bisindolylmaleimide IV

Ligand id: 5937

Name: bisindolylmaleimide IV

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 5
Hydrogen bond donors 3
Rotatable bonds 2
Topological polar surface area 77.75
Molecular weight 327.1
XLogP 3.22
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
ribosomal protein S6 kinase A2 Rsk3/RSK3 Hs Inhibitor Inhibition 11.5 5.0 0.0
fms related tyrosine kinase 3 Flt3/FLT3 Hs Inhibitor Inhibition 16.1 19.0 1.0
Pim-1 proto-oncogene, serine/threonine kinase Pim-1/PIM1 Hs Inhibitor Inhibition 17.2 12.0 0.0
ribosomal protein S6 kinase A6 Rsk4/RSK4 Hs Inhibitor Inhibition 19.2 9.0 1.0
protein kinase C epsilon PKCε/PKCepsilon Hs Inhibitor Inhibition 24.0 63.0 21.0
protein kinase C beta PKCβI/PKCb1 Hs Inhibitor Inhibition 26.1 66.0 23.0
protein kinase C alpha PKCα/PKCa Hs Inhibitor Inhibition 27.7 26.0 4.0
glycogen synthase kinase 3 alpha GSK3α/GSK3a Hs Inhibitor Inhibition 27.7 19.0 4.0
glycogen synthase kinase 3 beta GSK3β/GSK3b Hs Inhibitor Inhibition 28.4 31.0 6.0
Pim-3 proto-oncogene, serine/threonine kinase Pim-3/PIM3 Hs Inhibitor Inhibition 32.7 93.0 73.0
Displaying the top 10 targets  View all targets in screen »