TABLE 1.

Structure−activity relationships (SARs) of BSTs 1–5.

Compounds	Linker	BRD4 (IC50, nM)	STAT3 (IC50, nM)
BST-1		15.73 ± 1.31	20.82 ± 1.94
BST-2		4.64 ± 0.17	27.16 ± 2.82
BST-3		7.09 ± 0.53	11.33 ± 0.95
BST-4		2.45 ± 0.11	8.07 ± 0.51
BST-5		10.12 ± 1.15	17.83 ± 1.24
RVX-208	—	39.86 ± 3.72	no inhibition
CJ-1383	—	no inhibition	936 ± 14.87