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. Author manuscript; available in PMC: 2019 May 10.
Published in final edited form as: Eur J Med Chem. 2018 Apr 3;151:450–461. doi: 10.1016/j.ejmech.2018.04.006

Table 3.

Binding affinities of compounds 28 and 35 with BRD4 and the selectivity over its BET family members BRD2, BRD3, BRDT as well as non-BET protein CBP.a

BDs\Compds (+)-JQ1 RVX-208 28 35
BRD4 BD1 (IC50, nM) 92 1,142 27 49
BRD4 BD2 (IC50, nM) 62 135 32 32
BRD2 BD1 (IC50, nM) 78 5,780 803 772
BRD2 BD2 (IC50, nM) 52 251 1,736 1,836
BRD3 BD1 (IC50, nM) 81 3,962 2,275 2,493
BRD3 BD2 (IC50, nM) 69 203 2,193 2,241
BRDT BD1 (IC50, nM) 183 4,836 3,183 3,292
BRDT BD2 (IC50, nM) 217 708 2,781 3,082
CBP (IC50, nM) 9,600 > 10,000 > 10,000 > 10,000
a

Binding affinity was measured using an TR-FRET assay with the isolated bromodomain. Reported as mean of at least two separate assay runs.