Discovery of hydroxyaniline amides as selective Extracellular Regulated Kinase (Erk) inhibitors

作者：Zhu Hugh Y^*; Desai Jagdish; Deng Yongqi; Cooper Alan; Wang James; Shipps Jerry; Samatar Ahmed; Carr Donna; Windsor William

来源：Bioorganic & Medicinal Chemistry Letters, 2015, 25(7): 1627-1629.

DOI：10.1016/j.bmcl.2015.01.049

• Erk
• Extracellular regulated kinase
• ALIS
• MAPK
• NeoMorph

Starting from weak mu M hits identified through affinity based Automated Ligand Identification System (ALIS) screenings, double digit nM hydroxyaniline amide Erk inhibitors were discovered. This class of compounds had the unique dual mechanism of inhibiting activated and non-activated forms of Erk. They generally had high degree of selectivity in kinase panel tested.

• 出版日期2015-4-1