Potent and selective PERK inhibitor (IC50
= 6 nM). Exhibits >160-fold selectivity for PERK over B-Raf and GCN2, as well as a panel of 387 other kinases. Orally bioavailable.
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By permission of the authors
Discovery of 1H-pyrazol-3(2H)-ones as potent and selective inhibitors of protein kinase R-like endoplasmic reticulum kinase (PERK).
Smith et al.