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 N terminal histidine tagged human recombinant ROCK1 (3 to 543 residues) in HASMC cells incubated for 2 hrs by ELISA method | B | 5.52 | pIC50 | 3000 | nM | IC50 | J Med Chem (2021) 64: 1786-1815 [PMID:33569941] |
| ChEMBL | Inhibition of N terminal histidine tagged human recombinant ROCK1 (3 to 543 residues) expressed in baculovirus infected Sf9 cells using biotin-Ahx-AKRRRLSSLRA-CONH2 as a substrate incubated for 10 mins by scintillation counting method | B | 7.46 | pIC50 | 35 | nM | IC50 | J Med Chem (2021) 64: 1786-1815 [PMID:33569941] |
| 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] |
| ChEMBL | Inhibition of ROCK1 (unknown origin) | B | 8.8 | pIC50 | 1.6 | nM | IC50 | Eur J Med Chem (2021) 225: 113742-113742 [PMID:34388381] |
| 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] |
| ChEMBL | Inhibition of ROCK2 (unknown origin) | B | 8.4 | pIC50 | 4 | nM | IC50 | Eur J Med Chem (2021) 225: 113742-113742 [PMID:34388381] |
| 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 34:
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]
