diacylglycerol kinase inhibitor II

Ligand id: 5957

Name: diacylglycerol kinase inhibitor II

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 4
Hydrogen bond donors 1
Rotatable bonds 5
Topological polar surface area 67.67
Molecular weight 489.17
XLogP 6.77
No. Lipinski's rules broken 1

Molecular properties generated using the CDK

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

Bioactivity Comments
R59949 selectively inhibits Ca2+-activated diacylglycerol kinases, whilst the Ca2+-independent DGKs are almost totally insensitive to this compound [4]. In in vitro assays using various purified DGK preparations, R59949 inhibits enzyme activity by between 70-95% for the Ca2+-activated DGKs, but by only 18-22% for the Ca2+-independent DGKs [4]. R59949 inhibits DGK in isolated platelet membranes and in intact platelets with IC50 values of 300 and 120 nM respectively [2].