AG 1296

Ligand id: 5915

Name: AG 1296

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 2
Hydrogen bond donors 0
Rotatable bonds 3
Topological polar surface area 44.24
Molecular weight 266.11
XLogP 3.9
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
mitogen-activated protein kinase kinase kinase kinase 4 nd/HGK(MAP4K4) Hs Inhibitor Inhibition 62.1
erb-b2 receptor tyrosine kinase 4 ErbB4/ERBB4(HER4) Hs Inhibitor Inhibition 65.9 88.0 85.0
fms related tyrosine kinase 3 Flt3/FLT3 Hs Inhibitor Inhibition 65.9 57.0 16.0
KIT proto-oncogene receptor tyrosine kinase cKit/c-Kit Hs Inhibitor Inhibition 67.3 84.0 24.0
aurora kinase B Aurora-B/Aurora B Hs Inhibitor Inhibition 74.4 83.0 50.0
transforming growth factor beta receptor 2 nd/TGFBR2 Hs Inhibitor Inhibition 75.0
p21 (RAC1) activated kinase 4 PAK4/PAK4 Hs Inhibitor Inhibition 75.9 102.0 93.0
Protein kinase G (PKG) 1 PKG1α/PKG1a Hs Inhibitor Inhibition 77.1 119.0 114.0
LIM domain kinase 1 LIMK1/LIMK1 Hs Inhibitor Inhibition 77.7 112.0 95.0
fibroblast growth factor receptor 4 FGFR4/FGFR4 Hs Inhibitor Inhibition 78.7 114.0 98.0
Displaying the top 10 targets  View all targets in screen »