. 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 5.

Activity in the Replicon Assay for a Selected Set of Compounds in the Bicyclic Series

compd	GT-1a EC₅₀ (nM)^a	GT-1b EC₅₀ (nM)^a	Ratio 1a/1b	GT-1a 40% HuS^b EC₅₀ (nM)^a	GT-1b 40% HuS EC₅₀ (nM)^a	Plasma Shift fold	GT-1a 40% HuS EC₉₀ (nM)^a	GT-1b 40% HuS EC₉₀ (nM)^a
7	8.0	3.0	2.7	66	22	7.3–8.2	531	128
35	7.2	3.2	2.2	16	5.6	1.7–2.2	123	29
39	5.2	3.1	1.7	4.0	11	0.8–3.5	25	47
41	1.1	1.0	1.1	10	3.8	3.8–9.4	63	19
42	4.6	3.2	1.4	10	3.5	1.7–2.1	48	20
50	17	12	1.4	10	7.5	0.6	61	44

EC₅₀ and EC₉₀ measured using stable HCV (GT-1a H77, GT-1b Con1) subgenomic replicon assay (n ≥ 2).

Human serum (HS).