OPC-51803 [Ligand Id: 2173] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL332447 |
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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]-AVP from human V1A receptor expressed in human HeLa cell membranes incubated for 2 hrs by scintillation counting method | B | 6.09 | pKi | 819 | nM | Ki | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
| GtoPdb | - | - | 6.1 | pKi | - | - | - | Br J Pharmacol (2000) 129: 1700-6 [PMID:10780976] |
| V1B receptor/Vasopressin V1b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1921] [GtoPdb: 367] [UniProtKB: P47901] | ||||||||
| ChEMBL | Displacement of [3H]-AVP from human V1B receptor expressed in human HeLa cell membranes incubated for 2 hrs by scintillation counting method | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
| V2 receptor/Vasopressin V2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1790] [GtoPdb: 368] [UniProtKB: P30518] | ||||||||
| GtoPdb | - | - | 7 | pKi | - | - | - | Br J Pharmacol (2000) 129: 1700-6 [PMID:10780976] |
| ChEMBL | Displacement of [3H]-AVP from human V2 receptor expressed in human HeLa cell membranes incubated for 2 hrs by scintillation counting method | B | 7.04 | pKi | 91.9 | nM | Ki | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
| ChEMBL | Binding affinity against human Vasopressin V2 receptor expressed in HeLa cells was determined | B | 6.48 | pIC50 | 330 | nM | IC50 | J Med Chem (2002) 45: 3805-3808 [PMID:12166952] |
| ChEMBL | Agonist activity at human V2 receptor expressed in human HeLa cells assessed as stimulation of cAMP accumulation by radioimmunoassay | F | 6.72 | pEC50 | 189 | nM | EC50 | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
| V2 receptor/Vasopressin V2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3766] [GtoPdb: 368] [UniProtKB: Q00788] | ||||||||
| ChEMBL | Binding affinity against Vasopressin V2 receptor was determined in Brattleboro rats | B | 6.64 | pIC50 | 230 | nM | IC50 | J Med Chem (2002) 45: 3805-3808 [PMID:12166952] |
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]
