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] |
| ChEMBL | Inhibition of human ROCK1 | B | 4.62 | pIC50 | 24000 | nM | IC50 | Eur J Med Chem (2021) 225: 113742-113742 [PMID:34388381] |
| ChEMBL | Inhibition of ROCK1 (unknown origin) | B | 4.62 | pIC50 | 24000 | nM | IC50 | J Med Chem (2023) 66: 4342-4360 [PMID:36940432] |
| ChEMBL | Inhibition of ROCK1 (unknown origin) | B | 4.62 | pIC50 | 24000 | nM | IC50 | J Med Chem (2023) 66: 15205-15229 [PMID:37943013] |
| GtoPdb | In a radiometric cell-free enzyme assay. | - | 4.62 | pIC50 | 24000 | nM | IC50 | Blood Coagul Fibrinolysis (2008) 19: 709-18 [PMID:18832915] |
| ChEMBL | Inhibition of ROCK1 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2021) 64: 1283-1345 [PMID:33481605] |
| ChEMBL | Inhibition of ROCK1 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 2269-2300 [PMID:26486225] |
| ChEMBL | Inhibition of ROCK1 (unknown origin) by HTRF assay | B | 5.49 | pIC50 | 3259.5 | nM | IC50 | J Med Chem (2023) 66: 15205-15229 [PMID:37943013] |
| 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] |
| ChEMBL | Inhibition of ROCK2 (unknown origin) by HTRF assay | B | 6.92 | pIC50 | 119.5 | nM | IC50 | J Med Chem (2023) 66: 15205-15229 [PMID:37943013] |
| ChEMBL | Inhibition of ROCK2 (unknown origin) | B | 6.96 | pIC50 | 110 | nM | IC50 | J Med Chem (2023) 66: 15205-15229 [PMID:37943013] |
| ChEMBL | Inhibition of ROCK2 (unknown origin) | B | 6.98 | pIC50 | 105 | nM | IC50 | J Med Chem (2023) 66: 4342-4360 [PMID:36940432] |
| ChEMBL | Inhibition of ROCK2 (unknown origin) | B | 6.98 | pIC50 | 105 | nM | IC50 | RSC Med Chem (2022) 13: 1300-1321 [PMID:36439976] |
| ChEMBL | Inhibition of human ROCK2 | B | 6.98 | pIC50 | 105 | nM | IC50 | Eur J Med Chem (2021) 225: 113742-113742 [PMID:34388381] |
| 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 | Inhibition of ROCK2 (unknown origin) | B | 7.22 | pIC50 | 60 | nM | IC50 | J Med Chem (2016) 59: 2269-2300 [PMID:26486225] |
| ChEMBL | Inhibition of ROCK2 (unknown origin) | B | 7.22 | pIC50 | 60 | nM | IC50 | J Med Chem (2021) 64: 1283-1345 [PMID:33481605] |
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]
