Table 1. Naphthyl Modification Improves Selectivitya.

| 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) |
Unless noted otherwise, data represent an average of ≥2 separate determinations.
Data represent a single determination.
Fold selectivity versus IRE1α enzyme.