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. 2020 Apr 3;11(5):740–746. doi: 10.1021/acsmedchemlett.9b00594

Table 3. SAR at P2 Pocket13.

graphic file with name ml9b00594_0009.jpg

cmpd R R′ n abIC50 (nM)
19 CO2H OH 1 862 ± 158
20 CONH2 OH 1 1558 ± 300
21 CONH2 OH 3 5539 ± 174
22 CO2H O(CH2)2OH 1 3102 ± 424
23 CONH2 O(CH2)2OH 1 2545 ± 357
a

IC50 for TR-FRET KEAP1 binding assay.

b

IC50 values are the average of at least three individual measurements ± standard deviation.