conivaptan [Ligand Id: 2203] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1755 (Conivaptan)
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  • V1A receptor/Vasopressin V1a receptor in Human [ChEMBL: CHEMBL1889] [GtoPdb: 366] [UniProtKB: P37288]
  • V1A receptor/Vasopressin V1a receptor in Rat [ChEMBL: CHEMBL2868] [GtoPdb: 366] [UniProtKB: P30560]
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  • V1B receptor/Vasopressin V1b receptor in Rat [ChEMBL: CHEMBL2659] [GtoPdb: 367] [UniProtKB: P48974]
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  • V2 receptor/Vasopressin V2 receptor in Human [ChEMBL: CHEMBL1790] [GtoPdb: 368] [UniProtKB: P30518]
  • V2 receptor/Vasopressin V2 receptor in Rat [ChEMBL: CHEMBL3766] [GtoPdb: 368] [UniProtKB: Q00788]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]