The binding affinities and IC50 values of the tested BET family member inhibitors for the BRD4 and BRD2 proteins bromodomains (BDs) were detected using a commercially available TR-FRET assay kits (Cayman Chemical, Ann Arbor, MI, USA) according to the manufacturer’s instructions and our recent publications (Borysko et al., 2018; Liu et al., 2018; Liu et al., 2020). The specificity of the designed and synthesized compounds for BRD4 was also evaluated through comparison with those for BRD2.
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