Molecule Details
InChIKeyACWZRVQXLIRSDF-UHFFFAOYSA-N
Canonical SMILESCn1cnc2c(F)c(Nc3ccc(Br)cc3F)c(C(=O)NOCCO)cc21
Clinical Status Data-mined Candidate
Targets (Human+Pathogen)2
Pfam Stratification Homologous
Avg pChEMBL7.92
SourceChEMBL;BindingDB
2D Structure
2D structure
Activity Profile
DrugBank Annotations
DrugBank ID DB11967
Drug NameBinimetinib
CAS Number606143-89-9
Groups approved investigational
ATC Codes L01EE03
DescriptionBinimetinib, also known as _Mektovi_, is a potent and selective oral mitogen-activated protein kinase 1/2 (MEK 1/2) inhibitor which is combined with [Encorafenib].[A34275,L3335] On June 27, 2018, the Food and Drug Administration approved the combination of [Encorafenib] and binimetinib (BRAFTOVI and...

Categories: Antineoplastic Agents Antineoplastic and Immunomodulating Agents BCRP/ABCG2 Substrates Cytochrome P-450 CYP1A2 Substrates Cytochrome P-450 CYP1A2 Substrates with a Narrow Therapeutic Index Cytochrome P-450 CYP2C19 Substrates Cytochrome P-450 CYP2C19 Substrates with a Narrow Therapeutic Index Cytochrome P-450 Substrates Heterocyclic Compounds, Fused-Ring Kinase Inhibitor MAP Kinase Kinase 1, antagonists & inhibitors MAP Kinase Kinase 2, antagonists & inhibitors Mitogen-activated protein kinase (MEK) inhibitors Narrow Therapeutic Index Drugs P-glycoprotein substrates P-glycoprotein substrates with a Narrow Therapeutic Index Protein Kinase Inhibitors UGT1A1 Substrates UGT1A1 Substrates with a Narrow Therapeutic Index
Cross-references: ChEBI: 145371 CHEMBL3187723 ChemSpider: 8463660 Drugs Product Database (DPD): 23571 PDB: QO7 PharmGKB: PA166179867 PubChem:10288191 PubChem:347828291 RxCUI: 2049122 Wikipedia: Binimetinib ZINC: ZINC000038460704
Target Activities (2)
Target Gene Organism Category Pfam pChEMBL Type Source
P36507 MAP2K2 Homo sapiens Human PF00069 7.9 IC50 ChEMBL
Q02750 MAP2K1 Homo sapiens Human PF00069 7.9 IC50 ChEMBL;BindingDB
DrugBank Target Actions (8)
Target Gene Target Name Action Type
P02768 ALB Albumin binder carriers
P05177 CYP1A2 Cytochrome P450 1A2 substrate enzymes
P22309 UGT1A1 UDP-glucuronosyltransferase 1A1 substrate enzymes
P33261 CYP2C19 Cytochrome P450 2C19 substrate enzymes
P36507 MAP2K2 Dual specificity mitogen-activated protein kinase kinase 2 inhibitor targets
Q02750 MAP2K1 Dual specificity mitogen-activated protein kinase kinase 1 inhibitor targets
P08183 ABCB1 ATP-dependent translocase ABCB1 substrate transporters
Q9UNQ0 ABCG2 Broad substrate specificity ATP-binding cassette transporter ABCG2 substrate transporters