CHIR-265

Ligand id: 5674

Name: CHIR-265

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 6
Hydrogen bond donors 2
Rotatable bonds 7
Topological polar surface area 80.65
Molecular weight 518.13
XLogP 7.09
No. Lipinski's rules broken 1

Molecular properties generated using the CDK

View interactive charts of activity data from ChEMBL and GtoPdb across species (New!)

Bioactivity Comments
In biochemical assays, CHIR-265 (as RAF265) inhibits B-RafV600E, B-Raf, c-Raf, VEGFR2, c-Kit, PDGFRβ with IC50s <100 nM [3]. In vivo, RAF265 inhibits tumour volume by >70% in HCT116 (human colon carcinoma cell) xenografts at 12 mg/kg [2].
Selectivity at human enzymes
Key to terms and symbols Click column headers to sort
Target Type Action Affinity Units Concentration range (M) Reference
B-Raf proto-oncogene, serine/threonine kinase Inhibitor Inhibition 5.9 pKd - 1
pKd 5.9 (Kd 1.2x10-6 M) [1]