Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10595143 | Bioorganic & Medicinal Chemistry Letters | 2013 | 6 Pages |
Abstract
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.
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Bei Li, Oana M. Cociorva, Tyzoon Nomanbhoy, Helge Weissig, Qiang Li, Kai Nakamura, Marek Liyanage, Melissa C. Zhang, Ann Y. Shih, Arwin Aban, Yi Hu, Julia Cajica, Lan Pham, John W. Kozarich, Kevin R. Shreder,