AG 1295   Click here for help

GtoPdb Ligand ID: 5914

Synonyms: AG-1295 | AG1295
Compound class: Synthetic organic
Comment: AG 1295 is a cell-permeable, reversible, ATP-competitive, and selective inhibitor of platelet-derived growth factor receptor (PDGFR) tyrosine kinase [3].
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 2
Hydrogen bond donors 0
Rotatable bonds 1
Topological polar surface area 25.78
Molecular weight 234.12
XLogP 3.87
No. Lipinski's rules broken 0
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Canonical SMILES Cc1cc2ncc(nc2cc1C)c1ccccc1
Isomeric SMILES Cc1cc2ncc(nc2cc1C)c1ccccc1
InChI InChI=1S/C16H14N2/c1-11-8-14-15(9-12(11)2)18-16(10-17-14)13-6-4-3-5-7-13/h3-10H,1-2H3

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
fms related receptor tyrosine kinase 3 Flt3/FLT3 Hs Inhibitor Inhibition 53.6 47.0 25.0
KIT proto-oncogene, receptor tyrosine kinase cKit/c-Kit Hs Inhibitor Inhibition 63.5 86.0 70.0
NIMA related kinase 2 NEK2/NEK2 Hs Inhibitor Inhibition 75.7 92.0 105.0
fibroblast growth factor receptor 4 FGFR4/FGFR4 Hs Inhibitor Inhibition 77.2 134.0 93.0
glycogen synthase kinase 3 beta GSK3β/GSK3b Hs Inhibitor Inhibition 79.5 88.0 106.0
serine/threonine kinase 17a DRAK1/DRAK1(STK17A) Hs Inhibitor Inhibition 80.0 70.0 95.0
MAPK interacting serine/threonine kinase 1 nd/MNK1 Hs Inhibitor Inhibition 80.3
Pim-2 proto-oncogene, serine/threonine kinase Pim-2/PIM2 Hs Inhibitor Inhibition 81.0 126.0 115.0
CDC42 binding protein kinase alpha MRCKα/MRCKa(CDC42BPA) Hs Inhibitor Inhibition 81.2 114.0 81.0
MER proto-oncogene, tyrosine kinase Mer/c-MER Hs Inhibitor Inhibition 81.4 107.0 90.0
Displaying the top 10 targets  View all targets in screen »