Target Validation Information
TTD ID T40492
Target Name Hepatitis C virus NS3 helicase (HCV NS3)
Type of Target
Successful
Drug Potency against Target 2,4,6-Trihydroxy-3-nitro-N-tridecyl-benzamide Drug Info IC50 = 5800 nM [2]
Ac-Glu-Cha-Cys Drug Info Ki = 4100 nM [1]
AcAsp-D-Gla-Leu-Ile-Cha-Cys Drug Info Ki = 0.75 nM [2]
AcAsp-Gla-Leu-Ile-Cha-Cys Drug Info Ki = 0.75 nM [1]
AcAsp-Glu-Cha-Val-Prb-Cpg Drug Info IC50 = 51 nM [2]
AcAsp-Glu-Cha-Val-Prb-Cys Drug Info IC50 = 33 nM [2]
AcAsp-Glu-Dif-Glu-Cha-Cys Drug Info Ki = 40 nM [2]
AcAsp-Glu-Dif-Glu-Cha-Fab Drug Info Ki = 10 nM [2]
AcAsp-Glu-Dif-Ile-Cha-Cys Drug Info Ki = 30 nM [1]
AcAsp-Glu-Dif-Ile-Cha-Cys-Iqc-Nle-Thr-TyrNH2 Drug Info IC50 = 100 nM [2]
AcAsp-Glu-Dif-Ile-Cha-Cys-Pro-Cha-Asp-ValNH2 Drug Info IC50 = 1300 nM [2]
AcAsp-Glu-Dif-Ile-Cha-Cys-Pro-Nle-Asp-ValNH2 Drug Info IC50 = 1800 nM [2]
AcAsp-Glu-Dif-Lys-Cha-Cys Drug Info Ki = 1240 nM [1]
AcAsp-Glu-Met-Glu-Cha-Cys Drug Info Ki = 400 nM [1]
AcAsp-Glu-Met-Glu-Glu-Cys Drug Info Ki = 600 nM [2]
AcAsp-Glu-Met-Glu-Nal-Cyse Drug Info Ki = 180 nM [1]
AcDif-Glu-Cha-Cys Drug Info Ki = 15000 nM [1]
AcDif-Ile-Cha-Cys Drug Info Ki = 2100 nM [1]
AcGlu-Asp-Val-Val-Leu-Cys-Iqc-Nle-Thr-TyrNH2 Drug Info IC50 = 1000 nM [2]
AcGlu-Dif-Glu-Cha-Cys Drug Info Ki = 700 nM [1]
AcGlu-Dif-Ile-Cha-Cys Drug Info Ki = 1200 nM [1]
Asp-D-Glu-Leu-Glu-Cha-Cys Drug Info Ki = 1540 nM [1]
Boc-Ile-Leu-L-(difluoro)aminobutyric aid Drug Info IC50 = 1000 nM [2]
Cbz-Ile-Leu-L-(difluoro)aminobutyric acid Drug Info IC50 = 1700 nM [2]
GNF-PF-3464 Drug Info IC50 = 7092 nM [3]
PATULIN Drug Info IC50 = 3800 nM [2]
SCH-68631 Drug Info IC50 = 7000 nM [2]
References
REF 1 Inhibition of hepatitis C virus NS3 protease activity by product-based peptides is dependent on helicase domain. Bioorg Med Chem Lett. 2001 Jan 22;11(2):203-6.
REF 2 Control of hepatitis C: a medicinal chemistry perspective. J Med Chem. 2005 Jan 13;48(1):1-20.
REF 3 In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6.

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