Molecule Details
InChIKeyOLAHOMJCDNXHFI-UHFFFAOYSA-N
Compound NameErdafitinib
Canonical SMILESCOc1cc(OC)cc(N(CCNC(C)C)c2ccc3ncc(-c4cnn(C)c4)nc3c2)c1
Clinical Status Data-mined Candidate
Targets (Human+Pathogen)6
Pfam Stratification Cross-Family
Avg pChEMBL7.99
SourceChEMBL;BindingDB
2D Structure
2D structure
Activity Profile
DrugBank Annotations
DrugBank ID DB12147
Drug NameErdafitinib
CAS Number1346242-81-6
Groups approved investigational
ATC Codes L01EN01
DescriptionIn early April of 2019, the US FDA approved Janssen Pharmaceutical Companies' brand name Balversa (erdafitinib) as the first-ever fibroblast growth factor receptor (FGFR) kinase inhibitor indicated for patients with locally advanced or metastatic urothelial carcinoma, with susceptible FGFR3 or FGFR2...

Categories: Antineoplastic Agents Antineoplastic and Immunomodulating Agents Cytochrome P-450 CYP2C9 Substrates Cytochrome P-450 CYP2C9 Substrates with a Narrow Therapeutic Index 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 CYP3A4 Substrates with a Narrow Therapeutic Index Cytochrome P-450 Enzyme Inducers Cytochrome P-450 Enzyme Inhibitors Cytochrome P-450 Substrates Fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitors Heterocyclic Compounds, Fused-Ring Kinase Inhibitor Narrow Therapeutic Index Drugs OCT2 Inhibitors P-glycoprotein inhibitors P-glycoprotein substrates P-glycoprotein substrates with a Narrow Therapeutic Index Protein Kinase Inhibitors Receptors, Fibroblast Growth Factor, antagonists & inhibitors Tumor Suppressor Proteins Tyrosine Kinase Inhibitors
Cross-references: BindingDB: 50525939 CHEMBL3545376 ChemSpider: 35308353 Drugs Product Database (DPD): 23382 PDB: 5SF PubChem:67462786 PubChem:347828443 RxCUI: 2123125 Wikipedia: Erdafitinib ZINC: ZINC000168520308
Target Activities (6)
Target Gene Organism Category Pfam pChEMBL Type Source
P11362 FGFR1 Homo sapiens Human PF07679 PF00047 PF07714 8.9 IC50 ChEMBL;BindingDB
P21802 FGFR2 Homo sapiens Human PF07679 PF13927 PF07714 8.6 IC50 ChEMBL;BindingDB
P22607 FGFR3 Homo sapiens Human PF21165 PF07679 PF13927 PF07714 8.5 IC50 ChEMBL;BindingDB
P22455 FGFR4 Homo sapiens Human PF07679 PF13927 PF07714 8.2 IC50 ChEMBL;BindingDB
P35968 KDR Homo sapiens Human PF07679 PF00047 PF13895 PF22971 PF07714 PF21339 PF17988 PF22854 7.4 IC50 ChEMBL;BindingDB
P41212 ETV6 Homo sapiens Human PF00178 PF02198 6.2 IC50 ChEMBL
DrugBank Target Actions (18)
Target Gene Target Name Action Type
P02763 P02763 alpha1-acid glycoprotein binder carriers
P08684 CYP3A4 Cytochrome P450 3A4 inducer enzymes
P08684 CYP3A4 Cytochrome P450 3A4 inhibitor enzymes
P08684 CYP3A4 Cytochrome P450 3A4 substrate enzymes
P11712 CYP2C9 Cytochrome P450 2C9 substrate enzymes
P11362 FGFR1 Fibroblast growth factor receptor 1 inhibitor targets
P21802 FGFR2 Fibroblast growth factor receptor 2 inhibitor targets
P22455 FGFR4 Fibroblast growth factor receptor 4 inhibitor targets
P22607 FGFR3 Fibroblast growth factor receptor 3 inhibitor targets
P07333 CSF1R Macrophage colony-stimulating factor 1 receptor substrate targets
P07949 RET Proto-oncogene tyrosine-protein kinase receptor Ret substrate targets
P09619 PDGFRB Platelet-derived growth factor receptor beta substrate targets
P10721 KIT Mast/stem cell growth factor receptor Kit substrate targets
P16234 PDGFRA Platelet-derived growth factor receptor alpha substrate targets
P35968 KDR Vascular endothelial growth factor receptor 2 substrate targets
O15244 SLC22A2 Solute carrier family 22 member 2 inhibitor transporters
P08183 ABCB1 ATP-dependent translocase ABCB1 inhibitor transporters
P08183 ABCB1 ATP-dependent translocase ABCB1 substrate transporters