darusentan [Ligand Id: 3508] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL23261 (Darusentan, HMR-4005, Lu-135252, LU-135252) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| ETA receptor/Endothelin receptor ET-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL252] [GtoPdb: 219] [UniProtKB: P25101] | ||||||||
| ChEMBL | Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting | B | 8.22 | pKi | 6 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 3381-3394 [PMID:27321813] |
| GtoPdb | - | - | 8.9 | pKi | - | - | - | J Med Chem (1996) 39: 2123-8 [PMID:8667356] |
| ChEMBL | Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor | B | 9.1 | pIC50 | 0.8 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 125-128 [PMID:11755336] |
| ETA receptor/Endothelin receptor ET-A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4566] [GtoPdb: 219] [UniProtKB: P26684] | ||||||||
| ChEMBL | Binding affinity towards Endothelin A receptor | B | 8.22 | pKi | 6 | nM | Ki | J Med Chem (2004) 47: 1969-1986 [PMID:15055997] |
| ETB receptor/Endothelin receptor ET-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1785] [GtoPdb: 220] [UniProtKB: P24530] | ||||||||
| ChEMBL | Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting | B | 6.43 | pKi | 371 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 3381-3394 [PMID:27321813] |
| ChEMBL | Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement. | B | 7.8 | pIC50 | 16 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 125-128 [PMID:11755336] |
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]
