn3)n2)CC1"	"IC50"	"'='"	"466.0"	"nM"	"6.33"	""	"400772"	"UO_0000065"	"14.88"	"0.28"	"3.57"	"4.55"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3902783"	""	"0"	"494.38"	"0"	"4.07"	"BDBM228996"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3cc(Cl)nc(Cl)c3)n2)CC1"	"IC50"	"'='"	"33.0"	"nM"	"7.48"	""	"400741"	"UO_0000065"	"15.13"	"0.31"	"3.41"	"5.38"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3936727"	""	"0"	"459.94"	"0"	"3.41"	"BDBM229001"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3cncc(Cl)c3)n2)CC1"	"IC50"	"'='"	"21.0"	"nM"	"7.68"	""	"400746"	"UO_0000065"	"16.69"	"0.33"	"4.27"	"5.52"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3896068"	""	"0"	"517.47"	"1"	"2.91"	"BDBM229018"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(-c4cn[nH]c4)nc3)n2)CCN(C(=O)OCC(F)(F)F)CC1"	"IC50"	"'='"	"0.6"	"nM"	"9.22"	""	"400762"	"UO_0000065"	"17.82"	"0.34"	"6.31"	"5.49"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3940671"	""	"0"	"443.48"	"0"	"2.90"	"BDBM229023"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(F)nc3)n2)CC1"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"400767"	"UO_0000065"	"18.39"	"0.35"	"5.25"	"5.86"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3897371"	""	"0"	"426.48"	"0"	"2.16"	"BDBM229024"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccnnc3)n2)CC1"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	"400768"	"UO_0000065"	"18.35"	"0.34"	"5.66"	"5.15"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4483633"	""	"0"	"339.75"	"0"	"2.44"	"21"	"O=C(Nc1ccc2[nH]ncc2c1)c1c(Cl)cccc1-n1cnnn1"	"IC50"	"'='"	"820.0"	"nM"	"6.09"	""	""	"UO_0000065"	"17.91"	"0.35"	"3.65"	"6.00"	"False"	"CHEMBL4481929"	"Inhibition of JAK2 (unknown origin) after 1 hr FRET-based Z'-Lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480435"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL3908086"	""	"0"	"422.54"	"0"	"3.14"	"BDBM239960"	"Cc1cnc(Nc2cnn(C)c2)nc1NC1CCC2(CC1)CCN(C(=O)CC#N)CC2"	"IC50"	"'='"	"86.0"	"nM"	"7.07"	""	"418580"	"UO_0000065"	"16.72"	"0.31"	"3.93"	"6.32"	"False"	"CHEMBL3888834"	"Kinase Assay: JAK2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 100 μM KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC, 10 mM MgAcetate and [γ-33P-ATP](specific activity approx. 500 cpm/pmol, concentration as required). The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of 3% phosphoric acid solution. 10 μL of the reaction is then spotted onto a P30 filtermat and washed three times for 5 minutes in 75 mM phosphoric acid and once in methanol prior to drying and scintillation counting."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886854"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3943922"	""	"0"	"435.92"	"0"	"3.20"	"BDBM239968"	"Cn1cc(Nc2ncc(Cl)c(NC3CC4CN(c5ccc(C#N)cn5)CC4C3)n2)cn1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"418588"	"UO_0000065"	"19.55"	"0.38"	"5.32"	"7.92"	"False"	"CHEMBL3888834"	"Kinase Assay: JAK2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 100 μM KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC, 10 mM MgAcetate and [γ-33P-ATP](specific activity approx. 500 cpm/pmol, concentration as required). The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of 3% phosphoric acid solution. 10 μL of the reaction is then spotted onto a P30 filtermat and washed three times for 5 minutes in 75 mM phosphoric acid and once in methanol prior to drying and scintillation counting."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886854"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3974859"	""	"0"	"567.05"	"2"	"5.28"	"BDBM230082"	"Cc1c(-c2c(Cl)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)c2ccccc2n(C)c1=O"	"IC50"	"'='"	"2000.0"	"nM"	"5.70"	""	"402014"	"UO_0000065"	"10.05"	"0.19"	"0.42"	"4.63"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3891545"	""	"0"	"571.01"	"2"	"5.18"	"BDBM230106"	"Cc1c(-c2c(F)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)cc2c(Cl)cccn2c1=O"	"IC50"	"'='"	"1300.0"	"nM"	"5.89"	""	"402041"	"UO_0000065"	"10.31"	"0.20"	"0.71"	"4.80"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3917869"	""	"0"	"559.05"	"2"	"5.10"	"BDBM230111"	"Cc1c(-c2c(Cl)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)cc2sccn2c1=O"	"IC50"	"'='"	"300.0"	"nM"	"6.52"	""	"402049"	"UO_0000065"	"11.67"	"0.23"	"1.42"	"5.32"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3943055"	""	"0"	"589.00"	"2"	"5.55"	"BDBM230119"	"Cc1c(-c2c(Cl)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)[nH]c2c(F)cc(F)cc2c1=O"	"IC50"	"'='"	"1100.0"	"nM"	"5.96"	""	"402059"	"UO_0000065"	"10.12"	"0.19"	"0.41"	"4.45"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3912426"	""	"0"	"589.00"	"2"	"5.25"	"BDBM230130"	"Cn1c(=O)n(-c2cccc(-c3c(F)cc(C(N)=O)c4[nH]c5cc(C(C)(C)O)ccc5c34)c2Cl)c(=O)c2cccc(F)c21"	"IC50"	"'='"	"1900.0"	"nM"	"5.72"	""	"402072"	"UO_0000065"	"9.71"	"0.19"	"0.47"	"4.65"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3981121"	""	"0"	"388.34"	"0"	"3.42"	"BDBM198588"	"FC(F)(F)C(F)(F)CN[C@H]1CC[C@@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"370.0"	"nM"	"6.43"	""	"352666"	"UO_0000065"	"16.56"	"0.33"	"3.01"	"9.07"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3953381"	""	"0"	"474.49"	"0"	"3.68"	"BDBM198595"	"COc1ccc(C(O)(CN[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C(F)(F)F)cc1"	"IC50"	"'='"	"25.0"	"nM"	"7.60"	""	"352673"	"UO_0000065"	"16.02"	"0.31"	"3.92"	"7.57"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3962051"	""	"0"	"292.35"	"0"	"2.79"	"BDBM198655"	"N#CC1CC12CCC(c1nnn3cnc4[nH]ccc4c13)CC2"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"352733"	"UO_0000065"	"27.52"	"0.50"	"5.26"	"9.73"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3902431"	""	"0"	"309.37"	"0"	"2.19"	"BDBM198656"	"OC12CC3CC(C1)CC(c1nnn4cnc5[nH]ccc5c14)(C3)C2"	"IC50"	"'='"	"130.0"	"nM"	"6.89"	""	"352734"	"UO_0000065"	"22.26"	"0.41"	"4.70"	"8.71"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3983335"	""	"0"	"451.41"	"0"	"2.37"	"BDBM229188"	"N#CCC1(n2cc(C(N)=O)c(Nc3cncc(F)c3)n2)CCN(C(=O)OCC(F)F)CC1"	"IC50"	"'='"	"19.0"	"nM"	"7.72"	""	"400925"	"UO_0000065"	"17.10"	"0.33"	"5.35"	"5.55"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3935881"	""	"0"	"470.51"	"0"	"2.89"	"BDBM229198"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(C(=O)OC2CCCOC2)CC1"	"IC50"	"'='"	"120.0"	"nM"	"6.92"	""	"400935"	"UO_0000065"	"14.71"	"0.28"	"4.03"	"5.11"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3917676"	""	"0"	"459.51"	"0"	"3.16"	"BDBM229212"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)OCc2cccnc2)CC1"	"IC50"	"'='"	"38.0"	"nM"	"7.42"	""	"400949"	"UO_0000065"	"16.15"	"0.30"	"4.26"	"5.33"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4106951"	""	"0"	"460.49"	"0"	"3.45"	"BDBM229514"	"CC(C)(C)OC(=O)N1CC[C@@](CC#N)(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@H](F)C1"	"IC50"	"'='"	"32.0"	"nM"	"7.50"	""	"401276"	"UO_0000065"	"16.28"	"0.31"	"4.04"	"5.94"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3940150"	""	"0"	"439.52"	"0"	"3.50"	"BDBM229064"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(Cc2ccc(C#N)cc2)CC1"	"IC50"	"'='"	"243.0"	"nM"	"6.61"	""	"400800"	"UO_0000065"	"15.05"	"0.27"	"3.11"	"5.34"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3912216"	""	"0"	"464.57"	"0"	"4.78"	"BDBM229068"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(Cc2cccc3ccccc23)CC1"	"IC50"	"'='"	"1298.0"	"nM"	"5.89"	""	"400804"	"UO_0000065"	"12.67"	"0.23"	"1.11"	"5.89"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3944536"	""	"0"	"430.51"	"0"	"3.34"	"BDBM229071"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(Cc2cccc(O)c2)CC1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"400807"	"UO_0000065"	"19.10"	"0.35"	"4.88"	"6.84"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3957645"	""	"0"	"483.40"	"0"	"4.94"	"BDBM229074"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(Cc2c(Cl)cccc2Cl)CC1"	"IC50"	"'='"	"224.0"	"nM"	"6.65"	""	"400810"	"UO_0000065"	"13.76"	"0.28"	"1.71"	"6.65"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3909340"	""	"0"	"468.48"	"0"	"4.05"	"BDBM229086"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(Cc2c(F)ccc(F)c2F)CC1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	"400822"	"UO_0000065"	"16.99"	"0.32"	"3.91"	"7.96"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3892219"	""	"0"	"454.54"	"0"	"2.93"	"BDBM229104"	"Cc1ncc(CN2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccnc(F)c4)n3)CC2)s1"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	"400840"	"UO_0000065"	"17.04"	"0.33"	"4.81"	"6.16"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3935528"	""	"0"	"440.51"	"0"	"2.62"	"BDBM229114"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2cscn2)CC1"	"IC50"	"'='"	"208.0"	"nM"	"6.68"	""	"400850"	"UO_0000065"	"15.17"	"0.29"	"4.06"	"5.31"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3962716"	""	"0"	"455.49"	"0"	"2.90"	"BDBM229248"	"C[C@H](OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CC1)C1CC1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"400987"	"UO_0000065"	"17.66"	"0.33"	"5.15"	"5.78"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3901595"	""	"0"	"456.45"	"0"	"2.28"	"BDBM229325"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(S(=O)(=O)C(F)(F)F)CC1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"401064"	"UO_0000065"	"18.01"	"0.36"	"5.94"	"6.13"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3978603"	""	"0"	"494.58"	"0"	"2.83"	"BDBM229329"	"COc1ccc(S(=O)(=O)N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)CC2)cc1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"401068"	"UO_0000065"	"17.23"	"0.33"	"5.69"	"5.95"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3927483"	""	"0"	"450.49"	"0"	"4.67"	"BDBM228193"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(Nc2cccc(F)c2)CC1"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	"401145"	"UO_0000065"	"17.19"	"0.32"	"3.07"	"7.12"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3960243"	""	"0"	"458.54"	"0"	"4.48"	"BDBM229409"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(N2CCc3ccccc32)CC1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"401150"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3909143"	""	"0"	"439.54"	"0"	"3.73"	"BDBM229410"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(NC2CCCCC2)CC1"	"IC50"	"'='"	"237.0"	"nM"	"6.62"	""	"401152"	"UO_0000065"	"15.07"	"0.28"	"2.90"	"5.45"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3942031"	""	"0"	"467.94"	"0"	"4.58"	"BDBM229425"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(Nc2ccc(Cl)cc2)CC1"	"IC50"	"'='"	"770.0"	"nM"	"6.11"	""	"401174"	"UO_0000065"	"13.06"	"0.25"	"1.53"	"5.03"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL1923573"	""	"0"	"401.47"	"0"	"3.99"	"11"	"COc1ccccc1-c1ccc2cnc(Nc3ccc(N4CCOCC4)cc3)nn12"	"IC50"	"'='"	"0.23"	"nM"	"9.64"	""	""	"UO_0000065"	"24.01"	"0.44"	"5.65"	"15.08"	"False"	"CHEMBL1926252"	"Inhibition of human recombinant JAK2 using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate after 20 mins by fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1921765"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1923585"	""	"0"	"519.68"	"1"	"3.97"	"26"	"CN1CCN(c2ccc(Nc3ncc4ccc(-c5cccc(S(=O)(=O)NC(C)(C)C)c5)n4n3)cc2)CC1"	"IC50"	"'='"	"0.33"	"nM"	"9.48"	""	""	"UO_0000065"	"18.24"	"0.35"	"5.51"	"9.99"	"False"	"CHEMBL1926252"	"Inhibition of human recombinant JAK2 using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate after 20 mins by fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1921765"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL4641006"	""	"0"	"446.51"	"0"	"2.18"	"23"	"N#C[C@]1(C2CC2)C(=O)N2C[C@H]1COCC(=O)NCCCc1cccc(n1)Nc1cc2ccn1"	"IC50"	"'='"	"100.0"	"nM"	"7.00"	""	""	"UO_0000065"	"15.68"	"0.29"	"4.82"	"5.82"	"False"	"CHEMBL4627620"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4627255"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL3924291"	""	"0"	"375.43"	"0"	"3.73"	"BDBM198195"	"O=C(OCc1ccccc1)N1CCCC(c2ncn3cnc4[nH]ccc4c23)C1"	"IC50"	"'='"	"130.0"	"nM"	"6.89"	""	"351817"	"UO_0000065"	"18.34"	"0.34"	"3.16"	"9.12"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3898786"	""	"0"	"308.35"	"0"	"1.83"	"BDBM198196"	"N#CCC(=O)N1CCCC(c2ncn3cnc4[nH]ccc4c23)C1"	"IC50"	"'='"	"26.0"	"nM"	"7.58"	""	"351818"	"UO_0000065"	"24.60"	"0.45"	"5.76"	"8.42"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3981338"	""	"0"	"367.84"	"0"	"3.03"	"BDBM198362"	"Clc1cnccc1CN1CCC(c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"34.0"	"nM"	"7.47"	""	"352440"	"UO_0000065"	"20.30"	"0.39"	"4.44"	"9.96"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3912419"	""	"0"	"374.49"	"0"	"3.71"	"BDBM198373"	"c1ccc(CCNC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"72.0"	"nM"	"7.14"	""	"352451"	"UO_0000065"	"19.07"	"0.35"	"3.43"	"10.07"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3898196"	""	"0"	"376.46"	"0"	"2.96"	"BDBM198407"	"O[C@@H](CN[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1)c1ccccc1"	"IC50"	"'='"	"190.0"	"nM"	"6.72"	""	"352485"	"UO_0000065"	"17.85"	"0.33"	"3.76"	"7.38"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3939795"	""	"0"	"597.07"	"2"	"5.29"	"BDBM230084"	"COc1ccc2c(=O)n(-c3cccc(-c4c(Cl)cc(C(N)=O)c5[nH]c6cc(C(C)(C)O)ccc6c45)c3C)c(=O)n(C)c2c1"	"IC50"	"'>'"	"2000.0"	"nM"	""	""	"402016"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3923822"	""	"0"	"554.55"	"1"	"4.66"	"BDBM230154"	"Cc1c(-c2c(F)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)cc2c(F)cccn2c1=O"	"IC50"	"'='"	"800.0"	"nM"	"6.10"	""	"402052"	"UO_0000065"	"10.99"	"0.20"	"1.44"	"4.97"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3954590"	""	"0"	"587.46"	"2"	"5.62"	"BDBM230113"	"Cn1c(=O)n(-c2cccc(-c3c(Cl)cc(C(N)=O)c4[nH]c5cc(C(C)(C)O)ccc5c34)c2Cl)c(=O)c2ccccc21"	"IC50"	"'='"	"1200.0"	"nM"	"5.92"	""	"402053"	"UO_0000065"	"10.08"	"0.20"	"0.30"	"4.81"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3699486"	""	"0"	"427.48"	"0"	"3.69"	"BDBM147501"	"CC(C)(C)OC(=O)[C@H]1CCC(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"464.0"	"nM"	"6.33"	""	"285428"	"UO_0000065"	"14.82"	"0.28"	"2.64"	"5.15"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665134"	""	"0"	"386.48"	"0"	"2.25"	"BDBM112521"	"CCCS(=O)(=O)N1CC[C@@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.3428"	"nM"	"9.46"	""	"233760"	"UO_0000065"	"24.49"	"0.48"	"7.21"	"9.11"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3699503"	""	"0"	"328.35"	"0"	"2.51"	"BDBM147520"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccnc(F)c2)n1"	"IC50"	"'='"	"21.0"	"nM"	"7.68"	""	"285450"	"UO_0000065"	"23.38"	"0.44"	"5.17"	"7.00"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3658101"	""	"0"	"555.73"	"2"	"5.58"	"BDBM148382"	"Cc1ccc(NC(=O)N2CCCCC2)cc1N1CCc2nc(Nc3ccc(OCCN4CCCC4)cc3)ncc2C1"	"IC50"	"'='"	"40.0"	"nM"	"7.40"	""	"286787"	"UO_0000065"	"13.31"	"0.25"	"1.82"	"8.62"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642383"	""	"0"	"491.62"	"0"	"3.24"	"BDBM99660"	"CN1CCN(c2cccc(Nc3nc4c(NCc5cccc(S(C)(=O)=O)c5)cccn4n3)c2)CC1"	"IC50"	"'='"	"398.69"	"nM"	"6.40"	""	"216350"	"UO_0000065"	"13.02"	"0.25"	"3.16"	"6.75"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3665162"	""	"0"	"401.50"	"0"	"2.03"	"BDBM112555"	"CCCS(=O)(=O)N1CCC[C@H](Nc2ncccc2-c2cnc3nc[nH]c3n2)C1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"233793"	"UO_0000065"	"22.42"	"0.44"	"6.97"	"7.71"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647929"	""	"0"	"370.43"	"0"	"2.66"	"BDBM148049"	"CN(C)[C@@H]1CC[C@H](C#N)[C@@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)C1"	"IC50"	"'>'"	"1500.0"	"nM"	""	""	"285423"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645007"	""	"0"	"471.57"	"0"	"3.10"	"BDBM99759"	"CN(C)C(=O)CN1CCC(c2ccc(Nc3nc4c(-c5ccc[nH]c5=O)cccn4n3)cc2)CC1"	"IC50"	"'='"	"270.24"	"nM"	"6.57"	""	"216447"	"UO_0000065"	"13.93"	"0.26"	"3.47"	"6.66"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3699553"	""	"0"	"361.81"	"0"	"3.77"	"BDBM147571"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)c(F)c2)n1"	"IC50"	"'='"	"37.0"	"nM"	"7.43"	""	"285506"	"UO_0000065"	"20.54"	"0.41"	"3.66"	"7.68"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3986588"	""	"0"	"398.47"	"0"	"3.17"	"BDBM198424"	"c1cn(-c2ccc(CN3CCC(c4nnn5cnc6[nH]ccc6c45)CC3)cc2)cn1"	"IC50"	"'='"	"90.0"	"nM"	"7.05"	""	"352502"	"UO_0000065"	"17.68"	"0.32"	"3.88"	"8.81"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3956911"	""	"0"	"349.44"	"0"	"2.72"	"BDBM198504"	"N#C[C@@H]1CCN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C1"	"IC50"	"'='"	"72.0"	"nM"	"7.14"	""	"352582"	"UO_0000065"	"20.44"	"0.38"	"4.42"	"8.32"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3929398"	""	"0"	"439.57"	"0"	"4.44"	"BDBM198513"	"N#CC1(c2ccccc2)CCN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)CC1"	"IC50"	"'='"	"380.0"	"nM"	"6.42"	""	"352591"	"UO_0000065"	"14.61"	"0.27"	"1.98"	"7.47"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4112721"	""	"0"	"435.45"	"0"	"2.63"	"BDBM198523"	"O=C(N[C@@H]1CCN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C1)C(F)(F)F"	"IC50"	"'='"	"57.0"	"nM"	"7.24"	""	"352601"	"UO_0000065"	"16.64"	"0.32"	"4.61"	"7.94"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3986686"	""	"0"	"339.43"	"0"	"2.44"	"BDBM198211"	"c1cc2c(ncn3nnc(C4CCCN(Cc5cncs5)C4)c23)[nH]1"	"IC50"	"'='"	"270.0"	"nM"	"6.57"	""	"352293"	"UO_0000065"	"19.35"	"0.37"	"4.13"	"8.76"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3931293"	""	"0"	"352.32"	"0"	"2.26"	"BDBM198221"	"O=C(CC(F)(F)F)N1CCC(c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"340.0"	"nM"	"6.47"	""	"352303"	"UO_0000065"	"18.36"	"0.35"	"4.21"	"8.17"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3922240"	""	"0"	"350.40"	"0"	"3.12"	"BDBM198235"	"Fc1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	"352317"	"UO_0000065"	"22.41"	"0.41"	"4.73"	"12.65"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3913228"	""	"0"	"360.47"	"0"	"3.42"	"BDBM198237"	"c1ccc(CCCN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"1000.0"	"nM"	"6.00"	""	"352319"	"UO_0000065"	"16.64"	"0.30"	"2.58"	"9.66"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3949285"	""	"0"	"372.89"	"0"	"3.70"	"BDBM198241"	"Clc1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)s1"	"IC50"	"'='"	"2.7"	"nM"	"8.57"	""	"352323"	"UO_0000065"	"22.98"	"0.47"	"4.87"	"13.80"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3950680"	""	"0"	"446.45"	"0"	"4.83"	"BDBM198305"	"Fc1ccc(CNC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1C(F)(F)F"	"IC50"	"'='"	"79.0"	"nM"	"7.10"	""	"352383"	"UO_0000065"	"15.91"	"0.30"	"2.27"	"10.02"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3899587"	""	"0"	"420.56"	"0"	"3.41"	"BDBM198506"	"OC12CC3CC(C1)C(NC[C@H]1CC[C@H](c4nnn5cnc6[nH]ccc6c45)CC1)C(C3)C2"	"IC50"	"'='"	"350.0"	"nM"	"6.46"	""	"352584"	"UO_0000065"	"15.35"	"0.28"	"3.05"	"7.08"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3934192"	""	"0"	"396.54"	"0"	"3.51"	"BDBM198509"	"OCCN(C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1)C1CCCCC1"	"IC50"	"'='"	"54.0"	"nM"	"7.27"	""	"352587"	"UO_0000065"	"18.33"	"0.34"	"3.76"	"8.83"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3986443"	""	"0"	"413.49"	"0"	"3.11"	"BDBM198565"	"N#Cc1ccc(CCNC(=O)[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"57.0"	"nM"	"7.24"	""	"352643"	"UO_0000065"	"17.52"	"0.32"	"4.13"	"6.48"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3962364"	""	"0"	"353.47"	"0"	"2.13"	"BDBM198630"	"CN(C)C1CN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C1"	"IC50"	"'='"	"720.0"	"nM"	"6.14"	""	"352708"	"UO_0000065"	"17.38"	"0.32"	"4.01"	"9.40"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4532227"	""	"0"	"320.32"	"0"	"1.37"	"24a"	"Nc1n[nH]c2ccc(NC(=O)c3ccccc3-n3cnnn3)cc12"	"IC50"	"'='"	"6340.0"	"nM"	"5.20"	""	""	"UO_0000065"	"16.23"	"0.30"	"3.83"	"4.08"	"False"	"CHEMBL4481929"	"Inhibition of JAK2 (unknown origin) after 1 hr FRET-based Z'-Lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480435"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4574380"	""	"0"	"286.72"	"0"	"3.05"	"30b"	"Nc1n[nH]c2ccc(NC(=O)c3ccccc3Cl)cc12"	"IC50"	"'='"	"101.0"	"nM"	"7.00"	""	""	"UO_0000065"	"24.40"	"0.48"	"3.95"	"8.35"	"False"	"CHEMBL4481929"	"Inhibition of JAK2 (unknown origin) after 1 hr FRET-based Z'-Lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480435"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL3699539"	""	"0"	"390.39"	"0"	"2.67"	"BDBM147557"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc([C@@H](O)C(F)F)nc2)n1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"285487"	"UO_0000065"	"21.51"	"0.41"	"5.73"	"6.47"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647922"	""	"0"	"423.45"	"0"	"2.98"	"BDBM148037"	"N#C[C@@H]1CCCC[C@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)F)cc2)n1"	"IC50"	"'='"	"28.0"	"nM"	"7.55"	""	"285978"	"UO_0000065"	"17.84"	"0.36"	"4.57"	"5.77"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4585913"	""	"0"	"354.76"	"0"	"2.03"	"24b"	"Nc1n[nH]c2ccc(NC(=O)c3c(Cl)cccc3-n3cnnn3)cc12"	"IC50"	"'='"	"76600.0"	"nM"	"4.12"	""	""	"UO_0000065"	"11.60"	"0.22"	"2.09"	"3.23"	"False"	"CHEMBL4481929"	"Inhibition of JAK2 (unknown origin) after 1 hr FRET-based Z'-Lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480435"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL3652329"	""	"0"	"512.70"	"1"	"1.89"	"BDBM113139"	"CN(C)S(=O)(=O)C[C@H]1CCCN(S(=O)(=O)C[C@H]2CC[C@H](N(C)c3ncnc4[nH]ccc34)CC2)C1"	"IC50"	"'='"	"50.8"	"nM"	"7.29"	""	"234582"	"UO_0000065"	"14.23"	"0.29"	"5.40"	"6.10"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3703013"	""	"0"	"488.51"	"0"	"3.15"	"BDBM147723"	"N#C[C@H]1C[C@@H](N2C[C@@H]3[C@@H](CO)[C@@H]3C2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	"285657"	"UO_0000065"	"15.76"	"0.30"	"4.55"	"6.41"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652374"	""	"0"	"470.60"	"0"	"2.27"	"BDBM113185"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC[C@](O)(c3ccccn3)C2)CC1"	"IC50"	"'='"	"35.8"	"nM"	"7.45"	""	"234628"	"UO_0000065"	"15.82"	"0.31"	"5.18"	"6.46"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3703066"	""	"0"	"418.45"	"0"	"3.12"	"BDBM147776"	"CN(C)[C@@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(OC(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"32.0"	"nM"	"7.50"	""	"285710"	"UO_0000065"	"17.91"	"0.34"	"4.37"	"6.86"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4577029"	""	"0"	"443.56"	"0"	"3.71"	"11e'"	"C=CC(=O)Nc1ccc(CNc2cc(Nc3ccc(N4CCN(C)CC4)cc3)ncn2)cc1"	"IC50"	"'>'"	"3000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4482009"	"Inhibition of human JAK2 using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and further incubated for 30 mins and subsequently measured after 1 hr by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480445"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4546009"	""	"0"	"456.55"	"0"	"3.44"	"14e"	"CN1CCN(c2ccc(Nc3cc(NCc4cccc(NC(=O)CC#N)c4)ncn3)cc2)CC1"	"IC50"	"'='"	"1015.0"	"nM"	"5.99"	""	""	"UO_0000065"	"13.13"	"0.24"	"2.55"	"5.49"	"False"	"CHEMBL4482009"	"Inhibition of human JAK2 using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and further incubated for 30 mins and subsequently measured after 1 hr by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480445"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4560222"	""	"0"	"444.54"	"0"	"4.18"	"12d"	"C/C=C/C(=O)Nc1ccc(CNc2cc(Nc3ccc(N4CCOCC4)cc3)ncn2)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4482009"	"Inhibition of human JAK2 using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and further incubated for 30 mins and subsequently measured after 1 hr by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480445"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4516549"	""	"0"	"401.47"	"0"	"3.56"	"15d"	"N#CNc1ccc(CNc2cc(Nc3ccc(N4CCOCC4)cc3)ncn2)cc1"	"IC50"	"'='"	"345.0"	"nM"	"6.46"	""	""	"UO_0000065"	"16.10"	"0.29"	"2.90"	"6.59"	"False"	"CHEMBL4482009"	"Inhibition of human JAK2 using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and further incubated for 30 mins and subsequently measured after 1 hr by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480445"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL3645045"	""	"0"	"503.48"	"2"	"5.49"	"BDBM99812"	"FC(F)COc1ccc(C(F)(F)F)cc1-c1cccn2nc(Nc3ccc4c(c3)CCNCC4)nc12"	"IC50"	"'='"	"257.43"	"nM"	"6.59"	""	"216485"	"UO_0000065"	"13.09"	"0.25"	"1.10"	"10.38"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703049"	""	"0"	"462.48"	"0"	"3.05"	"BDBM147759"	"N#C[C@H]1C[C@H](NC2COC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(CC(F)(F)F)cc2)n1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"285693"	"UO_0000065"	"18.16"	"0.35"	"5.35"	"7.12"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647860"	""	"0"	"360.81"	"0"	"2.00"	"BDBM147970"	"N#C[C@H]1C[C@@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)nc2)n1"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	"285904"	"UO_0000065"	"21.77"	"0.43"	"5.85"	"6.05"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702925"	""	"0"	"343.82"	"0"	"3.63"	"BDBM147624"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"25.0"	"nM"	"7.60"	""	"285554"	"UO_0000065"	"22.11"	"0.43"	"3.97"	"7.86"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4635255"	""	"0"	"382.83"	"0"	"4.91"	"16e"	"CC(Oc1cc(-c2cnn3ccccc23)cnc1N)c1cc(F)ccc1Cl"	"IC50"	"'='"	"61.0"	"nM"	"7.21"	""	""	"UO_0000065"	"18.85"	"0.36"	"2.30"	"11.02"	"False"	"CHEMBL4628503"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4627317"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL4638672"	""	"0"	"383.81"	"0"	"4.31"	"16f"	"CC(Oc1cc(-c2cnn3cccnc23)cnc1N)c1cc(F)ccc1Cl"	"IC50"	"'='"	"145.0"	"nM"	"6.84"	""	""	"UO_0000065"	"17.82"	"0.35"	"2.53"	"8.73"	"False"	"CHEMBL4628503"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4627317"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL4644279"	""	"0"	"416.88"	"0"	"4.81"	"16m"	"CC(Oc1cc(-c2cnn(C3CCOCC3)c2)cnc1N)c1cc(F)ccc1Cl"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	""	"UO_0000065"	"19.42"	"0.38"	"3.29"	"10.77"	"False"	"CHEMBL4628503"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4627317"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL4633005"	""	"0"	"388.83"	"0"	"4.03"	"16n"	"CC(Oc1cc(-c2cnn(C3COC3)c2)cnc1N)c1cc(F)ccc1Cl"	"IC50"	"'='"	"25.0"	"nM"	"7.60"	""	""	"UO_0000065"	"19.55"	"0.38"	"3.57"	"10.11"	"False"	"CHEMBL4628503"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4627317"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL3658106"	""	"0"	"567.66"	"2"	"5.37"	"BDBM148398"	"Cc1ccc(NC(=O)CC(C)C(F)(F)F)cc1N1CCc2nc(Nc3ccc(N4CCN(C)CC4)cc3)ncc2C1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"286792"	"UO_0000065"	"14.17"	"0.27"	"2.68"	"10.50"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645080"	""	"0"	"520.58"	"1"	"4.27"	"BDBM99849"	"CN(C)C(=O)CN1CCc2ccc(Nc3nc4c(-c5ccccc5OCC(F)F)cccn4n3)cc2CC1"	"IC50"	"'='"	"196.66"	"nM"	"6.71"	""	"216522"	"UO_0000065"	"12.88"	"0.24"	"2.44"	"8.94"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652310"	""	"0"	"420.58"	"0"	"1.92"	"BDBM113120"	"CC1CN(S(=O)(=O)C[C@H]2CC[C@H](N(C)c3ncnc4[nH]ccc34)CC2)CCN1C"	"IC50"	"'='"	"126.0"	"nM"	"6.90"	""	"234563"	"UO_0000065"	"16.41"	"0.32"	"4.98"	"8.08"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3622137"	""	"0"	"449.58"	"0"	"4.53"	"18"	"CCn1c(C(=O)N(C2CC2)C2CC2)cc2c3c(ncn3C)c(Nc3nc(C)c(C)s3)nc21"	"IC50"	"'='"	"2.5"	"nM"	"8.60"	""	""	"UO_0000065"	"19.13"	"0.37"	"4.07"	"10.64"	"False"	"CHEMBL3625473"	"Inhibition of JAK2 (unknown origin) using 5-FAMKKKKEEIYFFFG-OH as substrate after 60 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621098"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3652279"	""	"0"	"433.58"	"0"	"2.58"	"BDBM113087"	"CC(=O)C1CCCN(S(=O)(=O)C[C@H]2CC[C@H](N(C)c3ncnc4[nH]ccc34)CC2)C1"	"IC50"	"'='"	"21.9"	"nM"	"7.66"	""	"234531"	"UO_0000065"	"17.67"	"0.35"	"5.08"	"7.72"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3699536"	""	"0"	"422.41"	"0"	"3.15"	"BDBM147554"	"C[C@@](O)(c1ccc(Nc2nn([C@H]3CCCC[C@@H]3C#N)cc2C(N)=O)cn1)C(F)(F)F"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	"285484"	"UO_0000065"	"18.52"	"0.36"	"4.67"	"6.03"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645060"	""	"0"	"357.42"	"0"	"3.75"	"BDBM99828"	"COc1cccc(-c2cccn3nc(Nc4ccc5c(c4)CNC5)nc23)c1"	"IC50"	"'='"	"6.63"	"nM"	"8.18"	""	"216501"	"UO_0000065"	"22.88"	"0.41"	"4.43"	"12.88"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647801"	""	"0"	"444.97"	"0"	"3.63"	"BDBM147904"	"COC(C)(C)CN[C@H]1CCC(n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"48.0"	"nM"	"7.32"	""	"285838"	"UO_0000065"	"16.45"	"0.32"	"3.69"	"6.20"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642338"	""	"0"	"507.62"	"1"	"2.76"	"BDBM99610"	"CN1CCN(c2cccc(Nc3nc4c(Nc5cccnc5N(C)S(C)(=O)=O)cccn4n3)c2)CC1"	"IC50"	"'='"	"60.26"	"nM"	"7.22"	""	"216300"	"UO_0000065"	"14.22"	"0.27"	"4.46"	"6.50"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3622129"	""	"0"	"382.47"	"0"	"2.11"	"7"	"CNc1nc2c(cc(C(=O)N(C3CC3)C3CC3)n2C[C@@H](C)O)c2c1ncn2C"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	""	"UO_0000065"	"20.53"	"0.38"	"5.74"	"8.90"	"False"	"CHEMBL3625473"	"Inhibition of JAK2 (unknown origin) using 5-FAMKKKKEEIYFFFG-OH as substrate after 60 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621098"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL2062812"	""	"0"	"402.48"	"0"	"4.03"	"BDBM50389202"	"CN1CCN(c2cccc(Nc3nc4c(-c5ccc(F)cc5)cccn4n3)c2)CC1"	"IC50"	"'='"	"29.07"	"nM"	"7.54"	""	"216520"	"UO_0000065"	"18.73"	"0.34"	"3.51"	"15.48"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3645113"	""	"0"	"393.47"	"0"	"2.85"	"BDBM99887"	"CS(=O)(=O)c1ccc(-c2cccn3nc(NCCc4ccccn4)nc23)cc1"	"IC50"	"'='"	"9999.0"	"nM"	"5.00"	""	"216555"	"UO_0000065"	"12.71"	"0.24"	"2.15"	"5.60"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647804"	""	"0"	"410.52"	"0"	"2.97"	"BDBM147907"	"COCC(C)(C)N[C@H]1CCC(n2cc(C(N)=O)c(Nc3ccccc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"170.0"	"nM"	"6.77"	""	"285841"	"UO_0000065"	"16.49"	"0.31"	"3.80"	"5.74"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642394"	""	"0"	"535.67"	"1"	"4.08"	"BDBM99672"	"CN(Cc1ccccc1Nc1cccn2nc(Nc3ccc(OCCN4CCCC4)cc3)nc12)S(C)(=O)=O"	"IC50"	"'='"	"143.05"	"nM"	"6.84"	""	"216362"	"UO_0000065"	"12.78"	"0.25"	"2.76"	"6.57"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652335"	""	"0"	"416.55"	"0"	"2.52"	"BDBM113146"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCC[C@H](C#N)C2)CC1"	"IC50"	"'='"	"32.1"	"nM"	"7.49"	""	"234589"	"UO_0000065"	"17.99"	"0.35"	"4.97"	"7.07"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3621496"	""	"0"	"430.48"	"0"	"3.61"	"6"	"CN1CCN(C(=O)c2ccc3c(c2)[nH]c2c(C(N)=O)ccc(-c4ccccc4F)c23)CC1"	"IC50"	"'='"	"50.0"	"nM"	"7.30"	""	""	"UO_0000065"	"16.96"	"0.31"	"3.69"	"8.86"	"False"	"CHEMBL3627422"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621099"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3647845"	""	"0"	"451.45"	"0"	"3.11"	"BDBM147954"	"C[C@]1(O)CC[C@H](n2cc(C(N)=O)c(Nc3ccc([C@@](C)(O)C(F)(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"285888"	"UO_0000065"	"19.94"	"0.38"	"5.89"	"6.56"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642307"	""	"0"	"399.50"	"0"	"4.61"	"BDBM99577"	"c1ccc(-c2cccc3nc(Nc4ccc(OCCN5CCCC5)cc4)nn23)cc1"	"IC50"	"'='"	"9999.0"	"nM"	"5.00"	""	"216267"	"UO_0000065"	"12.52"	"0.23"	"0.39"	"9.14"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3644997"	""	"0"	"302.36"	"0"	"2.18"	"BDBM99749"	"Cc1cccn2nc(Nc3ccc(S(C)(=O)=O)cc3)nc12"	"IC50"	"'='"	"2623.32"	"nM"	"5.58"	""	"216437"	"UO_0000065"	"18.46"	"0.36"	"3.40"	"7.31"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3612840"	""	"0"	"511.61"	"2"	"5.06"	"13b"	"Nc1ncc(-c2cnn(CC(=O)N3CCOCC3)c2)c2scc(-c3ccc(Oc4ccccc4)cc3)c12"	"IC50"	"'='"	"6864.0"	"nM"	"5.16"	""	""	"UO_0000065"	"10.09"	"0.19"	"0.10"	"5.41"	"False"	"CHEMBL3614376"	"Inhibition of JAK2 (unknown origin) after 1 hr by ELISA based assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3611978"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3703098"	""	"0"	"423.50"	"0"	"2.98"	"BDBM147813"	"N#C[C@H]1C[C@@H](N2CC3(CCC3)C2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccnc(F)c2)n1"	"IC50"	"'='"	"36.0"	"nM"	"7.44"	""	"285747"	"UO_0000065"	"17.58"	"0.33"	"4.46"	"6.60"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651046"	""	"0"	"372.40"	"0"	"4.95"	"BDBM153223"	"C=C(C)C(=O)Nc1cccc(-c2ncnc3[nH]cc(-c4ccc(F)cc4)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294171"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3650683"	""	"0"	"387.47"	"0"	"2.38"	"BDBM47170"	"CS(=O)(=O)c1ccc(Nc2nn([C@@H]3CCCC[C@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"198680"	"UO_0000065"	"21.05"	"0.41"	"5.77"	"6.23"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665185"	""	"0"	"419.54"	"0"	"1.97"	"BDBM112579"	"CSc1ncc(-c2cnc3[nH]ccc3n2)c(N[C@H]2CCCN(S(C)(=O)=O)C2)n1"	"IC50"	"'='"	"0.139"	"nM"	"9.86"	""	"233816"	"UO_0000065"	"23.49"	"0.48"	"7.89"	"8.44"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3699535"	""	"0"	"422.41"	"0"	"3.15"	"BDBM147553"	"C[C@](O)(c1ccc(Nc2nn([C@H]3CCCC[C@@H]3C#N)cc2C(N)=O)cn1)C(F)(F)F"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	"285483"	"UO_0000065"	"18.84"	"0.36"	"4.81"	"6.13"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645061"	""	"0"	"472.57"	"0"	"4.55"	"BDBM99829"	"CN(C)C(=O)CN1CCC(c2ccc(Nc3nc4c(-c5ccc(F)cc5)cccn4n3)cc2)CC1"	"IC50"	"'='"	"10.36"	"nM"	"7.99"	""	"216502"	"UO_0000065"	"16.90"	"0.31"	"3.43"	"12.14"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647893"	""	"0"	"476.92"	"0"	"3.77"	"BDBM148005"	"N#C[C@H]1C[C@@H](C(=O)NC2CC(F)(F)C2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"172.0"	"nM"	"6.76"	""	"285940"	"UO_0000065"	"14.18"	"0.28"	"2.99"	"5.38"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651020"	""	"0"	"350.38"	"0"	"3.32"	"BDBM153197"	"C/C=C\C(=O)Nc1cccc(-c2ncnc3[nH]cc(C(=O)OCC)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294145"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL2035044"	""	"0"	"373.46"	"0"	"4.05"	"13d, 95:5 trans/Cis mixture"	"CN1C/C=C/CCOc2cc(ccn2)-c2ccnc(n2)Nc2cccc(c2)C1"	"IC50"	"'='"	"260.0"	"nM"	"6.58"	""	""	"UO_0000065"	"17.63"	"0.32"	"2.54"	"10.42"	"False"	"CHEMBL2040119"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2034857"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2035056"	""	"0"	"436.51"	"0"	"4.02"	"14h, 95:5 trans/Cis mixture"	"COCCOc1ccc2cc1CN(C)C/C=C/COCc1ccc(o1)-c1ccnc(n1)N2"	"IC50"	"'='"	"1100.0"	"nM"	"5.96"	""	""	"UO_0000065"	"13.65"	"0.25"	"1.94"	"7.28"	"False"	"CHEMBL2040119"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2034857"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL1923588"	""	"0"	"415.50"	"0"	"3.30"	"29"	"COc1ccc(-c2ccc3cnc(Nc4ccc(N5CCN(C)CC5)cc4)nn23)cn1"	"IC50"	"'='"	"0.3"	"nM"	"9.52"	""	""	"UO_0000065"	"22.92"	"0.42"	"6.22"	"13.45"	"False"	"CHEMBL1926252"	"Inhibition of human recombinant JAK2 using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate after 20 mins by fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1921765"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL1944698"	"ZOTIRACICLIB"	"1"	"372.47"	"0"	"4.66"	"50"	"CN1C/C=C/CCOc2cccc(c2)-c2ccnc(n2)Nc2cccc(c2)C1"	"IC50"	"'='"	"73.0"	"nM"	"7.14"	""	""	"UO_0000065"	"19.16"	"0.35"	"2.48"	"14.19"	"False"	"CHEMBL3856507"	"Inhibition of human recombinant GST-tagged JAK2 expressed in baculovirus expression system"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3856187"	"1"	"Scientific Literature"	"J Med Chem"	"2016"	"None"	""
"CHEMBL384820"	""	"0"	"435.54"	"1"	"5.12"	"26"	"C[C@H](Nc1cc(-c2ccc(N(C)C)cc2)nc(-n2cnc3ccncc32)n1)c1ccccc1"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	""	"UO_0000065"	"17.68"	"0.32"	"2.58"	"10.73"	"False"	"CHEMBL908418"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139695"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2006"	"None"	""
"CHEMBL222027"	""	"0"	"382.43"	"0"	"4.64"	"25"	"C[C@H](Nc1cc(-c2ccoc2)nc(-n2cnc3ccncc32)n1)c1ccccc1"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	""	"UO_0000065"	"20.39"	"0.37"	"3.16"	"9.55"	"False"	"CHEMBL908418"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139695"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2006"	"None"	""
"CHEMBL220969"	""	"0"	"417.48"	"0"	"4.92"	"31"	"C[C@H](Nc1cc(-c2cccc(C#N)c2)nc(-n2cnc3ccncc32)n1)c1ccccc1"	"IC50"	"'='"	"56.0"	"nM"	"7.25"	""	""	"UO_0000065"	"17.37"	"0.31"	"2.33"	"7.86"	"False"	"CHEMBL908418"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139695"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2006"	"None"	""
"CHEMBL221912"	""	"0"	"308.35"	"0"	"2.13"	"17"	"COC[C@H](C)Nc1ccnc(-n2cnc3ccc(C#N)cc32)n1"	"IC50"	"'='"	"124.0"	"nM"	"6.91"	""	""	"UO_0000065"	"22.40"	"0.41"	"4.78"	"7.79"	"False"	"CHEMBL908418"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139695"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2006"	"None"	""
"CHEMBL4248451"	""	"0"	"367.42"	"0"	"1.04"	"13h"	"COCCn1cc(-c2nn(C3CCN(C#N)CC3)c3ncnc(N)c23)cn1"	"IC50"	"'='"	"146.8"	"nM"	"6.83"	""	""	"UO_0000065"	"18.60"	"0.35"	"5.79"	"5.52"	"False"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL3622834"	""	"0"	"296.33"	"0"	"1.47"	"5k"	"NCCn1c(-c2ccc(O)cc2)nc2cc(C(N)=O)ccc21"	"IC50"	"'='"	"1300.0"	"nM"	"5.89"	""	""	"UO_0000065"	"19.86"	"0.37"	"4.42"	"5.49"	"False"	"CHEMBL3625898"	"Inhibition of JAK2 (unknown origin) using 35 uM of ATP and Tyr6 peptide by Z'-LYTE kinase assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621116"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL3703009"	""	"0"	"460.50"	"0"	"4.46"	"BDBM147719"	"C[C@@H]1C[C@@H](C)N1[C@@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(C(F)(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"575.0"	"nM"	"6.24"	""	"285653"	"UO_0000065"	"13.55"	"0.26"	"1.78"	"6.24"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703099"	""	"0"	"411.49"	"0"	"2.83"	"BDBM147814"	"CC1(C)CN([C@H]2CC[C@H](n3cc(C(N)=O)c(Nc4ccnc(F)c4)n3)[C@@H](C#N)C2)C1"	"IC50"	"'='"	"50.0"	"nM"	"7.30"	""	"285748"	"UO_0000065"	"17.74"	"0.33"	"4.47"	"6.47"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647836"	""	"0"	"385.86"	"0"	"3.16"	"BDBM147944"	"C=C[C@]1(O)CC[C@H](n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"25.0"	"nM"	"7.60"	""	"285878"	"UO_0000065"	"19.70"	"0.38"	"4.44"	"6.50"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702933"	""	"0"	"376.42"	"0"	"2.77"	"BDBM147635"	"N#C[C@H]1CCCCC1n1cc(C(N)=O)c(Nc2ccc(-c3cn[nH]c3)nc2)n1"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	"285566"	"UO_0000065"	"20.71"	"0.38"	"5.03"	"5.64"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL2385543"	""	"0"	"561.09"	"2"	"6.82"	"2n"	"O=C1c2oc(-c3ccc(Cl)cc3)cc2Cc2cc(N3CCNCC3)ccc2N1Cc1ccccc1-c1cccnc1"	"IC50"	"'='"	"11000.0"	"nM"	"4.96"	""	""	"UO_0000065"	"8.84"	"0.17"	"-1.86"	"8.05"	"False"	"CHEMBL2388367"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2384992"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL3746341"	""	"0"	"430.35"	"0"	"4.15"	"21"	"COc1ccc(-c2nc3c(NCC4CCN(C)CC4)c(Br)cnc3[nH]2)cc1"	"IC50"	"'='"	"4740.0"	"nM"	"5.32"	""	""	"UO_0000065"	"12.37"	"0.27"	"1.17"	"8.06"	"False"	"CHEMBL3751000"	"Inhibition of N-terminal GST-fused recombinant JAK2 (831 to 1132 residues) (unknown origin) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate by microfluidic capillary electrophoresis method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3745697"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3746783"	""	"0"	"399.93"	"0"	"4.35"	"8"	"COc1ccc(-c2nc3c(NCC4CCN(C)CC4)c(Cl)cnc3[nH]2)c(C)c1"	"IC50"	"'='"	"2700.0"	"nM"	"5.57"	""	""	"UO_0000065"	"13.92"	"0.27"	"1.22"	"8.43"	"False"	"CHEMBL3751000"	"Inhibition of N-terminal GST-fused recombinant JAK2 (831 to 1132 residues) (unknown origin) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate by microfluidic capillary electrophoresis method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3745697"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3746351"	""	"0"	"433.97"	"0"	"3.44"	"5"	"CN1CCC(CNc2c(Cl)cnc3[nH]c(-c4ccc(S(C)(=O)=O)cc4)nc23)CC1"	"IC50"	"'='"	"2780.0"	"nM"	"5.56"	""	""	"UO_0000065"	"12.80"	"0.26"	"2.12"	"6.11"	"False"	"CHEMBL3751000"	"Inhibition of N-terminal GST-fused recombinant JAK2 (831 to 1132 residues) (unknown origin) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate by microfluidic capillary electrophoresis method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3745697"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3747305"	""	"0"	"401.90"	"0"	"3.71"	"25"	"COc1ccc(-c2nc3c(NCC4CCNCC4)c(Cl)cnc3[nH]2)cc1OC"	"IC50"	"'='"	"2270.0"	"nM"	"5.64"	""	""	"UO_0000065"	"14.04"	"0.28"	"1.93"	"6.71"	"False"	"CHEMBL3751000"	"Inhibition of N-terminal GST-fused recombinant JAK2 (831 to 1132 residues) (unknown origin) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate by microfluidic capillary electrophoresis method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3745697"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3922588"	""	"0"	"457.54"	"0"	"3.03"	"16d"	"CN1CCN(c2ccc(Nc3nccc(-c4cc5c(o4)CCN(C(=O)CC#N)C5)n3)cc2)CC1"	"IC50"	"'='"	"2338.0"	"nM"	"5.63"	""	""	"UO_0000065"	"12.31"	"0.23"	"2.60"	"5.55"	"False"	"CHEMBL3868066"	"Inhibition of JAK2 in human TF1 cells assessed as suppression of cell growth"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3867460"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2017"	"CHEMBL3307972"	""
"CHEMBL3922588"	""	"0"	"457.54"	"0"	"3.03"	"16d"	"CN1CCN(c2ccc(Nc3nccc(-c4cc5c(o4)CCN(C(=O)CC#N)C5)n3)cc2)CC1"	"IC50"	"'='"	"53.7"	"nM"	"7.27"	""	""	"UO_0000065"	"15.89"	"0.29"	"4.24"	"7.16"	"False"	"CHEMBL3868063"	"Inhibition of GST-tagged recombinant human JAK2 expressed in baculovirus using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3867460"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2017"	"None"	""
"CHEMBL3658857"	""	"0"	"447.48"	"0"	"1.89"	"BDBM159776"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](CS(=O)(=O)N2CCC(O)(C(F)(F)F)CC2)C1"	"IC50"	"'='"	"88.0"	"nM"	"7.06"	""	"302586"	"UO_0000065"	"15.77"	"0.32"	"5.17"	"6.89"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642312"	""	"0"	"477.59"	"0"	"3.26"	"BDBM99584"	"CN1CCN(c2ccc(Nc3nc4cccc(-c5cccc(NS(C)(=O)=O)c5)n4n3)cc2)CC1"	"IC50"	"'='"	"19.0"	"nM"	"7.72"	""	"216274"	"UO_0000065"	"16.17"	"0.31"	"4.46"	"8.14"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL2062802"	""	"0"	"449.54"	"0"	"3.38"	"BDBM99529"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4cccc(N5CCOCC5)c4)nc23)cc1"	"IC50"	"'='"	"0.4"	"nM"	"9.40"	""	"216221"	"UO_0000065"	"20.91"	"0.40"	"6.02"	"10.58"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642421"	""	"0"	"473.56"	"0"	"4.03"	"BDBM99699"	"CN(c1ccccc1CNc1cccn2nc(Nc3ccc4cnccc4c3)nc12)S(C)(=O)=O"	"IC50"	"'='"	"116.17"	"nM"	"6.93"	""	"216389"	"UO_0000065"	"14.64"	"0.28"	"2.90"	"6.64"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703014"	""	"0"	"462.48"	"0"	"3.09"	"BDBM147724"	"N#C[C@H]1C[C@H](NCC2(O)CC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"48.0"	"nM"	"7.32"	""	"285658"	"UO_0000065"	"15.83"	"0.30"	"4.23"	"5.67"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642419"	""	"0"	"657.80"	"1"	"4.05"	"BDBM99697"	"CP(C)(=O)c1ccc(-c2cccn3nc(N(CCS(C)(=O)=O)c4cccc(C5CCN(CCS(C)(=O)=O)CC5)c4)nc23)cc1"	"IC50"	"'='"	"95.79"	"nM"	"7.02"	""	"216387"	"UO_0000065"	"10.67"	"0.22"	"2.97"	"5.75"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3702911"	""	"0"	"513.02"	"1"	"4.11"	"BDBM147610"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)NCc3ccc(Cl)cc3)cc2)n1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"285540"	"UO_0000065"	"16.37"	"0.33"	"4.29"	"5.88"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3658114"	""	"0"	"611.71"	"2"	"5.24"	"BDBM148429"	"Cc1ccc(NC(=O)CC(C)C(F)(F)F)cc1N1CCc2nc(Nc3ccc(OCCN4CCN(C)CC4)cc3)ncc2C1"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	"286818"	"UO_0000065"	"12.79"	"0.24"	"2.58"	"9.11"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647815"	""	"0"	"460.50"	"0"	"4.32"	"BDBM147920"	"CN(CC1CC1)[C@@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(C(F)(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"135.0"	"nM"	"6.87"	""	"285854"	"UO_0000065"	"14.92"	"0.28"	"2.55"	"6.87"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3301607"	"FILGOTINIB"	"4"	"425.51"	"0"	"1.98"	"Filgotinib"	"O=C(Nc1nc2cccc(-c3ccc(CN4CCS(=O)(=O)CC4)cc3)n2n1)C1CC1"	"IC50"	"'='"	"31.37"	"nM"	"7.50"	""	"221709"	"UO_0000065"	"17.63"	"0.34"	"5.52"	"7.76"	"False"	"CHEMBL3707887"	"Inhibition Assay: In vitro inhibition assay using various enzyme."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638964"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647897"	""	"0"	"508.93"	"1"	"4.32"	"BDBM148009"	"N#C[C@H]1C[C@@H](C(=O)N[C@@H](C2CC2)C(F)(F)F)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'>'"	"500.0"	"nM"	""	""	"285944"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703003"	""	"0"	"462.48"	"0"	"3.09"	"BDBM147713"	"N#C[C@H]1C[C@@H](NCC2(O)CC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"23.0"	"nM"	"7.64"	""	"285647"	"UO_0000065"	"16.52"	"0.32"	"4.55"	"5.92"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4457617"	""	"0"	"459.94"	"0"	"4.28"	"8e"	"COc1ccc(Nc2nc(Nc3cnn(CCCCCCC(=O)NO)c3)ncc2Cl)cc1"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	""	"UO_0000065"	"17.39"	"0.34"	"3.72"	"6.34"	"False"	"CHEMBL4347596"	"Inhibition of recombinant human JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate measured after 60 mins by LANCE assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4346670"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL3651026"	""	"0"	"418.38"	"0"	"4.25"	"BDBM153203"	"CCOC(=O)c1c[nH]c2ncnc(-c3cccc(NC(=O)/C=C(/C)C(F)(F)F)c3)c12"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294151"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699483"	""	"0"	"432.50"	"0"	"3.89"	"BDBM147498"	"N#C[C@H]1CC[C@H](NCc2ccccc2)C[C@@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"55.0"	"nM"	"7.26"	""	"285425"	"UO_0000065"	"16.79"	"0.31"	"3.37"	"6.67"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699491"	""	"0"	"337.43"	"0"	"3.62"	"BDBM147506"	"CC1(C)CC[C@@H](C#N)[C@@H](n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"176.0"	"nM"	"6.75"	""	"285433"	"UO_0000065"	"20.02"	"0.37"	"3.13"	"6.98"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647895"	""	"0"	"468.87"	"0"	"3.54"	"BDBM148007"	"N#C[C@H]1C[C@@H](C(=O)NCC(F)(F)F)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"218.0"	"nM"	"6.66"	""	"285942"	"UO_0000065"	"14.21"	"0.28"	"3.12"	"5.29"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4526274"	""	"0"	"450.33"	"0"	"4.53"	"8m"	"O=C(CCCCCn1cc(Nc2ncc(Cl)c(Nc3ccc(Cl)cc3)n2)cn1)NO"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	""	"UO_0000065"	"18.65"	"0.38"	"3.87"	"7.18"	"False"	"CHEMBL4347596"	"Inhibition of recombinant human JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate measured after 60 mins by LANCE assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4346670"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL3702897"	""	"0"	"365.40"	"0"	"1.62"	"BDBM147596"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2cnc3c(c2)CNC3=O)n1"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"285526"	"UO_0000065"	"22.32"	"0.41"	"6.53"	"5.88"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702945"	""	"0"	"399.47"	"0"	"3.20"	"BDBM147647"	"CC(C)(CF)c1ccc(Nc2nn([C@H]3CC[C@@H](O)C[C@@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"285579"	"UO_0000065"	"20.58"	"0.39"	"5.02"	"7.03"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL1789941"	"RUXOLITINIB"	"4"	"306.37"	"0"	"3.47"	"26; INCB018424"	"N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"2.8"	"nM"	"8.55"	""	""	"UO_0000065"	"27.92"	"0.51"	"5.08"	"10.28"	"False"	"CHEMBL4356086"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4354810"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL3622132"	""	"0"	"440.50"	"0"	"2.90"	"13"	"CCn1c(C(=O)N(C2CC2)C2CC2)cc2c3c(ncn3C)c(NC(=O)OCCOC)nc21"	"IC50"	"'='"	"25.0"	"nM"	"7.60"	""	""	"UO_0000065"	"17.26"	"0.32"	"4.70"	"7.34"	"False"	"CHEMBL3625473"	"Inhibition of JAK2 (unknown origin) using 5-FAMKKKKEEIYFFFG-OH as substrate after 60 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621098"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3622130"	""	"0"	"352.44"	"0"	"2.75"	"8"	"CCn1c(C(=O)N(C2CC2)C2CC2)cc2c3c(ncn3C)c(NC)nc21"	"IC50"	"'='"	"350.0"	"nM"	"6.46"	""	""	"UO_0000065"	"18.32"	"0.34"	"3.71"	"9.50"	"False"	"CHEMBL3625474"	"Inhibition of JAK2 in human SET2 cells assessed as inhibition of cell proliferation after 72 hrs by [3H]-thymidine incorporation assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621098"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3622132"	""	"0"	"440.50"	"0"	"2.90"	"13"	"CCn1c(C(=O)N(C2CC2)C2CC2)cc2c3c(ncn3C)c(NC(=O)OCCOC)nc21"	"IC50"	"'='"	"580.0"	"nM"	"6.24"	""	""	"UO_0000065"	"14.16"	"0.27"	"3.34"	"6.03"	"False"	"CHEMBL3625474"	"Inhibition of JAK2 in human SET2 cells assessed as inhibition of cell proliferation after 72 hrs by [3H]-thymidine incorporation assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621098"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3622139"	""	"0"	"358.40"	"0"	"0.21"	"2"	"CNc1nc2c(cc(C(=O)NC3CC3)n2C[C@H](O)CO)c2c1ncn2C"	"IC50"	"'='"	"570.0"	"nM"	"6.24"	""	""	"UO_0000065"	"17.42"	"0.33"	"6.03"	"5.33"	"False"	"CHEMBL3625473"	"Inhibition of JAK2 (unknown origin) using 5-FAMKKKKEEIYFFFG-OH as substrate after 60 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621098"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3647759"	""	"0"	"510.54"	"1"	"3.20"	"BDBM147862"	"CC1CN([C@H]2CC[C@H](n3cc(C(N)=O)c(Nc4ccc(S(=O)(=O)C(F)(F)F)cc4)n3)[C@@H](C#N)C2)C1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"285796"	"UO_0000065"	"15.76"	"0.31"	"4.85"	"6.00"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642267"	""	"0"	"373.42"	"0"	"3.51"	"BDBM99526"	"CNC(=O)c1ccc(-c2cccn3nc(Nc4ccccc4OC)nc23)cc1"	"IC50"	"'='"	"9999.0"	"nM"	"5.00"	""	"216218"	"UO_0000065"	"13.39"	"0.24"	"1.49"	"6.21"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL4237694"	""	"0"	"397.49"	"0"	"0.61"	"9e"	"CN(C)CC(=O)N1CCCC(Cn2nc(-c3cnn(C)c3)c3c(N)ncnc32)C1"	"IC50"	"'='"	"1947.0"	"nM"	"5.71"	""	""	"UO_0000065"	"14.37"	"0.27"	"5.10"	"5.15"	"False"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4247801"	""	"0"	"397.49"	"0"	"0.61"	"10e"	"CN(C)CC(=O)N1CCC(Cn2nc(-c3cnn(C)c3)c3c(N)ncnc32)CC1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4249492"	""	"0"	"396.46"	"0"	"1.27"	"12b"	"C=CC(=O)N1CCCC(n2nc(-c3cnn(CCOC)c3)c3c(N)ncnc32)C1"	"IC50"	"'='"	"590.0"	"nM"	"6.23"	""	""	"UO_0000065"	"15.71"	"0.29"	"4.96"	"5.32"	"False"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4452410"	""	"0"	"440.51"	"0"	"4.55"	"6"	"Cc1ccc(C(=O)Nc2cccc3c(-c4nc(NC(=O)C5CC5)ncc4C)c[nH]c23)c(C)n1"	"IC50"	"'='"	"2500.0"	"nM"	"5.60"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4406243"	"Inhibition of recombinant human N-terminal GST-tagged JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-labeled GEEPLYWSFPAKKK-NH2 peptide as substrate after 10 mins in presence of 5 mM ATP by caliper mobility shift assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402602"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL3699529"	""	"0"	"449.48"	"0"	"4.18"	"BDBM147547"	"CC(C)(c1ccc(Nc2nn([C@@H]3CCCC[C@H]3C#N)cc2C(N)=O)cc1)[C@H](O)C(F)(F)F"	"IC50"	"'='"	"30.0"	"nM"	"7.52"	""	"285477"	"UO_0000065"	"16.74"	"0.32"	"3.34"	"6.43"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647810"	""	"0"	"430.94"	"0"	"3.24"	"BDBM147913"	"COCC(C)N[C@H]1CCC(n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"38.0"	"nM"	"7.42"	""	"285848"	"UO_0000065"	"17.22"	"0.34"	"4.18"	"6.29"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652338"	""	"0"	"483.66"	"0"	"2.04"	"BDBM113149"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCC[C@H](CS(C)(=O)=O)C2)CC1"	"IC50"	"'='"	"92.2"	"nM"	"7.04"	""	"234592"	"UO_0000065"	"14.55"	"0.30"	"5.00"	"6.05"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3665190"	""	"0"	"407.89"	"0"	"1.90"	"BDBM112585"	"CS(=O)(=O)N1CCC[C@H](Nc2nc(Cl)ncc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.1314"	"nM"	"9.88"	""	"233822"	"UO_0000065"	"24.23"	"0.50"	"7.98"	"8.46"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3330106"	""	"0"	"355.83"	"0"	"3.38"	"8"	"Cc1ccc(Cl)cc1-c1[nH]c(-c2ccnc(N)n2)cc1C(=O)N(C)C"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL3374497"	"Inhibition of JAK2 V617F mutant in human SET2 cells"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3703027"	""	"0"	"476.50"	"0"	"3.43"	"BDBM147737"	"C[C@@](O)(c1ccc(Nc2nn([C@H]3CC[C@H](N4CCC4)C[C@@H]3C#N)cc2C(N)=O)cc1)C(F)(F)F"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"285671"	"UO_0000065"	"17.42"	"0.33"	"4.87"	"6.91"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652389"	""	"0"	"497.67"	"0"	"3.12"	"BDBM113201"	"Cc1ccc(N2CCN(S(=O)(=O)C[C@H]3CC[C@H](N(C)c4ncnc5[nH]ccc45)CC3)CC2)nc1C"	"IC50"	"'='"	"13.7"	"nM"	"7.86"	""	"234644"	"UO_0000065"	"15.80"	"0.31"	"4.74"	"8.00"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3648439"	""	"0"	"424.51"	"0"	"3.45"	"BDBM107148"	"O=C(CN1CCN(c2ccncc2)CC1)Nc1cccc(-c2cnc3ccccc3n2)c1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	"226386"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3655100"	""	"0"	"402.48"	"0"	"0.51"	"BDBM159767"	"Cn1cc2c(n1)CN(S(=O)(=O)N[C@H]1C[C@@H](N(C)c3ncnc4[nH]ccc34)C1)C2"	"IC50"	"'='"	"1080.0"	"nM"	"5.97"	""	"302577"	"UO_0000065"	"14.82"	"0.29"	"5.46"	"5.33"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645095"	""	"0"	"443.56"	"0"	"3.85"	"BDBM99869"	"COc1ccccc1CNc1cccn2nc(Nc3cccc(N4CCN(C)CC4)c3)nc12"	"IC50"	"'='"	"45.95"	"nM"	"7.34"	""	"216537"	"UO_0000065"	"16.54"	"0.30"	"3.49"	"10.49"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3665223"	""	"0"	"415.42"	"0"	"3.74"	"BDBM112623"	"N#CCC(N1CCC[C@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1)C(F)(F)F"	"IC50"	"'='"	"0.2305"	"nM"	"9.64"	""	"233860"	"UO_0000065"	"23.20"	"0.44"	"5.90"	"10.31"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652325"	""	"0"	"449.62"	"0"	"2.77"	"BDBM113135"	"CC[C@H](O)C1CCN(S(=O)(=O)C[C@H]2CC[C@H](N(C)c3ncnc4[nH]ccc34)CC2)CC1"	"IC50"	"'='"	"90.6"	"nM"	"7.04"	""	"234578"	"UO_0000065"	"15.66"	"0.31"	"4.27"	"6.88"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL2414545"	""	"0"	"462.58"	"0"	"3.30"	"BDBM99583"	"CN1CCN(c2ccc(Nc3nc4cccc(-c5cccc(S(C)(=O)=O)c5)n4n3)cc2)CC1"	"IC50"	"'='"	"9.2"	"nM"	"8.04"	""	"216273"	"UO_0000065"	"17.37"	"0.33"	"4.74"	"9.70"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3645047"	""	"0"	"519.05"	"2"	"5.07"	"BDBM99814"	"COc1cc(Cl)ccc1-c1cccn2nc(Nc3ccc(C4CCN(CC(=O)N(C)C)CC4)cc3)nc12"	"IC50"	"'='"	"37.11"	"nM"	"7.43"	""	"216487"	"UO_0000065"	"14.32"	"0.27"	"2.36"	"9.91"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3659504"	""	"0"	"337.36"	"0"	"3.16"	"BDBM98020"	"Cc1cc(-n2cnc3ccc(N[C@@H](C)c4ccc(F)cn4)nc32)n[nH]1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"213961"	"UO_0000065"	"25.26"	"0.47"	"5.36"	"10.11"	"False"	"CHEMBL3705269"	"Amplified Luminescent Proximity Assay: To measure JAK2 kinase activity, a commercially available purified enzyme may be used. The enzyme may be a C-terminal His6-tagged, recombinant, human JAK2, amino acids 808-end, (Genbank Accession number NM 004972) expressed by baculovirus in Sf21 cells (Upstate Biotechnology MA). After incubation of the kinase with a biotinylated substrate and adenosine triphosphate (ATP) for 60 minutes at room temperature, the kinase reaction may be stopped by the addition of 30 mM ethylenediaminetetraacetic acid (EDTA). The reaction may be performed in 384 well microtitre plates and the reaction products may be detected with the addition of streptavidin coated Donor Beads and phosphotyrosine-specific antibodies coated Acceptor Beads using the EnVision Multilabel Plate Reader after an overnight incubation at room temperature."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638534"	"37"	"BindingDB Database"	""	"2013"	"CHEMBL4106362"	""
"CHEMBL3702900"	""	"0"	"353.36"	"0"	"2.39"	"BDBM147599"	"N#Cc1ncc(Nc2nn([C@H]3CCCC[C@@H]3C#N)cc2C(N)=O)cc1F"	"IC50"	"'='"	"40.0"	"nM"	"7.40"	""	"285529"	"UO_0000065"	"20.94"	"0.39"	"5.01"	"5.55"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3335697"	""	"0"	"458.55"	"0"	"0.82"	"BDBM112605"	"CS(=O)(=O)N1CCC[C@H](Nc2nc(N3CC[C@@H](O)C3)ncc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.1804"	"nM"	"9.74"	""	"233842"	"UO_0000065"	"21.25"	"0.42"	"8.92"	"6.95"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3916507"	""	"0"	"421.57"	"0"	"1.99"	"BDBM113084"	"CN(c1ncnc2[nH]ccc12)C1CCC(CS(=O)(=O)N2CCC(CO)CC2)CC1"	"IC50"	"'='"	"43.8"	"nM"	"7.36"	""	"234528"	"UO_0000065"	"17.46"	"0.35"	"5.37"	"7.18"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3699521"	""	"0"	"446.43"	"0"	"3.50"	"BDBM147539"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc3c(c2)CN(CC(F)(F)F)C3=O)n1"	"IC50"	"'='"	"0.79"	"nM"	"9.10"	""	"285469"	"UO_0000065"	"20.39"	"0.39"	"5.60"	"7.78"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL1650733"	""	"0"	"417.42"	"0"	"2.33"	"16b"	"Cc1cc(Nc2nc(N[C@@H](C)c3ncc(F)cn3)nc(N3CCOCC3)c2F)n[nH]1"	"IC50"	"'<'"	"3.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1656588"	"Inhibition of JAK2 using Km ATP concentration"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1650727"	""	"0"	"349.76"	"0"	"2.97"	"9h"	"Cc1cc(Nc2nc(O[C@H](C)c3ncc(F)cn3)ncc2Cl)n[nH]1"	"IC50"	"'='"	"1300.0"	"nM"	"5.89"	""	""	"UO_0000065"	"16.83"	"0.33"	"2.92"	"5.80"	"False"	"CHEMBL1656589"	"Inhibition of JAK2 using 5 mM of ATP"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL3702918"	""	"0"	"563.68"	"1"	"3.50"	"BDBM147617"	"COc1cccc(N2CCN(S(=O)(=O)c3ccc(Nc4nn([C@H]5CCCC[C@@H]5C#N)cc4C(N)=O)cc3)CC2)c1"	"IC50"	"'='"	"24.0"	"nM"	"7.62"	""	"285547"	"UO_0000065"	"13.52"	"0.26"	"4.12"	"5.20"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL1650737"	""	"0"	"449.88"	"0"	"2.54"	"16f"	"COc1cc(Nc2nc(N[C@@H](C)c3ncc(F)cn3)nc(N3CCOCC3)c2Cl)n[nH]1"	"IC50"	"'='"	"90.0"	"nM"	"7.05"	""	""	"UO_0000065"	"15.66"	"0.31"	"4.51"	"5.59"	"False"	"CHEMBL1656589"	"Inhibition of JAK2 using 5 mM of ATP"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL3645028"	""	"0"	"425.54"	"0"	"4.62"	"BDBM99785"	"c1ccc(-c2cccn3nc(Nc4ccc5c(c4)CCNCC5)nc23)c(OCC2CC2)c1"	"IC50"	"'='"	"111.81"	"nM"	"6.95"	""	"216468"	"UO_0000065"	"16.34"	"0.30"	"2.33"	"10.95"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642250"	""	"0"	"509.61"	"2"	"5.36"	"BDBM2013"	"Cn1ncc2c(-c3cccn4nc(Nc5ccc6c(c5)CCN(C(=O)OC(C)(C)C)CC6)nc34)cccc21"	"IC50"	"'='"	"16.54"	"nM"	"7.78"	""	"2880"	"UO_0000065"	"15.27"	"0.28"	"2.42"	"8.69"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642384"	""	"0"	"506.66"	"1"	"3.89"	"BDBM99662"	"CN1CCN(c2ccc(Nc3nc4c(NCC5CCN(C(=O)OC(C)(C)C)C5)cccn4n3)cc2)CC1"	"IC50"	"'='"	"98.01"	"nM"	"7.01"	""	"216352"	"UO_0000065"	"13.83"	"0.26"	"3.12"	"7.76"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3645118"	""	"0"	"509.57"	"1"	"3.87"	"BDBM99892"	"CCN1CCP(=O)(c2ccc(Nc3nc4c(-c5ccc(S(C)(=O)=O)cc5)cccn4n3)cc2)CC1"	"IC50"	"'='"	"1.62"	"nM"	"8.79"	""	"216560"	"UO_0000065"	"17.25"	"0.34"	"4.92"	"9.09"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3622130"	""	"0"	"352.44"	"0"	"2.75"	"8"	"CCn1c(C(=O)N(C2CC2)C2CC2)cc2c3c(ncn3C)c(NC)nc21"	"IC50"	"'='"	"4.2"	"nM"	"8.38"	""	""	"UO_0000065"	"23.77"	"0.44"	"5.63"	"12.32"	"False"	"CHEMBL3625473"	"Inhibition of JAK2 (unknown origin) using 5-FAMKKKKEEIYFFFG-OH as substrate after 60 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621098"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3622128"	""	"0"	"382.47"	"0"	"2.11"	"6"	"CNc1nc2c(cc(C(=O)N(C3CC3)C3CC3)n2CCCO)c2c1ncn2C"	"IC50"	"'='"	"390.0"	"nM"	"6.41"	""	""	"UO_0000065"	"16.76"	"0.31"	"4.30"	"7.27"	"False"	"CHEMBL3625474"	"Inhibition of JAK2 in human SET2 cells assessed as inhibition of cell proliferation after 72 hrs by [3H]-thymidine incorporation assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621098"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3644955"	""	"0"	"565.77"	"1"	"4.11"	"BDBM99704"	"CN1CCN(c2cccc(Nc3nc4c(-c5ccc(N6CCC(N7CCN(C)CC7)CC6)cc5)cccn4n3)c2)CC1"	"IC50"	"'='"	"45.02"	"nM"	"7.35"	""	"216394"	"UO_0000065"	"12.99"	"0.24"	"3.24"	"12.58"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652327"	""	"0"	"448.59"	"0"	"1.87"	"BDBM113137"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCC(CC(N)=O)CC2)CC1"	"IC50"	"'='"	"84.8"	"nM"	"7.07"	""	"234580"	"UO_0000065"	"15.76"	"0.31"	"5.20"	"5.64"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3702959"	""	"0"	"398.44"	"0"	"3.07"	"BDBM147666"	"[C-]#[N+][C@@H]1C[C@H](OCC2CC2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccnc(F)c2)n1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"285598"	"UO_0000065"	"20.19"	"0.38"	"4.98"	"8.09"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647931"	""	"0"	"409.49"	"0"	"3.55"	"BDBM148051"	"CC(C)(C)OC(=O)C1CC[C@@H](C#N)C(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'>'"	"1500.0"	"nM"	""	""	"285444"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4641076"	""	"0"	"217.27"	"0"	"1.90"	"9"	"Cc1[nH]nc2[nH]c(=O)cc(CC3CCC3)c12"	"IC50"	"'='"	"570.0"	"nM"	"6.24"	""	""	"UO_0000065"	"28.74"	"0.53"	"4.34"	"10.15"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4632897"	""	"0"	"342.44"	"0"	"2.89"	"26"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](NC(=O)C4CCCC4)CC3)c12"	"IC50"	"'='"	"1600.0"	"nM"	"5.80"	""	""	"UO_0000065"	"16.93"	"0.32"	"2.91"	"6.39"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL3642325"	""	"0"	"367.41"	"0"	"2.00"	"BDBM99597"	"CN1CCN(c2nc3c(NCc4cccc([N+](=O)[O-])c4)cccn3n2)CC1"	"IC50"	"'='"	"9999.0"	"nM"	"5.00"	""	"216287"	"UO_0000065"	"13.61"	"0.25"	"3.00"	"5.44"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3699512"	""	"0"	"378.44"	"0"	"2.87"	"BDBM147530"	"N#C[C@H]1CCCCC1n1cc(C(N)=O)c(Nc2ccc3c(c2)CCC(=O)N3)n1"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	"285460"	"UO_0000065"	"21.40"	"0.39"	"5.23"	"6.43"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652304"	""	"0"	"407.54"	"0"	"1.60"	"BDBM113113"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC[C@H](CO)C2)CC1"	"IC50"	"'='"	"14.4"	"nM"	"7.84"	""	"234557"	"UO_0000065"	"19.24"	"0.38"	"6.24"	"7.66"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3645067"	""	"0"	"529.64"	"2"	"6.27"	"BDBM99835"	"COc1cccc(-c2cccn3nc(Nc4ccc(C5CCN(C(=O)OC(C)(C)C)CC5)cc4)nc23)c1OC"	"IC50"	"'='"	"326.43"	"nM"	"6.49"	""	"216508"	"UO_0000065"	"12.25"	"0.23"	"0.22"	"7.19"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3650673"	""	"0"	"309.37"	"0"	"2.98"	"BDBM148054"	"N#C[C@H]1CCCCC1n1cc(C(N)=O)c(Nc2ccccc2)n1"	"IC50"	"'='"	"30.0"	"nM"	"7.52"	""	"285568"	"UO_0000065"	"24.32"	"0.45"	"4.54"	"7.78"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703068"	""	"0"	"433.49"	"0"	"3.28"	"BDBM147778"	"N#C[C@H]1C[C@@H](NCc2ccccc2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccnc(F)c2)n1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"285712"	"UO_0000065"	"18.56"	"0.34"	"4.77"	"6.61"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4060528"	""	"0"	"521.60"	"1"	"2.75"	"53"	"COC[C@H](C(=O)Nc1cccc2c(-c3nc(Nc4cn(C)nc4C)ncc3F)c[nH]c12)N1CCN(C)CC1"	"IC50"	"'='"	"322.0"	"nM"	"6.49"	""	""	"UO_0000065"	"12.45"	"0.23"	"3.74"	"5.59"	"False"	"CHEMBL4022634"	"Inhibition of N-terminal GST fused recombinant JAK2 (831 to 1132 amino acids) (unknown origin) expressed in insect cells using ATP and peptide substrate (5FAM-GEEPLYWSFPAKKK-NH2"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020810"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2017"	"None"	""
"CHEMBL4078025"	""	"0"	"535.63"	"1"	"3.60"	"10b"	"CCOc1nn(C)cc1Nc1ncc(F)c(-c2c[nH]c3c(NC(=O)[C@H](C)N4CCN(C)C[C@@H]4C)cccc23)n1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022634"	"Inhibition of N-terminal GST fused recombinant JAK2 (831 to 1132 amino acids) (unknown origin) expressed in insect cells using ATP and peptide substrate (5FAM-GEEPLYWSFPAKKK-NH2"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020810"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2017"	"None"	""
"CHEMBL3309990"	""	"0"	"337.31"	"0"	"2.32"	"7o"	"Nc1nc2c3c(F)cccc3nc(Cc3ccc4c(c3)OCO4)n2n1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3381081"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352169"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3335690"	""	"0"	"428.56"	"0"	"3.27"	"20"	"CC(C)(C)CS(=O)(=O)N1CCC[C@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"24.0"	"nM"	"7.62"	""	""	"UO_0000065"	"17.78"	"0.35"	"4.35"	"7.34"	"False"	"CHEMBL3374010"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 1 hr in presence of [gamma-33P]ATP by scintillation counting analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351377"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3343034"	""	"0"	"400.44"	"0"	"4.65"	"5a"	"COc1cc2c(Nc3ccc(NC(=O)c4ccccc4)cc3)nc(C)nc2cc1O"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3380804"	"Inhibition of human JAK2 incubated for 20 mins prior to MgCl2 addition measured after 90 mins by mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351874"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3343047"	""	"0"	"377.40"	"0"	"3.49"	"16b"	"COc1cc(C(=O)Nc2ccc(NC(=O)c3ccccc3)cc2)c(N)cc1O"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3380804"	"Inhibition of human JAK2 incubated for 20 mins prior to MgCl2 addition measured after 90 mins by mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351874"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3343058"	""	"0"	"423.43"	"0"	"2.13"	"37"	"CCNC(=O)Nc1ccc(NC(=O)c2cc(OC)cc(-c3c[nH]c(=O)[nH]c3=O)c2)cc1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3380804"	"Inhibition of human JAK2 incubated for 20 mins prior to MgCl2 addition measured after 90 mins by mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351874"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3335687"	""	"0"	"394.50"	"0"	"1.78"	"14"	"CC(C)CS(=O)(=O)N1C[C@@H](C)C[C@H](NC(=O)Nc2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"56.0"	"nM"	"7.25"	""	""	"UO_0000065"	"18.38"	"0.37"	"5.47"	"6.04"	"False"	"CHEMBL3374010"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 1 hr in presence of [gamma-33P]ATP by scintillation counting analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351377"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3745954"	""	"0"	"389.86"	"0"	"3.84"	"28"	"COc1ccc(F)c(-c2nc3c(NCC4CCNCC4)c(Cl)cnc3[nH]2)c1"	"IC50"	"'='"	"13100.0"	"nM"	"4.88"	""	""	"UO_0000065"	"12.52"	"0.25"	"1.04"	"6.52"	"False"	"CHEMBL3751000"	"Inhibition of N-terminal GST-fused recombinant JAK2 (831 to 1132 residues) (unknown origin) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate by microfluidic capillary electrophoresis method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3745697"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3354186"	""	"0"	"390.45"	"0"	"3.10"	"5"	"COC1CCN(c2nccc(Nc3cc4[nH]c(-c5cn[nH]c5)cc4cn3)n2)CC1"	"IC50"	"'='"	"96.0"	"nM"	"7.02"	""	""	"UO_0000065"	"17.97"	"0.33"	"3.92"	"6.52"	"False"	"CHEMBL3375809"	"Inhibition of Jak2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351701"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL3354188"	""	"0"	"366.47"	"0"	"3.77"	"7"	"COC1CCN(c2nccc(Nc3cc4c(ccn4C(C)C)cn3)n2)CC1"	"IC50"	"'='"	"718.0"	"nM"	"6.14"	""	""	"UO_0000065"	"16.77"	"0.31"	"2.37"	"9.02"	"False"	"CHEMBL3375809"	"Inhibition of Jak2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351701"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL4635464"	""	"0"	"225.25"	"0"	"2.23"	"6"	"Cc1[nH]nc2[nH]c(=O)cc(-c3ccccc3)c12"	"IC50"	"'='"	"4200.0"	"nM"	"5.38"	""	""	"UO_0000065"	"23.87"	"0.43"	"3.15"	"8.74"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4640521"	""	"0"	"245.33"	"0"	"2.85"	"10"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CCCC[C@H]3C)c12"	"IC50"	"'='"	"340.0"	"nM"	"6.47"	""	""	"UO_0000065"	"26.37"	"0.49"	"3.62"	"10.51"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL3797207"	""	"0"	"411.43"	"0"	"3.47"	"17m"	"CNc1nc(Nc2cnn(C(CC(N)=O)C3CCCCC3)c2)ncc1C(F)(F)F"	"IC50"	"'='"	"98.0"	"nM"	"7.01"	""	""	"UO_0000065"	"17.04"	"0.33"	"3.54"	"6.33"	"False"	"CHEMBL3804597"	"Inhibition of human recombinant JAK2 expressed in Sf21 cells assessed as reduction in Ulight-CAGAGAIETDKEYYTVKD phosphorylation pre-incubated before substrate addition and measured after 60 mins by LANCE detection method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797141"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2016"	"CHEMBL4106362"	""
"CHEMBL3330104"	""	"0"	"327.78"	"0"	"2.78"	"6"	"Cc1ccc(Cl)cc1-c1[nH]c(-c2ccnc(N)n2)cc1C(N)=O"	"IC50"	"'='"	"430.0"	"nM"	"6.37"	""	""	"UO_0000065"	"19.42"	"0.38"	"3.59"	"5.75"	"False"	"CHEMBL3374497"	"Inhibition of JAK2 V617F mutant in human SET2 cells"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330107"	""	"0"	"355.83"	"0"	"3.43"	"9"	"CCNC(=O)c1cc(-c2ccnc(N)n2)[nH]c1-c1cc(Cl)ccc1C"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL3374497"	"Inhibition of JAK2 V617F mutant in human SET2 cells"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL218602"	""	"0"	"330.40"	"0"	"3.41"	"12"	"C[C@@H](c1ccccc1)N(C)c1ccnc(-n2cnc3ccncc32)n1"	"IC50"	"'='"	"153.0"	"nM"	"6.82"	""	""	"UO_0000065"	"20.63"	"0.37"	"3.41"	"11.41"	"False"	"CHEMBL908418"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139695"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2006"	"None"	""
"CHEMBL323994"	""	"0"	"287.32"	"0"	"3.57"	"1"	"O=C1Nc2ccc(-c3cccnc3)cc2/C1=C/c1ccc[nH]1"	"IC50"	"'='"	"600.0"	"nM"	"6.22"	""	""	"UO_0000065"	"21.65"	"0.39"	"2.65"	"10.77"	"False"	"CHEMBL908418"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1139695"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2006"	"None"	""
"CHEMBL3895231"	""	"0"	"403.44"	"0"	"4.88"	"5c"	"CCOC(=O)COc1cccc(Nc2ncc(C)c(-c3cc4ccccc4o3)n2)c1"	"IC50"	"'='"	"18.9"	"nM"	"7.72"	""	""	"UO_0000065"	"19.14"	"0.35"	"2.84"	"8.93"	"False"	"CHEMBL3868063"	"Inhibition of GST-tagged recombinant human JAK2 expressed in baculovirus using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3867460"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2017"	"None"	""
"CHEMBL3970092"	""	"0"	"478.50"	"0"	"2.96"	"16g"	"COc1cc(Nc2ncc(F)c(-c3cc4c(o3)CCN(S(C)(=O)=O)C4)n2)cc(OC)c1OC"	"IC50"	"'='"	"9.4"	"nM"	"8.03"	""	""	"UO_0000065"	"16.78"	"0.33"	"5.07"	"6.92"	"False"	"CHEMBL3868063"	"Inhibition of GST-tagged recombinant human JAK2 expressed in baculovirus using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3867460"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2017"	"None"	""
"CHEMBL3359909"	""	"0"	"260.34"	"0"	"2.28"	"3c"	"C[C@H](Nc1c(C(N)=O)cnn2cccc12)C(C)(C)C"	"IC50"	"'='"	"570.0"	"nM"	"6.24"	""	""	"UO_0000065"	"23.98"	"0.45"	"3.96"	"8.62"	"False"	"CHEMBL3377596"	"Inhibition of JAK2 (unknown origin) by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352641"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL1835140"	""	"0"	"402.50"	"0"	"4.06"	"51"	"CC(C)C(Nc1ncc(C(N)=O)c2[nH]c3cc(-c4cnn(C)c4)ccc3c12)C1CC1"	"IC50"	"'='"	"95.0"	"nM"	"7.02"	""	""	"UO_0000065"	"17.45"	"0.32"	"2.96"	"6.91"	"False"	"CHEMBL1840130"	"Inhibition of JAK2-mediated STAT5 phosphorylation in human HEL 92.1.7 irf1-bla cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308090"	""
"CHEMBL1835138"	""	"0"	"374.45"	"0"	"3.43"	"49"	"C[C@@H](Nc1ncc(C(N)=O)c2[nH]c3cc(-c4cnn(C)c4)ccc3c12)C1CC1"	"IC50"	"'='"	"79.0"	"nM"	"7.10"	""	""	"UO_0000065"	"18.97"	"0.35"	"3.67"	"6.99"	"False"	"CHEMBL1840130"	"Inhibition of JAK2-mediated STAT5 phosphorylation in human HEL 92.1.7 irf1-bla cells"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3308090"	""
"CHEMBL3933593"	""	"0"	"666.78"	"2"	"6.38"	"46"	"O=C(CCCCCC(=O)Nc1ccc(NCCOc2ccc3cc2COC/C=C/COCc2cccc(c2)-c2ccnc(n2)N3)cc1)NO"	"IC50"	"'='"	"6.9"	"nM"	"8.16"	""	""	"UO_0000065"	"12.24"	"0.23"	"1.78"	"5.23"	"False"	"CHEMBL3877344"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]ATP addition measured after 120 mins by Hotspot assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3877241"	"1"	"Scientific Literature"	"J Med Chem"	"2016"	"None"	""
"CHEMBL4282877"	""	"0"	"462.55"	"1"	"5.35"	"42i"	"COC(=O)CCCCCCOc1ccc(Nc2nccc(-c3ccc(NC(C)=O)cc3)n2)cc1"	"IC50"	"'='"	"239.0"	"nM"	"6.62"	""	""	"UO_0000065"	"14.32"	"0.27"	"1.27"	"6.46"	"False"	"CHEMBL4268221"	"Inhibition of human JAK2 using poly(Glu:Tyr)(4:1) as substrate preincubated for 20 mins followed by [gamma33P]ATP addition measured after 120 mins by ion exchange filter paper method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4265943"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2018"	"None"	""
"CHEMBL4280540"	""	"0"	"449.51"	"0"	"4.29"	"45e"	"CC(=O)Nc1ccc(-c2ccnc(Nc3cccc(OCCCCCC(=O)NO)c3)n2)cc1"	"IC50"	"'='"	"3.4"	"nM"	"8.47"	""	""	"UO_0000065"	"18.84"	"0.35"	"4.18"	"6.75"	"False"	"CHEMBL4268221"	"Inhibition of human JAK2 using poly(Glu:Tyr)(4:1) as substrate preincubated for 20 mins followed by [gamma33P]ATP addition measured after 120 mins by ion exchange filter paper method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4265943"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2018"	"None"	""
"CHEMBL4294153"	""	"0"	"463.54"	"0"	"4.68"	"45f"	"CC(=O)Nc1ccc(-c2ccnc(Nc3cccc(OCCCCCCC(=O)NO)c3)n2)cc1"	"IC50"	"'='"	"3.6"	"nM"	"8.44"	""	""	"UO_0000065"	"18.22"	"0.34"	"3.76"	"6.73"	"False"	"CHEMBL4268221"	"Inhibition of human JAK2 using poly(Glu:Tyr)(4:1) as substrate preincubated for 20 mins followed by [gamma33P]ATP addition measured after 120 mins by ion exchange filter paper method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4265943"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2018"	"None"	""
"CHEMBL4278951"	""	"0"	"433.51"	"0"	"4.67"	"69a"	"O=C(CCCCCCC(=O)Nc1ccc(-c2ccnc(Nc3ccccc3)n2)cc1)NO"	"IC50"	"'='"	"41.3"	"nM"	"7.38"	""	""	"UO_0000065"	"17.03"	"0.32"	"2.71"	"6.35"	"False"	"CHEMBL4268221"	"Inhibition of human JAK2 using poly(Glu:Tyr)(4:1) as substrate preincubated for 20 mins followed by [gamma33P]ATP addition measured after 120 mins by ion exchange filter paper method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4265943"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2018"	"None"	""
"CHEMBL4286867"	""	"0"	"518.62"	"1"	"4.51"	"69c"	"O=C(CCCCCCC(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1)NO"	"IC50"	"'='"	"3.1"	"nM"	"8.51"	""	""	"UO_0000065"	"16.41"	"0.31"	"4.00"	"6.61"	"False"	"CHEMBL4268221"	"Inhibition of human JAK2 using poly(Glu:Tyr)(4:1) as substrate preincubated for 20 mins followed by [gamma33P]ATP addition measured after 120 mins by ion exchange filter paper method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4265943"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2018"	"None"	""
"CHEMBL4549982"	""	"0"	"452.44"	"0"	"4.32"	"9"	"Nc1nn2cc(N3CCC[C@@H]3c3cc(F)ccc3F)cnc2c1C(=O)Nc1ccc(F)cc1"	"IC50"	"'>'"	"500.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4349458"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain (826 to 1132 end residues) expressed in baculovirus expression system using TK peptide as substrate after 120 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4346723"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2019"	"None"	""
"CHEMBL233969"	""	"0"	"539.64"	"1"	"3.33"	"13"	"C[C@H](Nc1nc(-n2cnc3ccncc32)nc2c1cc(C(=O)NCCCN1CCOCC1)n2C)c1ccccc1"	"IC50"	"'='"	"42.0"	"nM"	"7.38"	""	""	"UO_0000065"	"13.67"	"0.25"	"4.05"	"6.41"	"False"	"CHEMBL897052"	"Inhibition of JAK2 by kinase-Glo luminescent assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1148837"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2007"	"None"	""
"CHEMBL394174"	""	"0"	"490.55"	"0"	"2.56"	"12"	"C[C@H](Nc1nc(-n2cnc3ccncc32)nc2c1cc(C(=O)NS(C)(=O)=O)n2C)c1ccccc1"	"IC50"	"'='"	"55.0"	"nM"	"7.26"	""	""	"UO_0000065"	"14.80"	"0.28"	"4.70"	"5.31"	"False"	"CHEMBL897052"	"Inhibition of JAK2 by kinase-Glo luminescent assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1148837"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2007"	"None"	""
"CHEMBL4113680"	""	"0"	"424.44"	"0"	"2.41"	"BDBM237761"	"C#CCCOC(=O)N1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@H](C#N)C1"	"IC50"	"'='"	"1386.0"	"nM"	"5.86"	""	"414865"	"UO_0000065"	"13.80"	"0.26"	"3.45"	"4.64"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4110416"	""	"0"	"466.42"	"0"	"2.02"	"BDBM237788"	"N#C[C@@H]1CN(C(=O)OCC(F)(F)CO)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"1204.0"	"nM"	"5.92"	""	"414892"	"UO_0000065"	"12.69"	"0.24"	"3.90"	"4.04"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3893379"	""	"0"	"468.41"	"0"	"3.34"	"BDBM237791"	"CC(OC(=O)N1CC[C@@H](C#N)[C@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)C1)C(F)(F)F"	"IC50"	"'='"	"135.0"	"nM"	"6.87"	""	"414895"	"UO_0000065"	"14.67"	"0.28"	"3.53"	"5.44"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4532948"	""	"0"	"434.44"	"0"	"1.90"	"6"	"CNc1cc(Nc2cccn(-c3ccccn3)c2=O)nn2c(C(=O)N[C@@H]3C[C@@H]3F)cnc12"	"IC50"	"'>'"	"12500.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4402479"	"Inhibition of JAK2 (unknown origin) by cell-based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4400582"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2019"	"None"	""
"CHEMBL3939984"	""	"0"	"345.79"	"0"	"2.48"	"BDBM237870"	"N#C[C@@H]1CCOC[C@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"61.0"	"nM"	"7.21"	""	"414972"	"UO_0000065"	"20.86"	"0.41"	"4.73"	"6.81"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3897673"	""	"0"	"409.49"	"0"	"1.52"	"BDBM229258"	"CN(C)CC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)CC1"	"IC50"	"'='"	"318.0"	"nM"	"6.50"	""	"400997"	"UO_0000065"	"15.87"	"0.30"	"4.98"	"5.40"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4109943"	""	"0"	"382.42"	"0"	"1.53"	"BDBM237899"	"CN(C)C(=O)c1ccc(Nc2nn([C@H]3COCC[C@@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"0.2"	"nM"	"9.70"	""	"415001"	"UO_0000065"	"25.36"	"0.47"	"8.17"	"7.68"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3919061"	""	"0"	"461.45"	"0"	"2.54"	"BDBM229306"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(C(=O)C2CC(F)(F)C2)CC1"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	"401045"	"UO_0000065"	"16.96"	"0.32"	"5.28"	"6.02"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4107562"	""	"0"	"427.41"	"0"	"2.24"	"BDBM237858"	"N#C[C@@H]1CS(=O)(=O)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"769.0"	"nM"	"6.11"	""	"415014"	"UO_0000065"	"14.30"	"0.29"	"3.87"	"4.67"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3947800"	""	"0"	"437.48"	"0"	"1.90"	"BDBM229119"	"Cn1ccc(CN2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccnc(F)c4)n3)CC2)n1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"400855"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL2414555"	""	"0"	"379.45"	"0"	"3.25"	"25"	"Cc1cc(Nc2nc3cccc(-c4cccc(S(C)(=O)=O)c4)n3n2)ccn1"	"IC50"	"'='"	"446.0"	"nM"	"6.35"	""	""	"UO_0000065"	"16.74"	"0.32"	"3.10"	"7.12"	"False"	"CHEMBL2415128"	"Inhibition of JAK2 in human SET2 cells assessed as reduction of phosphorylated STAT5 level"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2412966"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL3953929"	""	"0"	"308.39"	"0"	"3.86"	"BDBM197716"	"CCCCCC(CC#N)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"2.2"	"nM"	"8.66"	""	"351113"	"UO_0000065"	"28.07"	"0.51"	"4.80"	"10.41"	"False"	"CHEMBL3887743"	"Kinase Assay: The compounds of the invention were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Biochemistry 1999, 269, 94-104. The catalytic domains of human JAK1 (a.a. 837-1142), JAK2 (a.a. 828-1132) and JAK3 (a.a. 781-1124) with an N-terminal His tag were expressed using baculovirus in insect cells and purified. The catalytic activity of JAK1, JAK2 or JAK3 was assayed by measuring the phosphorylation of a biotinylated peptide. The phosphorylated peptide was detected by homogenous time resolved fluorescence (HTRF). IC50 was measured for each kinase in the 40 uL reactions that contain the enzyme, ATP and 500 nM peptide in 50 mM Tris (pH 7.8) buffer with 100 mM NaCl, 5 mM DTT, and 0.1 mg/mL (0.01%) BSA. The ATP concentration in the reactions was 90 uM for Jak1, 30 uM for Jak2 and 3 uM for Jak3. Reactions were carried out at room temperature for 1 hr and then stopped with 20 uL 45 mM EDTA."	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886433"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3958797"	""	"0"	"333.40"	"0"	"2.38"	"BDBM198220"	"c1cncc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)c1"	"IC50"	"'='"	"40.0"	"nM"	"7.40"	""	"352302"	"UO_0000065"	"22.19"	"0.40"	"5.02"	"9.86"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3896798"	""	"0"	"351.41"	"0"	"2.59"	"BDBM198228"	"Cc1noc(C)c1CN1CCC(c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"180.0"	"nM"	"6.75"	""	"352310"	"UO_0000065"	"19.19"	"0.35"	"4.15"	"7.65"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3920671"	""	"0"	"451.48"	"0"	"3.30"	"BDBM229135"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(Cc2cccc(F)n2)CC1"	"IC50"	"'='"	"95.0"	"nM"	"7.02"	""	"400871"	"UO_0000065"	"15.55"	"0.29"	"3.72"	"6.22"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3917035"	""	"0"	"420.45"	"0"	"2.24"	"BDBM237814"	"N#C[C@@H]1CCN(Cc2cccnn2)C[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"77.0"	"nM"	"7.11"	""	"414918"	"UO_0000065"	"16.92"	"0.31"	"4.87"	"5.66"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3985566"	""	"0"	"456.48"	"0"	"2.23"	"BDBM229186"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(C(=O)OCC2(O)CC2)CC1"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	"400923"	"UO_0000065"	"16.87"	"0.32"	"5.47"	"5.26"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4112766"	""	"0"	"425.49"	"0"	"2.91"	"BDBM237840"	"N#C[C@@H]1CN(Cc2cscn2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"37.0"	"nM"	"7.43"	""	"414944"	"UO_0000065"	"17.47"	"0.34"	"4.52"	"6.58"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3917134"	""	"0"	"423.45"	"0"	"2.75"	"BDBM237855"	"Cc1ncoc1CN1CC[C@@H](C#N)[C@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)C1"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	"414959"	"UO_0000065"	"19.12"	"0.36"	"5.35"	"6.43"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3894596"	""	"0"	"377.40"	"0"	"1.36"	"BDBM237856"	"N#C[C@H]1CS(=O)(=O)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"112.0"	"nM"	"6.95"	""	"414960"	"UO_0000065"	"18.42"	"0.37"	"5.59"	"5.31"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3976529"	""	"0"	"484.56"	"0"	"3.73"	"BDBM229207"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)OC2Cc3ccccc3C2)CC1"	"IC50"	"'='"	"83.0"	"nM"	"7.08"	""	"400944"	"UO_0000065"	"14.61"	"0.27"	"3.35"	"5.61"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4113945"	""	"0"	"380.33"	"0"	"2.24"	"BDBM237879"	"N#C[C@H]1CCOC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)nc2)n1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"414981"	"UO_0000065"	"22.08"	"0.42"	"6.16"	"7.07"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3927391"	""	"0"	"380.33"	"0"	"2.24"	"BDBM237880"	"N#C[C@@H]1CCOC[C@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)nc2)n1"	"IC50"	"'='"	"157.0"	"nM"	"6.80"	""	"414982"	"UO_0000065"	"17.89"	"0.34"	"4.56"	"5.72"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4061128"	""	"0"	"336.36"	"0"	"1.70"	"BDBM237900"	"N#Cc1ccc(Nc2nn([C@H]3COCC[C@@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"0.7"	"nM"	"9.15"	""	"415002"	"UO_0000065"	"27.22"	"0.50"	"7.45"	"7.06"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3895755"	""	"0"	"330.32"	"0"	"1.36"	"BDBM237916"	"N#C[C@H]1COCC[C@@H]1n1cc(C(N)=O)c(Nc2ccnc(F)c2)n1"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	"415009"	"UO_0000065"	"23.78"	"0.45"	"6.49"	"6.61"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL553"	"ERLOTINIB"	"4"	"393.44"	"0"	"3.41"	"erlotinib"	"C#Cc1cccc(Nc2ncnc3cc(OCCOC)c(OCCOC)cc23)c1"	"IC50"	"'>'"	"20000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1007371"	"Inhibition of human JAK2 expressed in COS7 cells"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"COS-7"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1156429"	"1"	"Scientific Literature"	"J. Biol. Chem."	"2007"	"CHEMBL3307648"	""
"CHEMBL4582632"	""	"0"	"351.21"	"0"	"1.52"	"10e"	"C=CC(=O)N1CCCC(n2nc(Br)c3c(N)ncnc32)C1"	"IC50"	"'='"	"94.3"	"nM"	"7.03"	""	""	"UO_0000065"	"20.00"	"0.46"	"5.51"	"7.81"	"False"	"CHEMBL4402146"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-biotin as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4400567"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4442811"	""	"0"	"374.41"	"0"	"2.48"	"8a"	"C=CC(=O)Nc1cccc(Cn2ncc3c(Nc4cnn(C)c4)ncnc32)c1"	"IC50"	"'='"	"870.4"	"nM"	"6.06"	""	""	"UO_0000065"	"16.19"	"0.30"	"3.58"	"5.91"	"False"	"CHEMBL4402146"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-biotin as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4400567"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4535413"	""	"0"	"461.56"	"0"	"2.63"	"30"	"CCc1cc(O)c(F)cc1-c1cc(NS(=O)(=O)CCN2CCN(C)CC2)c2cn[nH]c2c1"	"IC50"	"'='"	"199.53"	"nM"	"6.70"	""	""	"UO_0000065"	"14.52"	"0.29"	"4.07"	"6.60"	"False"	"CHEMBL4478762"	"Inhibition of human His-tagged JAK2 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4477220"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2016"	"None"	""
"CHEMBL4569613"	""	"0"	"393.44"	"0"	"3.03"	"27"	"CCc1cc(O)c(F)cc1-c1cc(NS(=O)(=O)CCOC)c2cn[nH]c2c1"	"IC50"	"'='"	"15.85"	"nM"	"7.80"	""	""	"UO_0000065"	"19.83"	"0.39"	"4.77"	"7.48"	"False"	"CHEMBL4478762"	"Inhibition of human His-tagged JAK2 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4477220"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2016"	"None"	""
"CHEMBL4539949"	""	"0"	"349.39"	"0"	"3.01"	"18"	"CCc1cc(O)c(F)cc1-c1cc(NS(C)(=O)=O)c2cn[nH]c2c1"	"IC50"	"'='"	"7.943"	"nM"	"8.10"	""	""	"UO_0000065"	"23.18"	"0.46"	"5.09"	"8.52"	"False"	"CHEMBL4478762"	"Inhibition of human His-tagged JAK2 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4477220"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2016"	"None"	""
"CHEMBL4551312"	""	"0"	"331.40"	"0"	"3.01"	"13"	"CCS(=O)(=O)Nc1cc(-c2ccc(O)c(C)c2)cc2[nH]ncc12"	"IC50"	"'='"	"125.89"	"nM"	"6.90"	""	""	"UO_0000065"	"20.82"	"0.41"	"3.89"	"7.26"	"False"	"CHEMBL4478762"	"Inhibition of human His-tagged JAK2 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4477220"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2016"	"None"	""
"CHEMBL4557416"	""	"0"	"396.46"	"0"	"1.00"	"11f"	"C=CC(=O)N1CCC(n2nc(-c3cc(C(C)(C)O)n(C)n3)c3c(N)ncnc32)C1"	"IC50"	"'='"	"7.2"	"nM"	"8.14"	""	""	"UO_0000065"	"20.54"	"0.38"	"7.14"	"6.36"	"False"	"CHEMBL4402146"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-biotin as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4400567"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4247874"	""	"0"	"328.39"	"0"	"2.99"	"17c"	"NC(=O)c1cnc2[nH]ccc2c1NC1C2CC3CC1CC(F)(C3)C2"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4236469"	"Inhibition of recombinant human N-terminal His-tagged JAK2 catalytic domain (826 to 1132 residues) expressed in baculovirus expression system using Biotin-Lyn-Substrate2 after 1 hr by ELISA"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229549"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4242999"	""	"0"	"407.31"	"0"	"2.01"	"18, trans-isomer"	"Br.NC(=O)c1cnc2[nH]ccc2c1NC1C2CC3CC1CC(O)(C3)C2"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4236469"	"Inhibition of recombinant human N-terminal His-tagged JAK2 catalytic domain (826 to 1132 residues) expressed in baculovirus expression system using Biotin-Lyn-Substrate2 after 1 hr by ELISA"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229549"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"Tofacitinib"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	""	"UO_0000065"	"26.57"	"0.49"	"6.76"	"9.34"	"True"	"CHEMBL4404825"	"Inhibition of JAK2-JH1/JH2 domain (532 to 1132 residues) (unknown origin) pre-incubated before NH2-KGGEEEEYFELVKK-CO2 substrate addition and measured after 90 mins by MS analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402578"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL3914600"	""	"0"	"502.60"	"1"	"2.77"	"BDBM228949"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(S(C)(=O)=O)cc3)n2)CC1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"400696"	"UO_0000065"	"17.91"	"0.35"	"6.23"	"5.61"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3942861"	""	"0"	"456.52"	"0"	"3.82"	"BDBM237721"	"CC(C)(C)CCOC(=O)N1CC[C@@H](C#N)[C@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)C1"	"IC50"	"'='"	"117.0"	"nM"	"6.93"	""	"414825"	"UO_0000065"	"15.18"	"0.29"	"3.11"	"5.49"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4106535"	""	"0"	"468.41"	"0"	"3.34"	"BDBM237722"	"CC(OC(=O)N1CC[C@@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@H](C#N)C1)C(F)(F)F"	"IC50"	"'='"	"387.0"	"nM"	"6.41"	""	"414826"	"UO_0000065"	"13.69"	"0.27"	"3.07"	"5.08"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4106649"	""	"0"	"418.40"	"0"	"2.36"	"BDBM237723"	"N#C[C@@H]1CN(C(=O)OCCF)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"104.0"	"nM"	"6.98"	""	"414827"	"UO_0000065"	"16.69"	"0.32"	"4.62"	"5.53"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4113865"	""	"0"	"485.52"	"0"	"1.72"	"BDBM237725"	"N#C[C@@H]1CN(C(=O)OCCN2CCOCC2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"835.0"	"nM"	"6.08"	""	"414829"	"UO_0000065"	"12.52"	"0.24"	"4.36"	"4.38"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4110166"	""	"0"	"453.48"	"0"	"2.94"	"BDBM237727"	"CC(C)(C#N)COC(=O)N1CC[C@@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@H](C#N)C1"	"IC50"	"'='"	"411.0"	"nM"	"6.39"	""	"414831"	"UO_0000065"	"14.08"	"0.26"	"3.45"	"4.26"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4113758"	""	"0"	"428.47"	"0"	"3.04"	"BDBM237731"	"CC(C)COC(=O)N1CC[C@@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@H](C#N)C1"	"IC50"	"'='"	"755.0"	"nM"	"6.12"	""	"414835"	"UO_0000065"	"14.29"	"0.27"	"3.08"	"4.85"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4277193"	""	"0"	"460.52"	"0"	"3.17"	"33"	"COc1ccc(S(=O)(=O)N[C@@H]2C[C@H](NC#N)c3cc(-c4ncnc5[nH]ccc45)ccc32)cc1"	"IC50"	"'='"	"2554.0"	"nM"	"5.59"	""	""	"UO_0000065"	"12.14"	"0.23"	"2.42"	"4.21"	"False"	"CHEMBL4265556"	"Inhibition of recombinant human GST-tagged JAK2 using KAIETDKEYYTVKD-NH2 as substrate in presence of 1 mM ATP concentration by coupled PK/LDH assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4261650"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL1789941"	"RUXOLITINIB"	"4"	"306.37"	"0"	"3.47"	"1"	"N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4406243"	"Inhibition of recombinant human N-terminal GST-tagged JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-labeled GEEPLYWSFPAKKK-NH2 peptide as substrate after 10 mins in presence of 5 mM ATP by caliper mobility shift assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402602"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4577523"	"AZD4205"	"2"	"489.58"	"0"	"2.69"	"21; AZD4205"	"COc1nn(C)cc1Nc1nccc(-c2c[nH]c3c(NC(=O)[C@@H](C)N4CCN(C)CC4)cccc23)n1"	"IC50"	"'>'"	"15000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4406243"	"Inhibition of recombinant human N-terminal GST-tagged JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-labeled GEEPLYWSFPAKKK-NH2 peptide as substrate after 10 mins in presence of 5 mM ATP by caliper mobility shift assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402602"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL3934627"	""	"0"	"354.46"	"0"	"2.65"	"BDBM198313"	"c1cc2c(ncn3nnc([C@H]4CC[C@H](CNC[C@@H]5CCCO5)CC4)c23)[nH]1"	"IC50"	"'='"	"200.0"	"nM"	"6.70"	""	"352391"	"UO_0000065"	"18.90"	"0.35"	"4.05"	"8.36"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3934664"	""	"0"	"363.43"	"0"	"2.39"	"BDBM198369"	"COc1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cn1"	"IC50"	"'='"	"110.0"	"nM"	"6.96"	""	"352447"	"UO_0000065"	"19.15"	"0.35"	"4.57"	"8.26"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3921365"	""	"0"	"367.50"	"0"	"2.52"	"BDBM198380"	"CN(C)[C@H]1CCN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C1"	"IC50"	"'='"	"130.0"	"nM"	"6.89"	""	"352458"	"UO_0000065"	"18.74"	"0.35"	"4.37"	"10.54"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3894535"	""	"0"	"450.57"	"0"	"3.35"	"BDBM198388"	"CS(=O)(=O)c1ccc2c(c1)CCN2C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"38.0"	"nM"	"7.42"	""	"352466"	"UO_0000065"	"16.47"	"0.32"	"4.07"	"7.71"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3919034"	""	"0"	"479.61"	"0"	"3.19"	"BDBM198389"	"CN(C)S(=O)(=O)c1ccc2c(c1)CCN2C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"98.0"	"nM"	"7.01"	""	"352467"	"UO_0000065"	"14.61"	"0.28"	"3.82"	"7.04"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3942424"	""	"0"	"364.43"	"0"	"3.56"	"BDBM198395"	"Fc1ccc(CN[C@H]2CC[C@@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"550.0"	"nM"	"6.26"	""	"352473"	"UO_0000065"	"17.18"	"0.32"	"2.70"	"8.83"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3938956"	""	"0"	"392.44"	"0"	"3.33"	"BDBM198410"	"O=C(NCc1ccc(F)cc1)[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"55.0"	"nM"	"7.26"	""	"352488"	"UO_0000065"	"18.50"	"0.34"	"3.93"	"8.25"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3960910"	""	"0"	"356.43"	"0"	"3.46"	"BDBM198413"	"N#Cc1ccc(CN2CCC(c3ncn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"19.0"	"nM"	"7.72"	""	"352491"	"UO_0000065"	"21.66"	"0.39"	"4.26"	"10.58"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3426225"	""	"0"	"576.63"	"1"	"4.16"	"1j"	"CCn1nc(C#Cc2cc(C(=O)Nc3ccc(CN4CCN(C)CC4)c(C(F)(F)F)c3)ccc2C)c2c(N)ncnc21"	"IC50"	"'='"	"2911.0"	"nM"	"5.54"	""	""	"UO_0000065"	"9.60"	"0.18"	"1.38"	"5.26"	"False"	"CHEMBL3429886"	"Inhibition of human JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3425429"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL1835014"	""	"0"	"272.28"	"0"	"2.39"	"3"	"CCNc1ncc(C(N)=O)c2[nH]c3ccc(F)cc3c12"	"IC50"	"'>'"	"15000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1840119"	"Competitive inhibition of JAK2 in the presence of 2 mM ATP"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1835014"	""	"0"	"272.28"	"0"	"2.39"	"3"	"CCNc1ncc(C(N)=O)c2[nH]c3ccc(F)cc3c12"	"IC50"	"'='"	"230.0"	"nM"	"6.64"	""	""	"UO_0000065"	"24.38"	"0.45"	"4.25"	"7.92"	"False"	"CHEMBL1840118"	"Competitive inhibition of JAK2 in the presence of 15 uM ATP"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1833803"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL4281393"	""	"0"	"275.31"	"0"	"2.68"	"12"	"N#CN[C@H]1CCc2ccc(-c3ncnc4[nH]ccc34)cc21"	"IC50"	"'='"	"1666.0"	"nM"	"5.78"	""	""	"UO_0000065"	"20.99"	"0.38"	"3.10"	"7.47"	"False"	"CHEMBL4265556"	"Inhibition of recombinant human GST-tagged JAK2 using KAIETDKEYYTVKD-NH2 as substrate in presence of 1 mM ATP concentration by coupled PK/LDH assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4261650"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4284799"	""	"0"	"333.40"	"0"	"2.87"	"14"	"COCCc1c[nH]c2ncnc(-c3ccc4c(c3)C(NC#N)CC4)c12"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4265556"	"Inhibition of recombinant human GST-tagged JAK2 using KAIETDKEYYTVKD-NH2 as substrate in presence of 1 mM ATP concentration by coupled PK/LDH assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4261650"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4279720"	""	"0"	"289.34"	"0"	"2.86"	"23"	"C[C@]1(NC#N)CCc2ccc(-c3ncnc4[nH]ccc34)cc21"	"IC50"	"'='"	"71.0"	"nM"	"7.15"	""	""	"UO_0000065"	"24.71"	"0.44"	"4.29"	"9.24"	"False"	"CHEMBL4265556"	"Inhibition of recombinant human GST-tagged JAK2 using KAIETDKEYYTVKD-NH2 as substrate in presence of 1 mM ATP concentration by coupled PK/LDH assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4261650"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4588587"	""	"0"	"461.57"	"0"	"2.86"	"9"	"Cc1cnc(NC(=O)C2CC2)nc1-c1c[nH]c2c(NC(=O)[C@@H](C)N3CCN(C)CC3)cccc12"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4406243"	"Inhibition of recombinant human N-terminal GST-tagged JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-labeled GEEPLYWSFPAKKK-NH2 peptide as substrate after 10 mins in presence of 5 mM ATP by caliper mobility shift assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402602"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4588128"	""	"0"	"475.60"	"0"	"3.25"	"12"	"Cc1cnc(NC(=O)C2CC2)nc1-c1c[nH]c2c(NC(=O)C(C)(C)N3CCN(C)CC3)cccc12"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4406243"	"Inhibition of recombinant human N-terminal GST-tagged JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-labeled GEEPLYWSFPAKKK-NH2 peptide as substrate after 10 mins in presence of 5 mM ATP by caliper mobility shift assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402602"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4577393"	""	"0"	"568.48"	"1"	"3.45"	"20"	"COc1nn(C)cc1Nc1ncc(Br)c(-c2c[nH]c3c(NC(=O)[C@@H](C)N4CCN(C)CC4)cccc23)n1"	"IC50"	"'='"	"1570.0"	"nM"	"5.80"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4406243"	"Inhibition of recombinant human N-terminal GST-tagged JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-labeled GEEPLYWSFPAKKK-NH2 peptide as substrate after 10 mins in presence of 5 mM ATP by caliper mobility shift assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402602"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL3655095"	""	"0"	"335.43"	"0"	"1.25"	"BDBM159762"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)CC2CC2)C1"	"IC50"	"'='"	"1200.0"	"nM"	"5.92"	""	"302572"	"UO_0000065"	"17.65"	"0.35"	"4.67"	"6.51"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642253"	""	"0"	"401.47"	"0"	"3.99"	"BDBM99511"	"COc1ccccc1-c1cccn2nc(Nc3ccc(N4CCOCC4)cc3)nc12"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	"216202"	"UO_0000065"	"19.18"	"0.35"	"3.71"	"12.04"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL2062813"	""	"0"	"460.52"	"0"	"4.14"	"39"	"CN1CCN(c2cccc(Nc3nc4c(-c5ccc(P(C)(C)=O)cc5)cccn4n3)c2)CC1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"18.51"	"0.35"	"4.38"	"12.96"	"False"	"CHEMBL2067611"	"Inhibition of human JAK2 expressed in baculovirus using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate preincubated for 1 hr measured after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2062813"	""	"0"	"460.52"	"0"	"4.14"	"39"	"CN1CCN(c2cccc(Nc3nc4c(-c5ccc(P(C)(C)=O)cc5)cccn4n3)c2)CC1"	"IC50"	"'='"	"318.0"	"nM"	"6.50"	""	""	"UO_0000065"	"14.11"	"0.27"	"2.36"	"9.88"	"False"	"CHEMBL2067179"	"Inhibition of JAK2 in human TF-1 cells using GM-CSF pretreated for 1 hr prior to GM-CSF addition measured after 5 hrs by FRET based GeneBLAzer assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"CHEMBL3307972"	""
"CHEMBL3651011"	""	"0"	"381.39"	"0"	"2.72"	"BDBM153187"	"C=C(C)C(=O)Nc1cc(-c2ncnc3[nH]cc(C(=O)OCC)c23)cnc1OC"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294135"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647891"	""	"0"	"476.92"	"0"	"3.77"	"BDBM148003"	"N#C[C@@H]1C[C@H](C(=O)NC2CC(F)(F)C2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"136.0"	"nM"	"6.87"	""	"285938"	"UO_0000065"	"14.40"	"0.28"	"3.10"	"5.46"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647914"	""	"0"	"436.93"	"0"	"2.16"	"BDBM148026"	"CS(=O)(=O)N[C@@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	"285963"	"UO_0000065"	"18.53"	"0.38"	"5.94"	"5.67"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703486"	""	"0"	"321.34"	"0"	"2.69"	"BDBM153130"	"CCOC(=O)c1c[nH]c2ncnc(-c3ccc4cn(C)nc4c3)c12"	"IC50"	"'='"	"273.0"	"nM"	"6.56"	""	"294078"	"UO_0000065"	"20.43"	"0.37"	"3.87"	"7.66"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651032"	""	"0"	"372.41"	"0"	"2.69"	"BDBM153209"	"C=CS(=O)(=O)Nc1cccc(-c2ncnc3[nH]cc(C(=O)OCC)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294157"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3622131"	""	"0"	"410.52"	"0"	"3.16"	"12"	"CCn1c(C(=O)N(C2CC2)C2CC2)cc2c3c(ncn3C)c(NCCCOC)nc21"	"IC50"	"'='"	"40.0"	"nM"	"7.40"	""	""	"UO_0000065"	"18.02"	"0.34"	"4.24"	"9.58"	"False"	"CHEMBL3625473"	"Inhibition of JAK2 (unknown origin) using 5-FAMKKKKEEIYFFFG-OH as substrate after 60 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621098"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3645058"	""	"0"	"487.58"	"1"	"6.39"	"BDBM99826"	"CC(C)(C)OC(=O)N1CCC(c2ccc(Nc3nc4c(-c5ccc(F)cc5)cccn4n3)cc2)CC1"	"IC50"	"'='"	"360.56"	"nM"	"6.44"	""	"216499"	"UO_0000065"	"13.21"	"0.24"	"0.05"	"8.98"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3645063"	""	"0"	"484.60"	"0"	"4.42"	"BDBM99831"	"COc1cccc(-c2cccn3nc(Nc4ccc(C5CCN(CC(=O)N(C)C)CC5)cc4)nc23)c1"	"IC50"	"'='"	"10.69"	"nM"	"7.97"	""	"216504"	"UO_0000065"	"16.45"	"0.30"	"3.55"	"10.63"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647903"	""	"0"	"456.93"	"0"	"2.45"	"BDBM148015"	"CC1(O)CN(C(=O)[C@H]2CC[C@H](n3cc(C(N)=O)c(Nc4ccc(Cl)cc4)n3)[C@@H](C#N)C2)C1"	"IC50"	"'='"	"180.0"	"nM"	"6.75"	""	"285950"	"UO_0000065"	"14.76"	"0.29"	"4.29"	"4.91"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642278"	""	"0"	"306.33"	"0"	"2.87"	"BDBM99541"	"COc1ccc(Nc2nc3c(-c4cn[nH]c4)cccn3n2)cc1"	"IC50"	"'='"	"32.6"	"nM"	"7.49"	""	"216233"	"UO_0000065"	"24.44"	"0.44"	"4.62"	"9.34"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL4284396"	""	"0"	"371.35"	"0"	"3.09"	"10"	"COCCc1c[nH]c2ncnc(-c3ccc4c(c3)N(C#N)CC(F)(F)O4)c12"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4265556"	"Inhibition of recombinant human GST-tagged JAK2 using KAIETDKEYYTVKD-NH2 as substrate in presence of 1 mM ATP concentration by coupled PK/LDH assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4261650"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4283198"	""	"0"	"289.34"	"0"	"2.93"	"21"	"C[C@@H]1Cc2ccc(-c3ncnc4[nH]ccc34)cc2[C@@H]1NC#N"	"IC50"	"'='"	"1870.0"	"nM"	"5.73"	""	""	"UO_0000065"	"19.80"	"0.36"	"2.80"	"7.40"	"False"	"CHEMBL4265556"	"Inhibition of recombinant human GST-tagged JAK2 using KAIETDKEYYTVKD-NH2 as substrate in presence of 1 mM ATP concentration by coupled PK/LDH assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4261650"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL2181083"	""	"0"	"472.59"	"0"	"4.96"	"21h, 85:15 trans/cis mixture"	"C1=CCOCc2cccc(c2)-c2ccnc(n2)Nc2cc(cc(OCCN3CCCC3)c2)COC1"	"IC50"	"'='"	"48.0"	"nM"	"7.32"	""	""	"UO_0000065"	"15.49"	"0.29"	"2.36"	"10.65"	"False"	"CHEMBL2184201"	"Inhibition of recombinant JAK2 using Poly (Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176955"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL2181328"	""	"0"	"437.93"	"1"	"5.11"	"21a, 85:15 trans/cis mixture"	"ClCCOc1ccc2cc1COCC=CCOCc1cccc(c1)-c1ccnc(n1)N2"	"IC50"	"'='"	"220.0"	"nM"	"6.66"	""	""	"UO_0000065"	"15.20"	"0.29"	"1.55"	"10.16"	"False"	"CHEMBL2184201"	"Inhibition of recombinant JAK2 using Poly (Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176955"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL3962448"	""	"0"	"350.39"	"0"	"1.24"	"BDBM228745"	"CN(c1ccc2[nH]c(=O)[nH]c2n1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399675"	"UO_0000065"	"29.28"	"0.54"	"9.02"	"9.36"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3622195"	""	"0"	"433.90"	"0"	"4.21"	"BDBM130256"	"NC(=O)c1cc(-c2cccc(Cl)c2)cc2c1[nH]c1ccc(C(=O)N3CCOCC3)cc12"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"262042"	"UO_0000065"	"20.74"	"0.40"	"4.79"	"10.18"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3646821"	""	"0"	"519.61"	"1"	"4.45"	"BDBM130267"	"COc1cccc(-c2cc(C(N)=O)c3[nH]c4cc(C(=O)N5CCN(Cc6cccnc6)CC5)ccc4c3c2)c1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"262053"	"UO_0000065"	"15.82"	"0.29"	"3.77"	"7.86"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3646826"	""	"0"	"441.49"	"0"	"3.41"	"BDBM130272"	"COc1cccc(-c2cc(C(N)=O)c3[nH]c4cc(C(=O)C5O[C@H]6CN[C@H]5C6)ccc4c3c2)c1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"262058"	"UO_0000065"	"18.62"	"0.34"	"4.81"	"7.72"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3589176"	""	"0"	"447.47"	"0"	"3.71"	"BDBM130281"	"COc1ccc(-c2cc(C(N)=O)c3[nH]c4cc(C(=O)N5CCOCC5)ccc4c3c2)cc1F"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"262067"	"UO_0000065"	"18.22"	"0.34"	"4.44"	"8.35"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3639457"	""	"0"	"519.55"	"1"	"2.95"	"BDBM130286"	"COc1cc(-c2cc(C(N)=O)c3[nH]c4ccc(C(=O)N5CCOC(CO)C5)cc4c3c2)cc(OC)c1OC"	"IC50"	"'='"	"160.0"	"nM"	"6.80"	""	"262072"	"UO_0000065"	"13.08"	"0.24"	"3.85"	"4.98"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649633"	""	"0"	"457.52"	"0"	"3.56"	"BDBM130327"	"NC(=O)c1cc(-c2ccc3scnc3c2)nc2c1[nH]c1cc(C(=O)N3CCOCC3)ccc12"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"262113"	"UO_0000065"	"19.67"	"0.37"	"5.44"	"7.88"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649635"	""	"0"	"391.39"	"0"	"1.94"	"BDBM130329"	"NC(=O)c1cc(-c2cnoc2)nc2c1[nH]c1cc(C(=O)N3CCOCC3)ccc12"	"IC50"	"'='"	"112.0"	"nM"	"6.95"	""	"262115"	"UO_0000065"	"17.76"	"0.33"	"5.01"	"5.46"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649637"	""	"0"	"498.59"	"0"	"2.71"	"BDBM130331"	"CN1CCN(c2ccc(-c3cc(C(N)=O)c4[nH]c5cc(C(=O)N6CCOCC6)ccc5c4n3)cc2)CC1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"262117"	"UO_0000065"	"16.49"	"0.30"	"5.51"	"7.63"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649654"	""	"0"	"456.53"	"0"	"4.17"	"BDBM130349"	"NC(=O)c1cc(-c2ccc3scnc3c2)cc2c1[nH]c1cc(C(=O)N3CCOCC3)ccc12"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"262135"	"UO_0000065"	"18.01"	"0.34"	"4.05"	"8.12"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL4435170"	"DEUCRAVACITINIB"	"3"	"425.47"	"0"	"1.73"	"11; BMS-986165"	"[2H]C([2H])([2H])NC(=O)c1nnc(NC(=O)C2CC2)cc1Nc1cccc(-c2ncn(C)n2)c1OC"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4377469"	"Inhibition of fluorescein labeled probe binding to human recombinant JAK2 JH1 domain incubated for 1 hr by HTRF assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4376812"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL2376154"	""	"0"	"488.94"	"0"	"2.66"	"6k"	"Cn1nc(-c2cnc3[nH]cc(C(=O)N[C@@H](C(=O)N4CC(C#N)C4)C4CC4)c3n2)c2ccc(Cl)cc21"	"IC50"	"'='"	"1.1"	"nM"	"8.96"	""	""	"UO_0000065"	"18.32"	"0.35"	"6.30"	"6.76"	"False"	"CHEMBL2378515"	"Inhibition of JAK2 (unknown origin) using [33gammaP]ATP and Biotin-KAIETDKEYYTVKD as substrate incubated for 10 mins prior to substrate addition measured after 30 mins by filtration assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375236"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2376149"	""	"0"	"458.48"	"0"	"1.62"	"6f"	"COc1ccc2c(-c3cnc4[nH]cc(C(=O)N[C@H](C)C(=O)N5CC(C#N)C5)c4n3)nn(C)c2c1"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	""	"UO_0000065"	"17.00"	"0.31"	"6.18"	"5.50"	"False"	"CHEMBL2378515"	"Inhibition of JAK2 (unknown origin) using [33gammaP]ATP and Biotin-KAIETDKEYYTVKD as substrate incubated for 10 mins prior to substrate addition measured after 30 mins by filtration assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375236"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL3642259"	""	"0"	"477.59"	"0"	"4.02"	"BDBM99517"	"CS(=O)(=O)c1cccc(-c2cccn3nc(Nc4ccc(OCCN5CCCC5)cc4)nc23)c1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"216209"	"UO_0000065"	"17.85"	"0.34"	"4.50"	"9.59"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647818"	""	"0"	"500.57"	"2"	"5.24"	"BDBM147923"	"N#C[C@H]1C[C@H](N(CC2CC2)C2CCC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"1500.0"	"nM"	"5.82"	""	"285857"	"UO_0000065"	"11.63"	"0.22"	"0.58"	"5.83"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647846"	""	"0"	"385.86"	"0"	"3.16"	"BDBM147955"	"C=C[C@@]1(O)CC[C@H](n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"285889"	"UO_0000065"	"21.31"	"0.42"	"5.06"	"7.03"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703042"	""	"0"	"504.56"	"1"	"4.07"	"BDBM147752"	"CC1(C)CN([C@H]2CC[C@H](n3cc(C(N)=O)c(Nc4ccc([C@@](C)(O)C(F)(F)F)cc4)n3)[C@@H](C#N)C2)C1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"285686"	"UO_0000065"	"17.84"	"0.34"	"4.93"	"7.49"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702926"	""	"0"	"377.37"	"0"	"4.00"	"BDBM147625"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"19.0"	"nM"	"7.72"	""	"285555"	"UO_0000065"	"20.46"	"0.39"	"3.72"	"7.98"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3335691"	""	"0"	"397.46"	"0"	"1.75"	"BDBM112546"	"N#CCS(=O)(=O)N1CCC[C@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.088"	"nM"	"10.06"	""	"233785"	"UO_0000065"	"25.30"	"0.49"	"8.31"	"7.88"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3702975"	""	"0"	"496.52"	"0"	"3.00"	"BDBM147685"	"N#C[C@H]1CC(NC2CC2)CCC1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"285618"	"UO_0000065"	"16.42"	"0.33"	"5.15"	"5.71"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652288"	""	"0"	"515.66"	"1"	"4.21"	"BDBM113097"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCCC(COc3ccc(F)cc3)C2)CC1"	"IC50"	"'='"	"32.0"	"nM"	"7.50"	""	"234541"	"UO_0000065"	"14.53"	"0.28"	"3.28"	"8.20"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL2062803"	""	"0"	"449.54"	"0"	"3.38"	"BDBM50389186"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4ccc(N5CCOCC5)cc4)nc23)cc1"	"IC50"	"'='"	"0.9"	"nM"	"9.05"	""	"216203"	"UO_0000065"	"20.12"	"0.39"	"5.67"	"10.18"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642310"	""	"0"	"394.46"	"0"	"3.55"	"BDBM99580"	"COc1cccc(Nc2nc3cccc(-c4cccc(S(C)(=O)=O)c4)n3n2)c1"	"IC50"	"'='"	"15.1"	"nM"	"7.82"	""	"216270"	"UO_0000065"	"19.83"	"0.38"	"4.27"	"9.14"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647926"	""	"0"	"367.41"	"0"	"2.33"	"BDBM148044"	"N#C[C@H]1CCC2(CC1n1cc(C(N)=O)c(Nc3ccccc3)n1)OCCO2"	"IC50"	"'='"	"235.0"	"nM"	"6.63"	""	"285986"	"UO_0000065"	"18.04"	"0.34"	"4.30"	"5.75"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703007"	""	"0"	"421.43"	"0"	"2.93"	"BDBM147717"	"CN(C)[C@H]1CC[C@@H](n2cc(C(N)=O)c(Nc3ccc(C(F)(F)F)nc3)n2)[C@H](C#N)C1"	"IC50"	"'='"	"800.0"	"nM"	"6.10"	""	"285651"	"UO_0000065"	"14.47"	"0.28"	"3.17"	"5.40"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647800"	""	"0"	"466.90"	"0"	"4.30"	"BDBM147903"	"N#C[C@H]1C[C@H](NC2(C(F)(F)F)CC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"186.0"	"nM"	"6.73"	""	"285837"	"UO_0000065"	"14.42"	"0.29"	"2.43"	"6.19"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699477"	""	"0"	"387.47"	"0"	"2.38"	"BDBM147492"	"CS(=O)(=O)c1ccc(Nc2nn(C3CCCCC3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"285417"	"UO_0000065"	"20.76"	"0.41"	"5.67"	"6.15"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4564903"	""	"0"	"352.40"	"0"	"1.08"	"11o"	"C=CC(=O)N1CCC(n2nc(-c3cc(C)n(C)n3)c3c(N)ncnc32)C1"	"IC50"	"'='"	"45.3"	"nM"	"7.34"	""	""	"UO_0000065"	"20.84"	"0.39"	"6.26"	"6.82"	"False"	"CHEMBL4402146"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-biotin as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4400567"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL2376145"	""	"0"	"462.90"	"0"	"2.27"	"6b"	"C[C@@H](NC(=O)c1c[nH]c2ncc(-c3nn(C)c4ccc(Cl)cc34)nc12)C(=O)N1CC(C#N)C1"	"IC50"	"'='"	"28.0"	"nM"	"7.55"	""	""	"UO_0000065"	"16.32"	"0.31"	"5.28"	"5.70"	"False"	"CHEMBL2378515"	"Inhibition of JAK2 (unknown origin) using [33gammaP]ATP and Biotin-KAIETDKEYYTVKD as substrate incubated for 10 mins prior to substrate addition measured after 30 mins by filtration assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375236"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL3702922"	""	"0"	"378.36"	"0"	"3.39"	"BDBM147621"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)nc2)n1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"285551"	"UO_0000065"	"21.26"	"0.41"	"4.66"	"7.34"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699510"	""	"0"	"423.45"	"0"	"2.98"	"BDBM147528"	"N#C[C@H]1CCCCC1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)F)cc2)n1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"285458"	"UO_0000065"	"19.60"	"0.39"	"5.32"	"6.34"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699559"	""	"0"	"361.81"	"0"	"3.77"	"BDBM147578"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(F)c(Cl)c2)n1"	"IC50"	"'='"	"42.0"	"nM"	"7.38"	""	"285508"	"UO_0000065"	"20.39"	"0.40"	"3.61"	"7.63"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699519"	""	"0"	"327.36"	"0"	"3.12"	"BDBM147537"	"N#C[C@H]1CCCCC1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	"285977"	"UO_0000065"	"23.90"	"0.45"	"4.70"	"8.09"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642277"	""	"0"	"409.47"	"0"	"3.63"	"BDBM99540"	"COc1ccc(Nc2nc3c(Nc4ccc(S(C)(=O)=O)cc4)cccn3n2)cc1"	"IC50"	"'='"	"470.2"	"nM"	"6.33"	""	"216232"	"UO_0000065"	"15.45"	"0.30"	"2.70"	"6.48"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647747"	""	"0"	"498.53"	"0"	"3.25"	"BDBM147850"	"CC(C)N[C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	"285784"	"UO_0000065"	"16.24"	"0.33"	"4.85"	"5.67"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699497"	""	"0"	"456.52"	"0"	"3.87"	"BDBM147513"	"CC(C)(C)OC(=O)NCC1CC[C@H](C#N)[C@@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)C1"	"IC50"	"'='"	"1300.0"	"nM"	"5.89"	""	"285442"	"UO_0000065"	"12.89"	"0.24"	"2.02"	"4.36"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL2170419"	""	"0"	"358.76"	"0"	"4.45"	"3o"	"O=C(O)c1ccc(Nc2ncc(F)c(Nc3ccccc3Cl)n2)cc1"	"IC50"	"'='"	"91.0"	"nM"	"7.04"	""	""	"UO_0000065"	"19.63"	"0.38"	"2.59"	"8.08"	"False"	"CHEMBL2174405"	"Inhibition of JAK2 by 33P kinase hotspot assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2169801"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL3647821"	""	"0"	"502.59"	"2"	"5.35"	"BDBM147926"	"CC(C)CN(CC1CC1)[C@H]1CC[C@@H](n2cc(C(N)=O)c(Nc3ccc(C(F)(F)F)cc3)n2)[C@H](C#N)C1"	"IC50"	"'='"	"910.0"	"nM"	"6.04"	""	"285860"	"UO_0000065"	"12.02"	"0.23"	"0.69"	"6.04"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699482"	""	"0"	"356.41"	"0"	"2.32"	"BDBM147497"	"CN[C@@H]1CC[C@H](C#N)[C@@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)C1"	"IC50"	"'>'"	"1500.0"	"nM"	""	""	"285424"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699546"	""	"0"	"338.42"	"0"	"2.44"	"BDBM147564"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(CN)cc2)n1"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	"285494"	"UO_0000065"	"23.64"	"0.44"	"5.56"	"6.52"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702885"	""	"0"	"453.47"	"0"	"2.47"	"BDBM147584"	"N#C[C@H]1CCCCC1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)F)c(CO)c2)n1"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	"285514"	"UO_0000065"	"17.32"	"0.35"	"5.38"	"5.20"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3655093"	""	"0"	"385.44"	"0"	"1.89"	"BDBM159760"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)CC2CC(F)(F)C2)C1"	"IC50"	"'='"	"413.0"	"nM"	"6.38"	""	"302570"	"UO_0000065"	"16.56"	"0.34"	"4.49"	"7.02"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL2181332"	""	"0"	"486.57"	"0"	"4.49"	"21e, 85:15 trans/cis mixture"	"O=C1CCCN1CCOc1ccc2cc1COCC=CCOCc1cccc(c1)-c1ccnc(n1)N2"	"IC50"	"'='"	"22.0"	"nM"	"7.66"	""	""	"UO_0000065"	"15.74"	"0.29"	"3.17"	"8.92"	"False"	"CHEMBL2184201"	"Inhibition of recombinant JAK2 using Poly (Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176955"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL3665211"	""	"0"	"459.58"	"0"	"1.22"	"BDBM112611"	"CN(C)CCNc1ncc(-c2cnc3[nH]ccc3n2)c(N[C@H]2CCCN(S(C)(=O)=O)C2)n1"	"IC50"	"'='"	"0.1921"	"nM"	"9.72"	""	"233848"	"UO_0000065"	"21.14"	"0.41"	"8.50"	"7.36"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL2181325"	""	"0"	"485.59"	"0"	"4.16"	"17f, 85:15 trans/cis mixture"	"CC(=O)N1CCN(c2ccc3cc2COCC=CCOCc2cccc(c2)-c2ccnc(n2)N3)CC1"	"IC50"	"'='"	"120.0"	"nM"	"6.92"	""	""	"UO_0000065"	"14.25"	"0.26"	"2.76"	"8.67"	"False"	"CHEMBL2184201"	"Inhibition of recombinant JAK2 using Poly (Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176955"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL3642386"	""	"0"	"490.63"	"0"	"4.57"	"BDBM99664"	"CN1CCC(c2ccc(Nc3nc4c(Nc5ccccc5CS(C)(=O)=O)cccn4n3)cc2)CC1"	"IC50"	"'='"	"39.89"	"nM"	"7.40"	""	"216354"	"UO_0000065"	"15.08"	"0.29"	"2.83"	"8.08"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3699519"	""	"0"	"327.36"	"0"	"3.12"	"BDBM147537"	"N#C[C@H]1CCCCC1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"150.0"	"nM"	"6.82"	""	"285976"	"UO_0000065"	"20.85"	"0.39"	"3.70"	"7.05"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3650674"	""	"0"	"484.50"	"0"	"2.81"	"BDBM148055"	"CN(C)[C@@H]1CCC(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	"285610"	"UO_0000065"	"16.35"	"0.33"	"5.11"	"5.91"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4278647"	""	"0"	"289.34"	"0"	"2.93"	"20"	"C[C@H]1Cc2ccc(-c3ncnc4[nH]ccc34)cc2[C@@H]1NC#N"	"IC50"	"'='"	"1046.0"	"nM"	"5.98"	""	""	"UO_0000065"	"20.67"	"0.37"	"3.05"	"7.73"	"False"	"CHEMBL4265556"	"Inhibition of recombinant human GST-tagged JAK2 using KAIETDKEYYTVKD-NH2 as substrate in presence of 1 mM ATP concentration by coupled PK/LDH assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4261650"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3647721"	""	"0"	"426.95"	"0"	"3.95"	"BDBM147823"	"CC1(C)CN([C@H]2CC[C@H](n3cc(C(N)=O)c(Nc4ccc(Cl)cc4)n3)[C@@H](C#N)C2)C1"	"IC50"	"'='"	"21.0"	"nM"	"7.68"	""	"285757"	"UO_0000065"	"17.98"	"0.35"	"3.73"	"7.68"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642395"	""	"0"	"519.68"	"1"	"4.42"	"BDBM99673"	"CN1CCC(c2ccc(Nc3nc4c(Nc5ccccc5CN(C)S(C)(=O)=O)cccn4n3)cc2)CC1"	"IC50"	"'='"	"111.13"	"nM"	"6.95"	""	"216363"	"UO_0000065"	"13.38"	"0.26"	"2.53"	"7.33"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL584052"	""	"0"	"341.37"	"0"	"4.02"	"9"	"O=C1Nc2ccccc2-c2ccnc3[nH]cc(c23)C1c1ccc(O)cc1"	"IC50"	"'='"	"870.0"	"nM"	"6.06"	""	""	"UO_0000065"	"17.75"	"0.32"	"2.04"	"7.77"	"False"	"CHEMBL1042418"	"Inhibition JAK2 V617F mutant in bone marrow aspirate from polycythemia vera patient assessed as blockade of formation of EPO-independent endogenous erythroid colonies by microscopy"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1154754"	"1"	"Scientific Literature"	"J. Med. Chem."	"2009"	"None"	""
"CHEMBL3702951"	""	"0"	"423.40"	"0"	"2.55"	"BDBM147653"	"N#C[C@H]1C[C@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc([C@@H](O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"285585"	"UO_0000065"	"20.13"	"0.39"	"5.97"	"6.21"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699511"	""	"0"	"401.49"	"0"	"2.77"	"BDBM147529"	"CCS(=O)(=O)c1ccc(Nc2nn(C3CCCC[C@@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"285459"	"UO_0000065"	"20.92"	"0.41"	"5.63"	"6.42"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642269"	""	"0"	"474.63"	"1"	"5.89"	"BDBM99530"	"CC1(C)CCC(C)(C)c2cc(Nc3nc4c(-c5ccc(S(C)(=O)=O)cc5)cccn4n3)ccc21"	"IC50"	"'='"	"27.7"	"nM"	"7.56"	""	"216222"	"UO_0000065"	"15.92"	"0.30"	"1.67"	"9.90"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3645065"	""	"0"	"417.49"	"0"	"4.75"	"BDBM99833"	"COc1cccc(-c2cccn3nc(Nc4ccc(C5CCNCC5)cc4)nc23)c1F"	"IC50"	"'='"	"30.45"	"nM"	"7.52"	""	"216506"	"UO_0000065"	"18.00"	"0.33"	"2.77"	"11.84"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703011"	""	"0"	"459.50"	"0"	"3.34"	"BDBM147721"	"C[C@H](N[C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(OC(F)F)nc3)n2)[C@@H](C#N)C1)C1CC1"	"IC50"	"'='"	"144.0"	"nM"	"6.84"	""	"285655"	"UO_0000065"	"14.89"	"0.28"	"3.50"	"5.23"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3694591"	""	"0"	"442.95"	"1"	"6.48"	"BDBM125912"	"Clc1cnc2nc1NCc1cc(ccc1-c1ccccc1)OCCCc1cccc(c1)N2"	"IC50"	"'='"	"41.0"	"nM"	"7.39"	""	"255685"	"UO_0000065"	"16.68"	"0.32"	"0.91"	"12.51"	"False"	"CHEMBL3707544"	"In Vitro Kinase Assay: One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Biochemistry 1999, 269, 94-104. The catalytic domains of human JAK1 (a.a. 837-1142), JAK2 (a.a. 828-1132) and JAK3 (a.a. 781-1124) with an N-terminal His tag were expressed using baculovirus in insect cells and purified. The catalytic activity of JAK1, JAK2 or JAK3 was assayed by measuring the phosphorylation of a biotinylated peptide. The phosphorylated peptide was detected by homogenous time resolved fluorescence (HTRF). IC50s of compounds were measured for each kinase in the reactions that contain the enzyme, ATP and 500 nM peptide in 50 mM Tris (pH 7.8) buffer with 100 mM NaCl, 5 mM DTT, and 0.1 mg/mL (0.01%) BSA. The ATP concentration in the reactions was 90 uM for JAK1, 30 uM for JAK2 and 3 uM for JAK3. Reactions were carried out at room temperature for 1 hr and then stopped with 20 uL 45 mM EDTA."	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639093"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3642409"	""	"0"	"463.56"	"0"	"2.98"	"BDBM99687"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4cccc([C@@H]5CCNC[C@@H]5O)c4)nc23)cc1"	"IC50"	"'='"	"1.43"	"nM"	"8.85"	""	"216376"	"UO_0000065"	"19.08"	"0.37"	"5.86"	"8.14"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652408"	""	"0"	"465.62"	"0"	"2.41"	"BDBM113220"	"COCCOC1CCCN(S(=O)(=O)C[C@H]2CC[C@H](N(C)c3ncnc4[nH]ccc34)CC2)C1"	"IC50"	"'='"	"0.00405"	"nM"	""	"Outside typical range"	"234663"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3360353"	""	"0"	"377.45"	"0"	"2.58"	"BDBM103728"	"O=C(Nc1nc2cccc(-c3ccc(CN4CCOCC4)cc3)n2n1)C1CC1"	"IC50"	"'='"	"152.3"	"nM"	"6.82"	""	"221714"	"UO_0000065"	"18.06"	"0.33"	"4.24"	"9.50"	"False"	"CHEMBL3707887"	"Inhibition Assay: In vitro inhibition assay using various enzyme."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638964"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3658124"	""	"0"	"598.99"	"2"	"6.21"	"BDBM148446"	"CNC(=O)c1ccc(Nc2ncc3c(n2)CCN(c2cc(NC(=O)c4cc(F)cc(C(F)(F)F)c4)ccc2Cl)C3)cc1"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	"286809"	"UO_0000065"	"13.36"	"0.26"	"1.79"	"8.06"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665152"	""	"0"	"412.52"	"0"	"2.64"	"BDBM112542"	"O=S(=O)(CC1CC1)N1CCC[C@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.0413"	"nM"	"10.38"	""	"233781"	"UO_0000065"	"25.17"	"0.49"	"7.74"	"10.00"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3702985"	""	"0"	"414.94"	"0"	"4.00"	"BDBM147695"	"CC(C)(C)N[C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	"285629"	"UO_0000065"	"18.66"	"0.36"	"3.74"	"7.12"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3622135"	""	"0"	"435.56"	"0"	"4.22"	"16"	"CCn1c(C(=O)N(C2CC2)C2CC2)cc2c3c(ncn3C)c(Nc3nc(C)cs3)nc21"	"IC50"	"'='"	"1.9"	"nM"	"8.72"	""	""	"UO_0000065"	"20.02"	"0.38"	"4.50"	"10.78"	"False"	"CHEMBL3625473"	"Inhibition of JAK2 (unknown origin) using 5-FAMKKKKEEIYFFFG-OH as substrate after 60 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621098"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3702969"	""	"0"	"397.45"	"0"	"3.52"	"BDBM147676"	"N#C[C@H]1C[C@@H](OCC2CC2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'>'"	"1500.0"	"nM"	""	""	"285608"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665151"	""	"0"	"386.48"	"0"	"2.25"	"BDBM112541"	"CS(=O)(=O)N1CCCC(Nc2ncccc2-c2cnc3[nH]ccc3n2)CC1"	"IC50"	"'='"	"0.0089"	"nM"	""	"Outside typical range"	"233780"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3360353"	""	"0"	"377.45"	"0"	"2.58"	"BDBM103728"	"O=C(Nc1nc2cccc(-c3ccc(CN4CCOCC4)cc3)n2n1)C1CC1"	"IC50"	"'='"	"38.73"	"nM"	"7.41"	""	"221713"	"UO_0000065"	"19.64"	"0.36"	"4.83"	"10.33"	"False"	"CHEMBL3707887"	"Inhibition Assay: In vitro inhibition assay using various enzyme."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638964"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647746"	""	"0"	"510.54"	"1"	"3.25"	"BDBM147849"	"N#C[C@H]1C[C@H](NCC2CC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"24.0"	"nM"	"7.62"	""	"285783"	"UO_0000065"	"14.92"	"0.30"	"4.37"	"5.33"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647808"	""	"0"	"456.98"	"0"	"3.77"	"BDBM147911"	"CC1(N[C@H]2CCC(n3cc(C(N)=O)c(Nc4ccc(Cl)cc4)n3)[C@@H](C#N)C2)CCOCC1"	"IC50"	"'='"	"25.0"	"nM"	"7.60"	""	"285845"	"UO_0000065"	"16.64"	"0.32"	"3.83"	"6.44"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3649628"	""	"0"	"362.36"	"0"	"4.23"	"BDBM130322"	"Cc1ccc(-c2cc(C(N)=O)c3[nH]c4ccc(C(=O)O)cc4c3c2)c(F)c1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"262108"	"UO_0000065"	"24.84"	"0.46"	"4.77"	"9.36"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL4471390"	""	"0"	"391.41"	"0"	"3.73"	"7h"	"Cc1cnc(Nc2ccc(F)cc2)nc1-c1cc2c(o1)CCN(C(=O)CC#N)C2"	"IC50"	"'='"	"9.2"	"nM"	"8.04"	""	""	"UO_0000065"	"20.53"	"0.38"	"4.31"	"8.45"	"False"	"CHEMBL4341343"	"Inhibition of JAK2 (unknown origin) using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition and measured by 30 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4458798"	""	"0"	"425.94"	"1"	"5.73"	"12s"	"CC(Oc1cc(-c2ccc(C3CCNCC3)cc2)cnc1N)c1cc(F)ccc1Cl"	"IC50"	"'='"	"48.0"	"nM"	"7.32"	""	""	"UO_0000065"	"17.18"	"0.33"	"1.59"	"12.16"	"False"	"CHEMBL4341687"	"Inhibition of human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr by Z'-LYTE assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340536"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2019"	"CHEMBL3308860"	""
"CHEMBL4516300"	""	"0"	"342.80"	"1"	"5.26"	"12p"	"CC(Oc1cc(-c2ccccc2)cnc1N)c1cc(F)ccc1Cl"	"IC50"	"'='"	"461.0"	"nM"	"6.34"	""	""	"UO_0000065"	"18.48"	"0.36"	"1.08"	"13.16"	"True"	"CHEMBL4341687"	"Inhibition of human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr by Z'-LYTE assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340536"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2019"	"CHEMBL3308860"	""
"CHEMBL4461078"	""	"0"	"445.93"	"0"	"4.39"	"12j"	"COc1ccc(F)c(Cl)c1C(C)Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N"	"IC50"	"'='"	"26.0"	"nM"	"7.58"	""	""	"UO_0000065"	"17.01"	"0.33"	"3.20"	"8.70"	"False"	"CHEMBL4341687"	"Inhibition of human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr by Z'-LYTE assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340536"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2019"	"CHEMBL3308860"	""
"CHEMBL1825138"	""	"0"	"450.35"	"1"	"5.04"	"12a"	"CC(Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl"	"IC50"	"'='"	"92.0"	"nM"	"7.04"	""	""	"UO_0000065"	"15.62"	"0.32"	"2.00"	"9.02"	"False"	"CHEMBL4341687"	"Inhibition of human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr by Z'-LYTE assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340536"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2019"	"CHEMBL3308860"	""
"CHEMBL1789941"	"RUXOLITINIB"	"4"	"306.37"	"0"	"3.47"	"1"	"N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"2.8"	"nM"	"8.55"	""	""	"UO_0000065"	"27.92"	"0.51"	"5.08"	"10.28"	"True"	"CHEMBL4341680"	"Inhibition of recombinant human N-terminal epitope-tagged JAK2 (828 to 1132 residues) expressed in baculovirus infected Sf21 insect cells using EQEDEPEGDYFEWLE as substrate after 1 hr by homogeneous time-resolved fluorescence assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340536"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2019"	"CHEMBL4106362"	""
"CHEMBL4537207"	""	"0"	"520.59"	"1"	"4.70"	"7p"	"Cc1cnc(Nc2ccc(N3CCOCC3)cc2)nc1-c1cc2c(o1)CCN(C(=O)c1ccc(C#N)cc1)C2"	"IC50"	"'='"	"28.8"	"nM"	"7.54"	""	""	"UO_0000065"	"14.48"	"0.26"	"2.84"	"7.01"	"False"	"CHEMBL4341343"	"Inhibition of JAK2 (unknown origin) using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition and measured by 30 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4440795"	""	"0"	"463.49"	"0"	"3.61"	"7n"	"COc1cc(Nc2ncc(C)c(-c3cc4c(o3)CCN(C(=O)CC#N)C4)n2)cc(OC)c1OC"	"IC50"	"'='"	"1.6"	"nM"	"8.80"	""	""	"UO_0000065"	"18.98"	"0.35"	"5.19"	"7.17"	"False"	"CHEMBL4341343"	"Inhibition of JAK2 (unknown origin) using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition and measured by 30 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4632980"	""	"0"	"256.31"	"0"	"2.48"	"19"	"Cc1[nH]nc2[nH]c(=O)c(C#N)c(C3CCCCC3)c12"	"IC50"	"'>'"	"40000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL4640029"	""	"0"	"284.36"	"0"	"3.14"	"22"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](CCC#N)CC3)c12"	"IC50"	"'='"	"13000.0"	"nM"	"4.89"	""	""	"UO_0000065"	"17.18"	"0.32"	"1.75"	"5.73"	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL4638808"	""	"0"	"350.44"	"0"	"1.67"	"30"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](NS(=O)(=O)C4CC4)CC3)c12"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL4636368"	""	"0"	"246.31"	"0"	"1.54"	"32"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](N)CC3)c12"	"IC50"	"'>'"	"40000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL4647506"	""	"0"	"247.30"	"0"	"1.58"	"33"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](O)CC3)c12"	"IC50"	"'>'"	"40000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL4634289"	""	"0"	"282.35"	"0"	"2.60"	"41"	"Cc1[nH]nc2[nH]c(=O)cc([C@@H]3C[C@@H]4C[C@H]3C[C@@H]4CC#N)c12"	"IC50"	"'='"	"24000.0"	"nM"	"4.62"	""	""	"UO_0000065"	"16.36"	"0.30"	"2.02"	"5.41"	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL3655081"	"ABROCITINIB"	"3"	"323.42"	"0"	"1.25"	"Abrocitinib"	"CCCS(=O)(=O)N[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"1400.0"	"nM"	"5.85"	""	""	"UO_0000065"	"18.10"	"0.36"	"4.60"	"6.43"	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL3702954"	""	"0"	"395.46"	"0"	"2.24"	"BDBM147656"	"CC1(c2ccc(Nc3nn([C@H]4CC[C@@H](O)C[C@@H]4C#N)cc3C(N)=O)cc2)COC1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"285588"	"UO_0000065"	"21.24"	"0.40"	"6.16"	"6.65"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3954206"	""	"0"	"490.57"	"0"	"3.53"	"262"	"N#CCC1(n2ccc(-c3ncnc4[nH]ccc34)c2)CN(C2CCN(C(=O)c3cccc(C#N)c3)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3986291"	""	"0"	"519.53"	"1"	"4.07"	"270"	"N#CCC1(n2ccc(-c3ncnc4[nH]ccc34)c2)CN(C2CCN(C(=O)c3c(F)ccc(F)c3F)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3907633"	""	"0"	"551.55"	"1"	"4.81"	"274"	"N#CCC1(n2ccc(-c3ncnc4[nH]ccc34)c2)CN(C2CCN(C(=O)c3cc(F)cc(C(F)(F)F)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3981082"	""	"0"	"535.53"	"1"	"3.46"	"300"	"N#CCC1(n2cc(-c3ccnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cncc(C(F)(F)F)n3)CC2)C1"	"IC50"	"'>'"	"100.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3986462"	""	"0"	"515.02"	"1"	"4.70"	"310"	"N#CCC1(n2cc(-c3ccnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3ccccc3Cl)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3980275"	""	"0"	"526.55"	"1"	"3.81"	"318"	"N#CCC1(n2cc(-c3c(F)cnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(F)c(C#N)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3895027"	""	"0"	"584.55"	"2"	"5.34"	"328"	"N#CCC1(n2cc(-c3c(F)cnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3ccc(F)cc3C(F)(F)F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3936845"	""	"0"	"540.59"	"1"	"3.27"	"338"	"N#CCC1(n2cc(-c3c(C#N)cnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc(C#N)cc(C#N)c3)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3941550"	""	"0"	"533.57"	"1"	"3.54"	"339"	"N#CCC1(n2cc(-c3c(C#N)cnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(C#N)cc3F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3978627"	""	"0"	"554.51"	"1"	"2.81"	"362"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN([C@@H]2CCN(C(=O)c3ccnc(C(F)(F)F)n3)C[C@@H]2F)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3644989"	""	"0"	"467.50"	"1"	"5.63"	"BDBM99741"	"COc1ccc(C(F)(F)F)cc1-c1cccn2nc(Nc3cccc(C4CCNCC4)c3)nc12"	"IC50"	"'='"	"28.92"	"nM"	"7.54"	""	"216429"	"UO_0000065"	"16.13"	"0.30"	"1.91"	"11.88"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642290"	""	"0"	"491.62"	"0"	"3.14"	"BDBM99556"	"CN1CCN(c2ccc(Nc3nc4c(-c5ccc(S(=O)(=O)N(C)C)cc5)cccn4n3)cc2)CC1"	"IC50"	"'='"	"1.7"	"nM"	"8.77"	""	"216247"	"UO_0000065"	"17.84"	"0.34"	"5.63"	"10.19"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3648440"	""	"0"	"362.43"	"0"	"2.69"	"BDBM107149"	"O=C(CN1CCC(O)CC1)Nc1cccc(-c2cnc3ccccc3n2)c1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	"226387"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647719"	""	"0"	"411.49"	"0"	"2.83"	"BDBM147821"	"CC1(C)CN([C@@H]2CC[C@H](n3cc(C(N)=O)c(Nc4ccnc(F)c4)n3)[C@@H](C#N)C2)C1"	"IC50"	"'='"	"141.0"	"nM"	"6.85"	""	"285755"	"UO_0000065"	"16.65"	"0.31"	"4.02"	"6.07"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4282720"	""	"0"	"459.51"	"0"	"3.23"	"19a"	"COc1cc2c(=O)n([C@@H](C(=O)N3CC(C#N)C3)C(C)C)c3c4cc[nH]c4ncc3c2cc1OC"	"IC50"	"'='"	"1171.0"	"nM"	"5.93"	""	""	"UO_0000065"	"12.91"	"0.24"	"2.70"	"5.24"	"False"	"CHEMBL4261266"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]-ATP addition measured after 2 hrs by filter-binding method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257589"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"Tofacitinib"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"1.09"	"nM"	"8.96"	""	""	"UO_0000065"	"28.69"	"0.53"	"7.42"	"10.08"	"False"	"CHEMBL4261266"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]-ATP addition measured after 2 hrs by filter-binding method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257589"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4065693"	""	"0"	"387.44"	"0"	"3.66"	"9a"	"C=CC(=O)Nc1cccc(CNc2cc(Nc3ccccc3)ncc2C(N)=O)c1"	"IC50"	"'='"	"1300.0"	"nM"	"5.89"	""	""	"UO_0000065"	"15.19"	"0.28"	"2.23"	"5.39"	"False"	"CHEMBL4047228"	"Inhibition of GST-tagged JAK2 (unknown origin) using fluoresceinated peptide as substrate after 3 hrs by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4043231"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4062932"	""	"0"	"349.39"	"0"	"2.56"	"13b"	"C/C=C/C(=O)Nc1cccc(CNc2c(C(N)=O)cnn3cccc23)c1"	"IC50"	"'>'"	"2000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4047228"	"Inhibition of GST-tagged JAK2 (unknown origin) using fluoresceinated peptide as substrate after 3 hrs by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4043231"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL1651521"	""	"0"	"348.40"	"0"	"2.55"	"1"	"COc1cc(O)c2c(c1)CCC[C@H](O)CC(=O)/C=C\C[C@H](C)OC2=O"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1656532"	"Inhibition of JAK2 by TR-FRET based LanthaScreen assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649097"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL4244213"	""	"0"	"337.39"	"0"	"1.00"	"9g"	"Cn1cc(-c2nn(CC3CCCN(C#N)C3)c3ncnc(N)c23)cn1"	"IC50"	"'='"	"867.3"	"nM"	"6.06"	""	""	"UO_0000065"	"17.97"	"0.33"	"5.06"	"5.30"	"False"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"1"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"4.3"	"nM"	"8.37"	""	""	"UO_0000065"	"26.78"	"0.50"	"6.83"	"9.41"	"True"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4251240"	""	"0"	"427.51"	"0"	"0.64"	"13f"	"COCCn1cc(-c2nn(C3CCN(C(=O)CN(C)C)CC3)c3ncnc(N)c23)cn1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4286762"	""	"0"	"409.44"	"0"	"3.56"	"13c"	"CCOC(=O)C(CC)n1c(=O)c2cc(OC)c(OC)cc2c2cnc3[nH]ccc3c21"	"IC50"	"'='"	"10.55"	"nM"	"7.98"	""	""	"UO_0000065"	"19.48"	"0.36"	"4.42"	"8.36"	"False"	"CHEMBL4261266"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]-ATP addition measured after 2 hrs by filter-binding method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257589"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3642306"	""	"0"	"548.67"	"1"	"4.60"	"BDBM99576"	"CC(C)(C)OC(=O)N1CCN(c2ccc(Nc3nc4cccc(-c5ccc(S(C)(=O)=O)cc5)n4n3)cc2)CC1"	"IC50"	"'='"	"1.3"	"nM"	"8.89"	""	"216266"	"UO_0000065"	"16.20"	"0.31"	"4.29"	"8.14"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3781427"	""	"0"	"310.36"	"0"	"2.51"	"2"	"O=c1[nH]ccc(NC2CCOCC2)c1-c1nc2ccccc2[nH]1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	""	"UO_0000065"	"26.75"	"0.49"	"5.79"	"10.03"	"False"	"CHEMBL3784139"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3779778"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3780091"	""	"0"	"323.40"	"0"	"2.60"	"10"	"N[C@H]1CC[C@@H](Nc2cc[nH]c(=O)c2-c2nc3ccccc3[nH]2)CC1"	"IC50"	"'='"	"48.0"	"nM"	"7.32"	""	""	"UO_0000065"	"22.63"	"0.42"	"4.72"	"7.35"	"False"	"CHEMBL3784147"	"Inhibition of JAK2 in human CD34+ cells assessed as inhibition of EPO-mediated cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"CD34+ cell"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3779778"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL4279402"	""	"0"	"390.51"	"0"	"1.59"	"55"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(S(=O)(=O)N2CCCCC2)CC12CC2"	"IC50"	"'='"	"150.0"	"nM"	"6.82"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4288323"	""	"0"	"311.39"	"0"	"1.80"	"13"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(C(=O)C2CC2)CC12CC2"	"IC50"	"'='"	"1200.0"	"nM"	"5.92"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4283881"	""	"0"	"342.40"	"0"	"0.52"	"14"	"CC(=O)NCC(=O)N1C[C@H](N(C)c2ncnc3[nH]ccc23)C2(CC2)C1"	"IC50"	"'='"	"16000.0"	"nM"	"4.80"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4293188"	""	"0"	"372.43"	"0"	"2.57"	"21"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(C(=O)c2cccc(C#N)c2)CC12CC2"	"IC50"	"'='"	"7400.0"	"nM"	"5.13"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4284136"	""	"0"	"326.43"	"0"	"2.10"	"25"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(C(=S)CC#N)CC12CC2"	"IC50"	"'='"	"160.0"	"nM"	"6.80"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4290189"	""	"0"	"428.47"	"0"	"2.16"	"48"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(S(=O)(=O)c2ccccc2[N+](=O)[O-])CC12CC2"	"IC50"	"'='"	"470.0"	"nM"	"6.33"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4287238"	""	"0"	"396.50"	"0"	"1.64"	"16"	"CC(=O)N1CCC(C(=O)N2C[C@H](N(C)c3ncnc4[nH]ccc34)C3(CC3)C2)CC1"	"IC50"	"'='"	"2500.0"	"nM"	"5.60"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4105015"	""	"0"	"411.94"	"0"	"4.07"	"16"	"CC1(C)[C@H](Nc2c(C(N)=O)cnn3cc(-c4ccccc4Cl)cc23)CC[C@]1(C)N"	"IC50"	"'='"	"27.0"	"nM"	"7.57"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4054822"	"Inhibition of GST-tagged JAK2 (unknown origin) after 3 hrs by Caliper assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4052645"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4088673"	""	"0"	"396.47"	"0"	"2.95"	"33"	"CC1(C)[C@H](Nc2c(C(N)=O)cnn3cc(-c4cncc(F)c4)cc23)CC[C@]1(C)N"	"IC50"	"'='"	"44.0"	"nM"	"7.36"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4054822"	"Inhibition of GST-tagged JAK2 (unknown origin) after 3 hrs by Caliper assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4052645"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL1650954"	""	"0"	"399.37"	"0"	"3.82"	"8"	"CN(C)c1ccc(C(F)(F)F)c(C2=C(c3c[nH]c4ccccc34)C(=O)NC2=O)c1"	"IC50"	"'='"	"9150.0"	"nM"	"5.04"	""	""	"UO_0000065"	"12.62"	"0.24"	"1.22"	"7.73"	"False"	"CHEMBL1657171"	"Inhibition of GST-tagged Jak2 expressed in insect cells using 20 uM ATP"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649080"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL3702930"	""	"0"	"399.48"	"0"	"2.31"	"BDBM147632"	"N#C[C@H]1CCCCC1n1cc(C(N)=O)c(Nc2ccc3c(c2)CCS3(=O)=O)n1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"285563"	"UO_0000065"	"20.58"	"0.40"	"5.91"	"6.28"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3648429"	""	"0"	"289.34"	"0"	"3.81"	"BDBM107138"	"C=CCC(=O)Nc1cccc(-c2cnc3ccccc3n2)c1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	"226376"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642333"	""	"0"	"480.57"	"0"	"3.43"	"BDBM99605"	"CN1CCN(c2ccc(Nc3nc4c(-c5ccc(S(C)(=O)=O)cc5)cc(F)cn4n3)cc2)CC1"	"IC50"	"'='"	"31.6"	"nM"	"7.50"	""	"216295"	"UO_0000065"	"15.61"	"0.30"	"4.07"	"9.05"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703053"	""	"0"	"490.53"	"0"	"3.90"	"BDBM147763"	"CC1(C)CN([C@@H]2CC[C@H](n3cc(C(N)=O)c(Nc4ccc([C@@H](O)C(F)(F)F)cc4)n3)[C@@H](C#N)C2)C1"	"IC50"	"'='"	"24.0"	"nM"	"7.62"	""	"285697"	"UO_0000065"	"15.53"	"0.30"	"3.72"	"6.34"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702964"	""	"0"	"477.49"	"0"	"3.98"	"BDBM147671"	"N#C[C@@H]1C[C@H](OCC2CC2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc([C@H](O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"32.0"	"nM"	"7.50"	""	"285603"	"UO_0000065"	"15.70"	"0.30"	"3.51"	"5.94"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4747591"	""	"0"	"389.41"	"0"	"1.79"	"10; PF-06700841"	"Cn1cc(Nc2nccc(N3CC4CCC(C3)N4C(=O)[C@@H]3CC3(F)F)n2)cn1"	"IC50"	"'='"	"77.0"	"nM"	"7.11"	""	""	""	"18.27"	"0.35"	"5.32"	"8.98"	"False"	"CHEMBL4714260"	"Inhibition of recombinant human JAK2 assessed as phosphorylation level in presence of 1 mM ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706695"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2021"	"None"	""
"CHEMBL4782814"	""	"0"	"402.51"	"0"	"3.73"	"12; TD-1473"	"Cc1cc(Nc2cc3ncccc3c(N[C@H]3CC[C@@H]4C[C@H](C3)N4CCC#N)n2)n[nH]1"	"IC50"	"'='"	"33.0"	"nM"	"7.48"	""	""	""	"18.59"	"0.34"	"3.75"	"7.09"	"False"	"CHEMBL4714260"	"Inhibition of recombinant human JAK2 assessed as phosphorylation level in presence of 1 mM ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706695"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2021"	"None"	""
"CHEMBL3699469"	""	"0"	"325.37"	"0"	"1.95"	"BDBM147484"	"N#C[C@H]1CCC[C@H](O)C1n1cc(C(N)=O)c(Nc2ccccc2)n1"	"IC50"	"'='"	"320.0"	"nM"	"6.50"	""	"285409"	"UO_0000065"	"19.96"	"0.37"	"4.54"	"5.55"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645030"	""	"0"	"447.97"	"1"	"5.27"	"BDBM99791"	"CCCOc1ccc(Cl)cc1-c1cccn2nc(Nc3ccc4c(c3)CCNCC4)nc12"	"IC50"	"'='"	"827.82"	"nM"	"6.08"	""	"216470"	"UO_0000065"	"13.58"	"0.26"	"0.81"	"9.58"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3644962"	""	"0"	"478.58"	"0"	"3.42"	"BDBM99712"	"CN1CCN(c2cccc(Nc3nc4c(Oc5ccc(S(C)(=O)=O)cc5)cccn4n3)c2)CC1"	"IC50"	"'='"	"1646.77"	"nM"	"5.78"	""	"216402"	"UO_0000065"	"12.08"	"0.23"	"2.36"	"6.28"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL4066906"	""	"0"	"416.46"	"0"	"1.18"	"23"	"C[C@@H]1NS(=O)(=O)c2ccc(Nc3nn([C@H]4COCC[C@@H]4C#N)cc3C(N)=O)cc21"	"IC50"	"'='"	"224.0"	"nM"	"6.65"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4033007"	"Inhibition of JAK2 in EPO-stimulated human TF1 cells expressing stably integrated beta-lactamase reporter gene under control of STAT5 response elements in interferon regulatory factor 1 gene promoter by fluorescence assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4098999"	""	"0"	"376.42"	"0"	"2.58"	"25"	"N#Cc1ccc(Nc2nn([C@H]3COCC[C@@H]3C#N)cc2C(N)=O)cc1C1CC1"	"IC50"	"'='"	"744.0"	"nM"	"6.13"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4033007"	"Inhibition of JAK2 in EPO-stimulated human TF1 cells expressing stably integrated beta-lactamase reporter gene under control of STAT5 response elements in interferon regulatory factor 1 gene promoter by fluorescence assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4071005"	""	"0"	"375.82"	"0"	"2.49"	"28"	"COc1cc(Nc2nn([C@H]3COCC[C@@H]3C#N)cc2C(N)=O)ccc1Cl"	"IC50"	"'='"	"320.0"	"nM"	"6.50"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4033007"	"Inhibition of JAK2 in EPO-stimulated human TF1 cells expressing stably integrated beta-lactamase reporter gene under control of STAT5 response elements in interferon regulatory factor 1 gene promoter by fluorescence assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4088262"	""	"0"	"410.41"	"0"	"2.52"	"31"	"COc1ccnc2c(F)cc(Nc3nn([C@H]4COCC[C@@H]4C#N)cc3C(N)=O)cc12"	"IC50"	"'='"	"2114.0"	"nM"	"5.67"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4033007"	"Inhibition of JAK2 in EPO-stimulated human TF1 cells expressing stably integrated beta-lactamase reporter gene under control of STAT5 response elements in interferon regulatory factor 1 gene promoter by fluorescence assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL1650723"	""	"0"	"364.77"	"0"	"2.71"	"9a"	"COc1cc(Nc2nc(N[C@@H](C)c3ncc(F)cn3)ncc2Cl)n[nH]1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"23.37"	"0.47"	"5.81"	"7.51"	"False"	"CHEMBL1656588"	"Inhibition of JAK2 using Km ATP concentration"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL3134612"	""	"0"	"371.82"	"0"	"4.57"	"C8"	"COc1cc(Nc2nccc(-c3ccc(Cl)cc3)n2)cc(OC)c1OC"	"IC50"	"'='"	"21513.0"	"nM"	"4.67"	""	""	"UO_0000065"	"12.55"	"0.25"	"0.10"	"7.13"	"False"	"CHEMBL3136746"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3132747"	"1"	"Scientific Literature"	"MedChemComm"	"2014"	"None"	""
"CHEMBL3262355"	""	"0"	"417.48"	"0"	"2.32"	"3a"	"N[C@H]1CCCC[C@H]1Nc1cc2nc[nH]c(=O)c2c(Nc2cccc(-n3nccn3)c2)n1"	"IC50"	"'='"	"120.0"	"nM"	"6.92"	""	""	"UO_0000065"	"16.58"	"0.30"	"4.60"	"4.96"	"False"	"CHEMBL3268711"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3259804"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3262622"	""	"0"	"405.46"	"0"	"2.08"	"10a"	"Cn1cc2c(Nc3nc(N[C@@H]4CCOC[C@@H]4N)cc4cc[nH]c(=O)c34)cccc2n1"	"IC50"	"'='"	"1500.0"	"nM"	"5.82"	""	""	"UO_0000065"	"14.36"	"0.27"	"3.74"	"4.74"	"False"	"CHEMBL3268711"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3259804"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL2017214"	""	"0"	"422.56"	"0"	"3.12"	"8"	"CSc1ccccc1Nc1nc(N2CCNCC2)nc2c(NCC3CC3)ncnc12"	"IC50"	"'>'"	"40000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2019675"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2016462"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL4761365"	""	"0"	"411.94"	"0"	"4.04"	"38b"	"CNC(=O)c1cnc2[nH]ccc2c1N[C@@H]1CCN(Cc2ccc(Cl)cc2)[C@H](C)C1"	"IC50"	"'='"	"625.0"	"nM"	"6.20"	""	""	""	"15.06"	"0.29"	"2.16"	"8.49"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL3262621"	""	"0"	"417.52"	"0"	"3.84"	"3k"	"Cc1nc2cc(N[C@@H]3CCCC[C@@H]3N)nc(Nc3cccc4c(C)c[nH]c34)c2c(=O)[nH]1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3268711"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3259804"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL2030386"	""	"0"	"364.20"	"0"	"2.00"	"6l"	"O=c1[nH]c(CN2CC[C@@H](O)C2)nc2c1oc1ccc(Br)cc12"	"IC50"	"'>'"	"3600.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2038177"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2034948"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL4128266"	""	"0"	"357.42"	"1"	"5.21"	"11"	"N#C/C=C/c1ccc(-c2nc3cnc4[nH]ccc4c3n2C2CCCCC2)o1"	"IC50"	"'='"	"53.0"	"nM"	"7.28"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4124183"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate in presence of 10 uM [gamma33P]ATP by radiometric method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4118225"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL104466"	""	"0"	"303.36"	"0"	"2.36"	"10/ RP-127963"	"COc1cc2ncc(N[C@H]3CC[C@H](O)CC3)nc2cc1OC"	"IC50"	"'>'"	"50000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL704112"	"Inhibition of Janus kinase 2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1136216"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2003"	"None"	""
"CHEMBL4093318"	""	"0"	"342.40"	"0"	"3.71"	"4"	"NC(=O)c1cnn2cc(-c3ccccc3)cc2c1NCc1ccccc1"	"IC50"	"'='"	"438.0"	"nM"	"6.36"	""	""	"UO_0000065"	"18.57"	"0.33"	"2.65"	"8.78"	"False"	"CHEMBL4047228"	"Inhibition of GST-tagged JAK2 (unknown origin) using fluoresceinated peptide as substrate after 3 hrs by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4043231"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"CP-690-550"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"2.5"	"nM"	"8.60"	""	""	"UO_0000065"	"27.54"	"0.51"	"7.06"	"9.68"	"False"	"CHEMBL3106995"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3102787"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3601862"	""	"0"	"771.34"	"3"	"3.70"	"85"	"C=CC(=O)Nc1cccc(CNc2nc(Nc3cnn(CCOCCOCCOCCNC(=O)CCCC[C@@H]4SC[C@@H]5NC(=O)N[C@H]45)c3)ncc2Cl)c1"	"IC50"	"'='"	"421.0"	"nM"	"6.38"	""	""	"UO_0000065"	"8.27"	"0.16"	"2.68"	"3.27"	"False"	"CHEMBL3603319"	"Inhibition of JAK2 (unknown origin) by Z'-Lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3600288"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL3601223"	""	"0"	"508.03"	"1"	"4.37"	"9"	"C=CC(=O)Nc1cccc(CNc2nc(Nc3ccc(N4CCN(C)CC4)cc3OC)ncc2Cl)c1"	"IC50"	"'='"	"1050.0"	"nM"	"5.98"	""	""	"UO_0000065"	"11.77"	"0.23"	"1.61"	"6.32"	"False"	"CHEMBL3603319"	"Inhibition of JAK2 (unknown origin) by Z'-Lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3600288"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL3334979"	""	"0"	"396.51"	"1"	"5.50"	"1"	"COc1ccc(-c2cnc3scc(NC(=O)C4CCCCC4)c3c2)cc1OC"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4014517"	"Inhibition of human JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4014275"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2017"	"None"	""
"CHEMBL3403547"	""	"0"	"381.75"	"0"	"3.29"	"20"	"NC(=O)c1cc(-c2cc(N)ncn2)cn1-c1cc(C(F)(F)F)ccc1Cl"	"IC50"	"'='"	"71.0"	"nM"	"7.15"	""	""	"UO_0000065"	"18.73"	"0.38"	"3.86"	"7.16"	"False"	"CHEMBL3404501"	"Inhibition of recombinant epitope-tagged JAK2 (808 to 1132) (unknown origin) using LPLDKDYYVVREPGQ as substrate by beta-countiing analysis in presence of 33P-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3400063"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3403546"	""	"0"	"365.82"	"0"	"3.50"	"19"	"CCc1ccc(Cl)cc1-n1cc(-c2ncnn3cccc23)cc1C(N)=O"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	""	"UO_0000065"	"21.05"	"0.40"	"4.20"	"9.84"	"False"	"CHEMBL3404501"	"Inhibition of recombinant epitope-tagged JAK2 (808 to 1132) (unknown origin) using LPLDKDYYVVREPGQ as substrate by beta-countiing analysis in presence of 33P-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3400063"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3403545"	""	"0"	"365.82"	"0"	"3.73"	"18"	"CCc1ccc(Cl)cc1-n1cc(-c2ncnc3[nH]ccc23)cc1C(N)=O"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	""	"UO_0000065"	"24.60"	"0.47"	"5.27"	"10.05"	"False"	"CHEMBL3404501"	"Inhibition of recombinant epitope-tagged JAK2 (808 to 1132) (unknown origin) using LPLDKDYYVVREPGQ as substrate by beta-countiing analysis in presence of 33P-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3400063"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3403537"	""	"0"	"351.80"	"0"	"3.48"	"10"	"Cc1ccc(Cl)cc1-c1cn(-c2ncnc3[nH]ccc23)cc1C(N)=O"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	""	"UO_0000065"	"22.16"	"0.43"	"4.32"	"8.70"	"False"	"CHEMBL3404501"	"Inhibition of recombinant epitope-tagged JAK2 (808 to 1132) (unknown origin) using LPLDKDYYVVREPGQ as substrate by beta-countiing analysis in presence of 33P-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3400063"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3403535"	""	"0"	"327.78"	"0"	"2.58"	"8"	"Cc1ccc(Cl)cc1-c1cn(-c2cc(N)ncn2)cc1C(N)=O"	"IC50"	"'='"	"369.0"	"nM"	"6.43"	""	""	"UO_0000065"	"19.63"	"0.38"	"3.85"	"6.44"	"False"	"CHEMBL3404501"	"Inhibition of recombinant epitope-tagged JAK2 (808 to 1132) (unknown origin) using LPLDKDYYVVREPGQ as substrate by beta-countiing analysis in presence of 33P-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3400063"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3417188"	""	"0"	"501.59"	"1"	"4.62"	"33"	"O=C(CCCCC(=O)N1C/C=C/CCOc2cccc(c2)-c2ccnc(n2)Nc2cccc(c2)C1)NO"	"IC50"	"'='"	"246.0"	"nM"	"6.61"	""	""	"UO_0000065"	"13.18"	"0.24"	"1.99"	"5.66"	"False"	"CHEMBL3419812"	"Inhibition of human recombinant JAK2 using Z'LYTETry6 peptide substrate after 1 hr by microplate reader"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3414525"	"1"	"Scientific Literature"	"Eur. J. Med. Chem."	"2015"	"None"	""
"CHEMBL3417192"	""	"0"	"487.60"	"0"	"4.84"	"37"	"O=C(CCCCCN1C/C=C/COCc2cccc(c2)-c2ccnc(n2)Nc2cccc(c2)C1)NO"	"IC50"	"'='"	"594.0"	"nM"	"6.23"	""	""	"UO_0000065"	"12.77"	"0.24"	"1.39"	"6.25"	"False"	"CHEMBL3419812"	"Inhibition of human recombinant JAK2 using Z'LYTETry6 peptide substrate after 1 hr by microplate reader"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3414525"	"1"	"Scientific Literature"	"Eur. J. Med. Chem."	"2015"	"None"	""
"CHEMBL2105759"	"BARICITINIB"	"4"	"371.43"	"0"	"1.10"	"Baricitinib"	"CCS(=O)(=O)N1CC(CC#N)(n2cc(-c3ncnc4[nH]ccc34)cn2)C1"	"IC50"	"'='"	"0.8"	"nM"	"9.10"	""	""	"UO_0000065"	"24.49"	"0.48"	"8.00"	"7.55"	"False"	"CHEMBL3766653"	"Inhibition of JAK2 (unknown origin) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent substrate phosphorylation after 45 mins by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3763089"	"1"	"Scientific Literature"	"J. Med. Chem."	"2016"	"None"	""
"CHEMBL3642319"	""	"0"	"505.60"	"1"	"3.20"	"BDBM99591"	"CN1CCN(c2ccc(NC(=O)Nc3nc4cccc(-c5ccc(S(C)(=O)=O)cc5)n4n3)cc2)CC1"	"IC50"	"'='"	"1531.9"	"nM"	"5.82"	""	"216281"	"UO_0000065"	"11.50"	"0.22"	"2.61"	"5.19"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642252"	""	"0"	"210.24"	"0"	"2.47"	"BDBM99510"	"c1ccc(Nc2nc3ccccn3n2)cc1"	"IC50"	"'='"	"1089.1"	"nM"	"5.96"	""	"216201"	"UO_0000065"	"28.36"	"0.51"	"3.49"	"14.12"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3699517"	""	"0"	"334.38"	"0"	"2.85"	"BDBM147535"	"N#Cc1ccc(Nc2nn([C@H]3CCCC[C@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"36.0"	"nM"	"7.44"	""	"285465"	"UO_0000065"	"22.26"	"0.41"	"4.59"	"6.18"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4115355"	""	"0"	"465.49"	"0"	"3.08"	"BDBM237760"	"N#CCC1(COC(=O)N2CC[C@@H](n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)[C@H](C#N)C2)CC1"	"IC50"	"'='"	"426.0"	"nM"	"6.37"	""	"414864"	"UO_0000065"	"13.69"	"0.26"	"3.29"	"4.25"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3647850"	""	"0"	"377.81"	"0"	"2.74"	"BDBM147959"	"N#C[C@H]1C[C@@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)c(F)c2)n1"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	"285893"	"UO_0000065"	"20.97"	"0.42"	"5.18"	"6.77"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4115173"	""	"0"	"440.48"	"0"	"3.19"	"BDBM237730"	"CC1(COC(=O)N2CC[C@@H](n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)[C@H](C#N)C2)CC1"	"IC50"	"'='"	"955.0"	"nM"	"6.02"	""	"414834"	"UO_0000065"	"13.67"	"0.26"	"2.83"	"4.77"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4110556"	""	"0"	"458.45"	"0"	"1.95"	"BDBM237759"	"CCOC(=O)COC(=O)N1CC[C@@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@H](C#N)C1"	"IC50"	"'='"	"73.0"	"nM"	"7.14"	""	"414863"	"UO_0000065"	"15.57"	"0.30"	"5.19"	"4.68"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3702993"	""	"0"	"459.50"	"0"	"3.34"	"BDBM147703"	"C[C@H](N[C@@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(OC(F)F)nc3)n2)[C@@H](C#N)C1)C1CC1"	"IC50"	"'='"	"175.0"	"nM"	"6.76"	""	"285637"	"UO_0000065"	"14.71"	"0.28"	"3.42"	"5.16"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642299"	""	"0"	"462.58"	"0"	"3.30"	"BDBM99569"	"CN1CCN(c2cccc(Nc3nc4c(-c5ccccc5S(C)(=O)=O)cccn4n3)c2)CC1"	"IC50"	"'='"	"2496.3"	"nM"	"5.60"	""	"216259"	"UO_0000065"	"12.11"	"0.23"	"2.30"	"6.76"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703044"	""	"0"	"448.45"	"0"	"3.56"	"BDBM147754"	"N#C[C@H]1C[C@H](N2CCC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(OC(F)(F)F)cc2)n1"	"IC50"	"'='"	"40.0"	"nM"	"7.40"	""	"285688"	"UO_0000065"	"16.50"	"0.32"	"3.84"	"6.77"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652383"	""	"0"	"431.53"	"0"	"0.90"	"BDBM113195"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC(c3nnn[nH]3)C2)CC1"	"IC50"	"'='"	"9.99"	"nM"	"8.00"	""	"234638"	"UO_0000065"	"18.54"	"0.36"	"7.10"	"5.85"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3622197"	""	"0"	"433.90"	"0"	"4.21"	"39"	"NC(=O)c1cc(-c2ccc(Cl)cc2)cc2c1[nH]c1ccc(C(=O)N3CCOCC3)cc12"	"IC50"	"'='"	"2.6"	"nM"	"8.59"	""	""	"UO_0000065"	"19.79"	"0.38"	"4.38"	"9.71"	"False"	"CHEMBL3627422"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621099"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3589164"	""	"0"	"468.34"	"0"	"4.87"	"40"	"NC(=O)c1cc(-c2ccc(Cl)c(Cl)c2)cc2c1[nH]c1ccc(C(=O)N3CCOCC3)cc12"	"IC50"	"'='"	"2.4"	"nM"	"8.62"	""	""	"UO_0000065"	"18.40"	"0.37"	"3.75"	"9.75"	"False"	"CHEMBL3627422"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621099"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3589169"	""	"0"	"446.94"	"0"	"4.13"	"41"	"CN1CCN(C(=O)c2ccc3[nH]c4c(C(N)=O)cc(-c5ccc(Cl)cc5)cc4c3c2)CC1"	"IC50"	"'='"	"1.2"	"nM"	"8.92"	""	""	"UO_0000065"	"19.96"	"0.38"	"4.79"	"10.82"	"False"	"CHEMBL3627422"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621099"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3622199"	""	"0"	"442.52"	"0"	"3.48"	"43"	"COc1ccc(-c2cc(C(N)=O)c3[nH]c4cc(C(=O)N5CCN(C)CC5)ccc4c3c2)cc1"	"IC50"	"'='"	"5.5"	"nM"	"8.26"	""	""	"UO_0000065"	"18.67"	"0.34"	"4.78"	"9.01"	"False"	"CHEMBL3627422"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621099"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3622200"	""	"0"	"481.38"	"0"	"4.78"	"44"	"CN1CCN(C(=O)c2ccc3c(c2)[nH]c2c(C(N)=O)cc(-c4ccc(Cl)c(Cl)c4)cc23)CC1"	"IC50"	"'='"	"6.2"	"nM"	"8.21"	""	""	"UO_0000065"	"17.05"	"0.34"	"3.43"	"9.96"	"False"	"CHEMBL3627422"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621099"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3593766"	""	"0"	"349.44"	"0"	"2.74"	"7c"	"NC(=O)c1cnc2[nH]ccc2c1N[C@@H]1CCCN(Cc2ccccc2)C1"	"IC50"	"'='"	"430.0"	"nM"	"6.37"	""	""	"UO_0000065"	"18.22"	"0.33"	"3.63"	"7.31"	"False"	"CHEMBL3594790"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593212"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3593579"	""	"0"	"270.34"	"0"	"2.96"	"6e"	"C[C@@H]1CCCC[C@@H]1n1c(=O)[nH]c2cnc3[nH]ccc3c21"	"IC50"	"'='"	"4.4"	"nM"	"8.36"	""	""	"UO_0000065"	"30.91"	"0.57"	"5.40"	"12.57"	"False"	"CHEMBL3594576"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate and ATP incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593193"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3593585"	""	"0"	"258.28"	"0"	"1.56"	"6k"	"O=c1[nH]c2cnc3[nH]ccc3c2n1C1CCOCC1"	"IC50"	"'='"	"500.0"	"nM"	"6.30"	""	""	"UO_0000065"	"24.40"	"0.45"	"4.74"	"8.32"	"False"	"CHEMBL3594576"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate and ATP incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593193"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL495306"	""	"0"	"523.82"	"0"	"2.24"	"18"	"CN(CCO/N=C1C(=C2/C(=O)Nc3cc(Br)ccc32)/Nc2ccccc2/1)CC(O)CO.Cl"	"IC50"	"'='"	"589.0"	"nM"	"6.23"	""	""	"UO_0000065"	"12.78"	"0.27"	"3.99"	"5.85"	"False"	"CHEMBL4042012"	"Inhibition of recombinant JAK2 (unknown origin) after 120 mins in presence of [33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4041496"	"1"	"Scientific Literature"	"J Nat Prod"	"2016"	"None"	""
"CHEMBL494685"	""	"0"	"453.34"	"0"	"4.05"	"19"	"O=C1Nc2cc(Br)ccc2/C1=C1/Nc2ccccc2/C1=N\OCCN1CCCC1"	"IC50"	"'='"	"7463.0"	"nM"	"5.13"	""	""	"UO_0000065"	"11.31"	"0.24"	"1.08"	"7.77"	"False"	"CHEMBL4042012"	"Inhibition of recombinant JAK2 (unknown origin) after 120 mins in presence of [33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4041496"	"1"	"Scientific Literature"	"J Nat Prod"	"2016"	"None"	""
"CHEMBL3593773"	""	"0"	"379.42"	"0"	"1.24"	"12a"	"NC(=O)c1ccc(N2CCC(Nc3c(C(N)=O)cnc4[nH]ccc34)CC2)nc1"	"IC50"	"'='"	"41.0"	"nM"	"7.39"	""	""	"UO_0000065"	"19.47"	"0.36"	"6.15"	"5.17"	"False"	"CHEMBL3594790"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593212"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL4089118"	""	"0"	"409.37"	"0"	"2.42"	"21"	"N#C[C@H]1CCOC[C@@H]1n1cc(C(N)=O)c(Nc2ccc([C@H](O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"0.47"	"nM"	"9.33"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4032997"	"Inhibition of GST-tagged recombinant human JAK2 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 as substrate preincubated for 30 mins followed by ATP addition measured after 120 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4066193"	""	"0"	"360.35"	"0"	"1.37"	"30"	"COc1cc(Nc2nn([C@H]3COCC[C@@H]3C#N)cc2C(N)=O)cc(F)n1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4032997"	"Inhibition of GST-tagged recombinant human JAK2 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 as substrate preincubated for 30 mins followed by ATP addition measured after 120 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4079092"	""	"0"	"377.41"	"0"	"2.08"	"33"	"Cc1ncnc2ccc(Nc3nn([C@H]4COCC[C@@H]4C#N)cc3C(N)=O)cc12"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4032997"	"Inhibition of GST-tagged recombinant human JAK2 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 as substrate preincubated for 30 mins followed by ATP addition measured after 120 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4085737"	""	"0"	"370.80"	"0"	"2.35"	"27"	"N#Cc1ccc(Nc2nn([C@H]3COCC[C@@H]3C#N)cc2C(N)=O)cc1Cl"	"IC50"	"'='"	"261.0"	"nM"	"6.58"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4033007"	"Inhibition of JAK2 in EPO-stimulated human TF1 cells expressing stably integrated beta-lactamase reporter gene under control of STAT5 response elements in interferon regulatory factor 1 gene promoter by fluorescence assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4092626"	""	"0"	"373.39"	"0"	"1.43"	"29"	"CN(C)c1cc(Nc2nn([C@H]3COCC[C@@H]3C#N)cc2C(N)=O)cc(F)n1"	"IC50"	"'='"	"530.0"	"nM"	"6.28"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4033007"	"Inhibition of JAK2 in EPO-stimulated human TF1 cells expressing stably integrated beta-lactamase reporter gene under control of STAT5 response elements in interferon regulatory factor 1 gene promoter by fluorescence assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL3357978"	""	"0"	"373.44"	"0"	"1.25"	"17"	"CS(=O)(=O)N1CCC[C@H](Nc2nccnc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"36.0"	"nM"	"7.44"	""	""	"UO_0000065"	"19.93"	"0.39"	"6.19"	"6.38"	"False"	"CHEMBL3374010"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 1 hr in presence of [gamma-33P]ATP by scintillation counting analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351377"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"1a"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4124183"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate in presence of 10 uM [gamma33P]ATP by radiometric method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4118225"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4126514"	""	"0"	"405.50"	"0"	"4.70"	"17"	"CN(C)C(=O)CCc1ccc(-c2nc3cnc4[nH]ccc4c3n2C2CCCCC2)o1"	"IC50"	"'='"	"183.0"	"nM"	"6.74"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4124183"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate in presence of 10 uM [gamma33P]ATP by radiometric method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4118225"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL1980297"	"ILORASERTIB"	"2"	"488.55"	"1"	"5.18"	"2, ABT-348"	"Nc1ncc(-c2cnn(CCO)c2)c2scc(-c3ccc(NC(=O)Nc4cccc(F)c4)cc3)c12"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2024909"	"Inhibition of JAK2 by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2021801"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL3589170"	""	"0"	"495.41"	"1"	"5.17"	"7"	"CN(C)[C@H]1CCN(C(=O)c2ccc3[nH]c4c(C(N)=O)cc(-c5ccc(Cl)c(Cl)c5)cc4c3c2)C1"	"IC50"	"'='"	"3.1"	"nM"	"8.51"	""	""	"UO_0000065"	"17.17"	"0.34"	"3.34"	"10.32"	"False"	"CHEMBL3592849"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3646819"	""	"0"	"460.51"	"0"	"3.62"	"BDBM130265"	"COc1ccc(-c2cc(C(N)=O)c3[nH]c4cc(C(=O)N5CCN(C)CC5)ccc4c3c2)cc1F"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"262051"	"UO_0000065"	"17.85"	"0.33"	"4.60"	"8.97"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL4103586"	""	"0"	"356.45"	"0"	"2.65"	"20"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](CS(=O)(=O)c2ccccc2)C1"	"IC50"	"'='"	"156.0"	"nM"	"6.81"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4065613"	""	"0"	"339.42"	"0"	"0.49"	"33"	"COCCS(=O)(=O)N[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"2703.0"	"nM"	"5.57"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4085264"	""	"0"	"338.44"	"0"	"0.71"	"37"	"CCN(C)S(=O)(=O)N[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"848.0"	"nM"	"6.07"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"1"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"302.0"	"nM"	"6.52"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4089286"	""	"0"	"323.42"	"0"	"1.11"	"21"	"CCNS(=O)(=O)C[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4066876"	""	"0"	"349.46"	"0"	"1.50"	"24"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](CS(=O)(=O)NCC2CC2)C1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4085264"	""	"0"	"338.44"	"0"	"0.71"	"37"	"CCN(C)S(=O)(=O)N[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"5350.0"	"nM"	"5.27"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3646827"	""	"0"	"361.40"	"0"	"3.76"	"BDBM130273"	"CNC(=O)c1cc(-c2ccc(OC)cc2)nc2c1[nH]c1cc(OC)ccc12"	"IC50"	"'='"	"1230.0"	"nM"	"5.91"	""	"262059"	"UO_0000065"	"16.35"	"0.30"	"2.15"	"7.75"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3646833"	""	"0"	"374.40"	"0"	"3.88"	"BDBM130279"	"COC(=O)c1ccc2c(c1)[nH]c1c(C(N)=O)cc(-c3cccc(OC)c3)cc12"	"IC50"	"'='"	"310.0"	"nM"	"6.51"	""	"262065"	"UO_0000065"	"17.38"	"0.32"	"2.63"	"6.89"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3787112"	""	"0"	"349.44"	"0"	"3.04"	"2"	"Nc1ncnc2c1c(-c1cccc(O)c1)cn2[C@H]1C[C@@H](CN2CCC2)C1"	"IC50"	"'='"	"1100.0"	"nM"	"5.96"	""	""	"UO_0000065"	"17.05"	"0.31"	"2.92"	"7.43"	"False"	"CHEMBL3789994"	"Inhibition of JAK2 (unknown origin) in presence of [gamma33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3785066"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3786167"	""	"0"	"508.60"	"1"	"3.25"	"28"	"CC(=O)N1CCN([C@H]2C[C@@H](n3cc(-c4cccc(OC[C@@H]5CCCO5)c4F)c4c(N)ncnc43)C2)CC1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3789994"	"Inhibition of JAK2 (unknown origin) in presence of [gamma33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3785066"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL388978"	"STAUROSPORINE"	"0"	"466.54"	"0"	"4.35"	"Staurosporine"	"CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4c(c5c6ccccc6n2c5c31)C(=O)NC4"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	""	"UO_0000065"	"18.65"	"0.34"	"4.35"	"12.53"	"False"	"CHEMBL3804597"	"Inhibition of human recombinant JAK2 expressed in Sf21 cells assessed as reduction in Ulight-CAGAGAIETDKEYYTVKD phosphorylation pre-incubated before substrate addition and measured after 60 mins by LANCE detection method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797141"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2016"	"CHEMBL4106362"	""
"CHEMBL4112568"	""	"0"	"442.45"	"0"	"2.18"	"BDBM237772"	"N#C[C@@H]1CN(C(=O)OC2CCOC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"414876"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4106521"	""	"0"	"428.47"	"0"	"3.04"	"BDBM237777"	"CC(C)COC(=O)N1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@H](C#N)C1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"414881"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4638727"	""	"0"	"402.86"	"0"	"4.42"	"16o"	"CC(Oc1cc(-c2cnn(C3CCOC3)c2)cnc1N)c1cc(F)ccc1Cl"	"IC50"	"'='"	"27.0"	"nM"	"7.57"	""	""	"UO_0000065"	"18.79"	"0.37"	"3.15"	"10.07"	"False"	"CHEMBL4628503"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4627317"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL4634591"	""	"0"	"416.88"	"0"	"4.81"	"16m-(R)"	"C[C@@H](Oc1cc(-c2cnn(C3CCOCC3)c2)cnc1N)c1cc(F)ccc1Cl"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"20.44"	"0.40"	"3.71"	"11.34"	"False"	"CHEMBL4628503"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4627317"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL4633741"	""	"0"	"416.88"	"0"	"4.81"	"16m-(S)"	"C[C@H](Oc1cc(-c2cnn(C3CCOCC3)c2)cnc1N)c1cc(F)ccc1Cl"	"IC50"	"'='"	"1399.0"	"nM"	"5.85"	""	""	"UO_0000065"	"14.04"	"0.28"	"1.04"	"7.79"	"False"	"CHEMBL4628503"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4627317"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL4128410"	""	"0"	"403.49"	"0"	"4.78"	"8"	"CN(C)C(=O)/C=C/c1ccc(-c2nc3cnc4[nH]ccc4c3n2C2CCCCC2)o1"	"IC50"	"'='"	"113.0"	"nM"	"6.95"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4124183"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate in presence of 10 uM [gamma33P]ATP by radiometric method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4118225"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4125861"	""	"0"	"483.58"	"0"	"4.36"	"28"	"CN1CCN(C(=O)C(C#N)=Cc2ccc(-c3nc4cnc5[nH]ccc5c4n3C3CCCCC3)o2)CC1"	"IC50"	"'='"	"765.0"	"nM"	"6.12"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4124183"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate in presence of 10 uM [gamma33P]ATP by radiometric method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4118225"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3703012"	""	"0"	"433.44"	"0"	"3.08"	"BDBM147722"	"N#C[C@H]1C[C@H](N2CCC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)nc2)n1"	"IC50"	"'='"	"180.0"	"nM"	"6.75"	""	"285656"	"UO_0000065"	"15.56"	"0.30"	"3.66"	"5.98"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699522"	""	"0"	"446.43"	"0"	"3.50"	"BDBM147540"	"N#C[C@@H]1CCCC[C@H]1n1cc(C(N)=O)c(Nc2ccc3c(c2)CN(CC(F)(F)F)C3=O)n1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"285470"	"UO_0000065"	"18.81"	"0.36"	"4.90"	"7.18"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3918580"	""	"0"	"502.57"	"2"	"5.32"	"6"	"Cc1c(-c2ccc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1cnc2ccccc2c1=O"	"IC50"	"'='"	"370.0"	"nM"	"6.43"	""	""	"UO_0000065"	"12.80"	"0.23"	"1.11"	"5.64"	"False"	"CHEMBL4429363"	"Inhibition of partial length human JAK2 expressed in bacterial system"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4428066"	"1"	"Scientific Literature"	"J Med Chem"	"2016"	"None"	""
"CHEMBL3589326"	""	"0"	"418.93"	"0"	"4.49"	"18"	"CN1CCN(c2ccc3c(c2)[nH]c2c(C(N)=O)cc(-c4cccc(Cl)c4)cc23)CC1"	"IC50"	"'='"	"2.9"	"nM"	"8.54"	""	""	"UO_0000065"	"20.38"	"0.39"	"4.05"	"13.06"	"False"	"CHEMBL3592849"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3589329"	""	"0"	"438.54"	"0"	"3.73"	"21"	"CN1CCN(c2ccc3c(c2)[nH]c2c(C(N)=O)cc(-c4ccc5c(cnn5C)c4)cc23)CC1"	"IC50"	"'='"	"5.5"	"nM"	"8.26"	""	""	"UO_0000065"	"18.83"	"0.34"	"4.53"	"9.93"	"False"	"CHEMBL3592849"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3589177"	""	"0"	"456.55"	"0"	"3.87"	"14"	"COc1cccc(-c2cc(C(N)=O)c3[nH]c4cc(C(=O)N5CC[C@H](N(C)C)C5)ccc4c3c2)c1"	"IC50"	"'='"	"3.5"	"nM"	"8.46"	""	""	"UO_0000065"	"18.52"	"0.34"	"4.59"	"9.23"	"False"	"CHEMBL3592849"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL4115639"	""	"0"	"310.38"	"0"	"-0.07"	"BDBM228645"	"CNS(=O)(=O)N(C)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"98.0"	"nM"	"7.01"	""	"399535"	"UO_0000065"	"22.58"	"0.46"	"7.08"	"7.44"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4108544"	""	"0"	"486.55"	"0"	"3.20"	"BDBM228642"	"CN(c1ccc(C(=O)NC2c3ccccc3C[C@H]2O)cc1F)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.5"	"nM"	"9.30"	""	"399539"	"UO_0000065"	"19.12"	"0.35"	"6.10"	"9.55"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3955757"	""	"0"	"311.43"	"0"	"2.97"	"BDBM228709"	"C=CCN(C1CCCC1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399626"	"UO_0000065"	"32.94"	"0.61"	"7.29"	"21.35"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4115095"	""	"0"	"450.42"	"0"	"2.70"	"BDBM237768"	"N#C[C@@H]1CN(C(=O)OC(CF)CF)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"1337.0"	"nM"	"5.87"	""	"414872"	"UO_0000065"	"13.04"	"0.25"	"3.17"	"4.65"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4238926"	""	"0"	"326.40"	"0"	"2.01"	"5"	"NC(=O)c1cnc2[nH]ccc2c1NC1C2CC3CC1CC(O)(C3)C2"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	""	""	"25.43"	"0.47"	"6.29"	"7.98"	"False"	"CHEMBL4714267"	"Inhibition of human JAK2 using Biotin-Lyn-Substrate-2 in presence of 1 mM ATP by phosphotyrosine-specific ELISA"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706695"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2021"	"None"	""
"CHEMBL3651602"	""	"0"	"418.50"	"0"	"2.44"	"BDBM103734"	"NC(=O)C1CCN(Cc2ccc(-c3cccc4nc(NC(=O)C5CC5)nn34)cc2)CC1"	"IC50"	"'='"	"7731.0"	"nM"	"5.11"	""	"221719"	"UO_0000065"	"12.21"	"0.23"	"2.67"	"4.84"	"False"	"CHEMBL3707887"	"Inhibition Assay: In vitro inhibition assay using various enzyme."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638964"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3639498"	""	"0"	"366.38"	"0"	"2.93"	"BDBM153171"	"C=CC(=O)Nc1cc(-c2ncnc3[nH]cc(C(=O)OCC)c23)ccc1OC"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294119"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645103"	""	"0"	"431.52"	"0"	"3.98"	"BDBM99877"	"CN1CCN(c2cccc(Nc3nc4c(NCc5ccc(F)cc5)cccn4n3)c2)CC1"	"IC50"	"'='"	"1434.69"	"nM"	"5.84"	""	"216545"	"UO_0000065"	"13.54"	"0.25"	"1.86"	"9.62"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3651603"	""	"0"	"418.50"	"0"	"2.41"	"BDBM103735"	"CC(=O)N1CCN(Cc2ccc(-c3cccc4nc(NC(=O)C5CC5)nn34)cc2)CC1"	"IC50"	"'='"	"848.7"	"nM"	"6.07"	""	"221721"	"UO_0000065"	"14.51"	"0.27"	"3.66"	"7.33"	"False"	"CHEMBL3707887"	"Inhibition Assay: In vitro inhibition assay using various enzyme."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638964"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703080"	""	"0"	"514.51"	"1"	"2.91"	"BDBM147793"	"N#C[C@H]1C[C@H](N2CC(F)C2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"285727"	"UO_0000065"	"15.98"	"0.32"	"5.31"	"6.13"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703056"	""	"0"	"462.48"	"0"	"3.26"	"BDBM147766"	"N#C[C@H]1C[C@H](N2CCC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc([C@@H](O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	"285700"	"UO_0000065"	"16.80"	"0.32"	"4.51"	"6.46"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702891"	""	"0"	"368.40"	"0"	"2.16"	"BDBM147590"	"COC(=O)c1ccc(Nc2nn([C@H]3CCCC[C@@H]3C#N)cc2C(N)=O)cn1"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	"285520"	"UO_0000065"	"21.41"	"0.40"	"5.73"	"5.80"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699499"	""	"0"	"457.43"	"0"	"2.24"	"BDBM147516"	"N#C[C@H]1C[C@@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"285446"	"UO_0000065"	"17.59"	"0.35"	"5.81"	"5.32"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647886"	""	"0"	"442.91"	"0"	"2.37"	"BDBM147998"	"N#C[C@@H]1C[C@H](C(=O)NC2COC2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"38.0"	"nM"	"7.42"	""	"285933"	"UO_0000065"	"16.75"	"0.33"	"5.05"	"5.49"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647758"	""	"0"	"524.57"	"1"	"3.64"	"BDBM147861"	"C[C@H](N[C@@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)(F)F)cc3)n2)[C@@H](C#N)C1)C1CC1"	"IC50"	"'='"	"83.0"	"nM"	"7.08"	""	"285795"	"UO_0000065"	"13.50"	"0.27"	"3.44"	"4.96"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699552"	""	"0"	"361.81"	"0"	"3.77"	"BDBM147570"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2cc(F)cc(Cl)c2)n1"	"IC50"	"'='"	"42.0"	"nM"	"7.38"	""	"285500"	"UO_0000065"	"20.39"	"0.40"	"3.61"	"7.63"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4162314"	""	"0"	"486.57"	"0"	"2.75"	"6"	"CN1CCN(c2cc(Nc3ncc(F)c(Nc4cccc(CO)c4)n3)cc(S(C)(=O)=O)c2)CC1"	"IC50"	"'='"	"6410.0"	"nM"	"5.19"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4145184"	"Inhibition of recombinant human JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate after 10 mins by caliper assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4138312"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4761780"	""	"0"	"457.49"	"0"	"4.22"	"10f"	"O=C(Nc1c[nH]nc1-c1nc(-c2ccc(CN3CCCC3)cc2)c[nH]1)c1ccc([N+](=O)[O-])cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4711870"	"Inhibition of JAK2 (unknown origin) incubated for 40 mins in presence of ATP by Kinase-glo luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706620"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2021"	"None"	"TIME = 0.6667 hr"
"CHEMBL4750823"	""	"0"	"456.55"	"0"	"4.71"	"10g"	"COc1ccc(C(=O)Nc2c[nH]nc2-c2nc(-c3ccc(CN4CCCCC4)cc3)c[nH]2)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4711870"	"Inhibition of JAK2 (unknown origin) incubated for 40 mins in presence of ATP by Kinase-glo luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706620"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2021"	"None"	"TIME = 0.6667 hr"
"CHEMBL4794655"	""	"0"	"450.93"	"0"	"3.79"	"10j"	"Cc1nc(Cl)cc(Nc2c[nH]nc2-c2nc(-c3ccc(CN4CCOCC4)cc3)c[nH]2)n1"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	""	""	"17.96"	"0.35"	"4.31"	"7.52"	"False"	"CHEMBL4711870"	"Inhibition of JAK2 (unknown origin) incubated for 40 mins in presence of ATP by Kinase-glo luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706620"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2021"	"None"	"TIME = 0.6667 hr"
"CHEMBL388978"	"STAUROSPORINE"	"0"	"466.54"	"0"	"4.35"	"BDBM2579"	"CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4c(c5c6ccccc6n2c5c31)C(=O)NC4"	"IC50"	"'<'"	"1.0"	"nM"	""	""	"348445"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3887684"	"Biochemical Inhibition Assay: 1H-pyrrolo[2,3-b]pyridine series of compounds and analogues in Table 3B were synthesized and tested in 10-dose IC50 mode with 3 fold serial dilutions starting at 100 μM. The reactions were carried out at 10 μM ATP for JAK3 and ITK. The compounds 5, 7, 8, 16, 19-33, 48-51, 57-60, 66, 75, 77-92 and 133-153 exhibited biochemical IC50=between 0.1 to 1 μM against JAK3 and ITK respectively."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886406"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3919033"	""	"0"	"371.42"	"1"	"5.47"	"BDBM195905"	"C=CC(=O)Nc1cccc(-c2cnc3[nH]cc(-c4cccc(C)c4F)c3c2)c1"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	"348611"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3887689"	"Biochemical Inhibition Assay: 1H-pyrrolo[2,3-b]pyridine, 1H-pyrazolo[3,4-b]pyridine and 5H-pyrrolo[2,3-b]pyrazine series of compounds exhibited over >100 fold selective against Janus and TEC family of kinases except for the BMX and TXK it had activity of 30 and 45 nM respectively."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886406"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3959421"	""	"0"	"320.36"	"0"	"1.33"	"BDBM228643"	"CN(c1ncc(C#N)cn1)[C@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"55.0"	"nM"	"7.26"	""	"399537"	"UO_0000065"	"22.66"	"0.41"	"5.93"	"7.44"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4112584"	""	"0"	"428.47"	"0"	"3.19"	"BDBM237716"	"CC(C)(C)OC(=O)N1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@H](C#N)C1"	"IC50"	"'='"	"841.0"	"nM"	"6.08"	""	"414820"	"UO_0000065"	"14.18"	"0.27"	"2.89"	"4.81"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4110058"	""	"0"	"328.35"	"0"	"1.54"	"BDBM237720"	"N#C[C@@H]1CNCCC1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"628.0"	"nM"	"6.20"	""	"414824"	"UO_0000065"	"18.89"	"0.35"	"4.66"	"5.70"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3582441"	""	"0"	"501.57"	"1"	"3.48"	"16"	"O=C(O)CN1CCN(c2cc(-c3cnc4ccc(N5CCC[C@@H]5c5cccc(F)c5)nn34)ccn2)CC1"	"IC50"	"'='"	"2700.0"	"nM"	"5.57"	""	""	"UO_0000065"	"11.10"	"0.21"	"2.09"	"6.18"	"False"	"CHEMBL3583131"	"Inhibition of Tel-fused JAK2 (unknown origin) expressed in mouse BA/F3 cells after 48 hrs by luciferase reporter gene assay in absence of recombinant mouse IL3"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3580662"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"CHEMBL3307634"	""
"CHEMBL3622957"	""	"0"	"451.96"	"0"	"3.73"	"16g"	"Cc1nn(-c2ccnc(Nc3ccc4c(c3)c(Cl)c(C)n4C)n2)cc1CN1CC[C@@H](O)C1"	"IC50"	"'='"	"162400.0"	"nM"	""	"Outside typical range"	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3627021"	"Inhibition of human JAK2 pre-incubated for 30 mins at room temperature before substrate addition and measured 1 hr after substrate addition by cell free kinase assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621069"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL4115659"	""	"0"	"441.47"	"0"	"1.88"	"BDBM237729"	"N#C[C@@H]1CN(C(=O)OCC2(N)CC2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"703.0"	"nM"	"6.15"	""	"414833"	"UO_0000065"	"13.94"	"0.26"	"4.27"	"4.04"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4108433"	""	"0"	"440.48"	"0"	"3.19"	"BDBM237735"	"N#C[C@@H]1CN(C(=O)OCCC2CC2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"430.0"	"nM"	"6.37"	""	"414839"	"UO_0000065"	"14.45"	"0.27"	"3.18"	"5.04"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4113767"	""	"0"	"436.39"	"0"	"2.65"	"BDBM237737"	"N#C[C@@H]1CN(C(=O)OCC(F)F)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"132.0"	"nM"	"6.88"	""	"414841"	"UO_0000065"	"15.76"	"0.30"	"4.23"	"5.45"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3234888"	""	"0"	"320.38"	"0"	"3.52"	"8"	"N#Cc1ccc(Nc2sc(-c3ccccc3)cc2C(N)=O)nc1"	"IC50"	"'='"	"146.0"	"nM"	"6.84"	""	""	"UO_0000065"	"21.34"	"0.41"	"3.32"	"7.45"	"False"	"CHEMBL3239499"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3232939"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL4109360"	""	"0"	"442.50"	"0"	"3.43"	"BDBM237738"	"CC(C)(C)COC(=O)N1CC[C@@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@H](C#N)C1"	"IC50"	"'='"	"1460.0"	"nM"	"5.84"	""	"414843"	"UO_0000065"	"13.19"	"0.25"	"2.41"	"4.62"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3917864"	""	"0"	"453.48"	"0"	"2.94"	"BDBM237790"	"CC(C)(C#N)COC(=O)N1CC[C@@H](C#N)[C@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)C1"	"IC50"	"'='"	"41.0"	"nM"	"7.39"	""	"414894"	"UO_0000065"	"16.29"	"0.31"	"4.45"	"4.92"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4084598"	""	"0"	"371.42"	"0"	"1.93"	"13c"	"C=CS(=O)(=O)Nc1cccc(CNc2c(C(N)=O)cnn3cccc23)c1"	"IC50"	"'='"	"1270.0"	"nM"	"5.90"	""	""	"UO_0000065"	"15.87"	"0.31"	"3.97"	"4.97"	"False"	"CHEMBL4047228"	"Inhibition of GST-tagged JAK2 (unknown origin) using fluoresceinated peptide as substrate after 3 hrs by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4043231"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"1"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"77.0"	"nM"	"7.11"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"Tofacitinib"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"14.3"	"nM"	"7.84"	""	""	"UO_0000065"	"25.11"	"0.47"	"6.30"	"8.82"	"False"	"CHEMBL4610789"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using Ulight-Poly GT as substrate incubated for 2 hrs by Lanthascreen TR-FRET assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610007"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2020"	"None"	""
"CHEMBL1650951"	""	"0"	"526.52"	"1"	"3.17"	"1"	"CC(C)(O)C(=O)N1CCN(c2ccc(C(F)(F)F)c(C3=C(c4c[nH]c5ccccc45)C(=O)NC3=O)c2)CC1"	"IC50"	"'='"	"2550.0"	"nM"	"5.59"	""	""	"UO_0000065"	"10.62"	"0.20"	"2.42"	"5.29"	"False"	"CHEMBL1657171"	"Inhibition of GST-tagged Jak2 expressed in insect cells using 20 uM ATP"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649080"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL1650952"	""	"0"	"374.29"	"0"	"3.89"	"5"	"O=C1NC(=O)C(c2c[nH]c3ccccc23)=C1c1cc(F)ccc1C(F)(F)F"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1657171"	"Inhibition of GST-tagged Jak2 expressed in insect cells using 20 uM ATP"	"B"	"BAO_0000219"	"cell-based format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649080"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL3914503"	""	"0"	"356.38"	"0"	"4.49"	"9"	"COc1cc(O)ccc1-c1ccc2c(-c3nc4ccccc4[nH]3)n[nH]c2c1"	"IC50"	"'='"	"5.4"	"nM"	"8.27"	""	""	"UO_0000065"	"23.20"	"0.42"	"3.78"	"9.52"	"False"	"CHEMBL4003453"	"Inhibition of GST tagged human recombinant JAK2 catalytic domain expressed in baculovirus using peptide substrate preincubated for 60 mins followed by substrate addition and measured after 60 mins by microfluidic assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4002590"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4074855"	""	"0"	"309.37"	"0"	"3.20"	"15"	"CCc1cc(O)ccc1-c1ccc2c(C(=O)N(C)C)n[nH]c2c1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4003453"	"Inhibition of GST tagged human recombinant JAK2 catalytic domain expressed in baculovirus using peptide substrate preincubated for 60 mins followed by substrate addition and measured after 60 mins by microfluidic assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4002590"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL2414540"	""	"0"	"388.43"	"0"	"4.15"	"36"	"O=C(O)c1ccc(Nc2nc3c(-c4cnn(C5CCCC5)c4)cccn3n2)cc1"	"IC50"	"'='"	"23.7"	"nM"	"7.62"	""	""	"UO_0000065"	"19.63"	"0.36"	"3.48"	"7.83"	"False"	"CHEMBL2415128"	"Inhibition of JAK2 in human SET2 cells assessed as reduction of phosphorylated STAT5 level"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2412966"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL4088027"	""	"0"	"403.45"	"0"	"1.95"	"13e"	"CN(C)/C=C(/C#N)C(=O)Nc1cccc(CNc2c(C(N)=O)cnn3cccc23)c1"	"IC50"	"'>'"	"2000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4047228"	"Inhibition of GST-tagged JAK2 (unknown origin) using fluoresceinated peptide as substrate after 3 hrs by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4043231"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4103698"	""	"0"	"375.43"	"0"	"2.04"	"9"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)c2ccc(F)cc2)C1"	"IC50"	"'='"	"6800.0"	"nM"	"5.17"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4093643"	""	"0"	"351.48"	"0"	"1.89"	"23"	"CCCCNS(=O)(=O)C[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4068319"	""	"0"	"349.46"	"0"	"1.64"	"30"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)CC2CCC2)C1"	"IC50"	"'='"	"538.0"	"nM"	"6.27"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4099048"	""	"0"	"348.43"	"0"	"1.15"	"35"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)CCCC#N)C1"	"IC50"	"'='"	"939.0"	"nM"	"6.03"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL2105759"	"BARICITINIB"	"4"	"371.43"	"0"	"1.10"	"2"	"CCS(=O)(=O)N1CC(CC#N)(n2cc(-c3ncnc4[nH]ccc34)cn2)C1"	"IC50"	"'='"	"88.0"	"nM"	"7.06"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4168707"	""	"0"	"590.64"	"1"	"4.11"	"12b"	"N#CCNC(=O)c1ccc(-c2ccnc(Nc3ccc(N4CCC(C(=O)Nc5ccc(C(=O)NO)cc5)CC4)cc3)n2)cc1"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	""	"UO_0000065"	"13.20"	"0.24"	"3.69"	"4.52"	"False"	"CHEMBL4150584"	"Inhibition of JAK2 (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition and measured after 25 mins in presence of ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4145634"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3644620"	""	"0"	"566.64"	"2"	"5.01"	"2; PF-06263276"	"CCc1cc(O)c(F)cc1-c1ccc2c(-c3nc4c([nH]3)CCN(C(=O)c3cnc(N5CCCCC5)cn3)C4)n[nH]c2c1"	"IC50"	"'='"	"5200.0"	"nM"	"5.28"	""	""	"UO_0000065"	"9.33"	"0.17"	"0.27"	"4.16"	"False"	"CHEMBL4003468"	"Inhibition of JAK2 homodimer in human whole blood assessed as inhibition of GM-CSF induced STAT5 phosphorylation preincubated for 45 mins followed by GM-CSF addition and measured after 20 mins by flow cytometric analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4002590"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4175654"	""	"0"	"484.53"	"0"	"4.73"	"19"	"Cc1cnc(Nc2cc(N3C[C@@H]4C[C@H]3CN4C)cc(C(F)F)c2F)nc1Nc1cccc(CO)c1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4145184"	"Inhibition of recombinant human JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate after 10 mins by caliper assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4138312"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3646814"	""	"0"	"467.36"	"0"	"4.49"	"BDBM130259"	"NC(=O)c1cc(-c2ccc(Cl)c(Cl)c2)cc2c1[nH]c1ccc(C(=O)N[C@@H]3CCNC3)cc12"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"262045"	"UO_0000065"	"17.59"	"0.35"	"3.73"	"8.22"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3622200"	""	"0"	"481.38"	"0"	"4.78"	"BDBM130262"	"CN1CCN(C(=O)c2ccc3c(c2)[nH]c2c(C(N)=O)cc(-c4ccc(Cl)c(Cl)c4)cc23)CC1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"262048"	"UO_0000065"	"17.08"	"0.34"	"3.44"	"9.97"	"True"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3646824"	""	"0"	"500.60"	"1"	"3.89"	"BDBM130270"	"COCCCN1CCN(C(=O)c2ccc3c(c2)[nH]c2c(C(N)=O)cc(-c4cccc(OC)c4)cc23)CC1"	"IC50"	"'<'"	"1.0"	"nM"	""	""	"262056"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676075"	""	"0"	"415.43"	"0"	"1.04"	"BDBM127836"	"NC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)cc(OCC(O)CO)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258504"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676092"	""	"0"	"410.45"	"0"	"2.19"	"BDBM127857"	"Cn1cc(F)cc([C@H]2CCCN2c2ccn3ncc(C(=O)NC4CCC4)c3n2)c1=O"	"IC50"	"'='"	"665.6"	"nM"	"6.18"	""	"258522"	"UO_0000065"	"15.05"	"0.28"	"3.99"	"7.31"	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676038"	""	"0"	"427.46"	"0"	"2.99"	"BDBM127796"	"O=C(N[C@H]1CC[C@H](O)C1)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'='"	"759.0"	"nM"	"6.12"	""	"258465"	"UO_0000065"	"14.32"	"0.27"	"3.13"	"7.39"	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675972"	""	"0"	"420.85"	"0"	"2.91"	"BDBM127724"	"O=C(NCC(F)CCl)c1cnn2ccc(N3CCC[C@@H]3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258398"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675981"	""	"0"	"396.43"	"0"	"1.86"	"BDBM127734"	"O=C(NC1(CO)CC1)c1cnn2ccc(N3CCCC3c3cncc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258408"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676003"	""	"0"	"422.39"	"0"	"3.29"	"BDBM127756"	"C[C@@H](NC(=O)c1cnn2ccc(N3CCCC3c3cncc(F)c3)nc12)C(F)(F)F"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258430"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL4448494"	""	"0"	"506.61"	"1"	"4.72"	"3c"	"Cc1nc2c(F)cc(-c3nc(Nc4ccc5c(n4)CCN(CCN(C)C)C5)ncc3F)cc2n1C(C)C"	"IC50"	"'='"	"170.0"	"nM"	"6.77"	""	""	"UO_0000065"	"13.36"	"0.25"	"2.05"	"9.03"	"False"	"CHEMBL4305822"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4304763"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2019"	"None"	""
"CHEMBL2414537"	""	"0"	"390.45"	"0"	"3.70"	"33"	"COc1ccc(-c2cccn3nc(Nc4cnn(C5CCOCC5)c4)nc23)cc1"	"IC50"	"'='"	"86.9"	"nM"	"7.06"	""	""	"UO_0000065"	"18.08"	"0.33"	"3.36"	"8.99"	"False"	"CHEMBL2415128"	"Inhibition of JAK2 in human SET2 cells assessed as reduction of phosphorylated STAT5 level"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2412966"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL4167685"	""	"0"	"601.69"	"1"	"4.23"	"20b"	"CS(=O)(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCC(C(=O)Nc5ccc(C(=O)NO)cc5)CC4)cc3)n2)cc1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	""	"UO_0000065"	"14.46"	"0.28"	"4.47"	"5.25"	"False"	"CHEMBL4150584"	"Inhibition of JAK2 (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition and measured after 25 mins in presence of ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4145634"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4749677"	""	"0"	"407.52"	"0"	"3.26"	"18e"	"CNC(=O)c1cnc2[nH]ccc2c1NCC1CCN(Cc2ccc(OC)cc2)CC1"	"IC50"	"'='"	"1080.0"	"nM"	"5.97"	""	""	""	"14.64"	"0.27"	"2.71"	"7.25"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL4744048"	""	"0"	"377.49"	"0"	"3.39"	"31a"	"CNC(=O)c1cnc2[nH]ccc2c1N[C@@H]1CCN(Cc2ccccc2)[C@@H](C)C1"	"IC50"	"'='"	"179.0"	"nM"	"6.75"	""	""	""	"17.87"	"0.33"	"3.36"	"9.24"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL4792719"	""	"0"	"419.53"	"0"	"3.54"	"17j"	"COc1cccc(CN2CCC(Nc3c(C(=O)NC4CC4)cnc4[nH]ccc34)CC2)c1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	""	""	""	""	""	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL4777577"	""	"0"	"411.94"	"0"	"4.04"	"31c"	"CNC(=O)c1cnc2[nH]ccc2c1N[C@@H]1CCN(Cc2ccc(Cl)cc2)[C@@H](C)C1"	"IC50"	"'='"	"245.0"	"nM"	"6.61"	""	""	""	"16.05"	"0.31"	"2.57"	"9.05"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL4786466"	""	"0"	"419.53"	"0"	"3.54"	"20e"	"CNC(=O)c1cnc2[nH]ccc2c1NC1CC2CCC(C1)N2Cc1ccc(OC)cc1"	"IC50"	"'='"	"162.0"	"nM"	"6.79"	""	""	""	"16.19"	"0.30"	"3.25"	"8.25"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL2012519"	""	"0"	"364.39"	"0"	"1.52"	"L-783277"	"COc1cc(O)c2c(c1)CCC[C@H](O)[C@H](O)C(=O)/C=C\C[C@H](C)OC2=O"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1656532"	"Inhibition of JAK2 by TR-FRET based LanthaScreen assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649097"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL3335678"	""	"0"	"342.33"	"0"	"2.11"	"rac-5"	"O=C(Nc1cnc2[nH]ccc2n1)NC1CCCN(CC(F)(F)F)C1"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	""	"UO_0000065"	"23.82"	"0.46"	"6.04"	"9.49"	"False"	"CHEMBL3374010"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 1 hr in presence of [gamma-33P]ATP by scintillation counting analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351377"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL2035182"	""	"0"	"452.58"	"0"	"4.49"	"14i, 95:5 trans/Cis mixture"	"COCCOc1ccc2cc1CN(C)C/C=C/COCc1ccc(s1)-c1ccnc(n1)N2"	"IC50"	"'='"	"170.0"	"nM"	"6.77"	""	""	"UO_0000065"	"14.96"	"0.29"	"2.28"	"9.85"	"False"	"CHEMBL2040119"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2034857"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2151321"	""	"0"	"381.42"	"0"	"3.64"	"2c"	"CC(C)Oc1cc(-n2cnc3ccc(N[C@@H](C)c4ccc(F)cn4)nc32)n[nH]1"	"IC50"	"'='"	"68.3"	"nM"	"7.17"	""	""	"UO_0000065"	"18.79"	"0.35"	"3.53"	"7.66"	"False"	"CHEMBL2154716"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2150905"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL3301607"	"FILGOTINIB"	"4"	"425.51"	"0"	"1.98"	"65, GLPG0634"	"O=C(Nc1nc2cccc(-c3ccc(CN4CCS(=O)(=O)CC4)cc3)n2n1)C1CC1"	"IC50"	"'='"	"3524.0"	"nM"	"5.45"	""	""	"UO_0000065"	"12.82"	"0.25"	"3.47"	"5.64"	"False"	"CHEMBL3382731"	"Inhibition of JAK2 in IL3-induced human TF1 cells assessed as pSTAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351789"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"CHEMBL3307972"	""
"CHEMBL3301607"	"FILGOTINIB"	"4"	"425.51"	"0"	"1.98"	"65, GLPG0634"	"O=C(Nc1nc2cccc(-c3ccc(CN4CCS(=O)(=O)CC4)cc3)n2n1)C1CC1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3382734"	"Inhibition of JAK2 in PRL-induced human 22Rv1 cells assessed as pSTAT5"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"CWR22R"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351789"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"CHEMBL3308004"	""
"CHEMBL3360353"	""	"0"	"377.45"	"0"	"2.58"	"60"	"O=C(Nc1nc2cccc(-c3ccc(CN4CCOCC4)cc3)n2n1)C1CC1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3382736"	"Inhibition of JAK2 in human whole blood assessed as inhibition of GM-CSF-induced pSTAT5"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"CHEMBL3638178"	"Blood"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351789"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL3702902"	""	"0"	"465.54"	"0"	"3.18"	"BDBM147601"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)Nc3ccncc3)cc2)n1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"285531"	"UO_0000065"	"18.69"	"0.36"	"5.52"	"5.58"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652285"	""	"0"	"423.54"	"0"	"0.71"	"BDBM113094"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC[C@@H](O)[C@H](O)C2)CC1"	"IC50"	"'='"	"11.8"	"nM"	"7.93"	""	"234538"	"UO_0000065"	"18.72"	"0.37"	"7.22"	"6.46"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3699516"	""	"0"	"327.36"	"0"	"3.12"	"BDBM147534"	"N#C[C@@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"76.0"	"nM"	"7.12"	""	"285464"	"UO_0000065"	"21.75"	"0.41"	"4.00"	"7.36"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL1650545"	""	"0"	"452.92"	"0"	"3.47"	"18"	"Cc1cn2c(-c3cn[nH]c3)cnc2c(Nc2cc(CN3CCC(F)(F)C3)ns2)n1.Cl"	"IC50"	"'>'"	"100.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1656192"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649074"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL3699501"	""	"0"	"344.35"	"0"	"1.49"	"BDBM147518"	"N#C[C@H]1C[C@H](O)CCC1n1cc(C(N)=O)c(Nc2ccnc(F)c2)n1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	"285589"	"UO_0000065"	"23.11"	"0.43"	"6.47"	"6.13"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652326"	""	"0"	"448.59"	"0"	"1.74"	"BDBM113136"	"CNC(=O)C1CCN(S(=O)(=O)C[C@H]2CC[C@H](N(C)c3ncnc4[nH]ccc34)CC2)CC1"	"IC50"	"'='"	"44.9"	"nM"	"7.35"	""	"234579"	"UO_0000065"	"16.38"	"0.32"	"5.61"	"6.60"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3642349"	""	"0"	"492.61"	"0"	"4.09"	"BDBM99625"	"CS(=O)(=O)c1ccccc1Nc1cccn2nc(Nc3ccc(OCCN4CCCC4)cc3)nc12"	"IC50"	"'='"	"14.35"	"nM"	"7.84"	""	"216315"	"UO_0000065"	"15.92"	"0.31"	"3.75"	"7.78"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL98"	"VORINOSTAT"	"4"	"264.32"	"0"	"2.47"	"SAHA"	"O=C(CCCCCCC(=O)Nc1ccccc1)NO"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3419812"	"Inhibition of human recombinant JAK2 using Z'LYTETry6 peptide substrate after 1 hr by microplate reader"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3414525"	"1"	"Scientific Literature"	"Eur. J. Med. Chem."	"2015"	"None"	""
"CHEMBL4778011"	""	"0"	"428.50"	"0"	"3.55"	"10a"	"O=C(Nc1c[nH]nc1-c1nc(-c2ccc(CN3CCOCC3)cc2)c[nH]1)c1ccccc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4711870"	"Inhibition of JAK2 (unknown origin) incubated for 40 mins in presence of ATP by Kinase-glo luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706620"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2021"	"None"	"TIME = 0.6667 hr"
"CHEMBL3393341"	""	"0"	"317.40"	"0"	"3.73"	"7"	"C[C@H]1CCCN(c2ncnc3[nH]cc(-c4cccc(C#N)c4)c23)C1"	"IC50"	"'='"	"575.0"	"nM"	"6.24"	""	""	"UO_0000065"	"19.66"	"0.36"	"2.51"	"9.10"	"False"	"CHEMBL3396723"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3393009"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL3354189"	""	"0"	"392.51"	"0"	"4.30"	"8"	"COC1CCN(c2nccc(Nc3cc4c(ccn4C4CCCC4)cn3)n2)CC1"	"IC50"	"'='"	"225.0"	"nM"	"6.65"	""	""	"UO_0000065"	"16.94"	"0.31"	"2.35"	"9.76"	"False"	"CHEMBL3375809"	"Inhibition of Jak2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351701"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL3354191"	""	"0"	"382.47"	"0"	"2.74"	"10"	"COC1CCN(c2nccc(Nc3cc4c(cn3)c(N)nn4C(C)C)n2)CC1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3375809"	"Inhibition of Jak2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351701"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL3655096"	""	"0"	"376.49"	"0"	"0.69"	"BDBM159763"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)C2CN(C3CC3)C2)C1"	"IC50"	"'='"	"597.0"	"nM"	"6.22"	""	"302573"	"UO_0000065"	"16.53"	"0.33"	"5.53"	"6.61"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3403552"	""	"0"	"351.80"	"0"	"3.68"	"25"	"Cc1ccc(Cl)cc1-c1cc(-c2ncnc3[nH]ccc23)[nH]c1C(N)=O"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	""	"UO_0000065"	"22.87"	"0.44"	"4.37"	"8.01"	"False"	"CHEMBL3404501"	"Inhibition of recombinant epitope-tagged JAK2 (808 to 1132) (unknown origin) using LPLDKDYYVVREPGQ as substrate by beta-countiing analysis in presence of 33P-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3400063"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3403544"	""	"0"	"355.83"	"0"	"3.29"	"17"	"CCc1ccc(Cl)cc1-n1cc(-c2cc(NC)ncn2)cc1C(N)=O"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	""	"UO_0000065"	"22.26"	"0.43"	"4.63"	"9.23"	"False"	"CHEMBL3404501"	"Inhibition of recombinant epitope-tagged JAK2 (808 to 1132) (unknown origin) using LPLDKDYYVVREPGQ as substrate by beta-countiing analysis in presence of 33P-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3400063"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3403539"	""	"0"	"327.77"	"0"	"2.58"	"12"	"Cc1ccc(Cl)cc1-n1cc(-c2cc(N)ncn2)cc1C(N)=O"	"IC50"	"'='"	"73.0"	"nM"	"7.14"	""	""	"UO_0000065"	"21.77"	"0.42"	"4.56"	"7.15"	"False"	"CHEMBL3404501"	"Inhibition of recombinant epitope-tagged JAK2 (808 to 1132) (unknown origin) using LPLDKDYYVVREPGQ as substrate by beta-countiing analysis in presence of 33P-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3400063"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3403534"	""	"0"	"327.77"	"0"	"2.58"	"7"	"Cc1ccc(Cl)cc1-n1cc(-c2ccnc(N)n2)cc1C(N)=O"	"IC50"	"'='"	"216.0"	"nM"	"6.67"	""	""	"UO_0000065"	"20.34"	"0.40"	"4.09"	"6.68"	"False"	"CHEMBL3404501"	"Inhibition of recombinant epitope-tagged JAK2 (808 to 1132) (unknown origin) using LPLDKDYYVVREPGQ as substrate by beta-countiing analysis in presence of 33P-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3400063"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3658097"	""	"0"	"505.50"	"2"	"5.15"	"BDBM148369"	"Cc1ccc(NC(=O)c2cccc(C(F)(F)F)c2)cc1N1CCc2nc(Nc3cncnc3)ncc2C1"	"IC50"	"'='"	"19.0"	"nM"	"7.72"	""	"286783"	"UO_0000065"	"15.27"	"0.29"	"2.57"	"8.05"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642407"	""	"0"	"563.68"	"1"	"4.63"	"BDBM99685"	"CC(C)(C)OC(=O)N1CC[C@@H](c2cccc(Nc3nc4c(-c5ccc(S(C)(=O)=O)cc5)cccn4n3)c2)[C@@H](O)C1"	"IC50"	"'='"	"1.35"	"nM"	"8.87"	""	"216374"	"UO_0000065"	"15.74"	"0.30"	"4.24"	"7.03"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3335679"	""	"0"	"338.39"	"0"	"0.50"	"6"	"CS(=O)(=O)N1CCC(NC(=O)Nc2cnc3[nH]ccc3n2)CC1"	"IC50"	"'='"	"234.0"	"nM"	"6.63"	""	""	"UO_0000065"	"19.60"	"0.39"	"6.13"	"5.52"	"False"	"CHEMBL3374010"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 1 hr in presence of [gamma-33P]ATP by scintillation counting analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351377"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3335680"	""	"0"	"302.34"	"0"	"1.09"	"rac-7"	"CC(=O)N1CCCC(NC(=O)Nc2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"92.0"	"nM"	"7.04"	""	""	"UO_0000065"	"23.27"	"0.44"	"5.95"	"6.83"	"False"	"CHEMBL3374010"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 1 hr in presence of [gamma-33P]ATP by scintillation counting analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351377"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL4127590"	""	"0"	"359.43"	"1"	"5.13"	"20"	"N#CCCc1ccc(-c2nc3cnc4[nH]ccc4c3n2C2CCCCC2)o1"	"IC50"	"'='"	"48.0"	"nM"	"7.32"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4124183"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate in presence of 10 uM [gamma33P]ATP by radiometric method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4118225"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3798740"	""	"0"	"414.47"	"0"	"4.34"	"12b"	"CCC(=O)Nc1ccc(-c2ncnc3c2cc(C(=O)OCc2ccccc2)n3C)cc1"	"IC50"	"'='"	"531.0"	"nM"	"6.28"	""	""	"UO_0000065"	"15.14"	"0.28"	"1.93"	"7.29"	"False"	"CHEMBL3802363"	"Inhibition of recombinant human GST-tagged JAK2 expressed in baculovirus expression system using Z'-LYTE Try6 peptide as substrate incubated for 1 hr by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3799168"	""	"0"	"468.56"	"0"	"3.71"	"15f"	"Cn1c(C(=O)NCCN2CCCC2)cc2c(-c3ccc(NC(=O)c4ccccc4)cc3)ncnc21"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL3802364"	"Inhibition of JAK2 in GMCSF-stimulated human TF1 cells assessed as suppression of STAT5 phosphorylation preincubated for 2 hrs followed by GMCSF stimulation for 50 mins by FACS reader analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"CHEMBL3307972"	""
"CHEMBL3799630"	""	"0"	"450.54"	"0"	"2.44"	"16b"	"CCC(=O)Nc1ccc(-c2ncnc3c2cc(C(=O)NCCCN2CCOCC2)n3C)cc1"	"IC50"	"'>'"	"20000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3802364"	"Inhibition of JAK2 in GMCSF-stimulated human TF1 cells assessed as suppression of STAT5 phosphorylation preincubated for 2 hrs followed by GMCSF stimulation for 50 mins by FACS reader analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"CHEMBL3307972"	""
"CHEMBL3797848"	""	"0"	"565.68"	"1"	"2.94"	"16d"	"C[C@H](NC(=O)OC(C)(C)C)C(=O)Nc1ccc(-c2ncnc3c2cc(C(=O)NCCCN2CCOCC2)n3C)cc1"	"IC50"	"'='"	"9300.0"	"nM"	"5.03"	""	""	"UO_0000065"	"8.89"	"0.17"	"2.09"	"3.60"	"False"	"CHEMBL3802364"	"Inhibition of JAK2 in GMCSF-stimulated human TF1 cells assessed as suppression of STAT5 phosphorylation preincubated for 2 hrs followed by GMCSF stimulation for 50 mins by FACS reader analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"CHEMBL3307972"	""
"CHEMBL3800528"	""	"0"	"498.59"	"0"	"3.34"	"16f"	"Cn1c(C(=O)NCCCN2CCOCC2)cc2c(-c3ccc(NC(=O)c4ccccc4)cc3)ncnc21"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL3802364"	"Inhibition of JAK2 in GMCSF-stimulated human TF1 cells assessed as suppression of STAT5 phosphorylation preincubated for 2 hrs followed by GMCSF stimulation for 50 mins by FACS reader analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"CHEMBL3307972"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"Tofacitinib"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"95.0"	"nM"	"7.02"	""	""	"UO_0000065"	"22.48"	"0.42"	"5.48"	"7.90"	"False"	"CHEMBL3802364"	"Inhibition of JAK2 in GMCSF-stimulated human TF1 cells assessed as suppression of STAT5 phosphorylation preincubated for 2 hrs followed by GMCSF stimulation for 50 mins by FACS reader analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"CHEMBL3307972"	""
"CHEMBL3593771"	""	"0"	"361.41"	"0"	"2.01"	"11b"	"N#Cc1ccc(N2CCC(Nc3c(C(N)=O)cnc4[nH]ccc34)CC2)nc1"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	""	"UO_0000065"	"21.43"	"0.39"	"5.73"	"6.26"	"True"	"CHEMBL3594790"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593212"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3593768"	""	"0"	"326.36"	"0"	"0.98"	"10c"	"N#CCC(=O)N1CCC(Nc2c(C(N)=O)cnc3[nH]ccc23)CC1"	"IC50"	"'='"	"200.0"	"nM"	"6.70"	""	""	"UO_0000065"	"20.53"	"0.38"	"5.72"	"5.24"	"False"	"CHEMBL3594790"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593212"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3593763"	""	"0"	"301.35"	"0"	"1.08"	"10a"	"CC(=O)N1CCC(Nc2c(C(N)=O)cnc3[nH]ccc23)CC1"	"IC50"	"'='"	"640.0"	"nM"	"6.19"	""	""	"UO_0000065"	"20.55"	"0.38"	"5.11"	"5.95"	"False"	"CHEMBL3594790"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593212"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3593589"	""	"0"	"335.39"	"0"	"0.80"	"10c"	"CS(=O)(=O)N1CCC[C@H](n2c(=O)[nH]c3cnc4[nH]ccc4c32)C1"	"IC50"	"'='"	"850.0"	"nM"	"6.07"	""	""	"UO_0000065"	"18.10"	"0.36"	"5.27"	"5.85"	"False"	"CHEMBL3594576"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate and ATP incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593193"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"1"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"190.0"	"nM"	"6.72"	""	""	"UO_0000065"	"21.52"	"0.40"	"5.18"	"7.56"	"False"	"CHEMBL2378973"	"Inhibition of JAK2 in human PBMC expressing CD14 assessed as inhibition of GM-CSF-induced STAT5a phosphorylation"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375291"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2381601"	""	"0"	"384.87"	"0"	"2.83"	"8e"	"NC(=O)c1cnc(N[C@H]2CC[C@H](N)CC2)c2nc(-c3ccc(Cl)cc3)cn12"	"IC50"	"'='"	"13000.0"	"nM"	"4.89"	""	""	"UO_0000065"	"12.70"	"0.25"	"2.06"	"4.39"	"False"	"CHEMBL2383899"	"Inhibition of human JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2380230"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL3954540"	""	"0"	"284.36"	"0"	"2.75"	"BDBM254998"	"CN1CN(C2CCCCC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	"443854"	"UO_0000065"	"27.42"	"0.51"	"5.05"	"14.93"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3944182"	""	"0"	"366.47"	"0"	"2.47"	"BDBM255005"	"CCN1CN([C@H]2CC[C@H](CNCC#N)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"21.0"	"nM"	"7.68"	""	"443861"	"UO_0000065"	"20.95"	"0.39"	"5.21"	"8.72"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL2376333"	""	"0"	"356.38"	"0"	"2.91"	"1d"	"COc1cc(OC)cc(Oc2cnc3[nH]cc(C(=O)NC(C)C)c3n2)c1"	"IC50"	"'='"	"1000.0"	"nM"	"6.00"	""	""	"UO_0000065"	"16.84"	"0.32"	"3.09"	"6.10"	"False"	"CHEMBL2378977"	"Inhibition of JAK2 (unknown origin) expressed in SF21 cells using Biotin-KAIETDKEYYTVKD as substrate and [33Pgamma]ATP incubated for 10 mins prior to substrate addition measured after 30 mins by Topcount analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375291"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"CHEMBL4106362"	""
"CHEMBL4437638"	""	"0"	"390.49"	"0"	"3.97"	"8"	"N#CC[C@H]1CC[C@H](n2c(CNC(=O)CC3CC3)nc3cnc4[nH]ccc4c32)CC1"	"IC50"	"'='"	"126.0"	"nM"	"6.90"	""	""	"UO_0000065"	"17.67"	"0.32"	"2.93"	"6.94"	"False"	"CHEMBL4404829"	"Inhibition of JAK2/JAK2 in human PBMC assessed as reduction in GM-CSF-induced STAT5 phosphorylation pre-incubated for 30 mins before GM-CSF stimulation for 30 mins AlphaLISAassay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402578"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4514898"	""	"0"	"475.64"	"0"	"4.34"	"3"	"CC(C)CN1CCC(NC(=O)Cc2nc3cnc4[nH]ccc4c3n2[C@H]2CC[C@H](CC#N)CC2)CC1"	"IC50"	"'='"	"148.0"	"nM"	"6.83"	""	""	"UO_0000065"	"14.36"	"0.27"	"2.49"	"6.65"	"False"	"CHEMBL4404829"	"Inhibition of JAK2/JAK2 in human PBMC assessed as reduction in GM-CSF-induced STAT5 phosphorylation pre-incubated for 30 mins before GM-CSF stimulation for 30 mins AlphaLISAassay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402578"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4588333"	""	"0"	"444.51"	"0"	"4.56"	"9"	"N#CC[C@H]1CC[C@H](n2c(CC(=O)NCc3ccc(F)cc3)nc3cnc4[nH]ccc4c32)CC1"	"IC50"	"'='"	"9.2"	"nM"	"8.04"	""	""	"UO_0000065"	"18.08"	"0.33"	"3.48"	"8.09"	"False"	"CHEMBL4404825"	"Inhibition of JAK2-JH1/JH2 domain (532 to 1132 residues) (unknown origin) pre-incubated before NH2-KGGEEEEYFELVKK-CO2 substrate addition and measured after 90 mins by MS analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402578"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL3986613"	""	"0"	"381.40"	"0"	"2.78"	"BDBM254999"	"O=C1NCN([C@H]2CC[C@H](CNCC(F)(F)F)CC2)c2c1cnc1[nH]ccc21"	"IC50"	"'='"	"4.6"	"nM"	"8.34"	""	"443855"	"UO_0000065"	"21.86"	"0.42"	"5.56"	"11.41"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3646838"	""	"0"	"463.92"	"0"	"3.57"	"BDBM130287"	"NC(=O)c1cc(-c2cccc(Cl)c2)cc2c1[nH]c1ccc(C(=O)N3CCOC(CO)C3)cc12"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"262073"	"UO_0000065"	"19.40"	"0.37"	"5.43"	"8.28"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649614"	""	"0"	"491.57"	"0"	"2.74"	"BDBM130308"	"NC(=O)c1cc(-c2ccc(CN3CCOCC3)s2)nc2c1[nH]c1cc(N3CCOCC3=O)ccc12"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"262094"	"UO_0000065"	"18.31"	"0.35"	"6.26"	"7.91"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649622"	""	"0"	"461.52"	"0"	"2.74"	"BDBM130316"	"NC(=O)c1cc(-c2cc(CN3CCOCC3)co2)nc2c1[nH]c1cc(N3CCOCC3)ccc12"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"262102"	"UO_0000065"	"17.81"	"0.33"	"5.48"	"7.48"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649632"	""	"0"	"454.49"	"0"	"2.84"	"BDBM130326"	"Cn1ncc2ccc(-c3cc(C(N)=O)c4[nH]c5cc(C(=O)N6CCOCC6)ccc5c4n3)cc21"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"262112"	"UO_0000065"	"17.94"	"0.33"	"5.31"	"6.85"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3589328"	""	"0"	"386.46"	"0"	"3.63"	"BDBM130337"	"Cc1ccc(-c2cc(C(N)=O)c3[nH]c4cc(N5CCOCC5)ccc4c3c2)cn1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"262123"	"UO_0000065"	"21.27"	"0.39"	"4.59"	"9.76"	"True"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3646813"	""	"0"	"492.37"	"1"	"5.02"	"BDBM130258"	"NC(=O)c1cc(-c2ccc(Cl)c(Cl)c2)cc2c1[nH]c1ccc(C(=O)NCCn3ccnc3)cc12"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"262044"	"UO_0000065"	"16.70"	"0.33"	"3.20"	"7.77"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3417190"	""	"0"	"543.67"	"2"	"5.79"	"35"	"O=C(CCCCCCCC(=O)N1C/C=C/CCOc2cccc(c2)-c2ccnc(n2)Nc2cccc(c2)C1)NO"	"IC50"	"'='"	"1475.0"	"nM"	"5.83"	""	""	"UO_0000065"	"10.73"	"0.20"	"0.04"	"5.00"	"False"	"CHEMBL3419812"	"Inhibition of human recombinant JAK2 using Z'LYTETry6 peptide substrate after 1 hr by microplate reader"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3414525"	"1"	"Scientific Literature"	"Eur. J. Med. Chem."	"2015"	"None"	""
"CHEMBL3814293"	""	"0"	"303.36"	"0"	"1.15"	"3a"	"NC(=O)c1ccc2c(c1)nc([C@H]1CC[C@H](O)CC1)n2CCO"	"IC50"	"'='"	"3200.0"	"nM"	"5.50"	""	""	"UO_0000065"	"18.11"	"0.34"	"4.34"	"5.42"	"False"	"CHEMBL3817413"	"Inhibition of JAK2 (unknown origin) using tyrosine 6 peptide as substrate by z'-lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3813615"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL4474787"	""	"0"	"254.30"	"0"	"2.10"	"39"	"C=C(C)Cn1nc(C)c(-c2ncnc3[nH]ccc23)n1"	"IC50"	"'='"	"67.4"	"nM"	"7.17"	""	""	"UO_0000065"	"28.20"	"0.52"	"5.07"	"9.92"	"False"	"CHEMBL4429697"	"Inhibition of recombinant human C-terminal 6His-tagged JAK2 (808 to end amino acids) expressed in Sf21 cells measured after 1 hr in presence of ATP by TR-FRET assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4428074"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2016"	"CHEMBL4106362"	""
"CHEMBL4537821"	""	"0"	"310.28"	"0"	"2.87"	"45"	"Cc1nn(CCCC(F)(F)F)nc1-c1ncnc2[nH]ccc12"	"IC50"	"'='"	"96.3"	"nM"	"7.02"	""	""	"UO_0000065"	"22.61"	"0.44"	"4.15"	"9.71"	"False"	"CHEMBL4429697"	"Inhibition of recombinant human C-terminal 6His-tagged JAK2 (808 to end amino acids) expressed in Sf21 cells measured after 1 hr in presence of ATP by TR-FRET assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4428074"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2016"	"CHEMBL4106362"	""
"CHEMBL3646832"	""	"0"	"413.30"	"1"	"6.18"	"BDBM130278"	"CC(C)Oc1ccc2[nH]c3c(C(N)=O)cc(-c4ccc(Cl)c(Cl)c4)cc3c2c1"	"IC50"	"'='"	"150.0"	"nM"	"6.82"	""	"262064"	"UO_0000065"	"16.51"	"0.33"	"0.64"	"10.02"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3125862"	""	"0"	"457.61"	"0"	"4.39"	"4"	"O=c1[nH]c(CSc2nnc(NCC3CCCO3)s2)nc2sc(-c3ccccc3)cc12"	"IC50"	"'='"	"8900.0"	"nM"	"5.05"	""	""	"UO_0000065"	"11.04"	"0.23"	"0.66"	"5.44"	"False"	"CHEMBL3130286"	"Inhibition of JAK2 (unknown origin) by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3124748"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL4460736"	""	"0"	"268.32"	"0"	"2.32"	"55"	"Cc1nn(CC2CCC2)nc1-c1ncnc2[nH]ccc12"	"IC50"	"'='"	"62.7"	"nM"	"7.20"	""	""	"UO_0000065"	"26.84"	"0.49"	"4.88"	"9.97"	"False"	"CHEMBL4429697"	"Inhibition of recombinant human C-terminal 6His-tagged JAK2 (808 to end amino acids) expressed in Sf21 cells measured after 1 hr in presence of ATP by TR-FRET assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4428074"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2016"	"CHEMBL4106362"	""
"CHEMBL4463043"	""	"0"	"415.46"	"0"	"2.06"	"14d"	"N#Cc1ccc(N2CCC(Nc3cc(Nc4ccncn4)ncc3C(N)=O)CC2)nc1"	"IC50"	"'='"	"5.5"	"nM"	"8.26"	""	""	"UO_0000065"	"19.88"	"0.36"	"6.20"	"5.67"	"False"	"CHEMBL4429528"	"Inhibition of human JAK2 assessed as reduction in phosphorylation of Biotin-Lyn-Substrate-2 after 1 hr in presence of ATP by ELISA"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4428070"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2016"	"None"	""
"CHEMBL4591633"	""	"0"	"429.49"	"0"	"2.37"	"14g"	"Cc1nccc(Nc2cc(NC3CCN(c4ccc(C#N)cn4)CC3)c(C(N)=O)cn2)n1"	"IC50"	"'='"	"3.2"	"nM"	"8.49"	""	""	"UO_0000065"	"19.78"	"0.36"	"6.12"	"5.83"	"False"	"CHEMBL4429528"	"Inhibition of human JAK2 assessed as reduction in phosphorylation of Biotin-Lyn-Substrate-2 after 1 hr in presence of ATP by ELISA"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4428070"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2016"	"None"	""
"CHEMBL3601242"	""	"0"	"383.84"	"0"	"3.34"	"32"	"C=CC(=O)Nc1cccc(CNc2nc(Nc3cnn(C)c3)ncc2Cl)c1"	"IC50"	"'='"	"107.0"	"nM"	"6.97"	""	""	"UO_0000065"	"18.16"	"0.35"	"3.63"	"7.20"	"False"	"CHEMBL3603319"	"Inhibition of JAK2 (unknown origin) by Z'-Lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3600288"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL4638206"	""	"0"	"420.52"	"0"	"2.56"	"7"	"CCNC(=O)c1ccc(Nc2nccc(N3CC4CCC(C3)N4C(=O)C3CC3)n2)cc1"	"IC50"	"'='"	"329.0"	"nM"	"6.48"	""	""	"UO_0000065"	"15.42"	"0.29"	"3.92"	"7.17"	"False"	"CHEMBL4620433"	"Inhibition of human recombinant JAK2 assessed as level of phosphorylation in presence of peptide substrate FITC-KGGEEEEYFELVKK and ATP by mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4619733"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2020"	"None"	""
"CHEMBL4647737"	""	"0"	"403.36"	"0"	"3.04"	"J-2"	"O=C(NCC(F)(F)F)c1ccc(-c2cccc3nc(NC(=O)C4CC4)nn23)cc1"	"IC50"	"'='"	"214.0"	"nM"	"6.67"	""	""	"UO_0000065"	"16.54"	"0.31"	"3.63"	"7.55"	"False"	"CHEMBL4624516"	"Inhibition of JAK2 (unknown origin) in presence of ATP at Km concentration by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4622902"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL4243458"	""	"0"	"504.60"	"1"	"4.76"	"13a"	"CCCn1cc(-c2nc(Nc3ccc(NC(=O)CCCCCCC(=O)NO)cc3)nc3[nH]ccc23)cn1"	"IC50"	"'='"	"0.15"	"nM"	"9.82"	""	""	"UO_0000065"	"19.47"	"0.36"	"5.06"	"6.56"	"False"	"CHEMBL4233426"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma-33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229421"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2018"	"None"	""
"CHEMBL4237600"	""	"0"	"568.66"	"1"	"3.39"	"13h"	"CS(=O)(=O)CCn1cc(-c2nc(Nc3ccc(NC(=O)CCCCCCC(=O)NO)cc3)nc3[nH]ccc23)cn1"	"IC50"	"'='"	"7.7"	"nM"	"8.11"	""	""	"UO_0000065"	"14.27"	"0.28"	"4.72"	"4.41"	"False"	"CHEMBL4233426"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma-33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229421"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2018"	"None"	""
"CHEMBL3589328"	""	"0"	"386.46"	"0"	"3.63"	"20"	"Cc1ccc(-c2cc(C(N)=O)c3[nH]c4cc(N5CCOCC5)ccc4c3c2)cn1"	"IC50"	"'='"	"120.0"	"nM"	"6.92"	""	""	"UO_0000065"	"17.91"	"0.33"	"3.29"	"8.22"	"False"	"CHEMBL3592855"	"Inhibition of JAK2 in human SET2 cells assessed as inhibition of cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3359917"	""	"0"	"302.38"	"0"	"1.78"	"4f"	"CC1(C)C[C@](C)(O)C[C@H]1Nc1c(C(N)=O)cnn2cccc12"	"IC50"	"'='"	"61.0"	"nM"	"7.21"	""	""	"UO_0000065"	"23.86"	"0.45"	"5.43"	"7.79"	"False"	"CHEMBL3377596"	"Inhibition of JAK2 (unknown origin) by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352641"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3359920"	""	"0"	"301.39"	"0"	"1.75"	"4i"	"CC1(C)[C@H](Nc2c(C(N)=O)cnn3cccc23)CC[C@@]1(C)N"	"IC50"	"'='"	"280.0"	"nM"	"6.55"	""	""	"UO_0000065"	"21.74"	"0.41"	"4.80"	"6.66"	"False"	"CHEMBL3377596"	"Inhibition of JAK2 (unknown origin) by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352641"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL4517545"	""	"0"	"397.49"	"0"	"0.84"	"11q"	"Cc1cc(-c2nn(C3CCCN(C(=O)CN(C)C)C3)c3ncnc(N)c23)nn1C"	"IC50"	"'='"	"985.9"	"nM"	"6.01"	""	""	"UO_0000065"	"15.11"	"0.28"	"5.17"	"5.41"	"False"	"CHEMBL4402146"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-biotin as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4400567"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4584510"	""	"0"	"351.21"	"0"	"1.52"	"10j"	"C=CC(=O)N1CCC(n2nc(Br)c3c(N)ncnc32)CC1"	"IC50"	"'='"	"62.0"	"nM"	"7.21"	""	""	"UO_0000065"	"20.52"	"0.47"	"5.69"	"8.01"	"False"	"CHEMBL4402146"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-biotin as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4400567"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4289875"	""	"0"	"340.36"	"0"	"2.59"	"12"	"Cc1cc(F)cc(Nc2cc(NC3CC3)c3ncc(C(N)=O)n3n2)c1"	"IC50"	"'>'"	"2000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4251837"	"Inhibition of JAK2 JH2 domain (unknown origin)"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4251544"	"1"	"Scientific Literature"	"MedChemComm"	"2017"	"None"	""
"CHEMBL4069365"	""	"0"	"421.38"	"0"	"4.14"	"13"	"CC1(C)OCC(=O)Nc2cc(Nc3nc(NCC(F)(F)F)c4occc4n3)ccc21"	"IC50"	"'='"	"236.0"	"nM"	"6.63"	""	""	"UO_0000065"	"15.73"	"0.30"	"2.49"	"6.54"	"False"	"CHEMBL4007715"	"Inhibition of JAK2 (unknown origin) after 60 mins by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4007384"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2016"	"None"	""
"CHEMBL4782433"	""	"0"	"458.52"	"0"	"3.56"	"10b"	"COc1ccc(C(=O)Nc2c[nH]nc2-c2nc(-c3ccc(CN4CCOCC4)cc3)c[nH]2)cc1"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	""	""	"17.13"	"0.32"	"4.29"	"7.26"	"False"	"CHEMBL4711870"	"Inhibition of JAK2 (unknown origin) incubated for 40 mins in presence of ATP by Kinase-glo luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706620"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2021"	"None"	"TIME = 0.6667 hr"
"CHEMBL1923593"	""	"0"	"457.58"	"0"	"4.71"	"34"	"COc1ccccc1-c1ccc2cnc(Nc3ccc(C4CCN(C[C@H](C)O)CC4)cc3)nn12"	"IC50"	"'='"	"0.6"	"nM"	"9.22"	""	""	"UO_0000065"	"20.15"	"0.37"	"4.51"	"12.31"	"False"	"CHEMBL1926252"	"Inhibition of human recombinant JAK2 using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate after 20 mins by fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1921765"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2011"	"None"	""
"CHEMBL3593765"	""	"0"	"349.44"	"0"	"2.74"	"17a"	"NC(=O)c1cnc2[nH]ccc2c1NC1CCN(Cc2ccccc2)CC1"	"IC50"	"'='"	"84.0"	"nM"	"7.08"	""	""	""	"20.25"	"0.37"	"4.34"	"8.13"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL4784576"	""	"0"	"447.58"	"0"	"4.32"	"17l"	"COc1cccc(CN2CCC(Nc3c(C(=O)NC4CCCC4)cnc4[nH]ccc34)CC2)c1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	""	""	""	""	""	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL4759666"	""	"0"	"411.94"	"0"	"4.04"	"30b"	"CNC(=O)c1cnc2[nH]ccc2c1NC1CCCN(Cc2cccc(Cl)c2)CC1"	"IC50"	"'='"	"57.7"	"nM"	"7.24"	""	""	""	"17.57"	"0.34"	"3.20"	"9.91"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL4747285"	""	"0"	"402.50"	"0"	"3.26"	"30f"	"CNC(=O)c1cnc2[nH]ccc2c1NC1CCCN(Cc2ccc(C#N)cc2)CC1"	"IC50"	"'='"	"150.0"	"nM"	"6.82"	""	""	""	"16.95"	"0.31"	"3.56"	"7.05"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL3933191"	""	"0"	"415.50"	"0"	"3.03"	"BDBM229062"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(Cc2cccnc2)CC1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	"400798"	"UO_0000065"	"19.15"	"0.35"	"4.93"	"7.05"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3343051"	""	"0"	"427.42"	"0"	"2.63"	"24b"	"O=C(Nc1ccc(NC(=O)c2ccccn2)cc1)c1cccc(-c2c[nH]c(=O)[nH]c2=O)c1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3380804"	"Inhibition of human JAK2 incubated for 20 mins prior to MgCl2 addition measured after 90 mins by mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351874"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL4634634"	""	"0"	"365.44"	"0"	"1.44"	"29"	"C[C@@H]1C[C@H]1C(=O)N1CCN(c2cnc(C#N)c(-c3cnn(C)c3)n2)C[C@H]1C"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4603513"	"Inhibition of human recombinant N-terminal GST tagged JAK2 JH1 catalytic domain (532 to 1132 residues) expressed in baculovirus expression system using Tyr6 peptide as measured after 1 hr in presence of ATP by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4602617"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL3702936"	""	"0"	"327.36"	"0"	"2.93"	"BDBM147638"	"N#C[C@@H]1CCCC(F)[C@@H]1n1cc(C(N)=O)c(Nc2ccccc2)n1"	"IC50"	"'='"	"212.0"	"nM"	"6.67"	""	"285570"	"UO_0000065"	"20.39"	"0.38"	"3.74"	"6.90"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647772"	""	"0"	"462.48"	"0"	"3.04"	"BDBM147875"	"CC1(O)CN([C@@H]2CC[C@H](n3cc(C(N)=O)c(Nc4ccc(C(F)(F)F)cc4)n3)[C@@H](C#N)C2)C1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"285809"	"UO_0000065"	"17.40"	"0.33"	"5.01"	"6.69"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703054"	""	"0"	"406.49"	"0"	"2.87"	"BDBM147764"	"CC(=O)c1ccc(Nc2nn([C@H]3CC[C@@H](N4CCC4)C[C@@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	"285698"	"UO_0000065"	"19.05"	"0.35"	"4.87"	"6.62"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL2208024"	""	"0"	"387.49"	"0"	"4.84"	"7a"	"CC(=O)Nc1ccc(-c2ccnc(Nc3cccc(N4CCCCC4)c3)n2)cc1"	"IC50"	"'='"	"1328.0"	"nM"	"5.88"	""	""	"UO_0000065"	"15.17"	"0.28"	"1.04"	"8.38"	"False"	"CHEMBL2214784"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT3 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL2208033"	""	"0"	"434.50"	"0"	"1.98"	"10c"	"N[C@H](CO)C(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"621.7"	"nM"	"6.21"	""	""	"UO_0000065"	"14.28"	"0.26"	"4.23"	"4.94"	"False"	"CHEMBL2214785"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT1 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL2208032"	""	"0"	"418.50"	"0"	"3.01"	"10b"	"C[C@@H](N)C(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"327.7"	"nM"	"6.49"	""	""	"UO_0000065"	"15.49"	"0.29"	"3.47"	"6.15"	"False"	"CHEMBL2214785"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT1 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL2207761"	""	"0"	"458.35"	"0"	"4.64"	"1"	"CC(=O)Nc1ccc(-c2ccnc(NCCCNC(=O)c3c(Cl)cccc3Cl)n2)cc1"	"IC50"	"'='"	"8138.0"	"nM"	"5.09"	""	""	"UO_0000065"	"11.10"	"0.22"	"0.45"	"5.30"	"False"	"CHEMBL2214785"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT1 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL2208033"	""	"0"	"434.50"	"0"	"1.98"	"10c"	"N[C@H](CO)C(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"2.7"	"nM"	"8.57"	""	""	"UO_0000065"	"19.72"	"0.37"	"6.59"	"6.82"	"False"	"CHEMBL2214787"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL2207765"	""	"0"	"493.35"	"1"	"5.80"	"6"	"CC(=O)Nc1ccc(-c2ccnc(Nc3cccc(NC(=O)c4c(Cl)cccc4Cl)n3)n2)cc1"	"IC50"	"'='"	"129.9"	"nM"	"6.89"	""	""	"UO_0000065"	"13.96"	"0.28"	"1.09"	"6.32"	"False"	"CHEMBL2214787"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL2207764"	""	"0"	"492.37"	"1"	"6.40"	"5"	"CC(=O)Nc1ccc(-c2ccnc(Nc3cccc(NC(=O)c4c(Cl)cccc4Cl)c3)n2)cc1"	"IC50"	"'='"	"12.6"	"nM"	"7.90"	""	""	"UO_0000065"	"16.04"	"0.32"	"1.50"	"8.23"	"False"	"CHEMBL2214787"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL3651064"	""	"0"	"360.38"	"0"	"3.50"	"BDBM47236"	"C=C(C)C(=O)Nc1cccc(-c2ncnc3[nH]cc(-c4nnc(C)o4)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"198770"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3958078"	""	"0"	"382.45"	"0"	"1.73"	"BDBM228766"	"CN([C@@H]1CCN(c2ncnc3[nH]ccc23)C1)S(=O)(=O)c1cccc(C#N)c1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399700"	"UO_0000065"	"24.21"	"0.47"	"7.53"	"8.74"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3931224"	""	"0"	"518.59"	"2"	"5.17"	"BDBM229039"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3cccc(-c4ccc(F)cc4)c3)n2)CC1"	"IC50"	"'='"	"1104.0"	"nM"	"5.96"	""	"400784"	"UO_0000065"	"11.49"	"0.21"	"0.79"	"4.72"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3904624"	""	"0"	"308.39"	"0"	"2.38"	"BDBM228785"	"Cc1ccc(N(C)[C@@H]2CCN(c3ncnc4[nH]ccc34)C2)nc1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399723"	"UO_0000065"	"30.03"	"0.55"	"6.88"	"15.19"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3981902"	""	"0"	"427.51"	"0"	"3.34"	"BDBM228797"	"CN(C(=O)c1ccc(N(C)[C@@H]2CCN(c3ncnc4[nH]ccc34)C2)nc1)c1ccccc1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399736"	"UO_0000065"	"21.66"	"0.40"	"5.92"	"11.40"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3951673"	""	"0"	"462.49"	"0"	"3.59"	"BDBM237803"	"N#C[C@@H]1CCN(C(=O)OCc2ccccc2)C[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"53.0"	"nM"	"7.28"	""	"414907"	"UO_0000065"	"15.73"	"0.29"	"3.69"	"5.76"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3894596"	""	"0"	"377.40"	"0"	"1.36"	"BDBM237856"	"N#C[C@H]1CS(=O)(=O)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"79.0"	"nM"	"7.10"	""	"414961"	"UO_0000065"	"18.82"	"0.37"	"5.74"	"5.43"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3899281"	""	"0"	"409.37"	"0"	"2.42"	"BDBM237871"	"N#C[C@@H]1CCOC[C@H]1n1cc(C(N)=O)c(Nc2ccc([C@@H](O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"21.0"	"nM"	"7.68"	""	"414973"	"UO_0000065"	"18.76"	"0.36"	"5.26"	"6.08"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3947292"	""	"0"	"405.41"	"0"	"2.30"	"BDBM237883"	"C[C@](O)(c1ccc(Nc2nn([C@@H]3COCC[C@H]3C#N)cc2C(N)=O)cc1)C(F)F"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	"414985"	"UO_0000065"	"19.54"	"0.37"	"5.62"	"6.28"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3916138"	""	"0"	"311.35"	"0"	"1.83"	"BDBM237903"	"N#C[C@@H]1CCOC[C@H]1n1cc(C(N)=O)c(Nc2ccccc2)n1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"415005"	"UO_0000065"	"27.37"	"0.51"	"6.69"	"8.04"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3932038"	""	"0"	"363.37"	"0"	"0.97"	"BDBM237860"	"N#C[C@H]1CS(=O)(=O)C[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	"415011"	"UO_0000065"	"21.45"	"0.43"	"6.83"	"5.96"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3912624"	""	"0"	"438.53"	"0"	"3.80"	"BDBM228888"	"CC(C)(C)OC(=O)NC1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)CC1"	"IC50"	"'='"	"267.0"	"nM"	"6.57"	""	"400635"	"UO_0000065"	"14.99"	"0.28"	"2.77"	"4.87"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3963309"	""	"0"	"433.49"	"0"	"3.48"	"BDBM228896"	"Cc1cc(N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)CC2)ccn1"	"IC50"	"'='"	"174.0"	"nM"	"6.76"	""	"400643"	"UO_0000065"	"15.59"	"0.29"	"3.28"	"5.99"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3960729"	""	"0"	"479.52"	"0"	"2.54"	"BDBM228902"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(c2cccc(OCCO)n2)CC1"	"IC50"	"'='"	"47.0"	"nM"	"7.33"	""	"400649"	"UO_0000065"	"15.28"	"0.29"	"4.79"	"5.15"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3984504"	""	"0"	"487.46"	"0"	"4.19"	"BDBM228920"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(c2ccc(C(F)(F)F)nc2)CC1"	"IC50"	"'='"	"26.0"	"nM"	"7.58"	""	"400667"	"UO_0000065"	"15.56"	"0.30"	"3.40"	"6.72"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3923710"	""	"0"	"433.49"	"0"	"3.48"	"BDBM228923"	"Cc1ccnc(N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)CC2)c1"	"IC50"	"'='"	"44.0"	"nM"	"7.36"	""	"400670"	"UO_0000065"	"16.97"	"0.31"	"3.88"	"6.52"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3920283"	""	"0"	"463.52"	"0"	"3.57"	"BDBM228928"	"CCOc1ccc(N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)CC2)cn1"	"IC50"	"'='"	"46.0"	"nM"	"7.34"	""	"400675"	"UO_0000065"	"15.83"	"0.29"	"3.77"	"6.01"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3916493"	""	"0"	"436.47"	"0"	"3.91"	"BDBM228930"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(c2ccc(F)cc2)CC1"	"IC50"	"'='"	"37.0"	"nM"	"7.43"	""	"400677"	"UO_0000065"	"17.03"	"0.32"	"3.52"	"7.43"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4095596"	""	"0"	"342.40"	"0"	"2.84"	"45"	"CC(CCCCCC(=O)NO)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"65.0"	"nM"	"7.19"	""	""	"UO_0000065"	"20.99"	"0.39"	"4.35"	"6.61"	"False"	"CHEMBL4031305"	"Inhibition of human JAK2 using poly[Glu:Tyr] as substrate in presence of [gamma-33P]-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028864"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4059703"	""	"0"	"403.45"	"0"	"2.84"	"41"	"O=C(/C=C/c1ccc(NCCCn2cc(-c3ncnc4[nH]ccc34)cn2)cc1)NO"	"IC50"	"'='"	"502.0"	"nM"	"6.30"	""	""	"UO_0000065"	"15.61"	"0.29"	"3.46"	"5.22"	"False"	"CHEMBL4031305"	"Inhibition of human JAK2 using poly[Glu:Tyr] as substrate in presence of [gamma-33P]-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028864"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4088824"	""	"0"	"300.32"	"0"	"1.50"	"22"	"O=C(CCCCn1cc(-c2ncnc3[nH]ccc23)cn1)NO"	"IC50"	"'='"	"219.0"	"nM"	"6.66"	""	""	"UO_0000065"	"22.17"	"0.41"	"5.16"	"6.13"	"False"	"CHEMBL4031305"	"Inhibition of human JAK2 using poly[Glu:Tyr] as substrate in presence of [gamma-33P]-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028864"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4089113"	""	"0"	"286.30"	"0"	"1.11"	"21"	"O=C(CCCn1cc(-c2ncnc3[nH]ccc23)cn1)NO"	"IC50"	"'='"	"3560.0"	"nM"	"5.45"	""	""	"UO_0000065"	"19.03"	"0.35"	"4.34"	"5.01"	"False"	"CHEMBL4031305"	"Inhibition of human JAK2 using poly[Glu:Tyr] as substrate in presence of [gamma-33P]-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028864"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4643764"	""	"0"	"350.38"	"0"	"1.61"	"J-7"	"N#CCC(=O)N1CC=C(c2cccc3nc(NC(=O)C4CC4)nn23)CC1"	"IC50"	"'='"	"157.0"	"nM"	"6.80"	""	""	"UO_0000065"	"19.42"	"0.36"	"5.19"	"6.58"	"False"	"CHEMBL4624516"	"Inhibition of JAK2 (unknown origin) in presence of ATP at Km concentration by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4622902"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL4644662"	""	"0"	"359.39"	"0"	"2.86"	"J-6"	"C=C(C#N)C(O)c1ccc(-c2cccc3nc(NC(=O)C4CC4)nn23)cc1"	"IC50"	"'='"	"1030.0"	"nM"	"5.99"	""	""	"UO_0000065"	"16.66"	"0.30"	"3.13"	"5.80"	"False"	"CHEMBL4624521"	"Inhibition of JAK2 (unknown origin) expressed in mouse BAF3 cells assessed as antiproliferative activity by cell-based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4622902"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"CHEMBL3307634"	""
"CHEMBL4641565"	""	"0"	"387.39"	"0"	"2.35"	"J-10"	"O=C(Nc1nc2cccc(C3=CCN(C(=O)C4CC4(F)F)CC3)n2n1)C1CC1"	"IC50"	"'='"	"192.0"	"nM"	"6.72"	""	""	"UO_0000065"	"17.34"	"0.33"	"4.37"	"8.44"	"False"	"CHEMBL4624516"	"Inhibition of JAK2 (unknown origin) in presence of ATP at Km concentration by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4622902"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL3909435"	""	"0"	"323.42"	"0"	"1.21"	"BDBM228769"	"CC(C)S(=O)(=O)N(C)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399705"	"UO_0000065"	"28.63"	"0.57"	"8.05"	"11.27"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3950519"	""	"0"	"400.87"	"0"	"2.17"	"BDBM239973"	"Cn1cnc(Nc2ncc(Cl)c(NC3CC4CN(C(=O)CC#N)CC4C3)n2)c1"	"IC50"	"'='"	"371.0"	"nM"	"6.43"	""	"418593"	"UO_0000065"	"16.04"	"0.31"	"4.26"	"5.75"	"False"	"CHEMBL3888834"	"Kinase Assay: JAK2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 100 μM KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC, 10 mM MgAcetate and [γ-33P-ATP](specific activity approx. 500 cpm/pmol, concentration as required). The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of 3% phosphoric acid solution. 10 μL of the reaction is then spotted onto a P30 filtermat and washed three times for 5 minutes in 75 mM phosphoric acid and once in methanol prior to drying and scintillation counting."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886854"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3927605"	""	"0"	"465.49"	"0"	"3.08"	"BDBM237809"	"N#CCC1(COC(=O)N2CC[C@@H](C#N)[C@H](n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)C2)CC1"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	"414913"	"UO_0000065"	"16.81"	"0.31"	"4.74"	"5.21"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3902593"	""	"0"	"428.42"	"0"	"1.79"	"BDBM237810"	"N#C[C@@H]1CCN(C(=O)OC2COC2)C[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"43.0"	"nM"	"7.37"	""	"414914"	"UO_0000065"	"17.19"	"0.32"	"5.58"	"5.44"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3930581"	""	"0"	"456.48"	"0"	"2.42"	"BDBM237811"	"CC1(COC(=O)N2CC[C@@H](C#N)[C@H](n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)C2)COC1"	"IC50"	"'='"	"96.0"	"nM"	"7.02"	""	"414915"	"UO_0000065"	"15.37"	"0.29"	"4.60"	"5.18"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3930874"	""	"0"	"434.48"	"0"	"2.87"	"BDBM228939"	"Cc1ncncc1N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CC1"	"IC50"	"'='"	"181.0"	"nM"	"6.74"	""	"400686"	"UO_0000065"	"15.52"	"0.29"	"3.87"	"5.36"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3924811"	""	"0"	"487.46"	"0"	"4.19"	"BDBM228947"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(c2cc(C(F)(F)F)ccn2)CC1"	"IC50"	"'='"	"75.0"	"nM"	"7.12"	""	"400694"	"UO_0000065"	"14.62"	"0.28"	"2.93"	"6.31"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3962429"	""	"0"	"451.49"	"0"	"2.03"	"BDBM228954"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3cnc(C#N)nc3)n2)CC1"	"IC50"	"'='"	"38.0"	"nM"	"7.42"	""	"400701"	"UO_0000065"	"16.43"	"0.31"	"5.39"	"4.22"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3967992"	""	"0"	"482.54"	"0"	"3.15"	"BDBM228967"	"COC(=O)c1ccc(Nc2nn(C3(CC#N)CCN(C(=O)OC(C)(C)C)CC3)cc2C(N)=O)cc1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"400712"	"UO_0000065"	"16.67"	"0.31"	"4.90"	"5.27"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3984315"	""	"0"	"506.57"	"1"	"3.72"	"BDBM228995"	"Cc1noc(-c2ccc(Nc3nn(C4(CC#N)CCN(C(=O)OC(C)(C)C)CC4)cc3C(N)=O)cc2)n1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"400740"	"UO_0000065"	"16.39"	"0.31"	"4.58"	"5.03"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3931250"	""	"0"	"509.49"	"1"	"2.75"	"BDBM229007"	"CC(C)(O)c1ccc(Nc2nn(C3(CC#N)CCN(C(=O)OCC(F)(F)F)CC3)cc2C(N)=O)cn1"	"IC50"	"'='"	"0.7"	"nM"	"9.15"	""	"400752"	"UO_0000065"	"17.97"	"0.35"	"6.40"	"5.74"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3929513"	""	"0"	"531.50"	"1"	"2.92"	"BDBM229016"	"Cn1cc(-c2ccc(Nc3nn(C4(CC#N)CCN(C(=O)OCC(F)(F)F)CC4)cc3C(N)=O)cn2)cn1"	"IC50"	"'='"	"0.5"	"nM"	"9.30"	""	"400761"	"UO_0000065"	"17.50"	"0.33"	"6.38"	"5.92"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL2207759"	""	"0"	"458.57"	"0"	"3.76"	"10g"	"CN1CCC[C@@H]1C(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"1051.0"	"nM"	"5.98"	""	""	"UO_0000065"	"13.04"	"0.24"	"2.22"	"7.24"	"False"	"CHEMBL2214784"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT3 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL2208029"	""	"0"	"457.46"	"0"	"4.70"	"9d"	"CC(=O)Nc1ccc(-c2nc(Nc3ccc(N4CCOCC4)cc3)ncc2C(F)(F)F)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL2214784"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT3 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL3646840"	""	"0"	"514.56"	"1"	"3.93"	"BDBM130289"	"COc1ccc(-c2cc(C(N)=O)c3[nH]c4ccc(C(=O)N5CCN(C(=O)C6CC6)CC5)cc4c3c2)cc1F"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"262075"	"UO_0000065"	"17.49"	"0.32"	"5.07"	"8.28"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3646842"	""	"0"	"461.49"	"0"	"3.83"	"BDBM130291"	"COc1ccc(-c2cc(C(N)=O)c3[nH]c4ccc(C(=O)N5CCC(O)CC5)cc4c3c2)cc1F"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"262077"	"UO_0000065"	"19.50"	"0.36"	"5.17"	"8.28"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3646846"	""	"0"	"476.51"	"0"	"2.80"	"BDBM130295"	"COc1ccc(-c2nc(C(N)=O)c3[nH]c4cc(C(=O)N5CCC(N(C)C)C5)ccc4c3n2)cc1F"	"IC50"	"'<'"	"1.0"	"nM"	""	""	"262081"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649606"	""	"0"	"476.02"	"1"	"5.05"	"BDBM130299"	"CC(C)(C)N1CCN(Cc2ccc3c(c2)[nH]c2c(C(N)=O)cc(-c4cccc(Cl)c4)nc23)CC1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"262085"	"UO_0000065"	"18.91"	"0.36"	"3.95"	"11.50"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3639484"	""	"0"	"433.49"	"0"	"3.38"	"BDBM130303"	"COc1ccc(-c2cc(C(N)=O)c3[nH]c4cc(N5CCN(C)CC5)ccc4c3n2)cc1F"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"262089"	"UO_0000065"	"20.76"	"0.38"	"5.62"	"10.29"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649625"	""	"0"	"409.45"	"0"	"1.12"	"BDBM130319"	"NC(=O)c1cc(N2CCOCC2)nc2c1[nH]c1cc(C(=O)N3CCOCC3)ccc12"	"IC50"	"'='"	"142.0"	"nM"	"6.85"	""	"262105"	"UO_0000065"	"16.72"	"0.31"	"5.73"	"6.02"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649631"	""	"0"	"456.53"	"0"	"4.17"	"BDBM130325"	"NC(=O)c1cc(-c2ccc3sccc3c2)nc2c1[nH]c1cc(C(=O)N3CCOCC3)ccc12"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"262111"	"UO_0000065"	"19.71"	"0.37"	"4.83"	"8.88"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649642"	""	"0"	"582.75"	"2"	"6.34"	"BDBM130336"	"Cc1cc(-c2cc(C(N)=O)c3[nH]c4cc(C5CCN(C(=O)OC(C)(C)C)CC5)ccc4c3c2)ccc1CN1CCOCC1"	"IC50"	"'='"	"818.0"	"nM"	"6.09"	""	"262122"	"UO_0000065"	"10.45"	"0.19"	"-0.25"	"6.03"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3646815"	""	"0"	"511.41"	"1"	"4.46"	"BDBM130260"	"NC(=O)c1cc(-c2ccc(Cl)c(Cl)c2)cc2c1[nH]c1ccc(C(=O)NCCN3CCOCC3)cc12"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"262046"	"UO_0000065"	"16.08"	"0.32"	"3.76"	"8.19"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3646822"	""	"0"	"479.56"	"0"	"3.21"	"BDBM130268"	"COc1cccc(-c2cc(C(N)=O)c3[nH]c4cc(C(=O)N(C)CCS(C)(=O)=O)ccc4c3c2)c1"	"IC50"	"'<'"	"1.0"	"nM"	""	""	"262054"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3646823"	""	"0"	"430.51"	"0"	"3.39"	"BDBM130269"	"COc1cccc(-c2cc(C(N)=O)c3[nH]c4cc(C(=O)NCCN(C)C)ccc4c3c2)c1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"262055"	"UO_0000065"	"19.10"	"0.35"	"4.83"	"8.19"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL2178266"	""	"0"	"346.39"	"0"	"3.00"	"14h"	"Cc1ccc(C)c(-c2nn(C)cc2NC(=O)c2cnn3cccnc23)c1"	"IC50"	"'='"	"64.2"	"nM"	"7.19"	""	""	"UO_0000065"	"20.76"	"0.38"	"4.19"	"9.33"	"False"	"CHEMBL2186603"	"Inhibition of JAK2 in human TF1 cells assessed as reduction in STAT5 phosphorylation incubated for 30 mins in presence of human recombinant EPO"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176876"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"CHEMBL3307972"	""
"CHEMBL3644618"	""	"0"	"499.52"	"1"	"5.36"	"22"	"CCc1cc(O)c(F)cc1-c1ccc2c(-c3nc4c([nH]3)CCN(C(=O)c3ccc(F)cc3)C4)n[nH]c2c1"	"IC50"	"'='"	"0.3"	"nM"	"9.52"	""	""	"UO_0000065"	"19.06"	"0.35"	"4.16"	"9.73"	"False"	"CHEMBL4003453"	"Inhibition of GST tagged human recombinant JAK2 catalytic domain expressed in baculovirus using peptide substrate preincubated for 60 mins followed by substrate addition and measured after 60 mins by microfluidic assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4002590"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL3234879"	""	"0"	"345.37"	"0"	"4.24"	"18"	"Cc1cccc(Nc2sc(-c3cccc(F)c3F)cc2C(N)=O)n1"	"IC50"	"'='"	"80.0"	"nM"	"7.10"	""	""	"UO_0000065"	"20.55"	"0.40"	"2.86"	"10.44"	"False"	"CHEMBL3239499"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3232939"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3234873"	""	"0"	"452.58"	"0"	"3.71"	"24"	"CC(C)(O)c1ccc(-c2cc(C(N)=O)c(Nc3cccc(CN4CCOCC4)n3)s2)cc1"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	""	"UO_0000065"	"17.01"	"0.33"	"3.99"	"7.64"	"False"	"CHEMBL3239499"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3232939"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL1983268"	"ENTRECTINIB"	"4"	"560.65"	"2"	"5.03"	"2; entrectinib"	"CN1CCN(c2ccc(C(=O)Nc3n[nH]c4ccc(Cc5cc(F)cc(F)c5)cc34)c(NC3CCOCC3)c2)CC1"	"IC50"	"'='"	"40.0"	"nM"	"7.40"	""	""	"UO_0000065"	"13.20"	"0.25"	"2.37"	"8.65"	"False"	"CHEMBL3807411"	"Inhibition of JAK2 (unknown origin) in presence of gamma33-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3804811"	"1"	"Scientific Literature"	"J. Med. Chem."	"2016"	"None"	""
"CHEMBL3622135"	""	"0"	"435.56"	"0"	"4.22"	"16"	"CCn1c(C(=O)N(C2CC2)C2CC2)cc2c3c(ncn3C)c(Nc3nc(C)cs3)nc21"	"IC50"	"'='"	"73.0"	"nM"	"7.14"	""	""	"UO_0000065"	"16.39"	"0.31"	"2.92"	"8.82"	"False"	"CHEMBL3625474"	"Inhibition of JAK2 in human SET2 cells assessed as inhibition of cell proliferation after 72 hrs by [3H]-thymidine incorporation assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621098"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3622137"	""	"0"	"449.58"	"0"	"4.53"	"18"	"CCn1c(C(=O)N(C2CC2)C2CC2)cc2c3c(ncn3C)c(Nc3nc(C)c(C)s3)nc21"	"IC50"	"'='"	"65.0"	"nM"	"7.19"	""	""	"UO_0000065"	"15.99"	"0.31"	"2.66"	"8.89"	"False"	"CHEMBL3625474"	"Inhibition of JAK2 in human SET2 cells assessed as inhibition of cell proliferation after 72 hrs by [3H]-thymidine incorporation assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621098"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3815154"	""	"0"	"316.41"	"0"	"1.37"	"3d"	"CNCCn1c2ccc(C(N)=O)cc2nc1[C@H]1CC[C@H](O)CC1"	"IC50"	"'='"	"3900.0"	"nM"	"5.41"	""	""	"UO_0000065"	"17.09"	"0.32"	"4.04"	"5.81"	"False"	"CHEMBL3817413"	"Inhibition of JAK2 (unknown origin) using tyrosine 6 peptide as substrate by z'-lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3813615"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3983775"	""	"0"	"498.57"	"0"	"4.19"	"309"	"N#CCC1(n2cc(-c3ccnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3ccccc3F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3925174"	""	"0"	"594.00"	"1"	"4.59"	"341"	"N#CCC1(n2cc(-c3c(C#N)cnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc(C(F)(F)F)ncc3Cl)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3986743"	""	"0"	"468.53"	"0"	"1.84"	"14"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cnccn3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3928990"	""	"0"	"532.01"	"1"	"3.11"	"37"	"COc1cc(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)cc(Cl)n1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3913246"	""	"0"	"520.52"	"1"	"3.47"	"48"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc(F)c(F)cc3F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3931636"	""	"0"	"484.56"	"0"	"3.26"	"65"	"Cc1cc(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)c(C)o1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3233031"	""	"0"	"327.38"	"0"	"4.10"	"14"	"Cc1cccc(Nc2sc(-c3ccccc3F)cc2C(N)=O)n1"	"IC50"	"'='"	"36.0"	"nM"	"7.44"	""	""	"UO_0000065"	"22.74"	"0.44"	"3.34"	"10.95"	"False"	"CHEMBL3239499"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3232939"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3234876"	""	"0"	"377.39"	"0"	"4.98"	"21"	"Cc1cccc(Nc2sc(-c3cccc(C(F)(F)F)c3)cc2C(N)=O)n1"	"IC50"	"'='"	"690.0"	"nM"	"6.16"	""	""	"UO_0000065"	"16.33"	"0.32"	"1.18"	"9.06"	"False"	"CHEMBL3239499"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3232939"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3644973"	""	"0"	"453.47"	"0"	"4.86"	"BDBM99723"	"COc1ccc(C(F)(F)F)cc1-c1cccc2nc(Nc3ccc4c(c3)CCNCC4)nn12"	"IC50"	"'='"	"23.38"	"nM"	"7.63"	""	"216413"	"UO_0000065"	"16.83"	"0.32"	"2.77"	"12.02"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642372"	""	"0"	"519.68"	"1"	"4.29"	"BDBM99648"	"CN1CCC(c2ccc(Nc3nc4c(NCc5ccccc5N(C)S(C)(=O)=O)cccn4n3)cc2)CC1"	"IC50"	"'='"	"38.5"	"nM"	"7.42"	""	"216338"	"UO_0000065"	"14.27"	"0.27"	"3.12"	"7.82"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642378"	""	"0"	"551.68"	"2"	"1.99"	"BDBM99654"	"CN(c1ncccc1CNc1cccn2nc(Nc3ccc(N4CCN(CCO)CC4)cc3)nc12)S(C)(=O)=O"	"IC50"	"'='"	"36.05"	"nM"	"7.44"	""	"216344"	"UO_0000065"	"13.49"	"0.26"	"5.45"	"5.67"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3702938"	""	"0"	"392.37"	"0"	"1.95"	"BDBM147640"	"N#C[C@H]1C[C@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(OC(F)F)nc2)n1"	"IC50"	"'='"	"84.0"	"nM"	"7.08"	""	"285572"	"UO_0000065"	"18.03"	"0.35"	"5.13"	"5.09"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703497"	""	"0"	"317.35"	"0"	"3.95"	"BDBM153141"	"CCOC(=O)c1c[nH]c2ncnc(-c3ccc4ccccc4c3)c12"	"IC50"	"'='"	"186.0"	"nM"	"6.73"	""	"294089"	"UO_0000065"	"21.21"	"0.38"	"2.78"	"9.92"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703033"	""	"0"	"476.50"	"0"	"4.25"	"BDBM147743"	"C[C@H](N[C@@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(OC(F)(F)F)cc3)n2)[C@@H](C#N)C1)C1CC1"	"IC50"	"'='"	"200.0"	"nM"	"6.70"	""	"285677"	"UO_0000065"	"14.06"	"0.27"	"2.45"	"5.68"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651040"	""	"0"	"368.37"	"0"	"3.27"	"BDBM153217"	"C=C(CF)C(=O)Nc1cccc(-c2ncnc3[nH]cc(C(=O)OCC)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294165"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3644996"	""	"0"	"324.39"	"0"	"1.93"	"BDBM99748"	"CN1CCN(c2ccc(Nc3nc4c(O)cccn4n3)cc2)CC1"	"IC50"	"'='"	"566.68"	"nM"	"6.25"	""	"216436"	"UO_0000065"	"19.26"	"0.36"	"4.32"	"9.06"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642374"	""	"0"	"414.52"	"0"	"3.23"	"BDBM99650"	"CN1CCN(c2ccc(Nc3nc4c(NCc5cccnc5)cccn4n3)cc2)CC1"	"IC50"	"'='"	"487.83"	"nM"	"6.31"	""	"216340"	"UO_0000065"	"15.23"	"0.28"	"3.08"	"8.57"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3702970"	""	"0"	"484.50"	"0"	"2.81"	"BDBM147677"	"CN(C)[C@H]1CCC(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"285609"	"UO_0000065"	"17.13"	"0.34"	"5.49"	"6.19"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3747199"	""	"0"	"385.90"	"0"	"3.72"	"19"	"COc1ccc(-c2nc3c(N(C)CC4CCNCC4)c(Cl)cnc3[nH]2)cc1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3751000"	"Inhibition of N-terminal GST-fused recombinant JAK2 (831 to 1132 residues) (unknown origin) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate by microfluidic capillary electrophoresis method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3745697"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3745933"	""	"0"	"318.76"	"0"	"2.69"	"11"	"COc1ccc(-c2nc3c(NCCO)c(Cl)cnc3[nH]2)cc1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3751000"	"Inhibition of N-terminal GST-fused recombinant JAK2 (831 to 1132 residues) (unknown origin) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate by microfluidic capillary electrophoresis method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3745697"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3745829"	""	"0"	"415.93"	"0"	"4.05"	"7"	"COc1ccc(-c2nc3c(NCC4CCN(C)CC4)c(Cl)cnc3[nH]2)cc1OC"	"IC50"	"'='"	"9900.0"	"nM"	"5.00"	""	""	"UO_0000065"	"12.03"	"0.24"	"0.95"	"6.65"	"False"	"CHEMBL3751000"	"Inhibition of N-terminal GST-fused recombinant JAK2 (831 to 1132 residues) (unknown origin) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate by microfluidic capillary electrophoresis method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3745697"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3926059"	""	"0"	"319.37"	"0"	"1.94"	"BDBM228742"	"CN(c1ncccc1C#N)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399671"	"UO_0000065"	"32.12"	"0.58"	"8.32"	"12.11"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3960416"	""	"0"	"318.38"	"0"	"2.05"	"BDBM228743"	"C#Cc1ccc(N(C)[C@@H]2CCN(c3ncnc4[nH]ccc34)C2)nc1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399673"	"UO_0000065"	"32.22"	"0.58"	"8.21"	"16.84"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3922588"	""	"0"	"457.54"	"0"	"3.03"	"16d"	"CN1CCN(c2ccc(Nc3nccc(-c4cc5c(o4)CCN(C(=O)CC#N)C5)n3)cc2)CC1"	"IC50"	"'='"	"7443.0"	"nM"	"5.13"	""	""	"UO_0000065"	"11.21"	"0.21"	"2.10"	"5.05"	"False"	"CHEMBL3868067"	"Inhibition of JAK2 V617F mutant in human HEL cells after 1 hr"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3867460"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2017"	"CHEMBL3308090"	""
"CHEMBL3928955"	""	"0"	"382.42"	"0"	"0.95"	"BDBM229288"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)CO)CC1"	"IC50"	"'='"	"248.0"	"nM"	"6.61"	""	"401027"	"UO_0000065"	"17.27"	"0.32"	"5.66"	"4.81"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4108853"	""	"0"	"443.48"	"0"	"1.51"	"BDBM229299"	"CC(C)[C@@H](O)C(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CC1"	"IC50"	"'='"	"139.0"	"nM"	"6.86"	""	"401038"	"UO_0000065"	"15.46"	"0.29"	"5.35"	"4.57"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3893756"	""	"0"	"450.52"	"0"	"2.18"	"BDBM229340"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CN(S(=O)(=O)Cc2ccccc2)C1"	"IC50"	"'='"	"521.0"	"nM"	"6.28"	""	"401079"	"UO_0000065"	"13.95"	"0.27"	"4.10"	"4.69"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4113177"	""	"0"	"463.93"	"0"	"3.84"	"BDBM229354"	"Cc1cc(Cl)ccc1NC(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"334.0"	"nM"	"6.48"	""	"401093"	"UO_0000065"	"13.96"	"0.27"	"2.64"	"5.02"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3941640"	""	"0"	"443.51"	"0"	"3.44"	"BDBM229374"	"CCc1ccc(NC(=O)N2CC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)C2)cc1"	"IC50"	"'='"	"28.0"	"nM"	"7.55"	""	"401113"	"UO_0000065"	"17.03"	"0.31"	"4.11"	"5.85"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3938914"	""	"0"	"443.51"	"0"	"3.44"	"BDBM229375"	"CCc1cccc(NC(=O)N2CC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)C2)c1"	"IC50"	"'='"	"144.0"	"nM"	"6.84"	""	"401114"	"UO_0000065"	"15.43"	"0.28"	"3.40"	"5.30"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3889558"	""	"0"	"529.53"	"1"	"2.56"	"BDBM229382"	"CS(=O)(=O)c1ccc(Nc2nn(C3(CC#N)CN(C(=O)Nc4cc(F)ccc4F)C3)cc2C(N)=O)cc1"	"IC50"	"'='"	"237.0"	"nM"	"6.62"	""	"401121"	"UO_0000065"	"12.51"	"0.24"	"4.07"	"4.06"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3949820"	""	"0"	"355.37"	"0"	"2.62"	"BDBM229393"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(=O)CC1"	"IC50"	"'='"	"39.0"	"nM"	"7.41"	""	"401131"	"UO_0000065"	"20.85"	"0.39"	"4.79"	"6.51"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3931773"	""	"0"	"433.49"	"0"	"3.92"	"BDBM229402"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(Nc2ccccn2)CC1"	"IC50"	"'='"	"73.0"	"nM"	"7.14"	""	"401141"	"UO_0000065"	"16.46"	"0.30"	"3.22"	"5.87"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3914311"	""	"0"	"447.52"	"0"	"3.95"	"BDBM229405"	"CN(c1ccccc1)C1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CC1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"401144"	"UO_0000065"	"19.44"	"0.36"	"4.75"	"7.71"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3950253"	""	"0"	"451.48"	"0"	"4.06"	"BDBM228201"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(Nc2ccccc2F)CC1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"401146"	"UO_0000065"	"19.93"	"0.37"	"4.94"	"7.40"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3950253"	""	"0"	"451.48"	"0"	"4.06"	"BDBM228201"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(Nc2ccccc2F)CC1"	"IC50"	"'='"	"184.0"	"nM"	"6.74"	""	"401153"	"UO_0000065"	"14.92"	"0.28"	"2.68"	"5.54"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3900088"	""	"0"	"440.52"	"0"	"2.87"	"BDBM228218"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(N2CCC(O)CC2)CC1"	"IC50"	"'='"	"273.0"	"nM"	"6.56"	""	"401156"	"UO_0000065"	"14.90"	"0.28"	"3.69"	"5.46"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3971240"	""	"0"	"518.63"	"1"	"4.53"	"BDBM229413"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc([S+]([O-])C(F)F)cc3)n2)CCC(NC2CCCCC2)CC1"	"IC50"	"'='"	"32.0"	"nM"	"7.50"	""	"401157"	"UO_0000065"	"14.45"	"0.28"	"2.96"	"5.96"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3893735"	""	"0"	"467.94"	"0"	"4.58"	"BDBM229414"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(Nc2cccc(Cl)c2)CC1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"401158"	"UO_0000065"	"17.95"	"0.35"	"3.82"	"6.90"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3946178"	""	"0"	"468.48"	"0"	"4.81"	"BDBM229419"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(Nc2ccc(F)c(F)c2)CC1"	"IC50"	"'='"	"30.0"	"nM"	"7.52"	""	"401164"	"UO_0000065"	"16.06"	"0.30"	"2.71"	"6.92"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3933473"	""	"0"	"469.47"	"0"	"4.20"	"BDBM228213"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(Nc2ccc(F)c(F)c2)CC1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"401165"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3900088"	""	"0"	"440.52"	"0"	"2.87"	"BDBM228218"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(N2CCC(O)CC2)CC1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"401170"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3906584"	""	"0"	"548.66"	"1"	"4.19"	"BDBM228219"	"CC(C)S(=O)(=O)c1ccc(Nc2nn(C3(CC#N)CCC(N4CCC(F)(F)CC4)CC3)cc2C(N)=O)cc1"	"IC50"	"'='"	"775.0"	"nM"	"6.11"	""	"401171"	"UO_0000065"	"11.14"	"0.22"	"1.92"	"4.56"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3942031"	""	"0"	"467.94"	"0"	"4.58"	"BDBM228238"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(Nc2ccc(Cl)cc2)CC1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"401190"	"UO_0000065"	"18.21"	"0.35"	"3.94"	"7.01"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3904265"	""	"0"	"469.47"	"0"	"4.20"	"BDBM228240"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(Nc2ccc(F)cc2F)CC1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"401192"	"UO_0000065"	"19.17"	"0.36"	"4.80"	"7.40"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3981419"	""	"0"	"410.50"	"0"	"3.42"	"BDBM229438"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(NCC2CC2)CC1"	"IC50"	"'='"	"667.0"	"nM"	"6.18"	""	"401198"	"UO_0000065"	"15.04"	"0.28"	"2.76"	"5.68"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3894605"	""	"0"	"414.49"	"0"	"2.65"	"BDBM229440"	"COCCNC1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CC1"	"IC50"	"'='"	"814.0"	"nM"	"6.09"	""	"401200"	"UO_0000065"	"14.69"	"0.28"	"3.44"	"5.16"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3936267"	""	"0"	"420.44"	"0"	"3.27"	"BDBM229445"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(NCC(F)F)CC1"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	"401206"	"UO_0000065"	"18.76"	"0.36"	"4.62"	"7.25"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3928653"	""	"0"	"446.53"	"0"	"4.21"	"BDBM229473"	"N#CC[C@]1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CC[C@@H](NCc2ccccc2)CC1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"401235"	"UO_0000065"	"19.48"	"0.36"	"4.49"	"8.00"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3915313"	""	"0"	"483.50"	"0"	"3.88"	"BDBM229478"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(NCc2ccc(F)cc2F)CC1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"401241"	"UO_0000065"	"17.99"	"0.34"	"4.82"	"7.15"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3938257"	""	"0"	"463.52"	"0"	"3.31"	"BDBM229481"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(NCc2ccccc2O)CC1"	"IC50"	"'='"	"468.0"	"nM"	"6.33"	""	"401244"	"UO_0000065"	"13.66"	"0.25"	"3.02"	"4.46"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3895727"	""	"0"	"447.52"	"0"	"3.60"	"BDBM229490"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(NCc2ccccc2)CC1"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	"401255"	"UO_0000065"	"17.88"	"0.33"	"4.40"	"6.58"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3898012"	""	"0"	"453.40"	"0"	"2.09"	"BDBM229498"	"CC(F)(F)C(=O)N1CC[C@](CC#N)(n2cc(C(N)=O)c(Nc3ccc(F)nc3)n2)[C@@H](F)C1"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	"401267"	"UO_0000065"	"17.39"	"0.34"	"5.80"	"6.07"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3972665"	""	"0"	"453.40"	"0"	"2.09"	"BDBM229502"	"CC(F)(F)C(=O)N1CC[C@@](CC#N)(n2cc(C(N)=O)c(Nc3ccc(F)nc3)n2)[C@@H](F)C1"	"IC50"	"'='"	"0.1"	"nM"	"10.00"	""	"401270"	"UO_0000065"	"22.06"	"0.43"	"7.91"	"7.70"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3218297"	""	"0"	"422.49"	"0"	"3.23"	"5g-Mes"	"CS(=O)(=O)O.O=C(NCc1cccc(O)c1)Nc1nc(-c2ccncc2)cs1"	"IC50"	"'<'"	"1.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3224485"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3217586"	"1"	"Scientific Literature"	"MedChemComm"	"2012"	"None"	""
"CHEMBL3911503"	""	"0"	"454.55"	"0"	"3.05"	"BDBM237824"	"CC(C)(O)C1CC(CN2CC[C@@H](C#N)[C@H](n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)C2)C1"	"IC50"	"'='"	"533.0"	"nM"	"6.27"	""	"414928"	"UO_0000065"	"13.80"	"0.26"	"3.22"	"5.22"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4107067"	""	"0"	"420.45"	"0"	"2.24"	"BDBM237835"	"N#C[C@@H]1CN(Cc2cccnn2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"220.0"	"nM"	"6.66"	""	"414939"	"UO_0000065"	"15.83"	"0.29"	"4.42"	"5.29"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3943572"	""	"0"	"359.44"	"0"	"2.72"	"BDBM228679"	"N#Cc1ccc(N(CC2CC2)[C@@H]2CCN(c3ncnc4[nH]ccc34)C2)nc1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399660"	"UO_0000065"	"28.54"	"0.52"	"7.54"	"12.11"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3951178"	""	"0"	"334.39"	"0"	"1.94"	"BDBM228680"	"CN(c1cc2cn[nH]c2cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399661"	"UO_0000065"	"30.68"	"0.56"	"8.32"	"11.45"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4112280"	""	"0"	"422.47"	"0"	"2.18"	"BDBM237839"	"Cn1ccc(CN2CC[C@@H](n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)[C@H](C#N)C2)n1"	"IC50"	"'='"	"148.0"	"nM"	"6.83"	""	"414943"	"UO_0000065"	"16.17"	"0.30"	"4.65"	"5.80"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4111931"	""	"0"	"436.50"	"0"	"2.49"	"BDBM237847"	"Cc1c(CN2CC[C@@H](n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)[C@H](C#N)C2)cnn1C"	"IC50"	"'='"	"111.0"	"nM"	"6.96"	""	"414951"	"UO_0000065"	"15.93"	"0.30"	"4.46"	"5.90"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4640690"	""	"0"	"381.84"	"1"	"5.74"	"16g"	"CC(Oc1cc(-c2c[nH]c3ccccc23)cnc1N)c1cc(F)ccc1Cl"	"IC50"	"'='"	"925.0"	"nM"	"6.03"	""	""	"UO_0000065"	"15.80"	"0.31"	"0.29"	"9.44"	"False"	"CHEMBL4628503"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4627317"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL4107174"	""	"0"	"420.45"	"0"	"2.24"	"BDBM237836"	"N#C[C@@H]1CN(Cc2cnccn2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"75.0"	"nM"	"7.12"	""	"414940"	"UO_0000065"	"16.95"	"0.31"	"4.88"	"5.67"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4294002"	""	"0"	"476.46"	"0"	"3.92"	"19b"	"COc1cc2c(=O)n([C@@H](C(=O)NCC(F)(F)F)C(C)C)c3c4cc[nH]c4ncc3c2cc1OC"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4261266"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]-ATP addition measured after 2 hrs by filter-binding method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257589"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4287893"	""	"0"	"378.43"	"0"	"2.97"	"17h"	"COc1cc2c(=O)n([C@@H]3CCCNC3)c3c4cc[nH]c4ncc3c2cc1OC"	"IC50"	"'='"	"8.91"	"nM"	"8.05"	""	""	"UO_0000065"	"21.27"	"0.39"	"5.08"	"9.92"	"False"	"CHEMBL4261266"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]-ATP addition measured after 2 hrs by filter-binding method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257589"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4281080"	""	"0"	"405.50"	"1"	"5.33"	"17d"	"COc1cc2c(=O)n(C3CCCCCCC3)c3c4cc[nH]c4ncc3c2cc1OC"	"IC50"	"'='"	"1.82"	"nM"	"8.74"	""	""	"UO_0000065"	"21.55"	"0.40"	"3.41"	"12.64"	"False"	"CHEMBL4261266"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]-ATP addition measured after 2 hrs by filter-binding method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257589"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4291720"	""	"0"	"391.47"	"0"	"4.94"	"17c"	"COc1cc2c(=O)n(C3CCCCCC3)c3c4cc[nH]c4ncc3c2cc1OC"	"IC50"	"'='"	"0.89"	"nM"	"9.05"	""	""	"UO_0000065"	"23.12"	"0.43"	"4.11"	"13.09"	"False"	"CHEMBL4261266"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]-ATP addition measured after 2 hrs by filter-binding method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257589"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4295151"	""	"0"	"377.44"	"0"	"4.55"	"17a"	"COc1cc2c(=O)n(C3CCCCC3)c3c4cc[nH]c4ncc3c2cc1OC"	"IC50"	"'='"	"1.07"	"nM"	"8.97"	""	""	"UO_0000065"	"23.77"	"0.44"	"4.42"	"12.97"	"False"	"CHEMBL4261266"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]-ATP addition measured after 2 hrs by filter-binding method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257589"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4278842"	""	"0"	"367.36"	"0"	"2.22"	"13b"	"COC(=O)Cn1c(=O)c2cc(OC)c(OC)cc2c2cnc3[nH]ccc3c21"	"IC50"	"'='"	"17.56"	"nM"	"7.75"	""	""	"UO_0000065"	"21.11"	"0.39"	"5.54"	"8.13"	"False"	"CHEMBL4261266"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]-ATP addition measured after 2 hrs by filter-binding method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257589"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4277379"	""	"0"	"365.39"	"0"	"2.89"	"7b"	"CN(C)CCCn1c(=O)c2cc([N+](=O)[O-])ccc2c2cnc3[nH]ccc3c21"	"IC50"	"'='"	"489.65"	"nM"	"6.31"	""	""	"UO_0000065"	"17.27"	"0.32"	"3.42"	"6.50"	"False"	"CHEMBL4261266"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]-ATP addition measured after 2 hrs by filter-binding method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257589"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4516300"	""	"0"	"342.80"	"1"	"5.26"	"16a"	"CC(Oc1cc(-c2ccccc2)cnc1N)c1cc(F)ccc1Cl"	"IC50"	"'='"	"461.0"	"nM"	"6.34"	""	""	"UO_0000065"	"18.48"	"0.36"	"1.08"	"13.16"	"False"	"CHEMBL4628503"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4627317"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL4293778"	""	"0"	"289.34"	"0"	"2.86"	"22"	"CC1(NC#N)CCc2ccc(-c3ncnc4[nH]ccc34)cc21"	"IC50"	"'='"	"97.0"	"nM"	"7.01"	""	""	"UO_0000065"	"24.24"	"0.44"	"4.15"	"9.06"	"False"	"CHEMBL4265556"	"Inhibition of recombinant human GST-tagged JAK2 using KAIETDKEYYTVKD-NH2 as substrate in presence of 1 mM ATP concentration by coupled PK/LDH assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4261650"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4290377"	""	"0"	"289.34"	"0"	"2.86"	"24"	"C[C@@]1(NC#N)CCc2ccc(-c3ncnc4[nH]ccc34)cc21"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4265556"	"Inhibition of recombinant human GST-tagged JAK2 using KAIETDKEYYTVKD-NH2 as substrate in presence of 1 mM ATP concentration by coupled PK/LDH assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4261650"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4283921"	""	"0"	"500.00"	"0"	"4.68"	"45i"	"CC(=O)Nc1ccc(-c2ccnc(Nc3ccc(OCCCCCCC(=O)NO)cc3)n2)cc1.Cl"	"IC50"	"'='"	"23.0"	"nM"	"7.64"	""	""	"UO_0000065"	"16.48"	"0.31"	"2.96"	"6.09"	"False"	"CHEMBL4268221"	"Inhibition of human JAK2 using poly(Glu:Tyr)(4:1) as substrate preincubated for 20 mins followed by [gamma33P]ATP addition measured after 120 mins by ion exchange filter paper method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4265943"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2018"	"None"	""
"CHEMBL2208028"	""	"0"	"403.49"	"0"	"3.99"	"49b"	"CC(=O)Nc1ccc(-c2nc(Nc3ccc(N4CCOCC4)cc3)ncc2C)cc1"	"IC50"	"'='"	"28.7"	"nM"	"7.54"	""	""	"UO_0000065"	"18.69"	"0.34"	"3.55"	"9.50"	"False"	"CHEMBL4268221"	"Inhibition of human JAK2 using poly(Glu:Tyr)(4:1) as substrate preincubated for 20 mins followed by [gamma33P]ATP addition measured after 120 mins by ion exchange filter paper method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4265943"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2018"	"None"	""
"CHEMBL2208024"	""	"0"	"387.49"	"0"	"4.84"	"64d"	"CC(=O)Nc1ccc(-c2ccnc(Nc3cccc(N4CCCCC4)c3)n2)cc1"	"IC50"	"'='"	"13.8"	"nM"	"7.86"	""	""	"UO_0000065"	"20.28"	"0.37"	"3.02"	"11.20"	"False"	"CHEMBL4268221"	"Inhibition of human JAK2 using poly(Glu:Tyr)(4:1) as substrate preincubated for 20 mins followed by [gamma33P]ATP addition measured after 120 mins by ion exchange filter paper method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4265943"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2018"	"None"	""
"CHEMBL4292408"	""	"0"	"531.66"	"1"	"4.42"	"69f"	"CN1CCN(c2ccc(Nc3nccc(-c4ccc(NC(=O)CCCCCCC(=O)NO)cc4)n3)cc2)CC1"	"IC50"	"'='"	"4.6"	"nM"	"8.34"	""	""	"UO_0000065"	"15.68"	"0.29"	"3.92"	"6.79"	"False"	"CHEMBL4268221"	"Inhibition of human JAK2 using poly(Glu:Tyr)(4:1) as substrate preincubated for 20 mins followed by [gamma33P]ATP addition measured after 120 mins by ion exchange filter paper method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4265943"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2018"	"None"	""
"CHEMBL3703071"	""	"0"	"383.43"	"0"	"2.20"	"BDBM147782"	"N#C[C@H]1C[C@H](N2CCC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccnc(F)c2)n1"	"IC50"	"'='"	"69.0"	"nM"	"7.16"	""	"285716"	"UO_0000065"	"18.68"	"0.35"	"4.96"	"6.35"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3593771"	""	"0"	"361.41"	"0"	"2.01"	"3"	"N#Cc1ccc(N2CCC(Nc3c(C(N)=O)cnc4[nH]ccc34)CC2)nc1"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	""	"UO_0000065"	"21.43"	"0.39"	"5.73"	"6.26"	"False"	"CHEMBL4429528"	"Inhibition of human JAK2 assessed as reduction in phosphorylation of Biotin-Lyn-Substrate-2 after 1 hr in presence of ATP by ELISA"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4428070"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2016"	"None"	""
"CHEMBL4523034"	""	"0"	"468.52"	"0"	"3.72"	"14i"	"Cc1nc2ccc(Nc3cc(NC4CCN(c5ccc(C#N)cn5)CC4)c(C(N)=O)cn3)cc2o1"	"IC50"	"'='"	"130.0"	"nM"	"6.89"	""	""	"UO_0000065"	"14.70"	"0.27"	"3.17"	"4.72"	"False"	"CHEMBL4429528"	"Inhibition of human JAK2 assessed as reduction in phosphorylation of Biotin-Lyn-Substrate-2 after 1 hr in presence of ATP by ELISA"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4428070"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2016"	"None"	""
"CHEMBL4125719"	""	"0"	"382.43"	"1"	"5.11"	"27"	"N#CC(C#N)=Cc1ccc(-c2nc3cnc4[nH]ccc4c3n2C2CCCCC2)o1"	"IC50"	"'='"	"188.0"	"nM"	"6.73"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4124183"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate in presence of 10 uM [gamma33P]ATP by radiometric method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4118225"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3642273"	""	"0"	"402.48"	"0"	"1.56"	"BDBM99535"	"COc1ccc(Nc2nc3c(N4CCN(S(C)(=O)=O)CC4)cccn3n2)cc1"	"IC50"	"'='"	"60.4"	"nM"	"7.22"	""	"216227"	"UO_0000065"	"17.94"	"0.35"	"5.66"	"7.84"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3645006"	""	"0"	"368.40"	"0"	"4.09"	"BDBM99758"	"COc1ncccc1-c1cccn2nc(Nc3ccc4ncccc4c3)nc12"	"IC50"	"'='"	"191.93"	"nM"	"6.72"	""	"216446"	"UO_0000065"	"18.23"	"0.33"	"2.63"	"8.70"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3665142"	""	"0"	"414.54"	"0"	"2.88"	"BDBM112529"	"CCCS(=O)(=O)N1C[C@@H](C)C[C@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.0676"	"nM"	"10.17"	""	"233768"	"UO_0000065"	"24.53"	"0.48"	"7.29"	"9.79"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3648433"	""	"0"	"357.39"	"0"	"2.21"	"BDBM107142"	"CS(=O)(=O)OCC(=O)Nc1cccc(-c2cnc3ccccc3n2)c1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	"226380"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3694585"	""	"0"	"366.85"	"0"	"4.46"	"BDBM125906"	"Clc1cnc2nc1NCCc1cccc(c1)OCCc1cccc(c1)N2"	"IC50"	"'='"	"23.0"	"nM"	"7.64"	""	"255679"	"UO_0000065"	"20.82"	"0.40"	"3.18"	"12.93"	"False"	"CHEMBL3707544"	"In Vitro Kinase Assay: One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Biochemistry 1999, 269, 94-104. The catalytic domains of human JAK1 (a.a. 837-1142), JAK2 (a.a. 828-1132) and JAK3 (a.a. 781-1124) with an N-terminal His tag were expressed using baculovirus in insect cells and purified. The catalytic activity of JAK1, JAK2 or JAK3 was assayed by measuring the phosphorylation of a biotinylated peptide. The phosphorylated peptide was detected by homogenous time resolved fluorescence (HTRF). IC50s of compounds were measured for each kinase in the reactions that contain the enzyme, ATP and 500 nM peptide in 50 mM Tris (pH 7.8) buffer with 100 mM NaCl, 5 mM DTT, and 0.1 mg/mL (0.01%) BSA. The ATP concentration in the reactions was 90 uM for JAK1, 30 uM for JAK2 and 3 uM for JAK3. Reactions were carried out at room temperature for 1 hr and then stopped with 20 uL 45 mM EDTA."	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639093"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3785951"	""	"0"	"508.60"	"1"	"3.25"	"33"	"CC(=O)N1CCN([C@H]2C[C@@H](n3cc(-c4cc(OC[C@@H]5CCCO5)ccc4F)c4c(N)ncnc43)C2)CC1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3789994"	"Inhibition of JAK2 (unknown origin) in presence of [gamma33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3785066"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL4642719"	""	"0"	"344.78"	"0"	"4.05"	"16c"	"CC(Oc1cc(-c2cncnc2)cnc1N)c1cc(F)ccc1Cl"	"IC50"	"'='"	"566.0"	"nM"	"6.25"	""	""	"UO_0000065"	"18.12"	"0.36"	"2.20"	"8.45"	"False"	"CHEMBL4628503"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4627317"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL4646543"	""	"0"	"381.84"	"1"	"5.74"	"16h"	"CC(Oc1cc(-c2cc3ccccc3[nH]2)cnc1N)c1cc(F)ccc1Cl"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4628503"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4627317"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL3114781"	""	"0"	"418.43"	"0"	"3.19"	"10a"	"O=C1NC(=O)C(c2ccccc2)=C1Nc1cccc(OCCNc2ccnc(F)c2)c1"	"IC50"	"'='"	"11080.0"	"nM"	"4.96"	""	""	"UO_0000065"	"11.84"	"0.22"	"1.77"	"5.37"	"False"	"CHEMBL3118993"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112442"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3642298"	""	"0"	"462.58"	"0"	"3.30"	"BDBM99568"	"CN1CCN(c2ccc(Nc3nc4c(-c5ccccc5S(C)(=O)=O)cccn4n3)cc2)CC1"	"IC50"	"'='"	"1326.3"	"nM"	"5.88"	""	"216258"	"UO_0000065"	"12.71"	"0.24"	"2.58"	"7.09"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"1"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"10.7"	"nM"	"7.97"	""	""	"UO_0000065"	"25.52"	"0.47"	"6.43"	"8.96"	"False"	"CHEMBL3118993"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112442"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL4641716"	""	"0"	"386.42"	"0"	"2.34"	"J-4"	"N#CC1CN(C(=O)c2ccc(-c3cccc4nc(NC(=O)C5CC5)nn34)cc2)C1"	"IC50"	"'='"	"79.0"	"nM"	"7.10"	""	""	"UO_0000065"	"18.38"	"0.33"	"4.76"	"6.87"	"False"	"CHEMBL4624516"	"Inhibition of JAK2 (unknown origin) in presence of ATP at Km concentration by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4622902"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL2105759"	"BARICITINIB"	"4"	"371.43"	"0"	"1.10"	"Baricitinib"	"CCS(=O)(=O)N1CC(CC#N)(n2cc(-c3ncnc4[nH]ccc34)cn2)C1"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	""	"UO_0000065"	"21.96"	"0.43"	"7.05"	"6.76"	"True"	"CHEMBL3803216"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797141"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2016"	"None"	""
"CHEMBL3977697"	""	"0"	"426.45"	"0"	"2.80"	"BDBM237802"	"N#C[C@@H]1CCN(C(=O)OCC2CC2)C[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"52.0"	"nM"	"7.28"	""	"414906"	"UO_0000065"	"17.08"	"0.32"	"4.48"	"5.77"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3972715"	""	"0"	"430.44"	"0"	"2.03"	"BDBM237804"	"COCCOC(=O)N1CC[C@@H](C#N)[C@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)C1"	"IC50"	"'='"	"120.0"	"nM"	"6.92"	""	"414908"	"UO_0000065"	"16.08"	"0.30"	"4.89"	"5.11"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3939728"	""	"0"	"458.45"	"0"	"1.95"	"BDBM237805"	"CCOC(=O)COC(=O)N1CC[C@@H](C#N)[C@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)C1"	"IC50"	"'='"	"187.0"	"nM"	"6.73"	""	"414909"	"UO_0000065"	"14.68"	"0.28"	"4.78"	"4.41"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3961679"	""	"0"	"456.48"	"0"	"2.57"	"BDBM237806"	"N#C[C@@H]1CCN(C(=O)OC2CCOCC2)C[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"87.0"	"nM"	"7.06"	""	"414910"	"UO_0000065"	"15.47"	"0.29"	"4.49"	"5.21"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3908048"	""	"0"	"440.48"	"0"	"3.19"	"BDBM237812"	"N#C[C@@H]1CCN(C(=O)OCCC2CC2)C[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"76.0"	"nM"	"7.12"	""	"414916"	"UO_0000065"	"16.16"	"0.30"	"3.93"	"5.64"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3944948"	""	"0"	"420.45"	"0"	"2.24"	"BDBM237815"	"N#C[C@@H]1CCN(Cc2cnccn2)C[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"26.0"	"nM"	"7.58"	""	"414919"	"UO_0000065"	"18.04"	"0.33"	"5.35"	"6.03"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3889987"	""	"0"	"436.50"	"0"	"2.49"	"BDBM237828"	"Cc1c(CN2CC[C@@H](C#N)[C@H](n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)C2)cnn1C"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	"414932"	"UO_0000065"	"17.64"	"0.33"	"5.21"	"6.54"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3912265"	""	"0"	"425.49"	"0"	"2.91"	"BDBM237854"	"N#C[C@@H]1CCN(Cc2cncs2)C[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"414958"	"UO_0000065"	"19.32"	"0.37"	"5.31"	"7.28"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4113190"	""	"0"	"381.44"	"0"	"2.11"	"BDBM237889"	"CC1(c2ccc(Nc3nn([C@H]4COCC[C@@H]4C#N)cc3C(N)=O)cc2)COC1"	"IC50"	"'='"	"0.6"	"nM"	"9.22"	""	"414991"	"UO_0000065"	"24.18"	"0.45"	"7.11"	"8.01"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4114959"	""	"0"	"437.45"	"0"	"2.99"	"BDBM237841"	"N#C[C@@H]1CN(Cc2cncc(F)c2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"58.0"	"nM"	"7.24"	""	"414945"	"UO_0000065"	"16.54"	"0.31"	"4.25"	"6.41"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4109347"	""	"0"	"440.52"	"0"	"3.07"	"BDBM237844"	"N#C[C@@H]1CN(CCC2CCOCC2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"258.0"	"nM"	"6.59"	""	"414948"	"UO_0000065"	"14.96"	"0.28"	"3.52"	"6.03"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4109793"	""	"0"	"427.41"	"0"	"2.24"	"BDBM60976"	"N#C[C@@H]1CS(=O)(=O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"371.0"	"nM"	"6.43"	""	"414963"	"UO_0000065"	"15.05"	"0.30"	"4.19"	"4.91"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3909589"	""	"0"	"364.36"	"0"	"0.37"	"BDBM237863"	"N#C[C@H]1CS(=O)(=O)C[C@H]1n1cc(C(N)=O)c(Nc2ccnc(F)c2)n1"	"IC50"	"'='"	"96.0"	"nM"	"7.02"	""	"414967"	"UO_0000065"	"19.26"	"0.38"	"6.65"	"4.88"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4111202"	""	"0"	"380.24"	"0"	"3.13"	"BDBM237875"	"N#C[C@H]1CCOC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)c(Cl)c2)n1"	"IC50"	"'='"	"245.0"	"nM"	"6.61"	""	"414977"	"UO_0000065"	"17.39"	"0.36"	"3.48"	"6.24"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4111885"	""	"0"	"363.37"	"0"	"0.97"	"BDBM237861"	"N#C[C@@H]1CS(=O)(=O)C[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"415010"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3972345"	""	"0"	"377.40"	"0"	"1.36"	"BDBM237911"	"C[C@]1(C#N)CS(=O)(=O)CC1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"415016"	"UO_0000065"	"21.79"	"0.43"	"6.86"	"6.28"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3642295"	""	"0"	"491.62"	"0"	"3.29"	"BDBM99564"	"CN1CCN(c2ccc(Nc3nc4c(-c5ccc(N(C)S(C)(=O)=O)cc5)cccn4n3)cc2)CC1"	"IC50"	"'='"	"0.6"	"nM"	"9.22"	""	"216254"	"UO_0000065"	"18.76"	"0.36"	"5.93"	"10.71"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647816"	""	"0"	"518.58"	"1"	"4.36"	"BDBM147921"	"CC(C)(O)C1CC(CN[C@H]2CC[C@@H](n3cc(C(N)=O)c(Nc4ccc(C(F)(F)F)cc4)n3)[C@H](C#N)C2)C1"	"IC50"	"'='"	"265.0"	"nM"	"6.58"	""	"285855"	"UO_0000065"	"12.68"	"0.24"	"2.22"	"5.10"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645017"	""	"0"	"401.47"	"0"	"3.41"	"BDBM99769"	"COc1cnc(-c2cccn3nc(Nc4ccc(C5CCNCC5)cc4)nc23)cn1"	"IC50"	"'='"	"73.75"	"nM"	"7.13"	""	"216456"	"UO_0000065"	"17.77"	"0.32"	"3.72"	"7.99"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3651036"	""	"0"	"350.38"	"0"	"2.95"	"BDBM153213"	"C=CC(=O)N(C)c1cccc(-c2ncnc3[nH]cc(C(=O)OCC)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294161"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3622148"	""	"0"	"446.56"	"0"	"3.98"	"12"	"CCn1nc(Nc2nc3c(cc(C(=O)N(C4CC4)C4CC4)n3CC)c3c2ncn3C)cc1C"	"IC50"	"'='"	"1.5"	"nM"	"8.82"	""	""	"UO_0000065"	"19.76"	"0.37"	"4.84"	"10.28"	"False"	"CHEMBL3625512"	"Inhibition of recombinant JAK2 (unknown origin) using 5-FAM-KKKKEEIYFFFG-OH substrate and ATP incubated for 180 mins by scintillation counting method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621135"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL4637163"	""	"0"	"308.39"	"0"	"2.95"	"1"	"N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3c2CCN3)cn1"	"IC50"	"'='"	"5.7"	"nM"	"8.24"	""	""	"UO_0000065"	"26.73"	"0.49"	"5.29"	"10.38"	"False"	"CHEMBL4628501"	"Inhibition of recombinant epitope-tagged JAK2 (828-1132 residues) (unknown origin) in presence of ATP by time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4627317"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL4645876"	""	"0"	"382.83"	"1"	"5.14"	"16j"	"CC(Oc1cc(-c2c[nH]c3ccncc23)cnc1N)c1cc(F)ccc1Cl"	"IC50"	"'='"	"22.0"	"nM"	"7.66"	""	""	"UO_0000065"	"20.00"	"0.39"	"2.52"	"9.97"	"False"	"CHEMBL4628503"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4627317"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL2035047"	""	"0"	"362.43"	"0"	"4.00"	"13g, 95:5 trans/Cis mixture"	"CN1C/C=C/COCc2ccc(o2)-c2ccnc(n2)Nc2cccc(c2)C1"	"IC50"	"'='"	"820.0"	"nM"	"6.09"	""	""	"UO_0000065"	"16.79"	"0.31"	"2.09"	"9.60"	"False"	"CHEMBL2040119"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2034857"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2035181"	""	"0"	"462.55"	"0"	"4.56"	"14n, 95:5 trans/Cis mixture"	"C1=C/COCc2cc(ccc2OCCN2CCCC2)Nc2nccc(n2)-c2cc(co2)COC/1"	"IC50"	"'='"	"110.0"	"nM"	"6.96"	""	""	"UO_0000065"	"15.04"	"0.28"	"2.40"	"8.50"	"False"	"CHEMBL2040119"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2034857"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL3642271"	""	"0"	"338.42"	"0"	"2.23"	"BDBM99532"	"COc1ccc(Nc2nc3c(N4CCN(C)CC4)cccn3n2)cc1"	"IC50"	"'='"	"440.6"	"nM"	"6.36"	""	"216224"	"UO_0000065"	"18.78"	"0.35"	"4.13"	"10.97"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3940483"	""	"0"	"384.45"	"0"	"2.93"	"BDBM198421"	"c1cnc2cc(CN3CCC(c4nnn5cnc6[nH]ccc6c45)CC3)ccc2n1"	"IC50"	"'='"	"140.0"	"nM"	"6.85"	""	"352499"	"UO_0000065"	"17.83"	"0.32"	"3.92"	"7.80"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3979988"	""	"0"	"356.82"	"0"	"3.23"	"BDBM198431"	"Clc1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)o1"	"IC50"	"'='"	"4.4"	"nM"	"8.36"	""	"352509"	"UO_0000065"	"23.42"	"0.46"	"5.13"	"11.11"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4115251"	""	"0"	"390.50"	"0"	"2.79"	"BDBM198435"	"c1cc[n+]2cc(CN3CCC(c4nnn5cnc6[nH]ccc6c45)CC3)sc2c1"	"IC50"	"'='"	"33.0"	"nM"	"7.48"	""	"352513"	"UO_0000065"	"19.16"	"0.36"	"4.69"	"11.30"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3920091"	""	"0"	"370.48"	"0"	"2.50"	"BDBM198456"	"O=C1SCCC1NC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"6.6"	"nM"	"8.18"	""	"352534"	"UO_0000065"	"22.08"	"0.43"	"5.68"	"9.30"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3947889"	""	"0"	"342.47"	"0"	"2.89"	"BDBM198457"	"c1cc2c(ncn3nnc([C@H]4CC[C@H](CN5CCSC5)CC4)c23)[nH]1"	"IC50"	"'='"	"24.0"	"nM"	"7.62"	""	"352535"	"UO_0000065"	"22.25"	"0.43"	"4.73"	"12.27"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3943055"	""	"0"	"589.00"	"2"	"5.55"	"BDBM230088"	"Cc1c(-c2c(Cl)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)[nH]c2c(F)cc(F)cc2c1=O"	"IC50"	"'>'"	"2000.0"	"nM"	""	""	"402021"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3908440"	""	"0"	"571.01"	"2"	"5.41"	"BDBM230124"	"Cc1c(-c2c(F)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)[nH]c2c(Cl)cccc2c1=O"	"IC50"	"'='"	"2200.0"	"nM"	"5.66"	""	"402064"	"UO_0000065"	"9.91"	"0.19"	"0.25"	"4.22"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3918580"	""	"0"	"502.57"	"2"	"5.32"	"BDBM230144"	"Cc1c(-c2ccc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1cnc2ccccc2c1=O"	"IC50"	"'='"	"240.0"	"nM"	"6.62"	""	"402086"	"UO_0000065"	"13.17"	"0.24"	"1.30"	"5.81"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3645064"	""	"0"	"517.61"	"2"	"6.40"	"BDBM99832"	"COc1cccc(-c2cccn3nc(Nc4ccc(C5CCN(C(=O)OC(C)(C)C)CC5)cc4)nc23)c1F"	"IC50"	"'='"	"529.59"	"nM"	"6.28"	""	"216505"	"UO_0000065"	"12.13"	"0.23"	"-0.12"	"7.75"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652286"	""	"0"	"423.54"	"0"	"0.71"	"BDBM113095"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC[C@@H](O)[C@@H](O)C2)CC1"	"IC50"	"'='"	"32.0"	"nM"	"7.50"	""	"234539"	"UO_0000065"	"17.70"	"0.35"	"6.78"	"6.11"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3651005"	""	"0"	"364.41"	"0"	"3.62"	"BDBM153181"	"C=C(C)C(=O)Nc1cc(C)cc(-c2ncnc3[nH]cc(C(=O)OCC)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294129"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3917906"	""	"0"	"413.51"	"0"	"1.51"	"BDBM228694"	"CN(c1ccc(S(=O)(=O)NC2CC2)cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399694"	"UO_0000065"	"24.81"	"0.48"	"8.75"	"9.58"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3944322"	""	"0"	"428.93"	"0"	"3.09"	"BDBM239955"	"Cn1cc(Nc2ncc(Cl)c(NC3CCC4(CC3)CCN(C(=O)CC#N)C4)n2)cn1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"418575"	"UO_0000065"	"19.35"	"0.38"	"5.21"	"7.43"	"False"	"CHEMBL3888834"	"Kinase Assay: JAK2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 100 μM KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC, 10 mM MgAcetate and [γ-33P-ATP](specific activity approx. 500 cpm/pmol, concentration as required). The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of 3% phosphoric acid solution. 10 μL of the reaction is then spotted onto a P30 filtermat and washed three times for 5 minutes in 75 mM phosphoric acid and once in methanol prior to drying and scintillation counting."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886854"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3902637"	""	"0"	"478.00"	"0"	"4.52"	"BDBM239962"	"Cn1cc(Nc2ncc(Cl)c(NC3CCC4(CC3)CCN(c3ccc(C#N)cn3)CC4)n2)cn1"	"IC50"	"'='"	"23.0"	"nM"	"7.64"	""	"418582"	"UO_0000065"	"15.98"	"0.31"	"3.12"	"7.10"	"False"	"CHEMBL3888834"	"Kinase Assay: JAK2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 100 μM KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC, 10 mM MgAcetate and [γ-33P-ATP](specific activity approx. 500 cpm/pmol, concentration as required). The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of 3% phosphoric acid solution. 10 μL of the reaction is then spotted onto a P30 filtermat and washed three times for 5 minutes in 75 mM phosphoric acid and once in methanol prior to drying and scintillation counting."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886854"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3977733"	""	"0"	"442.96"	"0"	"3.48"	"BDBM239974"	"Cn1cnc(Nc2ncc(Cl)c(NC3CCC4(CC3)CCN(C(=O)CC#N)CC4)n2)c1"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	"418594"	"UO_0000065"	"17.88"	"0.35"	"4.44"	"7.09"	"False"	"CHEMBL3888834"	"Kinase Assay: JAK2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 100 μM KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC, 10 mM MgAcetate and [γ-33P-ATP](specific activity approx. 500 cpm/pmol, concentration as required). The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of 3% phosphoric acid solution. 10 μL of the reaction is then spotted onto a P30 filtermat and washed three times for 5 minutes in 75 mM phosphoric acid and once in methanol prior to drying and scintillation counting."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886854"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3971783"	""	"0"	"490.61"	"1"	"5.30"	"BDBM229061"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(Cc2ccc(-c3ccccc3)cc2)CC1"	"IC50"	"'='"	"46.0"	"nM"	"7.34"	""	"400797"	"UO_0000065"	"14.96"	"0.27"	"2.04"	"7.34"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4089118"	""	"0"	"409.37"	"0"	"2.42"	"BDBM237874"	"N#C[C@H]1CCOC[C@@H]1n1cc(C(N)=O)c(Nc2ccc([C@H](O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"0.7"	"nM"	"9.15"	""	"414976"	"UO_0000065"	"22.36"	"0.43"	"6.73"	"7.25"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4101534"	""	"0"	"372.43"	"0"	"4.45"	"16"	"CCc1cc(O)ccc1-c1ccc2c(C(=O)Nc3ccc(C)nc3)n[nH]c2c1"	"IC50"	"'='"	"58.8"	"nM"	"7.23"	""	""	"UO_0000065"	"19.41"	"0.35"	"2.78"	"7.95"	"False"	"CHEMBL4003453"	"Inhibition of GST tagged human recombinant JAK2 catalytic domain expressed in baculovirus using peptide substrate preincubated for 60 mins followed by substrate addition and measured after 60 mins by microfluidic assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4002590"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL3917073"	""	"0"	"411.92"	"0"	"1.69"	"BDBM239966"	"Cn1cc(Nc2ncc(Cl)c(NC3CC4CN(S(C)(=O)=O)CC4C3)n2)cn1"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	"418586"	"UO_0000065"	"19.23"	"0.40"	"6.23"	"7.54"	"False"	"CHEMBL3888834"	"Kinase Assay: JAK2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 100 μM KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC, 10 mM MgAcetate and [γ-33P-ATP](specific activity approx. 500 cpm/pmol, concentration as required). The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of 3% phosphoric acid solution. 10 μL of the reaction is then spotted onto a P30 filtermat and washed three times for 5 minutes in 75 mM phosphoric acid and once in methanol prior to drying and scintillation counting."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886854"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3961729"	""	"0"	"415.85"	"0"	"3.29"	"BDBM239970"	"Cn1cc(Nc2ncc(Cl)c(NC3CC4CN(CC(F)(F)F)CC4C3)n2)cn1"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	"418590"	"UO_0000065"	"19.47"	"0.39"	"4.81"	"11.42"	"False"	"CHEMBL3888834"	"Kinase Assay: JAK2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 100 μM KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC, 10 mM MgAcetate and [γ-33P-ATP](specific activity approx. 500 cpm/pmol, concentration as required). The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of 3% phosphoric acid solution. 10 μL of the reaction is then spotted onto a P30 filtermat and washed three times for 5 minutes in 75 mM phosphoric acid and once in methanol prior to drying and scintillation counting."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886854"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3702950"	""	"0"	"365.44"	"0"	"2.83"	"BDBM147652"	"N#C[C@H]1C[C@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C3CC3)cc2)n1"	"IC50"	"'='"	"25.0"	"nM"	"7.60"	""	"285584"	"UO_0000065"	"20.80"	"0.38"	"4.77"	"6.50"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642287"	""	"0"	"461.59"	"0"	"4.35"	"BDBM99552"	"CN1CCC(c2ccc(Nc3nc4c(-c5ccc(S(C)(=O)=O)cc5)cccn4n3)cc2)CC1"	"IC50"	"'='"	"1.1"	"nM"	"8.96"	""	"216243"	"UO_0000065"	"19.41"	"0.37"	"4.61"	"11.25"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642381"	""	"0"	"549.70"	"1"	"3.95"	"BDBM99657"	"CN(Cc1ccccc1CNc1cccn2nc(Nc3ccc(OCCN4CCCC4)cc3)nc12)S(C)(=O)=O"	"IC50"	"'='"	"97.47"	"nM"	"7.01"	""	"216347"	"UO_0000065"	"12.75"	"0.25"	"3.06"	"6.73"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652356"	""	"0"	"502.64"	"1"	"2.65"	"BDBM113167"	"Cc1cc(CC[C@]2(O)CCN(S(=O)(=O)C[C@H]3CC[C@H](N(C)c4ncnc5[nH]ccc45)CC3)C2)on1"	"IC50"	"'='"	"46.2"	"nM"	"7.33"	""	"234610"	"UO_0000065"	"14.59"	"0.29"	"4.69"	"5.71"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3642341"	""	"0"	"463.56"	"0"	"3.38"	"BDBM99616"	"CS(=O)(=O)c1ccc(-c2cccc3nc(Nc4cccc(CN5CCOCC5)c4)nn23)cc1"	"IC50"	"'='"	"0.95"	"nM"	"9.02"	""	"216306"	"UO_0000065"	"19.46"	"0.37"	"5.64"	"10.16"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3905548"	""	"0"	"516.60"	"1"	"4.74"	"BDBM229042"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3cccc(-c4ccc(O)cc4)c3)n2)CC1"	"IC50"	"'='"	"293.0"	"nM"	"6.53"	""	"400787"	"UO_0000065"	"12.65"	"0.23"	"1.79"	"4.46"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3938294"	""	"0"	"366.81"	"0"	"0.57"	"BDBM236505"	"CN(c1nc(Nc2cnn(C)c2)ncc1Cl)C1COC2C(O)COC21"	"IC50"	"'='"	"689.0"	"nM"	"6.16"	""	"411890"	"UO_0000065"	"16.80"	"0.34"	"5.59"	"6.32"	"False"	"CHEMBL3888640"	"Kinase Assay: JAK2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 100 μM KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC, 10 mM MgAcetate and [γ-33P-ATP] (specific activity approx. 500 cpm/pmol, concentration as required). The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of 3% phosphoric acid solution. 10 μL of the reaction is then spotted onto a P30 filtermat and washed three times for 5 minutes in 75 mM phosphoric acid and once in methanol prior to drying and scintillation counting."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886792"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3958723"	""	"0"	"535.05"	"2"	"5.69"	"BDBM229038"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3cccc(-c4ccc(Cl)cc4)c3)n2)CC1"	"IC50"	"'='"	"1481.0"	"nM"	"5.83"	""	"400783"	"UO_0000065"	"10.90"	"0.21"	"0.14"	"4.62"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3925815"	""	"0"	"364.37"	"0"	"1.85"	"BDBM228783"	"CN(c1ncc(C#N)cc1[N+](=O)[O-])[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399721"	"UO_0000065"	"25.41"	"0.47"	"7.41"	"7.24"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3944048"	""	"0"	"425.49"	"0"	"2.76"	"BDBM228876"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccncc3)n2)CC1"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	"400623"	"UO_0000065"	"18.80"	"0.35"	"5.24"	"5.75"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3895300"	""	"0"	"436.52"	"0"	"3.37"	"BDBM228892"	"CC(C)(C)OC(=O)N1CC2(C1)CC(CC#N)(n1cc(C(N)=O)c(Nc3ccccc3)n1)C2"	"IC50"	"'='"	"1481.0"	"nM"	"5.83"	""	"400639"	"UO_0000065"	"13.35"	"0.25"	"2.46"	"4.62"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3919793"	""	"0"	"478.53"	"0"	"3.79"	"BDBM228893"	"COc1ccc(N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)CC2)cc1OC"	"IC50"	"'='"	"154.0"	"nM"	"6.81"	""	"400640"	"UO_0000065"	"14.24"	"0.27"	"3.02"	"5.75"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3918566"	""	"0"	"477.54"	"0"	"3.40"	"BDBM228899"	"CC(C)(O)c1cccc(N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)CC2)n1"	"IC50"	"'='"	"22.0"	"nM"	"7.66"	""	"400646"	"UO_0000065"	"16.04"	"0.30"	"4.26"	"5.75"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4107619"	""	"0"	"320.36"	"0"	"2.27"	"BDBM228890"	"N#CC[C@]1(n2cc(C(N)=O)c(Nc3ccccc3)n2)C[C@@H](C#N)C1"	"IC50"	"'='"	"405.0"	"nM"	"6.39"	""	"400637"	"UO_0000065"	"19.95"	"0.36"	"4.12"	"5.30"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3665121"	""	"0"	"338.37"	"0"	"2.27"	"BDBM112508"	"COC(=O)N1CC[C@@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.0986"	"nM"	"10.01"	""	"233747"	"UO_0000065"	"29.57"	"0.55"	"7.74"	"10.42"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3699494"	""	"0"	"323.40"	"0"	"3.23"	"BDBM147510"	"CC1CCC(C#N)C(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"38.0"	"nM"	"7.42"	""	"285438"	"UO_0000065"	"22.94"	"0.42"	"4.19"	"7.67"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3622824"	""	"0"	"247.30"	"0"	"-0.40"	"5a"	"NCCc1nc2cc(C(N)=O)ccc2n1CCN"	"IC50"	"'='"	"2900.0"	"nM"	"5.54"	""	""	"UO_0000065"	"22.39"	"0.42"	"5.94"	"4.90"	"False"	"CHEMBL3625898"	"Inhibition of JAK2 (unknown origin) using 35 uM of ATP and Tyr6 peptide by Z'-LYTE kinase assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621116"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL3645000"	""	"0"	"564.03"	"2"	"5.26"	"BDBM99752"	"CS(=O)(=O)CCN1CCc2ccc(Nc3nc4c(-c5cc(C(F)(F)F)ccc5Cl)cccn4n3)cc2CC1"	"IC50"	"'='"	"16.84"	"nM"	"7.77"	""	"216440"	"UO_0000065"	"13.78"	"0.28"	"2.51"	"9.77"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647923"	""	"0"	"455.46"	"0"	"3.32"	"BDBM148039"	"N#C[C@@H]1CCCCC1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)CC(F)(F)F)cc2)n1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"285981"	"UO_0000065"	"19.76"	"0.40"	"5.68"	"6.88"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647912"	""	"0"	"360.37"	"0"	"2.86"	"BDBM148024"	"[C-]#[N+][C@H]1C[C@@H](CF)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccnc(F)c2)n1"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	"285960"	"UO_0000065"	"21.88"	"0.41"	"5.03"	"8.74"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652342"	""	"0"	"409.51"	"0"	"0.32"	"BDBM113153"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2C[C@H](O)[C@H](O)C2)CC1"	"IC50"	"'='"	"8.54"	"nM"	"8.07"	""	"234596"	"UO_0000065"	"19.70"	"0.39"	"7.75"	"6.58"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3645545"	""	"0"	"423.52"	"0"	"4.06"	"BDBM107131"	"O=C(CN1CCN(c2ccccc2)CC1)Nc1cccc(-c2cnc3ccccc3n2)c1"	"IC50"	"'='"	"18000.0"	"nM"	"4.75"	""	"226369"	"UO_0000065"	"11.20"	"0.20"	"0.68"	"7.73"	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3644960"	""	"0"	"537.65"	"1"	"4.31"	"BDBM99710"	"CC(C)(C)OC(=O)N1CCC(n2cc(Nc3nc4c(-c5ccc(S(C)(=O)=O)cc5)cccn4n3)cn2)CC1"	"IC50"	"'='"	"0.5"	"nM"	"9.30"	""	"216400"	"UO_0000065"	"17.30"	"0.33"	"4.99"	"7.52"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3645086"	""	"0"	"538.57"	"1"	"4.41"	"BDBM99859"	"CN(C)C(=O)CN1CCc2ccc(Nc3nc4c(-c5cc(F)ccc5OCC(F)F)cccn4n3)cc2CC1"	"IC50"	"'='"	"519.79"	"nM"	"6.28"	""	"216528"	"UO_0000065"	"11.67"	"0.22"	"1.87"	"8.38"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3644959"	""	"0"	"398.45"	"0"	"2.89"	"BDBM99709"	"CCn1cc(Nc2nc3c(Oc4ccc(S(C)(=O)=O)cc4)cccn3n2)cn1"	"IC50"	"'='"	"1156.98"	"nM"	"5.94"	""	"216399"	"UO_0000065"	"14.90"	"0.29"	"3.05"	"5.74"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL4632766"	""	"0"	"351.35"	"0"	"2.78"	"29"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](OC(=O)[C@@H]4CC4(F)F)CC3)c12"	"IC50"	"'>'"	"25000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL4294556"	""	"0"	"451.47"	"0"	"3.27"	"53"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(S(=O)(=O)c2ccc(C(F)(F)F)cc2)CC12CC2"	"IC50"	"'='"	"1400.0"	"nM"	"5.85"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4285014"	""	"0"	"327.43"	"0"	"2.43"	"11"	"CC(C)CC(=O)N1C[C@H](N(C)c2ncnc3[nH]ccc23)C2(CC2)C1"	"IC50"	"'='"	"1100.0"	"nM"	"5.96"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4291735"	""	"0"	"342.40"	"0"	"0.52"	"15"	"CNC(=O)CC(=O)N1C[C@H](N(C)c2ncnc3[nH]ccc23)C2(CC2)C1"	"IC50"	"'='"	"13000.0"	"nM"	"4.89"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4287328"	""	"0"	"438.54"	"0"	"4.76"	"36"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(C(=O)Nc2ccccc2-c2ccccc2)CC12CC2"	"IC50"	"'='"	"9100.0"	"nM"	"5.04"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4283965"	""	"0"	"335.43"	"0"	"1.21"	"38"	"CCS(=O)(=O)N1C[C@H](N(C)c2ncnc3[nH]ccc23)C2(CC2)C1"	"IC50"	"'='"	"180.0"	"nM"	"6.75"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4293578"	""	"0"	"408.49"	"0"	"2.12"	"46"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(S(=O)(=O)c2cccc(C#N)c2)CC12CC2"	"IC50"	"'='"	"59.0"	"nM"	"7.23"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4279526"	""	"0"	"428.47"	"0"	"2.16"	"49"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(S(=O)(=O)c2cccc([N+](=O)[O-])c2)CC12CC2"	"IC50"	"'='"	"5.5"	"nM"	"8.26"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL2325900"	""	"0"	"270.34"	"0"	"2.36"	"3d"	"CC(NC(=O)c1c[nH]c2ncc(C3CC3)nc12)C1CC1"	"IC50"	"'='"	"22.4"	"nM"	"7.65"	""	""	"UO_0000065"	"28.30"	"0.52"	"5.29"	"10.82"	"False"	"CHEMBL2329570"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 30 mins by scintillation counting analysis in presence of [gamma-33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321829"	"1"	"Scientific Literature"	"J. Med. Chem."	"2013"	"None"	""
"CHEMBL4636220"	""	"0"	"243.31"	"0"	"2.46"	"12"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3C[C@H]4CC[C@@H]3C4)c12"	"IC50"	"'='"	"22000.0"	"nM"	"4.66"	""	""	"UO_0000065"	"19.14"	"0.35"	"2.20"	"7.57"	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL4647115"	""	"0"	"282.35"	"0"	"2.60"	"39"	"Cc1[nH]nc2[nH]c(=O)cc([C@@H]3C[C@@H]4C[C@H]3C[C@H]4CC#N)c12"	"IC50"	"'='"	"15000.0"	"nM"	"4.82"	""	""	"UO_0000065"	"17.08"	"0.31"	"2.22"	"5.65"	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL3125863"	""	"0"	"426.45"	"0"	"3.82"	"5"	"O=C(CCc1nc2ccccc2c(=O)[nH]1)Nc1ncc(Cc2ccc(F)c(F)c2)s1"	"IC50"	"'='"	"3700.0"	"nM"	"5.43"	""	""	"UO_0000065"	"12.74"	"0.25"	"1.61"	"6.19"	"False"	"CHEMBL3130286"	"Inhibition of JAK2 (unknown origin) by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3124748"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3126340"	""	"0"	"342.28"	"0"	"3.63"	"15"	"O=c1[nH]ccc2c(Nc3c(F)cc(F)cc3F)nc3ccncc3c12"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	""	"UO_0000065"	"23.83"	"0.45"	"4.52"	"11.54"	"False"	"CHEMBL3131376"	"Inhibition of recombinant Jak2 (unknown origin) using biotinylated synthetic peptide substrate by homogeneous time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3124786"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3114762"	""	"0"	"483.50"	"0"	"3.84"	"11f"	"O=C1NC(=O)C(c2c[nH]c3ccccc23)=C1Nc1cccc(O[C@@H]2CCN(c3ccnc(F)c3)C2)c1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3118993"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112442"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL4645742"	""	"0"	"382.83"	"1"	"5.14"	"16i"	"CC(Oc1cc(-c2c[nH]c3cccnc23)cnc1N)c1cc(F)ccc1Cl"	"IC50"	"'='"	"9963.0"	"nM"	"5.00"	""	""	"UO_0000065"	"13.06"	"0.25"	"-0.14"	"6.51"	"False"	"CHEMBL4628503"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4627317"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL4646060"	""	"0"	"404.87"	"0"	"4.50"	"16q"	"COCCCn1cc(-c2cnc(N)c(OC(C)c3cc(F)ccc3Cl)c2)cn1"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	""	"UO_0000065"	"19.32"	"0.38"	"3.32"	"10.41"	"False"	"CHEMBL4628503"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4627317"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL3651602"	""	"0"	"418.50"	"0"	"2.44"	"BDBM103734"	"NC(=O)C1CCN(Cc2ccc(-c3cccc4nc(NC(=O)C5CC5)nn34)cc2)CC1"	"IC50"	"'='"	"1355.0"	"nM"	"5.87"	""	"221720"	"UO_0000065"	"14.02"	"0.26"	"3.43"	"5.56"	"False"	"CHEMBL3707887"	"Inhibition Assay: In vitro inhibition assay using various enzyme."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638964"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647881"	""	"0"	"505.00"	"1"	"2.12"	"BDBM147993"	"CS(=O)(=O)C1CN(C(=O)[C@@H]2CC[C@@H](n3cc(C(N)=O)c(Nc4ccc(Cl)cc4)n3)[C@H](C#N)C2)C1"	"IC50"	"'='"	"19.0"	"nM"	"7.72"	""	"285928"	"UO_0000065"	"15.29"	"0.31"	"5.60"	"5.11"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3648434"	""	"0"	"321.34"	"0"	"2.80"	"BDBM107143"	"CC(=O)OCC(=O)Nc1cccc(-c2cnc3ccccc3n2)c1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	"226381"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3644969"	""	"0"	"381.48"	"0"	"4.90"	"BDBM99719"	"c1ccc2c(c1)CCCN2c1nc2cccc(N3CCCc4ccccc43)n2n1"	"IC50"	"'='"	"9999.0"	"nM"	"5.00"	""	"216409"	"UO_0000065"	"13.11"	"0.24"	"0.10"	"13.64"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703093"	""	"0"	"502.49"	"1"	"2.81"	"BDBM147807"	"N#C[C@H]1C[C@@H](NCC(F)F)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)F)cc2)n1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"285741"	"UO_0000065"	"16.52"	"0.33"	"5.49"	"5.81"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL2325895"	""	"0"	"380.45"	"0"	"1.96"	"3q"	"CC(C)(C)[C@@H](NC(=O)c1c[nH]c2ncc(C3CC3)nc12)C(=O)N1CC(C#N)C1"	"IC50"	"'='"	"0.8"	"nM"	"9.10"	""	""	"UO_0000065"	"23.91"	"0.44"	"7.14"	"7.93"	"True"	"CHEMBL2329570"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 30 mins by scintillation counting analysis in presence of [gamma-33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321829"	"1"	"Scientific Literature"	"J. Med. Chem."	"2013"	"None"	""
"CHEMBL2325913"	""	"0"	"341.42"	"0"	"1.82"	"3o"	"CC1CCN(C(=O)[C@@H](C)NC(=O)c2c[nH]c3ncc(C4CC4)nc23)C1"	"IC50"	"'='"	"134.2"	"nM"	"6.87"	""	""	"UO_0000065"	"20.13"	"0.38"	"5.05"	"7.55"	"False"	"CHEMBL2329570"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 30 mins by scintillation counting analysis in presence of [gamma-33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321829"	"1"	"Scientific Literature"	"J. Med. Chem."	"2013"	"None"	""
"CHEMBL2325905"	""	"0"	"288.35"	"0"	"1.72"	"3g"	"C[C@@H](NC(=O)c1c[nH]c2ncc(C3CC3)nc12)C(C)(C)O"	"IC50"	"'='"	"43.0"	"nM"	"7.37"	""	""	"UO_0000065"	"25.55"	"0.48"	"5.65"	"8.10"	"False"	"CHEMBL2329570"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 30 mins by scintillation counting analysis in presence of [gamma-33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321829"	"1"	"Scientific Literature"	"J. Med. Chem."	"2013"	"None"	""
"CHEMBL3417194"	""	"0"	"529.64"	"2"	"5.15"	"40"	"O=C(CCCCCCC(=O)N1C/C=C/COCc2cccc(c2)-c2ccnc(n2)Nc2cccc(c2)C1)NO"	"IC50"	"'='"	"684.0"	"nM"	"6.17"	""	""	"UO_0000065"	"11.64"	"0.22"	"1.01"	"5.28"	"False"	"CHEMBL3419812"	"Inhibition of human recombinant JAK2 using Z'LYTETry6 peptide substrate after 1 hr by microplate reader"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3414525"	"1"	"Scientific Literature"	"Eur. J. Med. Chem."	"2015"	"None"	""
"CHEMBL3417193"	""	"0"	"501.59"	"1"	"4.37"	"39"	"O=C(CCCCC(=O)N1C/C=C/COCc2cccc(c2)-c2ccnc(n2)Nc2cccc(c2)C1)NO"	"IC50"	"'='"	"547.0"	"nM"	"6.26"	""	""	"UO_0000065"	"12.48"	"0.23"	"1.89"	"5.37"	"False"	"CHEMBL3419812"	"Inhibition of human recombinant JAK2 using Z'LYTETry6 peptide substrate after 1 hr by microplate reader"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3414525"	"1"	"Scientific Literature"	"Eur. J. Med. Chem."	"2015"	"None"	""
"CHEMBL3417185"	""	"0"	"473.58"	"0"	"4.70"	"30"	"O=C(CCCCN1C/C=C/CCOc2cccc(c2)-c2ccnc(n2)Nc2cccc(c2)C1)NO"	"IC50"	"'='"	"293.0"	"nM"	"6.53"	""	""	"UO_0000065"	"13.80"	"0.25"	"1.83"	"6.56"	"False"	"CHEMBL3419812"	"Inhibition of human recombinant JAK2 using Z'LYTETry6 peptide substrate after 1 hr by microplate reader"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3414525"	"1"	"Scientific Literature"	"Eur. J. Med. Chem."	"2015"	"None"	""
"CHEMBL3114772"	""	"0"	"457.47"	"0"	"3.67"	"8b"	"O=C1NC(=O)C(c2c[nH]c3ccccc23)=C1Nc1ccc(OCCNc2ccnc(F)c2)cc1"	"IC50"	"'='"	"9687.0"	"nM"	"5.01"	""	""	"UO_0000065"	"10.96"	"0.20"	"1.34"	"4.64"	"False"	"CHEMBL3118993"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112442"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3114766"	""	"0"	"427.46"	"0"	"3.31"	"7a"	"O=C1NC(=O)C(c2c[nH]c3ccccc23)=C1Nc1cccc(OCCCn2ccnc2)c1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3118993"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112442"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3702982"	""	"0"	"432.45"	"0"	"3.83"	"BDBM147692"	"[C-]#[N+][C@H]1C[C@@H](N2CCC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"23.0"	"nM"	"7.64"	""	"285625"	"UO_0000065"	"17.66"	"0.34"	"3.81"	"9.48"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3126346"	""	"0"	"401.25"	"0"	"4.58"	"24"	"CC(O)c1cc(Cl)c(Nc2nc3ccncc3c3c(=O)[nH]ccc23)c(Cl)c1"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	""	"UO_0000065"	"19.74"	"0.40"	"3.34"	"8.71"	"False"	"CHEMBL3131375"	"Inhibition of Jak2 (unknown origin) assessed as inhibition of STAT5 phosphorylation by cell-based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3124786"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3309995"	""	"0"	"334.34"	"0"	"1.76"	"10b"	"Nc1ccc2c(c1)nc(Cc1ccc3c(c1)OCO3)n1nc(N)nc21"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3381081"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352169"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL2012881"	""	"0"	"280.29"	"0"	"1.66"	"16e"	"O=c1[nH]nc2cc(CO)c3ccc(-c4ccc[nH]4)cc3n12"	"IC50"	"'='"	"650.0"	"nM"	"6.19"	""	""	"UO_0000065"	"22.07"	"0.40"	"4.53"	"7.18"	"False"	"CHEMBL2013787"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2010637"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL3335694"	""	"0"	"388.46"	"0"	"0.83"	"23"	"CS(=O)(=O)N1CCC[C@H](Nc2nc(N)ncc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"71.0"	"nM"	"7.15"	""	""	"UO_0000065"	"18.40"	"0.36"	"6.32"	"5.01"	"False"	"CHEMBL3374010"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 1 hr in presence of [gamma-33P]ATP by scintillation counting analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351377"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3114765"	""	"0"	"453.48"	"0"	"3.79"	"11i"	"O=C1NC(=O)C(c2c[nH]c3ccccc23)=C1Nc1cccc(C2CN(c3ccnc(F)c3)C2)c1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3118993"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112442"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3114764"	""	"0"	"481.53"	"0"	"4.57"	"11h"	"O=C1NC(=O)C(c2c[nH]c3ccccc23)=C1Nc1cccc(C2CCN(c3ccnc(F)c3)CC2)c1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3118993"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112442"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3114771"	""	"0"	"471.49"	"0"	"4.06"	"8a"	"O=C1NC(=O)C(c2c[nH]c3ccccc23)=C1Nc1ccc(OCCCNc2ccnc(F)c2)cc1"	"IC50"	"'='"	"1270.0"	"nM"	"5.90"	""	""	"UO_0000065"	"12.51"	"0.23"	"1.84"	"5.45"	"False"	"CHEMBL3118993"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112442"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3114767"	""	"0"	"413.44"	"0"	"2.92"	"7b"	"O=C1NC(=O)C(c2c[nH]c3ccccc23)=C1Nc1cccc(OCCn2ccnc2)c1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3118993"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112442"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL2062811"	""	"0"	"452.48"	"0"	"4.91"	"37"	"CN1CCN(c2cccc(Nc3nc4c(-c5ccc(C(F)(F)F)cc5)cccn4n3)c2)CC1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	""	"UO_0000065"	"18.56"	"0.35"	"3.49"	"17.24"	"False"	"CHEMBL2067611"	"Inhibition of human JAK2 expressed in baculovirus using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate preincubated for 1 hr measured after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL3652294"	""	"0"	"482.65"	"0"	"3.63"	"BDBM113103"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCCC(Cc3ccccn3)C2)CC1"	"IC50"	"'='"	"33.0"	"nM"	"7.48"	""	"234547"	"UO_0000065"	"15.50"	"0.30"	"3.85"	"7.87"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3658118"	""	"0"	"616.65"	"2"	"5.15"	"BDBM148435"	"Cc1ccc(NC(=O)c2cc(C(F)(F)F)ccn2)cc1N1CCc2nc(Nc3ccc(N4CCN(C)CC4)cc3)ncc2C1=O"	"IC50"	"'='"	"48.0"	"nM"	"7.32"	""	"286802"	"UO_0000065"	"11.87"	"0.22"	"2.17"	"6.87"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652351"	""	"0"	"425.53"	"0"	"1.54"	"BDBM113162"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2C[C@H](F)[C@@H](CO)C2)CC1"	"IC50"	"'='"	"18.5"	"nM"	"7.73"	""	"234605"	"UO_0000065"	"18.17"	"0.36"	"6.19"	"7.55"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3665208"	""	"0"	"534.65"	"1"	"1.97"	"BDBM112608"	"CS(=O)(=O)N1CCC[C@H](Nc2nc(N3CCN(c4ccccn4)CC3)ncc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.1751"	"nM"	"9.76"	""	"233845"	"UO_0000065"	"18.25"	"0.35"	"7.79"	"7.17"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3650993"	""	"0"	"350.38"	"0"	"3.23"	"BDBM153168"	"C=CC(=O)Nc1cc(-c2ncnc3[nH]cc(C(=O)OCC)c23)ccc1C"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294116"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699460"	""	"0"	"309.37"	"0"	"2.98"	"BDBM147475"	"N#C[C@@H]1CCCCC1n1cc(C(N)=O)c(Nc2ccccc2)n1"	"IC50"	"'='"	"138.0"	"nM"	"6.86"	""	"285400"	"UO_0000065"	"22.17"	"0.41"	"3.88"	"7.09"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3648438"	""	"0"	"335.36"	"0"	"3.19"	"BDBM107147"	"CCOC(=O)CC(=O)Nc1cccc(-c2cnc3ccccc3n2)c1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	"226385"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703496"	""	"0"	"301.73"	"0"	"3.46"	"BDBM153140"	"CCOC(=O)c1c[nH]c2ncnc(-c3cccc(Cl)c3)c12"	"IC50"	"'='"	"145.0"	"nM"	"6.84"	""	"294088"	"UO_0000065"	"22.66"	"0.44"	"3.38"	"10.08"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642423"	""	"0"	"551.65"	"1"	"4.61"	"BDBM99701"	"CP(C)(=O)c1ccc(-c2cccn3nc(Nc4cccc(C5CCN(CCS(C)(=O)=O)CC5)c4)nc23)cc1"	"IC50"	"'='"	"165.79"	"nM"	"6.78"	""	"216391"	"UO_0000065"	"12.29"	"0.24"	"2.17"	"7.01"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3644961"	""	"0"	"437.53"	"0"	"2.66"	"BDBM99711"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4cnn(C5CCNCC5)c4)nc23)cc1"	"IC50"	"'='"	"0.71"	"nM"	"9.15"	""	"216401"	"UO_0000065"	"20.91"	"0.40"	"6.49"	"8.61"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3799170"	""	"0"	"464.53"	"0"	"3.07"	"14e"	"Cn1c(C(N)=O)cc2c(-c3ccc(NC(=O)[C@@H]4CCCN4C(=O)OC(C)(C)C)cc3)ncnc21"	"IC50"	"'='"	"1200.0"	"nM"	"5.92"	""	""	"UO_0000065"	"12.75"	"0.24"	"2.85"	"4.47"	"False"	"CHEMBL3802364"	"Inhibition of JAK2 in GMCSF-stimulated human TF1 cells assessed as suppression of STAT5 phosphorylation preincubated for 2 hrs followed by GMCSF stimulation for 50 mins by FACS reader analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"CHEMBL3307972"	""
"CHEMBL3797902"	""	"0"	"493.57"	"0"	"3.58"	"15g"	"Cn1c(C(=O)NCCN2CCCC2)cc2c(-c3ccc(NC(=O)c4ccc(C#N)cc4)cc3)ncnc21"	"IC50"	"'='"	"41.0"	"nM"	"7.39"	""	""	"UO_0000065"	"14.97"	"0.27"	"3.81"	"6.37"	"False"	"CHEMBL3802363"	"Inhibition of recombinant human GST-tagged JAK2 expressed in baculovirus expression system using Z'-LYTE Try6 peptide as substrate incubated for 1 hr by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3797795"	""	"0"	"309.33"	"0"	"1.69"	"14a"	"CC(=O)Nc1ccc(-c2ncnc3c2cc(C(N)=O)n3C)cc1"	"IC50"	"'='"	"184.0"	"nM"	"6.74"	""	""	"UO_0000065"	"21.77"	"0.40"	"5.05"	"6.55"	"False"	"CHEMBL3802363"	"Inhibition of recombinant human GST-tagged JAK2 expressed in baculovirus expression system using Z'-LYTE Try6 peptide as substrate incubated for 1 hr by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3798090"	""	"0"	"442.52"	"0"	"4.98"	"12c"	"Cn1c(C(=O)OCc2ccccc2)cc2c(-c3ccc(NC(=O)C(C)(C)C)cc3)ncnc21"	"IC50"	"'='"	"786.0"	"nM"	"6.11"	""	""	"UO_0000065"	"13.80"	"0.25"	"1.12"	"7.09"	"False"	"CHEMBL3802363"	"Inhibition of recombinant human GST-tagged JAK2 expressed in baculovirus expression system using Z'-LYTE Try6 peptide as substrate incubated for 1 hr by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3800493"	""	"0"	"535.65"	"1"	"3.31"	"15d"	"C[C@H](NC(=O)OC(C)(C)C)C(=O)Nc1ccc(-c2ncnc3c2cc(C(=O)NCCN2CCCC2)n3C)cc1"	"IC50"	"'='"	"1400.0"	"nM"	"5.85"	""	""	"UO_0000065"	"10.93"	"0.20"	"2.54"	"4.49"	"False"	"CHEMBL3802364"	"Inhibition of JAK2 in GMCSF-stimulated human TF1 cells assessed as suppression of STAT5 phosphorylation preincubated for 2 hrs followed by GMCSF stimulation for 50 mins by FACS reader analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"CHEMBL3307972"	""
"CHEMBL3798482"	""	"0"	"478.60"	"0"	"3.07"	"16c"	"Cn1c(C(=O)NCCCN2CCOCC2)cc2c(-c3ccc(NC(=O)C(C)(C)C)cc3)ncnc21"	"IC50"	"'='"	"140.0"	"nM"	"6.85"	""	""	"UO_0000065"	"14.32"	"0.27"	"3.78"	"6.76"	"False"	"CHEMBL3802364"	"Inhibition of JAK2 in GMCSF-stimulated human TF1 cells assessed as suppression of STAT5 phosphorylation preincubated for 2 hrs followed by GMCSF stimulation for 50 mins by FACS reader analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3797127"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"CHEMBL3307972"	""
"CHEMBL3936249"	""	"0"	"585.04"	"2"	"5.42"	"BDBM230090"	"Cc1c(-c2c(Cl)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)c2cccc(F)c2n(C)c1=O"	"IC50"	"'='"	"2000.0"	"nM"	"5.70"	""	"402013"	"UO_0000065"	"9.74"	"0.19"	"0.28"	"4.63"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3912426"	""	"0"	"589.00"	"2"	"5.25"	"BDBM230117"	"Cn1c(=O)n(-c2cccc(-c3c(F)cc(C(N)=O)c4[nH]c5cc(C(C)(C)O)ccc5c34)c2Cl)c(=O)c2cccc(F)c21"	"IC50"	"'='"	"2000.0"	"nM"	"5.70"	""	"402057"	"UO_0000065"	"9.68"	"0.19"	"0.45"	"4.63"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3116055"	""	"0"	"353.37"	"0"	"2.54"	"23a, enantiomeric mixture"	"CC(Nc1nc(Nc2cn(C)cn2)c2[nH]ccc2n1)c1ncc(F)cn1"	"IC50"	"'<'"	"3.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3118240"	"Inhibition of Jak2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112447"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL3948378"	""	"0"	"333.40"	"0"	"2.25"	"BDBM228741"	"Cc1cc(N(C)[C@@H]2CCN(c3ncnc4[nH]ccc34)C2)ncc1C#N"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399670"	"UO_0000065"	"30.77"	"0.56"	"8.01"	"12.11"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3967688"	""	"0"	"377.44"	"0"	"2.83"	"BDBM255011"	"CN1CN([C@H]2CC[C@H](CNCC(F)F)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"8.2"	"nM"	"8.09"	""	"443867"	"UO_0000065"	"21.42"	"0.41"	"5.26"	"12.58"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3976204"	""	"0"	"352.44"	"0"	"2.08"	"BDBM255013"	"CN1CN([C@H]2CC[C@H](CNCC#N)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	"443869"	"UO_0000065"	"21.97"	"0.41"	"5.66"	"8.80"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3919463"	""	"0"	"391.50"	"0"	"1.52"	"BDBM254981"	"CN1CN([C@H]2CC[C@H](CNS(C)(=O)=O)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"2.7"	"nM"	"8.57"	""	"443888"	"UO_0000065"	"21.89"	"0.43"	"7.05"	"8.71"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3961430"	""	"0"	"439.48"	"0"	"3.44"	"BDBM254985"	"COCN1CN([C@H]2CC[C@H](CN(C)CC(F)(F)F)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"6.5"	"nM"	"8.19"	""	"443892"	"UO_0000065"	"18.63"	"0.36"	"4.75"	"12.65"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3893600"	""	"0"	"371.46"	"0"	"2.67"	"BDBM255031"	"O=C1NCN([C@H]2CC[C@H](CN3CC[C@@H](F)C3)CC2)c2c1cnc1[nH]ccc21"	"IC50"	"'='"	"67.0"	"nM"	"7.17"	""	"443903"	"UO_0000065"	"19.31"	"0.36"	"4.50"	"11.16"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3601115"	""	"0"	"427.90"	"0"	"3.45"	"45"	"C=CC(=O)Nc1cccc(CNc2nc(Nc3cnn(CCOC)c3)ncc2Cl)c1"	"IC50"	"'='"	"51.0"	"nM"	"7.29"	""	""	"UO_0000065"	"17.04"	"0.33"	"3.84"	"6.88"	"False"	"CHEMBL3603319"	"Inhibition of JAK2 (unknown origin) by Z'-Lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3600288"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL3601235"	""	"0"	"500.94"	"1"	"4.73"	"25"	"C=CC(=O)Nc1cccc(CNc2nc(Nc3cc(F)c(N4CCOCC4)c(F)c3)ncc2Cl)c1"	"IC50"	"'='"	"351.0"	"nM"	"6.46"	""	""	"UO_0000065"	"12.89"	"0.25"	"1.72"	"7.06"	"False"	"CHEMBL3603319"	"Inhibition of JAK2 (unknown origin) by Z'-Lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3600288"	"1"	"Scientific Literature"	"J. Med. Chem."	"2015"	"None"	""
"CHEMBL3934943"	""	"0"	"398.42"	"0"	"3.59"	"BDBM198423"	"FC(F)Oc1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"86.0"	"nM"	"7.07"	""	"352501"	"UO_0000065"	"17.73"	"0.33"	"3.48"	"9.90"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3978366"	""	"0"	"375.41"	"0"	"3.00"	"BDBM198426"	"N#Cc1cc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)ccc1F"	"IC50"	"'='"	"31.0"	"nM"	"7.51"	""	"352504"	"UO_0000065"	"20.00"	"0.37"	"4.51"	"8.74"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3907076"	""	"0"	"354.46"	"0"	"2.34"	"BDBM198469"	"OC[C@@H]1CCCN1C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"110.0"	"nM"	"6.96"	""	"352547"	"UO_0000065"	"19.63"	"0.37"	"4.62"	"8.45"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3933397"	""	"0"	"417.47"	"0"	"3.32"	"BDBM198477"	"O=C1COc2ccc(NC[C@H]3CC[C@H](c4nnn5cnc6[nH]ccc6c45)CC3)cc2N1"	"IC50"	"'='"	"29.0"	"nM"	"7.54"	""	"352555"	"UO_0000065"	"18.06"	"0.33"	"4.22"	"6.90"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3926516"	""	"0"	"420.49"	"0"	"3.53"	"BDBM198525"	"Fc1ccc(C2(NC[C@H]3CC[C@H](c4nnn5cnc6[nH]ccc6c45)CC3)COC2)cc1"	"IC50"	"'='"	"7.1"	"nM"	"8.15"	""	"352603"	"UO_0000065"	"19.38"	"0.36"	"4.62"	"10.17"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3902256"	""	"0"	"423.57"	"0"	"2.68"	"BDBM198537"	"c1cc2c(ncn3nnc([C@H]4CC[C@H](CN5CCC(N6CCOCC6)CC5)CC4)c23)[nH]1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"352615"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3963994"	""	"0"	"343.39"	"0"	"2.86"	"BDBM198579"	"N#Cc1ccc(N2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"190.0"	"nM"	"6.72"	""	"352657"	"UO_0000065"	"19.57"	"0.35"	"3.86"	"7.82"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3962138"	""	"0"	"490.56"	"0"	"4.39"	"BDBM198593"	"CSc1ccc(C(O)(CN[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C(F)(F)F)cc1"	"IC50"	"'='"	"27.0"	"nM"	"7.57"	""	"352671"	"UO_0000065"	"15.43"	"0.30"	"3.18"	"8.31"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3932456"	""	"0"	"338.34"	"0"	"2.78"	"BDBM198602"	"FC(F)(F)CN[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	"352680"	"UO_0000065"	"23.64"	"0.46"	"5.22"	"11.28"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3950137"	""	"0"	"380.37"	"0"	"2.95"	"BDBM198652"	"O=C(C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1)NCC(F)(F)F"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	"352730"	"UO_0000065"	"20.65"	"0.40"	"4.90"	"8.93"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3589171"	""	"0"	"442.52"	"0"	"3.48"	"8"	"COc1cccc(-c2cc(C(N)=O)c3[nH]c4ccc(C(=O)N5CCN(C)CC5)cc4c3c2)c1"	"IC50"	"'='"	"3.5"	"nM"	"8.46"	""	""	"UO_0000065"	"19.11"	"0.35"	"4.98"	"9.23"	"False"	"CHEMBL3592849"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3911142"	""	"0"	"334.37"	"0"	"2.73"	"BDBM198458"	"FC(F)CNC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	"352536"	"UO_0000065"	"23.40"	"0.45"	"5.09"	"11.04"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3126341"	""	"0"	"375.19"	"0"	"4.66"	"16"	"O=c1[nH]ccc2c(Nc3c(Cl)cc(F)cc3Cl)nc3ccncc3c12"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	""	"UO_0000065"	"20.93"	"0.43"	"3.19"	"11.11"	"False"	"CHEMBL3131375"	"Inhibition of Jak2 (unknown origin) assessed as inhibition of STAT5 phosphorylation by cell-based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3124786"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL4072239"	""	"0"	"318.38"	"0"	"3.54"	"3"	"NC(=O)c1cnc(Nc2ccccc2)cc1NCc1ccccc1"	"IC50"	"'='"	"203.0"	"nM"	"6.69"	""	""	"UO_0000065"	"21.02"	"0.38"	"3.15"	"8.36"	"False"	"CHEMBL4047228"	"Inhibition of GST-tagged JAK2 (unknown origin) using fluoresceinated peptide as substrate after 3 hrs by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4043231"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL3975440"	""	"0"	"350.34"	"0"	"1.82"	"BDBM228784"	"N#Cc1cnc(NC2CCN(c3ncnc4[nH]ccc34)C2)c([N+](=O)[O-])c1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399722"	"UO_0000065"	"26.43"	"0.49"	"7.44"	"6.78"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3964413"	""	"0"	"360.40"	"0"	"2.69"	"BDBM228789"	"C#CCN(c1ccc(C#N)cc1F)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399727"	"UO_0000065"	"25.69"	"0.47"	"6.57"	"12.89"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3943693"	""	"0"	"396.84"	"0"	"0.56"	"BDBM236507"	"Cn1cc(Nc2ncc(Cl)c(NC3COC4C(OCCO)COC34)n2)cn1"	"IC50"	"'='"	"68.0"	"nM"	"7.17"	""	"411891"	"UO_0000065"	"18.06"	"0.36"	"6.61"	"6.20"	"False"	"CHEMBL3888641"	"Kinase Assay: Aurora-A (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 200 μM LRRASLG (Kemptide), 10 mM MgAcetate and [γ-33P-ATP](specific activity approx. 500 cpm/pmol, concentration as required). The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of 3% phosphoric acid solution. 10 μL of the reaction is then spotted onto a P30 filtermat and washed three times for 5 minutes in 75 mM phosphoric acid and once in methanol prior to drying and scintillation counting."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886792"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4110850"	""	"0"	"398.45"	"0"	"1.67"	"BDBM228891"	"CS(=O)(=O)c1ccc(Nc2nn([C@]3(CC#N)C[C@@H](C#N)C3)cc2C(N)=O)cc1"	"IC50"	"'='"	"127.0"	"nM"	"6.90"	""	"400638"	"UO_0000065"	"17.31"	"0.34"	"5.23"	"4.46"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3905278"	""	"0"	"437.45"	"0"	"3.31"	"BDBM228897"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(c2cncc(F)c2)CC1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"400644"	"UO_0000065"	"19.20"	"0.36"	"5.09"	"7.44"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3896471"	""	"0"	"487.46"	"0"	"4.19"	"BDBM228900"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(c2cncc(C(F)(F)F)c2)CC1"	"IC50"	"'='"	"54.0"	"nM"	"7.27"	""	"400647"	"UO_0000065"	"14.91"	"0.28"	"3.08"	"6.44"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3980404"	""	"0"	"433.49"	"0"	"3.48"	"BDBM228912"	"Cc1cccc(N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)CC2)n1"	"IC50"	"'='"	"102.0"	"nM"	"6.99"	""	"400659"	"UO_0000065"	"16.13"	"0.30"	"3.51"	"6.19"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3956730"	""	"0"	"449.49"	"0"	"3.18"	"BDBM228915"	"COc1cccnc1N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CC1"	"IC50"	"'='"	"559.0"	"nM"	"6.25"	""	"400662"	"UO_0000065"	"13.91"	"0.26"	"3.07"	"5.12"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3920825"	""	"0"	"433.49"	"0"	"3.48"	"BDBM228940"	"Cc1cncc(N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)CC2)c1"	"IC50"	"'='"	"26.0"	"nM"	"7.58"	""	"400687"	"UO_0000065"	"17.50"	"0.32"	"4.11"	"6.72"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3948006"	""	"0"	"491.57"	"0"	"3.48"	"BDBM228941"	"CC(C)(O)Cc1cccc(N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)CC2)n1"	"IC50"	"'='"	"147.0"	"nM"	"6.83"	""	"400688"	"UO_0000065"	"13.90"	"0.26"	"3.35"	"5.13"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3895272"	""	"0"	"437.45"	"0"	"3.31"	"BDBM228943"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(c2cccnc2F)CC1"	"IC50"	"'='"	"0.6"	"nM"	"9.22"	""	"400690"	"UO_0000065"	"21.08"	"0.39"	"5.91"	"8.17"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3933722"	""	"0"	"449.49"	"0"	"3.18"	"BDBM228945"	"COc1ccc(N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)CC2)cn1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"400692"	"UO_0000065"	"17.90"	"0.33"	"4.87"	"6.59"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3948482"	""	"0"	"510.60"	"1"	"3.93"	"BDBM228950"	"CC(C)OC(=O)c1ccc(Nc2nn(C3(CC#N)CCN(C(=O)OC(C)(C)C)CC3)cc2C(N)=O)cc1"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	"400697"	"UO_0000065"	"15.08"	"0.28"	"3.77"	"5.05"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3957158"	""	"0"	"581.56"	"1"	"3.92"	"BDBM228952"	"N#CCC1(n2cc(C(N)=O)c(Nc3cccc(Cn4nnc5ccccc54)c3)n2)CCN(C(=O)OCC(F)(F)F)CC1"	"IC50"	"'='"	"23.0"	"nM"	"7.64"	""	"400699"	"UO_0000065"	"13.13"	"0.25"	"3.72"	"4.87"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3974368"	""	"0"	"325.37"	"0"	"2.14"	"BDBM228959"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCOCC1"	"IC50"	"'='"	"133.0"	"nM"	"6.88"	""	"400706"	"UO_0000065"	"21.13"	"0.39"	"4.74"	"6.49"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3934229"	""	"0"	"391.43"	"0"	"1.68"	"BDBM228964"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCS(=O)(=O)CC1"	"IC50"	"'='"	"813.0"	"nM"	"6.09"	""	"400710"	"UO_0000065"	"15.56"	"0.31"	"4.41"	"4.65"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3951123"	""	"0"	"483.57"	"0"	"2.99"	"BDBM228971"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(C(C)(C)O)nc3)n2)CC1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"400716"	"UO_0000065"	"17.62"	"0.33"	"5.53"	"5.35"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3926301"	""	"0"	"504.60"	"1"	"3.77"	"BDBM228978"	"Cn1ccc(-c2ccc(Nc3nn(C4(CC#N)CCN(C(=O)OC(C)(C)C)CC4)cc3C(N)=O)cc2)n1"	"IC50"	"'='"	"138.0"	"nM"	"6.86"	""	"400723"	"UO_0000065"	"13.60"	"0.25"	"3.09"	"4.76"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3931150"	""	"0"	"531.64"	"1"	"2.62"	"BDBM228986"	"CN(C)S(=O)(=O)c1ccc(Nc2nn(C3(CC#N)CCN(C(=O)OC(C)(C)C)CC3)cc2C(N)=O)cc1"	"IC50"	"'='"	"0.8"	"nM"	"9.10"	""	"400731"	"UO_0000065"	"17.11"	"0.34"	"6.48"	"5.56"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3917002"	""	"0"	"459.94"	"0"	"3.41"	"BDBM228994"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccnc(Cl)c3)n2)CC1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"400739"	"UO_0000065"	"18.53"	"0.36"	"5.11"	"6.12"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3904453"	""	"0"	"310.41"	"0"	"2.63"	"BDBM198603"	"c1cc2c(ncn3nnc([C@H]4CC[C@H](NCC5CC5)CC4)c23)[nH]1"	"IC50"	"'='"	"190.0"	"nM"	"6.72"	""	"352681"	"UO_0000065"	"21.65"	"0.40"	"4.09"	"9.48"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4114359"	""	"0"	"340.43"	"0"	"1.95"	"BDBM198612"	"O[C@@H]1CCN(C[C@H]2CC[C@@H](c3nnn4cnc5[nH]ccc5c34)CC2)C1"	"IC50"	"'='"	"250.0"	"nM"	"6.60"	""	"352690"	"UO_0000065"	"19.39"	"0.36"	"4.65"	"8.02"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3933671"	""	"0"	"367.50"	"0"	"2.52"	"BDBM198631"	"CCN(C)C1CN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C1"	"IC50"	"'='"	"480.0"	"nM"	"6.32"	""	"352709"	"UO_0000065"	"17.19"	"0.32"	"3.80"	"9.67"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3956945"	""	"0"	"394.40"	"0"	"2.49"	"BDBM198632"	"OC1(C(F)(F)F)CN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C1"	"IC50"	"'='"	"22.0"	"nM"	"7.66"	""	"352710"	"UO_0000065"	"19.42"	"0.37"	"5.17"	"9.30"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647924"	""	"0"	"457.43"	"0"	"2.24"	"BDBM148041"	"N#C[C@H]1C[C@H](O)CCC1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"285983"	"UO_0000065"	"18.63"	"0.38"	"6.28"	"5.64"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3644976"	""	"0"	"538.57"	"1"	"4.66"	"BDBM99726"	"COc1ccc(C(F)(F)F)cc1-c1cccc2nc(Nc3ccc4c(c3)CCN(CC(=O)N(C)C)CC4)nn12"	"IC50"	"'='"	"53.86"	"nM"	"7.27"	""	"216416"	"UO_0000065"	"13.50"	"0.25"	"2.61"	"9.69"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3644956"	""	"0"	"474.51"	"0"	"3.67"	"BDBM99705"	"CN1CCN(c2cccc(Nc3nc4c(-c5ccc(P(C)(C)=O)cc5)cccn4n3)c2)C(=O)C1"	"IC50"	"'='"	"10.47"	"nM"	"7.98"	""	"216395"	"UO_0000065"	"16.82"	"0.32"	"4.31"	"9.63"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3645079"	""	"0"	"435.48"	"0"	"4.47"	"BDBM99848"	"FC(F)COc1ccccc1-c1cccn2nc(Nc3ccc4c(c3)CCNCC4)nc12"	"IC50"	"'='"	"129.8"	"nM"	"6.89"	""	"216521"	"UO_0000065"	"15.81"	"0.29"	"2.42"	"10.85"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3644977"	""	"0"	"559.61"	"1"	"4.61"	"BDBM99727"	"COc1cc(C(F)(F)F)ccc1-c1cccc2nc(Nc3ccc4c(c3)CCN(CCS(C)(=O)=O)CC4)nn12"	"IC50"	"'='"	"7.01"	"nM"	"8.15"	""	"216417"	"UO_0000065"	"14.57"	"0.29"	"3.54"	"9.18"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652352"	""	"0"	"470.62"	"0"	"0.91"	"BDBM113163"	"CNS(=O)(=O)[C@H]1CCN(S(=O)(=O)C[C@H]2CC[C@H](N(C)c3ncnc4[nH]ccc34)CC2)C1"	"IC50"	"'='"	"24.8"	"nM"	"7.61"	""	"234606"	"UO_0000065"	"16.16"	"0.34"	"6.70"	"5.93"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3699544"	""	"0"	"395.46"	"0"	"3.34"	"BDBM147562"	"CC(C)(C(=O)O)c1ccc(Nc2nn([C@@H]3CCCC[C@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"285492"	"UO_0000065"	"20.62"	"0.38"	"4.81"	"6.08"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652370"	""	"0"	"407.54"	"0"	"1.74"	"BDBM113181"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC[C@](C)(O)C2)CC1"	"IC50"	"'='"	"39.2"	"nM"	"7.41"	""	"234624"	"UO_0000065"	"18.17"	"0.36"	"5.67"	"7.23"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3665127"	""	"0"	"338.37"	"0"	"2.27"	"BDBM112514"	"COC(=O)N1CC[C@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.0276"	"nM"	"10.56"	""	"233753"	"UO_0000065"	"31.21"	"0.58"	"8.29"	"11.00"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642357"	""	"0"	"501.59"	"1"	"2.28"	"BDBM99633"	"CN(c1ncccc1CNc1cccn2nc(Nc3ccc(S(C)(=O)=O)cc3)nc12)S(C)(=O)=O"	"IC50"	"'='"	"17.32"	"nM"	"7.76"	""	"216323"	"UO_0000065"	"15.47"	"0.31"	"5.48"	"5.60"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3655097"	""	"0"	"350.45"	"0"	"0.76"	"BDBM159764"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)NCC2CC2)C1"	"IC50"	"'='"	"1100.0"	"nM"	"5.96"	""	"302574"	"UO_0000065"	"17.00"	"0.34"	"5.20"	"5.78"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703100"	""	"0"	"352.44"	"0"	"2.52"	"BDBM147815"	"CN(C)[C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccccc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"32.0"	"nM"	"7.50"	""	"285749"	"UO_0000065"	"21.27"	"0.39"	"4.97"	"7.50"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647786"	""	"0"	"482.89"	"0"	"3.22"	"BDBM147889"	"N#C[C@H]1C[C@@H](N2CC(O)(C(F)(F)F)C2)CCC1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	"285823"	"UO_0000065"	"16.40"	"0.33"	"4.70"	"6.59"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702979"	""	"0"	"520.48"	"1"	"3.11"	"BDBM147689"	"N#C[C@H]1C[C@@H](NCC(F)F)CCC1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	"285622"	"UO_0000065"	"15.29"	"0.31"	"4.85"	"5.57"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3942765"	""	"0"	"438.53"	"0"	"3.63"	"BDBM228866"	"CNC(=O)c1cn(C2(CC#N)CCN(C(=O)OC(C)(C)C)CC2)nc1Nc1ccccc1"	"IC50"	"'='"	"1481.0"	"nM"	"5.83"	""	"400616"	"UO_0000065"	"13.29"	"0.25"	"2.20"	"5.19"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3900700"	""	"0"	"482.54"	"0"	"2.99"	"BDBM229058"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(CC(=O)O)cc3)n2)CC1"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	"400794"	"UO_0000065"	"16.58"	"0.31"	"5.01"	"4.89"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL2381985"	""	"0"	"399.43"	"0"	"2.19"	"11"	"Cc1cc(Nc2nc(N[C@@H](C)c3ncc(F)cn3)cc(N3CCOCC3)n2)n[nH]1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	""	"UO_0000065"	"20.78"	"0.39"	"6.11"	"7.11"	"False"	"CHEMBL2383938"	"Inhibition of JAK2 (unknown origin) using biotinylated TYK2 peptide as substrate after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2380256"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2381981"	""	"0"	"416.44"	"0"	"2.93"	"7"	"Cc1cc(Nc2nc(N[C@@H](C)c3ccc(F)cn3)c(F)c(N3CCOCC3)n2)n[nH]1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	""	"UO_0000065"	"19.74"	"0.37"	"5.29"	"7.91"	"False"	"CHEMBL2383938"	"Inhibition of JAK2 (unknown origin) using biotinylated TYK2 peptide as substrate after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2380256"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL4107213"	""	"0"	"474.54"	"0"	"1.99"	"BDBM228874"	"CC(C)(C)OC(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(S(C)(=O)=O)cc3)n2)C1"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"400621"	"UO_0000065"	"17.18"	"0.34"	"6.16"	"5.08"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3652365"	""	"0"	"526.71"	"1"	"3.78"	"BDBM113176"	"CCc1ccc(COC[C@H]2CCN(S(=O)(=O)C[C@H]3CC[C@H](N(C)c4ncnc5[nH]ccc45)CC3)C2)nc1"	"IC50"	"'='"	"63.6"	"nM"	"7.20"	""	"234619"	"UO_0000065"	"13.66"	"0.27"	"3.42"	"6.90"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3665159"	""	"0"	"400.51"	"0"	"2.64"	"BDBM112552"	"CCCS(=O)(=O)N1CCC[C@H](Nc2ncccc2-c2cnc3cc[nH]c3n2)C1"	"IC50"	"'='"	"0.3102"	"nM"	"9.51"	""	"233790"	"UO_0000065"	"23.74"	"0.46"	"6.87"	"9.15"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647791"	""	"0"	"442.95"	"0"	"3.38"	"BDBM147894"	"N#C[C@H]1C[C@@H](NC2CCOCC2)CCC1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"102.0"	"nM"	"6.99"	""	"285828"	"UO_0000065"	"15.78"	"0.31"	"3.61"	"5.93"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647725"	""	"0"	"562.60"	"1"	"1.89"	"BDBM147827"	"CS(=O)(=O)CCNC1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"285761"	"UO_0000065"	"14.93"	"0.31"	"6.51"	"4.74"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647872"	""	"0"	"414.44"	"0"	"2.84"	"BDBM147984"	"CCNC(=O)O[C@@H]1CCC(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"285918"	"UO_0000065"	"19.41"	"0.37"	"5.21"	"5.96"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3933776"	""	"0"	"403.48"	"0"	"3.36"	"BDBM255035"	"O=C1c2cnc3[nH]ccc3c2N([C@H]2CC[C@H](CNCC(F)F)CC2)CN1C1CC1"	"IC50"	"'='"	"19.0"	"nM"	"7.72"	""	"443907"	"UO_0000065"	"19.14"	"0.36"	"4.36"	"12.02"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3702916"	""	"0"	"532.55"	"1"	"4.80"	"BDBM147615"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)Nc3ccc(C(F)(F)F)cc3)cc2)n1"	"IC50"	"'='"	"31.0"	"nM"	"7.51"	""	"285545"	"UO_0000065"	"14.10"	"0.28"	"2.71"	"5.25"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652401"	""	"0"	"421.57"	"0"	"1.84"	"BDBM113213"	"C[C@@H]1C[C@@H](CS(=O)(=O)N2CC[C@@H](CO)C2)CC[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"17.8"	"nM"	"7.75"	""	"234656"	"UO_0000065"	"18.38"	"0.36"	"5.91"	"7.57"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3665187"	""	"0"	"441.52"	"0"	"1.19"	"BDBM112582"	"CN(C)c1ncc(-c2cnc3[nH]cc(C#N)c3n2)c(N[C@H]2CCCN(S(C)(=O)=O)C2)n1"	"IC50"	"'='"	"0.3889"	"nM"	"9.41"	""	"233819"	"UO_0000065"	"21.31"	"0.41"	"8.22"	"6.54"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703060"	""	"0"	"504.56"	"1"	"4.07"	"BDBM147770"	"CC1(C)CN([C@H]2CC[C@H](n3cc(C(N)=O)c(Nc4ccc([C@](C)(O)C(F)(F)F)cc4)n3)[C@@H](C#N)C2)C1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"285704"	"UO_0000065"	"16.30"	"0.31"	"4.15"	"6.84"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647734"	""	"0"	"528.53"	"1"	"3.30"	"BDBM147837"	"N#C[C@H]1CC(N2CC[C@H](F)C2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	"285771"	"UO_0000065"	"14.70"	"0.29"	"4.47"	"5.79"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699479"	""	"0"	"343.36"	"0"	"2.09"	"BDBM147494"	"N#C[C@H]1C[C@H](O)CCC1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"46.0"	"nM"	"7.34"	""	"285420"	"UO_0000065"	"21.37"	"0.40"	"5.25"	"6.27"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699541"	""	"0"	"359.82"	"0"	"2.60"	"BDBM147559"	"N#C[C@H]1C[C@H](O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"285489"	"UO_0000065"	"23.07"	"0.45"	"5.70"	"7.10"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665198"	""	"0"	"431.53"	"0"	"0.62"	"BDBM112596"	"CS(=O)(=O)N1CCC[C@H](Nc2nc(NCCN)ncc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.1665"	"nM"	"9.78"	""	"233833"	"UO_0000065"	"22.66"	"0.45"	"9.16"	"6.32"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3702917"	""	"0"	"546.58"	"1"	"4.48"	"BDBM147616"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)NCc3ccc(C(F)(F)F)cc3)cc2)n1"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"285546"	"UO_0000065"	"14.92"	"0.29"	"3.67"	"5.71"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651012"	""	"0"	"367.37"	"0"	"2.00"	"BDBM153188"	"C=C(C)C(=O)Nc1cc(-c2ncnc3[nH]cc(C(=O)OCC)c23)c[nH]c1=O"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294136"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703086"	""	"0"	"426.95"	"0"	"4.00"	"BDBM147800"	"C[C@H](N[C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@@H](C#N)C1)C1CC1"	"IC50"	"'='"	"85.0"	"nM"	"7.07"	""	"285734"	"UO_0000065"	"16.56"	"0.32"	"3.07"	"6.50"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642414"	""	"0"	"472.57"	"0"	"3.21"	"BDBM99692"	"CN1Cc2ccc(Nc3nc4c(C#Cc5ccccc5N(C)S(C)(=O)=O)cccn4n3)cc2C1"	"IC50"	"'='"	"11.53"	"nM"	"7.94"	""	"216381"	"UO_0000065"	"16.80"	"0.32"	"4.73"	"9.58"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3665161"	""	"0"	"428.56"	"0"	"2.89"	"BDBM112554"	"CC(C)CS(=O)(=O)N1CCC[C@H](Nc2ncccc2-c2cnc3ccn(C)c3n2)C1"	"IC50"	"'='"	"0.5802"	"nM"	"9.24"	""	"233792"	"UO_0000065"	"21.55"	"0.42"	"6.35"	"9.93"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3645033"	""	"0"	"470.58"	"0"	"3.64"	"BDBM99797"	"COc1ccccc1-c1cccn2nc(Nc3ccc4c(c3)CCN(CC(=O)N(C)C)CC4)nc12"	"IC50"	"'='"	"39.21"	"nM"	"7.41"	""	"216473"	"UO_0000065"	"15.74"	"0.29"	"3.77"	"9.88"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703094"	""	"0"	"371.42"	"0"	"2.05"	"BDBM147808"	"CN(C)[C@@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"254.0"	"nM"	"6.59"	""	"285742"	"UO_0000065"	"17.76"	"0.33"	"4.55"	"5.84"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3650679"	""	"0"	"387.47"	"0"	"2.38"	"BDBM148061"	"CS(=O)(=O)c1ccc(Nc2nn([C@H]3CCCC[C@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"85.0"	"nM"	"7.07"	""	"285972"	"UO_0000065"	"18.25"	"0.36"	"4.69"	"5.40"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651035"	""	"0"	"336.35"	"0"	"2.93"	"BDBM153212"	"C=C(C)C(=O)Nc1cccc(-c2ncnc3[nH]cc(C(=O)OC)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294160"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702914"	""	"0"	"430.53"	"0"	"2.67"	"BDBM147613"	"CC(C)NS(=O)(=O)c1ccc(Nc2nn([C@H]3CCCC[C@@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"285543"	"UO_0000065"	"20.90"	"0.41"	"6.33"	"6.30"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699538"	""	"0"	"390.39"	"0"	"2.67"	"BDBM147556"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc([C@H](O)C(F)F)nc2)n1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"285486"	"UO_0000065"	"21.83"	"0.42"	"5.85"	"6.56"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647780"	""	"0"	"428.92"	"0"	"2.99"	"BDBM147883"	"CC1(N[C@H]2CCC(n3cc(C(N)=O)c(Nc4ccc(Cl)cc4)n3)[C@@H](C#N)C2)COC1"	"IC50"	"'='"	"22.0"	"nM"	"7.66"	""	"285817"	"UO_0000065"	"17.85"	"0.35"	"4.67"	"6.49"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3780467"	""	"0"	"385.47"	"0"	"1.72"	"21"	"COC(=O)C1CCc2[nH]c(-c3c(N[C@H]4CC[C@@H](N)CC4)cc[nH]c3=O)nc2C1"	"IC50"	"'='"	"40.0"	"nM"	"7.40"	""	""	"UO_0000065"	"19.19"	"0.36"	"5.68"	"5.88"	"False"	"CHEMBL3784139"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3779778"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3702995"	""	"0"	"488.51"	"0"	"3.15"	"BDBM147705"	"N#C[C@H]1C[C@H](N2C[C@@H]3[C@@H](CO)[C@@H]3C2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"22.0"	"nM"	"7.66"	""	"285639"	"UO_0000065"	"15.68"	"0.30"	"4.51"	"6.37"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645027"	""	"0"	"413.53"	"0"	"4.62"	"BDBM99783"	"CC(C)Oc1ccccc1-c1cccn2nc(Nc3ccc4c(c3)CCNCC4)nc12"	"IC50"	"'='"	"56.24"	"nM"	"7.25"	""	"216466"	"UO_0000065"	"17.53"	"0.32"	"2.63"	"11.42"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3665177"	""	"0"	"401.50"	"0"	"1.70"	"BDBM112570"	"CN(C)S(=O)(=O)N1CCC[C@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.1115"	"nM"	"9.95"	""	"233807"	"UO_0000065"	"24.79"	"0.49"	"8.25"	"9.29"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3891545"	""	"0"	"571.01"	"2"	"5.18"	"BDBM230150"	"Cc1c(-c2c(F)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)cc2c(Cl)cccn2c1=O"	"IC50"	"'='"	"1300.0"	"nM"	"5.89"	""	"402042"	"UO_0000065"	"10.31"	"0.20"	"0.71"	"4.80"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3960384"	""	"0"	"591.43"	"2"	"5.75"	"BDBM230118"	"CC(C)(O)c1ccc2c(c1)[nH]c1c(C(N)=O)cc(Cl)c(-c3cccc(-n4c(=O)[nH]c5c(F)cccc5c4=O)c3Cl)c12"	"IC50"	"'='"	"1800.0"	"nM"	"5.75"	""	"402058"	"UO_0000065"	"9.71"	"0.19"	"-0.01"	"4.29"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3894000"	""	"0"	"572.54"	"2"	"5.03"	"BDBM230120"	"Cc1c(-c2c(F)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)[nH]c2c(F)cc(F)cc2c1=O"	"IC50"	"'='"	"1200.0"	"nM"	"5.92"	""	"402061"	"UO_0000065"	"10.34"	"0.19"	"0.89"	"4.42"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3945408"	""	"0"	"575.04"	"1"	"4.90"	"BDBM230126"	"Cc1c(-c2c(Cl)cc(C(N)=O)c3[nH]c4c(c23)CC[C@H](C(C)(C)O)C4)cccc1-n1c(=O)[nH]c2c(F)cccc2c1=O"	"IC50"	"'>'"	"2000.0"	"nM"	""	""	"402067"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3896019"	""	"0"	"568.58"	"1"	"4.90"	"BDBM230143"	"Cc1c(-c2c(F)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)c2cccc(F)c2n(C)c1=O"	"IC50"	"'='"	"4300.0"	"nM"	"5.37"	""	"402085"	"UO_0000065"	"9.44"	"0.17"	"0.47"	"4.36"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL2414536"	""	"0"	"364.41"	"0"	"2.90"	"32"	"COc1ccc(-c2cccn3nc(Nc4cnn([C@H](C)CO)c4)nc23)cc1"	"IC50"	"'='"	"89.0"	"nM"	"7.05"	""	""	"UO_0000065"	"19.35"	"0.36"	"4.15"	"7.88"	"False"	"CHEMBL2415128"	"Inhibition of JAK2 in human SET2 cells assessed as reduction of phosphorylated STAT5 level"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2412966"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL3952795"	""	"0"	"572.61"	"1"	"4.40"	"BDBM230103"	"Cc1c(-c2c(F)cc(C(N)=O)c3[nH]c4c(c23)CC[C@@H](C(C)(C)O)C4)cccc1-n1c(=O)c2cccc(F)c2n(C)c1=O"	"IC50"	"'>'"	"2000.0"	"nM"	""	""	"402038"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3923822"	""	"0"	"554.55"	"1"	"4.66"	"BDBM230112"	"Cc1c(-c2c(F)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)cc2c(F)cccn2c1=O"	"IC50"	"'='"	"830.0"	"nM"	"6.08"	""	"402051"	"UO_0000065"	"10.97"	"0.20"	"1.42"	"4.96"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4095253"	""	"0"	"427.49"	"0"	"2.35"	"B6"	"C=CS(=O)(=O)N1CCC[C@@H]1Cn1cc(-c2ccc3c(c2)OCO3)c2c(N)ncnc21"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4058148"	"Inhibition of recombinant human C-terminal His6-tagged JAK2 (808 to end residues) expressed in baculovirus Sf21 insect cells preincubated for 5 mins followed by substrate addition after 30 to 60 mins in presence of ATP by fluorescence assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4052785"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL2035043"	""	"0"	"368.44"	"0"	"4.93"	"13c, 95:5 trans/Cis mixture"	"C1=C/Cn2ccc3ccc(cc32)-c2ccnc(n2)Nc2cccc(c2)COC/1"	"IC50"	"'='"	"150.0"	"nM"	"6.82"	""	""	"UO_0000065"	"18.52"	"0.33"	"1.89"	"13.13"	"False"	"CHEMBL2040119"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2034857"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL4537718"	""	"0"	"417.52"	"0"	"3.77"	"6"	"CC(C)(C#N)CNC(=O)Cc1nc2cnc3[nH]ccc3c2n1[C@H]1CC[C@H](CC#N)CC1"	"IC50"	"'='"	"69.0"	"nM"	"7.16"	""	""	"UO_0000065"	"17.15"	"0.32"	"3.39"	"5.81"	"False"	"CHEMBL4404829"	"Inhibition of JAK2/JAK2 in human PBMC assessed as reduction in GM-CSF-induced STAT5 phosphorylation pre-incubated for 30 mins before GM-CSF stimulation for 30 mins AlphaLISAassay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402578"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL3262618"	""	"0"	"349.40"	"0"	"2.30"	"3h"	"C[C@H](N)CNc1cc2nc[nH]c(=O)c2c(Nc2cccc3cc[nH]c23)n1"	"IC50"	"'='"	"980.0"	"nM"	"6.01"	""	""	"UO_0000065"	"17.20"	"0.32"	"3.71"	"4.83"	"False"	"CHEMBL3268711"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3259804"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3262624"	""	"0"	"390.45"	"0"	"2.68"	"10c"	"N[C@H]1COCC[C@H]1Nc1cc2cc[nH]c(=O)c2c(Nc2cccc3cc[nH]c23)n1"	"IC50"	"'='"	"680.0"	"nM"	"6.17"	""	""	"UO_0000065"	"15.80"	"0.29"	"3.49"	"5.10"	"False"	"CHEMBL3268711"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3259804"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL475251"	"R-406"	"2"	"470.46"	"0"	"3.63"	"2"	"COc1cc(Nc2ncc(F)c(Nc3ccc4c(n3)NC(=O)C(C)(C)O4)n2)cc(OC)c1OC"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	""	"UO_0000065"	"17.48"	"0.33"	"4.59"	"6.39"	"False"	"CHEMBL3268711"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3259804"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3262619"	""	"0"	"375.44"	"0"	"2.71"	"3i"	"O=c1[nH]cnc2cc(N[C@@H]3CCCNC3)nc(Nc3cccc4cc[nH]c34)c12"	"IC50"	"'='"	"950.0"	"nM"	"6.02"	""	""	"UO_0000065"	"16.04"	"0.29"	"3.31"	"5.45"	"False"	"CHEMBL3268711"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3259804"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL1995703"	""	"0"	"509.68"	"1"	"4.10"	"3; TG101209"	"Cc1cnc(Nc2ccc(N3CCN(C)CC3)cc2)nc1Nc1cccc(S(=O)(=O)NC(C)(C)C)c1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	""	""	"16.13"	"0.31"	"4.12"	"8.02"	"False"	"CHEMBL4728470"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4725348"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL3934831"	""	"0"	"402.45"	"0"	"2.72"	"BDBM255039"	"N#CCN1CN([C@H]2CC[C@H](CNCC(F)F)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"29.0"	"nM"	"7.54"	""	"443911"	"UO_0000065"	"18.73"	"0.35"	"4.82"	"8.56"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3913143"	""	"0"	"378.48"	"0"	"2.62"	"BDBM255042"	"N#CCN1CN([C@H]2CC[C@H](CNC3CC3)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"150.0"	"nM"	"6.82"	""	"443914"	"UO_0000065"	"18.03"	"0.33"	"4.20"	"7.75"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3950208"	""	"0"	"369.47"	"0"	"1.65"	"BDBM255044"	"CN1CN([C@H]2CC[C@H](CN3CC(O)C3)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"43.0"	"nM"	"7.37"	""	"443916"	"UO_0000065"	"19.94"	"0.37"	"5.72"	"9.73"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL2208032"	""	"0"	"418.50"	"0"	"3.01"	"10b"	"C[C@@H](N)C(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"452.0"	"nM"	"6.34"	""	""	"UO_0000065"	"15.16"	"0.28"	"3.33"	"6.02"	"False"	"CHEMBL2214784"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT3 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL3297762"	""	"0"	"512.10"	"1"	"3.80"	"15a"	"CN1CCN(C[C@@H](NC(=O)C[C@H]2CNC(=O)c3cc(-c4cccc(Cl)c4)cn32)C2CCCCC2)CC1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3300963"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3297733"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2013"	"None"	""
"CHEMBL2322136"	""	"0"	"254.34"	"0"	"3.50"	"6"	"Cn1nc(C2CCCCC2)c2c3cc[nH]c3ncc21"	"IC50"	"'='"	"50.0"	"nM"	"7.30"	""	""	"UO_0000065"	"28.71"	"0.52"	"3.80"	"15.70"	"False"	"CHEMBL2327345"	"Inhibition of JAK2 (unknown origin) after 2.5 hrs by time-resolved fluorescence resonance energy transfer assay in presence of 1 uM ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321825"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2325903"	""	"0"	"286.38"	"0"	"3.00"	"3e"	"C[C@H](NC(=O)c1c[nH]c2ncc(C3CC3)nc12)C(C)(C)C"	"IC50"	"'='"	"5480.0"	"nM"	"5.26"	""	""	"UO_0000065"	"18.37"	"0.34"	"2.26"	"7.44"	"False"	"CHEMBL2329053"	"Inhibition of JAK2 in human PBMC expressing CD14 assessed as inhibition of GM-CSF-stimulated STAT5a phosphorylation after 30 mins by flow cytometric analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321829"	"1"	"Scientific Literature"	"J. Med. Chem."	"2013"	"None"	""
"CHEMBL2325895"	""	"0"	"380.45"	"0"	"1.96"	"3q"	"CC(C)(C)[C@@H](NC(=O)c1c[nH]c2ncc(C3CC3)nc12)C(=O)N1CC(C#N)C1"	"IC50"	"'='"	"188.0"	"nM"	"6.73"	""	""	"UO_0000065"	"17.68"	"0.33"	"4.77"	"5.86"	"False"	"CHEMBL2329053"	"Inhibition of JAK2 in human PBMC expressing CD14 assessed as inhibition of GM-CSF-stimulated STAT5a phosphorylation after 30 mins by flow cytometric analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321829"	"1"	"Scientific Literature"	"J. Med. Chem."	"2013"	"None"	""
"CHEMBL4452803"	""	"0"	"482.61"	"0"	"2.86"	"7f"	"Cc1cnc(Nc2cccc(N3CCN(C)CC3)c2)nc1-c1cc2c(o1)CCN(S(C)(=O)=O)C2"	"IC50"	"'='"	"112.0"	"nM"	"6.95"	""	""	"UO_0000065"	"14.40"	"0.28"	"4.09"	"7.33"	"False"	"CHEMBL4341343"	"Inhibition of JAK2 (unknown origin) using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition and measured by 30 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4453064"	""	"0"	"384.46"	"0"	"3.11"	"7a"	"Cc1cnc(Nc2ccccc2)nc1-c1cc2c(o1)CCN(S(C)(=O)=O)C2"	"IC50"	"'='"	"2.7"	"nM"	"8.57"	""	""	"UO_0000065"	"22.29"	"0.43"	"5.46"	"9.70"	"False"	"CHEMBL4341343"	"Inhibition of JAK2 (unknown origin) using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition and measured by 30 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL3622821"	"UPADACITINIB"	"4"	"380.37"	"0"	"2.91"	"5"	"CC[C@@H]1CN(C(=O)NCC(F)(F)F)C[C@@H]1c1cnc2cnc3[nH]ccc3n12"	"IC50"	"'='"	"600.0"	"nM"	"6.22"	""	""	"UO_0000065"	"16.36"	"0.31"	"3.31"	"7.94"	"False"	"CHEMBL4341342"	"Inhibition of JAK2 (unknown origin) by cell based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4590082"	""	"0"	"458.52"	"0"	"3.42"	"7j"	"Cc1cnc(Nc2ccc(N3CCOCC3)cc2)nc1-c1cc2c(o1)CCN(C(=O)CC#N)C2"	"IC50"	"'='"	"145.7"	"nM"	"6.84"	""	""	"UO_0000065"	"14.91"	"0.27"	"3.42"	"6.36"	"False"	"CHEMBL4341349"	"Inhibition of JAK2 in human TF-1 cells assessed as reduction in GM-CSF-induced cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"CHEMBL3307972"	""
"CHEMBL2414534"	""	"0"	"435.51"	"0"	"3.25"	"30"	"CN(C)C(=O)c1ccc(Nc2nc3c(-c4ccc(S(C)(=O)=O)cc4)cccn3n2)cc1"	"IC50"	"'='"	"117.0"	"nM"	"6.93"	""	""	"UO_0000065"	"15.92"	"0.31"	"3.68"	"7.17"	"False"	"CHEMBL2415128"	"Inhibition of JAK2 in human SET2 cells assessed as reduction of phosphorylated STAT5 level"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2412966"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2414532"	""	"0"	"347.43"	"0"	"3.70"	"28"	"Cc1cc(Nc2nc3cccc(-c4cnn(CC(C)C)c4)n3n2)ccn1"	"IC50"	"'='"	"165.0"	"nM"	"6.78"	""	""	"UO_0000065"	"19.52"	"0.36"	"3.08"	"9.30"	"False"	"CHEMBL2415128"	"Inhibition of JAK2 in human SET2 cells assessed as reduction of phosphorylated STAT5 level"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2412966"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"1"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"107.0"	"nM"	"6.97"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4033007"	"Inhibition of JAK2 in EPO-stimulated human TF1 cells expressing stably integrated beta-lactamase reporter gene under control of STAT5 response elements in interferon regulatory factor 1 gene promoter by fluorescence assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4078799"	""	"0"	"391.44"	"0"	"2.23"	"18"	"Cn1cc(-c2ccc(Nc3nn([C@H]4COCC[C@@H]4C#N)cc3C(N)=O)cc2)cn1"	"IC50"	"'='"	"39.0"	"nM"	"7.41"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4033007"	"Inhibition of JAK2 in EPO-stimulated human TF1 cells expressing stably integrated beta-lactamase reporter gene under control of STAT5 response elements in interferon regulatory factor 1 gene promoter by fluorescence assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4096821"	""	"0"	"378.40"	"0"	"1.41"	"19"	"N#C[C@H]1CCOC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(-n3ccnn3)cc2)n1"	"IC50"	"'='"	"254.0"	"nM"	"6.59"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4033007"	"Inhibition of JAK2 in EPO-stimulated human TF1 cells expressing stably integrated beta-lactamase reporter gene under control of STAT5 response elements in interferon regulatory factor 1 gene promoter by fluorescence assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL3914311"	""	"0"	"447.52"	"0"	"3.95"	"BDBM228211"	"CN(c1ccccc1)C1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CC1"	"IC50"	"'='"	"105.0"	"nM"	"6.98"	""	"401163"	"UO_0000065"	"15.59"	"0.29"	"3.03"	"6.18"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3938031"	""	"0"	"528.59"	"1"	"4.43"	"BDBM229404"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc([S+]([O-])C(F)F)cc3)n2)CCC(Nc2cccc(O)c2)CC1"	"IC50"	"'='"	"0.8"	"nM"	"9.10"	""	"401173"	"UO_0000065"	"17.21"	"0.34"	"4.67"	"6.23"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3940414"	""	"0"	"516.52"	"1"	"3.13"	"BDBM229466"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)F)cc3)n2)CCC(NCC(F)F)CC1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"401227"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4062803"	""	"0"	"320.36"	"0"	"3.73"	"19"	"Cc1n[nH]c2cc(Nc3nc(NC4CC4)c4occc4n3)ccc12"	"IC50"	"'='"	"4170.0"	"nM"	"5.38"	""	""	"UO_0000065"	"16.79"	"0.31"	"1.65"	"5.87"	"False"	"CHEMBL4007715"	"Inhibition of JAK2 (unknown origin) after 60 mins by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4007384"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2016"	"None"	""
"CHEMBL3963715"	""	"0"	"402.44"	"0"	"1.77"	"BDBM228767"	"CN([C@@H]1CCN(c2ncnc3[nH]ccc23)C1)S(=O)(=O)c1cccc([N+](=O)[O-])c1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399701"	"UO_0000065"	"23.01"	"0.45"	"7.49"	"7.39"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4439418"	""	"0"	"418.42"	"0"	"3.78"	"7"	"N#CC[C@H]1CC[C@H](n2c(CC(=O)NCC(F)(F)F)nc3cnc4[nH]ccc4c32)CC1"	"IC50"	"'='"	"39.0"	"nM"	"7.41"	""	""	"UO_0000065"	"17.71"	"0.34"	"3.63"	"7.45"	"False"	"CHEMBL4404829"	"Inhibition of JAK2/JAK2 in human PBMC assessed as reduction in GM-CSF-induced STAT5 phosphorylation pre-incubated for 30 mins before GM-CSF stimulation for 30 mins AlphaLISAassay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402578"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4563534"	""	"0"	"389.46"	"0"	"3.13"	"4"	"N#CCCNC(=O)Cc1nc2cnc3[nH]ccc3c2n1[C@H]1CC[C@H](CC#N)CC1"	"IC50"	"'='"	"6.6"	"nM"	"8.18"	""	""	"UO_0000065"	"21.00"	"0.39"	"5.05"	"6.64"	"False"	"CHEMBL4404825"	"Inhibition of JAK2-JH1/JH2 domain (532 to 1132 residues) (unknown origin) pre-incubated before NH2-KGGEEEEYFELVKK-CO2 substrate addition and measured after 90 mins by MS analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402578"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4476802"	""	"0"	"375.39"	"0"	"1.67"	"5"	"Cn1c(=O)n(C2CCOCC2)c2nc(-c3cnc4ccc(C#N)cn34)ncc21"	"IC50"	"'='"	"100.0"	"nM"	"7.00"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4526498"	""	"0"	"412.36"	"0"	"2.20"	"23"	"O=c1[nH]cc(F)cc1Nc1ncc2[nH]c(=O)n([C@@H]3CCOc4c(F)cccc43)c2n1"	"IC50"	"'='"	"2.3"	"nM"	"8.64"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL3589175"	""	"0"	"429.48"	"0"	"3.57"	"12"	"COc1cccc(-c2cc(C(N)=O)c3[nH]c4cc(C(=O)N5CCOCC5)ccc4c3c2)c1"	"IC50"	"'='"	"210.0"	"nM"	"6.68"	""	""	"UO_0000065"	"15.55"	"0.29"	"3.11"	"6.84"	"False"	"CHEMBL3592855"	"Inhibition of JAK2 in human SET2 cells assessed as inhibition of cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3935988"	""	"0"	"335.38"	"0"	"1.34"	"BDBM228794"	"CN(c1ccc2nn[nH]c2n1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399733"	"UO_0000065"	"27.61"	"0.51"	"7.92"	"9.03"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3920398"	""	"0"	"417.50"	"0"	"0.34"	"BDBM228700"	"CN(c1ccc(S(=O)(=O)NCCO)cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399741"	"UO_0000065"	"22.18"	"0.44"	"8.92"	"7.27"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3940099"	""	"0"	"347.43"	"0"	"2.72"	"BDBM228729"	"CCCN(c1ccc(C#N)cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399650"	"UO_0000065"	"29.53"	"0.54"	"7.54"	"12.11"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3959358"	""	"0"	"362.36"	"0"	"3.09"	"BDBM228678"	"CN(c1ccc(C(F)(F)F)cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399659"	"UO_0000065"	"28.31"	"0.54"	"7.17"	"16.84"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL2002099"	""	"0"	"306.37"	"0"	"3.47"	"(rac)-Ruxolitinib"	"N#CCC(C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"0.92"	"nM"	"9.04"	""	""	""	"29.49"	"0.54"	"5.57"	"10.86"	"False"	"CHEMBL4714135"	"Inhibition of human JAK2 by radiometric assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEK293F"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706688"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	""
"CHEMBL4281492"	""	"0"	"409.44"	"0"	"3.42"	"17i"	"COC(=O)[C@@H](C(C)C)n1c(=O)c2cc(OC)c(OC)cc2c2cnc3[nH]ccc3c21"	"IC50"	"'='"	"63.04"	"nM"	"7.20"	""	""	"UO_0000065"	"17.59"	"0.33"	"3.78"	"7.54"	"False"	"CHEMBL4261266"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]-ATP addition measured after 2 hrs by filter-binding method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257589"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4288673"	""	"0"	"320.40"	"0"	"2.98"	"7a"	"CN(C)CCCn1c(=O)c2ccccc2c2cnc3[nH]ccc3c21"	"IC50"	"'='"	"229.25"	"nM"	"6.64"	""	""	"UO_0000065"	"20.72"	"0.38"	"3.66"	"12.31"	"False"	"CHEMBL4261266"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]-ATP addition measured after 2 hrs by filter-binding method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257589"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4289375"	""	"0"	"409.44"	"0"	"3.42"	"17j"	"COC(=O)[C@H](C(C)C)n1c(=O)c2cc(OC)c(OC)cc2c2cnc3[nH]ccc3c21"	"IC50"	"'='"	"220.8"	"nM"	"6.66"	""	""	"UO_0000065"	"16.26"	"0.30"	"3.24"	"6.97"	"False"	"CHEMBL4261266"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]-ATP addition measured after 2 hrs by filter-binding method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257589"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4291298"	""	"0"	"378.43"	"0"	"2.97"	"17f"	"COc1cc2c(=O)n(C3CCNCC3)c3c4cc[nH]c4ncc3c2cc1OC"	"IC50"	"'='"	"14.7"	"nM"	"7.83"	""	""	"UO_0000065"	"20.70"	"0.38"	"4.86"	"9.65"	"False"	"CHEMBL4261266"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]-ATP addition measured after 2 hrs by filter-binding method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257589"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4559926"	""	"0"	"450.33"	"0"	"4.53"	"8n"	"O=C(CCCCCn1cc(Nc2ncc(Cl)c(Nc3ccccc3Cl)n2)cn1)NO"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	""	"UO_0000065"	"17.20"	"0.35"	"3.21"	"6.62"	"False"	"CHEMBL4347596"	"Inhibition of recombinant human JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate measured after 60 mins by LANCE assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4346670"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4439450"	""	"0"	"401.39"	"0"	"2.93"	"8s"	"CNc1nc(Nc2cnn(CCCCCCC(=O)NO)c2)ncc1C(F)(F)F"	"IC50"	"'='"	"85.0"	"nM"	"7.07"	""	""	"UO_0000065"	"17.62"	"0.34"	"4.14"	"6.04"	"False"	"CHEMBL4347596"	"Inhibition of recombinant human JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate measured after 60 mins by LANCE assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4346670"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4568644"	""	"0"	"419.85"	"0"	"3.63"	"8v"	"O=C(CCCCn1cc(Nc2ncc(Cl)c(Nc3ccc(F)cc3)n2)cn1)NO"	"IC50"	"'='"	"46.0"	"nM"	"7.34"	""	""	"UO_0000065"	"17.48"	"0.35"	"3.71"	"6.27"	"False"	"CHEMBL4347596"	"Inhibition of recombinant human JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate measured after 60 mins by LANCE assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4346670"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4279618"	""	"0"	"333.44"	"0"	"3.06"	"9"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(Cc2ccccc2)CC12CC2"	"IC50"	"'='"	"98000.0"	"nM"	"4.01"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4292871"	""	"0"	"326.36"	"0"	"1.70"	"10"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(C(=O)CN=[N+]=[N-])CC12CC2"	"IC50"	"'='"	"250.0"	"nM"	"6.60"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4280418"	""	"0"	"313.41"	"0"	"2.04"	"12"	"CC(C)C(=O)N1C[C@H](N(C)c2ncnc3[nH]ccc23)C2(CC2)C1"	"IC50"	"'='"	"2800.0"	"nM"	"5.55"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4285366"	""	"0"	"348.41"	"0"	"2.09"	"20"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(C(=O)c2ccncc2)CC12CC2"	"IC50"	"'='"	"6500.0"	"nM"	"5.19"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4282330"	""	"0"	"415.42"	"0"	"3.72"	"23"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(C(=O)c2ccccc2C(F)(F)F)CC12CC2"	"IC50"	"'='"	"9100.0"	"nM"	"5.04"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4287505"	""	"0"	"342.45"	"0"	"2.37"	"27"	"CCCCNC(=O)N1C[C@H](N(C)c2ncnc3[nH]ccc23)C2(CC2)C1"	"IC50"	"'='"	"2800.0"	"nM"	"5.55"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4285642"	""	"0"	"431.33"	"0"	"4.40"	"31"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(C(=O)Nc2ccc(Cl)cc2Cl)CC12CC2"	"IC50"	"'='"	"4700.0"	"nM"	"5.33"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4276682"	""	"0"	"514.50"	"2"	"5.29"	"37"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(C(=S)Nc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC12CC2"	"IC50"	"'='"	"11000.0"	"nM"	"4.96"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4291829"	""	"0"	"349.46"	"0"	"1.60"	"39"	"CC(C)S(=O)(=O)N1C[C@H](N(C)c2ncnc3[nH]ccc23)C2(CC2)C1"	"IC50"	"'='"	"130.0"	"nM"	"6.89"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4283883"	""	"0"	"383.48"	"0"	"2.25"	"41"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(S(=O)(=O)c2ccccc2)CC12CC2"	"IC50"	"'='"	"51.0"	"nM"	"7.29"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4289789"	""	"0"	"401.47"	"0"	"2.39"	"43"	"CN(c1ncnc2[nH]ccc12)[C@H]1CN(S(=O)(=O)c2cccc(F)c2)CC12CC2"	"IC50"	"'='"	"8.4"	"nM"	"8.08"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4258465"	"Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257478"	"1"	"Scientific Literature"	"MedChemComm"	"2018"	"None"	""
"CHEMBL4248054"	""	"0"	"624.75"	"2"	"6.60"	"13f"	"O=C(CCCCCCC(=O)Nc1ccc(Nc2nc(-c3cnn(CCCCCOc4ccccc4)c3)c3cc[nH]c3n2)cc1)NO"	"IC50"	"'='"	"21.0"	"nM"	"7.68"	""	""	"UO_0000065"	"12.29"	"0.23"	"1.08"	"4.83"	"False"	"CHEMBL4233426"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma-33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229421"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2018"	"None"	""
"CHEMBL3955361"	""	"0"	"391.48"	"0"	"2.73"	"BDBM229065"	"N#CCCCN1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)CC1"	"IC50"	"'='"	"314.0"	"nM"	"6.50"	""	"400801"	"UO_0000065"	"16.61"	"0.31"	"3.77"	"5.25"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3939054"	""	"0"	"432.50"	"0"	"3.77"	"BDBM229078"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(Cc2cccc(F)c2)CC1"	"IC50"	"'='"	"73.0"	"nM"	"7.14"	""	"400814"	"UO_0000065"	"16.50"	"0.30"	"3.37"	"7.14"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3357634"	""	"0"	"447.87"	"0"	"4.53"	"1a(Z)"	"COc1cc2ncnc(Nc3ccc(F)c(Cl)c3)c2cc1NC(=O)/C(F)=C/CN(C)C"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3385200"	"Inhibition of wild type JAK2 (unknown origin) incubated for 5 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351667"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL3986976"	""	"0"	"449.44"	"0"	"2.54"	"BDBM229312"	"CCC(F)(F)C(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CC1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"401051"	"UO_0000065"	"18.96"	"0.36"	"5.98"	"6.56"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4110026"	""	"0"	"447.47"	"0"	"3.33"	"BDBM229377"	"Cc1ccc(NC(=O)N2CC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)C2)cc1F"	"IC50"	"'='"	"114.0"	"nM"	"6.94"	""	"401116"	"UO_0000065"	"15.52"	"0.29"	"3.61"	"5.38"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4241958"	""	"0"	"431.54"	"0"	"4.24"	"11"	"C=CC(=O)Nc1cccc(-c2ccc(C(N)=O)c3[nH]c4c(c23)CCC(C(C)(C)O)C4)c1C"	"IC50"	"'='"	"3300.0"	"nM"	"5.48"	""	""	"UO_0000065"	"12.70"	"0.23"	"1.24"	"5.07"	"False"	"CHEMBL4235700"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229517"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2018"	"None"	""
"CHEMBL3910522"	""	"0"	"464.55"	"0"	"2.82"	"BDBM229326"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(S(=O)(=O)c2ccccc2)CC1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"401065"	"UO_0000065"	"19.37"	"0.37"	"6.18"	"6.71"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3893139"	""	"0"	"494.58"	"0"	"2.83"	"BDBM229330"	"COc1cccc(S(=O)(=O)N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)CC2)c1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"401069"	"UO_0000065"	"17.23"	"0.33"	"5.69"	"5.95"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4114891"	""	"0"	"429.48"	"0"	"3.19"	"BDBM229346"	"Cc1ccc(NC(=O)N2CC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)C2)cc1"	"IC50"	"'='"	"69.0"	"nM"	"7.16"	""	"401085"	"UO_0000065"	"16.67"	"0.31"	"3.97"	"5.55"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3982094"	""	"0"	"541.56"	"1"	"2.84"	"BDBM229384"	"CC(C)NC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)(F)F)cc3)n2)CC1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"401123"	"UO_0000065"	"16.06"	"0.32"	"5.86"	"5.33"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3911564"	""	"0"	"370.43"	"0"	"2.64"	"BDBM229446"	"CNC1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CC1"	"IC50"	"'='"	"264.0"	"nM"	"6.58"	""	"401207"	"UO_0000065"	"17.76"	"0.33"	"3.94"	"6.05"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3929641"	""	"0"	"433.49"	"0"	"3.92"	"BDBM229454"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(Nc2ccccc2)CC1"	"IC50"	"'='"	"0.6"	"nM"	"9.22"	""	"401214"	"UO_0000065"	"21.27"	"0.39"	"5.30"	"7.58"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3923034"	""	"0"	"427.48"	"0"	"2.14"	"BDBM228271"	"COC1CN(C2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccnc(F)c4)n3)CC2)C1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"401222"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3952595"	""	"0"	"471.54"	"0"	"4.08"	"BDBM229464"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(NCc2ccc(C#N)cc2)CC1"	"IC50"	"'='"	"1037.0"	"nM"	"5.98"	""	"401225"	"UO_0000065"	"12.69"	"0.23"	"1.90"	"4.51"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3894383"	""	"0"	"460.49"	"0"	"3.45"	"BDBM228333"	"CC(C)(C)OC(=O)N1CC[C@](CC#N)(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@@H](F)C1"	"IC50"	"'='"	"83.0"	"nM"	"7.08"	""	"401277"	"UO_0000065"	"15.38"	"0.29"	"3.63"	"5.61"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3912531"	""	"0"	"456.48"	"0"	"2.49"	"BDBM229517"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(C(=O)O[C@H]2CCOC2)CC1"	"IC50"	"'='"	"47.0"	"nM"	"7.33"	""	"401282"	"UO_0000065"	"16.05"	"0.30"	"4.84"	"5.41"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"1"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"0.6"	"nM"	"9.22"	""	""	"UO_0000065"	"29.52"	"0.55"	"7.68"	"10.37"	"False"	"CHEMBL3388144"	"Inhibition of human recombinant JAK2"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351789"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL2062810"	""	"0"	"490.63"	"0"	"4.07"	"36"	"CC(C)S(=O)(=O)c1ccc(-c2cccn3nc(Nc4cccc(N5CCN(C)CC5)c4)nc23)cc1"	"IC50"	"'='"	"85.0"	"nM"	"7.07"	""	""	"UO_0000065"	"14.41"	"0.28"	"3.00"	"8.54"	"False"	"CHEMBL2067179"	"Inhibition of JAK2 in human TF-1 cells using GM-CSF pretreated for 1 hr prior to GM-CSF addition measured after 5 hrs by FRET based GeneBLAzer assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"CHEMBL3307972"	""
"CHEMBL2062799"	""	"0"	"394.46"	"0"	"3.55"	"24"	"COc1ccc(Nc2nc3c(-c4ccc(S(C)(=O)=O)cc4)cccn3n2)cc1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"21.61"	"0.42"	"4.97"	"9.96"	"False"	"CHEMBL2067611"	"Inhibition of human JAK2 expressed in baculovirus using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate preincubated for 1 hr measured after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2035183"	""	"0"	"478.62"	"1"	"5.03"	"14j, 95:5 trans/Cis mixture"	"C1=C/COCc2cc(ccc2OCCN2CCCC2)Nc2nccc(n2)-c2ccc(s2)COC/1"	"IC50"	"'='"	"7.3"	"nM"	"8.14"	""	""	"UO_0000065"	"17.00"	"0.33"	"3.11"	"11.84"	"False"	"CHEMBL2040119"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2034857"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2035051"	""	"0"	"473.58"	"0"	"4.36"	"14c, 95:5 trans/Cis mixture"	"C1=C/COCc2cc(ccc2OCCN2CCCC2)Nc2nccc(n2)-c2cncc(c2)COC/1"	"IC50"	"'='"	"290.0"	"nM"	"6.54"	""	""	"UO_0000065"	"13.80"	"0.26"	"2.18"	"8.01"	"False"	"CHEMBL2040119"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2034857"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL3114784"	""	"0"	"497.53"	"0"	"4.23"	"11b"	"O=C1NC(=O)C(c2c[nH]c3ccccc23)=C1Nc1cccc(OC2CCCN(c3ccnc(F)c3)C2)c1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3118993"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112442"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3114785"	""	"0"	"469.48"	"0"	"3.45"	"11c"	"O=C1NC(=O)C(c2c[nH]c3ccccc23)=C1Nc1cccc(OC2CN(c3ccnc(F)c3)C2)c1"	"IC50"	"'='"	"10080.0"	"nM"	"5.00"	""	""	"UO_0000065"	"10.64"	"0.19"	"1.55"	"5.03"	"False"	"CHEMBL3118993"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112442"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3114782"	""	"0"	"342.33"	"0"	"1.66"	"10b"	"O=C1C=C(Nc2cccc(OCCNc3ccnc(F)c3)c2)C(=O)N1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3118993"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112442"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3335693"	""	"0"	"373.44"	"0"	"1.25"	"18"	"CS(=O)(=O)N1CCC[C@H](Nc2ncncc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"181.0"	"nM"	"6.74"	""	""	"UO_0000065"	"18.05"	"0.35"	"5.49"	"5.77"	"False"	"CHEMBL3374010"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 1 hr in presence of [gamma-33P]ATP by scintillation counting analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351377"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL2062794"	""	"0"	"316.36"	"0"	"4.15"	"19"	"COc1ccccc1-c1cccn2nc(Nc3ccccc3)nc12"	"IC50"	"'='"	"136.0"	"nM"	"6.87"	""	""	"UO_0000065"	"21.70"	"0.39"	"2.72"	"13.35"	"False"	"CHEMBL2067611"	"Inhibition of human JAK2 expressed in baculovirus using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate preincubated for 1 hr measured after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2062801"	""	"0"	"442.52"	"0"	"2.95"	"26"	"CS(=O)(=O)c1ccc(Nc2nc3c(-c4ccc(S(C)(=O)=O)cc4)cccn3n2)cc1"	"IC50"	"'='"	"1.3"	"nM"	"8.89"	""	""	"UO_0000065"	"20.08"	"0.40"	"5.94"	"8.04"	"True"	"CHEMBL2067611"	"Inhibition of human JAK2 expressed in baculovirus using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate preincubated for 1 hr measured after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2062805"	""	"0"	"462.58"	"0"	"3.30"	"30"	"CN1CCN(c2ccc(Nc3nc4c(-c5ccc(S(C)(=O)=O)cc5)cccn4n3)cc2)CC1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"18.42"	"0.35"	"5.22"	"10.29"	"False"	"CHEMBL2067611"	"Inhibition of human JAK2 expressed in baculovirus using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate preincubated for 1 hr measured after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2062529"	""	"0"	"545.71"	"1"	"3.76"	"34"	"CN1CCN(C2CCN(c3cccc(Nc4nc5c(-c6ccc(S(C)(=O)=O)cc6)cccn5n4)c3)CC2)CC1"	"IC50"	"'='"	"1.4"	"nM"	"8.85"	""	""	"UO_0000065"	"16.22"	"0.31"	"5.09"	"10.29"	"False"	"CHEMBL2067611"	"Inhibition of human JAK2 expressed in baculovirus using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate preincubated for 1 hr measured after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2062801"	""	"0"	"442.52"	"0"	"2.95"	"26"	"CS(=O)(=O)c1ccc(Nc2nc3c(-c4ccc(S(C)(=O)=O)cc4)cccn3n2)cc1"	"IC50"	"'='"	"118.0"	"nM"	"6.93"	""	""	"UO_0000065"	"15.66"	"0.32"	"3.98"	"6.27"	"False"	"CHEMBL2067179"	"Inhibition of JAK2 in human TF-1 cells using GM-CSF pretreated for 1 hr prior to GM-CSF addition measured after 5 hrs by FRET based GeneBLAzer assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"CHEMBL3307972"	""
"CHEMBL2062808"	""	"0"	"532.67"	"1"	"3.84"	"33"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4cccc(N5CCC(N6CCOCC6)CC5)c4)nc23)cc1"	"IC50"	"'='"	"89.0"	"nM"	"7.05"	""	""	"UO_0000065"	"13.24"	"0.25"	"3.21"	"7.66"	"False"	"CHEMBL2067179"	"Inhibition of JAK2 in human TF-1 cells using GM-CSF pretreated for 1 hr prior to GM-CSF addition measured after 5 hrs by FRET based GeneBLAzer assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"CHEMBL3307972"	""
"CHEMBL3925083"	""	"0"	"377.51"	"0"	"2.42"	"BDBM185701"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)NC2CCC2)CC1"	"IC50"	"'='"	"101.0"	"nM"	"7.00"	""	"335040"	"UO_0000065"	"18.53"	"0.37"	"4.58"	"7.69"	"True"	"CHEMBL3887373"	"Enzymatic Assay: Methods: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK-2 and JAK-3) or the IRS-1 peptide (JAK-1 and Tyk-2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 microliter total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 micromolar for JAK-2 and JAK-3, 40 micromolar for JAK-1 and 7 micromolar for Tyk-2)), 2% DMSO and 1 micromolar peptide substrate (JAKtide for JAK-2 and JAK-3 or IRS-1 peptide for JAK-1 and Tyk-2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 microliter reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK-2, 1 nM JAK-3, 7 nM Tyk2 or 20 nM JAK-1. The assay was run for 240 minutes for JAK-1, 150 minutes for JAK-2, 90 minutes for JAK-3."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886293"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL2062791"	""	"0"	"288.33"	"0"	"1.38"	"16"	"CS(=O)(=O)c1cccc(-c2cccn3nc(N)nc23)c1"	"IC50"	"'='"	"2165.0"	"nM"	"5.67"	""	""	"UO_0000065"	"19.65"	"0.39"	"4.28"	"6.27"	"False"	"CHEMBL2067611"	"Inhibition of human JAK2 expressed in baculovirus using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate preincubated for 1 hr measured after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL4112669"	""	"0"	"444.47"	"0"	"2.42"	"BDBM237753"	"COCCCOC(=O)N1CC[C@@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@H](C#N)C1"	"IC50"	"'='"	"275.0"	"nM"	"6.56"	""	"414857"	"UO_0000065"	"14.76"	"0.28"	"4.14"	"4.84"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL2062808"	""	"0"	"532.67"	"1"	"3.84"	"33"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4cccc(N5CCC(N6CCOCC6)CC5)c4)nc23)cc1"	"IC50"	"'='"	"1.1"	"nM"	"8.96"	""	""	"UO_0000065"	"16.82"	"0.32"	"5.12"	"9.73"	"False"	"CHEMBL2067611"	"Inhibition of human JAK2 expressed in baculovirus using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate preincubated for 1 hr measured after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL4113802"	""	"0"	"440.48"	"0"	"3.19"	"BDBM237762"	"N#C[C@@H]1CN(C(=O)OCCC2CC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"414866"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL2062809"	""	"0"	"461.59"	"0"	"4.35"	"35"	"CN1CCC(c2cccc(Nc3nc4c(-c5ccc(S(C)(=O)=O)cc5)cccn4n3)c2)CC1"	"IC50"	"'='"	"0.7"	"nM"	"9.15"	""	""	"UO_0000065"	"19.83"	"0.38"	"4.80"	"11.50"	"True"	"CHEMBL2067611"	"Inhibition of human JAK2 expressed in baculovirus using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate preincubated for 1 hr measured after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL4108708"	""	"0"	"442.50"	"0"	"3.43"	"BDBM237771"	"CC(C)(C)COC(=O)N1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@H](C#N)C1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"414875"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4112892"	""	"0"	"462.49"	"0"	"3.59"	"BDBM237773"	"N#C[C@@H]1CN(C(=O)OCc2ccccc2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"414877"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4115087"	""	"0"	"456.48"	"0"	"2.57"	"BDBM237781"	"N#C[C@@H]1CN(C(=O)OC2CCOCC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"414885"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL2062800"	""	"0"	"442.52"	"0"	"2.95"	"25"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4cccc(S(C)(=O)=O)c4)nc23)cc1"	"IC50"	"'='"	"490.0"	"nM"	"6.31"	""	""	"UO_0000065"	"14.26"	"0.29"	"3.36"	"5.71"	"False"	"CHEMBL2067179"	"Inhibition of JAK2 in human TF-1 cells using GM-CSF pretreated for 1 hr prior to GM-CSF addition measured after 5 hrs by FRET based GeneBLAzer assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"CHEMBL3307972"	""
"CHEMBL2062806"	""	"0"	"476.61"	"0"	"3.29"	"31"	"CN1CCN(Cc2cccc(Nc3nc4c(-c5ccc(S(C)(=O)=O)cc5)cccn4n3)c2)CC1"	"IC50"	"'='"	"345.0"	"nM"	"6.46"	""	""	"UO_0000065"	"13.56"	"0.26"	"3.17"	"7.80"	"False"	"CHEMBL2067179"	"Inhibition of JAK2 in human TF-1 cells using GM-CSF pretreated for 1 hr prior to GM-CSF addition measured after 5 hrs by FRET based GeneBLAzer assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"CHEMBL3307972"	""
"CHEMBL2062529"	""	"0"	"545.71"	"1"	"3.76"	"34"	"CN1CCN(C2CCN(c3cccc(Nc4nc5c(-c6ccc(S(C)(=O)=O)cc6)cccn5n4)c3)CC2)CC1"	"IC50"	"'='"	"177.0"	"nM"	"6.75"	""	""	"UO_0000065"	"12.37"	"0.24"	"2.99"	"7.84"	"False"	"CHEMBL2067179"	"Inhibition of JAK2 in human TF-1 cells using GM-CSF pretreated for 1 hr prior to GM-CSF addition measured after 5 hrs by FRET based GeneBLAzer assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"CHEMBL3307972"	""
"CHEMBL1789941"	"RUXOLITINIB"	"4"	"306.37"	"0"	"3.47"	"2"	"N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"0.7"	"nM"	"9.15"	""	""	"UO_0000065"	"29.88"	"0.54"	"5.68"	"11.01"	"False"	"CHEMBL3118993"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112442"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL2035053"	""	"0"	"487.60"	"0"	"4.92"	"14e, 95:5 trans/Cis mixture"	"Cc1cnc2nc1-c1ccnc(c1)OCC/C=C/COCc1cc(ccc1OCCN1CCCC1)N2"	"IC50"	"'='"	"14.0"	"nM"	"7.85"	""	""	"UO_0000065"	"16.11"	"0.30"	"2.93"	"9.62"	"False"	"CHEMBL2040119"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2034857"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2443139"	""	"0"	"466.54"	"0"	"4.19"	"31"	"CC(C)Nc1ccc(Oc2cc(O)cc(O)c2-c2cc(C(=O)NC3CCN(C)CC3)no2)cc1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2443999"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2439976"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2013"	"None"	""
"CHEMBL4078655"	""	"0"	"336.42"	"0"	"0.51"	"13"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)NC2CC2)C1"	"IC50"	"'='"	"940.0"	"nM"	"6.03"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4090590"	""	"0"	"322.43"	"0"	"2.00"	"18"	"CCCS(=O)(=O)C[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"550.0"	"nM"	"6.26"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL2376437"	""	"0"	"419.49"	"0"	"3.40"	"12b"	"CC(=O)N[C@@H]1CCc2ccc(Oc3cnc4[nH]cc(C(=O)N[C@H](C)C5CC5)c4n3)cc21"	"IC50"	"'='"	"16220.0"	"nM"	"4.79"	""	""	"UO_0000065"	"11.42"	"0.21"	"1.39"	"4.39"	"False"	"CHEMBL2378973"	"Inhibition of JAK2 in human PBMC expressing CD14 assessed as inhibition of GM-CSF-induced STAT5a phosphorylation"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375291"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2376438"	""	"0"	"487.52"	"0"	"1.97"	"12c"	"CC(=O)N[C@@H]1CCc2ccc(Oc3cnc4[nH]cc(C(=O)N[C@H](C)C(=O)N5CC(C#N)C5)c4n3)cc21"	"IC50"	"'='"	"1350.0"	"nM"	"5.87"	""	""	"UO_0000065"	"12.04"	"0.22"	"3.90"	"3.83"	"False"	"CHEMBL2378977"	"Inhibition of JAK2 (unknown origin) expressed in SF21 cells using Biotin-KAIETDKEYYTVKD as substrate and [33Pgamma]ATP incubated for 10 mins prior to substrate addition measured after 30 mins by Topcount analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375291"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"CHEMBL4106362"	""
"CHEMBL2381975"	""	"0"	"493.54"	"0"	"2.18"	"14, table2"	"Cc1cc(Nc2nc(N[C@@H](C)c3ccc(F)cn3)c(F)c(N3CCN(S(C)(=O)=O)CC3)n2)n[nH]1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"17.27"	"0.34"	"6.34"	"6.46"	"False"	"CHEMBL2383938"	"Inhibition of JAK2 (unknown origin) using biotinylated TYK2 peptide as substrate after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2380256"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2381984"	""	"0"	"435.41"	"0"	"3.04"	"10"	"Cc1cc(Nc2nc(O[C@@H](C)c3ncc(F)cc3F)c(F)c(N3CCOCC3)n2)n[nH]1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	""	"UO_0000065"	"19.29"	"0.37"	"5.36"	"8.31"	"False"	"CHEMBL2383938"	"Inhibition of JAK2 (unknown origin) using biotinylated TYK2 peptide as substrate after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2380256"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2381982"	""	"0"	"417.42"	"0"	"2.90"	"8"	"Cc1cc(Nc2nc(O[C@@H](C)c3ccc(F)cn3)c(F)c(N3CCOCC3)n2)n[nH]1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	""	"UO_0000065"	"20.12"	"0.38"	"5.50"	"8.31"	"False"	"CHEMBL2383938"	"Inhibition of JAK2 (unknown origin) using biotinylated TYK2 peptide as substrate after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2380256"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2381978"	""	"0"	"433.42"	"0"	"2.03"	"4"	"COc1cc(Nc2nc(N[C@@H](C)c3ncc(F)cn3)c(F)c(N3CCOCC3)n2)n[nH]1"	"IC50"	"'='"	"37.0"	"nM"	"7.43"	""	""	"UO_0000065"	"17.15"	"0.33"	"5.40"	"5.90"	"False"	"CHEMBL2383938"	"Inhibition of JAK2 (unknown origin) using biotinylated TYK2 peptide as substrate after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2380256"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL3128069"	""	"0"	"470.53"	"0"	"3.16"	"8e"	"Cc1nc([C@](C)(O)CO)sc1-c1cnc(N)c(O[C@H](C)c2cc(F)ccc2-n2nccn2)c1"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	""	"UO_0000065"	"16.83"	"0.33"	"4.76"	"5.99"	"False"	"CHEMBL3129257"	"Inhibition of JAK2 (unknown origin) using Km levels of ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3124869"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL4063642"	""	"0"	"350.45"	"0"	"0.85"	"38"	"CN(C1CC1)S(=O)(=O)N[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"328.0"	"nM"	"6.48"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3655104"	""	"0"	"363.45"	"0"	"0.60"	"40"	"CN(CCC#N)S(=O)(=O)N[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"412.0"	"nM"	"6.38"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL1789941"	"RUXOLITINIB"	"4"	"306.37"	"0"	"3.47"	"3"	"N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"677.0"	"nM"	"6.17"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4098094"	""	"0"	"338.44"	"0"	"0.76"	"12"	"CCCNS(=O)(=O)N[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4082035"	""	"0"	"363.45"	"0"	"0.65"	"15"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)NCCCC#N)C1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3658860"	""	"0"	"336.46"	"0"	"2.39"	"19"	"CCCCS(=O)(=O)C[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"4090.0"	"nM"	"5.39"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4099048"	""	"0"	"348.43"	"0"	"1.15"	"35"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)CCCC#N)C1"	"IC50"	"'>'"	"6930.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4066404"	""	"0"	"365.50"	"0"	"2.23"	"41"	"CCCCN(C)S(=O)(=O)C[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'>'"	"20000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4475216"	""	"0"	"521.58"	"1"	"3.32"	"6f"	"COC[C@@H](C)Nc1cc(NC(=O)N2CCCc3cc(CN4CCCCOC4=O)c(C=O)nc32)ncc1C#N"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4339991"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4339212"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4516272"	""	"0"	"394.41"	"0"	"2.90"	"8"	"CN(C)C(=O)c1cnc(Nc2ccc(F)cn2)cc1Nc1ccccc1C(N)=O"	"IC50"	"'>'"	"2000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4414788"	"Inhibition of JAK2 JH1 domain (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414548"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4647276"	""	"0"	"353.43"	"0"	"2.21"	"34"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](CC(=O)N4CC(C#N)C4)CC3)c12"	"IC50"	"'='"	"64.0"	"nM"	"7.19"	""	""	"UO_0000065"	"20.35"	"0.38"	"4.98"	"6.81"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL601719"	"CRIZOTINIB"	"4"	"450.35"	"1"	"5.04"	"4"	"C[C@@H](Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl"	"IC50"	"'='"	"27.0"	"nM"	"7.57"	""	""	"UO_0000065"	"16.81"	"0.34"	"2.53"	"9.70"	"False"	"CHEMBL4341687"	"Inhibition of human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr by Z'-LYTE assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340536"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2019"	"CHEMBL3308860"	""
"CHEMBL4248256"	""	"0"	"410.48"	"0"	"1.34"	"10b"	"C=CC(=O)N1CCC(Cn2nc(-c3cnn(CCOC)c3)c3c(N)ncnc32)CC1"	"IC50"	"'='"	"497.4"	"nM"	"6.30"	""	""	"UO_0000065"	"15.36"	"0.29"	"4.96"	"5.39"	"False"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4248368"	""	"0"	"381.44"	"0"	"1.11"	"10h"	"COCCn1cc(-c2nn(CC3CCN(C#N)CC3)c3ncnc(N)c23)cn1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4244148"	""	"0"	"352.40"	"0"	"1.16"	"12a"	"C=CC(=O)N1CCCC(n2nc(-c3cnn(C)c3)c3c(N)ncnc32)C1"	"IC50"	"'='"	"396.2"	"nM"	"6.40"	""	""	"UO_0000065"	"18.17"	"0.34"	"5.24"	"5.94"	"False"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4241889"	""	"0"	"427.51"	"0"	"0.64"	"12f"	"COCCn1cc(-c2nn(C3CCCN(C(=O)CN(C)C)C3)c3ncnc(N)c23)cn1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4244856"	""	"0"	"367.42"	"0"	"1.04"	"12h"	"COCCn1cc(-c2nn(C3CCCN(C#N)C3)c3ncnc(N)c23)cn1"	"IC50"	"'='"	"197.4"	"nM"	"6.71"	""	""	"UO_0000065"	"18.25"	"0.34"	"5.66"	"5.42"	"False"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4466590"	""	"0"	"488.57"	"0"	"3.79"	"16"	"Cc1cnc(Nc2cccnc2F)nc1-c1c[nH]c2c(NC(=O)[C@@H](C)N3CCN(C)CC3)cccc12"	"IC50"	"'='"	"30000.0"	"nM"	"4.52"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4406243"	"Inhibition of recombinant human N-terminal GST-tagged JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-labeled GEEPLYWSFPAKKK-NH2 peptide as substrate after 10 mins in presence of 5 mM ATP by caliper mobility shift assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402602"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL3909605"	""	"0"	"357.39"	"0"	"1.77"	"BDBM229519"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(N)CC1"	"IC50"	"'='"	"161.0"	"nM"	"6.79"	""	"401238"	"UO_0000065"	"19.01"	"0.36"	"5.02"	"5.01"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3910324"	""	"0"	"472.53"	"0"	"3.47"	"BDBM229480"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(NCc2ccc(C#N)cc2)CC1"	"IC50"	"'='"	"851.0"	"nM"	"6.07"	""	"401243"	"UO_0000065"	"12.85"	"0.24"	"2.60"	"4.17"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4445892"	""	"0"	"453.52"	"0"	"2.40"	"18"	"CCNC(=O)c1ncc(Nc2ncc(F)c(N3C[C@H]4CC[C@H](C3)N4C(=O)C3CC3)n2)cc1C"	"IC50"	"'='"	"12166.0"	"nM"	"4.92"	""	""	"UO_0000065"	"10.84"	"0.20"	"2.51"	"4.76"	"False"	"CHEMBL4411592"	"Inhibition of JAK2 homodimer signaling pathway in human spiked CD34 +ve cells of whole blood assessed as reduction in EPO induced STAT5 phosphorylation preincubated for 45 mins followed by EPO addition and measured measured after 15 mins by FACS assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4411260"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4460904"	""	"0"	"420.52"	"0"	"2.56"	"12"	"CCNC(=O)c1ccc(Nc2nccc(N3C[C@@H]4CC[C@H]3CN4C(=O)C3CC3)n2)cc1"	"IC50"	"'='"	"2782.0"	"nM"	"5.56"	""	""	"UO_0000065"	"13.21"	"0.24"	"3.00"	"6.14"	"False"	"CHEMBL4411595"	"Inhibition of human JAK2 using fluorescence labeled peptide as substrate and using 1 mM ATP by microfluidic based mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4411260"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4580985"	""	"0"	"371.42"	"0"	"1.68"	"17"	"Cn1cc(Nc2ncc(F)c(N3C[C@H]4CC[C@H](C3)N4C(=O)C3CC3)n2)cn1"	"IC50"	"'='"	"488.0"	"nM"	"6.31"	""	""	"UO_0000065"	"16.99"	"0.32"	"4.63"	"7.97"	"False"	"CHEMBL4411595"	"Inhibition of human JAK2 using fluorescence labeled peptide as substrate and using 1 mM ATP by microfluidic based mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4411260"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"1"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"77.0"	"nM"	"7.11"	""	""	"UO_0000065"	"22.77"	"0.42"	"5.57"	"8.00"	"True"	"CHEMBL4411595"	"Inhibition of human JAK2 using fluorescence labeled peptide as substrate and using 1 mM ATP by microfluidic based mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4411260"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL2376159"	""	"0"	"448.87"	"0"	"2.03"	"10"	"C[C@@H](NC(=O)c1c[nH]c2ncc(-c3cnc4cc(Cl)ccn34)nc12)C(=O)N1CC(C#N)C1"	"IC50"	"'='"	"57.0"	"nM"	"7.24"	""	""	"UO_0000065"	"16.14"	"0.31"	"5.21"	"5.49"	"False"	"CHEMBL2378515"	"Inhibition of JAK2 (unknown origin) using [33gammaP]ATP and Biotin-KAIETDKEYYTVKD as substrate incubated for 10 mins prior to substrate addition measured after 30 mins by filtration assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375236"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL4436572"	""	"0"	"479.65"	"1"	"5.81"	"18i"	"CCCCN(C)C1CCN(c2ccc(Nc3ncc(C)c(-c4cnn(C(C)C)c4)n3)cc2F)CC1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	""	"UO_0000065"	"18.14"	"0.34"	"2.89"	"14.01"	"False"	"CHEMBL4323930"	"Inhibition of human JAK2 (808 to end residues) using KTFCGTPEYLAP as substrate after 40 mins in presence of [gamma33P]-ATP by scintillation counting based radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4321837"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4085457"	"PF-06651600"	"3"	"285.35"	"0"	"1.94"	"11"	"C=CC(=O)N1C[C@H](Nc2ncnc3[nH]ccc23)CC[C@@H]1C"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"True"	"CHEMBL4005719"	"Inhibition of recombinant human GST-tagged cytoplasmic JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by microfluidic assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4004825"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4108862"	""	"0"	"443.51"	"0"	"3.50"	"BDBM229344"	"Cc1ccc(NC(=O)N2CC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)C2)cc1C"	"IC50"	"'='"	"191.0"	"nM"	"6.72"	""	"401083"	"UO_0000065"	"15.15"	"0.28"	"3.22"	"5.21"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4107770"	""	"0"	"451.44"	"0"	"3.16"	"BDBM229350"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CN(C(=O)Nc2cc(F)ccc2F)C1"	"IC50"	"'='"	"158.0"	"nM"	"6.80"	""	"401089"	"UO_0000065"	"15.07"	"0.28"	"3.64"	"5.27"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3944525"	""	"0"	"409.49"	"0"	"2.55"	"BDBM229386"	"CC(C)NC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)CC1"	"IC50"	"'='"	"59.0"	"nM"	"7.23"	""	"401125"	"UO_0000065"	"17.65"	"0.33"	"4.68"	"5.60"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3951300"	""	"0"	"467.94"	"0"	"4.58"	"BDBM228202"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(Nc2ccccc2Cl)CC1"	"IC50"	"'='"	"940.0"	"nM"	"6.03"	""	"401154"	"UO_0000065"	"12.88"	"0.25"	"1.45"	"4.95"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3950370"	""	"0"	"466.95"	"1"	"5.18"	"BDBM229429"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(Nc2ccc(Cl)cc2)CC1"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	"401181"	"UO_0000065"	"16.49"	"0.32"	"2.52"	"7.08"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3955899"	""	"0"	"448.51"	"0"	"3.00"	"BDBM229493"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(NCc2cccnc2)CC1"	"IC50"	"'='"	"1053.0"	"nM"	"5.98"	""	"401259"	"UO_0000065"	"13.33"	"0.25"	"2.98"	"4.44"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3126347"	""	"0"	"415.28"	"0"	"4.75"	"25"	"CC(C)(O)c1cc(Cl)c(Nc2nc3ccncc3c3c(=O)[nH]ccc23)c(Cl)c1"	"IC50"	"'='"	"0.5"	"nM"	"9.30"	""	""	"UO_0000065"	"22.40"	"0.45"	"4.55"	"10.23"	"False"	"CHEMBL3131376"	"Inhibition of recombinant Jak2 (unknown origin) using biotinylated synthetic peptide substrate by homogeneous time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3124786"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3126343"	""	"0"	"441.20"	"1"	"5.42"	"18"	"O=c1[nH]ccc2c(Nc3c(Cl)cc(OC(F)(F)F)cc3Cl)nc3ccncc3c12"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"19.32"	"0.40"	"3.10"	"10.67"	"False"	"CHEMBL3131376"	"Inhibition of recombinant Jak2 (unknown origin) using biotinylated synthetic peptide substrate by homogeneous time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3124786"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3126349"	""	"0"	"437.23"	"0"	"4.82"	"31"	"O=c1[nH]ccc2c(Nc3c(Cl)cc(C(O)C(F)F)cc3Cl)nc3ccncc3c12"	"IC50"	"'='"	"26.0"	"nM"	"7.58"	""	""	"UO_0000065"	"17.35"	"0.36"	"2.77"	"8.34"	"False"	"CHEMBL3131375"	"Inhibition of Jak2 (unknown origin) assessed as inhibition of STAT5 phosphorylation by cell-based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3124786"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL1289218"	""	"0"	"336.32"	"0"	"3.47"	"1"	"CC(C)[C@@H](Nc1nc2cc[nH]c(=O)c2c2cnccc12)C(F)(F)F"	"IC50"	"'='"	"40.0"	"nM"	"7.40"	""	""	"UO_0000065"	"22.00"	"0.42"	"3.93"	"10.47"	"False"	"CHEMBL3131375"	"Inhibition of Jak2 (unknown origin) assessed as inhibition of STAT5 phosphorylation by cell-based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3124786"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3126344"	""	"0"	"425.20"	"1"	"5.54"	"19"	"O=c1[nH]ccc2c(Nc3c(Cl)cc(C(F)(F)F)cc3Cl)nc3ccncc3c12"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	""	"UO_0000065"	"21.17"	"0.44"	"3.46"	"12.74"	"False"	"CHEMBL3131376"	"Inhibition of recombinant Jak2 (unknown origin) using biotinylated synthetic peptide substrate by homogeneous time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3124786"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3949226"	""	"0"	"435.58"	"0"	"2.50"	"BDBM255030"	"CN1CN([C@H]2CC[C@H](CN3CCN(CCC#N)CC3)CC2)c2c(cnc3[nH]ccc23)C1=O"	"IC50"	"'='"	"490.0"	"nM"	"6.31"	""	"443886"	"UO_0000065"	"14.49"	"0.27"	"3.81"	"7.65"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3898972"	""	"0"	"431.56"	"0"	"2.40"	"BDBM255027"	"CN(C[C@H]1CC[C@H](N2CN(C3CC3)C(=O)c3cnc4[nH]ccc4c32)CC1)S(C)(=O)=O"	"IC50"	"'='"	"6.7"	"nM"	"8.17"	""	"443883"	"UO_0000065"	"18.94"	"0.37"	"5.77"	"9.12"	"False"	"CHEMBL3889258"	"Enzyme Assay: The inhibitory activity of the compounds of the present invention against JAK was measured.The respective enzymes (JAK1, JAK2, JAK3 and Tyk2) were purchased from Carna Biosciences, Inc.As a substrate of the enzymes (hereinafter referred to as substrate), LANCE Ultra ULight-JAK-1 (Tyr1023) Peptide (manufactured by PerkinElmer Inc.) was used.As an antibody for detecting phosphorylation of the substrate, LANCE Ultra Europium-anti-phospho tyrosine antibody (PT66) (manufactured by PerkinElmer Inc.) was used.The other reagents were purchased from the following.Adenosine triphosphate (ATP): Sigma-Aldrich4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES): DOJINDO LABORATORIESGlycol ether diamine tetraacetic acid (EGTA): DOJINDO LABORATORIES Magnesium chloride (MgCl2): Wako Pure Chemical Industries, Ltd.Dithiothreitol (DTT): Wako Pure Chemical Industries, Ltd.Tween 20: Sigma-AldrichEthylenediaminetetraacetic acid (EDTA): DOJINDO LABORATORIESThe compounds of the present invention, the enzymes (JAK1, JAK2, JAK3 and Tyk2), the substrate and ATP were used for assay as diluted with assay buffer.Â  As the assay buffer, one having the following composition was used.Â  HEPES (pH7.5): 50 mM EGTA: 1 mM MgCl2: 10 mM DTT: 2 mM Tween 20: 0.01% (wt/wt). The dilute concentration and the addition amount on a well plate as described hereinafter were adjusted so that the following final concentrations were achieved on the well plate."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3887014"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4110316"	""	"0"	"330.32"	"0"	"1.36"	"BDBM237895"	"N#C[C@H]1CCOC[C@@H]1n1cc(C(N)=O)c(Nc2cncc(F)c2)n1"	"IC50"	"'='"	"306.0"	"nM"	"6.51"	""	"414997"	"UO_0000065"	"19.72"	"0.37"	"5.15"	"5.48"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4113597"	""	"0"	"410.36"	"0"	"2.16"	"BDBM237901"	"N#C[C@H]1CCOC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(OCC(F)(F)F)nc2)n1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"415003"	"UO_0000065"	"20.77"	"0.40"	"6.36"	"6.65"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3893456"	""	"0"	"377.40"	"0"	"1.36"	"BDBM237918"	"N#C[C@H]1CS(=O)(=O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"60.0"	"nM"	"7.22"	""	"415013"	"UO_0000065"	"19.14"	"0.38"	"5.86"	"5.52"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4114890"	""	"0"	"380.45"	"0"	"2.22"	"BDBM229290"	"CC(C)(C)C(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"570.0"	"nM"	"6.24"	""	"401029"	"UO_0000065"	"16.41"	"0.30"	"4.02"	"5.34"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3980147"	""	"0"	"439.50"	"0"	"2.68"	"BDBM229313"	"CC1(C(=O)N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccnc(F)c4)n3)CC2)CCC1"	"IC50"	"'='"	"115.0"	"nM"	"6.94"	""	"401052"	"UO_0000065"	"15.79"	"0.30"	"4.26"	"5.34"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3929554"	""	"0"	"454.51"	"0"	"2.41"	"BDBM229324"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(S(=O)(=O)c2ccco2)CC1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"401063"	"UO_0000065"	"19.14"	"0.37"	"6.29"	"5.91"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4106728"	""	"0"	"426.46"	"0"	"1.63"	"BDBM229337"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CN(S(=O)(=O)c2ccco2)C1"	"IC50"	"'='"	"247.0"	"nM"	"6.61"	""	"401076"	"UO_0000065"	"15.49"	"0.30"	"4.98"	"4.49"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4108782"	""	"0"	"421.51"	"0"	"2.69"	"BDBM229342"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CN(C(=O)NC2CCCCC2)C1"	"IC50"	"'='"	"628.0"	"nM"	"6.20"	""	"401081"	"UO_0000065"	"14.71"	"0.27"	"3.51"	"4.81"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3115322"	""	"0"	"330.34"	"0"	"3.41"	"4"	"O=C1NN(c2ccccc2)C(=O)/C1=C/c1ccc(-c2ccccc2)o1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL3119788"	"Inhibition of JAK2 (unknown origin) by radioactive ATP method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112544"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL3984973"	""	"0"	"452.47"	"0"	"2.70"	"BDBM229125"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2ccc(F)cn2)CC1"	"IC50"	"'='"	"97.0"	"nM"	"7.01"	""	"400861"	"UO_0000065"	"15.50"	"0.29"	"4.31"	"5.58"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3979997"	""	"0"	"452.47"	"0"	"2.70"	"BDBM229127"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2cncc(F)c2)CC1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"400863"	"UO_0000065"	"18.35"	"0.34"	"5.60"	"6.60"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3905110"	""	"0"	"434.48"	"0"	"2.56"	"BDBM229136"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(Cc2cccnn2)CC1"	"IC50"	"'='"	"100.0"	"nM"	"7.00"	""	"400872"	"UO_0000065"	"16.11"	"0.30"	"4.44"	"5.57"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3933102"	""	"0"	"449.49"	"0"	"2.87"	"BDBM229159"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2cccc(O)c2)CC1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"400895"	"UO_0000065"	"20.02"	"0.37"	"6.13"	"6.76"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3958656"	""	"0"	"470.51"	"0"	"2.74"	"BDBM229193"	"CC1(COC(=O)N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)CC2)COC1"	"IC50"	"'='"	"240.0"	"nM"	"6.62"	""	"400930"	"UO_0000065"	"14.07"	"0.27"	"3.88"	"4.89"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3947243"	""	"0"	"476.51"	"0"	"3.91"	"BDBM229206"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)OCc2ccccc2F)CC1"	"IC50"	"'='"	"40.0"	"nM"	"7.40"	""	"400943"	"UO_0000065"	"15.53"	"0.29"	"3.49"	"5.86"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3938472"	""	"0"	"426.48"	"0"	"2.21"	"BDBM229208"	"COCCOC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)CC1"	"IC50"	"'='"	"71.0"	"nM"	"7.15"	""	"400945"	"UO_0000065"	"16.76"	"0.31"	"4.94"	"5.28"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3979073"	""	"0"	"459.51"	"0"	"3.16"	"BDBM229211"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)OCc2ccccn2)CC1"	"IC50"	"'='"	"156.0"	"nM"	"6.81"	""	"400948"	"UO_0000065"	"14.81"	"0.27"	"3.65"	"4.89"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3977249"	""	"0"	"470.51"	"0"	"2.89"	"BDBM228004"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(C(=O)OC2CCOCC2)CC1"	"IC50"	"'='"	"103.0"	"nM"	"6.99"	""	"400957"	"UO_0000065"	"14.85"	"0.28"	"4.10"	"5.16"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3923856"	""	"0"	"430.47"	"0"	"2.99"	"BDBM229224"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CN(C(=O)OCc2ccccc2)C1"	"IC50"	"'='"	"262.0"	"nM"	"6.58"	""	"400963"	"UO_0000065"	"15.29"	"0.28"	"3.59"	"5.21"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3964431"	""	"0"	"444.50"	"0"	"3.03"	"BDBM229229"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CN(C(=O)OCCc2ccccc2)C1"	"IC50"	"'='"	"809.0"	"nM"	"6.09"	""	"400968"	"UO_0000065"	"13.71"	"0.25"	"3.06"	"4.82"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4115453"	""	"0"	"502.55"	"1"	"1.37"	"BDBM229247"	"CS(=O)(=O)c1ccc(Nc2nn(C3(CC#N)CN(C(=O)OC4CCOCC4)C3)cc2C(N)=O)cc1"	"IC50"	"'='"	"285.0"	"nM"	"6.54"	""	"400986"	"UO_0000065"	"13.02"	"0.26"	"5.18"	"3.86"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3907706"	""	"0"	"392.46"	"0"	"2.37"	"BDBM229254"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)C2CC2)CC1"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	"400993"	"UO_0000065"	"19.86"	"0.37"	"5.43"	"6.66"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3940586"	""	"0"	"434.53"	"0"	"3.33"	"BDBM229267"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)c2cccs2)CC1"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	"401006"	"UO_0000065"	"18.63"	"0.36"	"4.77"	"6.92"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3941235"	""	"0"	"478.56"	"0"	"4.42"	"BDBM229278"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)c2cccc3ccccc23)CC1"	"IC50"	"'='"	"350.0"	"nM"	"6.46"	""	"401017"	"UO_0000065"	"13.49"	"0.24"	"2.04"	"5.52"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3939999"	""	"0"	"440.52"	"0"	"3.18"	"BDBM229396"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(NC2CCOCC2)CC1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"401134"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3946481"	""	"0"	"529.57"	"1"	"3.78"	"BDBM229398"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)F)cc3)n2)CCC(Nc2cccnc2)CC1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"401137"	"UO_0000065"	"15.53"	"0.30"	"4.44"	"5.28"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3951181"	""	"0"	"450.49"	"0"	"4.67"	"BDBM229407"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC(Nc2ccc(F)cc2)CC1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"401147"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3983487"	""	"0"	"556.59"	"1"	"4.00"	"BDBM229416"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)F)cc3)n2)CCC(N2CCC(F)(F)CC2)CC1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"401160"	"UO_0000065"	"15.63"	"0.31"	"4.70"	"6.49"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3947052"	""	"0"	"451.48"	"0"	"4.06"	"BDBM229422"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(Nc2ccc(F)cc2)CC1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	"401169"	"UO_0000065"	"17.82"	"0.33"	"3.99"	"6.61"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3911515"	""	"0"	"536.61"	"1"	"3.04"	"BDBM229436"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)F)cc3)n2)CCC(NC2CCOCC2)CC1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"401195"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3978395"	""	"0"	"420.56"	"0"	"4.01"	"BDBM229069"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(CC2CCCCC2)CC1"	"IC50"	"'='"	"319.0"	"nM"	"6.50"	""	"400805"	"UO_0000065"	"15.45"	"0.29"	"2.49"	"6.50"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3930743"	""	"0"	"456.59"	"0"	"4.58"	"BDBM229082"	"CCCc1ccc(CN2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)CC2)cc1"	"IC50"	"'='"	"888.0"	"nM"	"6.05"	""	"400818"	"UO_0000065"	"13.25"	"0.24"	"1.47"	"6.05"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3942622"	""	"0"	"472.53"	"0"	"3.65"	"BDBM229109"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2ccc3[nH]ccc3c2)CC1"	"IC50"	"'='"	"31.0"	"nM"	"7.51"	""	"400845"	"UO_0000065"	"15.89"	"0.29"	"3.86"	"5.84"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3897711"	""	"0"	"437.45"	"0"	"2.99"	"BDBM237820"	"N#C[C@@H]1CCN(Cc2cc(F)ccn2)C[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"47.0"	"nM"	"7.33"	""	"414924"	"UO_0000065"	"16.75"	"0.31"	"4.34"	"6.49"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3963053"	""	"0"	"425.47"	"0"	"2.42"	"BDBM237833"	"CC1=NOC(CN2CC[C@@H](C#N)[C@H](n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)C2)C1"	"IC50"	"'='"	"98.0"	"nM"	"7.01"	""	"414937"	"UO_0000065"	"16.47"	"0.31"	"4.59"	"5.77"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4114576"	""	"0"	"408.44"	"0"	"2.17"	"BDBM237845"	"N#C[C@@H]1CN(Cc2ccn[nH]2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"35.0"	"nM"	"7.46"	""	"414949"	"UO_0000065"	"18.25"	"0.34"	"5.29"	"5.80"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4109371"	""	"0"	"436.50"	"0"	"2.67"	"BDBM237851"	"CCn1ccnc1CN1CC[C@@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@H](C#N)C1"	"IC50"	"'='"	"82.0"	"nM"	"7.09"	""	"414955"	"UO_0000065"	"16.23"	"0.30"	"4.42"	"6.02"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4107562"	""	"0"	"427.41"	"0"	"2.24"	"BDBM237858"	"N#C[C@@H]1CS(=O)(=O)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"146.0"	"nM"	"6.84"	""	"414962"	"UO_0000065"	"15.99"	"0.32"	"4.60"	"5.22"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3920418"	""	"0"	"383.45"	"0"	"2.71"	"BDBM237890"	"COC(C)(C)c1ccc(Nc2nn([C@@H]3COCC[C@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"0.4"	"nM"	"9.40"	""	"414992"	"UO_0000065"	"24.51"	"0.46"	"6.69"	"8.16"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3938373"	""	"0"	"346.78"	"0"	"1.88"	"BDBM237893"	"N#C[C@@H]1CCOC[C@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)nc2)n1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"414995"	"UO_0000065"	"24.22"	"0.48"	"6.52"	"7.07"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4107562"	""	"0"	"427.41"	"0"	"2.24"	"BDBM237858"	"N#C[C@@H]1CS(=O)(=O)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"33.0"	"nM"	"7.48"	""	"415015"	"UO_0000065"	"17.50"	"0.35"	"5.24"	"5.72"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3931158"	""	"0"	"440.48"	"0"	"3.12"	"BDBM229192"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(C(=O)OCC2CC2)CC1"	"IC50"	"'='"	"37.0"	"nM"	"7.43"	""	"400929"	"UO_0000065"	"16.87"	"0.32"	"4.31"	"5.89"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3951569"	""	"0"	"494.56"	"0"	"4.18"	"BDBM229225"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CN(C(=O)OCCc2cccc3ccccc23)C1"	"IC50"	"'='"	"1481.0"	"nM"	"5.83"	""	"400964"	"UO_0000065"	"11.79"	"0.22"	"1.65"	"4.62"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4108920"	""	"0"	"412.45"	"0"	"1.82"	"BDBM229232"	"COCCCOC(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"603.0"	"nM"	"6.22"	""	"400971"	"UO_0000065"	"15.08"	"0.28"	"4.40"	"4.59"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4113324"	""	"0"	"425.49"	"0"	"1.74"	"BDBM229242"	"CN(C)CCCOC(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"1481.0"	"nM"	"5.83"	""	"400981"	"UO_0000065"	"13.70"	"0.26"	"4.09"	"4.50"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3934244"	""	"0"	"352.40"	"0"	"1.59"	"BDBM229289"	"CCC(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"298.0"	"nM"	"6.53"	""	"401028"	"UO_0000065"	"18.52"	"0.34"	"4.94"	"5.58"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL1789941"	"RUXOLITINIB"	"4"	"306.37"	"0"	"3.47"	"1"	"N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"0.6"	"nM"	"9.22"	""	""	"UO_0000065"	"30.10"	"0.55"	"5.75"	"11.09"	"False"	"CHEMBL4341687"	"Inhibition of human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr by Z'-LYTE assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340536"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2019"	"CHEMBL3308860"	""
"CHEMBL4544757"	""	"0"	"432.36"	"0"	"4.90"	"12m"	"CC(Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)cccc1Cl"	"IC50"	"'='"	"442.0"	"nM"	"6.36"	""	""	"UO_0000065"	"14.70"	"0.30"	"1.45"	"8.15"	"False"	"CHEMBL4341687"	"Inhibition of human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr by Z'-LYTE assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340536"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2019"	"CHEMBL3308860"	""
"CHEMBL3359921"	""	"0"	"301.39"	"0"	"1.75"	"4j"	"CC1(C)[C@H](Nc2c(C(N)=O)cnn3cccc23)CC[C@]1(C)N"	"IC50"	"'='"	"62.0"	"nM"	"7.21"	""	""	"UO_0000065"	"23.91"	"0.45"	"5.46"	"7.32"	"False"	"CHEMBL3377596"	"Inhibition of JAK2 (unknown origin) by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352641"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3359908"	""	"0"	"272.35"	"0"	"2.42"	"3b"	"CC1(C)CCC[C@H]1Nc1c(C(N)=O)cnn2cccc12"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	""	"UO_0000065"	"28.62"	"0.53"	"5.38"	"10.76"	"False"	"CHEMBL3377596"	"Inhibition of JAK2 (unknown origin) by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352641"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3359911"	""	"0"	"244.30"	"0"	"1.79"	"3e"	"NC(=O)c1cnn2cccc2c1NC1CCCC1"	"IC50"	"'='"	"250.0"	"nM"	"6.60"	""	""	"UO_0000065"	"27.02"	"0.50"	"4.81"	"9.12"	"False"	"CHEMBL3377596"	"Inhibition of JAK2 (unknown origin) by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352641"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3359914"	""	"0"	"302.38"	"0"	"1.78"	"4c"	"CC1(C)[C@H](Nc2c(C(N)=O)cnn3cccc23)CC[C@]1(C)O"	"IC50"	"'='"	"100.0"	"nM"	"7.00"	""	""	"UO_0000065"	"23.15"	"0.43"	"5.22"	"7.56"	"False"	"CHEMBL3377596"	"Inhibition of JAK2 (unknown origin) by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352641"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3359923"	""	"0"	"274.32"	"0"	"1.15"	"5b"	"C[C@@]1(O)CCC[C@H]1Nc1c(C(N)=O)cnn2cccc12"	"IC50"	"'='"	"400.0"	"nM"	"6.40"	""	""	"UO_0000065"	"23.32"	"0.44"	"5.25"	"6.91"	"False"	"CHEMBL3377596"	"Inhibition of JAK2 (unknown origin) by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352641"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3359926"	""	"0"	"283.34"	"0"	"1.93"	"5e"	"C[C@]1(C#N)CCC[C@H]1Nc1c(C(N)=O)cnn2cccc12"	"IC50"	"'='"	"31.0"	"nM"	"7.51"	""	""	"UO_0000065"	"26.50"	"0.49"	"5.58"	"7.80"	"False"	"CHEMBL3377596"	"Inhibition of JAK2 (unknown origin) by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352641"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3352892"	""	"0"	"283.34"	"0"	"1.93"	"5f"	"C[C@@]1(C#N)CCC[C@H]1Nc1c(C(N)=O)cnn2cccc12"	"IC50"	"'='"	"120.0"	"nM"	"6.92"	""	""	"UO_0000065"	"24.43"	"0.45"	"4.99"	"7.19"	"False"	"CHEMBL3377596"	"Inhibition of JAK2 (unknown origin) by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352641"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3359927"	""	"0"	"276.32"	"0"	"2.13"	"5g"	"C[C@]1(F)CCC[C@H]1Nc1c(C(N)=O)cnn2cccc12"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	""	"UO_0000065"	"28.03"	"0.53"	"5.61"	"10.69"	"False"	"CHEMBL3377596"	"Inhibition of JAK2 (unknown origin) by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352641"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL4107859"	""	"0"	"451.58"	"0"	"3.57"	"BDBM229369"	"CC(C)(C)CC(C)(C)NC(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"1481.0"	"nM"	"5.83"	""	"401108"	"UO_0000065"	"12.91"	"0.24"	"2.26"	"4.52"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3933473"	""	"0"	"469.47"	"0"	"4.20"	"BDBM229408"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(Nc2ccc(F)c(F)c2)CC1"	"IC50"	"'='"	"43.0"	"nM"	"7.37"	""	"401149"	"UO_0000065"	"15.69"	"0.30"	"3.17"	"6.06"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3892313"	""	"0"	"434.48"	"0"	"3.32"	"BDBM228199"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCC(Nc2ccccn2)CC1"	"IC50"	"'='"	"195.0"	"nM"	"6.71"	""	"401151"	"UO_0000065"	"15.44"	"0.29"	"3.39"	"4.99"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4066664"	""	"0"	"348.29"	"0"	"3.82"	"8"	"FC(F)(F)CNc1nc(Nc2ccc3cn[nH]c3c2)nc2ccoc12"	"IC50"	"'='"	"4920.0"	"nM"	"5.31"	""	""	"UO_0000065"	"15.24"	"0.29"	"1.49"	"5.79"	"False"	"CHEMBL4007715"	"Inhibition of JAK2 (unknown origin) after 60 mins by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4007384"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2016"	"None"	""
"CHEMBL3115321"	""	"0"	"337.38"	"0"	"4.47"	"3"	"O=C1Nc2ccccc2/C1=C(\c1ccccc1)c1nc2ccccc2[nH]1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL3119788"	"Inhibition of JAK2 (unknown origin) by radioactive ATP method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112544"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2325898"	""	"0"	"378.44"	"0"	"1.72"	"3t"	"N#C[C@H]1CCN(C(=O)[C@H](NC(=O)c2c[nH]c3ncc(C4CC4)nc23)C2CC2)C1"	"IC50"	"'='"	"0.5"	"nM"	"9.30"	""	""	"UO_0000065"	"24.58"	"0.45"	"7.58"	"8.10"	"False"	"CHEMBL2329570"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 30 mins by scintillation counting analysis in presence of [gamma-33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321829"	"1"	"Scientific Literature"	"J. Med. Chem."	"2013"	"None"	""
"CHEMBL2181084"	""	"0"	"488.59"	"0"	"4.20"	"21i, 85:15 trans/cis mixture"	"C1=CCOCc2cccc(c2)-c2ccnc(n2)Nc2cc(cc(OCCN3CCOCC3)c2)COC1"	"IC50"	"'='"	"96.0"	"nM"	"7.02"	""	""	"UO_0000065"	"14.36"	"0.27"	"2.82"	"9.00"	"False"	"CHEMBL2184201"	"Inhibition of recombinant JAK2 using Poly (Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176955"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL2181329"	""	"0"	"474.61"	"1"	"5.21"	"21b, 85:15 trans/cis mixture"	"CCN(CC)CCOc1ccc2cc1COCC=CCOCc1cccc(c1)-c1ccnc(n1)N2"	"IC50"	"'='"	"24.0"	"nM"	"7.62"	""	""	"UO_0000065"	"16.05"	"0.30"	"2.41"	"11.08"	"False"	"CHEMBL2184201"	"Inhibition of recombinant JAK2 using Poly (Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176955"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL2181320"	""	"0"	"375.43"	"0"	"4.20"	"16f, 85:15 trans/cis mixture"	"Oc1ccc2cc1COCC=CCOCc1cccc(c1)-c1ccnc(n1)N2"	"IC50"	"'='"	"53.0"	"nM"	"7.28"	""	""	"UO_0000065"	"19.38"	"0.35"	"3.08"	"9.51"	"False"	"CHEMBL2184201"	"Inhibition of recombinant JAK2 using Poly (Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176955"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL2181319"	""	"0"	"389.46"	"0"	"4.50"	"16e, 85:15 trans/cis mixture"	"COc1ccc2cc1COCC=CCOCc1cccc(c1)-c1ccnc(n1)N2"	"IC50"	"'='"	"70.0"	"nM"	"7.16"	""	""	"UO_0000065"	"18.37"	"0.34"	"2.65"	"10.92"	"False"	"CHEMBL2184201"	"Inhibition of recombinant JAK2 using Poly (Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176955"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL3301607"	"FILGOTINIB"	"4"	"425.51"	"0"	"1.98"	"Filgotinib"	"O=C(Nc1nc2cccc(-c3ccc(CN4CCS(=O)(=O)CC4)cc3)n2n1)C1CC1"	"IC50"	"'='"	"2400.0"	"nM"	"5.62"	""	""	""	"13.21"	"0.26"	"3.64"	"5.81"	"False"	"CHEMBL4714260"	"Inhibition of recombinant human JAK2 assessed as phosphorylation level in presence of 1 mM ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706695"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2021"	"None"	""
"CHEMBL3301607"	"FILGOTINIB"	"4"	"425.51"	"0"	"1.98"	"Filgotinib"	"O=C(Nc1nc2cccc(-c3ccc(CN4CCS(=O)(=O)CC4)cc3)n2n1)C1CC1"	"IC50"	"'='"	"171.0"	"nM"	"6.77"	""	""	""	"15.90"	"0.31"	"4.79"	"7.00"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL4747270"	""	"0"	"363.47"	"0"	"3.00"	"17c"	"CNC(=O)c1cnc2[nH]ccc2c1NC1CCN(Cc2ccccc2)CC1"	"IC50"	"'='"	"660.0"	"nM"	"6.18"	""	""	""	"17.00"	"0.31"	"3.18"	"8.46"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL4781679"	""	"0"	"388.48"	"0"	"2.87"	"17h"	"CNC(=O)c1cnc2[nH]ccc2c1NC1CCN(Cc2cccc(C#N)c2)CC1"	"IC50"	"'='"	"759.0"	"nM"	"6.12"	""	""	""	"15.75"	"0.29"	"3.25"	"6.32"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL4761631"	""	"0"	"377.49"	"0"	"3.39"	"30a"	"CNC(=O)c1cnc2[nH]ccc2c1NC1CCCN(Cc2ccccc2)CC1"	"IC50"	"'='"	"89.3"	"nM"	"7.05"	""	""	""	"18.67"	"0.34"	"3.66"	"9.65"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL4785998"	""	"0"	"397.91"	"0"	"3.78"	"31k"	"C[C@@H]1C[C@H](Nc2c(C(N)=O)cnc3[nH]ccc23)CCN1Cc1cccc(Cl)c1"	"IC50"	"'='"	"93.8"	"nM"	"7.03"	""	""	""	"17.66"	"0.34"	"3.25"	"8.07"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL1789941"	"RUXOLITINIB"	"4"	"306.37"	"0"	"3.47"	"2, INCB018424"	"N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"2.8"	"nM"	"8.55"	""	""	"UO_0000065"	"27.92"	"0.51"	"5.08"	"10.28"	"True"	"CHEMBL2155751"	"Inhibition of human JAK2 kinase domain expressed in Sf21 cells using EQEDEPEGDYFEWLE as substrate after 1 hr by HTRF assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2150873"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"CHEMBL4106362"	""
"CHEMBL3642396"	""	"0"	"505.65"	"1"	"3.28"	"BDBM99674"	"CN1CCN(c2ccc(Nc3nc4c(-c5cccc(CN(C)S(C)(=O)=O)c5)cccn4n3)cc2)CC1"	"IC50"	"'='"	"7.95"	"nM"	"8.10"	""	"216364"	"UO_0000065"	"16.02"	"0.31"	"4.82"	"9.41"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3645110"	""	"0"	"360.42"	"0"	"3.80"	"BDBM99884"	"COc1ccccc1CNc1cccn2nc(Nc3ccc(C)nc3)nc12"	"IC50"	"'='"	"27.56"	"nM"	"7.56"	""	"216552"	"UO_0000065"	"20.97"	"0.38"	"3.76"	"9.90"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3658860"	""	"0"	"336.46"	"0"	"2.39"	"BDBM159779"	"CCCCS(=O)(=O)C[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"220.0"	"nM"	"6.66"	""	"302589"	"UO_0000065"	"19.79"	"0.40"	"4.27"	"8.43"	"True"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651018"	""	"0"	"370.80"	"0"	"3.49"	"BDBM153195"	"C=C(Cl)C(=O)Nc1cccc(-c2ncnc3[nH]cc(C(=O)OCC)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294143"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665207"	""	"0"	"495.61"	"0"	"2.75"	"BDBM112607"	"CS(=O)(=O)N1CCC[C@H](Nc2nc(NC3CCC(C#N)CC3)ncc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.1455"	"nM"	"9.84"	""	"233844"	"UO_0000065"	"19.85"	"0.38"	"7.09"	"6.45"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL4759953"	""	"0"	"520.64"	"2"	"5.61"	"13aa"	"Cc1ccc(C(=O)/C=C/C(=O)N2CCc3cc(Nc4ncc(C)c(-c5cnn(C(C)C)c5)n4)ccc3C2)cc1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	""	"16.37"	"0.30"	"2.91"	"9.16"	"False"	"CHEMBL4723820"	"Inhibition of recombinant human JAK2 (808 to end residues) KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate measured after 40 mins in presence of [gamm33P]ATP by scintillation counting method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 0.6667 hr"
"CHEMBL3647827"	""	"0"	"460.50"	"0"	"4.37"	"BDBM147932"	"N#C[C@@H]1C[C@@H](NCC2CCC2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"242.0"	"nM"	"6.62"	""	"285866"	"UO_0000065"	"14.37"	"0.27"	"2.25"	"6.08"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703082"	""	"0"	"534.51"	"1"	"3.45"	"BDBM147795"	"CN(CC(F)F)[C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"29.0"	"nM"	"7.54"	""	"285729"	"UO_0000065"	"14.10"	"0.29"	"4.09"	"5.62"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3953856"	""	"0"	"393.51"	"0"	"1.35"	"BDBM113083"	"CN(c1ncnc2[nH]ccc12)C1CCC(CS(=O)(=O)N2CC[C@@H](O)C2)CC1"	"IC50"	"'='"	"18.1"	"nM"	"7.74"	""	"234527"	"UO_0000065"	"19.68"	"0.39"	"6.39"	"7.56"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3642398"	""	"0"	"520.66"	"1"	"4.01"	"BDBM99676"	"CN(Cc1cccc(-c2cccn3nc(Nc4ccc(OCCN5CCCC5)cc4)nc23)c1)S(C)(=O)=O"	"IC50"	"'='"	"7.34"	"nM"	"8.13"	""	"216366"	"UO_0000065"	"15.62"	"0.30"	"4.12"	"8.83"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647774"	""	"0"	"516.45"	"1"	"3.59"	"BDBM147877"	"N#C[C@H]1C[C@H](N2CC(O)(C(F)(F)F)C2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"62.0"	"nM"	"7.21"	""	"285811"	"UO_0000065"	"13.96"	"0.27"	"3.62"	"6.00"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3658089"	""	"0"	"615.70"	"2"	"6.11"	"BDBM148325"	"Cc1ccc(NC(=O)c2cccc(C(F)(F)F)c2)cc1N1CCc2nc(Nc3cccc(CN4CCN(C)CC4)c3)ncc2C1"	"IC50"	"'='"	"28.0"	"nM"	"7.55"	""	"286815"	"UO_0000065"	"12.27"	"0.23"	"1.44"	"9.86"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702899"	""	"0"	"382.42"	"0"	"2.47"	"BDBM147598"	"COC(=O)c1ncc(Nc2nn([C@H]3CCCC[C@@H]3C#N)cc2C(N)=O)cc1C"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	"285528"	"UO_0000065"	"20.32"	"0.38"	"5.30"	"5.72"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642263"	""	"0"	"384.36"	"1"	"5.17"	"BDBM99522"	"COc1ccccc1Nc1nc2c(-c3ccc(C(F)(F)F)cc3)cccn2n1"	"IC50"	"'='"	"9999.0"	"nM"	"5.00"	""	"216214"	"UO_0000065"	"13.01"	"0.24"	"-0.17"	"9.72"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3639411"	""	"0"	"463.56"	"0"	"3.38"	"BDBM99548"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4cccc(CN5CCOCC5)c4)nc23)cc1"	"IC50"	"'='"	"0.6"	"nM"	"9.22"	""	"216240"	"UO_0000065"	"19.89"	"0.38"	"5.84"	"10.38"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3650996"	""	"0"	"368.37"	"0"	"3.46"	"BDBM153172"	"C=C(C)C(=O)Nc1cc(-c2ncnc3[nH]cc(C(=O)OCC)c23)ccc1F"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294120"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642251"	""	"0"	"493.59"	"0"	"2.90"	"BDBM2061"	"C=Cc1nc(NC(=O)Nc2ccc(N3CCNCC3)cc2)nn1C(=C)c1ccc(S(C)(=O)=O)cc1"	"IC50"	"'='"	"9999.0"	"nM"	"5.00"	""	"3041"	"UO_0000065"	"10.13"	"0.20"	"2.10"	"4.12"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642347"	""	"0"	"536.66"	"1"	"3.35"	"BDBM99623"	"CN(c1ncccc1CNc1cccn2nc(Nc3ccc(OCCN4CCCC4)cc3)nc12)S(C)(=O)=O"	"IC50"	"'='"	"41.18"	"nM"	"7.38"	""	"216313"	"UO_0000065"	"13.76"	"0.27"	"4.04"	"6.31"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL4758253"	""	"0"	"406.53"	"0"	"3.71"	"13e"	"Cc1cnc(Nc2ccc3c(c2)CCN(CCCO)C3)nc1-c1cnn(C(C)C)c1"	"IC50"	"'='"	"394.0"	"nM"	"6.41"	""	""	""	"15.75"	"0.29"	"2.69"	"8.10"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL4791651"	""	"0"	"401.52"	"0"	"4.24"	"13u"	"Cc1cnc(Nc2ccc3c(c2)CCN(CCC#N)C3)nc1-c1cnn(C(C)C)c1"	"IC50"	"'='"	"296.0"	"nM"	"6.53"	""	""	""	"16.26"	"0.30"	"2.29"	"7.90"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL4753549"	""	"0"	"459.60"	"0"	"3.98"	"13ac"	"Cc1cnc(Nc2ccc3c(c2)CCN(C(=O)/C=C/CN(C)C)C3)nc1-c1cnn(C(C)C)c1"	"IC50"	"'='"	"11.7"	"nM"	"7.93"	""	""	""	"17.26"	"0.32"	"3.95"	"10.02"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL4777006"	""	"0"	"461.61"	"0"	"4.20"	"13ad"	"Cc1cnc(Nc2ccc3c(c2)CCN(C(=O)CCCN(C)C)C3)nc1-c1cnn(C(C)C)c1"	"IC50"	"'='"	"985.0"	"nM"	"6.01"	""	""	""	"13.01"	"0.24"	"1.81"	"7.59"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL4757237"	""	"0"	"542.73"	"1"	"4.49"	"13af"	"Cc1cnc(Nc2ccc3c(c2)CCN(C/C=C/C(=O)NCCN2CCCCC2)C3)nc1-c1cnn(C(C)C)c1"	"IC50"	"'='"	"554.0"	"nM"	"6.26"	""	""	""	"11.53"	"0.21"	"1.77"	"6.86"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL3904533"	""	"0"	"387.47"	"0"	"0.60"	"BDBM159773"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)N2C[C@@H]3C[C@]3(C#N)C2)C1"	"IC50"	"'='"	"987.0"	"nM"	"6.01"	""	"302583"	"UO_0000065"	"15.50"	"0.30"	"5.41"	"5.09"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647911"	""	"0"	"401.90"	"0"	"3.78"	"BDBM148023"	"[C-]#[N+][C@H]1C[C@@H](C(C)(C)O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	"285959"	"UO_0000065"	"19.16"	"0.38"	"3.92"	"7.89"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3941571"	""	"0"	"483.59"	"0"	"3.27"	"16e"	"CS(=O)(=O)N1CCc2oc(-c3ccnc(Nc4ccc(OCCN5CCCC5)cc4)n3)cc2C1"	"IC50"	"'='"	"4311.0"	"nM"	"5.37"	""	""	"UO_0000065"	"11.09"	"0.22"	"2.10"	"5.32"	"False"	"CHEMBL3868066"	"Inhibition of JAK2 in human TF1 cells assessed as suppression of cell growth"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3867460"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2017"	"CHEMBL3307972"	""
"CHEMBL3966342"	""	"0"	"411.47"	"0"	"4.65"	"5f"	"Cc1cnc(Nc2ccc(N3CCOCC3)cc2)nc1-c1cc2cc(C#N)ccc2o1"	"IC50"	"'='"	"3088.0"	"nM"	"5.51"	""	""	"UO_0000065"	"13.39"	"0.24"	"0.86"	"6.32"	"False"	"CHEMBL3868067"	"Inhibition of JAK2 V617F mutant in human HEL cells after 1 hr"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3867460"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2017"	"CHEMBL3308090"	""
"CHEMBL3115319"	""	"0"	"369.83"	"0"	"2.60"	"1"	"O=C1NC(=S)N/C1=C1\C(=O)N(Cc2ccccc2Cl)c2ccccc21"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL3119788"	"Inhibition of JAK2 (unknown origin) by radioactive ATP method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112544"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2414552"	""	"0"	"342.45"	"1"	"5.57"	"22"	"Cc1cccc(Nc2nc3cccc(-c4cccc(C(C)C)c4)n3n2)c1"	"IC50"	"'='"	"2000.0"	"nM"	"5.70"	""	""	"UO_0000065"	"16.64"	"0.30"	"0.13"	"13.50"	"False"	"CHEMBL2415128"	"Inhibition of JAK2 in human SET2 cells assessed as reduction of phosphorylated STAT5 level"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2412966"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL3947205"	""	"0"	"569.98"	"1"	"4.12"	"342"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc(C(F)(F)F)ncc3Cl)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3976158"	""	"0"	"571.51"	"1"	"3.55"	"361"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN([C@@H]2CCN(C(=O)c3ccnc(C(F)(F)F)c3F)C[C@@H]2F)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3948879"	""	"0"	"554.53"	"1"	"3.60"	"363"	"[2H]C1(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CCN(C(=O)c2ccnc(C(F)(F)F)c2F)CC1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3979504"	""	"0"	"500.54"	"1"	"2.90"	"6"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(O)c(F)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3917339"	""	"0"	"502.53"	"1"	"3.33"	"42"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(F)cc3F)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3958836"	""	"0"	"530.63"	"1"	"3.91"	"62"	"CSc1ccc(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)cc1F"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3894266"	""	"0"	"603.11"	"1"	"3.84"	"107"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)C3CCN(c4ncc(Cl)cc4F)CC3)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3977214"	""	"0"	"549.47"	"1"	"4.29"	"112"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Cc3c(Cl)cccc3Cl)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3900135"	""	"0"	"600.66"	"1"	"4.50"	"135"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(-c4ccc5nccn5c4)c(F)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3935448"	""	"0"	"535.59"	"1"	"3.59"	"138"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CC3CCC(C2)N3C(=O)c2cc(F)cc(C#N)c2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3973035"	""	"0"	"522.60"	"1"	"3.95"	"151"	"CC1CC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CCN1C(=O)C1CCC(F)(F)CC1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3976504"	""	"0"	"498.57"	"0"	"3.58"	"152"	"CC1(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CCN(C(=O)c2cccc(F)c2)CC1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3980875"	""	"0"	"534.00"	"1"	"4.23"	"162"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3ccc(F)cc3Cl)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3935680"	""	"0"	"550.55"	"1"	"3.86"	"165; 291"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3cnccc3C(F)(F)F)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3901336"	""	"0"	"534.00"	"1"	"4.23"	"177"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3cccc(Cl)c3F)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3948999"	""	"0"	"511.59"	"1"	"3.45"	"180"	"COc1ccccc1NC(=O)N1CCC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3980116"	""	"0"	"599.12"	"2"	"5.22"	"195"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3nc(-c4ccc(Cl)cc4)cs3)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3982556"	""	"0"	"499.58"	"0"	"2.66"	"196"	"CCn1nccc1NC(=O)N1CCC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3953617"	""	"0"	"501.54"	"1"	"3.93"	"276"	"N#CCC1(n2ccc(-c3ncnc4[nH]ccc34)c2)CN(C2CCN(C(=O)c3cccc(F)c3F)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3904301"	""	"0"	"519.53"	"1"	"4.07"	"280"	"N#CCC1(n2ccc(-c3ncnc4[nH]ccc34)c2)CN(C2CCN(C(=O)c3ccc(F)c(F)c3F)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3961564"	""	"0"	"544.66"	"2"	"5.20"	"233"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(Cc3cccc(Oc4ccccc4)c3)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3895021"	""	"0"	"566.56"	"2"	"5.21"	"283"	"N#CCC1(n2ccc(-c3ncnc4[nH]ccc34)c2)CN(C2CCN(C(=O)Nc3ccc(F)cc3C(F)(F)F)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3935274"	""	"0"	"566.56"	"2"	"5.21"	"303"	"N#CCC1(n2cc(-c3ccnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3ccc(F)cc3C(F)(F)F)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3961498"	""	"0"	"540.03"	"1"	"4.57"	"313"	"N#CCC1(n2cc(-c3ccnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3ccc(C#N)cc3Cl)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3924659"	""	"0"	"517.54"	"1"	"3.64"	"322"	"N#CCC1(n2cc(-c3c(F)cnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(O)c(F)c3)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3930325"	""	"0"	"567.55"	"1"	"4.60"	"329"	"N#CCC1(n2cc(-c3c(F)cnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3ncccc3C(F)(F)F)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL2178805"	""	"0"	"381.83"	"0"	"2.93"	"7k"	"Cc1ccc(Cl)cc1-c1nn(C)cc1NC(=O)c1cnn2ccc(N)nc12"	"IC50"	"'='"	"9.8"	"nM"	"8.01"	""	""	"UO_0000065"	"20.97"	"0.41"	"5.08"	"7.77"	"False"	"CHEMBL2186603"	"Inhibition of JAK2 in human TF1 cells assessed as reduction in STAT5 phosphorylation incubated for 30 mins in presence of human recombinant EPO"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176876"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"CHEMBL3307972"	""
"CHEMBL2178254"	""	"0"	"367.80"	"0"	"2.62"	"7c"	"Cn1cc(NC(=O)c2cnn3ccc(N)nc23)c(-c2cccc(Cl)c2)n1"	"IC50"	"'='"	"30.4"	"nM"	"7.52"	""	""	"UO_0000065"	"20.44"	"0.39"	"4.90"	"7.29"	"False"	"CHEMBL2186598"	"Inhibition of JAK2 V617F mutant in human SET2 cells assessed as reduction in STAT5 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176876"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL3952364"	""	"0"	"553.62"	"2"	"5.10"	"43"	"O=C(NO)c1cccc(NCCOc2ccc3cc2COC/C=C/COCc2cccc(c2)-c2ccnc(n2)N3)c1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	""	"UO_0000065"	"14.53"	"0.27"	"2.95"	"6.34"	"False"	"CHEMBL3877344"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]ATP addition measured after 120 mins by Hotspot assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3877241"	"1"	"Scientific Literature"	"J Med Chem"	"2016"	"None"	""
"CHEMBL3951291"	""	"0"	"504.59"	"1"	"4.93"	"50"	"O=C(CCCCCOc1ccc2cc1COC/C=C/COCc1cccc(c1)-c1ccnc(n1)N2)NO"	"IC50"	"'='"	"4.3"	"nM"	"8.37"	""	""	"UO_0000065"	"16.58"	"0.31"	"3.44"	"7.29"	"False"	"CHEMBL3877344"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]ATP addition measured after 120 mins by Hotspot assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3877241"	"1"	"Scientific Literature"	"J Med Chem"	"2016"	"None"	""
"CHEMBL3898123"	""	"0"	"514.57"	"1"	"3.20"	"26"	"COc1cc(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)ccc1F"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3959899"	""	"0"	"514.57"	"1"	"3.20"	"27"	"COc1ccc(F)c(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)c1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3957208"	""	"0"	"518.98"	"1"	"3.84"	"28"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc(F)cc(Cl)c3)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3908773"	""	"0"	"654.37"	"1"	"4.58"	"50"	"COc1c(Br)cc(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)cc1Br"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3895594"	""	"0"	"581.58"	"1"	"3.67"	"60"	"CN(C)c1c(F)c(F)c(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)c(F)c1F"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3965032"	""	"0"	"575.07"	"2"	"5.06"	"91"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3sc4cc(F)ccc4c3Cl)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3974722"	""	"0"	"541.06"	"1"	"4.12"	"111"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)C3(c4ccc(Cl)cc4)CC3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3910532"	""	"0"	"561.63"	"1"	"4.25"	"123"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(-c4cccnc4)c(F)c3)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3979825"	""	"0"	"603.64"	"1"	"4.87"	"128"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(-c4cc(F)cc(C#N)c4)c(F)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3944093"	""	"0"	"496.58"	"0"	"3.15"	"198"	"Cc1ncccc1NC(=O)N1CCC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3941704"	""	"0"	"539.60"	"1"	"3.23"	"206"	"COC(=O)c1ccccc1NC(=O)N1CCC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3955753"	""	"0"	"521.46"	"1"	"4.72"	"210"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(Cc3cc(Cl)cc(Cl)c3)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3956061"	""	"0"	"549.56"	"1"	"4.38"	"282"	"N#CCC1(n2ccc(-c3ncnc4[nH]ccc34)c2)CN(C2CCN(C(=O)c3ccc(O)c(C(F)(F)F)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3934142"	""	"0"	"568.09"	"1"	"4.62"	"238"	"COc1cccc2nc(Cl)c(CN3CCC(N4CC(CC#N)(n5cc(-c6ncnc7[nH]ccc67)cn5)C4)CC3)cc12"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3976720"	""	"0"	"540.03"	"1"	"4.57"	"293"	"N#CCC1(n2ccc(-c3ncnc4[nH]ccc34)c2)CN(C2CCN(C(=O)Nc3ccc(Cl)cc3C#N)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3647924"	""	"0"	"457.43"	"0"	"2.24"	"BDBM148041"	"N#C[C@H]1C[C@H](O)CCC1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"31.0"	"nM"	"7.51"	""	"285982"	"UO_0000065"	"16.41"	"0.33"	"5.27"	"4.97"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3658864"	""	"0"	"373.48"	"0"	"2.28"	"BDBM159783"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](CS(=O)(=O)[C@H]2CC[C@H](C#N)C2)C1"	"IC50"	"'='"	"309.0"	"nM"	"6.51"	""	"302593"	"UO_0000065"	"17.43"	"0.34"	"4.23"	"6.34"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL2062799"	""	"0"	"394.46"	"0"	"3.55"	"BDBM99521"	"COc1ccc(Nc2nc3c(-c4ccc(S(C)(=O)=O)cc4)cccn3n2)cc1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"216213"	"UO_0000065"	"22.82"	"0.44"	"5.45"	"10.52"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3702941"	""	"0"	"350.38"	"0"	"1.82"	"BDBM147643"	"N#Cc1ccc(Nc2nn([C@H]3CC[C@@H](O)C[C@@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"285575"	"UO_0000065"	"24.32"	"0.45"	"6.70"	"6.06"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645101"	""	"0"	"376.42"	"0"	"3.50"	"BDBM99875"	"COc1cccc(CNc2cccn3nc(Nc4ccc(OC)nc4)nc23)c1"	"IC50"	"'='"	"9999.0"	"nM"	"5.00"	""	"216543"	"UO_0000065"	"13.28"	"0.24"	"1.50"	"5.84"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL4645113"	""	"0"	"217.27"	"0"	"2.30"	"14"	"O=c1cc(C2CCCCC2)c2c[nH]nc2[nH]1"	"IC50"	"'='"	"35000.0"	"nM"	"4.46"	""	""	"UO_0000065"	"20.51"	"0.38"	"2.16"	"7.24"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4639973"	""	"0"	"350.37"	"0"	"2.36"	"27"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](NC(=O)[C@@H]4CC4(F)F)CC3)c12"	"IC50"	"'='"	"120.0"	"nM"	"6.92"	""	""	"UO_0000065"	"19.75"	"0.38"	"4.56"	"7.64"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4643061"	""	"0"	"282.35"	"0"	"2.60"	"40"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3C[C@H]4C[C@@H]3C[C@@H]4CC#N)c12"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	""	"UO_0000065"	"28.05"	"0.52"	"5.32"	"9.28"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL3126348"	""	"0"	"423.26"	"0"	"4.91"	"28"	"O=c1[nH]ccc2c(Nc3c(Cl)cc(-c4ccn[nH]4)cc3Cl)nc3ccncc3c12"	"IC50"	"'='"	"37.0"	"nM"	"7.43"	""	""	"UO_0000065"	"17.56"	"0.35"	"2.52"	"7.48"	"False"	"CHEMBL3131375"	"Inhibition of Jak2 (unknown origin) assessed as inhibition of STAT5 phosphorylation by cell-based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3124786"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3343042"	""	"0"	"506.57"	"2"	"5.39"	"12a"	"COc1cc2c(Nc3ccc(NC(=O)c4ccccc4)cc3)nc(NCCc3ccccn3)nc2cc1O"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3380804"	"Inhibition of human JAK2 incubated for 20 mins prior to MgCl2 addition measured after 90 mins by mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351874"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL4758891"	""	"0"	"401.47"	"0"	"3.85"	"8"	"C=CC(=O)Nc1cccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)c1"	"IC50"	"'='"	"1796.0"	"nM"	"5.75"	""	""	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL4750671"	""	"0"	"391.48"	"0"	"3.16"	"19"	"C/C=C/C(=O)Nc1cccc(-c2cc(Nc3cnn(CCN(C)C)c3)ncn2)c1"	"IC50"	"'='"	"1886.0"	"nM"	"5.72"	""	""	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL4762354"	""	"0"	"390.41"	"0"	"1.59"	"23"	"Cn1cc(Nc2cc(-c3cccc(NC(=O)CNC(=O)CC#N)c3)ncn2)cn1"	"IC50"	"'='"	"69.0"	"nM"	"7.16"	""	""	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL4780644"	""	"0"	"471.52"	"0"	"2.69"	"28"	"N#CCC(=O)NCC(=O)Nc1cccc(-c2cc(Nc3ccc(N4CCOCC4)cc3)ncn2)c1"	"IC50"	"'='"	"309.0"	"nM"	"6.51"	""	""	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL4743357"	""	"0"	"415.50"	"0"	"4.24"	"30"	"C/C=C/C(=O)Nc1cccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)c1"	"IC50"	"'='"	"2788.0"	"nM"	"5.55"	""	""	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL4744519"	""	"0"	"377.41"	"0"	"2.58"	"37"	"COCCn1cc(Nc2nccc(-c3ccc(NC(=O)CC#N)cc3)n2)cn1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL4750568"	""	"0"	"480.62"	"1"	"5.68"	"(R )-1"	"N#CC[C@H](C1CCCC1)n1cc(-c2nc(Nc3ccc(C4CCNCC4)cc3)nc3[nH]ccc23)cn1"	"IC50"	"'='"	"0.15"	"nM"	"9.82"	""	""	""	"20.44"	"0.37"	"4.14"	"9.16"	"False"	"CHEMBL4714135"	"Inhibition of human JAK2 by radiometric assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEK293F"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706688"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	""
"CHEMBL2376142"	""	"0"	"392.42"	"0"	"0.94"	"4"	"CCn1cc(-c2cnc3[nH]cc(C(=O)N[C@H](C)C(=O)N4CC(C#N)C4)c3n2)cn1"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	""	"UO_0000065"	"19.74"	"0.36"	"6.80"	"5.84"	"False"	"CHEMBL2378515"	"Inhibition of JAK2 (unknown origin) using [33gammaP]ATP and Biotin-KAIETDKEYYTVKD as substrate incubated for 10 mins prior to substrate addition measured after 30 mins by filtration assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375236"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2376340"	""	"0"	"393.45"	"0"	"3.01"	"1k"	"CC(=O)N[C@@H]1CCc2ccc(Oc3cnc4[nH]cc(C(=O)NC(C)C)c4n3)cc21"	"IC50"	"'='"	"1010.0"	"nM"	"6.00"	""	""	"UO_0000065"	"15.24"	"0.28"	"2.99"	"5.50"	"False"	"CHEMBL2378977"	"Inhibition of JAK2 (unknown origin) expressed in SF21 cells using Biotin-KAIETDKEYYTVKD as substrate and [33Pgamma]ATP incubated for 10 mins prior to substrate addition measured after 30 mins by Topcount analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375291"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"CHEMBL4106362"	""
"CHEMBL2381987"	""	"0"	"429.48"	"0"	"2.85"	"16"	"Cc1cc(Nc2nc(N[C@@H](C)c3ccc(F)cn3)c(F)c(N3CCN(C)CC3)n2)n[nH]1"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	""	"UO_0000065"	"18.09"	"0.34"	"4.92"	"7.94"	"False"	"CHEMBL2383938"	"Inhibition of JAK2 (unknown origin) using biotinylated TYK2 peptide as substrate after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2380256"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2381983"	""	"0"	"434.43"	"0"	"3.07"	"9"	"Cc1cc(Nc2nc(N[C@@H](C)c3ncc(F)cc3F)c(F)c(N3CCOCC3)n2)n[nH]1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"19.62"	"0.38"	"5.45"	"8.20"	"False"	"CHEMBL2383938"	"Inhibition of JAK2 (unknown origin) using biotinylated TYK2 peptide as substrate after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2380256"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2381980"	""	"0"	"418.41"	"0"	"2.30"	"6"	"Cc1cc(Nc2nc(O[C@@H](C)c3ncc(F)cn3)c(F)c(N3CCOCC3)n2)n[nH]1"	"IC50"	"'<'"	"3.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2383938"	"Inhibition of JAK2 (unknown origin) using biotinylated TYK2 peptide as substrate after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2380256"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2381979"	""	"0"	"417.42"	"0"	"2.33"	"5"	"Cc1cc(Nc2nc(N[C@@H](C)c3ncc(F)cn3)c(F)c(N3CCOCC3)n2)n[nH]1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"20.42"	"0.39"	"6.19"	"7.30"	"False"	"CHEMBL2383938"	"Inhibition of JAK2 (unknown origin) using biotinylated TYK2 peptide as substrate after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2380256"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL1080151"	""	"0"	"434.48"	"0"	"3.06"	"2"	"Cc1cnc(Nc2nc(N[C@@H](C)c3ncc(F)cn3)nc(N3CCOCC3)c2F)s1"	"IC50"	"'='"	"25.0"	"nM"	"7.60"	""	""	"UO_0000065"	"17.50"	"0.35"	"4.54"	"7.53"	"False"	"CHEMBL2383938"	"Inhibition of JAK2 (unknown origin) using biotinylated TYK2 peptide as substrate after 60 mins"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2380256"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL4085457"	"PF-06651600"	"3"	"285.35"	"0"	"1.94"	"7"	"C=CC(=O)N1C[C@H](Nc2ncnc3[nH]ccc23)CC[C@@H]1C"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	""	""	""	""	""	"False"	"CHEMBL4714260"	"Inhibition of recombinant human JAK2 assessed as phosphorylation level in presence of 1 mM ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706695"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2021"	"None"	""
"CHEMBL3234880"	""	"0"	"345.37"	"0"	"4.24"	"17"	"Cc1cccc(Nc2sc(-c3ccc(F)cc3F)cc2C(N)=O)n1"	"IC50"	"'='"	"178.0"	"nM"	"6.75"	""	""	"UO_0000065"	"19.54"	"0.38"	"2.51"	"9.92"	"False"	"CHEMBL3239499"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3232939"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3116063"	""	"0"	"399.82"	"0"	"3.26"	"13f, enantiomeric mixture"	"CC(Nc1nc(Nc2cn(C)cn2)c2ccc(Cl)nc2n1)c1ncc(F)cn1"	"IC50"	"'<'"	"3.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3118240"	"Inhibition of Jak2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112447"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL4647223"	""	"0"	"401.45"	"0"	"0.90"	"12"	"C[C@@H]1[C@@H]2CN(c3nc(Nc4cnn(CCO)c4)ncc3F)C[C@]12NC(=O)C1CC1"	"IC50"	"'='"	"1617.0"	"nM"	"5.79"	""	""	"UO_0000065"	"14.43"	"0.27"	"4.89"	"5.35"	"False"	"CHEMBL4620433"	"Inhibition of human recombinant JAK2 assessed as level of phosphorylation in presence of peptide substrate FITC-KGGEEEEYFELVKK and ATP by mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4619733"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2020"	"None"	""
"CHEMBL3116053"	""	"0"	"354.35"	"0"	"1.93"	"19d, enantiomeric mixture"	"CC(Nc1nc(Nc2cn(C)cn2)c2cn[nH]c2n1)c1ncc(F)cn1"	"IC50"	"'='"	"50.0"	"nM"	"7.30"	""	""	"UO_0000065"	"20.60"	"0.38"	"5.37"	"5.98"	"False"	"CHEMBL3118240"	"Inhibition of Jak2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112447"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL388978"	"STAUROSPORINE"	"0"	"466.54"	"0"	"4.35"	"Staurosporine"	"CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4c(c5c6ccccc6n2c5c31)C(=O)NC4"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	""	"UO_0000065"	"18.65"	"0.34"	"4.35"	"12.53"	"True"	"CHEMBL3118637"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112393"	"1"	"Scientific Literature"	"Eur. J. Med. Chem."	"2014"	"None"	""
"CHEMBL3215571"	""	"0"	"599.36"	"1"	"3.22"	"28"	"COCCN1CCN(CCO/N=C2C(=C3/C(=O)Nc4cc(Br)ccc43)/Nc3ccccc3/2)CC1.Cl.Cl"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4042012"	"Inhibition of recombinant JAK2 (unknown origin) after 120 mins in presence of [33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4041496"	"1"	"Scientific Literature"	"J Nat Prod"	"2016"	"None"	""
"CHEMBL4645110"	""	"0"	"431.50"	"0"	"3.21"	"27"	"N#C[C@]1(C2CC2)C(=O)N2C[C@H]1COC/C=C/COCc1cccc(n1)Nc1cc2ccn1"	"IC50"	"'='"	"140.0"	"nM"	"6.85"	""	""	"UO_0000065"	"15.88"	"0.29"	"3.64"	"6.83"	"False"	"CHEMBL4627620"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4627255"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL4643899"	""	"0"	"431.50"	"0"	"3.21"	"28"	"N#C[C@]1(C2CC2)C(=O)N2C[C@H]1COC/C=C\COCc1cccc(n1)Nc1cc2ccn1"	"IC50"	"'='"	"130.0"	"nM"	"6.89"	""	""	"UO_0000065"	"15.96"	"0.29"	"3.68"	"6.86"	"False"	"CHEMBL4627620"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4627255"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL4644578"	""	"0"	"426.46"	"0"	"0.65"	"15"	"C[C@@H]1[C@@H]2CN(c3nc(Nc4cnn(CCO)c4)ncc3F)C[C@]12NC(=O)[C@@H]1C[C@H]1C#N"	"IC50"	"'='"	"128.0"	"nM"	"6.89"	""	""	"UO_0000065"	"16.16"	"0.30"	"6.24"	"5.22"	"False"	"CHEMBL4620433"	"Inhibition of human recombinant JAK2 assessed as level of phosphorylation in presence of peptide substrate FITC-KGGEEEEYFELVKK and ATP by mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4619733"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2020"	"None"	""
"CHEMBL3651064"	""	"0"	"360.38"	"0"	"3.50"	"BDBM47236"	"C=C(C)C(=O)Nc1cccc(-c2ncnc3[nH]cc(-c4nnc(C)o4)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"198771"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3658862"	""	"0"	"348.47"	"0"	"2.39"	"BDBM159781"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](CS(=O)(=O)CCC2CC2)C1"	"IC50"	"'='"	"426.0"	"nM"	"6.37"	""	"302591"	"UO_0000065"	"18.28"	"0.36"	"3.98"	"8.07"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642354"	""	"0"	"507.62"	"1"	"2.76"	"BDBM99630"	"CN1CCN(c2ccc(Nc3nc4c(Nc5cccnc5N(C)S(C)(=O)=O)cccn4n3)cc2)CC1"	"IC50"	"'='"	"11.41"	"nM"	"7.94"	""	"216320"	"UO_0000065"	"15.65"	"0.30"	"5.18"	"7.16"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703501"	""	"0"	"283.29"	"0"	"2.51"	"BDBM153145"	"CCOC(=O)c1c[nH]c2ncnc(-c3cccc(O)c3)c12"	"IC50"	"'='"	"127.0"	"nM"	"6.90"	""	"294093"	"UO_0000065"	"24.34"	"0.45"	"4.39"	"7.83"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3648435"	""	"0"	"279.30"	"0"	"2.23"	"BDBM107144"	"O=C(CO)Nc1cccc(-c2cnc3ccccc3n2)c1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	"226382"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707587"	"In Vitro Kinase Enzyme Assay: In vitro kinase enzyme assay using Jak3, Jak2, Jak1, and Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638666"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3658100"	""	"0"	"622.72"	"2"	"6.90"	"BDBM148381"	"Cc1ccc(NC(=O)c2ccc(C(F)(F)F)s2)cc1N1CCc2nc(Nc3ccc(OCCN4CCCC4)cc3)ncc2C1"	"IC50"	"'='"	"18.0"	"nM"	"7.75"	""	"286786"	"UO_0000065"	"12.44"	"0.24"	"0.84"	"9.37"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3890701"	""	"0"	"353.39"	"0"	"2.28"	"BDBM228671"	"Cc1cc(N(C)[C@@H]2CCN(c3ncnc4[nH]ccc34)C2)ncc1[N+](=O)[O-]"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399715"	"UO_0000065"	"26.20"	"0.49"	"6.98"	"8.90"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3906422"	""	"0"	"339.40"	"0"	"1.86"	"BDBM228790"	"CCOc1cnc(N(C)[C@@H]2CCN(c3ncnc4[nH]ccc34)C2)cn1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399728"	"UO_0000065"	"27.28"	"0.51"	"7.40"	"11.15"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3973893"	""	"0"	"376.49"	"0"	"3.80"	"BDBM228791"	"CN(c1ccc(-c2cccs2)cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399729"	"UO_0000065"	"24.59"	"0.47"	"5.46"	"15.19"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3703498"	""	"0"	"285.28"	"0"	"2.94"	"BDBM153142"	"CCOC(=O)c1c[nH]c2ncnc(-c3ccccc3F)c12"	"IC50"	"'='"	"168.0"	"nM"	"6.78"	""	"294090"	"UO_0000065"	"23.75"	"0.44"	"3.83"	"9.98"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652375"	""	"0"	"467.64"	"0"	"3.85"	"BDBM113186"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC[C@H](Cc3ccccc3)C2)CC1"	"IC50"	"'='"	"65.4"	"nM"	"7.18"	""	"234629"	"UO_0000065"	"15.36"	"0.30"	"3.33"	"8.74"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3920581"	""	"0"	"294.36"	"0"	"2.07"	"BDBM228740"	"CN(c1ccccn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399669"	"UO_0000065"	"34.85"	"0.64"	"8.19"	"16.84"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3945908"	""	"0"	"379.40"	"0"	"1.99"	"BDBM228686"	"CN(c1ccc(-c2nnn[nH]2)cc1F)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399672"	"UO_0000065"	"27.04"	"0.50"	"8.27"	"10.01"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3914972"	""	"0"	"457.54"	"0"	"2.53"	"BDBM228749"	"CN(c1ccc(C(=O)N[C@@H](CO)c2ccccc2)cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399679"	"UO_0000065"	"22.42"	"0.41"	"7.73"	"9.30"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3939312"	""	"0"	"486.55"	"0"	"3.20"	"BDBM228752"	"CN(c1ccc(C(=O)NC2c3ccccc3CC2O)cc1F)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399682"	"UO_0000065"	"21.09"	"0.39"	"7.06"	"10.54"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3126340"	""	"0"	"342.28"	"0"	"3.63"	"15"	"O=c1[nH]ccc2c(Nc3c(F)cc(F)cc3F)nc3ccncc3c12"	"IC50"	"'='"	"90.0"	"nM"	"7.05"	""	""	"UO_0000065"	"20.58"	"0.38"	"3.42"	"9.97"	"False"	"CHEMBL3131375"	"Inhibition of Jak2 (unknown origin) assessed as inhibition of STAT5 phosphorylation by cell-based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3124786"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL4636957"	""	"0"	"365.40"	"0"	"1.40"	"J-8"	"N#CCNC(=O)N1CC=C(c2cccc3nc(NC(=O)C4CC4)nn23)CC1"	"IC50"	"'='"	"175.0"	"nM"	"6.76"	""	""	"UO_0000065"	"18.49"	"0.34"	"5.36"	"5.85"	"False"	"CHEMBL4624516"	"Inhibition of JAK2 (unknown origin) in presence of ATP at Km concentration by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4622902"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL2035187"	"PACRITINIB"	"3"	"472.59"	"0"	"4.96"	"21c, SB1518, 85:15 trans/cis mixture"	"C1=C/COCc2cc(ccc2OCCN2CCCC2)Nc2nccc(n2)-c2cccc(c2)COC/1"	"IC50"	"'='"	"19.0"	"nM"	"7.72"	""	""	"UO_0000065"	"16.34"	"0.30"	"2.76"	"11.23"	"False"	"CHEMBL2183761"	"Inhibition of JAK2 V617F mutant expressed in mouse Ba/f3 cells"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176955"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"CHEMBL3307634"	""
"CHEMBL1933582"	""	"0"	"501.51"	"1"	"3.16"	"25"	"CN1CCN(c2ccc(OC(F)(F)F)c(Nc3nccc(-c4cc5c(n4C)CCNC5=O)n3)c2)CC1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1936520"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1933058"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL4634979"	""	"0"	"638.74"	"1"	"4.58"	"Quinoxaline 2"	"COc1cc(-c2cnc3cccc(-c4cc(F)c(CN5CCS(=O)(=O)CC5)c(F)c4)c3n2)ccc1OCCCN1CCOCC1"	"IC50"	"'='"	"0.2512"	"nM"	"9.60"	""	""	"UO_0000065"	"15.03"	"0.29"	"5.02"	"10.20"	"False"	"CHEMBL4627716"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4627263"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2020"	"None"	""
"CHEMBL3234874"	""	"0"	"412.49"	"0"	"3.62"	"23"	"NC(=O)c1cc(-c2ccccc2F)sc1Nc1cccc(CN2CCOCC2)n1"	"IC50"	"'='"	"34.0"	"nM"	"7.47"	""	""	"UO_0000065"	"18.11"	"0.35"	"3.85"	"9.28"	"False"	"CHEMBL3239499"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3232939"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3234895"	""	"0"	"491.56"	"0"	"4.45"	"25"	"CC(C)(O)COCc1cccc(Nc2sc(-c3c(F)cc(C(C)(C)O)cc3F)cc2C(N)=O)n1"	"IC50"	"'='"	"7.5"	"nM"	"8.12"	""	""	"UO_0000065"	"16.53"	"0.33"	"3.67"	"6.90"	"False"	"CHEMBL3239499"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3232939"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL4636334"	""	"0"	"337.38"	"0"	"1.88"	"J-11"	"C=CC(=O)N1CC=C(c2cccc3nc(NC(=O)C4CC4)nn23)CC1"	"IC50"	"'='"	"424.0"	"nM"	"6.37"	""	""	"UO_0000065"	"18.89"	"0.35"	"4.49"	"8.01"	"False"	"CHEMBL4624516"	"Inhibition of JAK2 (unknown origin) in presence of ATP at Km concentration by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4622902"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL2322137"	""	"0"	"241.29"	"0"	"3.75"	"8"	"c1cc2c(ncc3onc(C4CCCCC4)c32)[nH]1"	"IC50"	"'='"	"30.0"	"nM"	"7.52"	""	""	"UO_0000065"	"31.18"	"0.57"	"3.77"	"13.75"	"False"	"CHEMBL2327345"	"Inhibition of JAK2 (unknown origin) after 2.5 hrs by time-resolved fluorescence resonance energy transfer assay in presence of 1 uM ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321825"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2414541"	""	"0"	"402.46"	"0"	"4.54"	"37"	"O=C(O)c1ccc(Nc2nc3c(-c4cnn(C5CCCCC5)c4)cccn3n2)cc1"	"IC50"	"'='"	"31.0"	"nM"	"7.51"	""	""	"UO_0000065"	"18.66"	"0.34"	"2.97"	"7.71"	"False"	"CHEMBL2415128"	"Inhibition of JAK2 in human SET2 cells assessed as reduction of phosphorylated STAT5 level"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2412966"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2376144"	""	"0"	"462.90"	"0"	"2.27"	"6a"	"C[C@@H](NC(=O)c1c[nH]c2ncc(-c3nn(C)c4cc(Cl)ccc34)nc12)C(=O)N1CC(C#N)C1"	"IC50"	"'='"	"22.0"	"nM"	"7.66"	""	""	"UO_0000065"	"16.54"	"0.32"	"5.39"	"5.78"	"False"	"CHEMBL2378515"	"Inhibition of JAK2 (unknown origin) using [33gammaP]ATP and Biotin-KAIETDKEYYTVKD as substrate incubated for 10 mins prior to substrate addition measured after 30 mins by filtration assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375236"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2376040"	""	"0"	"464.48"	"0"	"1.75"	"3"	"COc1cc(-c2cnc3[nH]cc(C(=O)N[C@H](C)C(=O)N4CC(C#N)C4)c3n2)cc(OC)c1OC"	"IC50"	"'='"	"200.0"	"nM"	"6.70"	""	""	"UO_0000065"	"14.42"	"0.27"	"4.95"	"4.70"	"False"	"CHEMBL2378509"	"Inhibition of JAK2 in human monocytes expressing CD14 assessed as inhibition of GM-CSF-stimulated STAT5a phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375236"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"20"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"2.7"	"nM"	"8.57"	""	""	"UO_0000065"	"27.43"	"0.51"	"7.03"	"9.64"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4640029"	""	"0"	"284.36"	"0"	"3.14"	"22"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](CCC#N)CC3)c12"	"IC50"	"'='"	"160.0"	"nM"	"6.80"	""	""	"UO_0000065"	"23.90"	"0.44"	"3.66"	"7.96"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4637596"	""	"0"	"256.31"	"0"	"2.36"	"23"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](C#N)CC3)c12"	"IC50"	"'='"	"5100.0"	"nM"	"5.29"	""	""	"UO_0000065"	"20.65"	"0.38"	"2.93"	"6.20"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4647115"	""	"0"	"282.35"	"0"	"2.60"	"39"	"Cc1[nH]nc2[nH]c(=O)cc([C@@H]3C[C@@H]4C[C@H]3C[C@H]4CC#N)c12"	"IC50"	"'='"	"93.0"	"nM"	"7.03"	""	""	"UO_0000065"	"24.90"	"0.46"	"4.43"	"8.24"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL3417191"	""	"0"	"473.58"	"0"	"4.45"	"36"	"O=C(CCCCN1C/C=C/COCc2cccc(c2)-c2ccnc(n2)Nc2cccc(c2)C1)NO"	"IC50"	"'='"	"392.0"	"nM"	"6.41"	""	""	"UO_0000065"	"13.53"	"0.25"	"1.96"	"6.43"	"False"	"CHEMBL3419812"	"Inhibition of human recombinant JAK2 using Z'LYTETry6 peptide substrate after 1 hr by microplate reader"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3414525"	"1"	"Scientific Literature"	"Eur. J. Med. Chem."	"2015"	"None"	""
"CHEMBL3986824"	"LANRAPLENIB"	"2"	"443.52"	"0"	"2.03"	"39; GS-9876"	"Nc1cncc(-c2cn3ccnc3c(Nc3ccc(N4CCN(C5COC5)CC4)cc3)n2)n1"	"IC50"	"'='"	"120.0"	"nM"	"6.92"	""	""	"UO_0000065"	"15.60"	"0.29"	"4.89"	"6.31"	"False"	"CHEMBL4605710"	"Inhibition of wild-type human partial length JAK2 JH1 catalytic domain (A829 to G1132 residues) expressed in mammalian expression system by Kinomescan method"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4602710"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2020"	"None"	""
"CHEMBL4636995"	""	"0"	"466.57"	"0"	"3.59"	"4"	"COc1ccc(-c2cnn3c(N)c(-c4nccs4)c(OC4CCN(C)CC4)nc23)cc1OC"	"IC50"	"'='"	"3800.0"	"nM"	"5.42"	""	""	"UO_0000065"	"11.62"	"0.22"	"1.83"	"5.42"	"False"	"CHEMBL4605806"	"Inhibition of JAK2 (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction in cell viability incubated for 48 hrs by brightglo-luciferase reporter gene assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4602715"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2020"	"CHEMBL3307634"	""
"CHEMBL2207767"	""	"0"	"423.48"	"1"	"5.10"	"6b"	"CC(=O)Nc1ccc(-c2ccnc(Nc3cccc(NC(=O)c4ccccc4)c3)n2)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL2214784"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT3 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL2207764"	""	"0"	"492.37"	"1"	"6.40"	"5"	"CC(=O)Nc1ccc(-c2ccnc(Nc3cccc(NC(=O)c4c(Cl)cccc4Cl)c3)n2)cc1"	"IC50"	"'='"	"763.0"	"nM"	"6.12"	""	""	"UO_0000065"	"12.42"	"0.25"	"-0.28"	"6.37"	"False"	"CHEMBL2214785"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT1 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL2207760"	""	"0"	"472.59"	"0"	"4.15"	"10h"	"CCN1CCC[C@@H]1C(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"9.1"	"nM"	"8.04"	""	""	"UO_0000065"	"17.01"	"0.31"	"3.89"	"9.73"	"False"	"CHEMBL2214787"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL2207766"	""	"0"	"457.92"	"1"	"5.75"	"6a"	"CC(=O)Nc1ccc(-c2ccnc(Nc3cccc(NC(=O)c4ccccc4Cl)c3)n2)cc1"	"IC50"	"'='"	"6.9"	"nM"	"8.16"	""	""	"UO_0000065"	"17.82"	"0.34"	"2.41"	"8.50"	"False"	"CHEMBL2214787"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"None"	""
"CHEMBL4640335"	""	"0"	"217.27"	"0"	"2.22"	"8"	"Cc1[nH]nc2[nH]c(=O)cc(C3CCCC3)c12"	"IC50"	"'>'"	"40000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL4637596"	""	"0"	"256.31"	"0"	"2.36"	"23"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](C#N)CC3)c12"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL4633028"	""	"0"	"314.39"	"0"	"2.11"	"24"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](NC(=O)C4CC4)CC3)c12"	"IC50"	"'>'"	"14000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL4638953"	""	"0"	"350.37"	"0"	"2.36"	"28"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](NC(=O)[C@H]4CC4(F)F)CC3)c12"	"IC50"	"'>'"	"40000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL4638030"	""	"0"	"367.45"	"0"	"2.60"	"35"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](CC(=O)N4CCC(C#N)C4)CC3)c12"	"IC50"	"'>'"	"45000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL4649484"	""	"0"	"418.54"	"0"	"3.92"	"36"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](CC(=O)N4CC(Cc5ccccc5)C4)CC3)c12"	"IC50"	"'='"	"5100.0"	"nM"	"5.29"	""	""	"UO_0000065"	"12.64"	"0.23"	"1.37"	"6.47"	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL2031893"	""	"0"	"528.54"	"2"	"5.23"	"1"	"COc1cc2nccc(Oc3ccc(NC(=O)c4c(C)n(C)n(-c5ccccc5)c4=O)cc3F)c2cc1OC"	"IC50"	"'='"	"1000.0"	"nM"	"6.00"	""	""	"UO_0000065"	"11.35"	"0.21"	"0.77"	"6.21"	"False"	"CHEMBL2032473"	"Inhibition of JAK2"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2029218"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2035187"	"PACRITINIB"	"3"	"472.59"	"0"	"4.96"	"21c, SB1518, 85:15 trans/cis mixture"	"C1=C/COCc2cc(ccc2OCCN2CCCC2)Nc2nccc(n2)-c2cccc(c2)COC/1"	"IC50"	"'='"	"23.0"	"nM"	"7.64"	""	""	"UO_0000065"	"16.16"	"0.30"	"2.68"	"11.11"	"False"	"CHEMBL2184201"	"Inhibition of recombinant JAK2 using Poly (Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176955"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL2376157"	""	"0"	"432.42"	"0"	"1.51"	"8"	"C[C@@H](NC(=O)c1c[nH]c2ncc(-c3ncn4cc(F)ccc34)nc12)C(=O)N1CC(C#N)C1"	"IC50"	"'='"	"4230.0"	"nM"	"5.37"	""	""	"UO_0000065"	"12.43"	"0.23"	"3.86"	"4.07"	"False"	"CHEMBL2378509"	"Inhibition of JAK2 in human monocytes expressing CD14 assessed as inhibition of GM-CSF-stimulated STAT5a phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375236"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2376144"	""	"0"	"462.90"	"0"	"2.27"	"6a"	"C[C@@H](NC(=O)c1c[nH]c2ncc(-c3nn(C)c4cc(Cl)ccc34)nc12)C(=O)N1CC(C#N)C1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2378509"	"Inhibition of JAK2 in human monocytes expressing CD14 assessed as inhibition of GM-CSF-stimulated STAT5a phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375236"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"1a"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"184.0"	"nM"	"6.74"	""	""	"UO_0000065"	"21.56"	"0.40"	"5.20"	"7.58"	"False"	"CHEMBL2378509"	"Inhibition of JAK2 in human monocytes expressing CD14 assessed as inhibition of GM-CSF-stimulated STAT5a phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375236"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2376440"	""	"0"	"529.60"	"1"	"3.00"	"12e"	"CC(=O)N[C@@H]1CCc2ccc(Oc3cnc4[nH]cc(C(=O)N[C@@H](C(=O)N5CC(C#N)C5)C(C)(C)C)c4n3)cc21"	"IC50"	"'='"	"446.0"	"nM"	"6.35"	""	""	"UO_0000065"	"11.99"	"0.22"	"3.35"	"4.15"	"False"	"CHEMBL2378977"	"Inhibition of JAK2 (unknown origin) expressed in SF21 cells using Biotin-KAIETDKEYYTVKD as substrate and [33Pgamma]ATP incubated for 10 mins prior to substrate addition measured after 30 mins by Topcount analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375291"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"CHEMBL4106362"	""
"CHEMBL2376339"	""	"0"	"393.45"	"0"	"3.01"	"1j"	"CC(=O)N[C@H]1CCc2ccc(Oc3cnc4[nH]cc(C(=O)NC(C)C)c4n3)cc21"	"IC50"	"'='"	"1710.0"	"nM"	"5.77"	""	""	"UO_0000065"	"14.66"	"0.27"	"2.76"	"5.29"	"False"	"CHEMBL2378977"	"Inhibition of JAK2 (unknown origin) expressed in SF21 cells using Biotin-KAIETDKEYYTVKD as substrate and [33Pgamma]ATP incubated for 10 mins prior to substrate addition measured after 30 mins by Topcount analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375291"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"CHEMBL4106362"	""
"CHEMBL2376335"	""	"0"	"321.34"	"0"	"2.76"	"1f"	"CC(C)NC(=O)c1c[nH]c2ncc(Oc3ccc(C#N)cc3)nc12"	"IC50"	"'='"	"900.0"	"nM"	"6.05"	""	""	"UO_0000065"	"18.81"	"0.34"	"3.29"	"5.83"	"False"	"CHEMBL2378977"	"Inhibition of JAK2 (unknown origin) expressed in SF21 cells using Biotin-KAIETDKEYYTVKD as substrate and [33Pgamma]ATP incubated for 10 mins prior to substrate addition measured after 30 mins by Topcount analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375291"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"CHEMBL4106362"	""
"CHEMBL1077458"	""	"0"	"389.46"	"0"	"3.68"	"7c"	"CC(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"795.0"	"nM"	"6.10"	""	""	"UO_0000065"	"15.66"	"0.29"	"2.42"	"7.68"	"False"	"CHEMBL2214784"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT3 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL2208025"	""	"0"	"389.46"	"0"	"3.68"	"7b"	"CC(=O)Nc1ccc(-c2ccnc(Nc3cccc(N4CCOCC4)c3)n2)cc1"	"IC50"	"'='"	"591.0"	"nM"	"6.23"	""	""	"UO_0000065"	"15.99"	"0.29"	"2.55"	"7.85"	"False"	"CHEMBL2214784"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT3 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL2207765"	""	"0"	"493.35"	"1"	"5.80"	"6"	"CC(=O)Nc1ccc(-c2ccnc(Nc3cccc(NC(=O)c4c(Cl)cccc4Cl)n3)n2)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL2214784"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT3 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL3301625"	"SPEBRUTINIB"	"2"	"423.45"	"0"	"4.25"	"CC292"	"C=CC(=O)Nc1cccc(Nc2nc(Nc3ccc(OCCOC)cc3)ncc2F)c1"	"IC50"	"'='"	"533.7"	"nM"	"6.27"	""	""	"UO_0000065"	"14.81"	"0.28"	"2.02"	"6.44"	"False"	"CHEMBL4610789"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using Ulight-Poly GT as substrate incubated for 2 hrs by Lanthascreen TR-FRET assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610007"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2020"	"None"	""
"CHEMBL4645290"	""	"0"	"483.26"	"None"	"None"	"14j"	"C=CC(=O)Nc1cccc(Nc2nc(Nc3ccc4c(c3)B(O)OC4(C)C)ncc2C(F)(F)F)c1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4610789"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using Ulight-Poly GT as substrate incubated for 2 hrs by Lanthascreen TR-FRET assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610007"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2020"	"None"	""
"CHEMBL3593578"	""	"0"	"270.34"	"0"	"2.79"	"6d"	"O=c1[nH]c2cnc3[nH]ccc3c2n1CC1CCCCC1"	"IC50"	"'='"	"88.0"	"nM"	"7.06"	""	""	"UO_0000065"	"26.10"	"0.48"	"4.27"	"10.61"	"False"	"CHEMBL3594576"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate and ATP incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593193"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3343048"	""	"0"	"420.42"	"0"	"3.66"	"17a"	"COc1cc(C(=O)Nc2ccc(NC(=O)c3ccccc3)cc2)ccc1OCC(=O)O"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3380804"	"Inhibition of human JAK2 incubated for 20 mins prior to MgCl2 addition measured after 90 mins by mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351874"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3622821"	"UPADACITINIB"	"4"	"380.37"	"0"	"2.91"	"11"	"CC[C@@H]1CN(C(=O)NCC(F)(F)F)C[C@@H]1c1cnc2cnc3[nH]ccc3n12"	"IC50"	"'='"	"120.0"	"nM"	"6.92"	""	""	"UO_0000065"	"18.19"	"0.35"	"4.01"	"8.84"	"True"	"CHEMBL4309409"	"Inhibition of recombinant JAK2 (unknown origin) by alpha-screen assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4308837"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3582427"	""	"0"	"325.38"	"0"	"3.88"	"1"	"N#Cc1ccc(-c2cnc3ccc(NCc4ccccc4)nn23)cc1"	"IC50"	"'='"	"4700.0"	"nM"	"5.33"	""	""	"UO_0000065"	"16.37"	"0.29"	"1.45"	"8.07"	"False"	"CHEMBL3583131"	"Inhibition of Tel-fused JAK2 (unknown origin) expressed in mouse BA/F3 cells after 48 hrs by luciferase reporter gene assay in absence of recombinant mouse IL3"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3580662"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"CHEMBL3307634"	""
"CHEMBL4563723"	""	"0"	"453.87"	"0"	"4.12"	"8y"	"O=C(NO)c1ccc(Cn2cc(Nc3ncc(Cl)c(Nc4ccc(F)cc4)n3)cn2)cc1"	"IC50"	"'='"	"21.0"	"nM"	"7.68"	""	""	"UO_0000065"	"16.92"	"0.33"	"3.56"	"6.56"	"False"	"CHEMBL4347596"	"Inhibition of recombinant human JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate measured after 60 mins by LANCE assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4346670"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL3314276"	""	"0"	"355.37"	"0"	"4.22"	"20"	"C#Cc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3cc[nH]c(=O)c3)[nH]2)cc1"	"IC50"	"'='"	"14300.0"	"nM"	"4.84"	""	""	"UO_0000065"	"13.63"	"0.25"	"0.62"	"7.87"	"False"	"CHEMBL3363474"	"Inhibition of JAK2 (unknown origin) by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352554"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3343045"	""	"0"	"378.34"	"0"	"3.20"	"14b"	"O=C(Nc1ccc(NC(=O)c2ccccn2)cc1)c1ccc(O)c([N+](=O)[O-])c1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3380804"	"Inhibition of human JAK2 incubated for 20 mins prior to MgCl2 addition measured after 90 mins by mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351874"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3343057"	""	"0"	"463.49"	"0"	"2.07"	"27"	"COc1cc(C(=O)Nc2ccc(NC(=O)C3CCCCN3)cc2)cc(-c2c[nH]c(=O)[nH]c2=O)c1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3380804"	"Inhibition of human JAK2 incubated for 20 mins prior to MgCl2 addition measured after 90 mins by mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351874"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3582442"	""	"0"	"458.54"	"0"	"4.23"	"17"	"OC1CCN(c2cc(-c3cnc4ccc(N5CCC[C@@H]5c5cccc(F)c5)nn34)ccn2)CC1"	"IC50"	"'='"	"5600.0"	"nM"	"5.25"	""	""	"UO_0000065"	"11.45"	"0.21"	"1.02"	"7.53"	"False"	"CHEMBL3583131"	"Inhibition of Tel-fused JAK2 (unknown origin) expressed in mouse BA/F3 cells after 48 hrs by luciferase reporter gene assay in absence of recombinant mouse IL3"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3580662"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"CHEMBL3307634"	""
"CHEMBL3582439"	""	"0"	"359.41"	"0"	"4.27"	"14"	"Fc1cccc([C@H]2CCCN2c2ccc3ncc(-c4ccccn4)n3n2)c1"	"IC50"	"'='"	"6700.0"	"nM"	"5.17"	""	""	"UO_0000065"	"14.40"	"0.26"	"0.90"	"11.17"	"False"	"CHEMBL3583131"	"Inhibition of Tel-fused JAK2 (unknown origin) expressed in mouse BA/F3 cells after 48 hrs by luciferase reporter gene assay in absence of recombinant mouse IL3"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"BaF3"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3580662"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"CHEMBL3307634"	""
"CHEMBL3343046"	""	"0"	"362.39"	"0"	"3.91"	"16a"	"COc1cc(C(=O)Nc2ccc(NC(=O)c3ccccc3)cc2)ccc1O"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3380804"	"Inhibition of human JAK2 incubated for 20 mins prior to MgCl2 addition measured after 90 mins by mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351874"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3343052"	""	"0"	"457.45"	"0"	"2.64"	"24c"	"COc1ccc(C(=O)Nc2ccc(NC(=O)c3ccccn3)cc2)cc1-c1c[nH]c(=O)[nH]c1=O"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3380804"	"Inhibition of human JAK2 incubated for 20 mins prior to MgCl2 addition measured after 90 mins by mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351874"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3665163"	""	"0"	"415.52"	"0"	"2.28"	"BDBM112556"	"CC(C)CS(=O)(=O)N1CCC[C@H](Nc2ncccc2-c2cnc3nc[nH]c3n2)C1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"233794"	"UO_0000065"	"20.51"	"0.40"	"6.24"	"7.30"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3699475"	""	"0"	"325.37"	"0"	"1.95"	"BDBM147490"	"N#C[C@H]1CC[C@@H](O)CC1n1cc(C(N)=O)c(Nc2ccccc2)n1"	"IC50"	"'='"	"185.0"	"nM"	"6.73"	""	"285415"	"UO_0000065"	"20.69"	"0.38"	"4.78"	"5.76"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3622134"	""	"0"	"421.53"	"0"	"3.91"	"15"	"CCn1c(C(=O)N(C2CC2)C2CC2)cc2c3c(ncn3C)c(Nc3nccs3)nc21"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	""	"UO_0000065"	"18.26"	"0.35"	"3.79"	"9.52"	"False"	"CHEMBL3625474"	"Inhibition of JAK2 in human SET2 cells assessed as inhibition of cell proliferation after 72 hrs by [3H]-thymidine incorporation assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621098"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3622138"	""	"0"	"383.42"	"1"	"0.31"	"1"	"CNc1nc2c(cc(-c3nnnn3C3CC3)n2C[C@H](O)CO)c2c1ncn2C"	"IC50"	"'='"	"1300.0"	"nM"	"5.89"	""	""	"UO_0000065"	"15.35"	"0.29"	"5.58"	"4.47"	"False"	"CHEMBL3625474"	"Inhibition of JAK2 in human SET2 cells assessed as inhibition of cell proliferation after 72 hrs by [3H]-thymidine incorporation assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621098"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3650983"	""	"0"	"400.46"	"0"	"2.04"	"BDBM153157"	"CCOC(=O)c1c[nH]c2ncnc(-c3ccc(N4CCS(=O)(=O)CC4)cc3)c12"	"IC50"	"'='"	"348.0"	"nM"	"6.46"	""	"294105"	"UO_0000065"	"16.13"	"0.32"	"4.42"	"6.14"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703040"	""	"0"	"462.48"	"0"	"3.26"	"BDBM147750"	"N#C[C@H]1C[C@H](N2CCC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc([C@H](O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	"285684"	"UO_0000065"	"17.13"	"0.33"	"4.66"	"6.59"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642348"	""	"0"	"476.61"	"0"	"4.43"	"BDBM99624"	"CN1CCC(c2ccc(Nc3nc4c(Nc5ccccc5S(C)(=O)=O)cccn4n3)cc2)CC1"	"IC50"	"'='"	"6.6"	"nM"	"8.18"	""	"216314"	"UO_0000065"	"17.16"	"0.33"	"3.75"	"8.93"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3699528"	""	"0"	"351.41"	"0"	"3.18"	"BDBM147546"	"CC(=O)c1ccc(Nc2nn([C@H]3CCCC[C@@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"285476"	"UO_0000065"	"24.75"	"0.46"	"5.52"	"7.64"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3650998"	""	"0"	"368.37"	"0"	"3.46"	"BDBM153174"	"C=C(C)C(=O)Nc1ccc(F)c(-c2ncnc3[nH]cc(C(=O)OCC)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294122"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699543"	""	"0"	"344.81"	"0"	"3.03"	"BDBM147561"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)nc2)n1"	"IC50"	"'='"	"178.0"	"nM"	"6.75"	""	"285491"	"UO_0000065"	"19.57"	"0.38"	"3.72"	"6.16"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702889"	""	"0"	"501.61"	"1"	"1.59"	"BDBM147588"	"N#C[C@@H]1CCCC[C@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)NCCN3CCOCC3)cc2)n1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"285518"	"UO_0000065"	"17.94"	"0.35"	"7.41"	"5.79"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3622136"	""	"0"	"435.56"	"0"	"4.22"	"17"	"CCn1c(C(=O)N(C2CC2)C2CC2)cc2c3c(ncn3C)c(Nc3ncc(C)s3)nc21"	"IC50"	"'='"	"2.1"	"nM"	"8.68"	""	""	"UO_0000065"	"19.92"	"0.38"	"4.46"	"10.73"	"False"	"CHEMBL3625473"	"Inhibition of JAK2 (unknown origin) using 5-FAMKKKKEEIYFFFG-OH as substrate after 60 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621098"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3622133"	""	"0"	"439.52"	"0"	"2.48"	"14"	"CCn1c(C(=O)N(C2CC2)C2CC2)cc2c3c(ncn3C)c(NC(=O)NCCOC)nc21"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	""	"UO_0000065"	"18.02"	"0.34"	"5.44"	"7.45"	"False"	"CHEMBL3625473"	"Inhibition of JAK2 (unknown origin) using 5-FAMKKKKEEIYFFFG-OH as substrate after 60 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621098"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3330112"	""	"0"	"417.90"	"0"	"4.61"	"15"	"Cc1ccc(Cl)cc1-c1[nH]c(-c2ccnc(N)n2)cc1C(=O)NCc1ccccc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL3374497"	"Inhibition of JAK2 V617F mutant in human SET2 cells"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3120985"	""	"0"	"472.33"	"0"	"2.72"	"8"	"Cn1c(-c2cn(CCP(=O)([O-])[O-])nn2)nc(-c2ccc(F)cc2)c1-c1ccncc1.[Na+].[Na+]"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3363474"	"Inhibition of JAK2 (unknown origin) by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352554"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3314275"	""	"0"	"556.43"	"1"	"3.15"	"17"	"CSc1nccc(-c2c(-c3ccc(F)cc3)nc3nc(-c4cn(CCP(=O)([O-])[O-])nn4)ccn23)n1.[Na+].[Na+]"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3363474"	"Inhibition of JAK2 (unknown origin) by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352554"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3314281"	""	"0"	"347.35"	"0"	"3.94"	"25"	"O=c1cc(-c2[nH]c(-c3ccc(O)cc3)nc2-c2ccc(F)cc2)cc[nH]1"	"IC50"	"'='"	"911.0"	"nM"	"6.04"	""	""	"UO_0000065"	"17.39"	"0.32"	"2.10"	"7.39"	"False"	"CHEMBL3363474"	"Inhibition of JAK2 (unknown origin) by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352554"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3330121"	""	"0"	"516.05"	"1"	"4.71"	"24"	"Cc1ccc(Cl)cc1-c1c(C(N)=O)cc(-c2ccnc(Nc3ccc(N4CCN(C)CC4)cc3)n2)n1C"	"IC50"	"'='"	"250.0"	"nM"	"6.60"	""	""	"UO_0000065"	"12.79"	"0.24"	"1.89"	"7.15"	"False"	"CHEMBL3374497"	"Inhibition of JAK2 V617F mutant in human SET2 cells"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3593769"	""	"0"	"374.45"	"0"	"2.61"	"10d"	"N#Cc1cccc(CN2CCC(Nc3c(C(N)=O)cnc4[nH]ccc34)CC2)c1"	"IC50"	"'='"	"46.0"	"nM"	"7.34"	""	""	"UO_0000065"	"19.59"	"0.36"	"4.73"	"6.62"	"False"	"CHEMBL3594790"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593212"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL4085905"	""	"0"	"505.60"	"1"	"3.51"	"49"	"CC[C@H](C(=O)Nc1cccc2c(-c3nc(Nc4cn(C)nc4C)ncc3F)c[nH]c12)N1CCN(C)CC1"	"IC50"	"'='"	"1770.0"	"nM"	"5.75"	""	""	"UO_0000065"	"11.38"	"0.21"	"2.24"	"5.38"	"False"	"CHEMBL4022634"	"Inhibition of N-terminal GST fused recombinant JAK2 (831 to 1132 amino acids) (unknown origin) expressed in insect cells using ATP and peptide substrate (5FAM-GEEPLYWSFPAKKK-NH2"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020810"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2017"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"1, CP-690,550"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"3.1"	"nM"	"8.51"	""	""	"UO_0000065"	"27.24"	"0.51"	"6.97"	"9.57"	"False"	"CHEMBL3594576"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate and ATP incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593193"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3593588"	""	"0"	"335.39"	"0"	"0.80"	"10b"	"CS(=O)(=O)N1CCC[C@@H](n2c(=O)[nH]c3cnc4[nH]ccc4c32)C1"	"IC50"	"'='"	"82.0"	"nM"	"7.09"	""	""	"UO_0000065"	"21.13"	"0.42"	"6.29"	"6.82"	"False"	"CHEMBL3594576"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate and ATP incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593193"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3116062"	""	"0"	"383.37"	"0"	"2.74"	"13e"	"C[C@H](Nc1nc(Nc2cn(C)cn2)c2cc(F)cnc2n1)c1ncc(F)cn1"	"IC50"	"'='"	"490.0"	"nM"	"6.31"	""	""	"UO_0000065"	"16.46"	"0.31"	"3.57"	"5.93"	"False"	"CHEMBL3118240"	"Inhibition of Jak2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112447"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL3116057"	""	"0"	"348.77"	"0"	"2.71"	"26"	"C[C@H](Nc1ncc(Cl)c(Nc2cn(C)cn2)n1)c1ncc(F)cn1"	"IC50"	"'='"	"120.0"	"nM"	"6.92"	""	""	"UO_0000065"	"19.84"	"0.39"	"4.21"	"7.41"	"False"	"CHEMBL3118240"	"Inhibition of Jak2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112447"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL3116060"	""	"0"	"394.41"	"0"	"3.22"	"13c, enantiomeric mixture"	"COc1ccc2c(Nc3cn(C)cn3)nc(NC(C)c3ncc(F)cn3)nc2c1"	"IC50"	"'='"	"24.0"	"nM"	"7.62"	""	""	"UO_0000065"	"19.32"	"0.36"	"4.40"	"7.42"	"False"	"CHEMBL3118240"	"Inhibition of Jak2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112447"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL3593590"	""	"0"	"324.34"	"0"	"1.28"	"11"	"N#CCC(=O)N1CCC[C@@H](n2c(=O)[nH]c3cnc4[nH]ccc4c32)C1"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	""	"UO_0000065"	"23.95"	"0.44"	"6.49"	"7.03"	"False"	"CHEMBL3594576"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate and ATP incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593193"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3593777"	""	"0"	"379.40"	"0"	"1.96"	"31"	"N#Cc1ccc(N2CC[C@@H](Nc3c(C(N)=O)cnc4[nH]ccc34)[C@@H](F)C2)nc1"	"IC50"	"'='"	"3.2"	"nM"	"8.49"	""	""	"UO_0000065"	"22.39"	"0.41"	"6.53"	"6.87"	"True"	"CHEMBL3594790"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593212"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3593774"	""	"0"	"366.43"	"0"	"1.63"	"12b"	"NC(=O)c1cnc2[nH]ccc2c1NC1CCN(c2ccc(CO)cn2)CC1"	"IC50"	"'='"	"100.0"	"nM"	"7.00"	""	""	"UO_0000065"	"19.10"	"0.35"	"5.37"	"5.83"	"False"	"CHEMBL3594790"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593212"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3593764"	""	"0"	"337.41"	"0"	"0.50"	"10b"	"CS(=O)(=O)N1CCC(Nc2c(C(N)=O)cnc3[nH]ccc23)CC1"	"IC50"	"'='"	"190.0"	"nM"	"6.72"	""	""	"UO_0000065"	"19.92"	"0.40"	"6.22"	"5.55"	"False"	"CHEMBL3594790"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593212"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL3593583"	""	"0"	"374.40"	"0"	"3.35"	"6i"	"CC1(C)CCCCC1n1c(=O)[nH]c2cnc3[nH]ccc3c21.O=C(O)C(=O)O"	"IC50"	"'='"	"85.0"	"nM"	"7.07"	""	""	"UO_0000065"	"24.86"	"0.46"	"3.72"	"10.64"	"False"	"CHEMBL3594576"	"Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate and ATP incubated for 1 hr by ELISA method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3593193"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"None"	""
"CHEMBL4471710"	""	"0"	"464.36"	"0"	"4.92"	"8a"	"O=C(CCCCCCn1cc(Nc2ncc(Cl)c(Nc3cccc(Cl)c3)n2)cn1)NO"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	""	"UO_0000065"	"17.23"	"0.35"	"3.08"	"6.84"	"False"	"CHEMBL4347596"	"Inhibition of recombinant human JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate measured after 60 mins by LANCE assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4346670"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4469297"	""	"0"	"395.90"	"0"	"3.35"	"8j"	"CCCNc1nc(Nc2cnn(CCCCCCC(=O)NO)c2)ncc1Cl"	"IC50"	"'='"	"30.0"	"nM"	"7.52"	""	""	"UO_0000065"	"19.00"	"0.38"	"4.17"	"6.43"	"False"	"CHEMBL4347596"	"Inhibition of recombinant human JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate measured after 60 mins by LANCE assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4346670"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4462229"	""	"0"	"450.33"	"0"	"4.53"	"8l"	"O=C(CCCCCn1cc(Nc2ncc(Cl)c(Nc3cccc(Cl)c3)n2)cn1)NO"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	""	"UO_0000065"	"18.11"	"0.37"	"3.62"	"6.97"	"False"	"CHEMBL4347596"	"Inhibition of recombinant human JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate measured after 60 mins by LANCE assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4346670"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4756015"	""	"0"	"434.46"	"0"	"3.84"	"6a"	"O=C1C=CC2(C=C1)OCC(=O)N2c1nc(-c2cccc3ccccc23)nn1-c1ccccc1"	"IC50"	"'='"	"59000.0"	"nM"	"4.23"	""	""	""	"9.73"	"0.18"	"0.39"	"5.47"	"False"	"CHEMBL4734888"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4732107"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2021"	"None"	""
"CHEMBL4447949"	""	"0"	"240.27"	"0"	"1.71"	"38"	"C=CCn1nc(C)c(-c2ncnc3[nH]ccc23)n1"	"IC50"	"'='"	"511.0"	"nM"	"6.29"	""	""	"UO_0000065"	"26.19"	"0.48"	"4.58"	"8.70"	"False"	"CHEMBL4429697"	"Inhibition of recombinant human C-terminal 6His-tagged JAK2 (808 to end amino acids) expressed in Sf21 cells measured after 1 hr in presence of ATP by TR-FRET assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4428074"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2016"	"CHEMBL4106362"	""
"CHEMBL4458964"	""	"0"	"295.35"	"0"	"2.61"	"53"	"Cc1nn(CCCCCC#N)nc1-c1ncnc2[nH]ccc12"	"IC50"	"'='"	"165.0"	"nM"	"6.78"	""	""	"UO_0000065"	"22.96"	"0.42"	"4.17"	"7.06"	"False"	"CHEMBL4429697"	"Inhibition of recombinant human C-terminal 6His-tagged JAK2 (808 to end amino acids) expressed in Sf21 cells measured after 1 hr in presence of ATP by TR-FRET assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4428074"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2016"	"CHEMBL4106362"	""
"CHEMBL4541291"	""	"0"	"415.90"	"0"	"4.38"	"12k"	"CC(Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1cc(F)ccc1Cl"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	""	"UO_0000065"	"19.77"	"0.39"	"3.84"	"10.54"	"False"	"CHEMBL4341687"	"Inhibition of human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr by Z'-LYTE assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340536"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2019"	"CHEMBL3308860"	""
"CHEMBL3234893"	""	"0"	"294.38"	"0"	"4.26"	"3"	"NC(=O)c1cc(-c2ccccc2)sc1Nc1ccccc1"	"IC50"	"'='"	"1010.0"	"nM"	"6.00"	""	""	"UO_0000065"	"20.37"	"0.39"	"1.74"	"10.88"	"False"	"CHEMBL3239499"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3232939"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL1789941"	"RUXOLITINIB"	"4"	"306.37"	"0"	"3.47"	"3"	"N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"0.056"	"nM"	"10.25"	""	""	"UO_0000065"	"33.46"	"0.61"	"6.78"	"12.32"	"False"	"CHEMBL4233426"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma-33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229421"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2018"	"None"	""
"CHEMBL4243347"	""	"0"	"462.51"	"1"	"3.88"	"8"	"O=C(CCCCCCC(=O)Nc1ccc(Nc2nc(-c3cn[nH]c3)c3cc[nH]c3n2)cc1)NO"	"IC50"	"'='"	"0.96"	"nM"	"9.02"	""	""	"UO_0000065"	"19.50"	"0.36"	"5.14"	"5.61"	"False"	"CHEMBL4233426"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma-33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229421"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2018"	"None"	""
"CHEMBL4242626"	""	"0"	"515.58"	"1"	"4.26"	"13i"	"N#CCCn1cc(-c2nc(Nc3ccc(NC(=O)CCCCCCC(=O)NO)cc3)nc3[nH]ccc23)cn1"	"IC50"	"'='"	"0.04"	"nM"	"10.40"	""	""	"UO_0000065"	"20.17"	"0.37"	"6.14"	"5.99"	"False"	"CHEMBL4233426"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma-33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229421"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2018"	"None"	""
"CHEMBL3262356"	""	"0"	"389.46"	"0"	"3.22"	"3b"	"N[C@H]1CCCC[C@H]1Nc1cc2nc[nH]c(=O)c2c(Nc2cccc3cc[nH]c23)n1"	"IC50"	"'='"	"105.0"	"nM"	"6.98"	""	""	"UO_0000065"	"17.92"	"0.33"	"3.76"	"5.61"	"False"	"CHEMBL3268711"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3259804"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3262358"	""	"0"	"423.91"	"0"	"3.88"	"3d"	"N[C@H]1CCCC[C@H]1Nc1cc2nc[nH]c(=O)c2c(Nc2cccc3c(Cl)c[nH]c23)n1"	"IC50"	"'='"	"1810.0"	"nM"	"5.74"	""	""	"UO_0000065"	"13.55"	"0.26"	"1.86"	"4.61"	"False"	"CHEMBL3268711"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3259804"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL4247128"	""	"0"	"516.61"	"1"	"4.93"	"13b"	"C=CCCn1cc(-c2nc(Nc3ccc(NC(=O)CCCCCCC(=O)NO)cc3)nc3[nH]ccc23)cn1"	"IC50"	"'='"	"0.041"	"nM"	"10.39"	""	""	"UO_0000065"	"20.11"	"0.37"	"5.46"	"6.93"	"False"	"CHEMBL4233426"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma-33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229421"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2018"	"None"	""
"CHEMBL4440261"	""	"0"	"308.39"	"0"	"3.17"	"12"	"CC(C)CNc1c(C(N)=O)cnn2cc(-c3ccccc3)cc12"	"IC50"	"'='"	"160.0"	"nM"	"6.80"	""	""	"UO_0000065"	"22.04"	"0.40"	"3.63"	"9.38"	"False"	"CHEMBL4339747"	"Inhibition of GST-tagged JAK2 (unknown origin) using fluoresceinated peptide as substrate measured after 3 hrs by electrophoresis method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4339199"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2019"	"None"	""
"CHEMBL3814406"	""	"0"	"317.39"	"0"	"1.53"	"3c"	"C[C@@H](O)Cn1c2ccc(C(N)=O)cc2nc1[C@H]1CC[C@H](O)CC1"	"IC50"	"'='"	"12100.0"	"nM"	"4.92"	""	""	"UO_0000065"	"15.49"	"0.29"	"3.39"	"4.85"	"False"	"CHEMBL3817413"	"Inhibition of JAK2 (unknown origin) using tyrosine 6 peptide as substrate by z'-lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3813615"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3126352"	""	"0"	"358.74"	"0"	"4.15"	"14"	"O=c1[nH]ccc2c(Nc3c(F)cc(F)cc3Cl)nc3ccncc3c12"	"IC50"	"'='"	"0.9"	"nM"	"9.05"	""	""	"UO_0000065"	"25.22"	"0.49"	"4.90"	"12.80"	"False"	"CHEMBL3131376"	"Inhibition of recombinant Jak2 (unknown origin) using biotinylated synthetic peptide substrate by homogeneous time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3124786"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3622376"	""	"0"	"242.24"	"0"	"0.62"	"65"	"c1nc(-c2cn(CC3CO3)nn2)c2cc[nH]c2n1"	"IC50"	"'='"	"2451.0"	"nM"	"5.61"	""	""	"UO_0000065"	"23.16"	"0.43"	"4.99"	"6.62"	"True"	"CHEMBL4351042"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4350951"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL3359912"	""	"0"	"288.35"	"0"	"1.39"	"4a"	"CC1(C)[C@@H](O)CC[C@H]1Nc1c(C(N)=O)cnn2cccc12"	"IC50"	"'='"	"130.0"	"nM"	"6.89"	""	""	"UO_0000065"	"23.88"	"0.45"	"5.50"	"7.43"	"False"	"CHEMBL3377596"	"Inhibition of JAK2 (unknown origin) by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352641"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3355482"	""	"0"	"380.47"	"0"	"3.76"	"2"	"CN(Cc1ccccc1)C(=O)c1ccc(S(=O)(=O)Nc2ccccc2)cc1"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3372981"	"Inhibition of Jak2 (unknown origin) in presence of 1 mM ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351882"	"1"	"Scientific Literature"	"ACS Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"1; CP-690,550"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"1.2"	"nM"	"8.92"	""	""	"UO_0000065"	"28.56"	"0.53"	"7.38"	"10.03"	"False"	"CHEMBL4630016"	"Inhibition of N-terminal GST-fused human JAK2 (880 to end residues) expressed in baculovirus infected Sf21 cells using TK-substrate-biotin as substrate incubated for 60 mins in presence of ATP by fluorescence method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4627398"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL4106362"	""
"CHEMBL3915198"	""	"0"	"486.62"	"0"	"3.71"	"102"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)C3CCCCCC3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3927538"	""	"0"	"517.54"	"1"	"3.72"	"175"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3cc(F)cc(F)c3)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3930823"	""	"0"	"499.55"	"0"	"3.50"	"297"	"N#CCC1(n2cc(-c3ccnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(O)cc3F)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3941336"	""	"0"	"541.56"	"1"	"3.53"	"344"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3nc(C(F)(F)F)cs3)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL4753147"	""	"0"	"410.50"	"0"	"3.54"	"13i"	"CC(C)n1cc(-c2nc(Nc3ccc4c(c3)CCN(CCCO)C4)ncc2F)cn1"	"IC50"	"'='"	"311.0"	"nM"	"6.51"	""	""	""	"15.85"	"0.30"	"2.97"	"8.23"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL4741668"	""	"0"	"387.49"	"0"	"3.85"	"13ai"	"Cc1cnc(Nc2ccc3c(c2)CN(CC#N)CC3)nc1-c1cnn(C(C)C)c1"	"IC50"	"'='"	"94.6"	"nM"	"7.02"	""	""	""	"18.13"	"0.33"	"3.17"	"8.50"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL4744166"	""	"0"	"407.52"	"0"	"3.11"	"13a"	"Cc1cnc(Nc2ccc3c(n2)CCN(CCCO)C3)nc1-c1cnn(C(C)C)c1"	"IC50"	"'='"	"2180.0"	"nM"	"5.66"	""	""	""	"13.89"	"0.26"	"2.55"	"6.15"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL4741075"	""	"0"	"506.61"	"2"	"5.30"	"13aj"	"Cc1cnc(Nc2ccc3c(c2)CN(C(=O)/C=C/C(=O)c2ccccc2)CC3)nc1-c1cnn(C(C)C)c1"	"IC50"	"'='"	"42.7"	"nM"	"7.37"	""	""	""	"14.55"	"0.26"	"2.07"	"7.92"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL3895028"	""	"0"	"464.45"	"0"	"4.93"	"5k"	"N#Cc1ccc2oc(-c3nc(Nc4ccc(N5CCNCC5)cc4)ncc3C(F)(F)F)cc2c1"	"IC50"	"'='"	"136.7"	"nM"	"6.86"	""	""	"UO_0000065"	"14.78"	"0.28"	"1.93"	"7.63"	"False"	"CHEMBL3868063"	"Inhibition of GST-tagged recombinant human JAK2 expressed in baculovirus using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3867460"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2017"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"Tofacitinib"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"4724.0"	"nM"	"5.33"	""	""	"UO_0000065"	"17.05"	"0.32"	"3.79"	"5.99"	"True"	"CHEMBL3868067"	"Inhibition of JAK2 V617F mutant in human HEL cells after 1 hr"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3867460"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2017"	"CHEMBL3308090"	""
"CHEMBL4741075"	""	"0"	"506.61"	"2"	"5.30"	"13aj"	"Cc1cnc(Nc2ccc3c(c2)CN(C(=O)/C=C/C(=O)c2ccccc2)CC3)nc1-c1cnn(C(C)C)c1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	""	""	"17.17"	"0.31"	"3.40"	"9.35"	"False"	"CHEMBL4723820"	"Inhibition of recombinant human JAK2 (808 to end residues) KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate measured after 40 mins in presence of [gamm33P]ATP by scintillation counting method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 0.6667 hr"
"CHEMBL3398138"	""	"0"	"375.45"	"0"	"2.88"	"7e"	"Cc1ccccc1S(=O)(=O)Nc1cnc(N2CCCCC2)c(C(=O)O)c1"	"IC50"	"'='"	"6900.0"	"nM"	"5.16"	""	""	"UO_0000065"	"13.75"	"0.27"	"2.28"	"5.18"	"False"	"CHEMBL3399759"	"Inhibition of IL4-induced JAK2 autophosphorylation in human HT-29 cells by SDS-polyacrylamide gel electrophoresis and Western blot method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HT-29"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3397032"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2015"	"CHEMBL3307768"	""
"CHEMBL3952353"	""	"0"	"502.53"	"1"	"3.33"	"43"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3cc(F)ccc3F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3967883"	""	"0"	"552.54"	"1"	"4.21"	"82"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(C(F)(F)F)cc3F)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3961956"	""	"0"	"508.58"	"1"	"3.56"	"100"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)C3CCC(F)(F)CC3)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3335683"	""	"0"	"338.39"	"0"	"0.50"	"10"	"CS(=O)(=O)N1CCC[C@H](NC(=O)Nc2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"101.0"	"nM"	"7.00"	""	""	"UO_0000065"	"20.67"	"0.42"	"6.50"	"5.83"	"False"	"CHEMBL3374010"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 1 hr in presence of [gamma-33P]ATP by scintillation counting analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351377"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3335685"	""	"0"	"380.47"	"0"	"1.53"	"12"	"CC(C)CS(=O)(=O)N1CCC[C@H](NC(=O)Nc2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"47.0"	"nM"	"7.33"	""	""	"UO_0000065"	"19.26"	"0.38"	"5.80"	"6.10"	"False"	"CHEMBL3374010"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 1 hr in presence of [gamma-33P]ATP by scintillation counting analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351377"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3335691"	""	"0"	"397.46"	"0"	"1.75"	"21"	"N#CCS(=O)(=O)N1CCC[C@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"9.0"	"nM"	"8.05"	""	""	"UO_0000065"	"20.24"	"0.39"	"6.30"	"6.30"	"False"	"CHEMBL3374010"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 1 hr in presence of [gamma-33P]ATP by scintillation counting analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351377"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3335692"	""	"0"	"428.56"	"0"	"3.13"	"22"	"CC(C)CS(=O)(=O)N1C[C@@H](C)C[C@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"51.0"	"nM"	"7.29"	""	""	"UO_0000065"	"17.02"	"0.33"	"4.16"	"7.02"	"False"	"CHEMBL3374010"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 1 hr in presence of [gamma-33P]ATP by scintillation counting analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351377"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3907726"	""	"0"	"585.65"	"1"	"4.73"	"124"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(-c4ccccc4C#N)c(F)c3)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3984226"	""	"0"	"528.57"	"1"	"3.86"	"139"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CC3CCC(C2)N3C(=O)c2ccc(F)c(F)c2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3898099"	""	"0"	"561.57"	"1"	"4.00"	"144"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CC3CCC(C2)N3C(=O)c2ccnc(C(F)(F)F)c2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3914358"	""	"0"	"486.62"	"0"	"3.71"	"153"	"CC1(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CCN(C(=O)C2CCCCC2)CC1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3972573"	""	"0"	"535.53"	"1"	"3.86"	"172"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3ccc(F)c(F)c3F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3917324"	""	"0"	"495.57"	"0"	"3.42"	"220"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(Cc3ccc(F)c(C#N)c3)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3910630"	""	"0"	"519.03"	"1"	"4.59"	"244"	"CC1CC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CCN1Cc1c(F)cccc1Cl"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3961088"	""	"0"	"521.61"	"1"	"2.20"	"260"	"Cc1noc(C)c1S(=O)(=O)N1CCC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CC1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL4740411"	""	"0"	"410.45"	"0"	"2.68"	"13f"	"CC(C)n1cc(-c2nc(Nc3ccc4c(c3)CCN(C(=O)CO)C4)ncc2F)cn1"	"IC50"	"'='"	"574.0"	"nM"	"6.24"	""	""	""	"15.21"	"0.28"	"3.56"	"6.49"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL4776686"	""	"0"	"400.53"	"0"	"4.35"	"13w"	"CC#CCN1CCc2cc(Nc3ncc(C)c(-c4cnn(C(C)C)c4)n3)ccc2C1"	"IC50"	"'='"	"794.0"	"nM"	"6.10"	""	""	""	"15.23"	"0.28"	"1.75"	"10.36"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL4789273"	""	"0"	"520.64"	"2"	"5.61"	"13al"	"Cc1ccc(C(=O)/C=C/C(=O)N2CCc3ccc(Nc4ncc(C)c(-c5cnn(C(C)C)c5)n4)cc3C2)cc1"	"IC50"	"'='"	"25.0"	"nM"	"7.60"	""	""	""	"14.60"	"0.27"	"1.99"	"8.17"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL3914084"	""	"0"	"501.54"	"1"	"3.93"	"279"	"N#CCC1(n2ccc(-c3ncnc4[nH]ccc34)c2)CN(C2CCN(C(=O)c3c(F)cccc3F)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3965177"	""	"0"	"499.55"	"0"	"3.58"	"292"	"N#CCC1(n2ccc(-c3ncnc4[nH]ccc34)c2)CN(C2CCN(C(=O)Nc3ncccc3F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3984360"	""	"0"	"502.53"	"1"	"3.33"	"320"	"N#CCC1(n2cc(-c3c(F)cnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccncc3F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3916000"	""	"0"	"963.74"	"1"	"3.75"	"380"	"CC(C)(C)NCc1cc(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)nc(C(F)(F)F)n1.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3977874"	""	"0"	"474.57"	"0"	"3.15"	"387"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)OCC3CCC3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL1995703"	""	"0"	"509.68"	"1"	"4.10"	"TG101209"	"Cc1cnc(Nc2ccc(N3CCN(C)CC3)cc2)nc1Nc1cccc(S(=O)(=O)NC(C)(C)C)c1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	""	"UO_0000065"	"16.13"	"0.31"	"4.12"	"8.02"	"True"	"CHEMBL3877189"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3875233"	"1"	"Scientific Literature"	"Nat Rev Drug Discov"	"2017"	"None"	""
"CHEMBL3978964"	""	"0"	"577.55"	"1"	"4.08"	"332"	"N#CCC1(n2cc(-c3c(C#N)cnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccnc(C(F)(F)F)c3F)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3980203"	""	"0"	"490.56"	"0"	"4.54"	"49"	"O=C(CCCCOc1ccc2cc1COC/C=C/COCc1cccc(c1)-c1ccnc(n1)N2)NO"	"IC50"	"'='"	"2.45"	"nM"	"8.61"	""	""	"UO_0000065"	"17.55"	"0.33"	"4.07"	"7.50"	"False"	"CHEMBL3877344"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]ATP addition measured after 120 mins by Hotspot assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3877241"	"1"	"Scientific Literature"	"J Med Chem"	"2016"	"None"	""
"CHEMBL3359916"	""	"0"	"302.38"	"0"	"1.78"	"4e"	"CC1(C)C[C@@](C)(O)C[C@H]1Nc1c(C(N)=O)cnn2cccc12"	"IC50"	"'='"	"350.0"	"nM"	"6.46"	""	""	"UO_0000065"	"21.35"	"0.40"	"4.68"	"6.97"	"False"	"CHEMBL3377596"	"Inhibition of JAK2 (unknown origin) by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352641"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL1789941"	"RUXOLITINIB"	"4"	"306.37"	"0"	"3.47"	"INCB018424"	"N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	""	""	""	""	""	""	"False"	"CHEMBL4685358"	"Inhibition of recombinant epitope tagged JAK2 (828 to 1132 residues) (unknown origin) using Chk2 as substrate by HTRF assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	""
"CHEMBL4783966"	""	"0"	"382.39"	"0"	"1.67"	"ABT-494"	"CC[C@H]1CN(C(=O)NCC(F)(F)F)C[C@H]1C1C=NC2=CN=C3NC=CC3N21"	"IC50"	"'='"	"120.0"	"nM"	"6.92"	""	""	""	""	""	""	""	"False"	"CHEMBL4685363"	"Inhibition of recombinant human C-terminal His6-tagged JAK2 (808 to end residues) expressed in baculovirus infected Sf21 insect cells using Biotin-TYR1 (Biotin-(Ahx)-GAEEEIYAAFFA-COOH as substrate"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	""
"CHEMBL4642546"	""	"0"	"275.35"	"0"	"2.14"	"18"	"Cc1[nH]nc2[nH]c(=O)c(CCO)c(C3CCCCC3)c12"	"IC50"	"'='"	"3900.0"	"nM"	"5.41"	""	""	"UO_0000065"	"19.64"	"0.37"	"3.27"	"6.61"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4645814"	""	"0"	"270.34"	"0"	"2.75"	"21"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](CC#N)CC3)c12"	"IC50"	"'='"	"360.0"	"nM"	"6.44"	""	""	"UO_0000065"	"23.84"	"0.44"	"3.69"	"7.55"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4639048"	""	"0"	"378.50"	"0"	"2.31"	"31"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](NS(=O)(=O)CC4CCC4)CC3)c12"	"IC50"	"'='"	"570.0"	"nM"	"6.24"	""	""	"UO_0000065"	"16.50"	"0.33"	"3.93"	"5.80"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4638030"	""	"0"	"367.45"	"0"	"2.60"	"35"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](CC(=O)N4CCC(C#N)C4)CC3)c12"	"IC50"	"'='"	"89.0"	"nM"	"7.05"	""	""	"UO_0000065"	"19.19"	"0.36"	"4.45"	"6.67"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4649484"	""	"0"	"418.54"	"0"	"3.92"	"36"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](CC(=O)N4CC(Cc5ccccc5)C4)CC3)c12"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	""	"UO_0000065"	"18.69"	"0.34"	"3.90"	"9.56"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"1"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"4.1"	"nM"	"8.39"	""	""	"UO_0000065"	"26.85"	"0.50"	"6.85"	"9.43"	"True"	"CHEMBL3299213"	"Inhibition of recombinant JAK2 kinase domain (unknown origin) using FITC-KGGEEEEYFELVKK as substrate assessed as inhibition of substrate phosphorylation by peptide mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3297690"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL2414539"	""	"0"	"373.42"	"0"	"4.36"	"35"	"CC(C)c1cc(-c2cccn3nc(Nc4ccc(C(=O)O)cc4)nc23)ccn1"	"IC50"	"'='"	"379.0"	"nM"	"6.42"	""	""	"UO_0000065"	"17.20"	"0.31"	"2.06"	"6.95"	"False"	"CHEMBL2415128"	"Inhibition of JAK2 in human SET2 cells assessed as reduction of phosphorylated STAT5 level"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2412966"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2208034"	""	"0"	"444.54"	"0"	"3.41"	"10d, XL019"	"O=C(Nc1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1)[C@H]1CCCN1"	"IC50"	"'='"	"695.0"	"nM"	"6.16"	""	""	"UO_0000065"	"13.85"	"0.25"	"2.75"	"6.74"	"False"	"CHEMBL2214784"	"Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT3 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2203210"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2012"	"CHEMBL3308090"	""
"CHEMBL3330124"	""	"0"	"361.33"	"0"	"3.15"	"27"	"Cc1ccc(C(F)(F)F)cc1-c1[nH]c(-c2ccnc(N)n2)cc1C(N)=O"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	""	"UO_0000065"	"22.14"	"0.42"	"4.85"	"7.23"	"False"	"CHEMBL3374493"	"Inhibition of recombinant human JAK2 (808-1132 residues) using LPLDKDYYVVREPGQ as substrate by radiometric assay in presence of [33P]-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330121"	""	"0"	"516.05"	"1"	"4.71"	"24"	"Cc1ccc(Cl)cc1-c1c(C(N)=O)cc(-c2ccnc(Nc3ccc(N4CCN(C)CC4)cc3)n2)n1C"	"IC50"	"'='"	"22.0"	"nM"	"7.66"	""	""	"UO_0000065"	"14.84"	"0.28"	"2.95"	"8.30"	"False"	"CHEMBL3374493"	"Inhibition of recombinant human JAK2 (808-1132 residues) using LPLDKDYYVVREPGQ as substrate by radiometric assay in presence of [33P]-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL2325906"	""	"0"	"297.36"	"0"	"2.50"	"3h"	"C[C@H](NC(=O)c1c[nH]c2ncc(C3CC3)nc12)C(C)(C)C#N"	"IC50"	"'='"	"10.9"	"nM"	"7.96"	""	""	"UO_0000065"	"26.78"	"0.49"	"5.46"	"8.43"	"False"	"CHEMBL2329570"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 30 mins by scintillation counting analysis in presence of [gamma-33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321829"	"1"	"Scientific Literature"	"J. Med. Chem."	"2013"	"None"	""
"CHEMBL2325909"	""	"0"	"341.42"	"0"	"1.97"	"3k"	"C[C@@H](NC(=O)c1c[nH]c2ncc(C3CC3)nc12)C(=O)N1CCCCC1"	"IC50"	"'='"	"123.1"	"nM"	"6.91"	""	""	"UO_0000065"	"20.24"	"0.38"	"4.94"	"7.59"	"False"	"CHEMBL2329570"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 30 mins by scintillation counting analysis in presence of [gamma-33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321829"	"1"	"Scientific Literature"	"J. Med. Chem."	"2013"	"None"	""
"CHEMBL4171692"	""	"0"	"482.61"	"0"	"2.92"	"7"	"Cc1cnc(Nc2cc(N3CCN(C)CC3)cc(S(C)(=O)=O)c2)nc1Nc1cccc(CO)c1"	"IC50"	"'='"	"929.0"	"nM"	"6.03"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4145184"	"Inhibition of recombinant human JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate after 10 mins by caliper assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4138312"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4159048"	""	"0"	"434.52"	"0"	"3.80"	"21"	"Cc1cnc(Nc2cc(N3C[C@@H]4C[C@H]3CN4C)ccc2F)nc1Nc1cccc(CO)c1"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4145184"	"Inhibition of recombinant human JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate after 10 mins by caliper assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4138312"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3330128"	""	"0"	"381.75"	"0"	"3.49"	"31"	"NC(=O)c1cc(-c2ccnc(N)n2)[nH]c1-c1cc(Cl)ccc1C(F)(F)F"	"IC50"	"'='"	"53.0"	"nM"	"7.28"	""	""	"UO_0000065"	"19.06"	"0.38"	"3.79"	"6.57"	"False"	"CHEMBL3374493"	"Inhibition of recombinant human JAK2 (808-1132 residues) using LPLDKDYYVVREPGQ as substrate by radiometric assay in presence of [33P]-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330122"	""	"0"	"348.19"	"0"	"3.13"	"25"	"NC(=O)c1cc(-c2ccnc(N)n2)[nH]c1-c1cc(Cl)ccc1Cl"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	""	"UO_0000065"	"22.75"	"0.47"	"4.79"	"7.16"	"False"	"CHEMBL3374493"	"Inhibition of recombinant human JAK2 (808-1132 residues) using LPLDKDYYVVREPGQ as substrate by radiometric assay in presence of [33P]-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330118"	""	"0"	"341.80"	"0"	"3.24"	"21"	"CNc1nccc(-c2cc(C(N)=O)c(-c3cc(Cl)ccc3C)[nH]2)n1"	"IC50"	"'='"	"43.0"	"nM"	"7.37"	""	""	"UO_0000065"	"21.55"	"0.42"	"4.13"	"7.62"	"False"	"CHEMBL3374493"	"Inhibition of recombinant human JAK2 (808-1132 residues) using LPLDKDYYVVREPGQ as substrate by radiometric assay in presence of [33P]-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL2414538"	""	"0"	"376.42"	"0"	"3.69"	"34"	"CC(C)Cn1cc(-c2cccn3nc(Nc4ccc(C(=O)O)cc4)nc23)cn1"	"IC50"	"'='"	"156.0"	"nM"	"6.81"	""	""	"UO_0000065"	"18.08"	"0.33"	"3.12"	"6.99"	"False"	"CHEMBL2415128"	"Inhibition of JAK2 in human SET2 cells assessed as reduction of phosphorylated STAT5 level"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2412966"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL3330125"	""	"0"	"381.75"	"0"	"3.49"	"28"	"NC(=O)c1cc(-c2ccnc(N)n2)[nH]c1-c1cc(C(F)(F)F)ccc1Cl"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	""	"UO_0000065"	"21.21"	"0.43"	"4.61"	"7.32"	"False"	"CHEMBL3374493"	"Inhibition of recombinant human JAK2 (808-1132 residues) using LPLDKDYYVVREPGQ as substrate by radiometric assay in presence of [33P]-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL4287153"	""	"0"	"520.64"	"1"	"4.18"	"3"	"CNc1nc2sc(-c3cccc([C@@H](C)NC(=O)c4ccccc4S(C)(=O)=O)c3)nc2c2c1ncn2C"	"IC50"	"'>'"	"2000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4251837"	"Inhibition of JAK2 JH2 domain (unknown origin)"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4251544"	"1"	"Scientific Literature"	"MedChemComm"	"2017"	"None"	""
"CHEMBL4568482"	""	"0"	"398.40"	"0"	"1.39"	"7"	"O=c1n(CCO)c2cnc(-c3cnc4ccc(F)cn34)nc2n1C1CCOCC1"	"IC50"	"'='"	"90.0"	"nM"	"7.05"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4441275"	""	"0"	"435.44"	"1"	"0.48"	"10"	"N#Cc1ccc2ncc(-c3ncc4c(n3)n(C3CCOCC3)c(=O)n4C[C@H](O)CO)n2c1"	"IC50"	"'='"	"75.0"	"nM"	"7.12"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4558494"	""	"0"	"394.37"	"0"	"2.06"	"22"	"O=c1[nH]cccc1Nc1ncc2[nH]c(=O)n([C@@H]3CCOc4c(F)cccc43)c2n1"	"IC50"	"'='"	"3.2"	"nM"	"8.49"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4517586"	""	"0"	"385.33"	"0"	"1.83"	"29"	"C[C@H](c1ccc(F)cn1)n1c(=O)[nH]c2cnc(Nc3cc(F)c[nH]c3=O)nc21"	"IC50"	"'='"	"4.8"	"nM"	"8.32"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4460058"	""	"0"	"401.79"	"0"	"2.35"	"30"	"C[C@H](c1ccc(F)cn1)n1c(=O)[nH]c2cnc(Nc3cc(Cl)c[nH]c3=O)nc21"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4587709"	""	"0"	"394.40"	"0"	"0.63"	"33"	"N#CCC(=O)N1CCC[C@@H](n2c(=O)[nH]c3cnc(Nc4ccc[nH]c4=O)nc32)C1"	"IC50"	"'='"	"7.4"	"nM"	"8.13"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416474"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL4463007"	""	"0"	"365.40"	"0"	"2.20"	"34"	"N#CC[C@H]1CC[C@H](n2c(=O)[nH]c3cnc(Nc4ccc[nH]c4=O)nc32)CC1"	"IC50"	"'='"	"219.0"	"nM"	"6.66"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4416531"	"Inhibition of JAK2 in human PBMC assessed as reduction in GM-CSF induced STAT5 phosphorylation preincubated for 30 mins followed by GM-CSF stimulation and measured after 30 mins by Alexa 488-antibody-based FACS analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4414617"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"2"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"4.1"	"nM"	"8.39"	""	""	"UO_0000065"	"26.85"	"0.50"	"6.85"	"9.43"	"True"	"CHEMBL4429697"	"Inhibition of recombinant human C-terminal 6His-tagged JAK2 (808 to end amino acids) expressed in Sf21 cells measured after 1 hr in presence of ATP by TR-FRET assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4428074"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2016"	"CHEMBL4106362"	""
"CHEMBL4459730"	""	"0"	"258.28"	"0"	"1.17"	"43"	"COCCn1nc(C)c(-c2ncnc3[nH]ccc23)n1"	"IC50"	"'='"	"210.0"	"nM"	"6.68"	""	""	"UO_0000065"	"25.85"	"0.48"	"5.51"	"8.19"	"False"	"CHEMBL4429697"	"Inhibition of recombinant human C-terminal 6His-tagged JAK2 (808 to end amino acids) expressed in Sf21 cells measured after 1 hr in presence of ATP by TR-FRET assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4428074"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2016"	"CHEMBL4106362"	""
"CHEMBL4473540"	""	"0"	"258.29"	"0"	"0.91"	"46"	"Cc1nn(CCCO)nc1-c1ncnc2[nH]ccc12"	"IC50"	"'='"	"156.0"	"nM"	"6.81"	""	""	"UO_0000065"	"26.35"	"0.49"	"5.90"	"7.36"	"False"	"CHEMBL4429697"	"Inhibition of recombinant human C-terminal 6His-tagged JAK2 (808 to end amino acids) expressed in Sf21 cells measured after 1 hr in presence of ATP by TR-FRET assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4428074"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2016"	"CHEMBL4106362"	""
"CHEMBL3914490"	""	"0"	"522.64"	"1"	"4.27"	"96"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3csc4ccccc34)CC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL2414542"	""	"0"	"362.39"	"0"	"3.62"	"38"	"CC(C)n1cc(-c2cccn3nc(Nc4ccc(C(=O)O)cc4)nc23)cn1"	"IC50"	"'='"	"151.0"	"nM"	"6.82"	""	""	"UO_0000065"	"18.82"	"0.35"	"3.20"	"7.01"	"False"	"CHEMBL2415128"	"Inhibition of JAK2 in human SET2 cells assessed as reduction of phosphorylated STAT5 level"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2412966"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL2443138"	""	"0"	"452.51"	"0"	"3.44"	"30"	"CN1CCC(NC(=O)c2cc(-c3c(O)cc(O)cc3Oc3ccc(N(C)C)cc3)on2)CC1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2443999"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2439976"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2013"	"None"	""
"CHEMBL4589134"	""	"0"	"373.21"	"0"	"2.34"	"10a"	"C=CC(=O)Nc1cccc(Cn2nc(Br)c3c(N)ncnc32)c1"	"IC50"	"'='"	"73.1"	"nM"	"7.14"	""	""	"UO_0000065"	"19.12"	"0.42"	"4.80"	"7.23"	"False"	"CHEMBL4402146"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-biotin as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4400567"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4456730"	""	"0"	"345.37"	"0"	"2.24"	"8b"	"Cn1cc(Nc2ncnc3c2cnn3Cc2cccc(NC#N)c2)cn1"	"IC50"	"'='"	"589.5"	"nM"	"6.23"	""	""	"UO_0000065"	"18.04"	"0.33"	"3.99"	"5.70"	"False"	"CHEMBL4402146"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-biotin as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4400567"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4459635"	""	"0"	"364.21"	"0"	"1.25"	"10f"	"N#CCC(=O)N1CCCC(n2nc(Br)c3c(N)ncnc32)C1"	"IC50"	"'='"	"82.1"	"nM"	"7.09"	""	""	"UO_0000065"	"19.45"	"0.44"	"5.84"	"6.23"	"False"	"CHEMBL4402146"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-biotin as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4400567"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4561431"	""	"0"	"366.39"	"0"	"0.58"	"11k"	"C=CC(=O)N1CCC(n2nc(-c3cc(C=O)n(C)n3)c3c(N)ncnc32)C1"	"IC50"	"'='"	"9.7"	"nM"	"8.01"	""	""	"UO_0000065"	"21.87"	"0.41"	"7.43"	"6.42"	"False"	"CHEMBL4402146"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-biotin as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4400567"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4069283"	""	"0"	"342.40"	"0"	"2.67"	"25"	"O=C(CCCCCCCn1cc(-c2ncnc3[nH]ccc23)cn1)NO"	"IC50"	"'='"	"481.0"	"nM"	"6.32"	""	""	"UO_0000065"	"18.45"	"0.35"	"3.65"	"5.81"	"False"	"CHEMBL4031305"	"Inhibition of human JAK2 using poly[Glu:Tyr] as substrate in presence of [gamma-33P]-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028864"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL2062787"	""	"0"	"240.27"	"0"	"1.99"	"12"	"COc1ccccc1-c1cccn2nc(N)nc12"	"IC50"	"'='"	"2132.0"	"nM"	"5.67"	""	""	"UO_0000065"	"23.60"	"0.43"	"3.68"	"8.67"	"False"	"CHEMBL2067611"	"Inhibition of human JAK2 expressed in baculovirus using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate preincubated for 1 hr measured after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2062792"	""	"0"	"288.33"	"0"	"1.38"	"17"	"CS(=O)(=O)c1ccc(-c2cccn3nc(N)nc23)cc1"	"IC50"	"'='"	"47.0"	"nM"	"7.33"	""	""	"UO_0000065"	"25.41"	"0.50"	"5.95"	"8.11"	"False"	"CHEMBL2067611"	"Inhibition of human JAK2 expressed in baculovirus using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate preincubated for 1 hr measured after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2062800"	""	"0"	"442.52"	"0"	"2.95"	"25"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4cccc(S(C)(=O)=O)c4)nc23)cc1"	"IC50"	"'='"	"5.6"	"nM"	"8.25"	""	""	"UO_0000065"	"18.65"	"0.38"	"5.30"	"7.47"	"True"	"CHEMBL2067611"	"Inhibition of human JAK2 expressed in baculovirus using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate preincubated for 1 hr measured after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2062809"	""	"0"	"461.59"	"0"	"4.35"	"35"	"CN1CCC(c2cccc(Nc3nc4c(-c5ccc(S(C)(=O)=O)cc5)cccn4n3)c2)CC1"	"IC50"	"'='"	"50.0"	"nM"	"7.30"	""	""	"UO_0000065"	"15.82"	"0.30"	"2.95"	"9.17"	"False"	"CHEMBL2067179"	"Inhibition of JAK2 in human TF-1 cells using GM-CSF pretreated for 1 hr prior to GM-CSF addition measured after 5 hrs by FRET based GeneBLAzer assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"CHEMBL3307972"	""
"CHEMBL4076794"	""	"0"	"407.52"	"0"	"3.43"	"11"	"COc1cccc(-c2cc3c(N[C@@H]4CC[C@](C)(N)C4(C)C)c(C(N)=O)cnn3c2)c1"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4054822"	"Inhibition of GST-tagged JAK2 (unknown origin) after 3 hrs by Caliper assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4052645"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4073562"	""	"0"	"392.51"	"0"	"3.12"	"27"	"Cc1cc(-c2cc3c(N[C@@H]4CC[C@](C)(N)C4(C)C)c(C(N)=O)cnn3c2)ccn1"	"IC50"	"'='"	"3.5"	"nM"	"8.46"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4054822"	"Inhibition of GST-tagged JAK2 (unknown origin) after 3 hrs by Caliper assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4052645"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4228653"	""	"0"	"832.00"	"4"	"8.04"	"39"	"CCNC(=O)c1cc2c(-c3cccc(OCCCCCCOc4ccc(Nc5nc(-c6cnn(CCCCCCC(=O)NO)c6)c6cc[nH]c6n5)cc4)c3)nc(N)nc2s1"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4222523"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma33P]-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219149"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2018"	"None"	""
"CHEMBL4533885"	""	"0"	"514.63"	"1"	"3.53"	"15a"	"CC(=O)c1ccc(NC(=O)N2CCN(c3ccnc(Nc4ccc(N5CCN(C)CC5)cc4)n3)CC2)cc1"	"IC50"	"'='"	"13.8"	"nM"	"7.86"	""	""	"UO_0000065"	"15.27"	"0.28"	"4.33"	"8.11"	"False"	"CHEMBL4362531"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain (826 to 1132 resiudes) expressed in baculovirus expression system using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition measured after 1 hr in presence of ATP by mobility shift assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4359878"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2019"	"None"	""
"CHEMBL3939795"	""	"0"	"597.07"	"2"	"5.29"	"BDBM230147"	"COc1ccc2c(=O)n(-c3cccc(-c4c(Cl)cc(C(N)=O)c5[nH]c6cc(C(C)(C)O)ccc6c45)c3C)c(=O)n(C)c2c1"	"IC50"	"'='"	"1500.0"	"nM"	"5.82"	""	"402017"	"UO_0000065"	"9.75"	"0.18"	"0.53"	"4.40"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3946439"	""	"0"	"585.04"	"2"	"5.42"	"BDBM230087"	"Cc1c(-c2c(Cl)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)c2ccc(F)cc2n(C)c1=O"	"IC50"	"'>'"	"2000.0"	"nM"	""	""	"402020"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3936249"	""	"0"	"585.04"	"2"	"5.42"	"BDBM230089"	"Cc1c(-c2c(Cl)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)c2cccc(F)c2n(C)c1=O"	"IC50"	"'='"	"910.0"	"nM"	"6.04"	""	"402022"	"UO_0000065"	"10.33"	"0.20"	"0.62"	"4.91"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3936156"	""	"0"	"571.01"	"2"	"5.41"	"BDBM230091"	"Cc1c(-c2c(Cl)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)[nH]c2c(F)cccc2c1=O"	"IC50"	"'='"	"570.0"	"nM"	"6.24"	""	"402024"	"UO_0000065"	"10.94"	"0.21"	"0.83"	"4.66"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3896019"	""	"0"	"568.58"	"1"	"4.90"	"BDBM230143"	"Cc1c(-c2c(F)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)c2cccc(F)c2n(C)c1=O"	"IC50"	"'='"	"2000.0"	"nM"	"5.70"	""	"402030"	"UO_0000065"	"10.02"	"0.19"	"0.80"	"4.63"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3913962"	""	"0"	"597.05"	"2"	"5.72"	"BDBM230099"	"Cc1c(-c2c(Cl)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)ccn(-c2ccc(F)cc2)c1=O"	"IC50"	"'='"	"440.0"	"nM"	"6.36"	""	"402034"	"UO_0000065"	"10.65"	"0.20"	"0.64"	"5.16"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3892891"	""	"0"	"439.52"	"0"	"3.07"	"BDBM229027"	"Cc1cccc(Nc2nn(C3(CC#N)CCN(C(=O)OC(C)(C)C)CC3)cc2C(N)=O)n1"	"IC50"	"'='"	"1009.0"	"nM"	"6.00"	""	"400771"	"UO_0000065"	"13.64"	"0.26"	"2.93"	"4.31"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3899672"	""	"0"	"318.38"	"0"	"2.54"	"BDBM228673"	"CN(c1ccc(C#N)cc1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399654"	"UO_0000065"	"32.22"	"0.58"	"7.72"	"14.28"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3977452"	""	"0"	"474.54"	"0"	"3.28"	"BDBM228750"	"CN(c1ccc(C(=O)N[C@@H](CO)c2ccccc2)cc1F)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399680"	"UO_0000065"	"21.62"	"0.40"	"6.98"	"10.54"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3891000"	""	"0"	"441.51"	"0"	"2.93"	"BDBM229307"	"CC(C)(C)CC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CC1"	"IC50"	"'='"	"44.0"	"nM"	"7.36"	""	"401046"	"UO_0000065"	"16.66"	"0.31"	"4.43"	"5.66"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3908935"	""	"0"	"481.45"	"0"	"3.08"	"BDBM229308"	"CC(C)(C(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CC1)C(F)(F)F"	"IC50"	"'='"	"28.0"	"nM"	"7.55"	""	"401047"	"UO_0000065"	"15.69"	"0.30"	"4.47"	"5.81"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4109620"	""	"0"	"429.46"	"0"	"1.26"	"BDBM229315"	"C[C@@H](O)CC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CC1"	"IC50"	"'='"	"47.0"	"nM"	"7.33"	""	"401054"	"UO_0000065"	"17.06"	"0.32"	"6.07"	"4.88"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4107077"	""	"0"	"428.40"	"0"	"1.50"	"BDBM229338"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CN(S(=O)(=O)C(F)(F)F)C1"	"IC50"	"'='"	"585.0"	"nM"	"6.23"	""	"401077"	"UO_0000065"	"14.55"	"0.29"	"4.73"	"4.65"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3918828"	""	"0"	"448.96"	"0"	"4.28"	"BDBM229066"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(Cc2ccccc2Cl)CC1"	"IC50"	"'='"	"55.0"	"nM"	"7.26"	""	"400802"	"UO_0000065"	"16.17"	"0.31"	"2.98"	"7.26"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3976451"	""	"0"	"472.60"	"None"	"None"	"BDBM229183"	"C[Si](C)(C)COC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CC1"	"IC50"	"'='"	"745.0"	"nM"	"6.13"	""	"400920"	"UO_0000065"	"12.97"	"None"	"None"	"None"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3946128"	""	"0"	"451.41"	"0"	"2.37"	"BDBM229200"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(C(=O)OCC(F)F)CC1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	"400937"	"UO_0000065"	"18.39"	"0.35"	"5.93"	"5.97"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3945721"	""	"0"	"396.45"	"0"	"1.60"	"BDBM229255"	"COCC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)CC1"	"IC50"	"'='"	"93.0"	"nM"	"7.03"	""	"400994"	"UO_0000065"	"17.74"	"0.33"	"5.43"	"5.57"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3893763"	""	"0"	"422.49"	"0"	"2.14"	"BDBM229259"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)C2CCCO2)CC1"	"IC50"	"'='"	"107.0"	"nM"	"6.97"	""	"400998"	"UO_0000065"	"16.50"	"0.31"	"4.83"	"5.52"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3925830"	""	"0"	"449.52"	"0"	"1.58"	"BDBM229268"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)CN2CCCC2=O)CC1"	"IC50"	"'='"	"194.0"	"nM"	"6.71"	""	"401007"	"UO_0000065"	"14.93"	"0.28"	"5.13"	"4.89"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4114423"	""	"0"	"431.46"	"0"	"2.38"	"BDBM229237"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CN(C(=O)OCc2ccncc2)C1"	"IC50"	"'='"	"353.0"	"nM"	"6.45"	""	"400976"	"UO_0000065"	"14.95"	"0.28"	"4.07"	"4.64"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4108860"	""	"0"	"460.49"	"0"	"3.00"	"BDBM229241"	"COc1cccc(COC(=O)N2CC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)C2)c1"	"IC50"	"'='"	"423.0"	"nM"	"6.37"	""	"400980"	"UO_0000065"	"13.84"	"0.26"	"3.37"	"4.70"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3912257"	""	"0"	"408.51"	"0"	"3.15"	"BDBM229257"	"CCCCC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)CC1"	"IC50"	"'='"	"70.0"	"nM"	"7.16"	""	"400996"	"UO_0000065"	"17.51"	"0.33"	"4.00"	"6.11"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL2325897"	""	"0"	"378.44"	"0"	"1.72"	"3s"	"N#C[C@@H]1CCN(C(=O)[C@H](NC(=O)c2c[nH]c3ncc(C4CC4)nc23)C2CC2)C1"	"IC50"	"'<'"	"0.3"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2329570"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 30 mins by scintillation counting analysis in presence of [gamma-33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321829"	"1"	"Scientific Literature"	"J. Med. Chem."	"2013"	"None"	""
"CHEMBL2325908"	""	"0"	"301.35"	"0"	"1.04"	"3j"	"C[C@@H](NC(=O)c1c[nH]c2ncc(C3CC3)nc12)C(=O)N(C)C"	"IC50"	"'='"	"231.2"	"nM"	"6.64"	""	""	"UO_0000065"	"22.02"	"0.41"	"5.60"	"7.29"	"False"	"CHEMBL2329570"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 30 mins by scintillation counting analysis in presence of [gamma-33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321829"	"1"	"Scientific Literature"	"J. Med. Chem."	"2013"	"None"	""
"CHEMBL2325907"	""	"0"	"312.42"	"0"	"3.53"	"3i"	"C[C@H](NC(=O)c1c[nH]c2ncc(C3CC3)nc12)C1CCCCC1"	"IC50"	"'='"	"355.2"	"nM"	"6.45"	""	""	"UO_0000065"	"20.64"	"0.38"	"2.92"	"9.13"	"False"	"CHEMBL2329570"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 30 mins by scintillation counting analysis in presence of [gamma-33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2321829"	"1"	"Scientific Literature"	"J. Med. Chem."	"2013"	"None"	""
"CHEMBL3929953"	""	"0"	"558.59"	"1"	"4.39"	"BDBM230129"	"Cc1c(-c2c(F)cc(C(N)=O)c3[nH]c4c(c23)CC[C@H](C(C)(C)O)C4)cccc1-n1c(=O)[nH]c2c(F)cccc2c1=O"	"IC50"	"'>'"	"2000.0"	"nM"	""	""	"402070"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3234886"	""	"0"	"313.36"	"0"	"3.79"	"10"	"NC(=O)c1cc(-c2ccccc2)sc1Nc1cc(F)ccn1"	"IC50"	"'='"	"227.0"	"nM"	"6.64"	""	""	"UO_0000065"	"21.20"	"0.41"	"2.85"	"9.77"	"False"	"CHEMBL3239499"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3232939"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3903692"	""	"0"	"556.57"	"1"	"3.66"	"BDBM228980"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)(F)F)cc3)n2)CC1"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	"400725"	"UO_0000065"	"14.17"	"0.28"	"4.23"	"4.92"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4109662"	""	"0"	"488.53"	"0"	"0.98"	"BDBM229246"	"CS(=O)(=O)c1ccc(Nc2nn(C3(CC#N)CN(C(=O)OC4CCOC4)C3)cc2C(N)=O)cc1"	"IC50"	"'='"	"221.0"	"nM"	"6.66"	""	"400985"	"UO_0000065"	"13.62"	"0.27"	"5.68"	"3.92"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3958861"	""	"0"	"444.47"	"0"	"2.09"	"BDBM229250"	"CC(CO)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CC1"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	"400989"	"UO_0000065"	"18.22"	"0.35"	"6.01"	"5.53"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3895843"	""	"0"	"466.49"	"0"	"3.92"	"BDBM228904"	"COc1cc(F)cc(N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)CC2)c1"	"IC50"	"'='"	"40.0"	"nM"	"7.40"	""	"400651"	"UO_0000065"	"15.86"	"0.30"	"3.48"	"6.77"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3971268"	""	"0"	"450.48"	"0"	"2.57"	"BDBM228917"	"COc1ncc(N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)CC2)cn1"	"IC50"	"'='"	"21.0"	"nM"	"7.68"	""	"400664"	"UO_0000065"	"17.04"	"0.32"	"5.11"	"5.69"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3948102"	""	"0"	"449.49"	"0"	"3.18"	"BDBM228929"	"COc1cncc(N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)CC2)c1"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	"400676"	"UO_0000065"	"17.29"	"0.32"	"4.59"	"6.36"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3938961"	""	"0"	"467.53"	"0"	"3.75"	"BDBM229275"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)c2cc3ccccc3[nH]2)CC1"	"IC50"	"'='"	"176.0"	"nM"	"6.75"	""	"401014"	"UO_0000065"	"14.45"	"0.26"	"3.00"	"5.09"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3901898"	""	"0"	"513.60"	"1"	"3.11"	"BDBM229281"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)c2cccc(N3CCOCC3)c2)CC1"	"IC50"	"'='"	"1049.0"	"nM"	"5.98"	""	"401020"	"UO_0000065"	"11.64"	"0.21"	"2.87"	"4.62"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3982937"	""	"0"	"451.47"	"0"	"1.54"	"BDBM229297"	"Cn1cc(C(=O)N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccnc(F)c4)n3)CC2)cn1"	"IC50"	"'='"	"63.0"	"nM"	"7.20"	""	"401036"	"UO_0000065"	"15.95"	"0.30"	"5.66"	"4.87"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3986274"	""	"0"	"425.47"	"0"	"2.29"	"BDBM229298"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(C(=O)CC2CC2)CC1"	"IC50"	"'='"	"46.0"	"nM"	"7.34"	""	"401037"	"UO_0000065"	"17.25"	"0.32"	"5.05"	"5.65"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3930750"	""	"0"	"371.81"	"0"	"2.73"	"BDBM228724"	"CN(c1nc(Cl)c(C#N)cc1F)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399645"	"UO_0000065"	"27.59"	"0.54"	"7.53"	"12.11"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3903286"	""	"0"	"327.42"	"0"	"1.45"	"BDBM228727"	"CN(C1NC(C#N)=CS1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399648"	"UO_0000065"	"31.33"	"0.61"	"8.81"	"12.23"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3961670"	""	"0"	"295.35"	"0"	"1.46"	"BDBM228684"	"CN(c1ccncn1)[C@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399730"	"UO_0000065"	"31.35"	"0.57"	"7.80"	"12.54"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3981986"	""	"0"	"471.57"	"0"	"3.59"	"BDBM229072"	"CC(=O)Nc1ccc(CN2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)CC2)cc1"	"IC50"	"'='"	"128.0"	"nM"	"6.89"	""	"400808"	"UO_0000065"	"14.62"	"0.27"	"3.30"	"5.34"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3954853"	""	"0"	"450.49"	"0"	"3.91"	"BDBM229083"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(Cc2c(F)cccc2F)CC1"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	"400819"	"UO_0000065"	"17.51"	"0.33"	"3.98"	"7.89"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3931808"	""	"0"	"438.54"	"0"	"3.48"	"BDBM229085"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(CC#Cc2ccccc2)CC1"	"IC50"	"'='"	"747.0"	"nM"	"6.13"	""	"400821"	"UO_0000065"	"13.97"	"0.25"	"2.65"	"6.13"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3926055"	""	"0"	"442.57"	"0"	"4.25"	"BDBM229088"	"Cc1ccc(CN2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccccc4)n3)CC2)cc1C"	"IC50"	"'='"	"453.0"	"nM"	"6.34"	""	"400824"	"UO_0000065"	"14.33"	"0.26"	"2.09"	"6.35"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3944548"	""	"0"	"437.48"	"0"	"2.20"	"BDBM229093"	"Cc1c[nH]c(CN2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccnc(F)c4)n3)CC2)n1"	"IC50"	"'='"	"1180.0"	"nM"	"5.93"	""	"400829"	"UO_0000065"	"13.55"	"0.25"	"3.73"	"4.19"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3943338"	""	"0"	"438.55"	"0"	"4.15"	"BDBM229095"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(CC2CCCCC2)CC1"	"IC50"	"'='"	"211.0"	"nM"	"6.68"	""	"400831"	"UO_0000065"	"15.22"	"0.28"	"2.53"	"6.68"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3901174"	""	"0"	"473.52"	"0"	"2.81"	"BDBM229106"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2cnn3ccccc23)CC1"	"IC50"	"'='"	"503.0"	"nM"	"6.30"	""	"400842"	"UO_0000065"	"13.30"	"0.25"	"3.49"	"4.84"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3949065"	""	"0"	"437.45"	"0"	"3.31"	"BDBM228936"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(c2cc(F)ccn2)CC1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"400683"	"UO_0000065"	"18.79"	"0.35"	"4.91"	"7.28"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3933330"	""	"0"	"437.45"	"0"	"3.31"	"BDBM228946"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(c2cccc(F)n2)CC1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"400693"	"UO_0000065"	"19.20"	"0.36"	"5.09"	"7.44"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3906220"	""	"0"	"456.52"	"0"	"3.75"	"BDBM228955"	"CC(C#N)C1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(C(=O)OC(C)(C)C)CC1"	"IC50"	"'='"	"162.0"	"nM"	"6.79"	""	"400702"	"UO_0000065"	"14.87"	"0.28"	"3.04"	"5.38"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3984652"	""	"0"	"399.43"	"0"	"2.79"	"BDBM228960"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCC2(CC1)OCCO2"	"IC50"	"'='"	"48.0"	"nM"	"7.32"	""	"400707"	"UO_0000065"	"18.32"	"0.34"	"4.53"	"6.35"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3976977"	""	"0"	"449.52"	"0"	"3.24"	"BDBM228970"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(C#N)cc3)n2)CC1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"400715"	"UO_0000065"	"18.29"	"0.34"	"4.98"	"5.48"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3960876"	""	"0"	"468.56"	"0"	"3.42"	"BDBM228974"	"CC(O)c1ccc(Nc2nn(C3(CC#N)CCN(C(=O)OC(C)(C)C)CC3)cc2C(N)=O)cc1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"400719"	"UO_0000065"	"17.55"	"0.33"	"4.80"	"5.61"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3901812"	""	"0"	"466.54"	"0"	"3.57"	"BDBM228975"	"CC(=O)c1ccc(Nc2nn(C3(CC#N)CCN(C(=O)OC(C)(C)C)CC3)cc2C(N)=O)cc1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"400720"	"UO_0000065"	"18.27"	"0.34"	"4.95"	"5.95"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3939638"	""	"0"	"493.49"	"0"	"3.78"	"BDBM228988"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccnc(C(F)(F)F)c3)n2)CC1"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	"400733"	"UO_0000065"	"16.21"	"0.31"	"4.22"	"5.75"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3902563"	""	"0"	"537.62"	"1"	"2.84"	"BDBM228990"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(C(=O)N4CCOCC4)cc3)n2)CC1"	"IC50"	"'='"	"0.7"	"nM"	"9.15"	""	"400735"	"UO_0000065"	"17.03"	"0.32"	"6.31"	"5.88"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3908774"	""	"0"	"443.48"	"0"	"2.90"	"BDBM229000"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3cncc(F)c3)n2)CC1"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	"400745"	"UO_0000065"	"17.58"	"0.33"	"4.90"	"5.60"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3924108"	""	"0"	"516.48"	"1"	"3.52"	"BDBM229010"	"N#CCC1(n2cc(C(N)=O)c(Nc3cccc(-c4cc[nH]n4)c3)n2)CCN(C(=O)OCC(F)(F)F)CC1"	"IC50"	"'='"	"29.0"	"nM"	"7.54"	""	"400755"	"UO_0000065"	"14.59"	"0.28"	"4.02"	"4.86"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3945825"	""	"0"	"531.50"	"1"	"2.92"	"BDBM229012"	"Cn1cc(-c2cncc(Nc3nn(C4(CC#N)CCN(C(=O)OCC(F)(F)F)CC4)cc3C(N)=O)c2)cn1"	"IC50"	"'='"	"71.0"	"nM"	"7.15"	""	"400757"	"UO_0000065"	"13.45"	"0.26"	"4.23"	"4.55"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3965904"	""	"0"	"479.54"	"0"	"2.61"	"BDBM229025"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc4c(c3)CNC4=O)n2)CC1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"400769"	"UO_0000065"	"18.14"	"0.34"	"6.09"	"5.60"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4060201"	""	"0"	"328.38"	"0"	"2.28"	"24"	"O=C(CCCCCCn1cc(-c2ncnc3[nH]ccc23)cn1)NO"	"IC50"	"'='"	"75.0"	"nM"	"7.12"	""	""	"UO_0000065"	"21.70"	"0.41"	"4.84"	"6.55"	"False"	"CHEMBL4031305"	"Inhibition of human JAK2 using poly[Glu:Tyr] as substrate in presence of [gamma-33P]-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028864"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4447631"	""	"0"	"467.59"	"0"	"4.01"	"18e"	"Cc1cnc(Nc2ccc(N3CCC(N(C)CCO)CC3)c(F)c2)nc1-c1cnn(C(C)C)c1"	"IC50"	"'='"	"269.9"	"nM"	"6.57"	""	""	"UO_0000065"	"14.05"	"0.26"	"2.56"	"7.98"	"False"	"CHEMBL4323960"	"Inhibition of JAK2 in human TF-1 cells assessed as reduction in IL-3-induced STAT5 phosphorylation by flow cytometry"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4321837"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"CHEMBL3307972"	""
"CHEMBL3925083"	""	"0"	"377.51"	"0"	"2.42"	"BDBM185701"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)NC2CCC2)CC1"	"IC50"	"'='"	"101.0"	"nM"	"7.00"	""	"370425"	"UO_0000065"	"18.53"	"0.37"	"4.58"	"7.69"	"False"	"CHEMBL3888064"	"JAK Enzymatic Assay: Methods: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK-2 and JAK-3) or the IRS-1 peptide (JAK-1 and Tyk-2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 microliter total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 micromolar for JAK-2 and JAK-3, 40 micromolar for JAK-1 and 7 micromolar for Tyk-2)), 2% DMSO and 1 micromolar peptide substrate (JAKtide for JAK-2 and JAK-3 or IRS-1 peptide for JAK-1 and Tyk-2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 microliter reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK-2, 1 nM JAK-3, 7 nM Tyk2 or 20 nM JAK-1. The assay was run for 240 minutes for JAK-1, 150 minutes for JAK-2, 90 minutes for JAK-3 and 60 minutes for Tyk-2."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886558"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL2062810"	""	"0"	"490.63"	"0"	"4.07"	"36"	"CC(C)S(=O)(=O)c1ccc(-c2cccn3nc(Nc4cccc(N5CCN(C)CC5)c4)nc23)cc1"	"IC50"	"'='"	"1.27"	"nM"	"8.90"	""	""	"UO_0000065"	"18.13"	"0.35"	"4.83"	"10.74"	"True"	"CHEMBL2067611"	"Inhibition of human JAK2 expressed in baculovirus using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate preincubated for 1 hr measured after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2062812"	""	"0"	"402.48"	"0"	"4.03"	"38"	"CN1CCN(c2cccc(Nc3nc4c(-c5ccc(F)cc5)cccn4n3)c2)CC1"	"IC50"	"'='"	"26.0"	"nM"	"7.58"	""	""	"UO_0000065"	"18.85"	"0.35"	"3.56"	"15.58"	"False"	"CHEMBL2067611"	"Inhibition of human JAK2 expressed in baculovirus using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate preincubated for 1 hr measured after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2062811"	""	"0"	"452.48"	"0"	"4.91"	"37"	"CN1CCN(c2cccc(Nc3nc4c(-c5ccc(C(F)(F)F)cc5)cccn4n3)c2)CC1"	"IC50"	"'='"	"476.0"	"nM"	"6.32"	""	""	"UO_0000065"	"13.97"	"0.26"	"1.41"	"12.98"	"False"	"CHEMBL2067179"	"Inhibition of JAK2 in human TF-1 cells using GM-CSF pretreated for 1 hr prior to GM-CSF addition measured after 5 hrs by FRET based GeneBLAzer assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"CHEMBL3307972"	""
"CHEMBL4071806"	""	"0"	"395.48"	"0"	"3.56"	"14"	"CC1(C)[C@H](Nc2c(C(N)=O)cnn3cc(-c4cccc(F)c4)cc23)CC[C@]1(C)N"	"IC50"	"'='"	"22.0"	"nM"	"7.66"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4054822"	"Inhibition of GST-tagged JAK2 (unknown origin) after 3 hrs by Caliper assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4052645"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4077508"	""	"0"	"395.48"	"0"	"3.56"	"15"	"CC1(C)[C@H](Nc2c(C(N)=O)cnn3cc(-c4ccc(F)cc4)cc23)CC[C@]1(C)N"	"IC50"	"'='"	"27.0"	"nM"	"7.57"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4054822"	"Inhibition of GST-tagged JAK2 (unknown origin) after 3 hrs by Caliper assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4052645"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4076823"	""	"0"	"411.94"	"0"	"4.07"	"17"	"CC1(C)[C@H](Nc2c(C(N)=O)cnn3cc(-c4cccc(Cl)c4)cc23)CC[C@]1(C)N"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4054822"	"Inhibition of GST-tagged JAK2 (unknown origin) after 3 hrs by Caliper assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4052645"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4062062"	""	"0"	"411.94"	"0"	"4.07"	"18"	"CC1(C)[C@H](Nc2c(C(N)=O)cnn3cc(-c4ccc(Cl)cc4)cc23)CC[C@]1(C)N"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4054822"	"Inhibition of GST-tagged JAK2 (unknown origin) after 3 hrs by Caliper assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4052645"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4079880"	""	"0"	"396.47"	"0"	"2.95"	"28"	"CC1(C)[C@H](Nc2c(C(N)=O)cnn3cc(-c4ccncc4F)cc23)CC[C@]1(C)N"	"IC50"	"'='"	"70.0"	"nM"	"7.16"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4054822"	"Inhibition of GST-tagged JAK2 (unknown origin) after 3 hrs by Caliper assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4052645"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL3671805"	""	"0"	"392.51"	"0"	"3.12"	"31"	"Cc1ccncc1-c1cc2c(N[C@@H]3CC[C@](C)(N)C3(C)C)c(C(N)=O)cnn2c1"	"IC50"	"'='"	"140.0"	"nM"	"6.85"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4054822"	"Inhibition of GST-tagged JAK2 (unknown origin) after 3 hrs by Caliper assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4052645"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4060444"	""	"0"	"392.51"	"0"	"3.12"	"32"	"Cc1ccc(-c2cc3c(N[C@@H]4CC[C@](C)(N)C4(C)C)c(C(N)=O)cnn3c2)cn1"	"IC50"	"'='"	"22.0"	"nM"	"7.66"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4054822"	"Inhibition of GST-tagged JAK2 (unknown origin) after 3 hrs by Caliper assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4052645"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4080797"	""	"0"	"408.51"	"0"	"2.82"	"35"	"COc1ccc(-c2cc3c(N[C@@H]4CC[C@](C)(N)C4(C)C)c(C(N)=O)cnn3c2)cn1"	"IC50"	"'='"	"15.0"	"nM"	"7.82"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4054822"	"Inhibition of GST-tagged JAK2 (unknown origin) after 3 hrs by Caliper assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4052645"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4096795"	""	"0"	"403.49"	"0"	"2.68"	"38"	"CC1(C)[C@H](Nc2c(C(N)=O)cnn3cc(-c4ccc(C#N)nc4)cc23)CC[C@]1(C)N"	"IC50"	"'='"	"29.0"	"nM"	"7.54"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4054822"	"Inhibition of GST-tagged JAK2 (unknown origin) after 3 hrs by Caliper assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4052645"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL3935745"	""	"0"	"490.63"	"0"	"4.30"	"BDBM99661"	"CN1CCC(c2ccc(Nc3nc4c(NCc5cccc(S(C)(=O)=O)c5)cccn4n3)cc2)CC1"	"IC50"	"'='"	"327.52"	"nM"	"6.49"	""	"216351"	"UO_0000065"	"13.22"	"0.25"	"2.18"	"7.08"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL4435302"	""	"0"	"405.46"	"0"	"1.67"	"9"	"CCNC(=O)c1ccc(Nc2nccc(N3C[C@H]4C[C@@H]3CN4C(=O)CC#N)n2)cc1"	"IC50"	"'>'"	"4216.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4411532"	"Inhibition of human JAK2 using fluorescence labeled peptide as substrate and using ATP at its Km level by microfluidic based mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4411260"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3977017"	""	"0"	"367.84"	"0"	"3.03"	"BDBM198417"	"Clc1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cn1"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	"352495"	"UO_0000065"	"21.44"	"0.41"	"4.86"	"10.51"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4458435"	""	"0"	"389.41"	"0"	"1.79"	"23; PF-06700841"	"Cn1cc(Nc2nccc(N3C[C@H]4CC[C@H](C3)N4C(=O)[C@@H]3CC3(F)F)n2)cn1"	"IC50"	"'='"	"77.0"	"nM"	"7.11"	""	""	"UO_0000065"	"18.27"	"0.35"	"5.32"	"8.98"	"False"	"CHEMBL4411595"	"Inhibition of human JAK2 using fluorescence labeled peptide as substrate and using 1 mM ATP by microfluidic based mobility shift assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4411260"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4524537"	""	"0"	"461.57"	"0"	"4.17"	"7r"	"Cc1cnc(Nc2ccc(N3CCOCC3)cc2)nc1-c1cc2c(o1)CCN(C(=O)C(C)C)C2"	"IC50"	"'='"	"6.4"	"nM"	"8.19"	""	""	"UO_0000065"	"17.75"	"0.33"	"4.02"	"9.79"	"False"	"CHEMBL4341343"	"Inhibition of JAK2 (unknown origin) using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition and measured by 30 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4590082"	""	"0"	"458.52"	"0"	"3.42"	"7j"	"Cc1cnc(Nc2ccc(N3CCOCC3)cc2)nc1-c1cc2c(o1)CCN(C(=O)CC#N)C2"	"IC50"	"'='"	"0.5"	"nM"	"9.30"	""	""	"UO_0000065"	"20.28"	"0.37"	"5.88"	"8.65"	"False"	"CHEMBL4341343"	"Inhibition of JAK2 (unknown origin) using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition and measured by 30 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4440795"	""	"0"	"463.49"	"0"	"3.61"	"7n"	"COc1cc(Nc2ncc(C)c(-c3cc4c(o3)CCN(C(=O)CC#N)C4)n2)cc(OC)c1OC"	"IC50"	"'='"	"141.1"	"nM"	"6.85"	""	""	"UO_0000065"	"14.78"	"0.28"	"3.24"	"5.58"	"False"	"CHEMBL4341349"	"Inhibition of JAK2 in human TF-1 cells assessed as reduction in GM-CSF-induced cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"CHEMBL3307972"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"1"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"275.1"	"nM"	"6.56"	""	""	"UO_0000065"	"21.00"	"0.39"	"5.02"	"7.38"	"False"	"CHEMBL4341349"	"Inhibition of JAK2 in human TF-1 cells assessed as reduction in GM-CSF-induced cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"CHEMBL3307972"	""
"CHEMBL2178800"	""	"0"	"366.81"	"0"	"3.34"	"13e"	"Cc1ccc(Cl)cc1-c1nn(C)cc1NC(=O)c1cnn2cccnc12"	"IC50"	"'='"	"34.5"	"nM"	"7.46"	""	""	"UO_0000065"	"20.34"	"0.39"	"4.12"	"9.68"	"False"	"CHEMBL2186603"	"Inhibition of JAK2 in human TF1 cells assessed as reduction in STAT5 phosphorylation incubated for 30 mins in presence of human recombinant EPO"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176876"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"CHEMBL3307972"	""
"CHEMBL3676063"	""	"0"	"424.48"	"0"	"2.56"	"BDBM127823"	"Cc1ncc(F)cc1C1CCCN1c1ccn2ncc(C(=O)N[C@H]3CC[C@H](O)C3)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258492"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676067"	""	"0"	"438.51"	"0"	"2.81"	"BDBM127827"	"CCc1ncc(F)cc1C1CCCN1c1ccn2ncc(C(=O)N[C@H]3CC[C@H](O)C3)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258496"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676074"	""	"0"	"455.49"	"0"	"1.83"	"BDBM127835"	"O=C(NC1CC1)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)cc(OCC(O)CO)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258503"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676083"	""	"0"	"355.37"	"0"	"1.54"	"BDBM127845"	"CNC(=O)c1cnn2ccc(N3C[C@@H](O)C[C@@H]3c3cccc(F)c3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258513"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL4763801"	""	"0"	"393.49"	"0"	"3.01"	"17e"	"CNC(=O)c1cnc2[nH]ccc2c1NC1CCN(Cc2cccc(OC)c2)CC1"	"IC50"	"'='"	"469.0"	"nM"	"6.33"	""	""	""	"16.08"	"0.30"	"3.32"	"7.69"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL4750605"	""	"0"	"383.88"	"0"	"3.26"	"19b"	"CNC(=O)c1cnc2[nH]ccc2c1NC1CCN(Cc2cccc(Cl)c2)C1"	"IC50"	"'='"	"514.0"	"nM"	"6.29"	""	""	""	"16.38"	"0.32"	"3.03"	"8.61"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL4759320"	""	"0"	"423.95"	"0"	"4.18"	"20b"	"CNC(=O)c1cnc2[nH]ccc2c1NC1CC2CCC(C1)N2Cc1cccc(Cl)c1"	"IC50"	"'='"	"153.0"	"nM"	"6.82"	""	""	""	"16.08"	"0.31"	"2.64"	"9.33"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL4779340"	""	"0"	"407.52"	"0"	"3.40"	"31i"	"CNC(=O)c1cnc2[nH]ccc2c1N[C@@H]1CCN(Cc2ccc(OC)cc2)[C@H](C)C1"	"IC50"	"'='"	"63.2"	"nM"	"7.20"	""	""	""	"17.67"	"0.33"	"3.80"	"8.75"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL4098094"	""	"0"	"338.44"	"0"	"0.76"	"12"	"CCCNS(=O)(=O)N[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"893.0"	"nM"	"6.05"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4082035"	""	"0"	"363.45"	"0"	"0.65"	"15"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)NCCCC#N)C1"	"IC50"	"'='"	"3420.0"	"nM"	"5.47"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4087044"	""	"0"	"353.45"	"0"	"0.88"	"34"	"COCCCS(=O)(=O)N[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"1801.0"	"nM"	"5.74"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4092805"	""	"0"	"309.40"	"0"	"0.86"	"6"	"CCS(=O)(=O)N[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'>'"	"15900.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4075575"	""	"0"	"320.42"	"0"	"1.75"	"17"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](CS(=O)(=O)C2CC2)C1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4087044"	""	"0"	"353.45"	"0"	"0.88"	"34"	"COCCCS(=O)(=O)N[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'>'"	"15348.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3676048"	""	"0"	"443.50"	"0"	"3.49"	"BDBM127807"	"CC(C)(C)[C@@H](CO)NC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258476"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL4789251"	""	"0"	"541.08"	"1"	"4.79"	"18a"	"CSc1nc(Cl)c(C)c(Nc2c[nH]nc2-c2ncc(-c3ccc(OCCCN4CCOCC4)cc3)[nH]2)n1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4711870"	"Inhibition of JAK2 (unknown origin) incubated for 40 mins in presence of ATP by Kinase-glo luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706620"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2021"	"None"	"TIME = 0.6667 hr"
"CHEMBL4101725"	""	"0"	"323.42"	"0"	"1.25"	"26"	"CCCS(=O)(=O)N[C@H]1C[C@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'>'"	"20000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4087961"	""	"0"	"337.45"	"0"	"1.64"	"27"	"CCCCS(=O)(=O)N[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"16100.0"	"nM"	"4.79"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL2035049"	""	"0"	"481.60"	"1"	"5.40"	"14a, 95:5 trans/Cis mixture"	"C1=C/Cn2ccc3ccc(cc32)-c2ccnc(n2)Nc2ccc(OCCN3CCCC3)c(c2)COC/1"	"IC50"	"'='"	"63.0"	"nM"	"7.20"	""	""	"UO_0000065"	"14.95"	"0.27"	"1.80"	"11.17"	"False"	"CHEMBL2040119"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2034857"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2035050"	""	"0"	"495.63"	"1"	"5.71"	"14b, 95:5 trans/Cis mixture"	"Cc1cnc2nc1-c1ccc3ccn(c3c1)C/C=C/COCc1cc(ccc1OCCN1CCCC1)N2"	"IC50"	"'='"	"370.0"	"nM"	"6.43"	""	""	"UO_0000065"	"12.98"	"0.24"	"0.72"	"9.98"	"False"	"CHEMBL2040119"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2034857"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2035055"	""	"0"	"491.66"	"0"	"4.94"	"14g, 95:5 trans/Cis mixture"	"CN1C/C=C/COCc2ccc(s2)-c2ccnc(n2)Nc2ccc(OCCN3CCCC3)c(c2)C1"	"IC50"	"'='"	"90.0"	"nM"	"7.05"	""	""	"UO_0000065"	"14.33"	"0.27"	"2.11"	"11.23"	"False"	"CHEMBL2040119"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2034857"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL4066730"	""	"0"	"348.37"	"0"	"1.90"	"13d"	"N#CCC(=O)Nc1cccc(CNc2c(C(N)=O)cnn3cccc23)c1"	"IC50"	"'='"	"658.0"	"nM"	"6.18"	""	""	"UO_0000065"	"17.74"	"0.32"	"4.28"	"4.93"	"False"	"CHEMBL4047228"	"Inhibition of GST-tagged JAK2 (unknown origin) using fluoresceinated peptide as substrate after 3 hrs by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4043231"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL2105759"	"BARICITINIB"	"4"	"371.43"	"0"	"1.10"	"2"	"CCS(=O)(=O)N1CC(CC#N)(n2cc(-c3ncnc4[nH]ccc34)cn2)C1"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4075575"	""	"0"	"320.42"	"0"	"1.75"	"17"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](CS(=O)(=O)C2CC2)C1"	"IC50"	"'='"	"572.0"	"nM"	"6.24"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4552628"	""	"0"	"425.89"	"0"	"3.66"	"27"	"Cc1sc(C(=O)N[C@@H]2[C@H](N)CCCC2(F)F)cc1-c1cnn2cc(Cl)cnc12"	"IC50"	"'='"	"4400.0"	"nM"	"5.36"	""	""	"UO_0000065"	"12.58"	"0.26"	"1.70"	"6.28"	"False"	"CHEMBL4479735"	"Inhibition of recombinant human GST-tagged cytoplasmic JAK2 (809 to 1153 residues) expressed in baculovirus expression system by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4477252"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2016"	"None"	""
"CHEMBL3665147"	""	"0"	"376.39"	"0"	"3.46"	"BDBM112537"	"FC(F)(F)CN1CCC[C@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.035"	"nM"	"10.46"	""	"233776"	"UO_0000065"	"27.78"	"0.53"	"7.00"	"14.99"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3699492"	""	"0"	"442.50"	"0"	"3.62"	"BDBM147507"	"CC(C)(C)OC(=O)NC1CC[C@H](C#N)C(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)C1"	"IC50"	"'='"	"49.0"	"nM"	"7.31"	""	"285435"	"UO_0000065"	"16.52"	"0.31"	"3.69"	"5.41"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702883"	""	"0"	"415.48"	"0"	"1.80"	"BDBM147582"	"N#C[C@H]1CCCCC1n1cc(C(N)=O)c(Nc2ccc3c(c2)C(O)CS3(=O)=O)n1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"285512"	"UO_0000065"	"20.94"	"0.41"	"6.90"	"5.76"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3655102"	""	"0"	"361.43"	"0"	"0.21"	"BDBM159769"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)N2CC(C#N)C2)C1"	"IC50"	"'='"	"171.0"	"nM"	"6.77"	""	"302579"	"UO_0000065"	"18.72"	"0.37"	"6.56"	"5.73"	"False"	"CHEMBL3707926"	"Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639016"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3655080"	""	"0"	"363.37"	"0"	"1.41"	"8"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)CC(F)(F)F)C1"	"IC50"	"'='"	"4120.0"	"nM"	"5.38"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4103586"	""	"0"	"356.45"	"0"	"2.65"	"20"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](CS(=O)(=O)c2ccccc2)C1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3651062"	""	"0"	"345.36"	"0"	"3.79"	"BDBM47233"	"C=C(C)C(=O)Nc1cccc(-c2ncnc3[nH]cc(-c4ncco4)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"198767"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4091582"	""	"0"	"402.50"	"0"	"3.29"	"21"	"CC1(C)[C@H](Nc2c(C(N)=O)cnn3cc(-c4ccc(C#N)cc4)cc23)CC[C@]1(C)N"	"IC50"	"'='"	"7.3"	"nM"	"8.14"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4054822"	"Inhibition of GST-tagged JAK2 (unknown origin) after 3 hrs by Caliper assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4052645"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4069127"	""	"0"	"408.51"	"0"	"2.82"	"30"	"COc1cc(-c2cc3c(N[C@@H]4CC[C@](C)(N)C4(C)C)c(C(N)=O)cnn3c2)ccn1"	"IC50"	"'='"	"36.0"	"nM"	"7.44"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4054822"	"Inhibition of GST-tagged JAK2 (unknown origin) after 3 hrs by Caliper assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4052645"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL3671132"	""	"0"	"456.50"	"0"	"2.41"	"BDBM127631"	"O=C(NCCN1CCOCC1)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258305"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675926"	""	"0"	"395.44"	"0"	"2.59"	"BDBM127675"	"O=C(NC1CC1)c1cnn2ccc(N3CCCC3c3cc(F)ccc3CO)nc12"	"IC50"	"'='"	"429.0"	"nM"	"6.37"	""	"258349"	"UO_0000065"	"16.10"	"0.30"	"3.78"	"7.69"	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676020"	""	"0"	"430.44"	"0"	"0.70"	"BDBM127776"	"COc1ncc(F)cc1[C@H]1CCCN1c1ccn2ncc(C(=O)NCC(O)CO)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258447"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL2035041"	""	"0"	"379.51"	"0"	"3.45"	"13a, 95:5 trans/Cis mixture"	"CN1C/C=C/COCC2CCCN(C2)c2ccnc(n2)Nc2cccc(c2)C1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL2040119"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2034857"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2035186"	""	"0"	"462.55"	"0"	"4.56"	"14m, 95:5 trans/Cis mixture"	"C1=C/COCc2cc(ccc2OCCN2CCCC2)Nc2nccc(n2)-c2coc(c2)COC/1"	"IC50"	"'='"	"67.0"	"nM"	"7.17"	""	""	"UO_0000065"	"15.51"	"0.29"	"2.61"	"8.76"	"False"	"CHEMBL2040119"	"Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminometric assay"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2034857"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL4067915"	""	"0"	"330.32"	"0"	"1.36"	"20"	"N#C[C@H]1CCOC[C@@H]1n1cc(C(N)=O)c(Nc2ccnc(F)c2)n1"	"IC50"	"'='"	"2.8"	"nM"	"8.55"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4032997"	"Inhibition of GST-tagged recombinant human JAK2 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 as substrate preincubated for 30 mins followed by ATP addition measured after 120 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4071005"	""	"0"	"375.82"	"0"	"2.49"	"28"	"COc1cc(Nc2nn([C@H]3COCC[C@@H]3C#N)cc2C(N)=O)ccc1Cl"	"IC50"	"'='"	"3.9"	"nM"	"8.41"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4032997"	"Inhibition of GST-tagged recombinant human JAK2 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 as substrate preincubated for 30 mins followed by ATP addition measured after 120 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4088262"	""	"0"	"410.41"	"0"	"2.52"	"31"	"COc1ccnc2c(F)cc(Nc3nn([C@H]4COCC[C@@H]4C#N)cc3C(N)=O)cc12"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4032997"	"Inhibition of GST-tagged recombinant human JAK2 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 as substrate preincubated for 30 mins followed by ATP addition measured after 120 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4100288"	""	"0"	"311.35"	"0"	"1.83"	"7; 13"	"N#C[C@H]1CCOC[C@@H]1n1cc(C(N)=O)c(Nc2ccccc2)n1"	"IC50"	"'='"	"209.0"	"nM"	"6.68"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4033007"	"Inhibition of JAK2 in EPO-stimulated human TF1 cells expressing stably integrated beta-lactamase reporter gene under control of STAT5 response elements in interferon regulatory factor 1 gene promoter by fluorescence assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4079092"	""	"0"	"377.41"	"0"	"2.08"	"33"	"Cc1ncnc2ccc(Nc3nn([C@H]4COCC[C@@H]4C#N)cc3C(N)=O)cc12"	"IC50"	"'='"	"1635.0"	"nM"	"5.79"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4033007"	"Inhibition of JAK2 in EPO-stimulated human TF1 cells expressing stably integrated beta-lactamase reporter gene under control of STAT5 response elements in interferon regulatory factor 1 gene promoter by fluorescence assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4077614"	""	"0"	"364.48"	"0"	"1.25"	"39"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)N2CCCCC2)C1"	"IC50"	"'='"	"10200.0"	"nM"	"4.99"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3649630"	""	"0"	"453.50"	"0"	"3.45"	"BDBM130324"	"Cn1ccc2cc(-c3cc(C(N)=O)c4[nH]c5cc(C(=O)N6CCOCC6)ccc5c4n3)ccc21"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"262110"	"UO_0000065"	"19.85"	"0.36"	"5.55"	"8.47"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL494867"	""	"0"	"487.35"	"0"	"2.24"	"17"	"CN(CCO/N=C1C(=C2/C(=O)Nc3cc(Br)ccc32)/Nc2ccccc2/1)CC(O)CO"	"IC50"	"'='"	"551.0"	"nM"	"6.26"	""	""	"UO_0000065"	"12.84"	"0.28"	"4.02"	"5.88"	"False"	"CHEMBL4042012"	"Inhibition of recombinant JAK2 (unknown origin) after 120 mins in presence of [33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4041496"	"1"	"Scientific Literature"	"J Nat Prod"	"2016"	"None"	""
"CHEMBL493883"	""	"0"	"489.80"	"0"	"4.05"	"20"	"Cl.O=C1Nc2cc(Br)ccc2/C1=C1/Nc2ccccc2/C1=N\OCCN1CCCC1"	"IC50"	"'='"	"4410.0"	"nM"	"5.36"	""	""	"UO_0000065"	"11.81"	"0.25"	"1.31"	"8.12"	"False"	"CHEMBL4042012"	"Inhibition of recombinant JAK2 (unknown origin) after 120 mins in presence of [33P]ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4041496"	"1"	"Scientific Literature"	"J Nat Prod"	"2016"	"None"	""
"CHEMBL4085582"	""	"0"	"264.29"	"0"	"2.75"	"6"	"C=CC(=O)Nc1cccc(-c2ncnc3[nH]ccc23)c1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4005719"	"Inhibition of recombinant human GST-tagged cytoplasmic JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by microfluidic assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4004825"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL3234892"	""	"0"	"295.37"	"0"	"3.65"	"4"	"NC(=O)c1cc(-c2ccccc2)sc1Nc1cccnc1"	"IC50"	"'='"	"319.0"	"nM"	"6.50"	""	""	"UO_0000065"	"21.99"	"0.42"	"2.85"	"9.55"	"False"	"CHEMBL3239499"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3232939"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3234890"	""	"0"	"309.39"	"0"	"3.96"	"6"	"Cc1cccc(Nc2sc(-c3ccccc3)cc2C(N)=O)n1"	"IC50"	"'='"	"270.0"	"nM"	"6.57"	""	""	"UO_0000065"	"21.23"	"0.41"	"2.61"	"9.66"	"False"	"CHEMBL3239499"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3232939"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3642371"	""	"0"	"520.66"	"1"	"3.23"	"BDBM99647"	"CN1CCN(c2cccc(Nc3nc4c(NCc5ccccc5N(C)S(C)(=O)=O)cccn4n3)c2)CC1"	"IC50"	"'='"	"66.38"	"nM"	"7.18"	""	"216337"	"UO_0000065"	"13.79"	"0.26"	"3.95"	"7.32"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647766"	""	"0"	"514.47"	"1"	"4.91"	"BDBM147869"	"N#C[C@H]1C[C@H](N[C@H](C2CC2)C(F)(F)F)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"1000.0"	"nM"	"6.00"	""	"285803"	"UO_0000065"	"11.66"	"0.23"	"1.09"	"5.52"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647867"	""	"0"	"468.53"	"0"	"4.16"	"BDBM147979"	"N#C[C@H]1C[C@@H](OC(=O)NC2CCCCC2)CCC1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"164.0"	"nM"	"6.79"	""	"285913"	"UO_0000065"	"14.48"	"0.27"	"2.63"	"5.02"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702913"	""	"0"	"514.61"	"1"	"2.51"	"BDBM147612"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)N3CCC4(CC3)OCCO4)cc2)n1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"285542"	"UO_0000065"	"16.56"	"0.32"	"6.01"	"5.59"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3646844"	""	"0"	"317.35"	"0"	"3.49"	"BDBM130293"	"COc1cccc(-c2cc(C(N)=O)c3[nH]c4cccnc4c3c2)c1"	"IC50"	"'='"	"29.0"	"nM"	"7.54"	""	"262079"	"UO_0000065"	"23.75"	"0.43"	"4.05"	"9.31"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649621"	""	"0"	"534.69"	"1"	"3.14"	"BDBM130315"	"COCCN1CCN(Cc2ccc(-c3cc(C(N)=O)c4[nH]c5cc(N6CCOCC6)ccc5c4n3)s2)CC1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"262101"	"UO_0000065"	"15.38"	"0.30"	"5.08"	"8.23"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL4632980"	""	"0"	"256.31"	"0"	"2.48"	"19"	"Cc1[nH]nc2[nH]c(=O)c(C#N)c(C3CCCCC3)c12"	"IC50"	"'='"	"17000.0"	"nM"	"4.77"	""	""	"UO_0000065"	"18.61"	"0.34"	"2.29"	"5.59"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4648820"	""	"0"	"282.35"	"0"	"2.60"	"42"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3C[C@H]4C[C@@H]3C[C@H]4CC#N)c12"	"IC50"	"'='"	"360.0"	"nM"	"6.44"	""	""	"UO_0000065"	"22.82"	"0.42"	"3.84"	"7.55"	"False"	"CHEMBL4612622"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL3671145"	""	"0"	"415.44"	"0"	"2.85"	"BDBM127644"	"CC(C)(O)CNC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258318"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675963"	""	"0"	"433.42"	"0"	"1.36"	"BDBM127715"	"O=C(NOC[C@@H](O)CO)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258389"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3676061"	""	"0"	"410.45"	"0"	"2.17"	"BDBM127820"	"Cc1ncc(F)cc1C1CCCN1c1ccn2ncc(C(=O)NC3(CO)CC3)c2n1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258489"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3671146"	""	"0"	"413.43"	"0"	"2.56"	"BDBM127645"	"O=C(c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12)N1CC[C@H](O)C1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258319"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675965"	""	"0"	"439.49"	"0"	"3.13"	"BDBM127717"	"COCCOc1ccc(F)cc1[C@H]1CCCN1c1ccn2ncc(C(=O)NC3CC3)c2n1"	"IC50"	"'='"	"472.0"	"nM"	"6.33"	""	"258391"	"UO_0000065"	"14.39"	"0.27"	"3.20"	"7.81"	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL4061128"	""	"0"	"336.36"	"0"	"1.70"	"22"	"N#Cc1ccc(Nc2nn([C@H]3COCC[C@@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"1.2"	"nM"	"8.92"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4032997"	"Inhibition of GST-tagged recombinant human JAK2 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 as substrate preincubated for 30 mins followed by ATP addition measured after 120 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4068357"	""	"0"	"342.45"	"0"	"2.32"	"3"	"C[C@@H]1CCN(C(=O)N2CCCC2)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"123.6"	"nM"	"6.91"	""	""	"UO_0000065"	"20.17"	"0.38"	"4.59"	"10.11"	"False"	"CHEMBL4003453"	"Inhibition of GST tagged human recombinant JAK2 catalytic domain expressed in baculovirus using peptide substrate preincubated for 60 mins followed by substrate addition and measured after 60 mins by microfluidic assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4002590"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL3928932"	""	"0"	"354.41"	"1"	"5.04"	"5"	"CCc1cc(O)ccc1-c1ccc2c(-c3nc4ccccc4[nH]3)n[nH]c2c1"	"IC50"	"'='"	"2.2"	"nM"	"8.66"	""	""	"UO_0000065"	"24.43"	"0.44"	"3.62"	"11.16"	"False"	"CHEMBL4003453"	"Inhibition of GST tagged human recombinant JAK2 catalytic domain expressed in baculovirus using peptide substrate preincubated for 60 mins followed by substrate addition and measured after 60 mins by microfluidic assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4002590"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4104931"	""	"0"	"368.44"	"1"	"5.43"	"8"	"CCCc1cc(O)ccc1-c1ccc2c(-c3nc4ccccc4[nH]3)n[nH]c2c1"	"IC50"	"'='"	"17.3"	"nM"	"7.76"	""	""	"UO_0000065"	"21.07"	"0.38"	"2.33"	"10.00"	"False"	"CHEMBL4003453"	"Inhibition of GST tagged human recombinant JAK2 catalytic domain expressed in baculovirus using peptide substrate preincubated for 60 mins followed by substrate addition and measured after 60 mins by microfluidic assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4002590"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4096219"	""	"0"	"281.31"	"0"	"2.60"	"13"	"CCc1cc(O)ccc1-c1ccc2c(C(N)=O)n[nH]c2c1"	"IC50"	"'='"	"4.2"	"nM"	"8.38"	""	""	"UO_0000065"	"29.78"	"0.54"	"5.78"	"9.11"	"False"	"CHEMBL4003453"	"Inhibition of GST tagged human recombinant JAK2 catalytic domain expressed in baculovirus using peptide substrate preincubated for 60 mins followed by substrate addition and measured after 60 mins by microfluidic assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4002590"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4078165"	""	"0"	"295.34"	"0"	"2.86"	"14"	"CCc1cc(O)ccc1-c1ccc2c(C(=O)NC)n[nH]c2c1"	"IC50"	"'='"	"40.9"	"nM"	"7.39"	""	""	"UO_0000065"	"25.02"	"0.46"	"4.53"	"9.47"	"False"	"CHEMBL4003453"	"Inhibition of GST tagged human recombinant JAK2 catalytic domain expressed in baculovirus using peptide substrate preincubated for 60 mins followed by substrate addition and measured after 60 mins by microfluidic assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4002590"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL3703085"	""	"0"	"386.89"	"0"	"3.17"	"2"	"CN(C)[C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"19.0"	"nM"	"7.72"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4032997"	"Inhibition of GST-tagged recombinant human JAK2 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 as substrate preincubated for 30 mins followed by ATP addition measured after 120 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4076473"	""	"0"	"414.83"	"0"	"3.17"	"32"	"N#C[C@H]1CCOC[C@@H]1n1cc(C(N)=O)c(Nc2cc(F)c3nccc(Cl)c3c2)n1"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4032997"	"Inhibition of GST-tagged recombinant human JAK2 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 as substrate preincubated for 30 mins followed by ATP addition measured after 120 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4089118"	""	"0"	"409.37"	"0"	"2.42"	"21"	"N#C[C@H]1CCOC[C@@H]1n1cc(C(N)=O)c(Nc2ccc([C@H](O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"48.0"	"nM"	"7.32"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4033007"	"Inhibition of JAK2 in EPO-stimulated human TF1 cells expressing stably integrated beta-lactamase reporter gene under control of STAT5 response elements in interferon regulatory factor 1 gene promoter by fluorescence assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL3703085"	""	"0"	"386.89"	"0"	"3.17"	"2"	"CN(C)[C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"692.0"	"nM"	"6.16"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4033007"	"Inhibition of JAK2 in EPO-stimulated human TF1 cells expressing stably integrated beta-lactamase reporter gene under control of STAT5 response elements in interferon regulatory factor 1 gene promoter by fluorescence assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4067915"	""	"0"	"330.32"	"0"	"1.36"	"20"	"N#C[C@H]1CCOC[C@@H]1n1cc(C(N)=O)c(Nc2ccnc(F)c2)n1"	"IC50"	"'='"	"414.0"	"nM"	"6.38"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4033007"	"Inhibition of JAK2 in EPO-stimulated human TF1 cells expressing stably integrated beta-lactamase reporter gene under control of STAT5 response elements in interferon regulatory factor 1 gene promoter by fluorescence assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4072848"	""	"0"	"366.38"	"0"	"1.71"	"24"	"COc1cc(Nc2nn([C@H]3COCC[C@@H]3C#N)cc2C(N)=O)ccc1C#N"	"IC50"	"'='"	"430.0"	"nM"	"6.37"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4033007"	"Inhibition of JAK2 in EPO-stimulated human TF1 cells expressing stably integrated beta-lactamase reporter gene under control of STAT5 response elements in interferon regulatory factor 1 gene promoter by fluorescence assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4064171"	""	"0"	"361.37"	"0"	"1.57"	"26"	"N#Cc1ccc(Nc2nn([C@H]3COCC[C@@H]3C#N)cc2C(N)=O)cc1C#N"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4032997"	"Inhibition of GST-tagged recombinant human JAK2 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 as substrate preincubated for 30 mins followed by ATP addition measured after 120 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4064171"	""	"0"	"361.37"	"0"	"1.57"	"26"	"N#Cc1ccc(Nc2nn([C@H]3COCC[C@@H]3C#N)cc2C(N)=O)cc1C#N"	"IC50"	"'='"	"1192.0"	"nM"	"5.92"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4033007"	"Inhibition of JAK2 in EPO-stimulated human TF1 cells expressing stably integrated beta-lactamase reporter gene under control of STAT5 response elements in interferon regulatory factor 1 gene promoter by fluorescence assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL4066193"	""	"0"	"360.35"	"0"	"1.37"	"30"	"COc1cc(Nc2nn([C@H]3COCC[C@@H]3C#N)cc2C(N)=O)cc(F)n1"	"IC50"	"'='"	"600.0"	"nM"	"6.22"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4033007"	"Inhibition of JAK2 in EPO-stimulated human TF1 cells expressing stably integrated beta-lactamase reporter gene under control of STAT5 response elements in interferon regulatory factor 1 gene promoter by fluorescence assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028908"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL3903790"	""	"0"	"371.45"	"0"	"3.29"	"BDBM198334"	"N#Cc1ccc(CN[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"39.0"	"nM"	"7.41"	""	"352412"	"UO_0000065"	"19.95"	"0.36"	"4.12"	"7.82"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3952151"	""	"0"	"341.42"	"0"	"1.47"	"BDBM198337"	"c1cc2c(ncn3nnc([C@H]4CC[C@@H](NN5CCOCC5)CC4)c23)[nH]1"	"IC50"	"'='"	"400.0"	"nM"	"6.40"	""	"352415"	"UO_0000065"	"18.74"	"0.35"	"4.93"	"7.67"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4447631"	""	"0"	"467.59"	"0"	"4.01"	"18e"	"Cc1cnc(Nc2ccc(N3CCC(N(C)CCO)CC3)c(F)c2)nc1-c1cnn(C(C)C)c1"	"IC50"	"'='"	"0.7"	"nM"	"9.15"	""	""	"UO_0000065"	"19.58"	"0.37"	"5.14"	"11.12"	"False"	"CHEMBL4323930"	"Inhibition of human JAK2 (808 to end residues) using KTFCGTPEYLAP as substrate after 40 mins in presence of [gamma33P]-ATP by scintillation counting based radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4321837"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL3936565"	""	"0"	"434.85"	"0"	"4.66"	"BDBM198354"	"FC(F)(F)c1cc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)ccc1Cl"	"IC50"	"'='"	"32.0"	"nM"	"7.50"	""	"352432"	"UO_0000065"	"17.24"	"0.34"	"2.83"	"12.07"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3116050"	""	"0"	"353.37"	"0"	"2.54"	"19a"	"C[C@H](Nc1nc(Nc2cn(C)cn2)c2cc[nH]c2n1)c1ncc(F)cn1"	"IC50"	"'<'"	"3.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3118240"	"Inhibition of Jak2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112447"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL3963532"	""	"0"	"254.34"	"0"	"3.57"	"BDBM198193"	"Cc1nc(C2CCCCC2)c2c3cc[nH]c3ncn12"	"IC50"	"'='"	"310.0"	"nM"	"6.51"	""	"351815"	"UO_0000065"	"25.59"	"0.47"	"2.94"	"14.16"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3906872"	""	"0"	"376.42"	"0"	"3.12"	"BDBM198206"	"O=C(OCc1ccccc1)N1CCCC(c2nnn3cnc4[nH]ccc4c23)C1"	"IC50"	"'='"	"110.0"	"nM"	"6.96"	""	"352288"	"UO_0000065"	"18.49"	"0.34"	"3.84"	"7.87"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3985597"	""	"0"	"342.40"	"0"	"2.72"	"BDBM198216"	"CC(C)(C)OC(=O)N1CCC(c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"510.0"	"nM"	"6.29"	""	"352298"	"UO_0000065"	"18.38"	"0.34"	"3.57"	"7.12"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3929096"	""	"0"	"324.31"	"0"	"2.35"	"BDBM198217"	"FC(F)(F)CN1CCC(c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"47.0"	"nM"	"7.33"	""	"352299"	"UO_0000065"	"22.60"	"0.44"	"4.98"	"11.80"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3944831"	""	"0"	"332.41"	"0"	"2.99"	"BDBM198224"	"c1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"36.0"	"nM"	"7.44"	""	"352306"	"UO_0000065"	"22.39"	"0.41"	"4.45"	"11.98"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3916915"	""	"0"	"400.41"	"0"	"4.00"	"BDBM198225"	"FC(F)(F)c1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"19.0"	"nM"	"7.72"	""	"352307"	"UO_0000065"	"19.28"	"0.36"	"3.72"	"12.43"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3912192"	""	"0"	"432.48"	"0"	"4.60"	"BDBM198230"	"FC(F)(F)Sc1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"32.0"	"nM"	"7.50"	""	"352312"	"UO_0000065"	"17.33"	"0.34"	"2.89"	"12.07"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3927649"	""	"0"	"411.31"	"0"	"3.75"	"BDBM198233"	"Brc1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"6.1"	"nM"	"8.21"	""	"352315"	"UO_0000065"	"19.97"	"0.43"	"4.46"	"13.23"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3956311"	""	"0"	"392.43"	"0"	"3.91"	"BDBM198249"	"FC(F)(F)C1CCC(N2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)CC1"	"IC50"	"'='"	"600.0"	"nM"	"6.22"	""	"352331"	"UO_0000065"	"15.85"	"0.30"	"2.31"	"10.02"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3975158"	""	"0"	"285.35"	"0"	"2.53"	"BDBM198255"	"COC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"31.0"	"nM"	"7.51"	""	"352337"	"UO_0000065"	"26.31"	"0.49"	"4.98"	"11.03"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3943557"	""	"0"	"257.30"	"0"	"1.62"	"BDBM198276"	"O[C@H]1CC[C@@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"48.0"	"nM"	"7.32"	""	"352355"	"UO_0000065"	"28.44"	"0.53"	"5.70"	"9.25"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3917030"	""	"0"	"340.43"	"0"	"2.21"	"BDBM198284"	"c1cc2c(ncn3nnc([C@H]4CC[C@H](CN5CCOCC5)CC4)c23)[nH]1"	"IC50"	"'='"	"94.0"	"nM"	"7.03"	""	"352362"	"UO_0000065"	"20.64"	"0.38"	"4.82"	"9.85"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3909814"	""	"0"	"364.43"	"0"	"4.13"	"BDBM198293"	"Fc1ccc(NC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"45.0"	"nM"	"7.35"	""	"352371"	"UO_0000065"	"20.16"	"0.37"	"3.22"	"10.36"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3924171"	""	"0"	"444.46"	"1"	"5.20"	"BDBM198297"	"Cc1cc(OC(F)(F)F)ccc1NC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"352375"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3897849"	""	"0"	"385.48"	"0"	"3.89"	"BDBM198301"	"CN(C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1)c1ccc(C#N)cc1"	"IC50"	"'='"	"24.0"	"nM"	"7.62"	""	"352379"	"UO_0000065"	"19.77"	"0.36"	"3.73"	"8.87"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3973486"	""	"0"	"430.43"	"0"	"4.89"	"BDBM198307"	"FC(F)(F)Oc1ccc(NC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"430.0"	"nM"	"6.37"	""	"352385"	"UO_0000065"	"14.79"	"0.28"	"1.48"	"7.95"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3919766"	""	"0"	"389.44"	"0"	"4.00"	"BDBM198309"	"N#Cc1cc(F)ccc1NC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"32.0"	"nM"	"7.50"	""	"352387"	"UO_0000065"	"19.25"	"0.35"	"3.49"	"7.92"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3973017"	""	"0"	"432.43"	"1"	"5.15"	"BDBM198310"	"Fc1ccc(NC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)c(C(F)(F)F)c1"	"IC50"	"'='"	"360.0"	"nM"	"6.44"	""	"352388"	"UO_0000065"	"14.90"	"0.28"	"1.29"	"9.09"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3970109"	""	"0"	"349.44"	"0"	"2.87"	"BDBM198320"	"N#CC1CCN(C2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)CC1"	"IC50"	"'='"	"190.0"	"nM"	"6.72"	""	"352398"	"UO_0000065"	"19.23"	"0.35"	"3.85"	"7.82"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3975250"	""	"0"	"375.41"	"0"	"3.75"	"BDBM198322"	"N#Cc1ccc(NC2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)c(F)c1"	"IC50"	"'='"	"78.0"	"nM"	"7.11"	""	"352400"	"UO_0000065"	"18.93"	"0.35"	"3.36"	"7.51"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3968423"	""	"0"	"371.45"	"0"	"3.29"	"BDBM198333"	"N#Cc1ccc(CN[C@H]2CC[C@@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"490.0"	"nM"	"6.31"	""	"352411"	"UO_0000065"	"16.99"	"0.31"	"3.02"	"6.66"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4071850"	""	"0"	"324.41"	"0"	"0.37"	"11"	"CCNS(=O)(=O)N[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"1390.0"	"nM"	"5.86"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3974989"	""	"0"	"418.40"	"0"	"4.14"	"BDBM198356"	"Fc1cc(C(F)(F)F)ccc1CN1CCC(c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	"352434"	"UO_0000065"	"18.40"	"0.35"	"3.56"	"12.40"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3962232"	""	"0"	"392.46"	"0"	"2.36"	"BDBM198367"	"OCCOc1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"710.0"	"nM"	"6.15"	""	"352445"	"UO_0000065"	"15.67"	"0.29"	"3.79"	"6.71"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3954454"	""	"0"	"394.91"	"0"	"4.32"	"BDBM198376"	"Clc1ccc(CNC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"31.0"	"nM"	"7.51"	""	"352454"	"UO_0000065"	"19.01"	"0.37"	"3.19"	"10.59"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4454640"	""	"0"	"415.46"	"0"	"2.06"	"14c"	"N#Cc1ccc(N2CCC(Nc3cc(Nc4cnccn4)ncc3C(N)=O)CC2)nc1"	"IC50"	"'='"	"4.1"	"nM"	"8.39"	""	""	"UO_0000065"	"20.19"	"0.37"	"6.33"	"5.75"	"False"	"CHEMBL4429528"	"Inhibition of human JAK2 assessed as reduction in phosphorylation of Biotin-Lyn-Substrate-2 after 1 hr in presence of ATP by ELISA"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4428070"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2016"	"None"	""
"CHEMBL3699500"	""	"0"	"439.44"	"0"	"1.95"	"BDBM147517"	"N#C[C@H]1C[C@H](O)CCC1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)F)cc2)n1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"285447"	"UO_0000065"	"19.39"	"0.39"	"6.57"	"5.64"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3694583"	""	"0"	"368.82"	"0"	"4.26"	"BDBM125904"	"Clc1cnc2nc1NCc1cccc(c1)OCCOc1cccc(c1)N2"	"IC50"	"'='"	"8.3"	"nM"	"8.08"	""	"255677"	"UO_0000065"	"21.91"	"0.42"	"3.82"	"11.83"	"False"	"CHEMBL3707544"	"In Vitro Kinase Assay: One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Biochemistry 1999, 269, 94-104. The catalytic domains of human JAK1 (a.a. 837-1142), JAK2 (a.a. 828-1132) and JAK3 (a.a. 781-1124) with an N-terminal His tag were expressed using baculovirus in insect cells and purified. The catalytic activity of JAK1, JAK2 or JAK3 was assayed by measuring the phosphorylation of a biotinylated peptide. The phosphorylated peptide was detected by homogenous time resolved fluorescence (HTRF). IC50s of compounds were measured for each kinase in the reactions that contain the enzyme, ATP and 500 nM peptide in 50 mM Tris (pH 7.8) buffer with 100 mM NaCl, 5 mM DTT, and 0.1 mg/mL (0.01%) BSA. The ATP concentration in the reactions was 90 uM for JAK1, 30 uM for JAK2 and 3 uM for JAK3. Reactions were carried out at room temperature for 1 hr and then stopped with 20 uL 45 mM EDTA."	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639093"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3652371"	""	"0"	"453.61"	"0"	"3.77"	"BDBM113182"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CC[C@@H](c3ccccc3)C2)CC1"	"IC50"	"'='"	"40.7"	"nM"	"7.39"	""	"234625"	"UO_0000065"	"16.29"	"0.32"	"3.62"	"8.99"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3975634"	""	"0"	"452.51"	"0"	"4.75"	"BDBM139540"	"CN[C@H]1CC2OC([C@H]1OC)n1c3ccccc3c3c4c(c5c6ccccc6n2c5c31)C(O)=NC4"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"273892"	"UO_0000065"	"20.46"	"0.37"	"4.51"	"12.69"	"False"	"CHEMBL3707840"	"Kinase Inhibition Assay: The compound of Example 39, 2-(1H-indol-5-ylamino)-6-(2,4-difluorophenylsulfonyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one, was subjected to a kinase inhibition assay for the kinases. Compounds were tested in 5 dose IC50 mode with 10-fold serial dilution starting at 10 μM. Staurosporine, a known protein kinase inhibitor, was tested in 5-dose IC50 mode with 3-fold serial dilution starting at 20 μM. Reactions were carried out in 10 μM ATP. The results are shown in Table 5. The results show that the compound of Example 39 is a kinase inhibitor highly selective for the kinase Plk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639034"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3646831"	""	"0"	"465.51"	"1"	"5.84"	"BDBM130277"	"COc1cccc(-c2cc(C(N)=O)c3[nH]c4cc(NC(=O)OCc5ccccc5)ccc4c3c2)c1"	"IC50"	"'='"	"290.0"	"nM"	"6.54"	""	"262063"	"UO_0000065"	"14.04"	"0.26"	"0.70"	"6.14"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3703503"	""	"0"	"310.36"	"0"	"2.87"	"BDBM153147"	"CCOC(=O)c1c[nH]c2ncnc(-c3ccc(N(C)C)cc3)c12"	"IC50"	"'='"	"90.0"	"nM"	"7.05"	""	"294095"	"UO_0000065"	"22.70"	"0.42"	"4.18"	"9.91"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642366"	""	"0"	"506.63"	"1"	"3.05"	"BDBM99642"	"C[C@@H](O)CN1CCN(c2cccc(Nc3nc4c(-c5ccc(S(C)(=O)=O)cc5)cccn4n3)c2)CC1"	"IC50"	"'='"	"1.13"	"nM"	"8.95"	""	"216332"	"UO_0000065"	"17.66"	"0.34"	"5.90"	"8.68"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3335694"	""	"0"	"388.46"	"0"	"0.83"	"BDBM112581"	"CS(=O)(=O)N1CCC[C@H](Nc2nc(N)ncc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.0713"	"nM"	"10.15"	""	"233818"	"UO_0000065"	"26.12"	"0.51"	"9.32"	"7.11"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3665168"	""	"0"	"414.54"	"0"	"2.88"	"BDBM112561"	"CC(C)CS(=O)(=O)N1CCC[C@H](Nc2ncccc2-c2cnc3cc[nH]c3n2)C1"	"IC50"	"'='"	"0.1915"	"nM"	"9.72"	""	"233799"	"UO_0000065"	"23.44"	"0.46"	"6.84"	"9.36"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647736"	""	"0"	"514.49"	"1"	"1.93"	"BDBM147839"	"N#C[C@H]1CC(NCC(=O)O)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"285773"	"UO_0000065"	"17.49"	"0.35"	"7.07"	"4.99"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3665150"	""	"0"	"442.59"	"0"	"3.58"	"BDBM112540"	"Cc1ccc(-c2cnc3[nH]ccc3n2)c(NC2CCCN(S(=O)(=O)CC(C)(C)C)C2)n1"	"IC50"	"'='"	"0.1338"	"nM"	"9.87"	""	"233779"	"UO_0000065"	"22.31"	"0.43"	"6.29"	"9.51"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652284"	""	"0"	"406.56"	"0"	"1.71"	"BDBM113093"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCC(N)CC2)CC1"	"IC50"	"'='"	"97.5"	"nM"	"7.01"	""	"234537"	"UO_0000065"	"17.24"	"0.34"	"5.30"	"6.48"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3651013"	""	"0"	"381.39"	"0"	"2.01"	"BDBM153189"	"C=C(C)C(=O)Nc1cc(-c2ncnc3[nH]cc(C(=O)OCC)c23)cn(C)c1=O"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294137"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL191003"	"JNJ-7706621"	"0"	"394.36"	"0"	"1.22"	"1; JNJ7706621"	"Nc1nc(Nc2ccc(S(N)(=O)=O)cc2)nn1C(=O)c1c(F)cccc1F"	"IC50"	"'='"	"11050.0"	"nM"	"4.96"	""	""	"UO_0000065"	"12.57"	"0.25"	"3.74"	"3.40"	"False"	"CHEMBL4359667"	"Inhibition of full length human C-terminal FLAG-tagged JAK2 V617F mutant (1 to 1132 residues) autophosphorylation expressed in HEK293T cells incubated in buffer with compound for 1 hr followed by treatment with enzyme and [gamma32P]-ATP for 15 mins by immunoprecipitation assay based autoradiography"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4354882"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL3961357"	""	"0"	"375.41"	"0"	"3.00"	"BDBM198425"	"N#Cc1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cc1F"	"IC50"	"'='"	"33.0"	"nM"	"7.48"	""	"352503"	"UO_0000065"	"19.93"	"0.36"	"4.48"	"8.71"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3980369"	""	"0"	"375.44"	"0"	"2.08"	"BDBM198444"	"NC(=O)c1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"170.0"	"nM"	"6.77"	""	"352522"	"UO_0000065"	"18.03"	"0.33"	"4.69"	"6.43"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4437650"	""	"0"	"364.21"	"0"	"1.25"	"10k"	"N#CCC(=O)N1CCC(n2nc(Br)c3c(N)ncnc32)CC1"	"IC50"	"'='"	"182.0"	"nM"	"6.74"	""	""	"UO_0000065"	"18.51"	"0.42"	"5.49"	"5.93"	"False"	"CHEMBL4402146"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-biotin as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4400567"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4590588"	""	"0"	"432.49"	"0"	"2.21"	"11e"	"C=CC(=O)Nc1ccc(Cn2nc(-c3cc(C(C)(C)O)n(C)n3)c3c(N)ncnc32)cc1"	"IC50"	"'='"	"437.1"	"nM"	"6.36"	""	""	"UO_0000065"	"14.70"	"0.27"	"4.15"	"4.65"	"False"	"CHEMBL4402146"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-biotin as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4400567"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL3699514"	""	"0"	"310.36"	"0"	"2.38"	"BDBM147532"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2cccnc2)n1"	"IC50"	"'='"	"36.0"	"nM"	"7.44"	""	"285462"	"UO_0000065"	"23.98"	"0.44"	"5.06"	"6.79"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3699465"	""	"0"	"367.41"	"0"	"2.33"	"BDBM147480"	"N#CC1CCC2(CC1n1cc(C(N)=O)c(Nc3ccccc3)n1)OCCO2"	"IC50"	"'='"	"47.0"	"nM"	"7.33"	""	"285405"	"UO_0000065"	"19.94"	"0.37"	"5.00"	"6.36"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3234875"	""	"0"	"377.39"	"0"	"4.98"	"22"	"Cc1cccc(Nc2sc(-c3ccc(C(F)(F)F)cc3)cc2C(N)=O)n1"	"IC50"	"'='"	"380.0"	"nM"	"6.42"	""	""	"UO_0000065"	"17.01"	"0.34"	"1.44"	"9.44"	"False"	"CHEMBL3239499"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3232939"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3647852"	""	"0"	"350.38"	"0"	"1.82"	"BDBM147962"	"N#Cc1ccc(Nc2nn([C@H]3CC[C@H](O)C[C@@H]3C#N)cc2C(N)=O)cc1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"285896"	"UO_0000065"	"24.32"	"0.45"	"6.70"	"6.06"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703072"	""	"0"	"430.46"	"0"	"3.27"	"BDBM147784"	"N#C[C@H]1C[C@@H](N2CCC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(OC(F)F)cc2)n1"	"IC50"	"'='"	"31.0"	"nM"	"7.51"	""	"285723"	"UO_0000065"	"17.44"	"0.33"	"4.24"	"6.88"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4071255"	""	"0"	"407.52"	"0"	"3.43"	"10"	"COc1ccccc1-c1cc2c(N[C@@H]3CC[C@](C)(N)C3(C)C)c(C(N)=O)cnn2c1"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4054822"	"Inhibition of GST-tagged JAK2 (unknown origin) after 3 hrs by Caliper assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4052645"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4083798"	""	"0"	"402.50"	"0"	"3.29"	"19"	"CC1(C)[C@H](Nc2c(C(N)=O)cnn3cc(-c4ccccc4C#N)cc23)CC[C@]1(C)N"	"IC50"	"'='"	"25.0"	"nM"	"7.60"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4054822"	"Inhibition of GST-tagged JAK2 (unknown origin) after 3 hrs by Caliper assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4052645"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL3671804"	""	"0"	"378.48"	"0"	"2.81"	"22"	"CC1(C)[C@H](Nc2c(C(N)=O)cnn3cc(-c4cccnc4)cc23)CC[C@]1(C)N"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4054822"	"Inhibition of GST-tagged JAK2 (unknown origin) after 3 hrs by Caliper assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4052645"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4070136"	""	"0"	"436.56"	"0"	"3.60"	"37"	"CC(C)Oc1ccc(-c2cc3c(N[C@@H]4CC[C@](C)(N)C4(C)C)c(C(N)=O)cnn3c2)cn1"	"IC50"	"'='"	"20.0"	"nM"	"7.70"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4054822"	"Inhibition of GST-tagged JAK2 (unknown origin) after 3 hrs by Caliper assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4052645"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4112271"	""	"0"	"441.99"	"0"	"4.10"	"BDBM147938"	"CC1(C)C[N+](C)(C2CC[C@H](n3cc(C(N)=O)c(Nc4ccc(Cl)cc4)n3)[C@@H](C#N)C2)C1"	"IC50"	"'='"	"34.0"	"nM"	"7.47"	""	"285872"	"UO_0000065"	"16.90"	"0.33"	"3.37"	"7.72"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3675923"	""	"0"	"505.55"	"1"	"1.75"	"BDBM127672"	"NS(=O)(=O)N1CCC(NC(=O)c2cnn3ccc(N4CCCC4c4cc(F)ccc4F)nc23)CC1"	"IC50"	"'='"	"195.0"	"nM"	"6.71"	""	"258346"	"UO_0000065"	"13.27"	"0.26"	"4.96"	"5.33"	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675933"	""	"0"	"492.55"	"0"	"2.41"	"BDBM127684"	"CC(C)(CNS(C)(=O)=O)NC(=O)c1cnn2ccc(N3CCCC3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258358"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675941"	""	"0"	"373.36"	"0"	"2.64"	"BDBM127692"	"CONC(=O)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258366"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3675962"	""	"0"	"494.57"	"0"	"2.81"	"BDBM127714"	"O=C(NC1CC1)c1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3OCCN3CCOCC3)nc12"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"258388"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3705391"	"Inhibition Assay: Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 μM ATP, 10 μM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 μL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210)."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638907"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649634"	""	"0"	"419.44"	"0"	"2.56"	"BDBM130328"	"Cc1noc(C)c1-c1cc(C(N)=O)c2[nH]c3cc(C(=O)N4CCOCC4)ccc3c2n1"	"IC50"	"'='"	"146.0"	"nM"	"6.84"	""	"262114"	"UO_0000065"	"16.30"	"0.30"	"4.28"	"5.37"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3649651"	""	"0"	"470.53"	"0"	"3.26"	"BDBM130346"	"CN(C)C(=O)c1ccc(-c2cc(C(N)=O)c3[nH]c4cc(C(=O)N5CCOCC5)ccc4c3c2)cc1"	"IC50"	"'='"	"286.0"	"nM"	"6.54"	""	"262132"	"UO_0000065"	"13.91"	"0.26"	"3.28"	"6.02"	"False"	"CHEMBL3706008"	"Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM Beta-Glycerolphosphate, 0.015% Brij35 and 4 mM DTT). The reaction was initiated by the combination of JAK2 with substrates and test compounds. The reaction was incubated at room temperature for 60 min. and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assays is ATP, 30 uM; JAK2 fluorescent peptide, 1.5 uM; JAK2, 1 nM; and DMSO, 1.6%."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638719"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL4569850"	""	"0"	"378.23"	"0"	"1.32"	"10m"	"N#CCC(=O)N1CCC(Cn2nc(Br)c3c(N)ncnc32)CC1"	"IC50"	"'='"	"1162.8"	"nM"	"5.93"	""	""	"UO_0000065"	"15.69"	"0.35"	"4.61"	"5.22"	"False"	"CHEMBL4402146"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-biotin as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4400567"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL3979242"	""	"0"	"440.48"	"0"	"3.19"	"BDBM237793"	"CC1(COC(=O)N2CC[C@@H](C#N)[C@H](n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)C2)CC1"	"IC50"	"'='"	"69.0"	"nM"	"7.16"	""	"414897"	"UO_0000065"	"16.26"	"0.31"	"3.97"	"5.67"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL2178804"	""	"0"	"402.25"	"0"	"3.27"	"7j"	"Cn1cc(NC(=O)c2cnn3ccc(N)nc23)c(-c2cc(Cl)ccc2Cl)n1"	"IC50"	"'='"	"7.4"	"nM"	"8.13"	""	""	"UO_0000065"	"20.21"	"0.41"	"4.86"	"7.88"	"False"	"CHEMBL2186603"	"Inhibition of JAK2 in human TF1 cells assessed as reduction in STAT5 phosphorylation incubated for 30 mins in presence of human recombinant EPO"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176876"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"CHEMBL3307972"	""
"CHEMBL2178803"	""	"0"	"361.41"	"0"	"2.58"	"7i"	"Cc1ccc(C)c(-c2nn(C)cc2NC(=O)c2cnn3ccc(N)nc23)c1"	"IC50"	"'='"	"40.4"	"nM"	"7.39"	""	""	"UO_0000065"	"20.46"	"0.37"	"4.81"	"7.17"	"False"	"CHEMBL2186603"	"Inhibition of JAK2 in human TF1 cells assessed as reduction in STAT5 phosphorylation incubated for 30 mins in presence of human recombinant EPO"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176876"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"CHEMBL3307972"	""
"CHEMBL2178802"	""	"0"	"347.38"	"0"	"2.27"	"7h"	"Cc1ccccc1-c1nn(C)cc1NC(=O)c1cnn2ccc(N)nc12"	"IC50"	"'='"	"68.6"	"nM"	"7.16"	""	""	"UO_0000065"	"20.62"	"0.38"	"4.89"	"6.95"	"False"	"CHEMBL2186603"	"Inhibition of JAK2 in human TF1 cells assessed as reduction in STAT5 phosphorylation incubated for 30 mins in presence of human recombinant EPO"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176876"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"CHEMBL3307972"	""
"CHEMBL2178799"	""	"0"	"387.23"	"0"	"3.69"	"14i"	"Cn1cc(NC(=O)c2cnn3cccnc23)c(-c2cc(Cl)ccc2Cl)n1"	"IC50"	"'='"	"42.3"	"nM"	"7.37"	""	""	"UO_0000065"	"19.04"	"0.39"	"3.68"	"9.56"	"False"	"CHEMBL2186603"	"Inhibition of JAK2 in human TF1 cells assessed as reduction in STAT5 phosphorylation incubated for 30 mins in presence of human recombinant EPO"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176876"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"CHEMBL3307972"	""
"CHEMBL2178255"	""	"0"	"353.77"	"0"	"2.61"	"7d"	"Nc1ccn2ncc(C(=O)Nc3c[nH]nc3-c3cccc(Cl)c3)c2n1"	"IC50"	"'='"	"205.0"	"nM"	"6.69"	""	""	"UO_0000065"	"18.91"	"0.37"	"4.08"	"5.87"	"False"	"CHEMBL2186598"	"Inhibition of JAK2 V617F mutant in human SET2 cells assessed as reduction in STAT5 phosphorylation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2176876"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL3952555"	""	"0"	"345.41"	"0"	"2.62"	"BDBM228721"	"CN(c1ncnc2ccccc12)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399641"	"UO_0000065"	"29.70"	"0.54"	"7.64"	"13.90"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4109631"	""	"0"	"476.51"	"0"	"3.63"	"BDBM237757"	"N#C[C@@H]1CN(C(=O)OCCc2ccccc2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"823.0"	"nM"	"6.08"	""	"414861"	"UO_0000065"	"12.77"	"0.24"	"2.45"	"4.82"	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4110420"	""	"0"	"430.44"	"0"	"2.03"	"BDBM237775"	"COCCOC(=O)N1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@H](C#N)C1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"414879"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888749"	"Biochemical HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 μL of 1.11× enzyme and 1.11× substrate in 1× assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 μL of 10×ATP in 1× assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at ambient temperature for 120 minutes. At the end of the incubation, 20 μL of 2× stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction. Plates were shaken and centrifuged and then incubated 60 minutes at ambient temperature and then read on a Perkin Elmer Envision (λex=337 nm, λem=665 and 615 nm, TRF delay time=20 μs). HTRF signal=10,000*665 nm reading/615 nm reading."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886818"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL2062798"	""	"0"	"394.46"	"0"	"3.55"	"23"	"COc1cccc(Nc2nc3c(-c4ccc(S(C)(=O)=O)cc4)cccn3n2)c1"	"IC50"	"'='"	"1.4"	"nM"	"8.85"	""	""	"UO_0000065"	"22.45"	"0.43"	"5.30"	"10.34"	"False"	"CHEMBL2067611"	"Inhibition of human JAK2 expressed in baculovirus using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate preincubated for 1 hr measured after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2062802"	""	"0"	"449.54"	"0"	"3.38"	"27"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4cccc(N5CCOCC5)c4)nc23)cc1"	"IC50"	"'='"	"0.8"	"nM"	"9.10"	""	""	"UO_0000065"	"20.24"	"0.39"	"5.72"	"10.24"	"False"	"CHEMBL2067611"	"Inhibition of human JAK2 expressed in baculovirus using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate preincubated for 1 hr measured after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL4761365"	""	"0"	"411.94"	"0"	"4.04"	"38b"	"CNC(=O)c1cnc2[nH]ccc2c1N[C@@H]1CCN(Cc2ccc(Cl)cc2)[C@H](C)C1"	"IC50"	"'='"	"760.0"	"nM"	"6.12"	""	""	""	"14.85"	"0.29"	"2.08"	"8.38"	"False"	"CHEMBL4713349"	"Inhibition of JAK2 pathway in human TF-1 cells assessed as decrease in IL3-induced STAT5 phosphorylation preincubated for 1 hr followed by IL-3 stimulation and measured after 20 mins by immunoassay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.333 hr"
"CHEMBL3922934"	""	"0"	"503.40"	"1"	"4.13"	"BDBM228871"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(Br)cc3)n2)CC1"	"IC50"	"'='"	"23.0"	"nM"	"7.64"	""	"400618"	"UO_0000065"	"15.17"	"0.33"	"3.51"	"6.05"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL2062806"	""	"0"	"476.61"	"0"	"3.29"	"31"	"CN1CCN(Cc2cccc(Nc3nc4c(-c5ccc(S(C)(=O)=O)cc5)cccn4n3)c2)CC1"	"IC50"	"'='"	"3.1"	"nM"	"8.51"	""	""	"UO_0000065"	"17.85"	"0.34"	"5.22"	"10.27"	"True"	"CHEMBL2067611"	"Inhibition of human JAK2 expressed in baculovirus using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate preincubated for 1 hr measured after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL2062807"	""	"0"	"511.63"	"1"	"2.77"	"32"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4cccc(CN5CCS(=O)(=O)CC5)c4)nc23)cc1"	"IC50"	"'='"	"0.64"	"nM"	"9.19"	""	""	"UO_0000065"	"17.97"	"0.36"	"6.42"	"8.08"	"False"	"CHEMBL2067611"	"Inhibition of human JAK2 expressed in baculovirus using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate preincubated for 1 hr measured after 20 mins by time resolved fluorescence assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2062471"	"1"	"Scientific Literature"	"J. Med. Chem."	"2012"	"None"	""
"CHEMBL3746067"	""	"0"	"371.87"	"0"	"3.70"	"15"	"COc1ccc(-c2nc3c(NCC4CCNCC4)c(Cl)cnc3[nH]2)cc1"	"IC50"	"'='"	"1450.0"	"nM"	"5.84"	""	""	"UO_0000065"	"15.70"	"0.31"	"2.14"	"7.80"	"False"	"CHEMBL3751000"	"Inhibition of N-terminal GST-fused recombinant JAK2 (831 to 1132 residues) (unknown origin) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 as substrate by microfluidic capillary electrophoresis method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3745697"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL3941105"	""	"0"	"435.47"	"0"	"1.95"	"BDBM229124"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(Cc2cccnn2)CC1"	"IC50"	"'='"	"145.0"	"nM"	"6.84"	""	"400860"	"UO_0000065"	"15.70"	"0.29"	"4.89"	"4.93"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3905579"	""	"0"	"469.40"	"0"	"2.66"	"BDBM229174"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccnc(F)c3)n2)CCN(C(=O)OCC(F)(F)F)CC1"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	"400911"	"UO_0000065"	"17.25"	"0.34"	"5.44"	"5.82"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3915170"	""	"0"	"465.51"	"0"	"3.61"	"BDBM229133"	"Cc1cnc(F)c(CN2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)CC2)c1"	"IC50"	"'='"	"22.0"	"nM"	"7.66"	""	"400869"	"UO_0000065"	"16.45"	"0.31"	"4.05"	"6.79"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3935250"	""	"0"	"451.48"	"0"	"3.30"	"BDBM229137"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(Cc2ccc(F)cn2)CC1"	"IC50"	"'='"	"73.0"	"nM"	"7.14"	""	"400873"	"UO_0000065"	"15.81"	"0.30"	"3.84"	"6.32"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3944980"	""	"0"	"388.42"	"0"	"2.54"	"BDBM229163"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(CCF)CC1"	"IC50"	"'='"	"59.0"	"nM"	"7.23"	""	"400899"	"UO_0000065"	"18.61"	"0.35"	"4.69"	"7.23"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3952618"	""	"0"	"450.54"	"0"	"3.90"	"BDBM229204"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)CCN(C(=O)OC2CCCCC2)CC1"	"IC50"	"'='"	"318.0"	"nM"	"6.50"	""	"400941"	"UO_0000065"	"14.42"	"0.27"	"2.60"	"5.15"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4116008"	"CERDULATINIB"	"2"	"445.55"	"0"	"1.37"	"91; PRT-062070"	"CCS(=O)(=O)N1CCN(c2ccc(Nc3ncc(C(N)=O)c(NC4CC4)n3)cc2)CC1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	""	"UO_0000065"	"18.45"	"0.36"	"6.85"	"6.16"	"False"	"CHEMBL4272394"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4270539"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4293619"	""	"0"	"308.35"	"0"	"2.15"	"10"	"NC(=O)c1cnc2c(NC3CC3)cc(Nc3ccccc3)nn12"	"IC50"	"'>'"	"2000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4251837"	"Inhibition of JAK2 JH2 domain (unknown origin)"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4251544"	"1"	"Scientific Literature"	"MedChemComm"	"2017"	"None"	""
"CHEMBL4441479"	""	"0"	"468.52"	"0"	"4.37"	"5"	"COc1nn(C)cc1Nc1ncc(C)c(-c2c[nH]c3c(NC(=O)c4cccnc4C)cccc23)n1"	"IC50"	"'='"	"2200.0"	"nM"	"5.66"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4406243"	"Inhibition of recombinant human N-terminal GST-tagged JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-labeled GEEPLYWSFPAKKK-NH2 peptide as substrate after 10 mins in presence of 5 mM ATP by caliper mobility shift assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402602"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL3589169"	""	"0"	"446.94"	"0"	"4.13"	"6"	"CN1CCN(C(=O)c2ccc3[nH]c4c(C(N)=O)cc(-c5ccc(Cl)cc5)cc4c3c2)CC1"	"IC50"	"'='"	"1.2"	"nM"	"8.92"	""	""	"UO_0000065"	"19.96"	"0.38"	"4.79"	"10.82"	"True"	"CHEMBL3592849"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3589178"	""	"0"	"443.50"	"0"	"4.46"	"15"	"COc1cccc(-c2cc(C(N)=O)c3[nH]c4cc(NC(=O)C5CCOCC5)ccc4c3c2)c1"	"IC50"	"'='"	"100.0"	"nM"	"7.00"	""	""	"UO_0000065"	"15.78"	"0.29"	"2.54"	"6.58"	"False"	"CHEMBL3592855"	"Inhibition of JAK2 in human SET2 cells assessed as inhibition of cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3689514"	""	"0"	"324.39"	"0"	"1.69"	"BDBM109863"	"CC1CN(C(=O)CC#N)C12CCCN(c1ncnc3[nH]ccc13)C2"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"230593"	"UO_0000065"	"27.74"	"0.51"	"7.31"	"10.12"	"False"	"CHEMBL3705639"	"Inhibition Assay: In the kinase reactions, fused proteins (6His tag-fused hJAK2 kinase domain (aa808-end)) which were coexpressed in Sf21 cells and purified by Ni2+/NTA agarose were used."	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638515"	"37"	"BindingDB Database"	""	"2013"	"CHEMBL4106362"	""
"CHEMBL4107883"	""	"0"	"363.43"	"0"	"2.25"	"BDBM198560"	"N#C[C@H]1CCN(C(=O)[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C1"	"IC50"	"'='"	"330.0"	"nM"	"6.48"	""	"352638"	"UO_0000065"	"17.83"	"0.33"	"4.23"	"6.29"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3954792"	""	"0"	"439.56"	"0"	"3.48"	"BDBM198540"	"CC(C)(C)OC(=O)N1CC[C@H](NC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C1"	"IC50"	"'='"	"340.0"	"nM"	"6.47"	""	"352618"	"UO_0000065"	"14.72"	"0.28"	"2.99"	"6.44"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3897648"	""	"0"	"284.37"	"0"	"2.19"	"BDBM198604"	"CN(C)[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"210.0"	"nM"	"6.68"	""	"352682"	"UO_0000065"	"23.48"	"0.43"	"4.49"	"10.75"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3946758"	""	"0"	"320.35"	"0"	"2.49"	"BDBM198606"	"FC(F)CN[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"29.0"	"nM"	"7.54"	""	"352684"	"UO_0000065"	"23.53"	"0.45"	"5.05"	"10.63"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3937456"	""	"0"	"294.36"	"0"	"3.04"	"BDBM198647"	"CC(C#N)[C@H]1CC[C@@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"340.0"	"nM"	"6.47"	""	"352725"	"UO_0000065"	"21.97"	"0.40"	"3.43"	"7.83"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL388978"	"STAUROSPORINE"	"0"	"466.54"	"0"	"4.35"	"Staurosporine"	"CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4c(c5c6ccccc6n2c5c31)C(=O)NC4"	"IC50"	"'='"	"0.189"	"nM"	"9.72"	""	""	"UO_0000065"	"20.84"	"0.38"	"5.37"	"14.00"	"False"	"CHEMBL4328459"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4325871"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2019"	"None"	""
"CHEMBL3589327"	""	"0"	"518.06"	"1"	"4.32"	"19"	"CN1CCN(c2ccc3c(c2)[nH]c2c(C(N)=O)cc(-c4ccc(CN5CCOCC5)c(Cl)c4)cc23)CC1"	"IC50"	"'='"	"5.2"	"nM"	"8.28"	""	""	"UO_0000065"	"15.99"	"0.31"	"3.96"	"10.64"	"False"	"CHEMBL3592849"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3589174"	""	"0"	"399.45"	"0"	"3.56"	"11"	"NC(=O)c1cc(-c2ccccc2)cc2c1[nH]c1cc(C(=O)N3CCOCC3)ccc12"	"IC50"	"'='"	"7.4"	"nM"	"8.13"	""	""	"UO_0000065"	"20.35"	"0.37"	"4.57"	"9.20"	"False"	"CHEMBL3592849"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3589172"	""	"0"	"413.48"	"0"	"3.48"	"9"	"NC(=O)c1cc(Cc2ccccc2)cc2c1[nH]c1ccc(C(=O)N3CCOCC3)cc12"	"IC50"	"'='"	"17.0"	"nM"	"7.77"	""	""	"UO_0000065"	"18.79"	"0.34"	"4.29"	"8.79"	"False"	"CHEMBL3592849"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3588791"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL4435170"	"DEUCRAVACITINIB"	"3"	"425.47"	"0"	"1.73"	"11; BMS-986165"	"[2H]C([2H])([2H])NC(=O)c1nnc(NC(=O)C2CC2)cc1Nc1cccc(-c2ncn(C)n2)c1OC"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4377393"	"Inhibition of JAK2 in human whole blood assessed as decrease in TPO-induced STAT5 phosphorylation in platelets"	"A"	"BAO_0000221"	"tissue-based format"	"Homo sapiens"	"CHEMBL3638178"	"Blood"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4376812"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL3917783"	""	"0"	"403.88"	"0"	"4.00"	"BDBM198438"	"N#C/C(=C\N1CCC(c2nnn3cnc4[nH]ccc4c23)CC1)c1ccc(Cl)cc1"	"IC50"	"'='"	"370.0"	"nM"	"6.43"	""	"352516"	"UO_0000065"	"15.93"	"0.30"	"2.43"	"7.49"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3979388"	""	"0"	"339.43"	"0"	"2.44"	"BDBM198443"	"c1cc2c(ncn3nnc(C4CCN(Cc5cscn5)CC4)c23)[nH]1"	"IC50"	"'='"	"110.0"	"nM"	"6.96"	""	"352521"	"UO_0000065"	"20.50"	"0.40"	"4.52"	"9.28"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3900738"	""	"0"	"425.42"	"0"	"3.88"	"BDBM198446"	"N#Cc1cc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)ccc1C(F)(F)F"	"IC50"	"'='"	"290.0"	"nM"	"6.54"	""	"352524"	"UO_0000065"	"15.37"	"0.29"	"2.66"	"7.61"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3946824"	""	"0"	"405.89"	"0"	"4.52"	"BDBM198450"	"N#Cc1ccc(NC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1Cl"	"IC50"	"'='"	"90.0"	"nM"	"7.05"	""	"352528"	"UO_0000065"	"17.36"	"0.33"	"2.53"	"7.44"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3969516"	""	"0"	"396.46"	"0"	"3.73"	"BDBM198465"	"N#Cc1ccc(NC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1C#N"	"IC50"	"'='"	"45.0"	"nM"	"7.35"	""	"352543"	"UO_0000065"	"18.53"	"0.33"	"3.62"	"6.20"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3965307"	""	"0"	"404.52"	"0"	"3.37"	"BDBM198471"	"OCCN(Cc1ccccc1)C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"36.0"	"nM"	"7.44"	""	"352549"	"UO_0000065"	"18.40"	"0.34"	"4.07"	"9.04"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4114175"	""	"0"	"439.56"	"0"	"3.48"	"BDBM198502"	"CC(C)(C)OC(=O)N[C@@H]1CCN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C1"	"IC50"	"'='"	"170.0"	"nM"	"6.77"	""	"352580"	"UO_0000065"	"15.40"	"0.29"	"3.29"	"6.74"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3947422"	""	"0"	"439.56"	"0"	"3.48"	"BDBM198510"	"CC(C)(C)OC(=O)N[C@H]1CCN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C1"	"IC50"	"'='"	"260.0"	"nM"	"6.58"	""	"352588"	"UO_0000065"	"14.98"	"0.28"	"3.11"	"6.56"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3902428"	""	"0"	"383.50"	"0"	"1.49"	"BDBM198518"	"OCCN1CCN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)CC1"	"IC50"	"'='"	"200.0"	"nM"	"6.70"	""	"352596"	"UO_0000065"	"17.47"	"0.33"	"5.21"	"7.83"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3980992"	""	"0"	"342.45"	"0"	"2.46"	"BDBM198528"	"COCCN(C)C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"58.0"	"nM"	"7.24"	""	"352606"	"UO_0000065"	"21.13"	"0.40"	"4.78"	"10.14"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3917056"	""	"0"	"490.46"	"0"	"3.58"	"BDBM198550"	"O=C(NCC(O)(c1ccc(F)cc1)C(F)(F)F)[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"110.0"	"nM"	"6.96"	""	"352628"	"UO_0000065"	"14.19"	"0.27"	"3.38"	"6.43"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3931368"	""	"0"	"270.34"	"0"	"1.85"	"BDBM198605"	"CN[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"110.0"	"nM"	"6.96"	""	"352683"	"UO_0000065"	"25.74"	"0.48"	"5.11"	"9.81"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3938593"	""	"0"	"327.39"	"0"	"2.83"	"BDBM198646"	"CCOC(=O)CC1CCC(c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"44.0"	"nM"	"7.36"	""	"352724"	"UO_0000065"	"22.47"	"0.42"	"4.53"	"8.64"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3981130"	""	"0"	"346.39"	"0"	"2.83"	"BDBM198542"	"FC1(F)CN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C1"	"IC50"	"'='"	"52.0"	"nM"	"7.28"	""	"352620"	"UO_0000065"	"21.03"	"0.40"	"4.45"	"11.73"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3923030"	""	"0"	"395.39"	"0"	"1.90"	"BDBM198590"	"O=C(CN[C@H]1CC[C@@H](c2nnn3cnc4[nH]ccc4c23)CC1)NCC(F)(F)F"	"IC50"	"'='"	"560.0"	"nM"	"6.25"	""	"352668"	"UO_0000065"	"15.81"	"0.30"	"4.35"	"6.25"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3904571"	""	"0"	"376.42"	"0"	"2.15"	"BDBM198615"	"N#CCC(=O)N(CC#N)C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	"352693"	"UO_0000065"	"20.95"	"0.38"	"5.74"	"6.22"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3980246"	""	"0"	"377.45"	"0"	"2.78"	"BDBM198616"	"N#CCC(=O)N(C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1)C1CC1"	"IC50"	"'='"	"32.0"	"nM"	"7.50"	""	"352694"	"UO_0000065"	"19.86"	"0.37"	"4.71"	"7.28"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL1231124"	"AZD-1480"	"2"	"348.77"	"0"	"3.01"	"AZD-1480"	"Cc1cc(Nc2nc(N[C@@H](C)c3ncc(F)cn3)ncc2Cl)[nH]n1"	"IC50"	"'<'"	"3.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL1656588"	"Inhibition of JAK2 using Km ATP concentration"	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1649076"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL4640249"	""	"0"	"382.83"	"0"	"4.91"	"16k"	"CC(Oc1cc(-c2ccc3nccn3c2)cnc1N)c1cc(F)ccc1Cl"	"IC50"	"'='"	"51.0"	"nM"	"7.29"	""	""	"UO_0000065"	"19.05"	"0.37"	"2.38"	"11.14"	"False"	"CHEMBL4628503"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4627317"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL4541296"	""	"0"	"305.30"	"0"	"1.79"	"B39; 4"	"O=C(Nc1ccc2[nH]ncc2c1)c1ccccc1-n1cnnn1"	"IC50"	"'='"	"2380.0"	"nM"	"5.62"	""	""	"UO_0000065"	"18.42"	"0.33"	"3.83"	"5.55"	"False"	"CHEMBL4481929"	"Inhibition of JAK2 (unknown origin) after 1 hr FRET-based Z'-Lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480435"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4569041"	""	"0"	"280.33"	"0"	"3.25"	"25"	"CCNc1ccccc1C(=O)Nc1ccc2[nH]ncc2c1"	"IC50"	"'='"	"3960.0"	"nM"	"5.40"	""	""	"UO_0000065"	"19.27"	"0.35"	"2.15"	"7.74"	"False"	"CHEMBL4481929"	"Inhibition of JAK2 (unknown origin) after 1 hr FRET-based Z'-Lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480435"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4475579"	""	"0"	"281.32"	"0"	"2.22"	"50"	"Cc1nn(CCCCC#N)nc1-c1ncnc2[nH]ccc12"	"IC50"	"'='"	"63.6"	"nM"	"7.20"	""	""	"UO_0000065"	"25.58"	"0.47"	"4.98"	"7.49"	"False"	"CHEMBL4429697"	"Inhibition of recombinant human C-terminal 6His-tagged JAK2 (808 to end amino acids) expressed in Sf21 cells measured after 1 hr in presence of ATP by TR-FRET assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4428074"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2016"	"CHEMBL4106362"	""
"CHEMBL4518995"	""	"0"	"282.35"	"0"	"2.72"	"56"	"Cc1nn(CC2CCCC2)nc1-c1ncnc2[nH]ccc12"	"IC50"	"'='"	"71.8"	"nM"	"7.14"	""	""	"UO_0000065"	"25.30"	"0.46"	"4.42"	"9.88"	"False"	"CHEMBL4429697"	"Inhibition of recombinant human C-terminal 6His-tagged JAK2 (808 to end amino acids) expressed in Sf21 cells measured after 1 hr in presence of ATP by TR-FRET assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf21"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4428074"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2016"	"CHEMBL4106362"	""
"CHEMBL4470355"	""	"0"	"429.49"	"0"	"2.37"	"14e"	"Cc1cncc(Nc2cc(NC3CCN(c4ccc(C#N)cn4)CC3)c(C(N)=O)cn2)n1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	""	"UO_0000065"	"19.55"	"0.36"	"6.03"	"5.76"	"False"	"CHEMBL4429528"	"Inhibition of human JAK2 assessed as reduction in phosphorylation of Biotin-Lyn-Substrate-2 after 1 hr in presence of ATP by ELISA"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4428070"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2016"	"None"	""
"CHEMBL4514375"	""	"0"	"319.33"	"0"	"1.85"	"7"	"O=C(Nc1ccc2[nH]ncc2c1)c1ccccc1Cn1cnnn1"	"IC50"	"'='"	"3540.0"	"nM"	"5.45"	""	""	"UO_0000065"	"17.07"	"0.31"	"3.60"	"5.38"	"False"	"CHEMBL4481929"	"Inhibition of JAK2 (unknown origin) after 1 hr FRET-based Z'-Lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480435"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4585646"	""	"0"	"252.28"	"0"	"2.40"	"30a"	"Nc1n[nH]c2ccc(NC(=O)c3ccccc3)cc12"	"IC50"	"'='"	"2780.0"	"nM"	"5.56"	""	""	"UO_0000065"	"22.02"	"0.40"	"3.16"	"6.63"	"False"	"CHEMBL4481929"	"Inhibition of JAK2 (unknown origin) after 1 hr FRET-based Z'-Lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480435"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4514766"	""	"0"	"252.28"	"0"	"2.40"	"35a"	"Nc1n[nH]c2ccc(C(=O)Nc3ccccc3)cc12"	"IC50"	"'='"	"3230.0"	"nM"	"5.49"	""	""	"UO_0000065"	"21.76"	"0.39"	"3.09"	"6.55"	"False"	"CHEMBL4481929"	"Inhibition of JAK2 (unknown origin) after 1 hr FRET-based Z'-Lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480435"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4540569"	""	"0"	"286.72"	"0"	"3.05"	"35b"	"Nc1n[nH]c2ccc(C(=O)Nc3ccccc3Cl)cc12"	"IC50"	"'='"	"126.0"	"nM"	"6.90"	""	""	"UO_0000065"	"24.06"	"0.47"	"3.85"	"8.23"	"False"	"CHEMBL4481929"	"Inhibition of JAK2 (unknown origin) after 1 hr FRET-based Z'-Lyte assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480435"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4544007"	""	"0"	"442.91"	"0"	"4.33"	"2"	"N#CC[C@H]([C@H]1CCN(c2cccc(Cl)c2C#N)C1)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"2400.0"	"nM"	"5.62"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4406243"	"Inhibition of recombinant human N-terminal GST-tagged JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-labeled GEEPLYWSFPAKKK-NH2 peptide as substrate after 10 mins in presence of 5 mM ATP by caliper mobility shift assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402602"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4449567"	""	"0"	"484.61"	"0"	"3.95"	"15"	"Cc1cnc(Nc2cccnc2C)nc1-c1c[nH]c2c(NC(=O)[C@@H](C)N3CCN(C)CC3)cccc12"	"IC50"	"'>'"	"30000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4406243"	"Inhibition of recombinant human N-terminal GST-tagged JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-labeled GEEPLYWSFPAKKK-NH2 peptide as substrate after 10 mins in presence of 5 mM ATP by caliper mobility shift assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402602"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4541637"	""	"0"	"507.57"	"1"	"2.82"	"19"	"COc1nn(C)cc1Nc1ncc(F)c(-c2c[nH]c3c(NC(=O)[C@@H](C)N4CCN(C)CC4)cccc23)n1"	"IC50"	"'='"	"6600.0"	"nM"	"5.18"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4406243"	"Inhibition of recombinant human N-terminal GST-tagged JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-labeled GEEPLYWSFPAKKK-NH2 peptide as substrate after 10 mins in presence of 5 mM ATP by caliper mobility shift assay"	"A"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402602"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4115335"	""	"0"	"427.96"	"0"	"3.85"	"BDBM147937"	"CC[N+]1(C2CC[C@H](n3cc(C(N)=O)c(Nc4ccc(Cl)cc4)n3)[C@@H](C#N)C2)CCC1"	"IC50"	"'='"	"28.0"	"nM"	"7.55"	""	"285871"	"UO_0000065"	"17.65"	"0.34"	"3.70"	"7.81"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703488"	""	"0"	"365.31"	"0"	"3.74"	"BDBM153132"	"CCOC(=O)c1c[nH]c2ncnc(-c3cccc(OCC(F)(F)F)c3)c12"	"IC50"	"'='"	"73.0"	"nM"	"7.14"	""	"294080"	"UO_0000065"	"19.54"	"0.37"	"3.40"	"9.26"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3621515"	""	"0"	"483.57"	"0"	"3.74"	"25"	"CC(=O)Nc1cccc(-c2ccc(C(N)=O)c3[nH]c4cc(C(=O)N5CCN(C)CC5)ccc4c23)c1C"	"IC50"	"'='"	"212.0"	"nM"	"6.67"	""	""	"UO_0000065"	"13.80"	"0.25"	"2.93"	"5.98"	"False"	"CHEMBL3627422"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621099"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3589166"	""	"0"	"429.48"	"0"	"3.57"	"36"	"COc1cccc(-c2cc(C(N)=O)c3[nH]c4ccc(C(=O)N5CCOCC5)cc4c3c2)c1"	"IC50"	"'='"	"2.8"	"nM"	"8.55"	""	""	"UO_0000065"	"19.91"	"0.37"	"4.98"	"8.76"	"False"	"CHEMBL3627422"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621099"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3622196"	""	"0"	"429.48"	"0"	"3.57"	"38"	"COc1ccc(-c2cc(C(N)=O)c3[nH]c4ccc(C(=O)N5CCOCC5)cc4c3c2)cc1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	""	"UO_0000065"	"20.25"	"0.37"	"5.13"	"8.91"	"False"	"CHEMBL3627422"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3621099"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2015"	"None"	""
"CHEMBL3976626"	""	"0"	"607.65"	"1"	"3.36"	"382"	"CC(C)NCc1cc(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)nc(C(F)(F)F)n1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3912283"	""	"0"	"567.65"	"1"	"4.31"	"122"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(-c4nccs4)c(F)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3955118"	""	"0"	"611.69"	"2"	"5.41"	"134"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)c3ccc(-c4ccc5cccnc5c4)c(F)c3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3986198"	""	"0"	"498.64"	"0"	"3.85"	"147"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CC3CCC(C2)N3C(=O)C2CCCCC2)C1"	"IC50"	"'<='"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3965587"	""	"0"	"566.49"	"1"	"4.27"	"159"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3cscc3Br)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3939938"	""	"0"	"547.57"	"1"	"4.04"	"164"	"N#CCC1(n2cc(-c3ncnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3ccccc3OC(F)F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3902174"	""	"0"	"552.66"	"1"	"3.88"	"242, diastereomer 1"	"CC1CC(N2CC(CC#N)(n3cc(-c4ncnc5[nH]ccc45)cn3)C2)CCN1Cc1ccc(N(C)C)c(C#N)c1F"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL1650951"	""	"0"	"526.52"	"1"	"3.17"	"2; NIBR3049"	"CC(C)(O)C(=O)N1CCN(c2ccc(C(F)(F)F)c(C3=C(c4c[nH]c5ccccc45)C(=O)NC3=O)c2)CC1"	"IC50"	"'='"	"578.0"	"nM"	"6.24"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4124183"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate in presence of 10 uM [gamma33P]ATP by radiometric method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4118225"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4128181"	""	"0"	"428.50"	"0"	"4.67"	"23; FM-381"	"CN(C)C(=O)C(C#N)=Cc1ccc(-c2nc3cnc4[nH]ccc4c3n2C2CCCCC2)o1"	"IC50"	"'='"	"3460.0"	"nM"	"5.46"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4124184"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate in presence of 200 uM [gamma33P]ATP by radiometric method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4118225"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL1287853"	"FEDRATINIB"	"4"	"524.69"	"1"	"4.82"	"TG101348"	"Cc1cnc(Nc2ccc(OCCN3CCCC3)cc2)nc1Nc1cccc(S(=O)(=O)NC(C)(C)C)c1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"16.24"	"0.31"	"3.70"	"7.86"	"True"	"CHEMBL3877189"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3875233"	"1"	"Scientific Literature"	"Nat Rev Drug Discov"	"2017"	"None"	""
"CHEMBL3970498"	""	"0"	"526.55"	"1"	"3.81"	"265"	"N#CCC1(n2ccc(-c3ncnc4[nH]ccc34)c2)CN(C2CCN(C(=O)c3c(F)cc(C#N)cc3F)CC2)C1"	"IC50"	"'>'"	"50.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3976508"	""	"0"	"567.55"	"1"	"4.60"	"331"	"N#CCC1(n2cc(-c3c(F)cnc4[nH]ccc34)cn2)CN(C2CCN(C(=O)Nc3ccncc3C(F)(F)F)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3971619"	""	"0"	"540.58"	"1"	"4.13"	"346"	"N#CCC1(n2ccc(-c3ncnc4[nH]ccc34)c2)CN(C2CCN(C(=O)c3nc(C(F)(F)F)cs3)CC2)C1"	"IC50"	"'>'"	"10.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3880335"	"Inhibition of human N-terminal His-tagged JAK2 catalytic domain (828 to 1132 residues) expressed in baculovirus infected insect cells assessed as decrease in phosphorylation of biotinylated peptide substrate after 1 hr in presence of 1 mM ATP by HTRF method"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3879909"	"38"	"Patent Bioactivity Data"	""	"2014"	"None"	""
"CHEMBL3645037"	""	"0"	"573.64"	"2"	"5.00"	"BDBM99804"	"CCOc1ccc(C(F)(F)F)cc1-c1cccn2nc(Nc3ccc4c(c3)CCN(CCS(C)(=O)=O)CC4)nc12"	"IC50"	"'='"	"159.91"	"nM"	"6.80"	""	"216477"	"UO_0000065"	"11.85"	"0.23"	"1.80"	"7.65"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3764637"	""	"0"	"300.37"	"0"	"1.92"	"9"	"CC(C)C(C)n1cc(-c2ccn(C)n2)c2[nH]nc(N)c2c1=O"	"IC50"	"'='"	"310.0"	"nM"	"6.51"	""	""	"UO_0000065"	"21.67"	"0.40"	"4.59"	"6.89"	"False"	"CHEMBL3766653"	"Inhibition of JAK2 (unknown origin) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent substrate phosphorylation after 45 mins by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3763089"	"1"	"Scientific Literature"	"J. Med. Chem."	"2016"	"None"	""
"CHEMBL3702986"	""	"0"	"428.97"	"0"	"4.34"	"BDBM147696"	"CN([C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@@H](C#N)C1)C(C)(C)C"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	"285630"	"UO_0000065"	"18.17"	"0.35"	"3.46"	"7.80"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645096"	""	"0"	"522.64"	"2"	"2.02"	"BDBM99870"	"CN1CCN(c2cncc(Nc3nc4c(NCc5ccccc5N(C)S(C)(=O)=O)cccn4n3)n2)CC1"	"IC50"	"'='"	"6499.0"	"nM"	"5.19"	""	"216538"	"UO_0000065"	"9.92"	"0.19"	"3.17"	"4.19"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3903970"	""	"0"	"581.07"	"2"	"5.59"	"BDBM230083"	"Cc1c(-c2c(Cl)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)c2cccc(C)c2n(C)c1=O"	"IC50"	"'='"	"350.0"	"nM"	"6.46"	""	"402015"	"UO_0000065"	"11.11"	"0.21"	"0.87"	"5.24"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3936249"	""	"0"	"585.04"	"2"	"5.42"	"BDBM230090"	"Cc1c(-c2c(Cl)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)c2cccc(F)c2n(C)c1=O"	"IC50"	"'='"	"1900.0"	"nM"	"5.72"	""	"402023"	"UO_0000065"	"9.78"	"0.19"	"0.30"	"4.65"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3907348"	""	"0"	"554.55"	"1"	"4.89"	"BDBM230097"	"Cc1c(-c2c(F)cc(C(N)=O)c3[nH]c4cc(C(C)(C)O)ccc4c23)cccc1-n1c(=O)[nH]c2c(F)cccc2c1=O"	"IC50"	"'='"	"1200.0"	"nM"	"5.92"	""	"402031"	"UO_0000065"	"10.68"	"0.20"	"1.03"	"4.42"	"False"	"CHEMBL3888437"	"Jak2 Tyrosine Kinase Assay: The assays were performed in V-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substrates (fluoresceinated peptide and ATP) and test compounds in assay buffer (100 mM HEPES pH 7.4, 10 mM MgCl2, 25 mM beta-glycerolphosphate, 0.015% Brij 35 surfactant and 4 mM DTT). The reaction was initiated by the combination of Jak2 tyrosine kinase with substrates and test compounds. The reaction mixture was incubated at room temperature for 60 minutes and terminated by adding 45 μL of 35 mM EDTA to each sample."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886711"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3120986"	""	"0"	"457.92"	"0"	"3.42"	"6"	"Cl.Cn1c(-c2cn([C@H]3CCNC[C@@H]3F)nn2)nc(-c2ccc(F)cc2)c1-c1ccncc1"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3363474"	"Inhibition of JAK2 (unknown origin) by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352554"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3314278"	""	"0"	"484.49"	"0"	"4.06"	"22"	"CCOC(=O)Cn1cc(-c2ccc(-c3nc(-c4ccc(F)cc4)c(-c4cc[nH]c(=O)c4)[nH]3)cc2)nn1"	"IC50"	"'='"	"352.0"	"nM"	"6.45"	""	""	"UO_0000065"	"13.32"	"0.24"	"2.39"	"5.44"	"False"	"CHEMBL3363474"	"Inhibition of JAK2 (unknown origin) by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352554"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL4108070"	""	"0"	"420.50"	"0"	"2.78"	"BDBM228641"	"CN(c1ccc(C(=O)Nc2nccs2)cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"75.0"	"nM"	"7.12"	""	"399538"	"UO_0000065"	"16.94"	"0.32"	"4.34"	"6.92"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3893327"	""	"0"	"333.40"	"0"	"2.33"	"BDBM228735"	"CCN(c1ccc(C#N)cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399662"	"UO_0000065"	"30.77"	"0.56"	"7.93"	"12.11"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3330126"	""	"0"	"397.74"	"0"	"3.37"	"29"	"NC(=O)c1cc(-c2ccnc(N)n2)[nH]c1-c1cc(OC(F)(F)F)ccc1Cl"	"IC50"	"'='"	"24.0"	"nM"	"7.62"	""	""	"UO_0000065"	"19.16"	"0.39"	"4.25"	"6.35"	"False"	"CHEMBL3374493"	"Inhibition of recombinant human JAK2 (808-1132 residues) using LPLDKDYYVVREPGQ as substrate by radiometric assay in presence of [33P]-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330103"	""	"0"	"327.78"	"0"	"2.78"	"5"	"Cc1ccc(Cl)c(-c2[nH]c(-c3ccnc(N)n3)cc2C(N)=O)c1"	"IC50"	"'='"	"187.0"	"nM"	"6.73"	""	""	"UO_0000065"	"20.53"	"0.40"	"3.95"	"6.08"	"False"	"CHEMBL3374493"	"Inhibition of recombinant human JAK2 (808-1132 residues) using LPLDKDYYVVREPGQ as substrate by radiometric assay in presence of [33P]-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3330122"	""	"0"	"348.19"	"0"	"3.13"	"25"	"NC(=O)c1cc(-c2ccnc(N)n2)[nH]c1-c1cc(Cl)ccc1Cl"	"IC50"	"'='"	"700.0"	"nM"	"6.16"	""	""	"UO_0000065"	"17.68"	"0.37"	"3.02"	"5.56"	"False"	"CHEMBL3374497"	"Inhibition of JAK2 V617F mutant in human SET2 cells"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL2105759"	"BARICITINIB"	"4"	"371.43"	"0"	"1.10"	"6"	"CCS(=O)(=O)N1CC(CC#N)(n2cc(-c3ncnc4[nH]ccc34)cn2)C1"	"IC50"	"'='"	"6.6"	"nM"	"8.18"	""	""	"UO_0000065"	"22.02"	"0.43"	"7.08"	"6.79"	"False"	"CHEMBL3299201"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3297690"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"1"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"1377.0"	"nM"	"5.86"	""	""	"UO_0000065"	"18.76"	"0.35"	"4.32"	"6.59"	"False"	"CHEMBL3299216"	"Inhibition of JAK2 homodimer in human monocytes assessed as inhibition of GM-CSF-induced STAT-5 phosphorylation preincubated for 60 mins followed by GM-CSF addition measured after 8 to 20 mins by FACS analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3297690"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL3301607"	"FILGOTINIB"	"4"	"425.51"	"0"	"1.98"	"8"	"O=C(Nc1nc2cccc(-c3ccc(CN4CCS(=O)(=O)CC4)cc3)n2n1)C1CC1"	"IC50"	"'='"	"13200.0"	"nM"	"4.88"	""	""	"UO_0000065"	"11.47"	"0.22"	"2.90"	"5.05"	"False"	"CHEMBL3299209"	"Inhibition of JAK2 homodimer in human CD34+ cells spiked into human whole blood assessed as inhibition of EPO-induced STAT-5 phosphorylation preincubated for 45 mins followed by EPO addition measured after 15 mins by FACS analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"CHEMBL3638178"	"Blood"	"CD34+ cell"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3297690"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL4249872"	""	"0"	"410.48"	"0"	"1.34"	"9b"	"C=CC(=O)N1CCCC(Cn2nc(-c3cnn(CCOC)c3)c3c(N)ncnc32)C1"	"IC50"	"'='"	"1420.6"	"nM"	"5.85"	""	""	"UO_0000065"	"14.25"	"0.27"	"4.51"	"5.00"	"False"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4242842"	""	"0"	"381.44"	"0"	"1.11"	"9h"	"COCCn1cc(-c2nn(CC3CCCN(C#N)C3)c3ncnc(N)c23)cn1"	"IC50"	"'='"	"1397.6"	"nM"	"5.86"	""	""	"UO_0000065"	"15.35"	"0.29"	"4.74"	"4.73"	"False"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4237788"	""	"0"	"423.48"	"0"	"1.07"	"10d"	"COCCn1cc(-c2nn(CC3CCN(C(=O)CC#N)CC3)c3ncnc(N)c23)cn1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4249310"	""	"0"	"338.38"	"0"	"0.77"	"11a"	"C=CC(=O)N1CCC(n2nc(-c3cnn(C)c3)c3c(N)ncnc32)C1"	"IC50"	"'='"	"499.0"	"nM"	"6.30"	""	""	"UO_0000065"	"18.62"	"0.34"	"5.53"	"5.85"	"False"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL3702912"	""	"0"	"513.02"	"1"	"4.11"	"BDBM147611"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)NCc3ccccc3Cl)cc2)n1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"285541"	"UO_0000065"	"16.96"	"0.34"	"4.59"	"6.09"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3644971"	""	"0"	"484.60"	"0"	"3.78"	"BDBM99721"	"COCc1ccccc1-c1cccc2nc(Nc3ccc4c(c3)CCN(CC(=O)N(C)C)CC4)nn12"	"IC50"	"'='"	"47.41"	"nM"	"7.32"	""	"216411"	"UO_0000065"	"15.11"	"0.28"	"3.54"	"9.77"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3645029"	""	"0"	"441.58"	"1"	"5.17"	"BDBM99789"	"Cc1ccc(OCC(C)C)c(-c2cccn3nc(Nc4ccc5c(c4)CCNCC5)nc23)c1"	"IC50"	"'='"	"3084.02"	"nM"	"5.51"	""	"216469"	"UO_0000065"	"12.48"	"0.23"	"0.34"	"8.68"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3645100"	""	"0"	"443.56"	"0"	"3.85"	"BDBM99874"	"COc1ccc(CNc2cccn3nc(Nc4cccc(N5CCN(C)CC5)c4)nc23)cc1"	"IC50"	"'='"	"9999.0"	"nM"	"5.00"	""	"216542"	"UO_0000065"	"11.27"	"0.21"	"1.15"	"7.15"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647904"	""	"0"	"470.96"	"0"	"3.01"	"BDBM148016"	"CC1(CNC(=O)[C@H]2CC[C@H](n3cc(C(N)=O)c(Nc4ccc(Cl)cc4)n3)[C@@H](C#N)C2)COC1"	"IC50"	"'='"	"59.0"	"nM"	"7.23"	""	"285951"	"UO_0000065"	"15.35"	"0.30"	"4.22"	"5.35"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703004"	""	"0"	"472.52"	"0"	"4.46"	"BDBM147714"	"N#C[C@H]1C[C@H](N2CC3(CCC3)C2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"240.0"	"nM"	"6.62"	""	"285648"	"UO_0000065"	"14.01"	"0.27"	"2.16"	"6.62"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4280783"	""	"0"	"380.45"	"0"	"3.00"	"1"	"COc1cc2c(=O)n(CCCN(C)C)c3c4cc[nH]c4ncc3c2cc1OC"	"IC50"	"'='"	"72.97"	"nM"	"7.14"	""	""	"UO_0000065"	"18.76"	"0.35"	"4.14"	"9.86"	"False"	"CHEMBL4261266"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]-ATP addition measured after 2 hrs by filter-binding method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257589"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL2105759"	"BARICITINIB"	"4"	"371.43"	"0"	"1.10"	"6"	"CCS(=O)(=O)N1CC(CC#N)(n2cc(-c3ncnc4[nH]ccc34)cn2)C1"	"IC50"	"'='"	"87.8"	"nM"	"7.06"	""	""	"UO_0000065"	"19.00"	"0.37"	"5.96"	"5.85"	"False"	"CHEMBL3299209"	"Inhibition of JAK2 homodimer in human CD34+ cells spiked into human whole blood assessed as inhibition of EPO-induced STAT-5 phosphorylation preincubated for 45 mins followed by EPO addition measured after 15 mins by FACS analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"CHEMBL3638178"	"Blood"	"CD34+ cell"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3297690"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"1"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"302.0"	"nM"	"6.52"	""	""	"UO_0000065"	"20.87"	"0.39"	"4.98"	"7.33"	"True"	"CHEMBL3299209"	"Inhibition of JAK2 homodimer in human CD34+ cells spiked into human whole blood assessed as inhibition of EPO-induced STAT-5 phosphorylation preincubated for 45 mins followed by EPO addition measured after 15 mins by FACS analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"CHEMBL3638178"	"Blood"	"CD34+ cell"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3297690"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL4566849"	""	"0"	"430.51"	"0"	"3.79"	"11d'"	"C=CC(=O)Nc1ccc(CNc2cc(Nc3ccc(N4CCOCC4)cc3)ncn2)cc1"	"IC50"	"'='"	"916.0"	"nM"	"6.04"	""	""	"UO_0000065"	"14.03"	"0.26"	"2.25"	"6.61"	"False"	"CHEMBL4482009"	"Inhibition of human JAK2 using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and further incubated for 30 mins and subsequently measured after 1 hr by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480445"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4521305"	""	"0"	"445.57"	"0"	"3.93"	"13e'"	"CCC(=O)Nc1ccc(CNc2cc(Nc3ccc(N4CCN(C)CC4)cc3)ncn2)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4482009"	"Inhibition of human JAK2 using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and further incubated for 30 mins and subsequently measured after 1 hr by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480445"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4591192"	""	"0"	"472.47"	"0"	"4.17"	"16d"	"O=C(Nc1cccc(CNc2cc(Nc3ccc(N4CCOCC4)cc3)ncn2)c1)C(F)(F)F"	"IC50"	"'='"	"366.0"	"nM"	"6.44"	""	""	"UO_0000065"	"13.62"	"0.26"	"2.27"	"7.04"	"False"	"CHEMBL4482009"	"Inhibition of human JAK2 using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and further incubated for 30 mins and subsequently measured after 1 hr by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480445"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4552985"	""	"0"	"363.43"	"0"	"3.08"	"12a"	"C/C=C/C(=O)Nc1cccc(CNc2cc(Nc3cnn(C)c3)ncn2)c1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4482009"	"Inhibition of human JAK2 using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and further incubated for 30 mins and subsequently measured after 1 hr by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480445"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4528395"	""	"0"	"412.45"	"0"	"3.83"	"32"	"CCc1cc(O)c(F)cc1-c1cc(NS(=O)(=O)c2ccccn2)c2cn[nH]c2c1"	"IC50"	"'='"	"19.95"	"nM"	"7.70"	""	""	"UO_0000065"	"18.67"	"0.36"	"3.87"	"7.13"	"False"	"CHEMBL4478762"	"Inhibition of human His-tagged JAK2 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4477220"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2016"	"None"	""
"CHEMBL4483513"	""	"0"	"421.45"	"0"	"2.94"	"28"	"CCc1cc(O)c(F)cc1-c1cc(NS(=O)(=O)CCC(=O)OC)c2cn[nH]c2c1"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	""	"UO_0000065"	"18.98"	"0.38"	"5.06"	"6.59"	"False"	"CHEMBL4478762"	"Inhibition of human His-tagged JAK2 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4477220"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2016"	"None"	""
"CHEMBL4544386"	""	"0"	"363.41"	"0"	"3.03"	"20"	"CCc1cc(O)c(F)cc1-c1cc(N(C)S(C)(=O)=O)c2cn[nH]c2c1"	"IC50"	"'='"	"79.43"	"nM"	"7.10"	""	""	"UO_0000065"	"19.54"	"0.39"	"4.07"	"8.23"	"False"	"CHEMBL4478762"	"Inhibition of human His-tagged JAK2 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4477220"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2016"	"None"	""
"CHEMBL4577685"	""	"0"	"345.42"	"0"	"3.31"	"17"	"CCS(=O)(=O)Nc1cc(-c2c(C)cc(O)cc2C)cc2[nH]ncc12"	"IC50"	"'='"	"1995.26"	"nM"	"5.70"	""	""	"UO_0000065"	"16.50"	"0.32"	"2.39"	"5.99"	"False"	"CHEMBL4478762"	"Inhibition of human His-tagged JAK2 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4477220"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2016"	"None"	""
"CHEMBL4564318"	""	"0"	"347.40"	"0"	"2.71"	"16"	"CCS(=O)(=O)Nc1cc(-c2ccc(O)c(OC)c2)cc2[nH]ncc12"	"IC50"	"'='"	"1000.0"	"nM"	"6.00"	""	""	"UO_0000065"	"17.27"	"0.34"	"3.29"	"5.75"	"False"	"CHEMBL4478762"	"Inhibition of human His-tagged JAK2 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4477220"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2016"	"None"	""
"CHEMBL3645044"	""	"0"	"602.61"	"2"	"6.07"	"BDBM99811"	"CN(C)C(=O)CN1CCC(c2ccc(Nc3nc4c(-c5cc(C(F)(F)F)ccc5OCC(F)F)cccn4n3)cc2)CC1"	"IC50"	"'='"	"524.3"	"nM"	"6.28"	""	"216484"	"UO_0000065"	"10.42"	"0.20"	"0.21"	"8.37"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3335699"	""	"0"	"471.59"	"0"	"1.00"	"28"	"CN1CCN(c2ncc(-c3cnc4[nH]ccc4n3)c(N[C@H]3CCCN(S(C)(=O)=O)C3)n2)CC1"	"IC50"	"'='"	"45.0"	"nM"	"7.35"	""	""	"UO_0000065"	"15.58"	"0.30"	"6.35"	"5.96"	"False"	"CHEMBL3374010"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 1 hr in presence of [gamma-33P]ATP by scintillation counting analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351377"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL4750831"	""	"0"	"377.45"	"0"	"2.77"	"4"	"C=CC(=O)Nc1cccc(-c2cc(Nc3cnn(CCN(C)C)c3)ncn2)c1"	"IC50"	"'>'"	"3000.0"	"nM"	""	""	""	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL4756089"	""	"0"	"364.41"	"0"	"2.85"	"9"	"C=CC(=O)Nc1ccc(-c2cc(Nc3cnn(CCOC)c3)ncn2)cc1"	"IC50"	"'>'"	"3000.0"	"nM"	""	""	""	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL4746272"	""	"0"	"401.47"	"0"	"3.85"	"12"	"C=CC(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"1000.0"	"nM"	"6.00"	""	""	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL4740889"	""	"0"	"334.38"	"0"	"3.14"	"13"	"C/C=C/C(=O)Nc1cccc(-c2cc(Nc3cnn(C)c3)ncn2)c1"	"IC50"	"'='"	"2761.0"	"nM"	"5.56"	""	""	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL4763424"	""	"0"	"378.44"	"0"	"3.24"	"15"	"C/C=C/C(=O)Nc1cccc(-c2cc(Nc3cnn(CCOC)c3)ncn2)c1"	"IC50"	"'='"	"2580.0"	"nM"	"5.59"	""	""	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL4778980"	""	"0"	"415.50"	"0"	"4.24"	"17"	"C/C=C/C(=O)Nc1cccc(-c2cc(Nc3ccc(N4CCOCC4)cc3)ncn2)c1"	"IC50"	"'='"	"2129.0"	"nM"	"5.67"	""	""	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL4739907"	""	"0"	"363.38"	"0"	"1.93"	"22"	"N#CCC(=O)Nc1cccc(-c2cc(Nc3cnn(CCO)c3)ncn2)c1"	"IC50"	"'='"	"1143.0"	"nM"	"5.94"	""	""	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL4756648"	""	"0"	"421.46"	"0"	"1.97"	"24"	"C=CC(=O)NCC(=O)Nc1cccc(-c2cc(Nc3cnn(CCOC)c3)ncn2)c1"	"IC50"	"'='"	"1542.0"	"nM"	"5.81"	""	""	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL4747498"	""	"0"	"415.50"	"0"	"4.24"	"34"	"C/C=C/C(=O)Nc1ccc(-c2cc(Nc3ccc(N4CCOCC4)cc3)ncn2)cc1"	"IC50"	"'='"	"2155.0"	"nM"	"5.67"	""	""	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL4782611"	""	"0"	"378.44"	"0"	"3.24"	"36"	"C/C=C/C(=O)Nc1ccc(-c2ccnc(Nc3cnn(CCOC)c3)n2)cc1"	"IC50"	"'='"	"1981.0"	"nM"	"5.70"	""	""	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL4750184"	""	"0"	"415.50"	"0"	"4.24"	"38"	"C/C=C/C(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1"	"IC50"	"'='"	"1412.0"	"nM"	"5.85"	""	""	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL3658102"	""	"0"	"554.74"	"2"	"6.08"	"BDBM148383"	"Cc1ccc(NC(=O)CC2CCCC2)cc1N1CCc2nc(Nc3ccc(OCCN4CCCC4)cc3)ncc2C1"	"IC50"	"'='"	"12.0"	"nM"	"7.92"	""	"286788"	"UO_0000065"	"14.28"	"0.26"	"1.84"	"9.59"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3335690"	""	"0"	"428.56"	"0"	"3.27"	"BDBM112536"	"CC(C)(C)CS(=O)(=O)N1CCC[C@H](Nc2ncccc2-c2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"0.0245"	"nM"	"10.61"	""	"233775"	"UO_0000065"	"24.76"	"0.48"	"7.34"	"10.22"	"False"	"CHEMBL3707646"	"Inhibition Assay: The kinase activity of all three JAK kinases is measured using a radioactive, end-point assay and with trace amounts of 33P-ATP."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638973"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3642353"	""	"0"	"490.63"	"0"	"4.34"	"BDBM99629"	"CN1CCC(c2cccc(Nc3nc4c(-c5ccccc5N(C)S(C)(=O)=O)cccn4n3)c2)CC1"	"IC50"	"'='"	"1197.86"	"nM"	"5.92"	""	"216319"	"UO_0000065"	"12.07"	"0.23"	"1.58"	"7.15"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647817"	""	"0"	"500.57"	"2"	"5.29"	"BDBM147922"	"N#C[C@@H]1C[C@@H](NC2CC3(CCCC3)C2)CC[C@H]1n1cc(C(N)=O)c(Nc2ccc(C(F)(F)F)cc2)n1"	"IC50"	"'='"	"665.0"	"nM"	"6.18"	""	"285856"	"UO_0000065"	"12.34"	"0.23"	"0.89"	"5.68"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642397"	""	"0"	"505.65"	"1"	"3.28"	"BDBM99675"	"CN1CCN(c2cccc(Nc3nc4c(-c5cccc(CN(C)S(C)(=O)=O)c5)cccn4n3)c2)CC1"	"IC50"	"'='"	"5.94"	"nM"	"8.23"	""	"216365"	"UO_0000065"	"16.27"	"0.31"	"4.95"	"9.56"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647720"	""	"0"	"423.50"	"0"	"2.98"	"BDBM147822"	"N#C[C@H]1C[C@H](N2CC3(CCC3)C2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccnc(F)c2)n1"	"IC50"	"'='"	"122.0"	"nM"	"6.91"	""	"285756"	"UO_0000065"	"16.33"	"0.30"	"3.93"	"6.13"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642272"	""	"0"	"373.44"	"0"	"1.72"	"BDBM99533"	"COc1ccc(Nc2nc3c(N4CCS(=O)(=O)CC4)cccn3n2)cc1"	"IC50"	"'='"	"568.0"	"nM"	"6.25"	""	"216225"	"UO_0000065"	"16.72"	"0.33"	"4.53"	"7.03"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3780467"	""	"0"	"385.47"	"0"	"1.72"	"21"	"COC(=O)C1CCc2[nH]c(-c3c(N[C@H]4CC[C@@H](N)CC4)cc[nH]c3=O)nc2C1"	"IC50"	"'='"	"1699.0"	"nM"	"5.77"	""	""	"UO_0000065"	"14.97"	"0.28"	"4.05"	"4.58"	"False"	"CHEMBL3784147"	"Inhibition of JAK2 in human CD34+ cells assessed as inhibition of EPO-mediated cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"CD34+ cell"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3779778"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2016"	"None"	""
"CHEMBL2062800"	""	"0"	"442.52"	"0"	"2.95"	"BDBM99612"	"CS(=O)(=O)c1ccc(-c2cccn3nc(Nc4cccc(S(C)(=O)=O)c4)nc23)cc1"	"IC50"	"'='"	"5.57"	"nM"	"8.25"	""	"216302"	"UO_0000065"	"18.65"	"0.38"	"5.30"	"7.47"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3647874"	""	"0"	"400.41"	"0"	"2.45"	"BDBM147986"	"CNC(=O)O[C@H]1CCC(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"51.0"	"nM"	"7.29"	""	"285920"	"UO_0000065"	"18.21"	"0.34"	"4.84"	"5.40"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703018"	""	"0"	"390.85"	"0"	"2.97"	"BDBM147728"	"CN[C@@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(Cl)c(F)c3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"35.0"	"nM"	"7.46"	""	"285662"	"UO_0000065"	"19.08"	"0.38"	"4.49"	"6.86"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703051"	""	"0"	"462.48"	"0"	"3.05"	"BDBM147761"	"N#C[C@H]1C[C@@H](NC2COC2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(CC(F)(F)F)cc2)n1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"285695"	"UO_0000065"	"18.43"	"0.35"	"5.47"	"7.22"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702962"	""	"0"	"177.25"	"0"	"2.77"	"BDBM147669"	"[C-]#[N+]C1=CCC[C@@H](OCC2CC2)C1"	"IC50"	"'='"	"74.0"	"nM"	"7.13"	""	"285601"	"UO_0000065"	"40.23"	"0.75"	"4.36"	"52.47"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652332"	""	"0"	"405.57"	"0"	"3.01"	"BDBM113143"	"C[C@H]1CCCN(S(=O)(=O)C[C@H]2CC[C@H](N(C)c3ncnc4[nH]ccc34)CC2)C1"	"IC50"	"'='"	"72.2"	"nM"	"7.14"	""	"234586"	"UO_0000065"	"17.61"	"0.35"	"4.13"	"8.69"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL1287854"	""	"0"	"306.37"	"0"	"3.47"	"(S)-Ruxolitinib"	"N#CC[C@@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1"	"IC50"	"'='"	"5.0"	"nM"	"8.30"	""	""	""	"27.09"	"0.49"	"4.83"	"9.98"	"False"	"CHEMBL4714135"	"Inhibition of human JAK2 by radiometric assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEK293F"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706688"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"Tofacitinib"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"2.9"	"nM"	"8.54"	""	""	""	"27.33"	"0.51"	"7.00"	"9.60"	"False"	"CHEMBL4714135"	"Inhibition of human JAK2 by radiometric assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEK293F"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706688"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	""
"CHEMBL4760892"	""	"0"	"604.15"	"2"	"5.43"	"6"	"Cc1cnc(Nc2ccc(C(=O)NC3CCN(C)CC3)c(F)c2)nc1Nc1ccc(Cl)c(NS(=O)(=O)C(C)(C)C)c1"	"IC50"	"'='"	"11.4"	"nM"	"7.94"	""	""	""	"13.15"	"0.26"	"2.51"	"6.19"	"False"	"CHEMBL4714135"	"Inhibition of human JAK2 by radiometric assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEK293F"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706688"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	""
"CHEMBL4758261"	""	"0"	"462.94"	"0"	"4.20"	"10e"	"O=C(Nc1c[nH]nc1-c1nc(-c2ccc(CN3CCOCC3)cc2)c[nH]1)c1cccc(Cl)c1"	"IC50"	"'='"	"166.0"	"nM"	"6.78"	""	""	""	"14.65"	"0.28"	"2.58"	"6.85"	"False"	"CHEMBL4711870"	"Inhibition of JAK2 (unknown origin) incubated for 40 mins in presence of ATP by Kinase-glo luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706620"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2021"	"None"	"TIME = 0.6667 hr"
"CHEMBL3703489"	""	"0"	"296.33"	"0"	"2.69"	"BDBM153133"	"CCOC(=O)c1c[nH]c2ncnc(-c3ccc(C)c(N)c3)c12"	"IC50"	"'='"	"78.0"	"nM"	"7.11"	""	"294081"	"UO_0000065"	"23.99"	"0.44"	"4.42"	"7.57"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL2376439"	""	"0"	"513.56"	"1"	"2.36"	"12d"	"CC(=O)N[C@@H]1CCc2ccc(Oc3cnc4[nH]cc(C(=O)N[C@@H](C(=O)N5CC(C#N)C5)C5CC5)c4n3)cc21"	"IC50"	"'='"	"23300.0"	"nM"	"4.63"	""	""	"UO_0000065"	"9.02"	"0.17"	"2.27"	"3.03"	"False"	"CHEMBL2378973"	"Inhibition of JAK2 in human PBMC expressing CD14 assessed as inhibition of GM-CSF-induced STAT5a phosphorylation"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375291"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL3703037"	""	"0"	"490.53"	"0"	"3.90"	"BDBM147747"	"CC1(C)CN([C@H]2CC[C@H](n3cc(C(N)=O)c(Nc4ccc([C@@H](O)C(F)(F)F)cc4)n3)[C@@H](C#N)C2)C1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"285681"	"UO_0000065"	"17.12"	"0.33"	"4.50"	"6.99"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3884240"	""	"0"	"426.50"	"0"	"2.45"	"5m"	"NS(=O)(=O)c1cccc(Nc2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)c1"	"IC50"	"'='"	"129.0"	"nM"	"6.89"	""	""	"UO_0000065"	"16.15"	"0.31"	"4.44"	"5.63"	"False"	"CHEMBL3875838"	"Inhibition of human JAK2 using poly (Glu:Tyr) as substrate"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3875172"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2016"	"None"	""
"CHEMBL3884848"	""	"0"	"388.52"	"0"	"4.33"	"5n"	"Cc1cccc(Nc2ccnc(Nc3ccc(N4CCN(C)CC4)c(C)c3)n2)c1"	"IC50"	"'='"	"50.0"	"nM"	"7.30"	""	""	"UO_0000065"	"18.79"	"0.34"	"2.97"	"12.96"	"False"	"CHEMBL3875838"	"Inhibition of human JAK2 using poly (Glu:Tyr) as substrate"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3875172"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2016"	"None"	""
"CHEMBL3126351"	""	"0"	"336.32"	"0"	"3.47"	"13"	"CC(C)[C@H](Nc1nc2ccncc2c2c(=O)[nH]ccc12)C(F)(F)F"	"IC50"	"'='"	"170.0"	"nM"	"6.77"	""	""	"UO_0000065"	"20.13"	"0.39"	"3.30"	"9.58"	"False"	"CHEMBL3131375"	"Inhibition of Jak2 (unknown origin) assessed as inhibition of STAT5 phosphorylation by cell-based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3124786"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL1289218"	""	"0"	"336.32"	"0"	"3.47"	"1"	"CC(C)[C@@H](Nc1nc2cc[nH]c(=O)c2c2cnccc12)C(F)(F)F"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	""	"UO_0000065"	"26.76"	"0.51"	"5.53"	"12.74"	"False"	"CHEMBL3131376"	"Inhibition of recombinant Jak2 (unknown origin) using biotinylated synthetic peptide substrate by homogeneous time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3124786"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3645106"	""	"0"	"346.39"	"0"	"3.49"	"BDBM99880"	"COc1cccc(CNc2cccn3nc(Nc4ccncc4)nc23)c1"	"IC50"	"'='"	"998.92"	"nM"	"6.00"	""	"216548"	"UO_0000065"	"17.32"	"0.32"	"2.51"	"7.86"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL4755698"	""	"0"	"405.46"	"0"	"2.83"	"B16"	"C=CC(=O)N1CCC(Cn2cc(-c3ccc4c(c3)OCO4)c3c(N)ncnc32)CC1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	""	""	""	""	""	"False"	"CHEMBL4720228"	"Inhibition of recombinant human JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate incubate for 60 mins by LANCE assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715815"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2018"	"None"	"TIME = 1.0 hr"
"CHEMBL4754856"	""	"0"	"446.56"	"0"	"4.06"	"13x"	"COC(=O)/C=C/CN1CCc2cc(Nc3ncc(C)c(-c4cnn(C(C)C)c4)n3)ccc2C1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	""	""	"19.48"	"0.36"	"4.64"	"10.21"	"False"	"CHEMBL4723820"	"Inhibition of recombinant human JAK2 (808 to end residues) KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate measured after 40 mins in presence of [gamm33P]ATP by scintillation counting method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 0.6667 hr"
"CHEMBL3703010"	""	"0"	"419.44"	"0"	"2.52"	"BDBM147720"	"CN(C)[C@@H]1CC[C@@H](n2cc(C(N)=O)c(Nc3ccc(OC(F)F)nc3)n2)[C@H](C#N)C1"	"IC50"	"'='"	"1100.0"	"nM"	"5.96"	""	"285654"	"UO_0000065"	"14.21"	"0.27"	"3.44"	"4.88"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3116050"	""	"0"	"353.37"	"0"	"2.54"	"19a"	"C[C@H](Nc1nc(Nc2cn(C)cn2)c2cc[nH]c2n1)c1ncc(F)cn1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	""	"UO_0000065"	"24.62"	"0.46"	"6.16"	"7.96"	"False"	"CHEMBL3116823"	"Inhibition of Jak2 V617F mutant in human UKE1 cells assessed as inhibition of STAT5 phosphorylation after 1 hr by Western blotting analysis"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"UKE1"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3112447"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL4568087"	""	"0"	"421.53"	"0"	"2.86"	"19"	"Cn1cc(-c2cnc3c(-c4csc(C(=O)N[C@@H]5CCCC[C@@H]5N)c4)cnn3c2)cn1"	"IC50"	"'='"	"64.0"	"nM"	"7.19"	""	""	"UO_0000065"	"17.07"	"0.33"	"4.33"	"6.98"	"False"	"CHEMBL4479735"	"Inhibition of recombinant human GST-tagged cytoplasmic JAK2 (809 to 1153 residues) expressed in baculovirus expression system by Z'-LYTE assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4477252"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2016"	"None"	""
"CHEMBL4777200"	""	"0"	"415.90"	"0"	"3.60"	"32a"	"CNC(=O)c1cnc2[nH]ccc2c1N[C@@H]1CCN(Cc2cccc(Cl)c2)C[C@H]1F"	"IC50"	"'='"	"28.0"	"nM"	"7.55"	""	""	""	"18.16"	"0.36"	"3.95"	"10.34"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL4747742"	""	"0"	"411.48"	"0"	"2.96"	"32c"	"CNC(=O)c1cnc2[nH]ccc2c1N[C@@H]1CCN(Cc2cccc(OC)c2)C[C@@H]1F"	"IC50"	"'='"	"10.9"	"nM"	"7.96"	""	""	""	"19.35"	"0.36"	"5.00"	"9.68"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"Tofacitinib"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"4.98"	"nM"	"8.30"	""	""	""	"26.58"	"0.49"	"6.76"	"9.34"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL2105759"	"BARICITINIB"	"4"	"371.43"	"0"	"1.10"	"Baricitinib"	"CCS(=O)(=O)N1CC(CC#N)(n2cc(-c3ncnc4[nH]ccc34)cn2)C1"	"IC50"	"'='"	"0.29"	"nM"	"9.54"	""	""	""	"25.68"	"0.50"	"8.44"	"7.91"	"False"	"CHEMBL4714135"	"Inhibition of human JAK2 by radiometric assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEK293F"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706688"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	""
"CHEMBL4744236"	""	"0"	"562.66"	"2"	"6.04"	"5"	"Cc1cnc(Nc2cc(F)c(C3CCN(C)CC3)c(F)c2)nc1Nc1ccc(F)c(NS(=O)(=O)C(C)(C)C)c1"	"IC50"	"'='"	"8.2"	"nM"	"8.09"	""	""	""	"14.37"	"0.28"	"2.05"	"8.15"	"False"	"CHEMBL4714135"	"Inhibition of human JAK2 by radiometric assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEK293F"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706688"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	""
"CHEMBL4175555"	""	"0"	"627.73"	"1"	"4.63"	"20a"	"CS(=O)(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCC(C(=O)Nc5ccc(/C=C/C(=O)NO)cc5)CC4)cc3)n2)cc1"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	""	"UO_0000065"	"12.90"	"0.25"	"3.47"	"4.89"	"False"	"CHEMBL4150584"	"Inhibition of JAK2 (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition and measured after 25 mins in presence of ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4145634"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3120969"	""	"0"	"484.47"	"0"	"4.81"	"7"	"CCOP(=O)(CCn1cc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)n2C)nn1)OCC"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3363474"	"Inhibition of JAK2 (unknown origin) by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352554"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3120970"	""	"0"	"425.47"	"0"	"4.75"	"JNJ 7583979"	"C[C@H](Nc1nccc(-c2c(-c3ccc(F)cc3)nc3nc(N)ccn23)n1)c1ccccc1"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3363474"	"Inhibition of JAK2 (unknown origin) by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352554"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3314280"	""	"0"	"550.40"	"1"	"3.67"	"24"	"O=c1cc(-c2[nH]c(-c3ccc(-c4cn(CCP(=O)([O-])[O-])nn4)cc3)nc2-c2ccc(F)cc2)cc[nH]1.[Na+].[Na+]"	"IC50"	"'='"	"45500.0"	"nM"	"4.34"	""	""	"UO_0000065"	"8.57"	"0.16"	"0.67"	"2.90"	"False"	"CHEMBL3363474"	"Inhibition of JAK2 (unknown origin) by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352554"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3314284"	""	"0"	"437.48"	"0"	"3.42"	"31.K"	"O=c1cc(-c2[nH]c(-c3ccc(-c4nnn[n-]4)cc3)nc2-c2ccc(F)cc2)cc[nH]1.[K+]"	"IC50"	"'='"	"61.0"	"nM"	"7.21"	""	""	"UO_0000065"	"18.06"	"0.33"	"3.79"	"6.22"	"False"	"CHEMBL3363474"	"Inhibition of JAK2 (unknown origin) by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352554"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3645056"	""	"0"	"449.51"	"1"	"5.55"	"BDBM99824"	"COc1cc(C(F)F)ccc1-c1cccn2nc(Nc3ccc(C4CCNCC4)cc3)nc12"	"IC50"	"'='"	"65.86"	"nM"	"7.18"	""	"216497"	"UO_0000065"	"15.98"	"0.30"	"1.63"	"11.31"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3645083"	""	"0"	"598.68"	"1"	"3.68"	"BDBM99854"	"CN(C)C(=O)CN1CCc2ccc(Nc3nc4c(-c5cc(S(C)(=O)=O)ccc5OCC(F)F)cccn4n3)cc2CC1"	"IC50"	"'='"	"504.69"	"nM"	"6.30"	""	"216525"	"UO_0000065"	"10.52"	"0.20"	"2.62"	"5.77"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3126350"	""	"0"	"436.28"	"0"	"3.17"	"32"	"NS(=O)(=O)c1cc(Cl)c(Nc2nc3ccncc3c3c(=O)[nH]ccc23)c(Cl)c1"	"IC50"	"'='"	"113.0"	"nM"	"6.95"	""	""	"UO_0000065"	"15.92"	"0.34"	"3.78"	"5.31"	"False"	"CHEMBL3131375"	"Inhibition of Jak2 (unknown origin) assessed as inhibition of STAT5 phosphorylation by cell-based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3124786"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3126351"	""	"0"	"336.32"	"0"	"3.47"	"13"	"CC(C)[C@H](Nc1nc2ccncc2c2c(=O)[nH]ccc12)C(F)(F)F"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	""	"UO_0000065"	"23.79"	"0.46"	"4.53"	"11.32"	"False"	"CHEMBL3131376"	"Inhibition of recombinant Jak2 (unknown origin) using biotinylated synthetic peptide substrate by homogeneous time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3124786"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3126350"	""	"0"	"436.28"	"0"	"3.17"	"32"	"NS(=O)(=O)c1cc(Cl)c(Nc2nc3ccncc3c3c(=O)[nH]ccc23)c(Cl)c1"	"IC50"	"'='"	"0.15"	"nM"	"9.82"	""	""	"UO_0000065"	"22.52"	"0.48"	"6.65"	"7.51"	"False"	"CHEMBL3131376"	"Inhibition of recombinant Jak2 (unknown origin) using biotinylated synthetic peptide substrate by homogeneous time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3124786"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3126342"	""	"0"	"358.19"	"0"	"3.92"	"17"	"O=c1[nH]ccc2c(Nc3c(Cl)cncc3Cl)nc3ccncc3c12"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	""	"UO_0000065"	"24.29"	"0.50"	"4.78"	"10.41"	"False"	"CHEMBL3131376"	"Inhibition of recombinant Jak2 (unknown origin) using biotinylated synthetic peptide substrate by homogeneous time resolved fluorescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3124786"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3658104"	""	"0"	"547.54"	"1"	"4.86"	"BDBM148394"	"Cc1ccc(NC(=O)c2cccc(C(F)(F)F)c2)cc1N1CCc2nc(Nc3ccc(C(N)=O)nc3)ncc2C1"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	"286790"	"UO_0000065"	"14.79"	"0.28"	"3.24"	"6.42"	"False"	"CHEMBL3705799"	"TR-FRET Assay: Compounds were screened in the TR-FRET assay for JAK2 and c-Src kinase inhibition. Ultra light poly GT (Perkin Elmer) was used as the substrate for JAK2 and c-Src with the ATP concentration of 10 μM and 50 μM, respectively. The Eu-labelled anti-phospho tyrosine antibody (Perkin Elmer) was added at 1 nM and the fluorescence emission at 615 nm and 665 nm was measured with an excitation wavelength of 340 nm."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638677"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647933"	""	"0"	"359.38"	"0"	"3.46"	"BDBM148053"	"C[C@]1(C#N)CC[C@H](F)C[C@@H]1n1cc(C(N)=O)c(Nc2ccc(F)cc2)n1"	"IC50"	"'='"	"8.0"	"nM"	"8.10"	""	"285561"	"UO_0000065"	"22.53"	"0.43"	"4.64"	"8.37"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702905"	""	"0"	"479.57"	"0"	"2.85"	"BDBM147604"	"N#C[C@H]1CCCC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(S(=O)(=O)NCc3cccnc3)cc2)n1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"285534"	"UO_0000065"	"18.77"	"0.36"	"6.15"	"5.78"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4762807"	""	"0"	"552.72"	"2"	"5.71"	"7"	"Cc1cnc(Nc2ccc(C3CCN(C)CC3)c(F)c2)nc1Nc1ccc2c(c1)N(S(=O)(=O)C(C)(C)C)CC2"	"IC50"	"'='"	"3.6"	"nM"	"8.44"	""	""	""	"15.28"	"0.30"	"2.73"	"9.33"	"False"	"CHEMBL4714135"	"Inhibition of human JAK2 by radiometric assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEK293F"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706688"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	""
"CHEMBL3763991"	""	"0"	"382.47"	"0"	"2.42"	"14"	"CC(C)[C@H](C)n1cc(-c2ccc(N3CCOCC3)cn2)c2[nH]nc(N)c2c1=O"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	""	"UO_0000065"	"21.32"	"0.40"	"5.73"	"7.99"	"False"	"CHEMBL3766653"	"Inhibition of JAK2 (unknown origin) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent substrate phosphorylation after 45 mins by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3763089"	"1"	"Scientific Literature"	"J. Med. Chem."	"2016"	"None"	""
"CHEMBL4060602"	""	"0"	"314.35"	"0"	"1.89"	"23"	"O=C(CCCCCn1cc(-c2ncnc3[nH]ccc23)cn1)NO"	"IC50"	"'='"	"200.0"	"nM"	"6.70"	""	""	"UO_0000065"	"21.31"	"0.40"	"4.81"	"6.16"	"False"	"CHEMBL4031305"	"Inhibition of human JAK2 using poly[Glu:Tyr] as substrate in presence of [gamma-33P]-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4028864"	"1"	"Scientific Literature"	"J Med Chem"	"2017"	"None"	""
"CHEMBL3694593"	""	"0"	"352.83"	"0"	"3.56"	"BDBM125914"	"Nc1ccc2cc1CCc1cncc(c1)Nc1ncc(Cl)c(n1)NC2"	"IC50"	"'='"	"447.0"	"nM"	"6.35"	""	"255687"	"UO_0000065"	"18.00"	"0.35"	"2.79"	"7.15"	"False"	"CHEMBL3707544"	"In Vitro Kinase Assay: One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Biochemistry 1999, 269, 94-104. The catalytic domains of human JAK1 (a.a. 837-1142), JAK2 (a.a. 828-1132) and JAK3 (a.a. 781-1124) with an N-terminal His tag were expressed using baculovirus in insect cells and purified. The catalytic activity of JAK1, JAK2 or JAK3 was assayed by measuring the phosphorylation of a biotinylated peptide. The phosphorylated peptide was detected by homogenous time resolved fluorescence (HTRF). IC50s of compounds were measured for each kinase in the reactions that contain the enzyme, ATP and 500 nM peptide in 50 mM Tris (pH 7.8) buffer with 100 mM NaCl, 5 mM DTT, and 0.1 mg/mL (0.01%) BSA. The ATP concentration in the reactions was 90 uM for JAK1, 30 uM for JAK2 and 3 uM for JAK3. Reactions were carried out at room temperature for 1 hr and then stopped with 20 uL 45 mM EDTA."	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639093"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3647879"	""	"0"	"462.89"	"0"	"3.34"	"BDBM147991"	"N#C[C@H]1C[C@@H](C(=O)N2CC(F)(F)C2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc(Cl)cc2)n1"	"IC50"	"'>'"	"500.0"	"nM"	""	""	"285926"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645099"	""	"0"	"443.56"	"0"	"3.85"	"BDBM99873"	"COc1cccc(CNc2cccn3nc(Nc4cccc(N5CCN(C)CC5)c4)nc23)c1"	"IC50"	"'='"	"2999.0"	"nM"	"5.52"	""	"216541"	"UO_0000065"	"12.45"	"0.23"	"1.67"	"7.89"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3644982"	""	"0"	"505.64"	"1"	"3.98"	"BDBM99733"	"CCOc1ccccc1-c1cccn2nc(Nc3ccc4c(c3)CCN(CCS(C)(=O)=O)CC4)nc12"	"IC50"	"'='"	"70.04"	"nM"	"7.16"	""	"216422"	"UO_0000065"	"14.15"	"0.27"	"3.17"	"8.05"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3763252"	""	"0"	"382.47"	"0"	"2.42"	"13"	"CC(C)C(C)n1cc(-c2ccc(N3CCOCC3)cn2)c2[nH]nc(N)c2c1=O"	"IC50"	"'='"	"13.0"	"nM"	"7.89"	""	""	"UO_0000065"	"20.62"	"0.38"	"5.47"	"7.73"	"False"	"CHEMBL3766653"	"Inhibition of JAK2 (unknown origin) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent substrate phosphorylation after 45 mins by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3763089"	"1"	"Scientific Literature"	"J. Med. Chem."	"2016"	"None"	""
"CHEMBL3763833"	""	"0"	"316.36"	"0"	"3.27"	"7"	"Cc1ccccc1-n1cc(-c2ccccc2)c2[nH]nc(N)c2c1=O"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3766653"	"Inhibition of JAK2 (unknown origin) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent substrate phosphorylation after 45 mins by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3763089"	"1"	"Scientific Literature"	"J. Med. Chem."	"2016"	"None"	""
"CHEMBL3765131"	""	"0"	"340.77"	"0"	"2.35"	"5"	"Cn1ccc(-c2cn(-c3ccccc3Cl)c(=O)c3c(N)n[nH]c23)n1"	"IC50"	"'='"	"910.0"	"nM"	"6.04"	""	""	"UO_0000065"	"17.73"	"0.34"	"3.69"	"6.39"	"False"	"CHEMBL3766653"	"Inhibition of JAK2 (unknown origin) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent substrate phosphorylation after 45 mins by TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3763089"	"1"	"Scientific Literature"	"J. Med. Chem."	"2016"	"None"	""
"CHEMBL3647847"	""	"0"	"391.83"	"0"	"3.13"	"BDBM147956"	"C[C@]1(O)CC[C@H](n2cc(C(N)=O)c(Nc3ccc(Cl)c(F)c3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"11.0"	"nM"	"7.96"	""	"285890"	"UO_0000065"	"20.31"	"0.40"	"4.83"	"6.80"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3642352"	""	"0"	"490.63"	"0"	"4.34"	"BDBM99628"	"CN1CCC(c2cccc(Nc3nc4c(-c5cccc(N(C)S(C)(=O)=O)c5)cccn4n3)c2)CC1"	"IC50"	"'='"	"8.88"	"nM"	"8.05"	""	"216318"	"UO_0000065"	"16.41"	"0.31"	"3.71"	"9.72"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3644981"	""	"0"	"435.43"	"0"	"4.15"	"BDBM99732"	"FC1(F)Oc2cccc(-c3cccn4nc(Nc5ccc6c(c5)CCNCC6)nc34)c2O1"	"IC50"	"'='"	"43.61"	"nM"	"7.36"	""	"216421"	"UO_0000065"	"16.90"	"0.31"	"3.21"	"10.12"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3703065"	""	"0"	"370.43"	"0"	"2.66"	"BDBM147775"	"CN(C)[C@H]1CC[C@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"27.0"	"nM"	"7.57"	""	"285717"	"UO_0000065"	"20.43"	"0.38"	"4.91"	"7.57"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3644998"	""	"0"	"457.54"	"0"	"2.90"	"BDBM99750"	"CN1CCN(c2cccc(Nc3nc4c(OCc5ccccc5C(N)=O)cccn4n3)c2)CC1"	"IC50"	"'='"	"142.78"	"nM"	"6.84"	""	"216438"	"UO_0000065"	"14.96"	"0.27"	"3.95"	"6.78"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3699497"	""	"0"	"456.52"	"0"	"3.87"	"BDBM147513"	"CC(C)(C)OC(=O)NCC1CC[C@H](C#N)[C@@H](n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)C1"	"IC50"	"'='"	"434.0"	"nM"	"6.36"	""	"285441"	"UO_0000065"	"13.94"	"0.26"	"2.49"	"4.71"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3702981"	""	"0"	"514.53"	"1"	"2.49"	"BDBM147691"	"COCCN[C@H]1CCC(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)(F)F)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"35.0"	"nM"	"7.46"	""	"285624"	"UO_0000065"	"14.49"	"0.29"	"4.97"	"4.90"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703495"	""	"0"	"283.29"	"0"	"2.51"	"BDBM153139"	"CCOC(=O)c1c[nH]c2ncnc(-c3ccc(O)cc3)c12"	"IC50"	"'='"	"134.0"	"nM"	"6.87"	""	"294087"	"UO_0000065"	"24.26"	"0.45"	"4.36"	"7.80"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652321"	""	"0"	"523.73"	"1"	"2.82"	"BDBM113131"	"CN(c1ncnc2[nH]ccc12)[C@H]1CC[C@H](CS(=O)(=O)N2CCC(CS(=O)(=O)CC3CC3)CC2)CC1"	"IC50"	"'='"	"88.6"	"nM"	"7.05"	""	"234574"	"UO_0000065"	"13.47"	"0.28"	"4.23"	"6.06"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3650985"	""	"0"	"350.38"	"0"	"3.32"	"BDBM153159"	"C=C(C)C(=O)Nc1cccc(-c2ncnc3[nH]cc(C(=O)OCC)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294108"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3651037"	""	"0"	"443.49"	"0"	"1.85"	"BDBM153214"	"C=C(CNS(C)(=O)=O)C(=O)Nc1cccc(-c2ncnc3[nH]cc(C(=O)OCC)c23)c1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"294162"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3647812"	""	"0"	"444.97"	"0"	"3.58"	"BDBM147916"	"COCC(C)N(C)[C@H]1CCC(n2cc(C(N)=O)c(Nc3ccc(Cl)cc3)n2)[C@@H](C#N)C1"	"IC50"	"'='"	"27.0"	"nM"	"7.57"	""	"285850"	"UO_0000065"	"17.01"	"0.33"	"3.99"	"6.93"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3645050"	""	"0"	"567.61"	"2"	"7.28"	"BDBM99817"	"COc1ccc(C(F)(F)F)cc1-c1cccn2nc(Nc3ccc(C4CCN(C(=O)OC(C)(C)C)CC4)cc3)nc12"	"IC50"	"'='"	"6499.0"	"nM"	"5.19"	""	"216490"	"UO_0000065"	"9.14"	"0.17"	"-2.09"	"6.40"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3652316"	""	"0"	"462.62"	"0"	"2.26"	"BDBM113126"	"CCC1(C(N)=O)CCN(S(=O)(=O)C[C@H]2CC[C@H](N(C)c3ncnc4[nH]ccc34)CC2)CC1"	"IC50"	"'='"	"61.1"	"nM"	"7.21"	""	"234569"	"UO_0000065"	"15.59"	"0.31"	"4.95"	"5.76"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3703505"	""	"0"	"323.38"	"0"	"4.02"	"BDBM153149"	"CCOC(=O)c1c[nH]c2ncnc(-c3cc4ccccc4s3)c12"	"IC50"	"'='"	"54.0"	"nM"	"7.27"	""	"294097"	"UO_0000065"	"22.47"	"0.43"	"3.25"	"10.71"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3703059"	""	"0"	"502.54"	"1"	"4.04"	"BDBM147769"	"N#C[C@H]1C[C@@H](N2CC3(CCC3)C2)CC[C@@H]1n1cc(C(N)=O)c(Nc2ccc([C@H](O)C(F)(F)F)cc2)n1"	"IC50"	"'='"	"7.0"	"nM"	"8.15"	""	"285703"	"UO_0000065"	"16.23"	"0.31"	"4.11"	"6.78"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4635754"	""	"0"	"404.87"	"1"	"5.01"	"16p"	"CCOC(C)n1cc(-c2cnc(N)c(OC(C)c3cc(F)ccc3Cl)c2)cn1"	"IC50"	"'='"	"157.0"	"nM"	"6.80"	""	""	"UO_0000065"	"16.81"	"0.33"	"1.79"	"9.05"	"False"	"CHEMBL4628503"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4627317"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL3335681"	""	"0"	"327.35"	"0"	"0.98"	"rac-8"	"N#CCC(=O)N1CCCC(NC(=O)Nc2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"181.0"	"nM"	"6.74"	""	""	"UO_0000065"	"20.60"	"0.38"	"5.76"	"5.32"	"False"	"CHEMBL3374010"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 1 hr in presence of [gamma-33P]ATP by scintillation counting analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351377"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3335682"	""	"0"	"338.39"	"0"	"0.50"	"rac-9"	"CS(=O)(=O)N1CCCC(NC(=O)Nc2cnc3[nH]ccc3n2)C1"	"IC50"	"'='"	"48.0"	"nM"	"7.32"	""	""	"UO_0000065"	"21.63"	"0.43"	"6.82"	"6.09"	"False"	"CHEMBL3374010"	"Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 1 hr in presence of [gamma-33P]ATP by scintillation counting analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351377"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL4744513"	""	"0"	"473.49"	"0"	"3.46"	"10c"	"O=C(Nc1c[nH]nc1-c1nc(-c2ccc(CN3CCOCC3)cc2)c[nH]1)c1ccc([N+](=O)[O-])cc1"	"IC50"	"'='"	"1178.0"	"nM"	"5.93"	""	""	""	"12.52"	"0.23"	"2.47"	"4.17"	"False"	"CHEMBL4711870"	"Inhibition of JAK2 (unknown origin) incubated for 40 mins in presence of ATP by Kinase-glo luminescence assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706620"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2021"	"None"	"TIME = 0.6667 hr"
"CHEMBL3330107"	""	"0"	"355.83"	"0"	"3.43"	"9"	"CCNC(=O)c1cc(-c2ccnc(N)n2)[nH]c1-c1cc(Cl)ccc1C"	"IC50"	"'='"	"109.0"	"nM"	"6.96"	""	""	"UO_0000065"	"19.57"	"0.38"	"3.53"	"7.20"	"False"	"CHEMBL3374493"	"Inhibition of recombinant human JAK2 (808-1132 residues) using LPLDKDYYVVREPGQ as substrate by radiometric assay in presence of [33P]-gamma-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL1287853"	"FEDRATINIB"	"4"	"524.69"	"1"	"4.82"	"10, TG101348"	"Cc1cnc(Nc2ccc(OCCN3CCCC3)cc2)nc1Nc1cccc(S(=O)(=O)NC(C)(C)C)c1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"16.24"	"0.31"	"3.70"	"7.86"	"True"	"CHEMBL3225235"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3217496"	"1"	"Scientific Literature"	"MedChemComm"	"2012"	"None"	""
"CHEMBL4459585"	"ROPSACITINIB"	"2"	"383.42"	"0"	"2.54"	"22, PF-06826647"	"Cn1cc(-c2cn3nccc3c(-c3cnn([C@]4(CC#N)C[C@@H](C#N)C4)c3)n2)cn1"	"IC50"	"'='"	"148.0"	"nM"	"6.83"	""	""	""	""	""	""	""	"False"	"CHEMBL4675820"	"Inhibition of JAK2 homodimer signaling pathway in human whole blood spiked with CD34 +ve cells assessed as reduction in EPO induced STAT5 phosphorylation preincubated for 45 mins followed by EPO addition and measured measured after 15 mins by immunostaining based FACS assay"	"A"	"BAO_0000221"	"tissue-based format"	"Homo sapiens"	"None"	"Blood"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4673239"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 1.0 hr"
"CHEMBL3330119"	""	"0"	"447.93"	"0"	"4.82"	"22"	"COc1ccc(CNc2nccc(-c3cc(C(N)=O)c(-c4cc(Cl)ccc4C)[nH]3)n2)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL3374497"	"Inhibition of JAK2 V617F mutant in human SET2 cells"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352511"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL3967108"	""	"0"	"646.77"	"2"	"5.98"	"11"	"CCN1CCN(Cc2ccc(-c3cc4c(-c5cccc(N6CCOc7cc(C8CC8)cc(F)c7C6=O)c5CO)ccnc4[nH]3)nc2)CC1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4178255"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4177534"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL3966346"	""	"0"	"580.66"	"2"	"5.27"	"13"	"O=C1c2c(F)cc(C3CC3)cc2OCCN1c1cccc(-c2ccnc3[nH]c(C4=CCN(C5COC5)CC4)cc23)c1CO"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4178255"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4177534"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4756788"	""	"0"	"393.49"	"0"	"3.01"	"17d"	"CNC(=O)c1cnc2[nH]ccc2c1NC1CCN(Cc2ccccc2OC)CC1"	"IC50"	"'='"	"7060.0"	"nM"	"5.15"	""	""	""	"13.09"	"0.24"	"2.14"	"6.26"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL4755612"	""	"0"	"407.52"	"0"	"3.40"	"31h"	"CNC(=O)c1cnc2[nH]ccc2c1N[C@@H]1CCN(Cc2cccc(OC)c2)[C@H](C)C1"	"IC50"	"'='"	"28.4"	"nM"	"7.55"	""	""	""	"18.52"	"0.34"	"4.15"	"9.17"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL4226055"	""	"0"	"422.51"	"0"	"2.51"	"14"	"N#Cc1cccc(S(=O)(=O)N2CC[C@@H](N(CC3CC3)c3ncnc4[nH]ccc34)C2)c1"	"IC50"	"'='"	"1400.0"	"nM"	"5.85"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4228474"	""	"0"	"382.45"	"0"	"1.73"	"31"	"CN(c1ncnc2[nH]ccc12)[C@@H]1CCN(S(=O)(=O)c2ccccc2C#N)C1"	"IC50"	"'='"	"370.0"	"nM"	"6.43"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4220821"	"Inhibition of recombinant human JAK2 (808-end residues) in presence of ATP"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219073"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL3644979"	""	"0"	"399.50"	"0"	"4.23"	"BDBM99730"	"CCOc1ccccc1-c1cccn2nc(Nc3ccc4c(c3)CCNCC4)nc12"	"IC50"	"'='"	"16.51"	"nM"	"7.78"	""	"216467"	"UO_0000065"	"19.48"	"0.35"	"3.55"	"12.26"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL4750665"	""	"0"	"389.50"	"0"	"3.53"	"17i"	"O=C(NC1CC1)c1cnc2[nH]ccc2c1NC1CCN(Cc2ccccc2)CC1"	"IC50"	"'='"	"232.0"	"nM"	"6.63"	""	""	""	"17.03"	"0.31"	"3.10"	"9.08"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL4742822"	""	"0"	"383.88"	"0"	"3.26"	"19c"	"CNC(=O)c1cnc2[nH]ccc2c1NC1CCN(Cc2ccc(Cl)cc2)C1"	"IC50"	"'='"	"503.8"	"nM"	"6.30"	""	""	""	"16.41"	"0.32"	"3.04"	"8.62"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL4781706"	""	"0"	"411.94"	"0"	"4.04"	"30c"	"CNC(=O)c1cnc2[nH]ccc2c1NC1CCCN(Cc2ccc(Cl)cc2)CC1"	"IC50"	"'='"	"44.3"	"nM"	"7.35"	""	""	""	"17.85"	"0.35"	"3.31"	"10.07"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL4750779"	""	"0"	"407.52"	"0"	"3.40"	"31d"	"CNC(=O)c1cnc2[nH]ccc2c1N[C@@H]1CCN(Cc2cccc(OC)c2)[C@@H](C)C1"	"IC50"	"'='"	"88.5"	"nM"	"7.05"	""	""	""	"17.31"	"0.32"	"3.65"	"8.57"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL4761365"	""	"0"	"411.94"	"0"	"4.04"	"31g"	"CNC(=O)c1cnc2[nH]ccc2c1N[C@@H]1CCN(Cc2ccc(Cl)cc2)[C@H](C)C1"	"IC50"	"'='"	"3.7"	"nM"	"8.43"	""	""	""	"20.47"	"0.40"	"4.39"	"11.54"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL3651031"	""	"0"	"400.85"	"0"	"4.05"	"BDBM153208"	"CCOC(=O)c1c[nH]c2ncnc(-c3cccc(Nc4nc(Cl)ns4)c3)c12"	"IC50"	"'='"	"109.0"	"nM"	"6.96"	""	"294156"	"UO_0000065"	"17.37"	"0.35"	"2.91"	"6.59"	"False"	"CHEMBL3707801"	"HTRF Assay: The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384- well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser.Subsequent reagent additions employed an Agilent Bravo. Next, 18 of 1.1 IX enzyme and 1.1 IX substrate in IX assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639146"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4639308"	""	"0"	"343.79"	"0"	"4.66"	"16b"	"CC(Oc1cc(-c2cccnc2)cnc1N)c1cc(F)ccc1Cl"	"IC50"	"'='"	"90.0"	"nM"	"7.05"	""	""	"UO_0000065"	"20.49"	"0.40"	"2.39"	"11.54"	"False"	"CHEMBL4628503"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4627317"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2020"	"None"	""
"CHEMBL3902770"	""	"0"	"403.45"	"0"	"2.32"	"BDBM198428"	"O=C1COc2ccc(CN3CCC(c4nnn5cnc6[nH]ccc6c45)CC3)cc2N1"	"IC50"	"'='"	"200.0"	"nM"	"6.70"	""	"352506"	"UO_0000065"	"16.60"	"0.30"	"4.38"	"6.67"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3923802"	""	"0"	"338.46"	"0"	"3.41"	"BDBM198487"	"c1cc2c(ncn3nnc([C@H]4CC[C@H](CNC5CCCC5)CC4)c23)[nH]1"	"IC50"	"'='"	"150.0"	"nM"	"6.82"	""	"352565"	"UO_0000065"	"20.16"	"0.37"	"3.41"	"9.62"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3905617"	""	"0"	"467.62"	"0"	"4.12"	"BDBM198538"	"CC(C)(C)OC(=O)N1CCC(CNC[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)CC1"	"IC50"	"'='"	"290.0"	"nM"	"6.54"	""	"352616"	"UO_0000065"	"13.98"	"0.26"	"2.42"	"6.51"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3921202"	""	"0"	"472.47"	"0"	"3.45"	"BDBM198549"	"O=C(NCC(O)(c1ccccc1)C(F)(F)F)[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"60.0"	"nM"	"7.22"	""	"352627"	"UO_0000065"	"15.29"	"0.29"	"3.77"	"6.67"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4285555"	""	"0"	"455.50"	"0"	"3.03"	"31"	"N#CN[C@H]1C[C@@H](NS(=O)(=O)c2cccc(C#N)c2)c2ccc(-c3ncnc4[nH]ccc34)cc21"	"IC50"	"'='"	"2419.0"	"nM"	"5.62"	""	""	"UO_0000065"	"12.33"	"0.23"	"2.59"	"3.81"	"False"	"CHEMBL4265556"	"Inhibition of recombinant human GST-tagged JAK2 using KAIETDKEYYTVKD-NH2 as substrate in presence of 1 mM ATP concentration by coupled PK/LDH assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4261650"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4113632"	""	"0"	"297.32"	"0"	"1.36"	"BDBM228889"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccccc3)n2)COC1"	"IC50"	"'='"	"241.0"	"nM"	"6.62"	""	"400636"	"UO_0000065"	"22.26"	"0.41"	"5.26"	"6.25"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3967557"	""	"0"	"469.52"	"0"	"4.32"	"BDBM228894"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(c2cncc3ccccc23)CC1"	"IC50"	"'='"	"414.0"	"nM"	"6.38"	""	"400641"	"UO_0000065"	"13.59"	"0.25"	"2.06"	"5.66"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3895654"	""	"0"	"443.49"	"0"	"3.65"	"BDBM228918"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(c2ccc(C#N)cc2)CC1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"400665"	"UO_0000065"	"19.22"	"0.35"	"4.87"	"6.89"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3977394"	""	"0"	"436.47"	"0"	"3.91"	"BDBM228919"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(c2cccc(F)c2)CC1"	"IC50"	"'='"	"24.0"	"nM"	"7.62"	""	"400666"	"UO_0000065"	"17.46"	"0.33"	"3.71"	"7.62"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL278041"	"SB-202190"	"0"	"331.35"	"0"	"4.65"	"SB202190"	"Oc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3363474"	"Inhibition of JAK2 (unknown origin) by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352554"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3314272"	""	"0"	"361.41"	"0"	"3.70"	"13"	"C#Cc1ccn2c(-c3ccnc(SC)n3)c(-c3ccc(F)cc3)nc2n1"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3363474"	"Inhibition of JAK2 (unknown origin) by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352554"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3314286"	""	"0"	"386.46"	"1"	"5.04"	"35"	"C#Cc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccnc(SC)n3)[nH]2)cc1"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3363474"	"Inhibition of JAK2 (unknown origin) by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352554"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3313935"	""	"0"	"397.34"	"0"	"3.94"	"26.Na"	"O=C([O-])c1ccc(-c2nc(-c3ccc(F)cc3)c(-c3cc[nH]c(=O)c3)[nH]2)cc1.[Na+]"	"IC50"	"'='"	"274.0"	"nM"	"6.56"	""	""	"UO_0000065"	"17.48"	"0.32"	"2.62"	"6.64"	"False"	"CHEMBL3363474"	"Inhibition of JAK2 (unknown origin) by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352554"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3314283"	""	"0"	"338.39"	"0"	"3.04"	"30"	"O=c1cc(-c2[nH]c(C3CCNCC3)nc2-c2ccc(F)cc2)cc[nH]1"	"IC50"	"'='"	"6620.0"	"nM"	"5.18"	""	""	"UO_0000065"	"15.31"	"0.28"	"2.14"	"7.04"	"False"	"CHEMBL3363474"	"Inhibition of JAK2 (unknown origin) by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352554"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3120963"	""	"0"	"364.38"	"0"	"2.54"	"4"	"Cn1c(-c2cn(CCO)nn2)nc(-c2ccc(F)cc2)c1-c1ccncc1"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3363474"	"Inhibition of JAK2 (unknown origin) by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352554"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3647858"	""	"0"	"437.42"	"0"	"2.72"	"BDBM147968"	"C[C@](O)(c1ccc(Nc2nn([C@H]3CC[C@H](O)C[C@@H]3C#N)cc2C(N)=O)cc1)C(F)(F)F"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"285902"	"UO_0000065"	"19.89"	"0.38"	"5.98"	"6.34"	"False"	"CHEMBL3707623"	"HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638646"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3652331"	""	"0"	"421.57"	"0"	"2.39"	"BDBM113142"	"CO[C@@H]1CCCN(S(=O)(=O)C[C@H]2CC[C@H](N(C)c3ncnc4[nH]ccc34)CC2)C1"	"IC50"	"'='"	"23.7"	"nM"	"7.62"	""	"234585"	"UO_0000065"	"18.09"	"0.36"	"5.24"	"8.34"	"False"	"CHEMBL3707948"	"Enzymatic Assay: A peptide mobility shift assay was used to quantify the phosphorylation of the JAKtide (JAK2 and JAK3) or the IRS-1 peptide (JAK1 and Tyk2). Reactions were carried out in a 384-well plate (Matrical MP-101) in a 10 L total volume. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween-20, ATP (4 M for JAK2 and JAK3, 40 M for JAK1 and 7 M for Tyk2)), 2% DMSO and 1 M peptide substrate (JAKtide for JAK2 and JAK3 and IRS-1 peptide for JAK1 and Tyk2). Compounds were diluted serially in 100% dimethyl sulfoxide and tested in an 11 point dose response in duplicate or quadruplicate (200 nl of compound/DMSO was added per 10 L reaction). The reactions were initiated by the addition of enzyme to the final concentration of 2 nM JAK2, 1 nM JAK3, 12 nM Tyk2 or 20 nM JAK1. The assay was run for 240 minutes for JAK1, 150 minutes for JAK2, 90 minutes for JAK3 and 70 minutes for Tyk2."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3639159"	"37"	"BindingDB Database"	""	"2014"	"None"	""
"CHEMBL3645020"	""	"0"	"468.54"	"0"	"4.22"	"BDBM99772"	"CN1CCN(c2cccc(Nc3nc4c(-c5cnn(-c6ccc(F)cc6)c5)cccn4n3)c2)CC1"	"IC50"	"'='"	"5.64"	"nM"	"8.25"	""	"216459"	"UO_0000065"	"17.61"	"0.32"	"4.03"	"12.40"	"False"	"CHEMBL3707950"	"In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3638802"	"37"	"BindingDB Database"	""	"2013"	"None"	""
"CHEMBL3262623"	""	"0"	"422.92"	"0"	"4.48"	"10b"	"N[C@H]1CCCC[C@H]1Nc1cc2cc[nH]c(=O)c2c(Nc2cccc3c(Cl)c[nH]c23)n1"	"IC50"	"'='"	"1225.0"	"nM"	"5.91"	""	""	"UO_0000065"	"13.98"	"0.27"	"1.43"	"5.30"	"False"	"CHEMBL3268711"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3259804"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3655095"	""	"0"	"335.43"	"0"	"1.25"	"29"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)CC2CC2)C1"	"IC50"	"'='"	"1196.0"	"nM"	"5.92"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3314273"	""	"0"	"484.45"	"0"	"3.06"	"15"	"CSc1nccc(-c2c(-c3ccc(F)cc3)nc3nc(-c4cn(CC(=O)[O-])nn4)ccn23)n1.[Na+]"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3363474"	"Inhibition of JAK2 (unknown origin) by radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352554"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL4648820"	""	"0"	"282.35"	"0"	"2.60"	"42"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3C[C@H]4C[C@@H]3C[C@H]4CC#N)c12"	"IC50"	"'>'"	"43000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL4642642"	""	"0"	"455.21"	"None"	"None"	"14h"	"C=CC(=O)Nc1cccc(Nc2nc(Nc3ccc4c(c3)COB4O)ncc2C(F)(F)F)c1"	"IC50"	"'='"	"657.9"	"nM"	"6.18"	""	""	"UO_0000065"	"13.58"	"None"	"None"	"None"	"False"	"CHEMBL4610789"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using Ulight-Poly GT as substrate incubated for 2 hrs by Lanthascreen TR-FRET assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610007"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2020"	"None"	""
"CHEMBL4648837"	""	"0"	"455.21"	"None"	"None"	"14a; 9"	"C=CC(=O)Nc1cccc(Nc2nc(Nc3ccc4c(c3)B(O)OC4)ncc2C(F)(F)F)c1"	"IC50"	"'='"	"971.6"	"nM"	"6.01"	""	""	"UO_0000065"	"13.21"	"None"	"None"	"None"	"False"	"CHEMBL4610789"	"Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using Ulight-Poly GT as substrate incubated for 2 hrs by Lanthascreen TR-FRET assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610007"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2020"	"None"	""
"CHEMBL4639606"	""	"0"	"418.54"	"0"	"4.24"	"37"	"Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](CC(=O)N4CCC(c5ccccc5)C4)CC3)c12"	"IC50"	"'='"	"2400.0"	"nM"	"5.62"	""	""	"UO_0000065"	"13.43"	"0.25"	"1.38"	"6.87"	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL4648612"	""	"0"	"257.34"	"0"	"2.85"	"13"	"Cc1[nH]nc2[nH]c(=O)cc(C3CC4CCC3CC4)c12"	"IC50"	"'='"	"9100.0"	"nM"	"5.04"	""	""	"UO_0000065"	"19.59"	"0.36"	"2.19"	"8.19"	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL4645613"	""	"0"	"243.31"	"0"	"2.46"	"11"	"Cc1[nH]nc2[nH]c(=O)cc([C@@H]3C[C@H]4CC[C@@H]3C4)c12"	"IC50"	"'>'"	"40000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4612628"	"Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"TF-1"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4610114"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"CHEMBL3307972"	""
"CHEMBL3980335"	""	"0"	"518.59"	"2"	"5.17"	"BDBM229047"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3cccc(-c4ccccc4F)c3)n2)CC1"	"IC50"	"'='"	"841.0"	"nM"	"6.08"	""	"400792"	"UO_0000065"	"11.71"	"0.22"	"0.91"	"4.81"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4279986"	""	"0"	"387.49"	"0"	"4.84"	"64e"	"CC(=O)Nc1ccc(-c2ccnc(Nc3ccc(N4CCCCC4)cc3)n2)cc1"	"IC50"	"'='"	"2.9"	"nM"	"8.54"	""	""	"UO_0000065"	"22.03"	"0.40"	"3.70"	"12.17"	"False"	"CHEMBL4268221"	"Inhibition of human JAK2 using poly(Glu:Tyr)(4:1) as substrate preincubated for 20 mins followed by [gamma33P]ATP addition measured after 120 mins by ion exchange filter paper method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4265943"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2018"	"None"	""
"CHEMBL3965345"	""	"0"	"444.47"	"0"	"2.29"	"BDBM227819"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3cc(F)ncn3)n2)CC1"	"IC50"	"'='"	"16.0"	"nM"	"7.80"	""	"400781"	"UO_0000065"	"17.54"	"0.33"	"5.51"	"5.13"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3924664"	""	"0"	"519.61"	"1"	"4.64"	"BDBM229037"	"Cc1noc(C)c1-c1ccc(Nc2nn(C3(CC#N)CCN(C(=O)OC(C)(C)C)CC3)cc2C(N)=O)cc1"	"IC50"	"'='"	"38.0"	"nM"	"7.42"	""	"400782"	"UO_0000065"	"14.28"	"0.27"	"2.78"	"4.87"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3903164"	""	"0"	"440.51"	"0"	"2.46"	"BDBM229033"	"Cc1cncc(Nc2nn(C3(CC#N)CCN(C(=O)OC(C)(C)C)CC3)cc2C(N)=O)n1"	"IC50"	"'='"	"176.0"	"nM"	"6.75"	""	"400777"	"UO_0000065"	"15.33"	"0.29"	"4.29"	"4.44"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3975255"	""	"0"	"414.52"	"0"	"3.34"	"BDBM198429"	"CN(CCC#N)c1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'>'"	"1000.0"	"nM"	""	""	"352507"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3896461"	""	"0"	"354.46"	"0"	"2.34"	"BDBM198474"	"OC1CCN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)CC1"	"IC50"	"'='"	"63.0"	"nM"	"7.20"	""	"352552"	"UO_0000065"	"20.31"	"0.38"	"4.86"	"8.75"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3907394"	""	"0"	"386.50"	"0"	"2.47"	"BDBM198529"	"COCCN(CCOC)C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"310.0"	"nM"	"6.51"	""	"352607"	"UO_0000065"	"16.84"	"0.32"	"4.04"	"8.08"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3907565"	""	"0"	"350.40"	"0"	"3.88"	"BDBM198585"	"Fc1ccc(N[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)cc1"	"IC50"	"'='"	"57.0"	"nM"	"7.24"	""	"352663"	"UO_0000065"	"20.67"	"0.38"	"3.36"	"10.22"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4109724"	""	"0"	"310.36"	"0"	"1.28"	"BDBM229060"	"CN1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"1481.0"	"nM"	"5.83"	""	"400796"	"UO_0000065"	"18.78"	"0.35"	"4.55"	"5.83"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3968579"	""	"0"	"362.40"	"0"	"1.25"	"BDBM228793"	"CN(c1ccc(-c2nn[nH]n2)cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399732"	"UO_0000065"	"25.55"	"0.47"	"8.01"	"8.02"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3911946"	""	"0"	"445.50"	"0"	"3.48"	"BDBM228796"	"CN(C(=O)c1ccc(N(C)[C@@H]2CCN(c3ncnc4[nH]ccc34)C2)nc1)c1ccc(F)cc1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399735"	"UO_0000065"	"20.78"	"0.38"	"5.78"	"11.40"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3928129"	""	"0"	"457.56"	"0"	"1.53"	"BDBM228708"	"CN(c1ccc(S(=O)(=O)NC2CCOCC2)cn1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399743"	"UO_0000065"	"20.24"	"0.40"	"7.73"	"7.96"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3984895"	""	"0"	"451.41"	"0"	"2.52"	"BDBM229013"	"N#CCC1(n2cc(C(N)=O)c(Nc3cccnc3)n2)CCN(C(=O)OCC(F)(F)F)CC1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"400758"	"UO_0000065"	"18.60"	"0.36"	"5.88"	"6.03"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3927070"	""	"0"	"426.48"	"0"	"2.16"	"BDBM229026"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccncn3)n2)CC1"	"IC50"	"'='"	"139.0"	"nM"	"6.86"	""	"400770"	"UO_0000065"	"16.08"	"0.30"	"4.70"	"4.51"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3976587"	""	"0"	"336.44"	"0"	"3.02"	"BDBM198519"	"c1cc2c(ncn3nnc([C@H]4CC[C@H](CNC56CC(C5)C6)CC4)c23)[nH]1"	"IC50"	"'='"	"99.0"	"nM"	"7.00"	""	"352597"	"UO_0000065"	"20.82"	"0.38"	"3.98"	"9.88"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3906210"	""	"0"	"312.42"	"0"	"2.88"	"BDBM198534"	"CC(C)NC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"54.0"	"nM"	"7.27"	""	"352612"	"UO_0000065"	"23.26"	"0.43"	"4.39"	"10.25"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3935408"	""	"0"	"292.35"	"0"	"3.10"	"BDBM198645"	"CC(C#N)=C1CCC(c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"55.0"	"nM"	"7.26"	""	"352723"	"UO_0000065"	"24.83"	"0.45"	"4.16"	"8.78"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3889920"	""	"0"	"337.39"	"0"	"1.91"	"BDBM198654"	"N#CCNC(=O)C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"30.0"	"nM"	"7.52"	""	"352732"	"UO_0000065"	"22.30"	"0.41"	"5.61"	"6.73"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4534573"	""	"0"	"378.43"	"0"	"2.86"	"34"	"CCc1cc(O)c(F)cc1-c1cc(NS(=O)(=O)N(C)C)c2cn[nH]c2c1"	"IC50"	"'='"	"6.31"	"nM"	"8.20"	""	""	"UO_0000065"	"21.67"	"0.43"	"5.34"	"8.34"	"False"	"CHEMBL4478762"	"Inhibition of human His-tagged JAK2 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4477220"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2016"	"None"	""
"CHEMBL4543715"	""	"0"	"379.41"	"0"	"2.37"	"26"	"CCc1cc(O)c(F)cc1-c1cc(NS(=O)(=O)CCO)c2cn[nH]c2c1"	"IC50"	"'='"	"19.95"	"nM"	"7.70"	""	""	"UO_0000065"	"20.29"	"0.40"	"5.33"	"6.68"	"False"	"CHEMBL4478762"	"Inhibition of human His-tagged JAK2 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4477220"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2016"	"None"	""
"CHEMBL4580425"	""	"0"	"403.48"	"0"	"4.18"	"23"	"CCc1cc(O)c(F)cc1-c1cc(NS(=O)(=O)CC2CCC2)c2cn[nH]c2c1"	"IC50"	"'='"	"19.95"	"nM"	"7.70"	""	""	"UO_0000065"	"19.08"	"0.38"	"3.52"	"8.10"	"False"	"CHEMBL4478762"	"Inhibition of human His-tagged JAK2 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4477220"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2016"	"None"	""
"CHEMBL4554460"	""	"0"	"375.43"	"0"	"3.54"	"22"	"CCc1cc(O)c(F)cc1-c1cc(NS(=O)(=O)C2CC2)c2cn[nH]c2c1"	"IC50"	"'='"	"10.0"	"nM"	"8.00"	""	""	"UO_0000065"	"21.31"	"0.42"	"4.46"	"8.41"	"False"	"CHEMBL4478762"	"Inhibition of human His-tagged JAK2 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4477220"	"1"	"Scientific Literature"	"ACS Med Chem Lett"	"2016"	"None"	""
"CHEMBL4457210"	""	"0"	"517.66"	"1"	"4.33"	"17a"	"CC(=O)c1ccc(NC(=O)N2CCN(c3ccnc(Nc4ccc(N5CCSCC5)cc4)n3)CC2)cc1"	"IC50"	"'='"	"29.8"	"nM"	"7.53"	""	""	"UO_0000065"	"14.54"	"0.28"	"3.20"	"8.03"	"False"	"CHEMBL4362531"	"Inhibition of N-terminal His-tagged human JAK2 catalytic domain (826 to 1132 resiudes) expressed in baculovirus expression system using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition measured after 1 hr in presence of ATP by mobility shift assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4359878"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2019"	"None"	""
"CHEMBL4227007"	""	"0"	"553.65"	"1"	"4.68"	"17"	"CCNC(=O)c1cc2c(-c3cccc(OCCCCn4cc(-c5ncnc6[nH]ccc56)cn4)c3)nc(N)nc2s1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4222523"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma33P]-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219149"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2018"	"None"	""
"CHEMBL4226547"	""	"0"	"650.60"	"2"	"6.77"	"27"	"CCNC(=O)c1cc2c(-c3cc(OCCCCCCn4cc(-c5ncnc6[nH]ccc56)cn4)c(Cl)cc3Cl)nc(N)nc2s1"	"IC50"	"'='"	"1710.0"	"nM"	"5.77"	""	""	"UO_0000065"	"8.86"	"0.18"	"-1.00"	"3.86"	"False"	"CHEMBL4222523"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma33P]-ATP"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219149"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2018"	"None"	""
"CHEMBL4227082"	""	"0"	"388.46"	"0"	"3.61"	"12h"	"Cc1cn2c(-c3cn[nH]c3)cnc2c(Nc2cc(Cc3ccccn3)ns2)n1"	"IC50"	"'>'"	"500.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4222462"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4219148"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2018"	"None"	""
"CHEMBL3655086"	""	"0"	"351.43"	"0"	"0.49"	"36"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)CC2COC2)C1"	"IC50"	"'='"	"933.0"	"nM"	"6.03"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4077614"	""	"0"	"364.48"	"0"	"1.25"	"39"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)N2CCCCC2)C1"	"IC50"	"'='"	"437.0"	"nM"	"6.36"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4071850"	""	"0"	"324.41"	"0"	"0.37"	"11"	"CCNS(=O)(=O)N[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4085011"	""	"0"	"371.47"	"0"	"2.04"	"10"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)Cc2ccccc2)C1"	"IC50"	"'='"	"1990.0"	"nM"	"5.70"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3655097"	""	"0"	"350.45"	"0"	"0.76"	"14"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)NCC2CC2)C1"	"IC50"	"'='"	"1090.0"	"nM"	"5.96"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4066876"	""	"0"	"349.46"	"0"	"1.50"	"24"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](CS(=O)(=O)NCC2CC2)C1"	"IC50"	"'='"	"199.0"	"nM"	"6.70"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4128181"	""	"0"	"428.50"	"0"	"4.67"	"23; FM-381"	"CN(C)C(=O)C(C#N)=Cc1ccc(-c2nc3cnc4[nH]ccc4c3n2C2CCCCC2)o1"	"IC50"	"'='"	"346.0"	"nM"	"6.46"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4124183"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate in presence of 10 uM [gamma33P]ATP by radiometric method"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4118225"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4786783"	""	"0"	"292.30"	"0"	"1.11"	"66"	"C#Cc1nc(Nc2cccc(CC(N)=O)c2)nc2[nH]cnc12"	"IC50"	"'='"	"220.0"	"nM"	"6.66"	""	""	""	"22.78"	"0.41"	"5.55"	"6.08"	"False"	"CHEMBL4700137"	"Inhibition of human JAK2 by kinase-profiling analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4699418"	"1"	"Scientific Literature"	"RSC Med Chem"	"2020"	"None"	""
"CHEMBL4740191"	""	"0"	"364.41"	"0"	"2.59"	"21"	"C/C=C/C(=O)Nc1cccc(-c2cc(Nc3cnn(CCO)c3)ncn2)c1"	"IC50"	"'='"	"2808.0"	"nM"	"5.55"	""	""	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL4795109"	""	"0"	"472.55"	"0"	"3.35"	"27"	"C/C=C/C(=O)NCC(=O)Nc1cccc(-c2cc(Nc3ccc(N4CCOCC4)cc3)ncn2)c1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL4741588"	""	"0"	"377.41"	"0"	"2.58"	"16"	"COCCn1cc(Nc2cc(-c3cccc(NC(=O)CC#N)c3)ncn2)cn1"	"IC50"	"'='"	"587.0"	"nM"	"6.23"	""	""	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL4796206"	""	"0"	"458.52"	"0"	"2.96"	"26"	"C=CC(=O)NCC(=O)Nc1cccc(-c2cc(Nc3ccc(N4CCOCC4)cc3)ncn2)c1"	"IC50"	"'>'"	"3000.0"	"nM"	""	""	""	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL4755671"	""	"0"	"377.41"	"0"	"2.58"	"33"	"COCCn1cc(Nc2cc(-c3ccc(NC(=O)CC#N)cc3)ncn2)cn1"	"IC50"	"'='"	"1459.0"	"nM"	"5.84"	""	""	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL3968473"	""	"0"	"469.55"	"0"	"2.81"	"BDBM228972"	"CC(O)c1ccc(Nc2nn(C3(CC#N)CCN(C(=O)OC(C)(C)C)CC3)cc2C(N)=O)cn1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"400717"	"UO_0000065"	"18.53"	"0.35"	"5.89"	"5.46"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3918875"	""	"0"	"369.43"	"0"	"3.35"	"BDBM198433"	"N#C/C(=C\N1CCC(c2nnn3cnc4[nH]ccc4c23)CC1)c1ccccc1"	"IC50"	"'='"	"130.0"	"nM"	"6.89"	""	"352511"	"UO_0000065"	"18.64"	"0.34"	"3.54"	"8.02"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3965217"	""	"0"	"425.42"	"0"	"3.88"	"BDBM198447"	"N#Cc1ccc(CN2CCC(c3nnn4cnc5[nH]ccc5c34)CC2)cc1C(F)(F)F"	"IC50"	"'='"	"38.0"	"nM"	"7.42"	""	"352525"	"UO_0000065"	"17.44"	"0.33"	"3.54"	"8.64"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3955720"	""	"0"	"309.38"	"0"	"1.99"	"BDBM198462"	"N#CCNC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"8.1"	"nM"	"8.09"	""	"352540"	"UO_0000065"	"26.15"	"0.48"	"6.10"	"8.55"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3963443"	""	"0"	"310.41"	"0"	"2.63"	"BDBM198483"	"c1cc2c(ncn3nnc([C@H]4CC[C@H](CNC5CC5)CC4)c23)[nH]1"	"IC50"	"'='"	"62.0"	"nM"	"7.21"	""	"352561"	"UO_0000065"	"23.22"	"0.43"	"4.58"	"10.17"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3985390"	""	"0"	"328.40"	"0"	"2.53"	"BDBM198541"	"FC1CN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C1"	"IC50"	"'='"	"60.0"	"nM"	"7.22"	""	"352619"	"UO_0000065"	"21.99"	"0.41"	"4.69"	"11.63"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4107287"	""	"0"	"396.45"	"0"	"2.59"	"BDBM228872"	"CC(C)(C)OC(=O)N1CC(CC#N)(n2cc(C(N)=O)c(Nc3ccccc3)n2)C1"	"IC50"	"'='"	"57.0"	"nM"	"7.24"	""	"400619"	"UO_0000065"	"18.27"	"0.34"	"4.65"	"5.74"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3935508"	""	"0"	"585.69"	"1"	"2.24"	"BDBM228875"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(C(=O)N4CCS(=O)(=O)CC4)cc3)n2)CC1"	"IC50"	"'='"	"1.0"	"nM"	"9.00"	""	"400622"	"UO_0000065"	"15.37"	"0.30"	"6.76"	"4.98"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3916939"	""	"0"	"488.57"	"0"	"2.38"	"BDBM228885"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(S(C)(=O)=O)cc3)n2)C1"	"IC50"	"'='"	"2.0"	"nM"	"8.70"	""	"400632"	"UO_0000065"	"17.80"	"0.35"	"6.32"	"5.42"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3900124"	""	"0"	"500.60"	"2"	"5.03"	"BDBM229040"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3cccc(-c4ccccc4)c3)n2)CC1"	"IC50"	"'='"	"1050.0"	"nM"	"5.98"	""	"400785"	"UO_0000065"	"11.94"	"0.22"	"0.95"	"4.73"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4572373"	""	"0"	"379.42"	"0"	"2.15"	"11b"	"C=CC(=O)Nc1cccc(CNc2cc(Nc3cnn(CCO)c3)ncn2)c1"	"IC50"	"'>'"	"3000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4482009"	"Inhibition of human JAK2 using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and further incubated for 30 mins and subsequently measured after 1 hr by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480445"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL3953229"	""	"0"	"362.44"	"0"	"2.76"	"BDBM198583"	"N#CCCN(CCC#N)C1CCC(c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"2.5"	"nM"	"8.60"	""	"352661"	"UO_0000065"	"23.73"	"0.44"	"5.84"	"7.84"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3980120"	""	"0"	"406.46"	"0"	"4.15"	"BDBM198622"	"FC(F)(F)CN(CC1CC1)C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"95.0"	"nM"	"7.02"	""	"352700"	"UO_0000065"	"17.28"	"0.33"	"2.87"	"11.31"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4292341"	""	"0"	"381.44"	"0"	"3.84"	"35"	"N#CN[C@H]1CCc2ccc(-c3ncnc4[nH]cc(-c5cccc(CO)c5)c34)cc21"	"IC50"	"'>'"	"9925.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4265556"	"Inhibition of recombinant human GST-tagged JAK2 using KAIETDKEYYTVKD-NH2 as substrate in presence of 1 mM ATP concentration by coupled PK/LDH assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4261650"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4085457"	"PF-06651600"	"3"	"285.35"	"0"	"1.94"	"PF-06651600; 6"	"C=CC(=O)N1C[C@H](Nc2ncnc3[nH]ccc23)CC[C@@H]1C"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"True"	"CHEMBL4265556"	"Inhibition of recombinant human GST-tagged JAK2 using KAIETDKEYYTVKD-NH2 as substrate in presence of 1 mM ATP concentration by coupled PK/LDH assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4261650"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4284388"	""	"0"	"576.53"	"0"	"3.85"	"45a"	"CC(=O)Nc1ccc(-c2ccnc(Nc3cccc(NC(=O)CCCCC(=O)NO)c3)n2)cc1.O=C(O)C(F)(F)F"	"IC50"	"'='"	"2.6"	"nM"	"8.59"	""	""	"UO_0000065"	"18.56"	"0.34"	"4.74"	"5.91"	"False"	"CHEMBL4268221"	"Inhibition of human JAK2 using poly(Glu:Tyr)(4:1) as substrate preincubated for 20 mins followed by [gamma33P]ATP addition measured after 120 mins by ion exchange filter paper method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4265943"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2018"	"None"	""
"CHEMBL4289006"	""	"0"	"545.69"	"1"	"4.73"	"74b"	"Cc1cnc(Nc2ccc(N3CCN(C)CC3)cc2)nc1-c1ccc(NC(=O)CCCCCCC(=O)NO)cc1"	"IC50"	"'='"	"4.3"	"nM"	"8.37"	""	""	"UO_0000065"	"15.33"	"0.29"	"3.64"	"6.82"	"False"	"CHEMBL4268221"	"Inhibition of human JAK2 using poly(Glu:Tyr)(4:1) as substrate preincubated for 20 mins followed by [gamma33P]ATP addition measured after 120 mins by ion exchange filter paper method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4265943"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2018"	"None"	""
"CHEMBL3906967"	""	"0"	"271.32"	"0"	"1.87"	"BDBM198202"	"OC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"19.0"	"nM"	"7.72"	""	"351824"	"UO_0000065"	"28.46"	"0.53"	"5.85"	"9.76"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3914684"	""	"0"	"433.49"	"0"	"3.48"	"BDBM228921"	"Cc1ncccc1N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CC1"	"IC50"	"'='"	"209.0"	"nM"	"6.68"	""	"400668"	"UO_0000065"	"15.41"	"0.29"	"3.20"	"5.92"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3899162"	""	"0"	"419.46"	"0"	"3.17"	"BDBM228922"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(c2cccnc2)CC1"	"IC50"	"'='"	"6.0"	"nM"	"8.22"	""	"400669"	"UO_0000065"	"19.60"	"0.36"	"5.05"	"7.28"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3971438"	""	"0"	"450.49"	"0"	"4.22"	"BDBM228924"	"Cc1ccc(F)cc1N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CC1"	"IC50"	"'>'"	"1496.0"	"nM"	""	""	"400671"	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3892955"	""	"0"	"419.46"	"0"	"3.17"	"BDBM228938"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(F)cc3)n2)CCN(c2ccncc2)CC1"	"IC50"	"'='"	"78.0"	"nM"	"7.11"	""	"400685"	"UO_0000065"	"16.95"	"0.31"	"3.94"	"6.30"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4526018"	""	"0"	"349.40"	"0"	"2.69"	"11a'"	"C=CC(=O)Nc1ccc(CNc2cc(Nc3cnn(C)c3)ncn2)cc1"	"IC50"	"'>'"	"3000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4482009"	"Inhibition of human JAK2 using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and further incubated for 30 mins and subsequently measured after 1 hr by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480445"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"Tofacitinib"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"0.5"	"nM"	"9.30"	""	""	"UO_0000065"	"29.77"	"0.55"	"7.76"	"10.46"	"False"	"CHEMBL4482009"	"Inhibition of human JAK2 using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and further incubated for 30 mins and subsequently measured after 1 hr by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480445"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4555932"	""	"0"	"456.55"	"0"	"3.44"	"14e'"	"CN1CCN(c2ccc(Nc3cc(NCc4ccc(NC(=O)CC#N)cc4)ncn3)cc2)CC1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4482009"	"Inhibition of human JAK2 using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and further incubated for 30 mins and subsequently measured after 1 hr by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4480445"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4282878"	""	"0"	"291.31"	"0"	"2.52"	"18"	"N#CN[C@@H]1CCOc2ccc(-c3ncnc4[nH]ccc34)cc21"	"IC50"	"'='"	"470.0"	"nM"	"6.33"	""	""	"UO_0000065"	"21.72"	"0.39"	"3.81"	"7.31"	"False"	"CHEMBL4265556"	"Inhibition of recombinant human GST-tagged JAK2 using KAIETDKEYYTVKD-NH2 as substrate in presence of 1 mM ATP concentration by coupled PK/LDH assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4261650"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3234877"	""	"0"	"343.84"	"0"	"4.61"	"20"	"Cc1cccc(Nc2sc(-c3cccc(Cl)c3)cc2C(N)=O)n1"	"IC50"	"'='"	"312.0"	"nM"	"6.51"	""	""	"UO_0000065"	"18.92"	"0.39"	"1.90"	"9.57"	"False"	"CHEMBL3239499"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3232939"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL4092805"	""	"0"	"309.40"	"0"	"0.86"	"6"	"CCS(=O)(=O)N[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'>'"	"3310.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4741778"	""	"0"	"433.56"	"0"	"4.45"	"13j"	"CCCNC(=O)N1CCc2cc(Nc3ncc(C)c(-c4cnn(C(C)C)c4)n3)ccc2C1"	"IC50"	"'='"	"1760.0"	"nM"	"5.75"	""	""	""	"13.27"	"0.25"	"1.30"	"6.54"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL4745529"	""	"0"	"438.55"	"0"	"4.32"	"13n"	"CC(C)n1cc(-c2nc(Nc3ccc4c(c3)CCN(CCCCCO)C4)ncc2F)cn1"	"IC50"	"'='"	"492.0"	"nM"	"6.31"	""	""	""	"14.38"	"0.27"	"1.99"	"7.97"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL4790747"	""	"0"	"434.59"	"0"	"4.49"	"13p"	"Cc1cnc(Nc2ccc3c(c2)CCN(CCCCCO)C3)nc1-c1cnn(C(C)C)c1"	"IC50"	"'='"	"312.0"	"nM"	"6.51"	""	""	""	"14.97"	"0.28"	"2.02"	"8.22"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL4754856"	""	"0"	"446.56"	"0"	"4.06"	"13x"	"COC(=O)/C=C/CN1CCc2cc(Nc3ncc(C)c(-c4cnn(C(C)C)c4)n3)ccc2C1"	"IC50"	"'='"	"13.7"	"nM"	"7.86"	""	""	""	"17.61"	"0.33"	"3.80"	"9.23"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL4079179"	""	"0"	"391.42"	"0"	"2.19"	"32"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)CCCC(F)(F)F)C1"	"IC50"	"'='"	"489.0"	"nM"	"6.31"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4753549"	""	"0"	"459.60"	"0"	"3.98"	"13ac"	"Cc1cnc(Nc2ccc3c(c2)CCN(C(=O)/C=C/CN(C)C)C3)nc1-c1cnn(C(C)C)c1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	""	"18.54"	"0.34"	"4.54"	"10.76"	"False"	"CHEMBL4723820"	"Inhibition of recombinant human JAK2 (808 to end residues) KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate measured after 40 mins in presence of [gamm33P]ATP by scintillation counting method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 0.6667 hr"
"CHEMBL4079179"	""	"0"	"391.42"	"0"	"2.19"	"32"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)CCCC(F)(F)F)C1"	"IC50"	"'>'"	"20000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3655104"	""	"0"	"363.45"	"0"	"0.60"	"40"	"CN(CCC#N)S(=O)(=O)N[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"4460.0"	"nM"	"5.35"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3937439"	""	"0"	"337.36"	"0"	"2.08"	"BDBM228792"	"CN(c1ncc(C#N)cc1F)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399731"	"UO_0000065"	"27.45"	"0.51"	"7.18"	"10.93"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3983423"	""	"0"	"443.48"	"0"	"2.90"	"BDBM229029"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(F)cn3)n2)CC1"	"IC50"	"'='"	"183.0"	"nM"	"6.74"	""	"400773"	"UO_0000065"	"15.19"	"0.29"	"3.84"	"4.84"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3900832"	""	"0"	"455.52"	"0"	"2.77"	"BDBM229034"	"COc1cccc(Nc2nn(C3(CC#N)CCN(C(=O)OC(C)(C)C)CC3)cc2C(N)=O)n1"	"IC50"	"'='"	"186.0"	"nM"	"6.73"	""	"400778"	"UO_0000065"	"14.78"	"0.28"	"3.96"	"4.54"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3924625"	""	"0"	"397.28"	"0"	"3.31"	"BDBM228788"	"CN(c1ccc(C#N)cc1Br)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399726"	"UO_0000065"	"23.31"	"0.51"	"5.95"	"12.89"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3890129"	""	"0"	"451.48"	"0"	"3.62"	"BDBM228948"	"Cc1cc(N2CCC(CC#N)(n3cc(C(N)=O)c(Nc4ccc(F)cc4)n3)CC2)cnc1F"	"IC50"	"'='"	"23.0"	"nM"	"7.64"	""	"400695"	"UO_0000065"	"16.92"	"0.32"	"4.02"	"6.77"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3985138"	""	"0"	"440.51"	"0"	"2.34"	"BDBM228979"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccnc(N)c3)n2)CC1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"400724"	"UO_0000065"	"19.35"	"0.36"	"6.18"	"5.16"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3930265"	""	"0"	"460.49"	"0"	"3.64"	"BDBM228993"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(F)c(F)c3)n2)CC1"	"IC50"	"'='"	"24.0"	"nM"	"7.62"	""	"400738"	"UO_0000065"	"16.55"	"0.32"	"3.98"	"6.03"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3942252"	""	"0"	"582.48"	"1"	"3.42"	"BDBM229008"	"N#CCC1(n2cc(C(N)=O)c(Nc3ccc(S(=O)(=O)C(F)(F)F)cc3)n2)CCN(C(=O)OCC(F)(F)F)CC1"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	"400753"	"UO_0000065"	"14.42"	"0.29"	"4.98"	"5.24"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3892613"	""	"0"	"530.51"	"1"	"3.53"	"BDBM229011"	"Cn1cc(-c2cccc(Nc3nn(C4(CC#N)CCN(C(=O)OCC(F)(F)F)CC4)cc3C(N)=O)c2)cn1"	"IC50"	"'='"	"21.0"	"nM"	"7.68"	""	"400756"	"UO_0000065"	"14.47"	"0.28"	"4.15"	"5.33"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3912678"	""	"0"	"510.60"	"1"	"2.60"	"BDBM229022"	"CC(C)(C)OC(=O)N1CCC(CC#N)(n2cc(C(N)=O)c(Nc3ccc(N4CCOCC4)nc3)n2)CC1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	"400766"	"UO_0000065"	"16.69"	"0.31"	"5.92"	"5.62"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3927951"	""	"0"	"454.54"	"0"	"2.77"	"BDBM229035"	"Cc1cc(Nc2nn(C3(CC#N)CCN(C(=O)OC(C)(C)C)CC3)cc2C(N)=O)nc(C)n1"	"IC50"	"'='"	"178.0"	"nM"	"6.75"	""	"400779"	"UO_0000065"	"14.85"	"0.28"	"3.98"	"4.44"	"False"	"CHEMBL3888429"	"HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer # PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886705"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3907774"	""	"0"	"359.46"	"0"	"2.46"	"BDBM198569"	"O=S(=O)(C[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1)C1CC1"	"IC50"	"'='"	"28.0"	"nM"	"7.55"	""	"352647"	"UO_0000065"	"21.01"	"0.41"	"5.09"	"8.12"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL4111044"	""	"0"	"296.34"	"0"	"3.19"	"BDBM198572"	"[N-]=[N+]=NC[C@H]1CC[C@H](c2nnn3cnc4[nH]ccc4c23)CC1"	"IC50"	"'='"	"1.7"	"nM"	"8.77"	""	"352650"	"UO_0000065"	"29.59"	"0.54"	"5.58"	"8.15"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3977129"	""	"0"	"340.43"	"0"	"1.95"	"BDBM198629"	"CC1(O)CN(C[C@H]2CC[C@H](c3nnn4cnc5[nH]ccc5c34)CC2)C1"	"IC50"	"'='"	"51.0"	"nM"	"7.29"	""	"352707"	"UO_0000065"	"21.42"	"0.40"	"5.34"	"8.86"	"False"	"CHEMBL3887758"	"Enzyme Assay: JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd. (PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH7.5, 1 mM EGTA, 1 mM MgCl2, 2 mM DTT, 0.01% Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 μM, and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ethylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS."	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886441"	"37"	"BindingDB Database"	""	"2015"	"None"	""
"CHEMBL3982255"	""	"0"	"401.50"	"0"	"1.83"	"BDBM228761"	"CCS(=O)(=O)Nc1ccc(N(C)[C@@H]2CCN(c3ncnc4[nH]ccc34)C2)nc1"	"IC50"	"'='"	"0.055"	"nM"	"10.26"	""	"399692"	"UO_0000065"	"25.55"	"0.50"	"8.43"	"9.58"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL3960213"	""	"0"	"361.41"	"0"	"2.57"	"BDBM228768"	"CN(C(=O)Nc1ccc(C#N)cc1)[C@@H]1CCN(c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"0.55"	"nM"	"9.26"	""	"399703"	"UO_0000065"	"25.62"	"0.47"	"6.69"	"9.17"	"False"	"CHEMBL3888425"	"Enzymatic Assay: JAK1/2/3 kinase assay are performed in vitro using Kit-Tyr 6 Peptide (Invitrogen, Cat. No. PV4122). TYK2 kinase assay are performed in vitro using Z'-LYTE™ Kinase Assay Kit-Tyr 3 Peptide (Invitrogen, Cat. No. PV3192). Recombinant human JAK1/2/3 or TYK2 catalytic domains are from Invitrogen (Cat No. PV4774/PV4210/PV3855/PV4790); All reactions (20 μL) are started by adding 2.5 μL of the testing compound in 4% DMSO solution, 5 μL of Kinase/Peptide substrate Mixture (3.2, 0.04, 0.2 or 8 μg/mL for Recombinant human JAK1/2/3 catalytic domains, 4 μM for Z-LYTE™ Tyr 6 peptide or Z-LYTE™ Tyr 3 peptide) or Phospho-Peptide solution (Invitrogen, Cat. No. PV3192, diluted with 1.33× Kinase Buffer), 2.5 μL ATP Solution (300/100/40/100M, JAK1/JAK2/JAK3/TYK2) or 1.33× Kinase Buffer (Invitrogen, Cat. No. PV3189, 5× diluted with distilled water). The 384-well assay plate (Corning, Cat. No. 3575) is mixed and incubated at room temperature for 1 hour. 5 μL of the Development Solution (Dilute Development Reagent A (Cat. No. PV3297) is diluted to 1/64 with Development Buffer (Cat. No. PV3127) for JAK1, JAK2 and JAK3 assay; Development Reagent A (Cat. No. PV3297) is diluted to 1/2048 with Development Buffer (Cat. No. PV3127) for TYK2 assay. The diluted Development Solution is then added to each well, mixed and incubated at room temperature for another 1 hour. The kinase reaction is then stopped by adding 5 μL of the Stop Reagent (Invitrogen, Cat. No. PV3094), and the plate is read with Wallac 1420 VICTOR3 Multilabel Counter (PerkinElmer™) at 445 nm and 520 nm fluorescence. All compounds are initially tested at 8 different concentrations (1 μM down to 0.0003 μM) using a 1:3 serial dilution scheme."	"B"	"BAO_0000357"	"single protein format"	"None"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3886703"	"37"	"BindingDB Database"	""	"2016"	"None"	""
"CHEMBL4286103"	""	"0"	"445.48"	"0"	"2.98"	"20a"	"CC[C@H](C(=O)N1CC(C#N)C1)n1c(=O)c2cc(OC)c(OC)cc2c2cnc3[nH]ccc3c21"	"IC50"	"'='"	"29.6"	"nM"	"7.53"	""	""	"UO_0000065"	"16.90"	"0.31"	"4.55"	"6.65"	"False"	"CHEMBL4261266"	"Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]-ATP addition measured after 2 hrs by filter-binding method"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4257589"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3234882"	""	"0"	"327.38"	"0"	"4.10"	"15"	"Cc1cccc(Nc2sc(-c3cccc(F)c3)cc2C(N)=O)n1"	"IC50"	"'='"	"155.0"	"nM"	"6.81"	""	""	"UO_0000065"	"20.80"	"0.40"	"2.71"	"10.01"	"False"	"CHEMBL3239499"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3232939"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL4447497"	""	"0"	"487.61"	"0"	"3.79"	"11"	"N#CC[C@H]1CC[C@H](n2c(CC(=O)NC34CCC(C(N)=O)(CC3)CC4)nc3cnc4[nH]ccc4c32)CC1"	"IC50"	"'='"	"1962.0"	"nM"	"5.71"	""	""	"UO_0000065"	"11.70"	"0.22"	"1.92"	"4.01"	"False"	"CHEMBL4404829"	"Inhibition of JAK2/JAK2 in human PBMC assessed as reduction in GM-CSF-induced STAT5 phosphorylation pre-incubated for 30 mins before GM-CSF stimulation for 30 mins AlphaLISAassay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402578"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4447497"	""	"0"	"487.61"	"0"	"3.79"	"11"	"N#CC[C@H]1CC[C@H](n2c(CC(=O)NC34CCC(C(N)=O)(CC3)CC4)nc3cnc4[nH]ccc4c32)CC1"	"IC50"	"'='"	"2.8"	"nM"	"8.55"	""	""	"UO_0000065"	"17.54"	"0.32"	"4.76"	"6.00"	"False"	"CHEMBL4404825"	"Inhibition of JAK2-JH1/JH2 domain (532 to 1132 residues) (unknown origin) pre-incubated before NH2-KGGEEEEYFELVKK-CO2 substrate addition and measured after 90 mins by MS analysis"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402578"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4582390"	""	"0"	"434.54"	"0"	"3.52"	"10"	"N#CC[C@H]1CC[C@H](n2c(CC(=O)N[C@H]3CC[C@H](O)CC3)nc3cnc4[nH]ccc4c32)CC1"	"IC50"	"'='"	"399.0"	"nM"	"6.40"	""	""	"UO_0000065"	"14.73"	"0.27"	"2.88"	"5.35"	"False"	"CHEMBL4404829"	"Inhibition of JAK2/JAK2 in human PBMC assessed as reduction in GM-CSF-induced STAT5 phosphorylation pre-incubated for 30 mins before GM-CSF stimulation for 30 mins AlphaLISAassay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402578"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4563534"	""	"0"	"389.46"	"0"	"3.13"	"4"	"N#CCCNC(=O)Cc1nc2cnc3[nH]ccc3c2n1[C@H]1CC[C@H](CC#N)CC1"	"IC50"	"'='"	"90.0"	"nM"	"7.05"	""	""	"UO_0000065"	"18.09"	"0.33"	"3.92"	"5.72"	"False"	"CHEMBL4404829"	"Inhibition of JAK2/JAK2 in human PBMC assessed as reduction in GM-CSF-induced STAT5 phosphorylation pre-incubated for 30 mins before GM-CSF stimulation for 30 mins AlphaLISAassay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4402578"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL2105759"	"BARICITINIB"	"4"	"371.43"	"0"	"1.10"	"3"	"CCS(=O)(=O)N1CC(CC#N)(n2cc(-c3ncnc4[nH]ccc34)cn2)C1"	"IC50"	"'='"	"5.7"	"nM"	"8.24"	""	""	"UO_0000065"	"22.20"	"0.43"	"7.14"	"6.84"	"False"	"CHEMBL4341343"	"Inhibition of JAK2 (unknown origin) using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition and measured by 30 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4453064"	""	"0"	"384.46"	"0"	"3.11"	"7a"	"Cc1cnc(Nc2ccccc2)nc1-c1cc2c(o1)CCN(S(C)(=O)=O)C2"	"IC50"	"'>'"	"20000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4341350"	"Inhibition of JAK2 V617F mutant in human HEL cells assessed as reduction in cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"CHEMBL3308090"	""
"CHEMBL4789489"	""	"0"	"378.48"	"0"	"3.28"	"13c"	"Cc1cnc(Nc2ccc3c(c2)CN(CCO)C3)nc1-c1cnn(C(C)C)c1"	"IC50"	"'='"	"692.0"	"nM"	"6.16"	""	""	""	"16.28"	"0.30"	"2.88"	"7.79"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL4749454"	""	"0"	"420.56"	"0"	"4.37"	"13q"	"CCOCCN1CCc2cc(Nc3ncc(C)c(-c4cnn(C(C)C)c4)n3)ccc2C1"	"IC50"	"'='"	"339.0"	"nM"	"6.47"	""	""	""	"15.38"	"0.29"	"2.10"	"9.50"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL4748445"	""	"0"	"388.52"	"0"	"4.52"	"13s"	"C=CCN1CCc2cc(Nc3ncc(C)c(-c4cnn(C(C)C)c4)n3)ccc2C1"	"IC50"	"'='"	"288.0"	"nM"	"6.54"	""	""	""	"16.83"	"0.31"	"2.02"	"11.11"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL4756422"	""	"0"	"459.60"	"0"	"3.98"	"13am"	"Cc1cnc(Nc2ccc3c(c2)CN(C(=O)/C=C/CN(C)C)CC3)nc1-c1cnn(C(C)C)c1"	"IC50"	"'='"	"15.3"	"nM"	"7.82"	""	""	""	"17.00"	"0.31"	"3.84"	"9.87"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL4756516"	""	"0"	"487.65"	"0"	"4.80"	"13ag"	"Cc1cnc(Nc2ccc3c(c2)CCN(C/C=C/C(=O)NC(C)(C)C)C3)nc1-c1cnn(C(C)C)c1"	"IC50"	"'='"	"612.0"	"nM"	"6.21"	""	""	""	"12.74"	"0.24"	"1.41"	"7.06"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"20, CP-690550"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"682.0"	"nM"	"6.17"	""	""	"UO_0000065"	"19.74"	"0.37"	"4.63"	"6.94"	"False"	"CHEMBL1941461"	"Inhibition of JAK2 in human whole blood assessed as inhibition of TPO-stimulated STAT5 phosphorylation preincubated for 30 mins prior to TPO challenge measured after 15 mins by intracellular phosflow staining"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"CHEMBL3638178"	"Blood"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL1938231"	"1"	"Scientific Literature"	"J. Med. Chem."	"2011"	"None"	""
"CHEMBL4289149"	""	"0"	"401.35"	"0"	"3.04"	"7"	"N#Cc1cc(Nc2cc(NC3CC3)c3ncc(C(N)=O)n3n2)cc(C(F)(F)F)c1"	"IC50"	"'>'"	"50000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4251837"	"Inhibition of JAK2 JH2 domain (unknown origin)"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4251544"	"1"	"Scientific Literature"	"MedChemComm"	"2017"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"1"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"1110.0"	"nM"	"5.96"	""	""	"UO_0000065"	"19.06"	"0.35"	"4.41"	"6.70"	"False"	"CHEMBL4309398"	"Inhibition of JAK2 in human TF1 cells assessed as reduction in IL2-induced STAT6 phosphorylation at Tyr694/699 residues"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4308837"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"1"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"44.0"	"nM"	"7.36"	""	""	"UO_0000065"	"23.55"	"0.44"	"5.82"	"8.27"	"False"	"CHEMBL4309397"	"Inhibition of recombinant JAK2 (unknown origin) in presence of 0.1 mM ATP by alpha-screen assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4308837"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4283724"	""	"0"	"314.39"	"0"	"2.15"	"13"	"NC(=O)c1cnc2c(NC3CC3)cc(NC3CCCCC3)nn12"	"IC50"	"'>'"	"2000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4251837"	"Inhibition of JAK2 JH2 domain (unknown origin)"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4251544"	"1"	"Scientific Literature"	"MedChemComm"	"2017"	"None"	""
"CHEMBL4750448"	""	"0"	"369.39"	"0"	"2.53"	"26, trans"	"N#CC[C@]1(n2cc(-c3nc(-c4cc[nH]n4)cn4nccc34)cn2)C[C@H](C#N)C1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4675820"	"Inhibition of JAK2 homodimer signaling pathway in human whole blood spiked with CD34 +ve cells assessed as reduction in EPO induced STAT5 phosphorylation preincubated for 45 mins followed by EPO addition and measured measured after 15 mins by immunostaining based FACS assay"	"A"	"BAO_0000221"	"tissue-based format"	"Homo sapiens"	"None"	"Blood"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4673239"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 1.0 hr"
"CHEMBL1873475"	"IBRUTINIB"	"4"	"440.51"	"0"	"4.22"	"Ibrutinib"	"C=CC(=O)N1CCC[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	""	""	""	""	""	"False"	"CHEMBL4720228"	"Inhibition of recombinant human JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate incubate for 60 mins by LANCE assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715815"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2018"	"None"	"TIME = 1.0 hr"
"CHEMBL3622821"	"UPADACITINIB"	"4"	"380.37"	"0"	"2.91"	"11"	"CC[C@@H]1CN(C(=O)NCC(F)(F)F)C[C@@H]1c1cnc2cnc3[nH]ccc3n12"	"IC50"	"'='"	"608.0"	"nM"	"6.22"	""	""	"UO_0000065"	"16.34"	"0.31"	"3.31"	"7.94"	"False"	"CHEMBL4309398"	"Inhibition of JAK2 in human TF1 cells assessed as reduction in IL2-induced STAT6 phosphorylation at Tyr694/699 residues"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4308837"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4748354"	""	"0"	"506.61"	"2"	"5.30"	"13z"	"Cc1cnc(Nc2ccc3c(c2)CCN(C(=O)/C=C/C(=O)c2ccccc2)C3)nc1-c1cnn(C(C)C)c1"	"IC50"	"'='"	"52.1"	"nM"	"7.28"	""	""	""	"14.38"	"0.26"	"1.98"	"7.83"	"False"	"CHEMBL4723813"	"Inhibition of JAK2 V617F mutant in human SET-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"Bone marrow"	"SET2"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4715869"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	"TIME = 72.0 hr"
"CHEMBL4238436"	""	"0"	"323.36"	"0"	"0.93"	"13g"	"Cn1cc(-c2nn(C3CCN(C#N)CC3)c3ncnc(N)c23)cn1"	"IC50"	"'='"	"103.5"	"nM"	"6.99"	""	""	"UO_0000065"	"21.60"	"0.40"	"6.06"	"6.10"	"False"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL3234883"	""	"0"	"363.36"	"0"	"4.67"	"13"	"NC(=O)c1cc(-c2ccccc2)sc1Nc1cccc(C(F)(F)F)n1"	"IC50"	"'='"	"891.0"	"nM"	"6.05"	""	""	"UO_0000065"	"16.65"	"0.33"	"1.38"	"8.90"	"False"	"CHEMBL3239499"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3232939"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3234878"	""	"0"	"343.84"	"0"	"4.61"	"19"	"Cc1cccc(Nc2sc(-c3ccccc3Cl)cc2C(N)=O)n1"	"IC50"	"'='"	"93.0"	"nM"	"7.03"	""	""	"UO_0000065"	"20.45"	"0.42"	"2.42"	"10.34"	"False"	"CHEMBL3239499"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3232939"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3234895"	""	"0"	"491.56"	"0"	"4.45"	"25"	"CC(C)(O)COCc1cccc(Nc2sc(-c3c(F)cc(C(C)(C)O)cc3F)cc2C(N)=O)n1"	"IC50"	"'='"	"90.0"	"nM"	"7.05"	""	""	"UO_0000065"	"14.33"	"0.28"	"2.60"	"5.99"	"False"	"CHEMBL3239512"	"Inhibition of JAK2 (unknown origin)-mediated STAT5 phosphorylation by AlphaScreen assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3232939"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL4758931"	""	"0"	"435.49"	"0"	"2.36"	"25"	"C/C=C/C(=O)NCC(=O)Nc1cccc(-c2cc(Nc3cnn(CCOC)c3)ncn2)c1"	"IC50"	"'='"	"886.0"	"nM"	"6.05"	""	""	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL4746760"	""	"0"	"447.46"	"0"	"0.80"	"29"	"CNC(=O)Cn1cc(Nc2cc(-c3cccc(NC(=O)CNC(=O)CC#N)c3)ncn2)cn1"	"IC50"	"'='"	"2732.0"	"nM"	"5.56"	""	""	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL4093643"	""	"0"	"351.48"	"0"	"1.89"	"23"	"CCCCNS(=O)(=O)C[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"708.0"	"nM"	"6.15"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4103435"	""	"0"	"377.39"	"0"	"1.80"	"31"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)CCC(F)(F)F)C1"	"IC50"	"'='"	"592.0"	"nM"	"6.23"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3655082"	""	"0"	"337.45"	"0"	"1.50"	"7"	"CC(C)CS(=O)(=O)N[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"9400.0"	"nM"	"5.03"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4098682"	""	"0"	"333.40"	"0"	"3.63"	"6g"	"Cc1ccc(CNc2nc(N)nc3[nH]c4cc(C)c(O)cc4c23)cc1"	"IC50"	"'>'"	"100000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4021795"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020756"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2017"	"None"	""
"CHEMBL4093955"	""	"0"	"363.49"	"0"	"1.84"	"42"	"CN(CC1CC1)S(=O)(=O)C[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"199.0"	"nM"	"6.70"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3655095"	""	"0"	"335.43"	"0"	"1.25"	"29"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)CC2CC2)C1"	"IC50"	"'='"	"7540.0"	"nM"	"5.12"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4740169"	""	"0"	"414.47"	"0"	"3.58"	"35"	"N#CCC(=O)Nc1ccc(-c2cc(Nc3ccc(N4CCOCC4)cc3)ncn2)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL3655082"	""	"0"	"337.45"	"0"	"1.50"	"7"	"CC(C)CS(=O)(=O)N[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"542.0"	"nM"	"6.27"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4100048"	""	"0"	"308.41"	"0"	"1.61"	"16"	"CCS(=O)(=O)C[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"471.0"	"nM"	"6.33"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3658860"	""	"0"	"336.46"	"0"	"2.39"	"19"	"CCCCS(=O)(=O)C[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"220.0"	"nM"	"6.66"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4746952"	""	"0"	"411.94"	"0"	"3.90"	"18c"	"CNC(=O)c1cnc2[nH]ccc2c1NCC1CCN(Cc2ccc(Cl)cc2)CC1"	"IC50"	"'='"	"712.0"	"nM"	"6.15"	""	""	""	"14.92"	"0.29"	"2.25"	"8.42"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL4741376"	""	"0"	"407.52"	"0"	"3.40"	"30e"	"CNC(=O)c1cnc2[nH]ccc2c1NC1CCCN(Cc2ccc(OC)cc2)CC1"	"IC50"	"'='"	"175.0"	"nM"	"6.76"	""	""	""	"16.58"	"0.31"	"3.36"	"8.21"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL4779060"	""	"0"	"411.94"	"0"	"4.04"	"31f"	"CNC(=O)c1cnc2[nH]ccc2c1N[C@@H]1CCN(Cc2cccc(Cl)c2)[C@H](C)C1"	"IC50"	"'='"	"8.83"	"nM"	"8.05"	""	""	""	"19.55"	"0.38"	"4.01"	"11.03"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL4452772"	""	"0"	"426.92"	"0"	"4.67"	"12t"	"CC(Oc1cc(-c2cccc(N3CCNCC3)c2)cnc1N)c1cc(F)ccc1Cl"	"IC50"	"'='"	"27.0"	"nM"	"7.57"	""	""	"UO_0000065"	"17.73"	"0.34"	"2.90"	"11.94"	"False"	"CHEMBL4341687"	"Inhibition of human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr by Z'-LYTE assay"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"Sf9"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340536"	"1"	"Scientific Literature"	"Bioorg Med Chem Lett"	"2019"	"CHEMBL3308860"	""
"CHEMBL3309997"	""	"0"	"363.38"	"0"	"2.47"	"12a"	"OCCCNc1ccc2c(c1)nc(-c1ccc3c(c1)OCO3)n1ncnc21"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3381081"	"Inhibition of JAK2 (unknown origin)"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352169"	"1"	"Scientific Literature"	"Bioorg. Med. Chem."	"2014"	"None"	""
"CHEMBL4449906"	""	"0"	"494.50"	"0"	"3.70"	"7m"	"Cc1cnc(Nc2cc(F)c(N3CCOCC3)c(F)c2)nc1-c1cc2c(o1)CCN(C(=O)CC#N)C2"	"IC50"	"'='"	"1313.0"	"nM"	"5.88"	""	""	"UO_0000065"	"11.89"	"0.22"	"2.18"	"5.47"	"False"	"CHEMBL4341350"	"Inhibition of JAK2 V617F mutant in human HEL cells assessed as reduction in cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"CHEMBL3308090"	""
"CHEMBL3655081"	"ABROCITINIB"	"3"	"323.42"	"0"	"1.25"	"25; PF-04965842"	"CCCS(=O)(=O)N[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"7178.0"	"nM"	"5.14"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4239767"	""	"0"	"383.46"	"0"	"0.53"	"12e"	"CN(C)CC(=O)N1CCCC(n2nc(-c3cnn(C)c3)c3c(N)ncnc32)C1"	"IC50"	"'='"	"1932.5"	"nM"	"5.71"	""	""	"UO_0000065"	"14.90"	"0.28"	"5.18"	"5.15"	"False"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4245728"	""	"0"	"409.45"	"0"	"1.00"	"13d"	"COCCn1cc(-c2nn(C3CCN(C(=O)CC#N)CC3)c3ncnc(N)c23)cn1"	"IC50"	"'='"	"367.2"	"nM"	"6.43"	""	""	"UO_0000065"	"15.72"	"0.29"	"5.44"	"4.57"	"False"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4783938"	""	"0"	"411.94"	"0"	"4.04"	"38a"	"CNC(=O)c1cnc2[nH]ccc2c1N[C@H]1CCN(Cc2ccc(Cl)cc2)[C@@H](C)C1"	"IC50"	"'='"	"2.94"	"nM"	"8.53"	""	""	""	"20.71"	"0.40"	"4.49"	"11.68"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL4789693"	""	"0"	"411.94"	"0"	"4.04"	"31b"	"CNC(=O)c1cnc2[nH]ccc2c1N[C@@H]1CCN(Cc2cccc(Cl)c2)[C@@H](C)C1"	"IC50"	"'='"	"28.5"	"nM"	"7.54"	""	""	""	"18.32"	"0.36"	"3.51"	"10.33"	"False"	"CHEMBL4713240"	"Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4706658"	"1"	"Scientific Literature"	"J Med Chem"	"2021"	"None"	"TIME = 1.5 hr"
"CHEMBL4440795"	""	"0"	"463.49"	"0"	"3.61"	"7n"	"COc1cc(Nc2ncc(C)c(-c3cc4c(o3)CCN(C(=O)CC#N)C4)n2)cc(OC)c1OC"	"IC50"	"'='"	"1398.0"	"nM"	"5.85"	""	""	"UO_0000065"	"12.63"	"0.24"	"2.24"	"4.77"	"False"	"CHEMBL4341350"	"Inhibition of JAK2 V617F mutant in human HEL cells assessed as reduction in cell proliferation"	"B"	"BAO_0000219"	"cell-based format"	"Homo sapiens"	"None"	"None"	"HEL"	"None"	""	"O60674"	"V617F"	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"CHEMBL3308090"	""
"CHEMBL4741903"	""	"0"	"398.43"	"0"	"1.44"	"16"	"Cn1cc(-c2cn3nccc3c(-c3cnn(C4(CC#N)CN(CC#N)C4)c3)n2)cn1"	"IC50"	"'='"	"37.0"	"nM"	"7.43"	""	""	""	""	""	""	""	"False"	"CHEMBL4675813"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using FITC-KGGEEEEYFELVKK as substrate in presence of ATP at Km by microfluidic assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4673239"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4761132"	""	"0"	"401.43"	"0"	"1.46"	"14"	"CC(=O)N1CC(CC#N)(n2cc(-c3nc(-c4cnn(C)c4)cn4nccc34)cn2)C1"	"IC50"	"'='"	"1747.0"	"nM"	"5.76"	""	""	""	""	""	""	""	"False"	"CHEMBL4675813"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using FITC-KGGEEEEYFELVKK as substrate in presence of ATP at Km by microfluidic assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4673239"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4761611"	""	"0"	"413.49"	"0"	"2.33"	"13"	"Cn1cc(-c2cn3nccc3c(-c3cnn(C4(CC#N)CN(CC5CC5)C4)c3)n2)cn1"	"IC50"	"'='"	"187.0"	"nM"	"6.73"	""	""	""	""	""	""	""	"False"	"CHEMBL4675813"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system using FITC-KGGEEEEYFELVKK as substrate in presence of ATP at Km by microfluidic assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4673239"	"1"	"Scientific Literature"	"J Med Chem"	"2020"	"None"	""
"CHEMBL4521339"	""	"0"	"497.62"	"0"	"3.58"	"7c"	"Cc1cnc(Nc2ccc(OCCN3CCCC3)cc2)nc1-c1cc2c(o1)CCN(S(C)(=O)=O)C2"	"IC50"	"'='"	"4.1"	"nM"	"8.39"	""	""	"UO_0000065"	"16.85"	"0.33"	"4.81"	"8.32"	"False"	"CHEMBL4341343"	"Inhibition of JAK2 (unknown origin) using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition and measured by 30 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4777465"	""	"0"	"378.44"	"0"	"3.24"	"32"	"C/C=C/C(=O)Nc1ccc(-c2cc(Nc3cnn(CCOC)c3)ncn2)cc1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4685310"	"Inhibition of recombinant human GST-tagged JAK2 cytoplasmic domain (809 to 1153+9 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay"	"A"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4680201"	"1"	"Scientific Literature"	"Eur J Med Chem"	"2020"	"None"	"TIME = 0.5833 hr"
"CHEMBL4103698"	""	"0"	"375.43"	"0"	"2.04"	"9"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)c2ccc(F)cc2)C1"	"IC50"	"'='"	"240.0"	"nM"	"6.62"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4066404"	""	"0"	"365.50"	"0"	"2.23"	"41"	"CCCCN(C)S(=O)(=O)C[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"888.0"	"nM"	"6.05"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022970"	"Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4090590"	""	"0"	"322.43"	"0"	"2.00"	"18"	"CCCS(=O)(=O)C[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'>'"	"20000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4068319"	""	"0"	"349.46"	"0"	"1.64"	"30"	"CN(c1ncnc2[nH]ccc12)[C@H]1C[C@@H](NS(=O)(=O)CC2CCC2)C1"	"IC50"	"'>'"	"20000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL4093955"	""	"0"	"363.49"	"0"	"1.84"	"42"	"CN(CC1CC1)S(=O)(=O)C[C@H]1C[C@@H](N(C)c2ncnc3[nH]ccc23)C1"	"IC50"	"'='"	"2260.0"	"nM"	"5.65"	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL4022973"	"Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis"	"A"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4020822"	"1"	"Scientific Literature"	"J Med Chem"	"2018"	"None"	""
"CHEMBL3360356"	""	"0"	"411.46"	"0"	"3.98"	"63"	"O=C(Nc1nc2cccc(-c3ccc(CN4CCC(F)(F)CC4)cc3)n2n1)C1CC1"	"IC50"	"'>'"	"10000.0"	"nM"	""	""	""	"UO_0000065"	""	""	""	""	"False"	"CHEMBL3382736"	"Inhibition of JAK2 in human whole blood assessed as inhibition of GM-CSF-induced pSTAT5"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"CHEMBL3638178"	"Blood"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351789"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL3301607"	"FILGOTINIB"	"4"	"425.51"	"0"	"1.98"	"65, GLPG0634"	"O=C(Nc1nc2cccc(-c3ccc(CN4CCS(=O)(=O)CC4)cc3)n2n1)C1CC1"	"IC50"	"'='"	"17453.0"	"nM"	"4.76"	""	""	"UO_0000065"	"11.18"	"0.22"	"2.78"	"4.92"	"False"	"CHEMBL3382736"	"Inhibition of JAK2 in human whole blood assessed as inhibition of GM-CSF-induced pSTAT5"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"CHEMBL3638178"	"Blood"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3351789"	"1"	"Scientific Literature"	"J. Med. Chem."	"2014"	"None"	""
"CHEMBL4239312"	""	"0"	"418.46"	"0"	"2.09"	"8"	"C=CC(=O)Nc1cccc(Cn2nc(-c3cnn(CCOC)c3)c3c(N)ncnc32)c1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4241519"	""	"0"	"441.54"	"0"	"0.72"	"10f"	"COCCn1cc(-c2nn(CC3CCN(C(=O)CN(C)C)CC3)c3ncnc(N)c23)cn1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4549680"	""	"0"	"418.41"	"0"	"3.50"	"7i"	"Cc1cnc(Nc2ccc([N+](=O)[O-])cc2)nc1-c1cc2c(o1)CCN(C(=O)CC#N)C2"	"IC50"	"'='"	"14.2"	"nM"	"7.85"	""	""	"UO_0000065"	"18.76"	"0.35"	"4.35"	"5.68"	"False"	"CHEMBL4341343"	"Inhibition of JAK2 (unknown origin) using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition and measured by 30 mins by HTRF assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4340527"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2019"	"None"	""
"CHEMBL4461809"	""	"0"	"549.74"	"1"	"4.26"	"18p"	"Cc1cnc(Nc2ccc(N3CCC(N(C)CCN4CCN(C)CC4)CC3)c(F)c2)nc1-c1cnn(C(C)C)c1"	"IC50"	"'='"	"3.0"	"nM"	"8.52"	""	""	"UO_0000065"	"15.50"	"0.29"	"4.26"	"12.43"	"False"	"CHEMBL4323930"	"Inhibition of human JAK2 (808 to end residues) using KTFCGTPEYLAP as substrate after 40 mins in presence of [gamma33P]-ATP by scintillation counting based radiometric assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4321837"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
"CHEMBL3359907"	""	"0"	"260.34"	"0"	"2.28"	"3a"	"C[C@@H](Nc1c(C(N)=O)cnn2cccc12)C(C)(C)C"	"IC50"	"'='"	"30.0"	"nM"	"7.52"	""	""	"UO_0000065"	"28.90"	"0.54"	"5.24"	"10.39"	"False"	"CHEMBL3377596"	"Inhibition of JAK2 (unknown origin) by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352641"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3359919"	""	"0"	"287.37"	"0"	"1.36"	"4h"	"CC1(C)[C@@H](N)CC[C@H]1Nc1c(C(N)=O)cnn2cccc12"	"IC50"	"'='"	"130.0"	"nM"	"6.89"	""	""	"UO_0000065"	"23.96"	"0.45"	"5.53"	"7.00"	"False"	"CHEMBL3377596"	"Inhibition of JAK2 (unknown origin) by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352641"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3359929"	""	"0"	"276.32"	"0"	"2.13"	"5i"	"C[C@@]1(F)CCC[C@H]1Nc1c(C(N)=O)cnn2cccc12"	"IC50"	"'='"	"210.0"	"nM"	"6.68"	""	""	"UO_0000065"	"24.17"	"0.46"	"4.55"	"9.22"	"False"	"CHEMBL3377596"	"Inhibition of JAK2 (unknown origin) by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352641"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3359918"	""	"0"	"287.37"	"0"	"1.36"	"4g"	"CC1(C)[C@H](N)CC[C@H]1Nc1c(C(N)=O)cnn2cccc12"	"IC50"	"'='"	"170.0"	"nM"	"6.77"	""	""	"UO_0000065"	"23.56"	"0.44"	"5.41"	"6.88"	"False"	"CHEMBL3377596"	"Inhibition of JAK2 (unknown origin) by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352641"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL3359925"	""	"0"	"288.35"	"0"	"1.40"	"5d"	"C[C@@]1(CO)CCC[C@H]1Nc1c(C(N)=O)cnn2cccc12"	"IC50"	"'='"	"380.0"	"nM"	"6.42"	""	""	"UO_0000065"	"22.27"	"0.42"	"5.02"	"6.93"	"False"	"CHEMBL3377596"	"Inhibition of JAK2 (unknown origin) by caliper assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL3352641"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2014"	"None"	""
"CHEMBL221959"	"TOFACITINIB"	"4"	"312.38"	"0"	"1.54"	"1a"	"C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12"	"IC50"	"'='"	"4.0"	"nM"	"8.40"	""	""	"UO_0000065"	"26.88"	"0.50"	"6.86"	"9.45"	"True"	"CHEMBL2378515"	"Inhibition of JAK2 (unknown origin) using [33gammaP]ATP and Biotin-KAIETDKEYYTVKD as substrate incubated for 10 mins prior to substrate addition measured after 30 mins by filtration assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL2375236"	"1"	"Scientific Literature"	"Bioorg. Med. Chem. Lett."	"2013"	"None"	""
"CHEMBL4241272"	""	"0"	"366.43"	"0"	"1.23"	"9a"	"C=CC(=O)N1CCCC(Cn2nc(-c3cnn(C)c3)c3c(N)ncnc32)C1"	"IC50"	"'='"	"808.3"	"nM"	"6.09"	""	""	"UO_0000065"	"16.63"	"0.31"	"4.86"	"5.65"	"False"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL4237340"	""	"0"	"337.39"	"0"	"1.00"	"10g"	"Cn1cc(-c2nn(CC3CCN(C#N)CC3)c3ncnc(N)c23)cn1"	"IC50"	""	""	""	""	""	"Not Determined"	""	""	""	""	""	"False"	"CHEMBL4236384"	"Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition measured after 30 mins by HTRF assay"	"B"	"BAO_0000019"	"assay format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4229546"	"1"	"Scientific Literature"	"Bioorg Med Chem"	"2018"	"None"	""
"CHEMBL3622376"	""	"0"	"242.24"	"0"	"0.62"	"77"	"c1nc(-c2cn(CC3CO3)nn2)c2cc[nH]c2n1"	"IC50"	"'='"	"2451.0"	"nM"	"5.61"	""	""	"UO_0000065"	"23.16"	"0.43"	"4.99"	"6.62"	"False"	"CHEMBL4322092"	"Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) substrate preincubated for 20 mis followed by addition of ATP and measured after 120 mins in presence of 33P-gamma ATP by hotspot kinase assay"	"B"	"BAO_0000357"	"single protein format"	"Homo sapiens"	"None"	"None"	"None"	"None"	""	""	""	"CHEMBL2971"	"Tyrosine-protein kinase JAK2"	"Homo sapiens"	"SINGLE PROTEIN"	"CHEMBL4321787"	"1"	"Scientific Literature"	"J Med Chem"	"2019"	"None"	""
