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ChEMBL ligand: CHEMBL1755 (Conivaptan) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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OT receptor/Oxytocin receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3996] [GtoPdb: 369] [UniProtKB: P70536] | ||||||||
ChEMBL | Displacement of [3H]OT from OTR in Wistar rat uterus membranes incubated for 60 mins by microplate scintillation counting method | B | 7.35 | pKi | 44.4 | nM | Ki | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
V1A receptor/Vasopressin V1a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1889] [GtoPdb: 366] [UniProtKB: P37288] | ||||||||
GtoPdb | - | - | 8.4 | pKi | - | - | - |
Br J Pharmacol (1998) 125: 1463-70 [PMID:9884074]; Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 63-9 [PMID:9459574] |
ChEMBL | Displacement [3H]Arg human recombinant Vasopressin V1a receptor | B | 9.37 | pKi | 0.43 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 3742-3745 [PMID:20471258] |
ChEMBL | Antagonist activity at human Vasopressin V1a receptor assessed as inhibition of intracellular calcium mobilization by FLIPR assay | F | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3742-3745 [PMID:20471258] |
V1A receptor/Vasopressin V1a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2868] [GtoPdb: 366] [UniProtKB: P30560] | ||||||||
ChEMBL | Displacement of [3H]AVP from V1A receptor in Wistar rat liver membranes incubated for 60 mins by microplate scintillation counting method | B | 9.32 | pKi | 0.48 | nM | Ki | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
V1B receptor/Vasopressin V1b receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2659] [GtoPdb: 367] [UniProtKB: P48974] | ||||||||
ChEMBL | Displacement of [3H]AVP from V1B receptor in Wistar rat pituitary membranes incubated for 60 mins by microplate scintillation counting method | B | 5 | pKi | >10000 | nM | Ki | 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 | - | - | 9.44 | pKi | 0.36 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 3742-5 [PMID:20471258] |
ChEMBL | Displacement [3H]Arg human recombinant Vasopressin V2 receptor | B | 9.44 | pKi | 0.36 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 3742-3745 [PMID:20471258] |
ChEMBL | Antagonist activity at human Vasopressin 2 receptor assessed as inhibition of intracellular cAMP accumulation | F | 7.96 | pIC50 | 11 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3742-3745 [PMID:20471258] |
V2 receptor/Vasopressin V2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3766] [GtoPdb: 368] [UniProtKB: Q00788] | ||||||||
ChEMBL | Displacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting method | B | 8.52 | pKi | 3.04 | nM | Ki | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
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]