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. Author manuscript; available in PMC: 2020 Dec 20.
Published in final edited form as: ACS Chem Biol. 2019 Oct 14;14(12):2595–2605. doi: 10.1021/acschembio.9b00482

Table 2.

KIRAs Containing 4-aminophenol R2 Groupsa

graphic file with name nihms-1055716-t0028.jpg
compd R1 R2 R3 IRE1β RNase IC50 (nM) IRE1α RNase IC50 (nM) IRE1β RNase Selectivity (Fold)
8 graphic file with name nihms-1055716-t0029.jpg graphic file with name nihms-1055716-t0030.jpg graphic file with name nihms-1055716-t0031.jpg 4.4 ± 0.7 22 ± 9 5.0
9 graphic file with name nihms-1055716-t0032.jpg graphic file with name nihms-1055716-t0033.jpg graphic file with name nihms-1055716-t0034.jpg 120 ± 40 120 ± 10 1.0
10 graphic file with name nihms-1055716-t0035.jpg graphic file with name nihms-1055716-t0036.jpg graphic file with name nihms-1055716-t0037.jpg 50 ± 2 6.0 ± 1.7 0.12
11 graphic file with name nihms-1055716-t0038.jpg graphic file with name nihms-1055716-t0039.jpg graphic file with name nihms-1055716-t0040.jpg 99 ± 56 57 ± 11 0.57
12 graphic file with name nihms-1055716-t0041.jpg graphic file with name nihms-1055716-t0042.jpg graphic file with name nihms-1055716-t0043.jpg 150 ± 30 130 ± 70 0.87
13 graphic file with name nihms-1055716-t0044.jpg graphic file with name nihms-1055716-t0045.jpg graphic file with name nihms-1055716-t0046.jpg 3.9 ± 1.1 240 ± 50 60
14 graphic file with name nihms-1055716-t0047.jpg graphic file with name nihms-1055716-t0048.jpg graphic file with name nihms-1055716-t0049.jpg 13 ± 2 110 ± 10 8.1
15 graphic file with name nihms-1055716-t0050.jpg graphic file with name nihms-1055716-t0051.jpg graphic file with name nihms-1055716-t0052.jpg 3.5 ± 1.4 390 ± 270 110
16 graphic file with name nihms-1055716-t0053.jpg graphic file with name nihms-1055716-t0054.jpg graphic file with name nihms-1055716-t0055.jpg 430 ± 70 2000 ± 100 4.5
17 graphic file with name nihms-1055716-t0056.jpg graphic file with name nihms-1055716-t0057.jpg graphic file with name nihms-1055716-t0058.jpg 74 ± 14 270 ± 70 3.6
18 graphic file with name nihms-1055716-t0059.jpg graphic file with name nihms-1055716-t0060.jpg graphic file with name nihms-1055716-t0061.jpg 17 ± 2 83 ± 8 5.8
a

RNase IC50 data are shown as mean ± SEM, n=3. RNase selectivity was determined by dividing the IRE1α RNase IC50 by the IRE1β RNase IC50 value for each inhibitor (individual IC50 curves provided in Supp. Figure 2).