Assay Detail
Binding
CHEMBL3705251
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition Assay: Briefly, 2-10 nM of purified NS3 protease domains were pre-incubated at 37° C. for 10 minutes with 20 μM isogenic NS4A peptide cofactors (Sigma, St. Louis, Mo.), in 40% glycerol buffer with 50 mM HEPES pH 7.5 and 10 mM DTT. Compounds were diluted serially 1:3 in DMSO, incubated with the enzyme/cofactor mixture for 10 minutes and reactions were started by the addition of 2 μM RET S1 substrate (final concentration). Fluorescence increase was measured continuously over one hour using a Victor3 V fluorescence plate reader (Perkin Elmer, Waltham, Mass.).
66
Total Activities
66
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Hepatitis C virus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Genome polyprotein (CHEMBL4620) ↗| Type | SINGLE PROTEIN |
| Organism | Hepatitis C virus genotype 1a (isolate 1) (HCV) |
Publication
Antiviral compounds
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 66 | 7.32 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3644933 | — | — | 1 | 8.70 |
| CHEMBL3644934 | — | — | 1 | 8.70 |
| CHEMBL3644908 | — | — | 1 | 8.70 |
| CHEMBL3644896 | — | — | 1 | 8.70 |
| CHEMBL3644888 | — | — | 1 | 8.70 |
| CHEMBL3644893 | — | — | 1 | 8.70 |
| CHEMBL3644924 | — | — | 1 | 8.52 |
| CHEMBL3644898 | — | — | 1 | 8.52 |
| CHEMBL3644895 | — | — | 1 | 8.40 |
| CHEMBL3644884 | — | — | 1 | 8.40 |
| CHEMBL3644932 | — | — | 1 | 8.30 |
| CHEMBL3644912 | — | — | 1 | 8.30 |
| CHEMBL3644881 | — | — | 1 | 8.30 |
| CHEMBL3644897 | — | — | 1 | 8.22 |
| CHEMBL3644894 | — | — | 1 | 8.22 |
| CHEMBL3644905 | — | — | 1 | 8.05 |
| CHEMBL3644907 | — | — | 1 | 8.05 |
| CHEMBL3644906 | — | — | 1 | 8.00 |
| CHEMBL3644882 | — | — | 1 | 7.96 |
| CHEMBL3644909 | — | — | 1 | 7.92 |
| CHEMBL3644911 | — | — | 1 | 7.92 |
| CHEMBL3644879 | — | — | 1 | 7.89 |
| CHEMBL3644904 | — | — | 1 | 7.89 |
| CHEMBL3644899 | — | — | 1 | 7.85 |
| CHEMBL3644883 | — | — | 1 | 7.85 |
| CHEMBL3644891 | — | — | 1 | 7.80 |
| CHEMBL3644910 | — | — | 1 | 7.80 |
| CHEMBL3644902 | — | — | 1 | 7.72 |
| CHEMBL3644935 | — | — | 1 | 7.70 |
| CHEMBL3644878 | — | — | 1 | 7.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3644933 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3644893 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3644888 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3644896 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3644934 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3644908 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3644924 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3644898 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3644895 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3644884 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3644932 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3644912 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3644881 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3644897 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3644894 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3644905 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3644907 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3644906 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3644882 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3644909 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3644911 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3644879 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3644904 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3644899 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3644883 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3644891 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3644910 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3644902 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3644935 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3644878 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3644913 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3644885 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3644892 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3644922 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3644889 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3644914 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL3644915 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3644918 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3644903 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3644917 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL3644877 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL3644901 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL3644920 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL3644890 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL3644916 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL3644921 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3644887 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3644886 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3644875 | — | IC50 | = | 195.0 | nM | 6.71 |
| CHEMBL3644880 | — | IC50 | = | 403.0 | nM | 6.39 |