Chk2 inhibitor II

Ligand id: 5954

Name: Chk2 inhibitor II

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 4
Hydrogen bond donors 2
Rotatable bonds 4
Topological polar surface area 81
Molecular weight 363.08
XLogP 4.57
No. Lipinski's rules broken 0

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
checkpoint kinase 2 CHK2/CHK2 Hs Inhibitor Inhibition 1.4 0.0 0.0
fms related tyrosine kinase 3 Flt3/FLT3 Hs Inhibitor Inhibition 48.5 65.0 27.0
ribosomal protein S6 kinase A2 Rsk3/RSK3 Hs Inhibitor Inhibition 48.5 18.0 5.0
mitogen-activated protein kinase kinase kinase kinase 4 nd/HGK(MAP4K4) Hs Inhibitor Inhibition 55.9
ribosomal protein S6 kinase A6 Rsk4/RSK4 Hs Inhibitor Inhibition 60.7 27.0 29.0
KIT proto-oncogene receptor tyrosine kinase cKit/c-Kit Hs Inhibitor Inhibition 61.4 106.0 90.0
Protein kinase G (PKG) 2 nd/PKG2(PRKG2) Hs Inhibitor Inhibition 67.5
megakaryocyte-associated tyrosine kinase nd/CTK(MATK) Hs Inhibitor Inhibition 68.5
transforming growth factor beta receptor 2 nd/TGFBR2 Hs Inhibitor Inhibition 72.1
calcium/calmodulin dependent protein kinase I CaMKI/CAMK1a Hs Inhibitor Inhibition 72.5 94.0 92.0
Displaying the top 10 targets  View all targets in screen »