Molecule Details
InChIKeyIKENVDNFQMCRTR-UHFFFAOYSA-N
Compound NameConivaptan
Canonical SMILESCc1nc2c([nH]1)-c1ccccc1N(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)CC2
Clinical Status Data-mined Candidate
Targets (Human+Pathogen)2
Pfam Stratification Homologous
Avg pChEMBL8.82
SourceChEMBL;BindingDB
2D Structure
2D structure
Activity Profile
DrugBank Annotations
DrugBank ID DB00872
Drug NameConivaptan
CAS Number210101-16-9
Groups approved
ATC Codes C03XA02
DescriptionConivaptan is a non-peptide inhibitor of antidiuretic hormone (vasopressin). It was approved in 2004 for hyponatremia (low blood sodium levels) caused by syndrome of inappropriate antidiuretic hormone (SIADH). Conivaptan inhibits both isotypes of the vasopressin receptor (V1a and V2).

Categories: Antidiuretic Hormone Receptor Antagonists Cytochrome P-450 CYP3A Inhibitors Cytochrome P-450 CYP3A Substrates Cytochrome P-450 CYP3A4 Inhibitors Cytochrome P-450 CYP3A4 Inhibitors (strong) Cytochrome P-450 CYP3A4 Substrates Cytochrome P-450 CYP3A4 Substrates with a Narrow Therapeutic Index Cytochrome P-450 Enzyme Inhibitors Cytochrome P-450 Substrates Diuretics Heterocyclic Compounds, Fused-Ring Hypotensive Agents Narrow Therapeutic Index Drugs Natriuretic Agents P-glycoprotein inhibitors
Cross-references: BindingDB: 85095 ChEBI: 681850 CHEMBL1755 ChemSpider: 133239 Guide to Pharmacology: 2203 IUPHAR: 2203 D07748 PharmGKB: PA164742939 PubChem:151171 PubChem:46504533 RxCUI: 302285 Therapeutic Targets Database: DNC001525 Wikipedia: Conivaptan ZINC: ZINC000012503187
Target Activities (2)
Target Gene Organism Category Pfam pChEMBL Type Source
P37288 AVPR1A Homo sapiens Human PF00001 PF08983 8.9 IC50 ChEMBL;BindingDB
P30518 AVPR2 Homo sapiens Human PF00001 8.7 IC50 ChEMBL;BindingDB
DrugBank Target Actions (5)
Target Gene Target Name Action Type
P08684 CYP3A4 Cytochrome P450 3A4 inhibitor enzymes
P08684 CYP3A4 Cytochrome P450 3A4 substrate enzymes
P30518 AVPR2 Vasopressin V2 receptor antagonist targets
P37288 AVPR1A Vasopressin V1a receptor antagonist targets
P08183 ABCB1 ATP-dependent translocase ABCB1 inhibitor transporters