GSK269962A [Ligand Id: 8037] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL220241
  • mitogen-activated protein kinase 10/c-Jun N-terminal kinase 3 in Human [ChEMBL: CHEMBL2637] [GtoPdb: 1498] [UniProtKB: P53779]
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  • cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
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  • glycogen synthase kinase 3 alpha/Glycogen synthase kinase-3 alpha in Human [ChEMBL: CHEMBL2850] [GtoPdb: 2029] [UniProtKB: P49840]
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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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  • Rho associated coiled-coil containing protein kinase 1/Rho-associated protein kinase 1 in Human [ChEMBL: CHEMBL3231] [GtoPdb: 1503] [UniProtKB: Q13464]
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  • Rho associated coiled-coil containing protein kinase 2/Rho-associated protein kinase 2 in Human [ChEMBL: CHEMBL2973] [GtoPdb: 1504] [UniProtKB: O75116]
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  • ribosomal protein S6 kinase A1/Ribosomal protein S6 kinase alpha 1 in Human [ChEMBL: CHEMBL2553] [GtoPdb: 1527] [UniProtKB: Q15418]
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  • ribosomal protein S6 kinase A5/Ribosomal protein S6 kinase alpha 5 in Human [ChEMBL: CHEMBL4237] [GtoPdb: 1523] [UniProtKB: O75582]
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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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  • AKT serine/threonine kinase 2/Serine/threonine-protein kinase AKT2 in Human [ChEMBL: CHEMBL2431] [GtoPdb: 1480] [UniProtKB: P31751]
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  • AKT serine/threonine kinase 3/Serine/threonine-protein kinase AKT3 in Human [ChEMBL: CHEMBL4816] [GtoPdb: 2286] [UniProtKB: Q9Y243]
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  • polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
mitogen-activated protein kinase 10/c-Jun N-terminal kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2637] [GtoPdb: 1498] [UniProtKB: P53779]
ChEMBL Inhibition of JNK3 B 5 pIC50 >10000 nM IC50 J. Pharmacol. Exp. Ther. (2007) 320: 89-98 [PMID:17018693]
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 5.46 pIC50 3500 nM IC50 J. Pharmacol. Exp. Ther. (2007) 320: 89-98 [PMID:17018693]
glycogen synthase kinase 3 alpha/Glycogen synthase kinase-3 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2850] [GtoPdb: 2029] [UniProtKB: P49840]
ChEMBL Inhibition of GSK3alpha B 5.9 pIC50 1260 nM IC50 J. Pharmacol. Exp. Ther. (2007) 320: 89-98 [PMID:17018693]
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 IKK2 B 5 pIC50 >10000 nM IC50 J. Pharmacol. Exp. Ther. (2007) 320: 89-98 [PMID:17018693]
Rho associated coiled-coil containing protein kinase 1/Rho-associated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3231] [GtoPdb: 1503] [UniProtKB: Q13464]
ChEMBL Inhibition of human ROCK1 in Sf9 cells B 8.74 pIC50 1.8 nM IC50 J. Med. Chem. (2007) 50: 2-5 [PMID:17201404]
ChEMBL Inhibition of human recombinant N-terminal his-tagged ROCK1 (3-543) expressed in baculovirus infected Sf9 cells using Biotin-Ahx-AKRRLSSLRA-CONH2 substrate and [gamma-33P]ATP after 90 mins by scintillation proximity assay B 8.8 pIC50 1.6 nM IC50 J. Pharmacol. Exp. Ther. (2007) 320: 89-98 [PMID:17018693]
GtoPdb In vitro inhibitory activity against recombinant ROCK1. - 8.8 pIC50 1.6 nM IC50 J. Pharmacol. Exp. Ther. (2007) 320: 89-98 [PMID:17018693]
Rho associated coiled-coil containing protein kinase 2/Rho-associated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2973] [GtoPdb: 1504] [UniProtKB: O75116]
ChEMBL Inhibition of human ROCK2 B 8.4 pIC50 4 nM IC50 J. Pharmacol. Exp. Ther. (2007) 320: 89-98 [PMID:17018693]
GtoPdb In vitro inhibitory activity against recombinant ROCK2. - 8.4 pIC50 4 nM IC50 J. Pharmacol. Exp. Ther. (2007) 320: 89-98 [PMID:17018693]
ribosomal protein S6 kinase A1/Ribosomal protein S6 kinase alpha 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2553] [GtoPdb: 1527] [UniProtKB: Q15418]
ChEMBL Inhibition of RSK1 B 6.88 pIC50 132 nM IC50 J. Pharmacol. Exp. Ther. (2007) 320: 89-98 [PMID:17018693]
ribosomal protein S6 kinase A5/Ribosomal protein S6 kinase alpha 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4237] [GtoPdb: 1523] [UniProtKB: O75582]
ChEMBL Inhibition of MSK1 B 7.31 pIC50 49 nM IC50 J. Pharmacol. Exp. Ther. (2007) 320: 89-98 [PMID:17018693]
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 6.02 pIC50 955 nM IC50 J. Pharmacol. Exp. Ther. (2007) 320: 89-98 [PMID:17018693]
AKT serine/threonine kinase 2/Serine/threonine-protein kinase AKT2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2431] [GtoPdb: 1480] [UniProtKB: P31751]
ChEMBL Inhibition of AKT2 B 5.87 pIC50 1350 nM IC50 J. Pharmacol. Exp. Ther. (2007) 320: 89-98 [PMID:17018693]
AKT serine/threonine kinase 3/Serine/threonine-protein kinase AKT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4816] [GtoPdb: 2286] [UniProtKB: Q9Y243]
ChEMBL Inhibition of AKT3 B 5.82 pIC50 1510 nM IC50 J. Pharmacol. Exp. Ther. (2007) 320: 89-98 [PMID:17018693]
polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350]
ChEMBL Inhibition of PLK B 5 pIC50 >10000 nM IC50 J. Pharmacol. Exp. Ther. (2007) 320: 89-98 [PMID:17018693]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]