Molecule Details
InChIKeyTUYWTLTWNJOZNY-UHFFFAOYSA-N
Compound NameTezosentan
Canonical SMILESCOc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccnc(-c3nnn[nH]3)c2)nc1OCCO
Clinical Status Data-mined Candidate
Targets (Human+Pathogen)2
Pfam Stratification Homologous
Avg pChEMBL7.71
SourceChEMBL;BindingDB
2D Structure
2D structure
Activity Profile
DrugBank Annotations
DrugBank ID DB06558
Drug NameTezosentan
CAS Number180384-57-0
Groups investigational
ATC Codes nan
DescriptionTezosentan is an intravenous endothelin receptor A/B antagonist. Tezosentan was initially developed for vasodilation in patients with acute heart failure but studies have shown that it does not assist in the treatment of dyspnea or prevent cardiovascular events.

Categories: Cardiovascular Agents Receptors, Endothelin Vasodilating Agents
Cross-references: BindingDB: 50143800 CHEMBL61780 ChemSpider: 133242 PubChem:151174 Wikipedia: Tezosentan ZINC: ZINC000003954692
Target Activities (2)
Target Gene Organism Category Pfam pChEMBL Type Source
P25101 EDNRA Homo sapiens Human PF00001 7.7 IC50 ChEMBL;BindingDB
P24530 EDNRB Homo sapiens Human PF00001 7.7 IC50 ChEMBL;BindingDB
DrugBank Target Actions (2)
Target Gene Target Name Action Type
P24530 EDNRB Endothelin receptor type B binder targets
P25101 EDNRA Endothelin-1 receptor binder targets