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 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]
