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 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]