Table 1.

Binding affinities of our newly designed BET inhibitors and reference compounds (+)-JQ-1 and OTX-015 to BRD4 BD1 protein, as determined in our FP-based binding assay.

Compound	R	BRD4 BD1
		IC50(nM)	Ki(nM)
1 (JQ-1)		22 ± 3	5.3 ± 1.0
2		4400 ± 700	1500 ± 200
3	CH3	100 ± 10	33 ± 4
4	-H	2300 ± 600	820 ± 210
5	-isopropyl	9400 ± 600	3300 ± 200
6		8100 ± 700	2800 ± 300
7	-cyclopropyl	550 ± 110	190 ± 40
8		210 ± 10	70 ± 1
9		720 ± 60	250 ± 20
10		45 ± 4	13 ± 1
11		270 ± 10	92 ± 2
12		44 ± 3	13 ± 1
13		200 ± 90	68 ± 10
14		18 ± 2	3.7 ± 0.7
15		34 ± 3	9.5 ± 1.1
16		63 ± 10	20 ± 3
17		200 ± 24	66 ± 9
18		200 ± 9	68 ± 3
19		86 ± 11	28 ± 4
20		34 ± 2	9.6 ± 0.9
21		50 ± 9	15 ± 3
22 (QCA276)		10 ± 3	2.3 ± 1.0
23		14 ± 5	4.2 ± 0.8
24		11 ± 1	2.1 ± 0.3
25		13 ± 4	2.7 ± 1.2
OTX-015		23 ± 1	5.7 ± 0.5