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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 4. SAR for BRD9 and BRD4 BD1 activity of thienopyridone amidinesa.

graphic file with name EMS86579-i012.jpg
Cmpd R = BRD9 pIC50 BRD4 BD1 pIC50 Fold Selectivity
39 graphic file with name EMS86579-i013.jpg 8.1 ± 0.19 6.4 ± 0.02 ×50
40 graphic file with name EMS86579-i014.jpg 7.4 ± 0.13 5.8 ± 0.02 ×40
41 graphic file with name EMS86579-i015.jpg 7.9 ± 0.12 6.1 ± 0.06 ×60
42 graphic file with name EMS86579-i016.jpg 8.0 ± 0.23 6.3 ± 0.06 ×50
43 graphic file with name EMS86579-i017.jpg 7.4 ± 0.12 5.6 ± 0.04 ×60
44 graphic file with name EMS86579-i018.jpg 7.8 ± 0.21 5.6 ± 0.03 ×160
a

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