Table 1:

BPTF bromodomain inhibitors with in vitro affinity values and reported off-target effects. Functional groups acting as acetyl lysine mimics are shown in blue based on reported cocrystal structures.

Inhibitor	BPTF in vitro affinity	Reported off-targets	References, PDB ID
	Kd = 1.8 μM (ITC)	pan-bromodomain inhibitor	[71] 5IGK (with BRD4)
	rac-AU1 Kd = 2.8 μM (ITC)	Kinases: TRKC Kd = 200 nM CDKL2 Kd = 260 nM (KINOMEscan)	[26,37**,62*]
	Kd = 120 nM (ITC)	CECR2 Kd = 10 nM (ITC)	[36,39*] 7KDZ
	Kd = 3–71 nM (BROMOscan)	BRPF Kd = 37 nM CECR2 Kd = 66 nM GCN5L2 Kd = 62 nM PCAF Kd = 74 nM (BROMOscan)	[72]
	IC50 = 36 μM (AlphaScreen)	Not determined	[68*] 7KDW
	Kd = 1.7 μM (SPR)	PCAF/GCN5 Ki = 1.4 nM (BROMOscan)	[68*,76] 7K6R
	Kd = 6 μM (SPR)	Not determined	[68*]
	Kd = 17.9 μM (SPR)	Not reported	[73]
	Kd = 35.5 μM (Bio-layer Interferometry)	Not determined	[74]