Table 2. Structure–Activity Relationship of 6-Substituted Benzodiazepinones.
Time-resolved fluorescence resonance energy transfer (TR-FRET) assay with the isolated CBP bromodomain. N = 2.
LLE = pIC50 – clogP.
Bioluminesence resonance energy transfer cellular target engagement assay. N = 3.
TR-FRET assay with the isolated BRD4 BD-1 bromodomain. N = 3.