GF109203X   

GtoPdb Ligand ID: 5193

Synonyms: bisindolylmaleimide I | Gö6850 | GF 109203X
Compound class: Synthetic organic
Comment: GF109203X is a potent, ATP-competitive PKC inhibitor [3].
2D Structure
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Physico-chemical Properties
Hydrogen bond acceptors 4
Hydrogen bond donors 2
Rotatable bonds 6
Topological polar surface area 70.13
Molecular weight 412.19
XLogP 3.7
No. Lipinski's rules broken 0
SMILES / InChI / InChIKey
Canonical SMILES CN(CCCn1cc(c2c1cccc2)C1=C(C(=O)NC1=O)c1c[nH]c2c1cccc2)C
Isomeric SMILES CN(CCCn1cc(c2c1cccc2)C1=C(C(=O)NC1=O)c1c[nH]c2c1cccc2)C
InChI InChI=1S/C25H24N4O2/c1-28(2)12-7-13-29-15-19(17-9-4-6-11-21(17)29)23-22(24(30)27-25(23)31)18-14-26-20-10-5-3-8-16(18)20/h3-6,8-11,14-15,26H,7,12-13H2,1-2H3,(H,27,30,31)
InChI Key QMGUOJYZJKLOLH-UHFFFAOYSA-N

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
protein kinase C epsilon PKCε/PKCepsilon Hs Inhibitor Inhibition 0.5 10.0 1.0
ribosomal protein S6 kinase A2 Rsk3/RSK3 Hs Inhibitor Inhibition 1.4 1.0 -1.0
Pim-3 proto-oncogene, serine/threonine kinase Pim-3/PIM3 Hs Inhibitor Inhibition 1.9 22.0 5.0
ribosomal protein S6 kinase A3 Rsk2/RSK2 Hs Inhibitor Inhibition 2.5 1.0 1.0
protein kinase C beta PKCβI/PKCb1 Hs Inhibitor Inhibition 3.2 4.0 1.0
ribosomal protein S6 kinase A6 Rsk4/RSK4 Hs Inhibitor Inhibition 4.0 4.0 3.0
ribosomal protein S6 kinase A1 Rsk1/RSK1 Hs Inhibitor Inhibition 4.7 15.0 2.0
protein kinase C delta PKCδ/PKCd Hs Inhibitor Inhibition 4.7 2.0 -1.0
Pim-1 proto-oncogene, serine/threonine kinase Pim-1/PIM1 Hs Inhibitor Inhibition 5.3 1.0 1.0
fms related receptor tyrosine kinase 3 Flt3/FLT3 Hs Inhibitor Inhibition 5.6 10.0 1.0
Displaying the top 10 targets  View all targets in screen »