1452864-25-3Relevant articles and documents
Hit-to-lead optimization and kinase selectivity of imidazo[1,2-a] quinoxalin-4-amine derived JNK1 inhibitors
Li, Bei,Cociorva, Oana M.,Nomanbhoy, Tyzoon,Weissig, Helge,Li, Qiang,Nakamura, Kai,Liyanage, Marek,Zhang, Melissa C.,Shih, Ann Y.,Aban, Arwin,Hu, Yi,Cajica, Julia,Pham, Lan,Kozarich, John W.,Shreder, Kevin R.
, p. 5217 - 5222 (2013/09/12)
As the result of a rhJNK1 HTS, the imidazo[1,2-a]quinoxaline 1 was identified as a 1.6 μM rhJNK1 inhibitor. Optimization of this compound lead to AX13587 (rhJNK1 IC50 = 160 nM) which was co-crystallized with JNK1 to identify key molecular interactions. Kinase profiling against 125+ kinases revealed AX13587 was an inhibitor of JNK, MAST3, and MAST4 whereas its methylene homolog AX14373 (native JNK1 IC50 = 47 nM) was a highly specific JNK inhibitor.