Molecule Details
InChIKeyAHYMHWXQRWRBKT-UHFFFAOYSA-N
Canonical SMILESCN1CCC(COc2cnc(-c3cccc(Cn4nc(-c5cccc(C#N)c5)ccc4=O)c3)nc2)CC1
Clinical Status Data-mined Candidate
Targets (Human+Pathogen)2
Pfam Stratification Cross-Family
Avg pChEMBL7.29
SourceChEMBL;BindingDB
2D Structure
2D structure
Activity Profile
DrugBank Annotations
DrugBank ID DB15133
Drug NameTepotinib
CAS Number1100598-32-0
Groups approved investigational
ATC Codes L01EX21
DescriptionTepotinib is a MET tyrosine kinase inhibitor intended to treat a variety of MET-overexpressing solid tumors.[A228058] It was originally developed in partnership between EMD Serono and the University of Texas M.D. Anderson Cancer Center in 2009 and has since been investigated in the treatment of neur...

Categories: Antineoplastic Agents Antineoplastic and Immunomodulating Agents BCRP/ABCG2 Inhibitors BSEP/ABCB11 Inhibitors Cytochrome P-450 CYP2C8 Substrates Cytochrome P-450 CYP2C9 Inhibitors Cytochrome P-450 CYP2C9 Inhibitors (strong) Cytochrome P-450 CYP3A Inhibitors Cytochrome P-450 CYP3A Substrates Cytochrome P-450 CYP3A4 Inhibitors Cytochrome P-450 CYP3A4 Inhibitors (moderate) Cytochrome P-450 CYP3A4 Substrates Cytochrome P-450 Enzyme Inhibitors Cytochrome P-450 Substrates Kinase Inhibitor MATE 1 Inhibitors MATE 2 Inhibitors MATE inhibitors Mesenchymal Epithelial Transition Inhibitors OCT1 inhibitors OCT2 Inhibitors P-glycoprotein inhibitors P-glycoprotein substrates Protein Kinase Inhibitors Proto-Oncogene Proteins c-met, antagonists & inhibitors Tyrosine Kinase Inhibitors
Cross-references: BindingDB: 50065457 CHEMBL3402762 ChemSpider: 28637823 Drugs Product Database (DPD): 23595 PDB: 3E8 RxCUI: 2477103 Wikipedia: C-Met_inhibitor ZINC: ZINC000043202335
Target Activities (2)
Target Gene Organism Category Pfam pChEMBL Type Source
P08581 MET Homo sapiens Human PF07714 PF01437 PF01403 PF01833 8.5 IC50 ChEMBL;BindingDB
P16083 NQO2 Homo sapiens Human PF02525 6.1 Kd ChEMBL
DrugBank Target Actions (17)
Target Gene Target Name Action Type
P02763 P02763 Alpha-1-acid glycoprotein 1 binder carriers
P02768 ALB Albumin binder carriers
P08684 CYP3A4 Cytochrome P450 3A4 inhibitor enzymes
P11712 CYP2C9 Cytochrome P450 2C9 inhibitor enzymes
P08684 CYP3A4 Cytochrome P450 3A4 substrate enzymes
P10632 CYP2C8 Cytochrome P450 2C8 substrate enzymes
P08581 MET Hepatocyte growth factor receptor inhibitor targets
P49286 MTNR1B Melatonin receptor type 1B inhibitor targets
Q9Y2I1 NISCH Nischarin inhibitor targets
O15244 SLC22A2 Solute carrier family 22 member 2 inhibitor transporters
O15245 SLC22A1 Solute carrier family 22 member 1 inhibitor transporters
O95342 ABCB11 Bile salt export pump inhibitor transporters
P08183 ABCB1 ATP-dependent translocase ABCB1 inhibitor transporters
Q86VL8 SLC47A2 Multidrug and toxin extrusion protein 2 inhibitor transporters
Q96FL8 SLC47A1 Multidrug and toxin extrusion protein 1 inhibitor transporters
Q9UNQ0 ABCG2 Broad substrate specificity ATP-binding cassette transporter ABCG2 inhibitor transporters
P08183 ABCB1 ATP-dependent translocase ABCB1 substrate transporters