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Binding to BRD4-BD1 correlates with cellular antiproliferative potency: (A) BRD4-BD1 and BRD4-BD2 binding measured by TR-FRET for 1 compared to 27 (data normalized to DMSO as 100%); (B) BROMOscan of compound 27 against 40 bromodomain proteins; (C) correlation between BRD4-BD1 binding (TR-FRET) assay and potency for growth inhibition of MCF-7:CFR cells.
