Table 9SAR analysis of selected fully synthetic analogues for NS3 helicase inhibitor discovery

Compound IDcomplete structuretarget potency, MBHA (IC50, avg, μM)cell-based assaysantitarget potency (IC50, avg, μM)
#CID*1b(con1)replicon (% inhibition @ 10 μM)cell viability (% @ 10 μM)FID (SG)
%Displaced @ 100 μM
SSB
%Displaced @ 100 μM
SID2a(JFH1)EC50 (μM)SSB
EC50 (μM)
6449795072S
Image ml283fu60.jpg
>10080 ± 1739 ± 10ndnd
103162420>100ndnd
6549795073S
Image ml283fu61.jpg
60 ± 6.190 ± 3528 ± 5ndnd
10316242175 ± 32.6ndnd
*

Denotes whether the compound was synthesized (S) or purchased (P).

Denotes whether the compound was synthesized (S) or purchased (P).

From: Hepatitis C Virus NS3 Helicase Inhibitor Discovery

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