Basic Information
ID: ALA3705200
Type: Binding
Description: Enzymatic Assay: The aim of this in vitro assay was to measure the inhibition of HCV NS3/4A protease complexes by the compounds of the present invention. This assay provides an indication of how effective compounds of the present invention would be in inhibiting HCV NS3/4A proteolytic activity. The inhibition of full-length hepatitis C NS3 protease enzyme was measured essentially as described in Poliakov, 2002 Prot Expression & Purification 25 363 371. Briefly, the hydrolysis of a depsipeptide substrate, Ac-DED(Edans)EEAbuÃ[COO]ASK(Dabcyl)-NH2 (AnaSpec, San Jose, USA), was measured spectrofluorometrically in the presence of a peptide cofactor, KKGSVVIVGRIVLSGK (â «ke Engstrom, Department of Medical Biochemistry and Microbiology, Uppsala University, Sweden). [Landro, 1997 #Biochem 36 9340-9348].
Organism: Hepatitis C virus
Activity Charts
Bioactivity
Activity Types for Assay ALA3705200
Ki
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 749.96 | 5.25 | 5.25 |
| 770.37 | 5.60 | 5.60 |
| 771.36 | 5.29 | 5.29 |
| 785.39 | 5.68 | 5.68 |
| 784.40 | 5.99 | 5.99 |
| 763.98 | 5.64 | 5.64 |
| 667.23 | 6.08 | 6.08 |
| 749.96 | 5.30 | 5.30 |