. Author manuscript; available in PMC: 2017 Jun 19.

Published in final edited form as: J Med Chem. 2015 Jun 16;58(12):4927–4939. doi: 10.1021/acs.jmedchem.5b00613

Table 4.

Binding affinities of reference compounds 1–3 and new compounds 18 to BET proteins and representative bromodomain proteins in other 7 sub-families using Bio-layer Interferometry method.

	K_D (nM)
	1	2	3	18
BRD2(BD1)	14.7±1.9	159±11	54.8±7.8	48.1±4.0
BRD2(BD2)	6.2±1.8	45.4±1.0	70.3±7.3	29.6±6.9
BRD3 (BD1)	13.6±1.0	60.7±10.3	29.8±7.3	17.7±3.6
BRD3 (BD2)	11.7±1.5	40.7±8.5	40.5±7.2	16.3±4.1
BRD4 (BD1)	12.8±2.9	99.4±5.8	52.8±9.2	47.0±14.8
BRD4 (BD2)	6.7±0.7	47.6±2.7	215±29	44.6±22.1
CREBBP		> 10000	3084	670
ATAD2A		> 10000	> 10000	> 10000
ATAD2B				> 10000
TRIM24				~ 10000
BAZ2B				> 10000
MLL1				9500
TAF1B2				> 10000
BRG1				> 10000
PB1BR5				> 10000