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. Author manuscript; available in PMC: 2015 Mar 13.
Published in final edited form as: J Med Chem. 2013 Nov 6;57(5):1914–1931. doi: 10.1021/jm401329s

Table 4.

Replacements of tert-Butyl Group with Replicon (GT-1a and GT-1b) and in vitro Hepatocytes Data.

graphic file with name nihms538805u3.jpg
compd R GT-1a
EC50 (nM)a 		GT-1b
EC50 (nM)a 		HHb RHb
35 graphic file with name nihms538805t25.jpg 7.2 3.2 7.9 20
51 graphic file with name nihms538805t26.jpg 821 57 1.5 1.8
52 graphic file with name nihms538805t27.jpg 839 119 0.8 3.7
53 graphic file with name nihms538805t28.jpg 95 16 0.1 1.7
a

EC50 measured using stable HCV (GT-1a H77 and GT-1b Con1) subgenomic replicon assay (n ≥ 2).

b

Human hepatocytes (HH) and rat hepatocytes (RH) intrinsic clearance is reported in μL/min/106 cells. Human hepatocyte category ranking: high stability < 2.8, low stability > 15; rat hepatocyte category ranking: high stability < 5.4, low stability > 29.