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 Inhibition of ROCK1 (unknown origin) B 6.66 pKi 220 nM Ki Eur J Med Chem (2023) 250: 115181-115181 [PMID:36764122]
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 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]
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]
GtoPdb - - 6.85 pKi 140 nM Ki Nature (1997) 389: 990-4 [PMID:9353125]
ChEMBL Inhibition of ROCK1 (unknown origin) B 6.85 pKi 140 nM Ki J Med Chem (2021) 64: 1283-1345 [PMID:33481605]
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 N terminal histidine tagged human recombinant ROCK1 (3 to 543 residues) in HASMC cells incubated for 2 hrs by ELISA method B 4.52 pIC50 30000 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 5.85 pIC50 1400 nM IC50 J Med Chem (2021) 64: 1786-1815 [PMID:33569941]
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]
ChEMBL Inhibition of ROCK2 (unknown origin) B 6.52 pKi 300 nM Ki J Med Chem (2021) 64: 1283-1345 [PMID:33481605]
ChEMBL Inhibition of human ROCK2 (unknown origin) B 6.52 pKi 300 nM Ki Eur J Med Chem (2023) 250: 115181-115181 [PMID:36764122]
ChEMBL Inhibition of ROCK2 (unknown origin) assessed as inhibition constant B 6.85 pKi 140 nM Ki J Med Chem (2016) 59: 2269-2300 [PMID:26486225]
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 recombinant N-terminal GST-tagged human ROCK2 (5 to 554 residues) expressed in baculovirus infected Sf9 cells using S6K as substrate incubated for 30 mins in presence of ATP by ADP Glo kinase assay B 6.84 pIC50 143 nM IC50 J Med Chem (2022) 65: 9819-9845 [PMID:35816678]
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 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]
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 ROCK2 (unknown origin) assessed as phosphorylation of MYPT1 using Tetramethylbenzidine as substrate in presence of ATP B 8.08 pIC50 8.3 nM IC50 ACS Med Chem Lett (2020) 11: 1694-1703 [PMID:32944136]
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 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]