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 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]