encorafenib
Ligand Summary
Encorafenib is a kinase inhibitor that targets BRAF V600E, as well as wild-type BRAF and CRAF. Mutations in the BRAF gene, such as BRAF V600E, can result in constitutively activated BRAF kinases that may stimulate tumor cell growth. Encorafenib was also able to bind to other kinases in vitro including JNK1, JNK2, JNK3, LIMK1, LIMK2, MEK4, and STK36 and substantially reduce ligand binding to these kinases at clinically achievable concentrations. Encorafenib inhibited in vitro growth of tumor cell lines expressing BRAF V600 E, D, and K mutations. In mice implanted with tumor cells expressing BRAF V600E, encorafenib induced tumor regressions associated with RAF/MEK/ERK pathway suppression.
UNII: 8L7891MRB6
PubChem: 50922675
ChEMBL: CHEMBL3301612
DrugCentral: 5289
LyCHI: AC8LU4HSBKTN
Target Activities
16 Activities
Items per page:
1 – 10 of 16
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
IC50 | ||||||
IC50 | ||||||
IC50 | ||||||
IC50 | ||||||
IC50 | ||||||
IC50 | ||||||
IC50 | ||||||
IC50 | ||||||
Kd | ||||||
Kd | ||||||