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

Table 2. Significance of R Group to BRD4-D1 Binding Affinity.

graphic file with name ml9b00227_0006.jpg

compound	R	X	BRD4-D1 IC₅₀ (μM)^a
6	4–F-C₆H₄	H	>100^b^,^c
16	c-hexyl	H	>100^b
17	c-pentyl	H	>100^b
18	t-Bu	H	>100^b
19	i-Pr	C(NH)NH₂	>100^b
20	n-Pr	C(NH)NH₂	>100^b
21	c-Pr	C(NH)NH₂	61 ± 8.1
22	Me	C(NH)NH₂	9.7 ± 1.8

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

The IC₅₀ value was determined to be >100 μM by fluorescence anisotropy.

The IC₅₀ value was determined to be 27 μM by AlphaScreen by Reaction Biology.