Molecule Details
InChIKeyRENRQMCACQEWFC-UGKGYDQZSA-N
Compound NameIptacopan
Canonical SMILESCCO[C@H]1CCN(Cc2c(OC)cc(C)c3[nH]ccc23)[C@H](c2ccc(C(=O)O)cc2)C1
Clinical Status Data-mined Candidate
Targets (Human+Pathogen)2
Pfam Stratification Cross-Family
Avg pChEMBL7.69
SourceBindingDB;ChEMBL
2D Structure
2D structure
Activity Profile
DrugBank Annotations
DrugBank ID DB16200
Drug NameIptacopan
CAS Number1644670-37-0
Groups approved investigational
ATC Codes L04AJ08
DescriptionIptacopan is a small-molecule factor B inhibitor previously investigated as a potential treatment for the rare blood disease paroxysmal nocturnal hemoglobinuria (PNH) by inhibiting the complement factor B.[A262566] Factor B is a positive regulator of the alternative complement pathway, where it acti...

Categories: Acids, Carbocyclic Antineoplastic and Immunomodulating Agents Benzene Derivatives Complement Factor B Inhibitor Complement Inactivating Agents Cytochrome P-450 CYP2C8 Substrates Cytochrome P-450 CYP2D6 Substrates Cytochrome P-450 Substrates Heterocyclic Compounds, Fused-Ring Immunosuppressive Agents UGT1A1 Substrates UGT1A3 substrates
Cross-references: BindingDB: 160475 CHEMBL4594448 ChemSpider: 75533872 Drugs Product Database (DPD): 24049 PDB: JGQ RxCUI: 2671061 Wikipedia: Iptacopan ZINC: ZINC000223246892
Target Activities (2)
Target Gene Organism Category Pfam pChEMBL Type Source
P00751 CFB Homo sapiens Human PF00084 PF00089 PF00092 8.0 IC50 ChEMBL;BindingDB
P07911 UMOD Homo sapiens Human PF23283 PF12947 PF07645 PF00100 PF23344 7.4 IC50 BindingDB
DrugBank Target Actions (8)
Target Gene Target Name Action Type
P02763 P02763 Alpha-1-acid glycoprotein 1 binder carriers
P02768 ALB Albumin binder carriers
P10632 CYP2C8 Cytochrome P450 2C8 substrate enzymes
P10635 CYP2D6 Cytochrome P450 2D6 substrate enzymes
P22309 UGT1A1 UDP-glucuronosyltransferase 1A1 substrate enzymes
P35503 P35503 UDP-glucuronosyltransferase 1A3 substrate enzymes
Q9HAW9 Q9HAW9 UDP-glucuronosyltransferase 1A8 substrate enzymes
P00751 CFB Complement factor B inhibitor targets