fasudil [Ligand Id: 5181] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL38380 (Fasudil, AT 877, ZK-258594, AT-877, HA 1077, HA-1077)
  • CCR2/C-C chemokine receptor type 2 in Human [ChEMBL: CHEMBL4015] [GtoPdb: 59] [UniProtKB: P41597]
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  • Cell division control protein 42 homolog in Human [ChEMBL: CHEMBL6088] [UniProtKB: P60953]
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  • myosin light chain kinase/Myosin light chain kinase, smooth muscle in Human [ChEMBL: CHEMBL2428] [GtoPdb: 1552] [UniProtKB: Q15746]
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  • DM1 protein kinase/Myotonin-protein kinase in Human [ChEMBL: CHEMBL5320] [GtoPdb: 1505] [UniProtKB: Q09013]
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  • protein kinase C epsilon/Protein kinase C epsilon in Human [ChEMBL: CHEMBL3582] [GtoPdb: 1486] [UniProtKB: Q02156]
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  • protein kinase N1/Protein kinase N1 in Human [ChEMBL: CHEMBL3384] [GtoPdb: 1520] [UniProtKB: Q16512]
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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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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CCR2/C-C chemokine receptor type 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4015] [GtoPdb: 59] [UniProtKB: P41597]
ChEMBL Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2 F 4.46 pIC50 35000 nM IC50 Bioorg. Med. Chem. (2007) 15: 1022-1033 [PMID:17084087]
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 5.16 pIC50 6918.31 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 97-101 [PMID:21145740]
Cell division control protein 42 homolog in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6088] [UniProtKB: P60953]
ChEMBL Inhibition of CDc42 B 5.1 pIC50 >8000 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 3235-3239 [PMID:20462760]
ChEMBL Inhibition of Cdc42 B 5.3 pIC50 >5000 nM IC50 J. Med. Chem. (2010) 53: 759-777 [PMID:20000469]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Displacement of [3H]dofetilide from human ERG B 4.6 pKi 25118.86 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 97-101 [PMID:21145740]
myosin light chain kinase/Myosin light chain kinase, smooth muscle in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2428] [GtoPdb: 1552] [UniProtKB: Q15746]
ChEMBL Inhibition of MLCK by HTRF assay B 4.44 pKi 36000 nM Ki Bioorg. Med. Chem. (2011) 19: 429-439 [PMID:21130659]
ChEMBL Inhibition of MLCK by HTRF assay B 4.67 pIC50 21600 nM IC50 Bioorg. Med. Chem. (2011) 19: 429-439 [PMID:21130659]
ChEMBL Inhibition of myosin light chain kinase B 5.44 pIC50 3600 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
DM1 protein kinase/Myotonin-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5320] [GtoPdb: 1505] [UniProtKB: Q09013]
ChEMBL Inhibition of DMPK B 5.1 pIC50 >8000 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 3235-3239 [PMID:20462760]
protein kinase C epsilon/Protein kinase C epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3582] [GtoPdb: 1486] [UniProtKB: Q02156]
ChEMBL Inhibition of PKCepsilon B 5.52 pIC50 3000 nM IC50 J. Med. Chem. (2010) 53: 759-777 [PMID:20000469]
ChEMBL Inhibition of Prkce B 5.52 pIC50 3000 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 3235-3239 [PMID:20462760]
protein kinase N1/Protein kinase N1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3384] [GtoPdb: 1520] [UniProtKB: Q16512]
ChEMBL Inhibition of Protein kinase C related kinase 1 (PRK1) B 5.77 pIC50 1700 nM IC50 J. Med. Chem. (2003) 46: 1478-1483 [PMID:12672248]
protein kinase N2/Protein kinase N2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3032] [GtoPdb: 1521] [UniProtKB: Q16513]
ChEMBL Inhibition of His-tagged human PRK2 expressed in HEK293 cells B 5.4 pIC50 4000 nM IC50 Biochem. J. (2000) 351: 95-105 [PMID:10998351]
ChEMBL Inhibition of PKN2 B 6.11 pIC50 780 nM IC50 J. Med. Chem. (2010) 53: 759-777 [PMID:20000469]
ChEMBL Inhibition of Prkcl2 B 6.11 pIC50 780 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 3235-3239 [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 Inhibitory constant against ROCK1 B 6.28 pKi 530 nM Ki J. Biol. Chem. (2006) 281: 260-268 [PMID:16249185]
ChEMBL Inhibition of human ROCK1 by homogenous luciferase assay B 6.28 pKi 530 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 6.28 pKi 530 nM Ki J. Med. Chem. (2015) 58: 5028-5037 [PMID:26039570]
GtoPdb - - 7 pKi 100 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 97-101 [PMID:21145740]
ChEMBL Inhibition of ROCK-1 B 7 pKi 100 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 97-101 [PMID:21145740]
ChEMBL Inhibition of human ROCK1 by homogenous luciferase assay B 5.37 pIC50 4300 nM IC50 J. Med. Chem. (2010) 53: 759-777 [PMID:20000469]
ChEMBL Inhibition of ROCK-1 by Immobilized metal ion affinity-based fluorescence polarization assay B 5.5 pIC50 3162.28 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 97-101 [PMID:21145740]
GtoPdb - - 5.57 pIC50 2670 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 97-101 [PMID:21145740];
Hypertension (2009) 54: 676-83 [PMID:19597037]
ChEMBL Inhibition of ROCK1 B 6.18 pIC50 660 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 3235-3239 [PMID:20462760]
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 6.52 pIC50 300 nM IC50 J. Pharmacol. Exp. Ther. (2007) 320: 89-98 [PMID:17018693]
ChEMBL Inhibition of ROCK1 (unknown origin) B 6.59 pIC50 260 nM IC50 MedChemComm (2012) 3: 699-709 [PMID:23275831]
ChEMBL Inhibition of ROCK1 (unknown origin) B 6.59 pIC50 260 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 Displacement of fluorescent-ARC-1063 from His6-tagged recombinant human ROCK2 by luminescence intensity assay B 7.11 pKd 78 nM Kd Bioorg. Med. Chem. Lett. (2012) 22: 3425-3430 [PMID:22521647]
GtoPdb - - 6.57 pKi 271 nM Ki Hypertension (2009) 54: 676-83 [PMID:19597037]
ChEMBL Displacement of fluorescent-ARC-1063 from His6-tagged recombinant human ROCK2 by luminescence intensity assay B 4.93 pIC50 11748.98 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 3425-3430 [PMID:22521647]
ChEMBL Inhibition of Protein kinase ROCK2 (ROCKII) B 5.72 pIC50 1900 nM IC50 J. Med. Chem. (2003) 46: 1478-1483 [PMID:12672248]
ChEMBL Inhibition of ROCK-2 by Immobilized metal ion affinity-based fluorescence polarization assay B 5.87 pIC50 1348.96 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 97-101 [PMID:21145740]
GtoPdb - - 5.89 pIC50 1290 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 97-101 [PMID:21145740];
Hypertension (2009) 54: 676-83 [PMID:19597037]
ChEMBL Inhibition of human ROCK2 by homogenous luciferase assay B 6.18 pIC50 660 nM IC50 J. Med. Chem. (2010) 53: 759-777 [PMID:20000469]
ChEMBL Inhibition of ROCK2 B 6.4 pIC50 400 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 3235-3239 [PMID:20462760]
ChEMBL Inhibition of ROCK2 (unknown origin) B 6.49 pIC50 320 nM IC50 MedChemComm (2012) 3: 699-709 [PMID:23275831]
ChEMBL Inhibition of ROCK2 (unknown origin) B 6.49 pIC50 320 nM IC50 J. Med. Chem. (2016) 59: 788-809 [PMID:26356532]
ChEMBL Inhibition of ROCK2 (unknown origin) B 6.8 pIC50 158 nM IC50 Eur. J. Med. Chem. (2013) 70: 613-622 [PMID:24211637]
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 5.72 pIC50 1900 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 5.3 pIC50 5000 nM IC50 Biochem. J. (2000) 351: 95-105 [PMID:10998351]

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]