tolvaptan [Ligand Id: 2226] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL344159 (Jinarc, Jynarque, OPC-41061, OPC-41061(TOLVAPTAN), Samsca, Tolvaptan) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| V1A receptor/Vasopressin V1a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1889] [GtoPdb: 366] [UniProtKB: P37288] | ||||||||
| ChEMBL | Displacement of [3H]-arginine-vasopressin from human V1A receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay | B | 7.49 | pKi | 32 | nM | Ki | J Med Chem (2021) 64: 10445-10468 [PMID:34255509] |
| GtoPdb | - | - | 7.9 | pKi | - | - | - | J Pharmacol Exp Ther (1998) 287: 860-7 [PMID:9864265] |
| ChEMBL | Inhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate reader | F | 6.33 | pIC50 | 470 | nM | IC50 | J Med Chem (2021) 64: 10445-10468 [PMID:34255509] |
| V1A receptor in Rat [GtoPdb: 366] [UniProtKB: P30560] | ||||||||
| GtoPdb | - | - | 6.5 | pKi | - | - | - | J Pharmacol Exp Ther (1998) 287: 860-7 [PMID:9864265] |
| V2 receptor/Vasopressin V2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1790] [GtoPdb: 368] [UniProtKB: P30518] | ||||||||
| ChEMBL | Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay | B | 9 | pKi | 1 | nM | Ki | J Med Chem (2021) 64: 10445-10468 [PMID:34255509] |
| ChEMBL | Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50% | B | 9.37 | pKi | 0.43 | nM | Ki | J Med Chem (2000) 43: 4388-4397 [PMID:11087564] |
| GtoPdb | - | - | 9.37 | pKi | 0.43 | nM | Ki | J Pharmacol Exp Ther (1998) 287: 860-7 [PMID:9864265] |
| V2 receptor in Rat [GtoPdb: 368] [UniProtKB: Q00788] | ||||||||
| GtoPdb | - | - | 8.9 | pKi | - | - | - | J Pharmacol Exp Ther (1998) 287: 860-7 [PMID:9864265] |
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]
