Molecule Details
InChIKeyWOSKHXYHFSIKNG-UHFFFAOYSA-N
Compound NameLenvatinib
Canonical SMILESCOc1cc2nccc(Oc3ccc(NC(=O)NC4CC4)c(Cl)c3)c2cc1C(N)=O
Clinical Status Data-mined Candidate
Targets (Human+Pathogen)24
Pfam Stratification Cross-Family
Avg pChEMBL7.3
SourceBindingDB;ChEMBL
2D Structure
2D structure
Activity Profile
DrugBank Annotations
DrugBank ID DB09078
Drug NameLenvatinib
CAS Number417716-92-8
Groups approved investigational
ATC Codes L01EX08
DescriptionLenvatinib is a receptor tyrosine kinase (RTK) inhibitor that inhibits the kinase activities of vascular endothelial growth factor (VEGF) receptors VEGFR1 (FLT1), VEGFR2 (KDR), and VEGFR3 (FLT4). Lenvatinib also inhibits other RTKs that have been implicated in pathogenic angiogenesis, tumor growth, ...

Categories: Amides Antineoplastic Agents Antineoplastic and Immunomodulating Agents BCRP/ABCG2 Substrates BSEP/ABCB11 Inhibitors Benzene Derivatives Cytochrome P-450 CYP1A2 Inhibitors Cytochrome P-450 CYP1A2 Inhibitors (strength unknown) Cytochrome P-450 CYP2B6 Inhibitors Cytochrome P-450 CYP2B6 Inhibitors (strength unknown) Cytochrome P-450 CYP2C19 Inhibitors Cytochrome P-450 CYP2C19 inhibitors (strength unknown) Cytochrome P-450 CYP2C8 Inhibitors Cytochrome P-450 CYP2C8 Inhibitors (moderate) Cytochrome P-450 CYP2C9 Inhibitors Cytochrome P-450 CYP2C9 Inhibitors (strength unknown) Cytochrome P-450 CYP2D6 Inhibitors Cytochrome P-450 CYP2D6 Inhibitors (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 (weak) Cytochrome P-450 CYP3A4 Inhibitors Cytochrome P-450 CYP3A4 Inhibitors (weak) Cytochrome P-450 CYP3A4 Substrates Cytochrome P-450 Enzyme Inducers Cytochrome P-450 Enzyme Inhibitors Cytochrome P-450 Substrates Enzyme Inhibitors Heterocyclic Compounds, Fused-Ring Kinase Inhibitor Moderate Risk QTc-Prolonging Agents OAT1/SLC22A6 inhibitors OAT3/SLC22A8 Inhibitors OATP1B1/SLCO1B1 Inhibitors OATP1B3 inhibitors OCT2 Inhibitors P-glycoprotein inhibitors P-glycoprotein substrates Protein Kinase Inhibitors QTc Prolonging Agents Receptor Tyrosine Kinase Inhibitors Tyrosine Kinase Inhibitors
Cross-references: BindingDB: 50331094 ChEBI: 85994 CHEMBL1289601 ChemSpider: 7999567 Drugs Product Database (DPD): 22675 D09919 PDB: LEV PharmGKB: PA166153472 PubChem:9823820 PubChem:310265006 RxCUI: 1603296 Wikipedia: Lenvatinib ZINC: ZINC000003816292
Target Activities (24)
Target Gene Organism Category Pfam pChEMBL Type Source
P35968 KDR Homo sapiens Human PF07679 PF00047 PF13895 PF22971 PF07714 PF21339 PF17988 PF22854 8.4 IC50 ChEMBL;BindingDB
P35916 FLT4 Homo sapiens Human PF07679 PF13927 PF22971 PF07714 PF21339 PF17988 PF22854 8.3 IC50 ChEMBL;BindingDB
P07949 RET Homo sapiens Human PF00028 PF07714 PF17756 PF17812 PF17813 PF22540 8.1 IC50 ChEMBL;BindingDB
P33176 KIF5B Homo sapiens Human PF00225 8.0 IC50 ChEMBL
Q13772 NCOA4 Homo sapiens Human PF12489 8.0 IC50 ChEMBL
Q16204 CCDC6 Homo sapiens Human PF09755 8.0 IC50 ChEMBL
O43353 RIPK2 Homo sapiens Human PF00619 PF07714 8.0 Kd ChEMBL
P21802 FGFR2 Homo sapiens Human PF07679 PF13927 PF07714 8.0 IC50 ChEMBL;BindingDB
P17948 FLT1 Homo sapiens Human PF07679 PF00047 PF13927 PF22971 PF07714 PF21339 PF17988 PF22854 7.7 IC50 ChEMBL;BindingDB
P09619 PDGFRB Homo sapiens Human PF00047 PF13927 PF25305 PF07714 7.4 IC50 ChEMBL;BindingDB
Q08345 DDR1 Homo sapiens Human PF21114 PF00754 PF07714 7.3 Kd ChEMBL
P16234 PDGFRA Homo sapiens Human PF07679 PF25305 PF07714 7.3 IC50 ChEMBL;BindingDB
P22607 FGFR3 Homo sapiens Human PF21165 PF07679 PF13927 PF07714 7.2 IC50 BindingDB
P11362 FGFR1 Homo sapiens Human PF07679 PF00047 PF07714 7.2 IC50 ChEMBL;BindingDB
P49137 MAPKAPK2 Homo sapiens Human PF00069 7.2 Kd ChEMBL
P22455 FGFR4 Homo sapiens Human PF07679 PF13927 PF07714 7.2 IC50 ChEMBL;BindingDB
P35218 CA5A Homo sapiens Human PF00194 6.9 Ki ChEMBL;BindingDB
Q13882 PTK6 Homo sapiens Human PF07714 PF00017 PF00018 6.8 Kd ChEMBL
Q16539 MAPK14 Homo sapiens Human PF00069 6.7 Kd ChEMBL
Q16832 DDR2 Homo sapiens Human PF21114 PF00754 PF07714 6.7 Kd ChEMBL
Q9Y572 RIPK3 Homo sapiens Human PF00069 PF12721 6.5 Kd ChEMBL
Q9UKE5 TNIK Homo sapiens Human PF00780 PF00069 6.2 Kd ChEMBL
Q12851 MAP4K2 Homo sapiens Human PF00780 PF00069 6.2 Kd ChEMBL
O94804 STK10 Homo sapiens Human PF00069 PF12474 6.1 Kd ChEMBL
DrugBank Target Actions (29)
Target Gene Target Name Action Type
P08684 CYP3A4 Cytochrome P450 3A4 inducer enzymes
P05177 CYP1A2 Cytochrome P450 1A2 inhibitor enzymes
P08684 CYP3A4 Cytochrome P450 3A4 inhibitor enzymes
P10632 CYP2C8 Cytochrome P450 2C8 inhibitor enzymes
P10635 CYP2D6 Cytochrome P450 2D6 inhibitor enzymes
P11712 CYP2C9 Cytochrome P450 2C9 inhibitor enzymes
P20813 CYP2B6 Cytochrome P450 2B6 inhibitor enzymes
P33261 CYP2C19 Cytochrome P450 2C19 inhibitor enzymes
P08684 CYP3A4 Cytochrome P450 3A4 substrate enzymes
Q06278 AOX1 Aldehyde oxidase substrate enzymes
P07949 RET Proto-oncogene tyrosine-protein kinase receptor Ret inhibitor targets
P10721 KIT Mast/stem cell growth factor receptor Kit inhibitor targets
P11362 FGFR1 Fibroblast growth factor receptor 1 inhibitor targets
P16234 PDGFRA Platelet-derived growth factor receptor alpha inhibitor targets
P17948 FLT1 Vascular endothelial 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
P35916 FLT4 Vascular endothelial growth factor receptor 3 inhibitor targets
P35968 KDR Vascular endothelial growth factor receptor 2 inhibitor targets
O15244 SLC22A2 Solute carrier family 22 member 2 inhibitor transporters
O95342 ABCB11 Bile salt export pump inhibitor transporters
P08183 ABCB1 ATP-dependent translocase ABCB1 inhibitor transporters
Q4U2R8 SLC22A6 Solute carrier family 22 member 6 inhibitor transporters
Q8TCC7 SLC22A8 Organic anion transporter 3 inhibitor transporters
Q9NPD5 SLCO1B3 Solute carrier organic anion transporter family member 1B3 inhibitor transporters
Q9Y6L6 SLCO1B1 Solute carrier organic anion transporter family member 1B1 inhibitor transporters
P08183 ABCB1 ATP-dependent translocase ABCB1 substrate transporters
Q9UNQ0 ABCG2 Broad substrate specificity ATP-binding cassette transporter ABCG2 substrate transporters