ripasudil [Ligand Id: 10423] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3426621
  • 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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  • protein kinase, cAMP-dependent, catalytic, alpha subunit in Human [GtoPdb: 1476] [UniProtKB: P17612]
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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]
GtoPdb - - 7.29 pIC50 51 nM IC50 Curr. Eye Res. (2014) 39: 813-22 [PMID:24502505]
ChEMBL Inhibition of ROCK1 (unknown origin) B 7.29 pIC50 51 nM IC50 J. Med. Chem. (2016) 59: 788-809 [PMID:26356532]
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 N-terminal GST-tagged ROCK2 expressed in baculovirus-infected insect cells using long S6 kinase peptide as substrate by radiometric assay in presence of [32P]ATP and 200 uM ATP B 6.71 pIC50 197 nM IC50 J. Med. Chem. (2015) 58: 4309-4324 [PMID:25898023]
GtoPdb - - 7.72 pIC50 19 nM IC50 Curr. Eye Res. (2014) 39: 813-22 [PMID:24502505]
ChEMBL Inhibition of ROCK2 (unknown origin) B 7.72 pIC50 19 nM IC50 J. Med. Chem. (2016) 59: 788-809 [PMID:26356532]
ChEMBL Inhibition of human N-terminal GST-tagged ROCK2 expressed in baculovirus-infected insect cells using long S6 kinase peptide as substrate by radiometric assay in presence of [32P]ATP B 8.42 pIC50 3.8 nM IC50 J. Med. Chem. (2015) 58: 4309-4324 [PMID:25898023]
protein kinase, cAMP-dependent, catalytic, alpha subunit in Human [GtoPdb: 1476] [UniProtKB: P17612]
GtoPdb - - 5.68 pIC50 2100 nM IC50 Curr. Eye Res. (2014) 39: 813-22 [PMID:24502505]

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]