Skip to main content

View full-text article in PMC

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

Table 2.

graphic file with name ml-2010-002426_0005.jpg

			1b Replicon IC₅₀ (nM)^b
compd	R	1b K_i (nM)^a	10% FBS	50% NHS	rat PO plasma AUC (μM·h)^c	rat [liver] @ 4 h (μM)^d
14a	H	0.18	8.7	46	0.27	13.4
18a	5-Br	0.04	2	170	0.28	5.8
18b	5-I	0.03	2.3	56	1.4	24.5
18c	5-OMe	0.04	2.7	35	17.7	33.2
18d	5-OEt	0.37	6	500	6.9	15.2
18e	5-Et	0.14	2.5	90	2.1	12.5
18f	5-SMe	0.03	2	34	1.8	12.6
18g	5-CF₃	0.25	21	410
18h	5-SO₂Me	0.11	280	>1000
18i	5-OCF₃	0.75	50	4400	1.6	8.8
15a	6-OMe	0.04	3	113	9.6	3.0

^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.