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 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]
