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ChEMBL ligand: CHEMBL559147 (Y-27632) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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] |
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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]