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. 2016 Mar 15;7(5):531–536. doi: 10.1021/acsmedchemlett.6b00075

Table 2. Structure–Activity Relationship of 6-Substituted Benzodiazepinones.

graphic file with name ml-2016-00075v_0007.jpg

a

Time-resolved fluorescence resonance energy transfer (TR-FRET) assay with the isolated CBP bromodomain. N = 2.

b

LLE = pIC50 – clogP.

c

Bioluminesence resonance energy transfer cellular target engagement assay. N = 3.

d

TR-FRET assay with the isolated BRD4 BD-1 bromodomain. N = 3.