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. 2019 Aug 2;10(9):1296–1301. doi: 10.1021/acsmedchemlett.9b00227

Table 3. Effect of Nitrogen Atom(s) on BRD4-D1 Affinity.

graphic file with name ml9b00227_0007.jpg

compound N atom location BRD4-D1 IC50 (μM)a
22 1,2 9.7 ± 1.8
23 none 12 ± 1.1
5 1 3.6 ± 0.05
24 2 97 ± 2.6
25 3 >100
26 4 >100
a

IC50 values were determined by fluorescence anisotropy. Data represents the mean and standard deviation of three independent trials.