1644663-97-7Relevant articles and documents
Discovery of 1 H -pyrazol-3(2 H)-ones as potent and selective inhibitors of protein kinase R-like endoplasmic reticulum kinase (PERK)
Smith, Adrian L.,Andrews, Kristin L.,Beckmann, Holger,Bellon, Steven F.,Beltran, Pedro J.,Booker, Shon,Chen, Hao,Chung, Young-Ah,D'Angelo, Noel D.,Dao, Jennifer,Dellamaggiore, Kenneth R.,Jaeckel, Peter,Kendall, Richard,Labitzke, Katja,Long, Alexander M.,Materna-Reichelt, Silvia,Mitchell, Petia,Norman, Mark H.,Powers, David,Rose, Mark,Shaffer, Paul L.,Wu, Michelle M.,Lipford, J. Russell
, p. 1426 - 1441 (2015)
The structure-based design and optimization of a novel series of selective PERK inhibitors are described resulting in the identification of 44 as a potent, highly selective, and orally active tool compound suitable for PERK pathway biology exploration both in vitro and in vivo.