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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 2.

IC50 Values of Inhibitors 7–13 against BRD4 D1 by Fluorescence Anisotropy

graphic file with name nihms-1848605-t0009.jpg
compd R R1 BRD4 D1 IC50 by FA (μM)a
(+)-JQ1 <0.092b
7 Me Me 0.19 ± 0.02
8 H H 2.4 ± 0.1
9 H Me 0.50 ± 0.04
10 H Et 0.20 ± 0.01
11 H t-Bu 0.11 ± 0.03
12 Me Et <0.092b
13 Cl Cl 0.43 ± 0.05
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.