Table 1. Impact of Various Modifications on 1 CBP Potency.
Time-resolved fluorescence resonance energy transfer (TR-FRET) assay with the isolated CBP bromodomain. N = 2 or 3.
LLE for key compounds = pIC50 – clogP.
TR-FRET assay with the isolated BRD4 BD-1 bromodomain. N = 2 or 3.