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. 2014 Sep 24;6(1):68–72. doi: 10.1021/ml500315b

Table 1. Naphthyl Modification Improves Selectivitya.

graphic file with name ml-2014-00315b_0006.jpg

Cpd R IRE1α Enz IC50 (μM) XBP1-Luc IC50 (μM) Aurora p-histone H3 IC50 (μM) JNK3 Enz IC50 (μM)b (fold)c
1 H 0.071 0.27 16 0.35 (4.9)
2 Me 0.014 0.20 >50b 0.71 (51)
a

Unless noted otherwise, data represent an average of ≥2 separate determinations.

b

Data represent a single determination.

c

Fold selectivity versus IRE1α enzyme.