mozavaptan [Ligand Id: 2197] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL420762 (Mozavaptan, Mozavaptane)
  • OT receptor/Oxytocin receptor in Human [ChEMBL: CHEMBL2049] [GtoPdb: 369] [UniProtKB: P30559]
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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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  • 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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  • V1B receptor in Human [GtoPdb: 367] [UniProtKB: P47901]
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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 Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2049] [GtoPdb: 369] [UniProtKB: P30559]
ChEMBL Binding affinity to oxytocin receptor B 6.18 pKi 660 nM Ki J Med Chem (2012) 55: 8588-8602 [PMID:22984902]
V1A receptor/Vasopressin V1a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1889] [GtoPdb: 366] [UniProtKB: P37288]
ChEMBL Binding affinity to vasopressin V1a receptor B 6.71 pKi 195 nM Ki J Med Chem (2012) 55: 8588-8602 [PMID:22984902]
GtoPdb - - 7.1 pKi - - - Br J Pharmacol (1998) 125: 1463-70 [PMID:9884074];
Endocrinology (1997) 138: 4109-22 [PMID:9322919];
J Pharmacol Exp Ther (1998) 287: 860-7 [PMID:9864265]
V1A receptor/Vasopressin V1a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2868] [GtoPdb: 366] [UniProtKB: P30560]
GtoPdb - - 6.3 pKi - - - J Pharmacol Exp Ther (1998) 287: 860-7 [PMID:9864265]
ChEMBL Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liver B 5.85 pIC50 1400 nM IC50 J Med Chem (1996) 39: 3547-3555 [PMID:8784453]
V2 receptor/Vasopressin V2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1790] [GtoPdb: 368] [UniProtKB: P30518]
ChEMBL Binding affinity to vasopressin V2 receptor B 8.01 pKi 9.7 nM Ki J Med Chem (2012) 55: 8588-8602 [PMID:22984902]
ChEMBL Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50% B 8.03 pKi 9.42 nM Ki J Med Chem (2000) 43: 4388-4397 [PMID:11087564]
GtoPdb - - 8.1 pKi - - - Br J Pharmacol (1998) 125: 1463-70 [PMID:9884074];
Endocrinology (1997) 138: 4109-22 [PMID:9322919];
J Pharmacol Exp Ther (1998) 287: 860-7 [PMID:9864265];
Kidney Int (2000) 58: 1613-22 [PMID:11012895];
J Biol Chem (1998) 273: 29462-8 [PMID:9792651]
ChEMBL Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells B 6.3 pIC50 500 nM IC50 J Med Chem (1981) 24: 496-499 [PMID:7241506]
V2 receptor/Vasopressin V2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3766] [GtoPdb: 368] [UniProtKB: Q00788]
GtoPdb - - 8.2 pKi - - - J Pharmacol Exp Ther (1998) 287: 860-7 [PMID:9864265];
J Biol Chem (1998) 273: 29462-8 [PMID:9792651]
ChEMBL Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla B 6.52 pIC50 300 nM IC50 J Med Chem (1981) 24: 496-499 [PMID:7241506]
ChEMBL Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney B 7.92 pIC50 12 nM IC50 J Med Chem (1996) 39: 3547-3555 [PMID:8784453]
V1B receptor in Human [GtoPdb: 367] [UniProtKB: P47901]
GtoPdb - - 4.8 pKi - - - Endocrinology (1997) 138: 4109-22 [PMID:9322919]

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]