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. Author manuscript; available in PMC: 2017 Apr 28.
Published in final edited form as: J Med Chem. 2015 Nov 9;59(8):3609–3634. doi: 10.1021/acs.jmedchem.5b01457

Table 16. Further rigidification to azepinones (Merck Research Laboratories).

graphic file with name nihms-735690-t0178.jpg
Compd R X IC50a (nM)
135 Cl H 96
136 Cl Me 79
137 CN graphic file with name nihms-735690-t0179.jpg 4.9
138 CN graphic file with name nihms-735690-t0180.jpg 8.4
139 CN graphic file with name nihms-735690-t0181.jpg 6.8
140 Cl graphic file with name nihms-735690-t0182.jpg 5.7
141 CN graphic file with name nihms-735690-t0183.jpg 1.9
a

Measured in a IMAP assay.