Y27632 [Ligand Id: 5290] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL559147 (Y-27632)
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  • protein kinase N2/Protein kinase N2 in Human [ChEMBL: CHEMBL3032] [GtoPdb: 1521] [UniProtKB: Q16513]
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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]
  • Rho associated coiled-coil containing protein kinase 2/Rho-associated protein kinase 2 in Rat [ChEMBL: CHEMBL5490] [GtoPdb: 1504] [UniProtKB: Q62868]
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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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  • protein kinase C epsilon in Human [GtoPdb: 1486] [UniProtKB: Q02156]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
C-C motif chemokine 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1649052] [UniProtKB: P13500]
ChEMBL Inhibition of MCP1-mediated human THP cell migration B 5.58 pIC50 2630.27 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 97-101 [PMID:21145740]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Displacement of [3H]dofetilide from human ERG B 4.1 pKi 79432.82 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 97-101 [PMID:21145740]
protein kinase N2/Protein kinase N2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3032] [GtoPdb: 1521] [UniProtKB: Q16513]
ChEMBL Inhibition of Protein kinase C related kinase 2 (PRK2) B 6.22 pIC50 600 nM IC50 J. Med. Chem. (2003) 46: 1478-1483 [PMID:12672248]
ChEMBL Inhibition of His-tagged human PRK2 expressed in HEK293 cells B 6.22 pIC50 600 nM IC50 Biochem. J. (2000) 351: 95-105 [PMID:10998351]
GtoPdb - - 7.15 pIC50 70 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 3235-9 [PMID:20462760]
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 ROCK1 (unknown origin) B 6.66 pKi 220 nM Ki MedChemComm (2012) 3: 699-709 [PMID:23275831]
ChEMBL Inhibitory constant against ROCK1 B 6.82 pKi 150 nM Ki J. Biol. Chem. (2006) 281: 260-268 [PMID:16249185]
ChEMBL Inhibition of human ROCK1 by homogenous luciferase assay B 6.82 pKi 150 nM Ki J. Med. Chem. (2010) 53: 759-777 [PMID:20000469]
ChEMBL Inhibition of human leukocytic ROCK1 expressed in insect cells using KKRNRTLSV as substrate after 10 mins by pyruvate kinase/lactate dehydrogenase coupled assay B 6.82 pKi 150 nM Ki J. Med. Chem. (2015) 58: 5028-5037 [PMID:26039570]
GtoPdb - - 6.85 pKi 140 nM Ki Nature (1997) 389: 990-4 [PMID:9353125]
ChEMBL Inhibition of ROCK-1 B 7.6 pKi 25.12 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 97-101 [PMID:21145740]
ChEMBL Inhibition of ROCK-1 by Immobilized metal ion affinity-based fluorescence polarization assay B 6.06 pIC50 870.96 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 97-101 [PMID:21145740]
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 6.82 pIC50 150 nM IC50 J. Pharmacol. Exp. Ther. (2007) 320: 89-98 [PMID:17018693]
ChEMBL Inhibition of ROCK-1 (unknown origin) B 7.03 pIC50 93 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 4812-4817 [PMID:25248678]
GtoPdb - - 7.34 pIC50 46 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 3235-9 [PMID:20462760];
Hypertension (2009) 54: 676-83 [PMID:19597037]
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 by homogenous luciferase assay B 6.52 pKi 300 nM Ki J. Med. Chem. (2010) 53: 759-777 [PMID:20000469]
ChEMBL Inhibition of ROCK2 (unknown origin) B 6.52 pKi 300 nM Ki MedChemComm (2012) 3: 699-709 [PMID:23275831]
GtoPdb - - 6.94 pKi 114 nM Ki Nature (1997) 389: 990-4 [PMID:9353125];
Hypertension (2009) 54: 676-83 [PMID:19597037]
ChEMBL Inhibition of Protein kinase ROCK2 (ROCKII) B 6.15 pIC50 700 nM IC50 J. Med. Chem. (2003) 46: 1478-1483 [PMID:12672248]
ChEMBL Inhibition of human ROCK2 by homogenous luciferase assay B 6.59 pIC50 260 nM IC50 J. Med. Chem. (2010) 53: 759-777 [PMID:20000469]
ChEMBL Inhibition of ROCK-2 by Immobilized metal ion affinity-based fluorescence polarization assay B 6.61 pIC50 245.47 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 97-101 [PMID:21145740]
ChEMBL Inhibition of human recombinant ROCK-2 using KEAKEKRQEQIAKRRRLSSLRASTSKSGGSQK as substrate after 40 mins by scintillation counting analysis B 7.05 pIC50 89 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 4812-4817 [PMID:25248678]
GtoPdb - - 7.21 pIC50 61 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 3235-9 [PMID:20462760];
Hypertension (2009) 54: 676-83 [PMID:19597037]
ChEMBL Inhibition of ROCK2 (unknown origin) using long S6 kinase peptide as substrate by radiometric assay B 7.27 pIC50 54 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 6442-6446 [PMID:24119557]
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 7.27 pIC50 54 nM IC50 J. Med. Chem. (2015) 58: 4309-4324 [PMID:25898023]
Rho associated coiled-coil containing protein kinase 2/Rho-associated protein kinase 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5490] [GtoPdb: 1504] [UniProtKB: Q62868]
ChEMBL Inhibition of rat ROCK2 expressed in Sf9 cells B 6.1 pIC50 800 nM IC50 Biochem. J. (2000) 351: 95-105 [PMID:10998351]
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 His-tagged human MSK1 expressed in Sf9 cells B 5.08 pIC50 8300 nM IC50 Biochem. J. (2000) 351: 95-105 [PMID:10998351]
protein kinase C epsilon in Human [GtoPdb: 1486] [UniProtKB: Q02156]
GtoPdb - - 6.47 pIC50 335 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 3235-9 [PMID:20462760]

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]