GSK269962A [Ligand Id: 8037] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL220241 |
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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] |
| ChEMBL | Inhibition of N-terminal His-tagged human ROCK1 (3 to 543 residues) expressed in baculovirus infected Sf9 cells using biotin-Ahx-AKRRRLSSLRA-CONH2 as substrate incubated for 90 mins in presence of [gamma33P]ATP by scintillation counting method | B | 8.8 | pIC50 | 1.6 | nM | IC50 | Eur J Med Chem (2019) 180: 449-456 [PMID:31330446] |
| 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
