GSK481

GSK481 was tested at 10 μM in duplicate against 318 kinases in the Reaction Biology Corporation (RBC) kinase panel. Reactions were carried out at 10 μM ATP. A full list of the 318 kinases is available at http://www.reactionbiology.com. No inhibition >30% at 10 μM concentration was identified. GSK481 was tested at 10 μM in duplicate against 456 kinases (including 395 non-mutant kinases) in the DiscoveRx KINOMEscan® kinase profile panel. A full list of the 456 kinases is available at http://www.discoverx.com. ATP is not used in the KINOMEscan® competition binding assay platform. The only binding interaction identified was that of RIP1 kinase (100%); all other kinase binding interactions were <50%. Potency against RIP1 species in a fluorescence polarization (FP) assay is RIP1 human IC50 1.6 nM, RIP1 monkey IC50 2.5 nM, RIP1 rabbit IC50 2000 nM, RIP1 rat IC50 6300 nM, RIP1 mouse IC50 3200 nM, RIP1 dog IC50 7900 nM, RIP1 minipig IC50 >10,000 NM.