belumosudil [Ligand Id: 9558] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2005186 (Belumosudil, KD-025, KD025, Rock2 inhibitor kd025, SLx-2119, Slx-2119 free base) |
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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] | ||||||||
| ChEMBL | Inhibition of ROCK1 (unknown origin) | B | 4.62 | pKi | 24000 | nM | Ki | Bioorg Med Chem Lett (2020) 30: 127474-127474 [PMID:32805407] |
| ChEMBL | Inhibition of ROCK1 (unknown origin) | B | 7.4 | pKi | 40 | nM | Ki | J Med Chem (2018) 61: 9811-9840 [PMID:29969256] |
| GtoPdb | In a radiometric cell-free enzyme assay. | - | 4.62 | pIC50 | 24000 | nM | IC50 | Blood Coagul Fibrinolysis (2008) 19: 709-18 [PMID:18832915] |
| 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 ROCK2 (unknown origin) | B | 6.98 | pKi | 105 | nM | Ki | Bioorg Med Chem Lett (2020) 30: 127474-127474 [PMID:32805407] |
| GtoPdb | In a radiometric cell-free enzyme assay. | - | 6.98 | pIC50 | 105 | nM | IC50 | Blood Coagul Fibrinolysis (2008) 19: 709-18 [PMID:18832915] |
| ChEMBL | Inhibition of ROCK2 (unknown origin) | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (2018) 61: 9811-9840 [PMID:29969256] |
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]
