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

Large-scale screening data

EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx


Reference: 1,3

Key to terms and symbols Click column headers to sort
Target Name in screen Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
protein kinase C alpha PKCα/PKCa Hs Inhibitor Inhibition 73.1 108.0 105.0
mitogen-activated protein kinase kinase kinase 14 nd/NIK(MAP3K14) Hs Inhibitor Inhibition 75.7
mitogen-activated protein kinase 10 JNK3/JNK3 Hs Inhibitor Inhibition 76.2 98.0 54.0
cyclin dependent kinase 1 CDK1-cyclin B/CDK1-cyclin B Hs Inhibitor Inhibition 83.0 114.0 104.0
BMX non-receptor tyrosine kinase Bmx/BMX(ETK) Hs Inhibitor Inhibition 85.5 82.0 78.0
dual serine/threonine and tyrosine protein kinase nd/RIPK5 Hs Inhibitor Inhibition 86.5
erb-b2 receptor tyrosine kinase 4 ErbB4/ERBB4(HER4) Hs Inhibitor Inhibition 87.4 102.0 66.0
CDC like kinase 2 CLK2/CLK2 Hs Inhibitor Inhibition 87.8 115.0 94.0
MAP kinase interacting serine/threonine kinase 2 Mnk2/MNK2 Hs Inhibitor Inhibition 89.5 112.0 103.0
salt inducible kinase 2 nd/SIK2 Hs Inhibitor Inhibition 89.7
Displaying the top 10 targets  View all targets in screen »