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. 2012 Mar 2;3(4):332–336. doi: 10.1021/ml300017p

Table 1. In Vitro Activity.

graphic file with name ml-2012-00017p_0004.jpg

  Ki (nM)a
   
compd 1b 3a 1b replicon IC50 50% NHS (nM)b rat [liver] at 4 h (μM)c
3 0.02 200 10 21
4 0.05 45 19 7.8
5 0.05 12 19 96
6 0.06 130 21 25
7 1.1 1200 ND ND
8 1.9 520 ND ND
9 0.08 26 44 0.6
a

NS3/4a protease time-resolved fluorescence assay, mean of n ≥ 3 measurements.

b

Cell-based replicon assay, mean of n ≥ 3.

c

Liver levels from PK experiments described in the Supporting Information.