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 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]
