GSK429286A [Ligand Id: 9356] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL375312
  • 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 B1/Ribosomal protein S6 kinase 1 in Human [ChEMBL: CHEMBL4501] [GtoPdb: 1525] [UniProtKB: P23443]
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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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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 Affinity Phenotypic Cellular interaction (Western Blot (phosphorylation of MYPT at Thr850 in HEK293 cells)) EUB0000134b ROCK1 B 5 pIC50 <10000 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3
GtoPdb - - 7.85 pIC50 14 nM IC50 J Med Chem (2007) 50: 6-9 [PMID:17201405]
ChEMBL Inhibition of human recombinant ROCK1 expressed in Sf9 cells at 10 mM B 7.85 pIC50 14 nM IC50 J Med Chem (2007) 50: 6-9 [PMID:17201405]
ChEMBL Affinity Biochemical interaction (Scintillation Proximity Assay (SPA)) EUB0000134b ROCK1 B 7.85 pIC50 14 nM IC50 Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3
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 Affinity Phenotypic Cellular interaction (Western Blot (phosphorylation of MYPT at Thr850 in HEK293 cells)) EUB0000134b ROCK2 B 5 pIC50 <10000 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Affinity Biochemical interaction (Enzymatic inhibition assay (100 µM ATP)) EUB0000134b ROCK2 B 7.2 pIC50 63 nM IC50 Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3
ribosomal protein S6 kinase B1/Ribosomal protein S6 kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4501] [GtoPdb: 1525] [UniProtKB: P23443]
ChEMBL Inhibition of p70S6K B 5.71 pIC50 1940 nM IC50 J Med Chem (2007) 50: 6-9 [PMID:17201405]
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 6.11 pIC50 780 nM IC50 J Med Chem (2007) 50: 6-9 [PMID:17201405]
GtoPdb - - 6.11 pIC50 780 nM IC50 J Med Chem (2007) 50: 6-9 [PMID:17201405]

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]