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. Author manuscript; available in PMC: 2022 Nov 23.
Published in final edited form as: J Med Chem. 2022 Jan 10;65(3):2342–2360. doi: 10.1021/acs.jmedchem.1c01779

Table 1.

IC50 Values of 1 and Analogues 2–6 against BRD4 D1 by Fluorescence Anisotropy and AlphaScreen

graphic file with name nihms-1848605-t0008.jpg
compd R BRD4 D1 IC50 by FA (μM)a BRD4 D1 IC50 by AlphaScreen (μM)b
(+)-JQ1 <0.092c 0.051
1 25 F 11 ± 0.8 3.8
2 18 CF3 0.31 ± 0.06 0.64
3 Cl 0.61 ± 0.09 1.3
4 Br 0.20 ± 0.02 0.44
5 I <0.092c 0.20
6 OCH3 9.4 ± 0.4 3.9
a

Data represents the mean and standard deviation of three experimental replicates.

b

Data represents the mean of two experimental replicates.

c

IC50 is less than half the concentration of bound protein used.