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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 6.

IC50 Values of Inhibitors 23–32 against BRD4 D1, BRD2 D1, and BRDT D1 by Fluorescence Anisotropy

graphic file with name nihms-1848605-t0013.jpg
compd R3 stereocenter BRD4 D1 IC50 by FA (μM)a % Inhibition against BRD2 D1 at 50 μMa % Inhibition against BRDT D1 at 50 μMa
(+)-JQ1 <0.092b 0.14 ± 0.001c 0.12 ± 0.04c
23 H 0.36 ± 0.03 79% 68%
24 (CH2)2N(CH3)2 <0.092b 88% 88%
25 H 0.30 ± 0.01 84% 73%
26 (CH2)2N(CH3)2 <0.092b 89% 85%
27 H S 1.1 ± 0.3 49% 49%
28 (CH2)2N(CH3)2 S 0.11 ± 0.02 73% 70%
29 H S 0.88 ± 0.2 57% 54%
30 (CH2)2N(CH3)2 S <0.092b 87% 88%
31 H R 3.8 ± 0.5 41% 46%
32 (CH2)2N(CH3)2 R 0.44 ± 0.08 59% 72%
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.

c

IC50 values by fluorescent anisotropy.