EGFR/ErbB-2/ErbB-4 inhibitor

Ligand id: 5965

Name: EGFR/ErbB-2/ErbB-4 inhibitor

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 6
Hydrogen bond donors 2
Rotatable bonds 4
Topological polar surface area 79.8
Molecular weight 355.06
XLogP 3.36
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: 1-2

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
Janus kinase 3 JAK3/JAK3 Hs Inhibitor Inhibition -0.2 51.0 59.0
epidermal growth factor receptor EGFR/EGFR Hs Inhibitor Inhibition 1.2 -4.0 -3.0
TXK tyrosine kinase Txk/TXK Hs Inhibitor Inhibition 1.7 52.0 14.0
erb-b2 receptor tyrosine kinase 4 ErbB4/ERBB4(HER4) Hs Inhibitor Inhibition 1.9 16.0 14.0
erb-b2 receptor tyrosine kinase 2 nd/ERBB2(HER2) Hs Inhibitor Inhibition 2.4
BMX non-receptor tyrosine kinase Bmx/BMX(ETK) Hs Inhibitor Inhibition 2.5 18.0 19.0
Bruton tyrosine kinase BTK/BTK Hs Inhibitor Inhibition 2.9 47.0 16.0
BLK proto-oncogene, Src family tyrosine kinase Blk/BLK Hs Inhibitor Inhibition 21.3 82.0 49.0
receptor interacting serine/threonine kinase 2 RIPK2/RIPK2 Hs Inhibitor Inhibition 38.7 82.0 60.0
CDC like kinase 3 CLK3/CLK3 Hs Inhibitor Inhibition 47.1 83.0 125.0
Displaying the top 10 targets  View all targets in screen »