. 2025 Apr 17;68(9):9638–9660. doi: 10.1021/acs.jmedchem.5c00395

Table 1. Structure–Activity Relationships for BRD4 BD1 and CBP Binding as Determined by FRET for the Phenolic Exit Vector Analogues^a.

compound	R	BRD4 IC₅₀ (μM)	CBP IC₅₀ (μM)
6	H	3.0 ± 0.1	0.3 ± 0.1
7	Ac	1.3 ± 0.1	0.17 ± 0.04
8	(CH₂)₃CO₂Me	1.55 ± 0.01	0.5 ± 0.1
10	(CH₂)₃C(O)NH(CH₂)₂OMe	1.62 ± 0.01	0.33 ± 0.05
2	Me	2.4^b	0.12^b
1	(CH₂)₃NMe₂	1.5^b	0.65^b

Values given as mean ± SD (n = 3).

Values from literature.⁴³

Table 1. Structure–Activity Relationships for BRD4 BD1 and CBP Binding as Determined by FRET for the Phenolic Exit Vector Analoguesa.