Discovery of 1<i>H</i>‑Pyrazol-3(2<i>H</i>)‑ones as Potent and Selective Inhibitors of Protein Kinase R‑like Endoplasmic Reticulum Kinase (PERK)

The structure-based design and optimization of a novel series of selective PERK inhibitors are described resulting in the identification of <b>44</b> as a potent, highly selective, and orally active tool compound suitable for PERK pathway biology exploration both in vitro and in vivo