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. Author manuscript; available in PMC: 2017 Aug 25.
Published in final edited form as: J Med Chem. 2016 Aug 11;59(16):7617–7633. doi: 10.1021/acs.jmedchem.6b00855

Table 5.

In Vitro Potencies of Newly Synthesized Inhibitors with Modifications to the Pyridine-2-yl-piperizine Tail Region

graphic file with name nihms810803u6.jpg
Cmpd Structure IC50 (nM)
EZH2 EZH1
5 graphic file with name nihms810803t45.jpg <10 69 ± 14
64 graphic file with name nihms810803t46.jpg <10 88 ± 22
65 graphic file with name nihms810803t47.jpg <10 60 ± 9
66 graphic file with name nihms810803t48.jpg 41 ± 10 >1250
67 graphic file with name nihms810803t49.jpg 48 ± 17 >2500
68 graphic file with name nihms810803t50.jpg 66 ± 4 >1250
69 graphic file with name nihms810803t51.jpg 24 ± 4 681 ± 90
70 graphic file with name nihms810803t52.jpg 22 ± 5 773 ± 152
71 graphic file with name nihms810803t53.jpg 64 ± 20 >5000
72 graphic file with name nihms810803t54.jpg 11 ± 1 613 ± 29
73 graphic file with name nihms810803t55.jpg 17 ± 3 880 ± 173
74 graphic file with name nihms810803t56.jpg 42 ± 7 >2500
75 graphic file with name nihms810803t57.jpg 26 ± 4 >1250
76 graphic file with name nihms810803t58.jpg 35 ± 8 >5000