BMS-509744 [Ligand Id: 9994] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL209148 (BMS-509744)
  • calcium/calmodulin-dependent protein kinase II alpha subunit/CaM kinase II alpha in Human [ChEMBL: CHEMBL4147] [GtoPdb: 1555] [UniProtKB: Q9UQM7]
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  • protein kinase, cAMP-dependent, catalytic, alpha subunit/cAMP-dependent protein kinase alpha-catalytic subunit in Human [ChEMBL: CHEMBL4101] [GtoPdb: 1476] [UniProtKB: P17612]
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  • cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
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  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
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  • inhibitor of nuclear factor kappa B kinase subunit beta/Inhibitor of nuclear factor kappa B kinase beta subunit in Human [ChEMBL: CHEMBL1991] [GtoPdb: 2039] [UniProtKB: O14920]
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  • leukocyte receptor tyrosine kinase/Leukocyte tyrosine kinase receptor in Human [ChEMBL: CHEMBL5627] [GtoPdb: 1838] [UniProtKB: P29376]
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  • mitogen-activated protein kinase 3/MAP kinase ERK1 in Human [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361]
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  • protein kinase C alpha/Protein kinase C alpha in Human [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252]
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  • AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
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  • BMX non-receptor tyrosine kinase/Tyrosine-protein kinase BMX in Human [ChEMBL: CHEMBL3834] [GtoPdb: 1942] [UniProtKB: P51813]
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  • Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187]
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  • FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
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  • IL2 inducible T cell kinase/Tyrosine-protein kinase ITK/TSK in Human [ChEMBL: CHEMBL2959] [GtoPdb: 2046] [UniProtKB: Q08881]
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  • LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
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  • spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405]
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  • tec protein tyrosine kinase/Tyrosine-protein kinase TEC in Human [ChEMBL: CHEMBL4246] [GtoPdb: 2238] [UniProtKB: P42680]
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  • TXK tyrosine kinase/Tyrosine-protein kinase TXK in Human [ChEMBL: CHEMBL4367] [GtoPdb: 2268] [UniProtKB: P42681]
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  • zeta chain of T cell receptor associated protein kinase 70/Tyrosine-protein kinase ZAP-70 in Human [ChEMBL: CHEMBL2803] [GtoPdb: 2285] [UniProtKB: P43403]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
calcium/calmodulin-dependent protein kinase II alpha subunit/CaM kinase II alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4147] [GtoPdb: 1555] [UniProtKB: Q9UQM7]
ChEMBL Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a CAMK2A B 4.47 pIC50 33500 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
protein kinase, cAMP-dependent, catalytic, alpha subunit/cAMP-dependent protein kinase alpha-catalytic subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4101] [GtoPdb: 1476] [UniProtKB: P17612]
ChEMBL Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a PRKACA B 4.3 pIC50 >50000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
ChEMBL Inhibition of Cdk2 B 4.54 pIC50 29000 nM IC50 Bioorg Med Chem Lett (2006) 16: 3706-3712 [PMID:16682193]
ChEMBL Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a CDK2 B 4.54 pIC50 29000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Inhibition of EGFR B 4.3 pIC50 >50000 nM IC50 Bioorg Med Chem Lett (2006) 16: 3706-3712 [PMID:16682193]
ChEMBL Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a EGFR B 4.3 pIC50 >50000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
ChEMBL Inhibition of GSK3-beta B 4.44 pIC50 36000 nM IC50 Bioorg Med Chem Lett (2006) 16: 3706-3712 [PMID:16682193]
ChEMBL Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a GSK3B B 4.44 pIC50 36000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
inhibitor of nuclear factor kappa B kinase subunit beta/Inhibitor of nuclear factor kappa B kinase beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1991] [GtoPdb: 2039] [UniProtKB: O14920]
ChEMBL Inhibition of IKK-beta B 4.3 pIC50 >50000 nM IC50 Bioorg Med Chem Lett (2006) 16: 3706-3712 [PMID:16682193]
ChEMBL Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a IKBKB B 4.3 pIC50 >50000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213]
ChEMBL Inhibition of Insulin receptor B 5.96 pIC50 1100 nM IC50 Bioorg Med Chem Lett (2006) 16: 3706-3712 [PMID:16682193]
ChEMBL Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a INSR B 5.96 pIC50 1100 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
Interleukin-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5880] [UniProtKB: P60568]
ChEMBL Inhibition of IL-2 in human Jurkat T cells pretreated with compound for 16 hrs followed by anti-CD3 stimulation by ELISA analysis B 6.62 pEC50 237.6 nM EC50 J Med Chem (2023) 66: 4979-4998 [PMID:36959108]
leukocyte receptor tyrosine kinase/Leukocyte tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5627] [GtoPdb: 1838] [UniProtKB: P29376]
ChEMBL Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a LTK B 5.62 pIC50 2400 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
mitogen-activated protein kinase 3/MAP kinase ERK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361]
ChEMBL Inhibition of ERK1 B 4.3 pIC50 >50000 nM IC50 Bioorg Med Chem Lett (2006) 16: 3706-3712 [PMID:16682193]
ChEMBL Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a MAPK3 B 4.3 pIC50 >50000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
protein kinase C alpha/Protein kinase C alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252]
ChEMBL Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a PRKCA B 4.62 pIC50 24000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
ChEMBL Inhibition of Akt1 B 4.3 pIC50 >50000 nM IC50 Bioorg Med Chem Lett (2006) 16: 3706-3712 [PMID:16682193]
ChEMBL Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a AKT1 B 4.3 pIC50 >50000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
BMX non-receptor tyrosine kinase/Tyrosine-protein kinase BMX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3834] [GtoPdb: 1942] [UniProtKB: P51813]
ChEMBL Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a BMX B 4.3 pIC50 >50000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187]
ChEMBL Inhibition of Btk B 5.39 pIC50 4100 nM IC50 Bioorg Med Chem Lett (2006) 16: 3706-3712 [PMID:16682193]
ChEMBL Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a BTK B 5.39 pIC50 4100 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
ChEMBL Inhibition of Fyn B 5.96 pIC50 1100 nM IC50 Bioorg Med Chem Lett (2006) 16: 3706-3712 [PMID:16682193]
ChEMBL Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a FYN B 5.96 pIC50 1100 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
IL2 inducible T cell kinase/Tyrosine-protein kinase ITK/TSK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2959] [GtoPdb: 2046] [UniProtKB: Q08881]
ChEMBL Inhibition of ITK B 7.8 pKi 16 nM Ki Chem Biol (2005) 12: 621-637 [PMID:15975507]
ChEMBL Affinity Phenotypic Cellular interaction: (T-cell proliferation induced by the mixed lymphocyte reaction) EUB0000651a ITK F 6.37 pIC50 430 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (nhibition of IL-2 secretion (in human PBMCs)) EUB0000651a ITK F 6.41 pIC50 390 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (Inhibition of IL-2 Secretion in Jurkat cells) EUB0000651a ITK F 6.6 pIC50 250 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (Inhibition of IL-2 secretion (in murine EL4 cells)) EUB0000651a ITK F 7.14 pIC50 72 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (Dose-dependent inhibition of calcium mobilization) EUB0000651a ITK F 7.28 pIC50 52 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
GtoPdb - - 7.72 pIC50 19 nM IC50 Bioorg Med Chem Lett (2006) 16: 3706-12 [PMID:16682193]
ChEMBL Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a ITK B 7.72 pIC50 19 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of ITK (unknown origin) B 7.72 pIC50 19 nM IC50 J Med Chem (2023) 66: 4979-4998 [PMID:36959108]
ChEMBL Inhibition of Itk B 7.72 pIC50 19 nM IC50 Bioorg Med Chem Lett (2006) 16: 3706-3712 [PMID:16682193]
ChEMBL Affinity Biochemical interaction: (Enzymatic radiometric assay) EUB0000651a ITK B 7.72 pIC50 19 nM IC50 Affinity Biochemical Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of human ITK using poly-Glu-Tyr (4:1) as substrate incubated for 1 hr by ELISA B 7.99 pIC50 10.3 nM IC50 J Med Chem (2022) 65: 2694-2709 [PMID:35099969]
LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
ChEMBL Inhibition of LCK B 5.62 pIC50 2400 nM IC50 Bioorg Med Chem Lett (2006) 16: 3706-3712 [PMID:16682193]
spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405]
ChEMBL Inhibition of Syk B 4.3 pIC50 >50000 nM IC50 Bioorg Med Chem Lett (2006) 16: 3706-3712 [PMID:16682193]
ChEMBL Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a SYK B 4.3 pIC50 >50000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
tec protein tyrosine kinase/Tyrosine-protein kinase TEC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4246] [GtoPdb: 2238] [UniProtKB: P42680]
ChEMBL Inhibition of Tec B 4.77 pIC50 17000 nM IC50 Bioorg Med Chem Lett (2006) 16: 3706-3712 [PMID:16682193]
ChEMBL Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a TEC B 4.77 pIC50 17000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
TXK tyrosine kinase/Tyrosine-protein kinase TXK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4367] [GtoPdb: 2268] [UniProtKB: P42681]
ChEMBL Inhibition of Txk B 4.96 pIC50 11000 nM IC50 Bioorg Med Chem Lett (2006) 16: 3706-3712 [PMID:16682193]
ChEMBL Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a TXK B 4.96 pIC50 11000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
zeta chain of T cell receptor associated protein kinase 70/Tyrosine-protein kinase ZAP-70 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2803] [GtoPdb: 2285] [UniProtKB: P43403]
ChEMBL Inhibition of ZAP70 B 4.3 pIC50 >50000 nM IC50 Bioorg Med Chem Lett (2006) 16: 3706-3712 [PMID:16682193]
ChEMBL Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a ZAP70 B 4.3 pIC50 >50000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library

ChEMBL data shown on this page come from version 35:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]