Akt inhibitor VIII

Ligand id: 5921

Name: Akt inhibitor VIII

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 8
Hydrogen bond donors 2
Rotatable bonds 5
Topological polar surface area 90.04
Molecular weight 551.24
XLogP 7.27
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: 1-2

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
EPH receptor A3 EphA3/EPHA3 Hs Inhibitor Inhibition 71.9 112.0 76.0
protein kinase N2 PRK2/PKN2(PRK2) Hs Inhibitor Inhibition 73.2 112.0 115.0
death associated protein kinase 1 DAPK1/DAPK1 Hs Inhibitor Inhibition 82.9 93.0 95.0
mitogen-activated protein kinase kinase kinase 7 TAK1/TAK1 Hs Inhibitor Inhibition 84.1 97.0 96.0
protein kinase C alpha PKCα/PKCa Hs Inhibitor Inhibition 84.3 104.0 104.0
EPH receptor A1 EphA1/EPHA1 Hs Inhibitor Inhibition 84.4 102.0 90.0
cyclin dependent kinase 1 CDK1-cyclin B/CDK1-cyclin B Hs Inhibitor Inhibition 85.0 109.0 96.0
NIMA related kinase 11 NEK11/NEK11 Hs Inhibitor Inhibition 86.4 75.0 88.0
mitogen-activated protein kinase kinase 2 nd/MEK2 Hs Inhibitor Inhibition 86.6
beta adrenergic receptor kinase 2 nd/GRK3 Hs Inhibitor Inhibition 87.3
Displaying the top 10 targets  View all targets in screen »