AG 490

Ligand id: 5916

Name: AG 490

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 3
Hydrogen bond donors 3
Rotatable bonds 5
Topological polar surface area 93.35
Molecular weight 294.1
XLogP 3.48
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
unc-51 like kinase 3 ULK3/ULK3 Hs Inhibitor Inhibition 71.2 108.0 86.0
epidermal growth factor receptor EGFR/EGFR Hs Inhibitor Inhibition 72.4 125.0 92.0
3-phosphoinositide dependent protein kinase 1 PDK1/PDK1(PDPK1) Hs Inhibitor Inhibition 74.0 109.0 111.0
cyclin dependent kinase 9 CDK9-cyclin T1/CDK9-cyclin T1 Hs Inhibitor Inhibition 74.9 106.0 72.0
p21 (RAC1) activated kinase 2 PAK2/PAK2 Hs Inhibitor Inhibition 76.8 103.0 85.0
MAP kinase interacting serine/threonine kinase 1 nd/MNK1 Hs Inhibitor Inhibition 77.8
erb-b2 receptor tyrosine kinase 4 ErbB4/ERBB4(HER4) Hs Inhibitor Inhibition 80.9 95.0 110.0
casein kinase 2, alpha prime polypeptide subunit CK2α2/CK2a2 Hs Inhibitor Inhibition 81.9 129.0 100.0
fibroblast growth factor receptor 4 FGFR4/FGFR4 Hs Inhibitor Inhibition 84.2 125.0 105.0
PDZ binding kinase nd/PBK(TOPK) Hs Inhibitor Inhibition 84.2
Displaying the top 10 targets  View all targets in screen »