Table 1. PERK Inhibition and Pharmacokinetic Data for Compound 1 and Heteroaryl Acetamide Analogues.

^aCalculated using BioByte cLogP (the calculated logarithm of the 1-octanol–water partition coefficient of the nonionized molecule; see www.biobyte.com).

^bInhibitory activity as measured by cytoplasmic PERK domain phosphorylation of EIF2α. Average values are reported with standard deviation.

^cIC₅₀ estimated from a Western blot 6-point dose response, except for compounds 1 and 9a (3-point dose response).

^dAverage in vivo blood clearance determined after i.v. infusion in SD rats (n = 2).

^eData reported as the average of a single experiment.

^fNot determined.