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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 3.

IC50 Values of Inhibitors 14–18 against BRD4 D1 by Fluorescence Anisotropy

graphic file with name nihms-1848605-t0010.jpg
compd R R2 BRD4 D1 IC50 by FA (μM)a
(+)-JQ1 <0.092b
14 Me Me 0.27 ± 0.04
15 i-Pr Me <0.092b
16 H OH 3.0 ± 0.1
17 H OMe 2.4 ± 0.1
18 2.7 ± 0.3
a

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

b

IC50 is less than half the concentration of bound BRD4 D1 used.