carfilzomib

Ligand id: 7420

Name: carfilzomib

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 12
Hydrogen bond donors 4
Rotatable bonds 24
Topological polar surface area 158.47
Molecular weight 719.43
XLogP 7.56
No. Lipinski's rules broken 3

Molecular properties generated using the CDK

View interactive charts of activity data from GtoPdb and ChEMBL (where available) across species

Bioactivity Comments
Carfilzomib causes a dose-dependent inhibition of 20S proteasomal chymotrypsin-like activity in CD138+ plasma cells purified from MM patient samples [2]. Maximum inhibition of approximately 70% is achieved with 10-25nM carfilzomib.
Selectivity at enzymes
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Affinity Units Concentration range (M) Reference
proteasome subunit beta 5 Hs Inhibitor Inhibition 8.2 pIC50 - 3
pIC50 8.2 (IC50 5.7x10-9 M) [3]