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. 2011 Jan 12;2(3):207–212. doi: 10.1021/ml1002426

Table 3.

graphic file with name ml-2010-002426_0006.jpg

    Replicon IC50 (nM)b
   
compd 1b Ki (nM)a 1b 10% FBS 1b 50% NHS 2a 10% FBS rat PO plasma AUC (μM·h)c rat [liver] @ 4 h (μM)d
19 0.05 3.0 60.0 6.0 2.5 13.2
15c 0.03 2.0 80.0 - 18.1 8.0
15j (MK-1220) 0.02 4.0 11.0 5.0 11.8 23.0
14k 0.02 2.0 10.0 11.0 0.18 16.0
a

NS3/4A protease time-resolved fluorescence assay.

b

Cell-based replicon assay.

c

5 mg/kg dosed orally in PEG400 (n = 2); AUC calculated based on 4 h experiment.

d

5 mg/kg dosed orally in PEG400 (n = 2); liver levels after 4 h.