| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T40492 | ||||
| Target Name | Hepatitis C virus NS3 helicase (HCV NS3) | ||||
| Type of Target |
Successful |
||||
| Drug Potency against Target | Drug Info | IC50 = 1000 nM | [2] | ||
| 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-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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