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. Author manuscript; available in PMC: 2022 Jul 22.
Published in final edited form as: J Med Chem. 2021 Jul 8;64(14):10497–10511. doi: 10.1021/acs.jmedchem.1c00933

Table 3.

Affinity and Selectivity for Analogues with Alkyl Ethers and Substituted Benzene Ringsa

graphic file with name nihms-1741875-t0010.jpg
compound BRD4 D1 IC50 (μM) BRD4 D2 IC50 (μM) D2/D1 selectivity
  (+)-JQ1 0.0770 ± 0.006 0.0720 ± 0.02   –
  20  8.96 ± 0.8  22.5 ± 2   2.5
  21   >100   >100   –
  22  22.2 ± 4  20.2 ± 3   0.90
  23   0.790 ± 0.03  3.14 ± 0.06   4.0
  24  5.97 ± 2  12.2 ± 3   2.0
a

IC50 values were determined by FA. Data represents the mean and standard deviation of three experimental replicates.