Molecule Details
InChIKeyWRFHGDPIDHPWIQ-UHFFFAOYSA-N
Canonical SMILESCCCCC1=NC2(CCCC2)C(=O)N1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2noc(C)c2C)c(COCC)c1
Clinical Status Data-mined Candidate
Targets (Human+Pathogen)2
Pfam Stratification Homologous
Avg pChEMBL8.56
SourceChEMBL;BindingDB
2D Structure
2D structure
Activity Profile
DrugBank Annotations
DrugBank ID DB12548
Drug NameSparsentan
CAS Number254740-64-2
Groups approved investigational
ATC Codes C09XX01
DescriptionSparsentan is a dual antagonist of the endothelin type A receptor (ET<sub>A</sub>R) and the angiotensin II (Ang II) type 1 receptor (AT<sub>1</sub>R) with a similar affinity for both (9.3 nM for ET<sub>A</sub>R and 0.8 nM for AT<sub>1</sub>R).[A257330,L45300] Sparsentan is first in its class and ora...

Categories: Agents Acting on the Renin-Angiotensin System Amides Angiotensin 2 Receptor Blocker Angiotensin II Type 1 Receptor Blockers Angiotensin II receptor antagonists Angiotensin Receptor Antagonists BCRP/ABCG2 Inhibitors BCRP/ABCG2 Substrates Cytochrome P-450 CYP2B6 Inducers Cytochrome P-450 CYP2B6 Inducers (strength unknown) Cytochrome P-450 CYP2C19 Inducers Cytochrome P-450 CYP2C19 Inducers (strength unknown) Cytochrome P-450 CYP2C9 Inducers Cytochrome P-450 CYP2C9 Inducers (strength unknown) Cytochrome P-450 CYP3A Inducers Cytochrome P-450 CYP3A Inhibitors Cytochrome P-450 CYP3A Substrates Cytochrome P-450 CYP3A4 Inducers Cytochrome P-450 CYP3A4 Inducers (strength unknown) Cytochrome P-450 CYP3A4 Inhibitors Cytochrome P-450 CYP3A4 Inhibitors (strength unknown) Cytochrome P-450 CYP3A4 Substrates Cytochrome P-450 Enzyme Inducers Cytochrome P-450 Enzyme Inhibitors Cytochrome P-450 Substrates Dual Endothelin Type A Receptor/Ang II Subtype 1 Receptor Antagonist (DEARA) Endothelin Receptor Antagonists OAT3/SLC22A8 Inhibitors OATP1B3 inhibitors P-glycoprotein inhibitors P-glycoprotein substrates Sulfones Sulfur Compounds
Cross-references: BindingDB: 50175523 CHEMBL539423 ChemSpider: 8433365 PubChem:10257882 PubChem:347828773 RxCUI: 2630535 Wikipedia: Sparsentan
Target Activities (2)
Target Gene Organism Category Pfam pChEMBL Type Source
P30556 AGTR1 Homo sapiens Human PF00001 9.1 Ki ChEMBL;BindingDB
P25101 EDNRA Homo sapiens Human PF00001 8.0 Ki ChEMBL;BindingDB
DrugBank Target Actions (15)
Target Gene Target Name Action Type
P08684 CYP3A4 Cytochrome P450 3A4 inducer enzymes
P11712 CYP2C9 Cytochrome P450 2C9 inducer enzymes
P20813 CYP2B6 Cytochrome P450 2B6 inducer enzymes
P33261 CYP2C19 Cytochrome P450 2C19 inducer enzymes
P08684 CYP3A4 Cytochrome P450 3A4 inhibitor enzymes
P08684 CYP3A4 Cytochrome P450 3A4 substrate enzymes
P25101 EDNRA Endothelin-1 receptor antagonist targets
P30556 AGTR1 Type-1 angiotensin II receptor antagonist targets
P50052 AGTR2 Type-2 angiotensin II receptor antagonist targets
P08183 ABCB1 ATP-dependent translocase ABCB1 inhibitor transporters
Q8TCC7 SLC22A8 Organic anion transporter 3 inhibitor transporters
Q9NPD5 SLCO1B3 Solute carrier organic anion transporter family member 1B3 inhibitor transporters
Q9UNQ0 ABCG2 Broad substrate specificity ATP-binding cassette transporter ABCG2 inhibitor transporters
P08183 ABCB1 ATP-dependent translocase ABCB1 substrate transporters
Q9UNQ0 ABCG2 Broad substrate specificity ATP-binding cassette transporter ABCG2 substrate transporters