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ChEMBL ligand: CHEMBL420762 (Mozavaptan, Mozavaptane) |
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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 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]