Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL420762 (Mozavaptan, Mozavaptane) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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]