clazosentan [Ligand Id: 12286] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL109648 (ACT-108475, Axv-034, AXV-034343, AXV-343434, Clazosentan, Pivlaz, Ro 61-1790, RO-61-1790, VML-588) |
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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 | Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO) | B | 9.89 | pKi | 0.13 | nM | Ki | J Med Chem (1998) 41: 3261-3275 [PMID:9703472] |
| GtoPdb | Binding affinity measured as displacement of ET-1 from CHO cells expressing hETA | - | 9.89 | pKi | 0.13 | nM | Ki | J Med Chem (1998) 41: 3261-75 [PMID:9703472] |
| ChEMBL | Displacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cells | B | 8.77 | pIC50 | 1.7 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 3381-3394 [PMID:27321813] |
| GtoPdb | - | - | 9.5 | pA2 | - | - | - | J Pharmacol Exp Ther (1997) 283: 1110-8 [PMID:9399983] |
| ETB receptor/Endothelin receptor ET-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1785] [GtoPdb: 220] [UniProtKB: P24530] | ||||||||
| ChEMBL | Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO) | B | 6.76 | pKi | 175 | nM | Ki | J Med Chem (1998) 41: 3261-3275 [PMID:9703472] |
| GtoPdb | Binding affinity measured as displacement of ET-3 from CHO cells expressing hETB | - | 6.76 | pKi | 175 | nM | Ki | J Med Chem (1998) 41: 3261-75 [PMID:9703472] |
| ChEMBL | Displacement of radioligand from ETB receptor in human placenta cell membranes | B | 6.76 | pIC50 | 175 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 3381-3394 [PMID:27321813] |
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]
