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. Author manuscript; available in PMC: 2020 Jul 11.
Published in final edited form as: J Med Chem. 2015 Apr 30;59(4):1425–1439. doi: 10.1021/acs.jmedchem.5b00256

Table 5. SAR for BRD9 and BRD4 BD1 activity of 3-trifluoromethylphenyl substituted thienopyridone amidinesa.

graphic file with name EMS86579-i019.jpg
Cmpd BRD9 pIC50 BRD4 BD1 pIC50 Fold Selectivity
44 7.8 ± 0.21 5.6 ± 0.03 ×160
45 7.3 ± 0.18 5.3 ± 0.07 ×100
46 5.5 ± 0.26 <4.3 ≥×15
a

All results are n ≥ 3 as determined by TR-FRET analysis.