Akt inhibitor VIII   Click here for help

GtoPdb Ligand ID: 5921

Synonyms: isozyme-selective, Akti-1/2
PDB Ligand
Compound class: Synthetic organic
Comment: Akt Inhibitor VIII (compound 16h [3]) is a cell-permeable quinoxaline compound that has been shown to potently, selectively, allosterically, and reversibly inhibit Akt (protein kinase B), with selectivity for Akt1/2 over Akt3 [3].
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 5
Hydrogen bond donors 2
Rotatable bonds 5
Topological polar surface area 95.49
Molecular weight 551.24
XLogP 5
No. Lipinski's rules broken 1
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Canonical SMILES O=c1[nH]c2c(n1C1CCN(CC1)Cc1ccc(cc1)c1nc3cc4[nH]cnc4cc3nc1c1ccccc1)cccc2
Isomeric SMILES O=c1[nH]c2c(n1C1CCN(CC1)Cc1ccc(cc1)c1nc3cc4[nH]cnc4cc3nc1c1ccccc1)cccc2
InChI InChI=1S/C34H29N7O/c42-34-39-26-8-4-5-9-31(26)41(34)25-14-16-40(17-15-25)20-22-10-12-24(13-11-22)33-32(23-6-2-1-3-7-23)37-29-18-27-28(36-21-35-27)19-30(29)38-33/h1-13,18-19,21,25H,14-17,20H2,(H,35,36)(H,39,42)

Large-scale screening data

EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen Click here for help
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.


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 »