Assay Detail
Binding
CHEMBL3888022
Review assay metadata, readout intent, target linkage, and publication context from the same page.
ELISA-Based Assay: Measurement of inhibition by compounds was performed using the HCV replicon system. Several different replicons encoding different HCV genotypes or mutations were used. In addition, potency measurements were made using different formats of the replicon assay, including different ways of measurements and different plating formats. See Jan M. Vrolijk et al., A replicons-based bioassay for the measurement of interferons in patients with chronic hepatitis C, 110 J. VIROLOGICAL METHODS 201 (2003); Steven S. Carroll et al., Inhibition of Hepatitis C Virus RNA Replication by 2'-Modified Nucleoside Analogs, 278(14) J. BIOLOGICAL CHEMISTRY 11979 (2003). However, the underlying principles are common to all of these determinations, and are outlined below.Stable neomycin phosphotransferase encoding replicons-harboring cell lines were used, so all cell lines were maintained under G418 selection prior to the assay. Potency was determined using a cell ELISA assay with an antibody to the replicons encoded NS3/4a protease. See Caterina Trozzi et al., In Vitro Selection and Characterization of Hepatitis C Virus Serine Protease Variants Resistant to an Active-Site Peptide Inhibitor, 77(6) J. Virol. 3669 (2003).
211
Total Activities
195
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Genome polyprotein (CHEMBL3988603) ↗| Type | SINGLE PROTEIN |
| Organism | Hepatitis C virus genotype 1b (isolate Japanese) (HCV) |
Publication
Tetracyclic heterocycle compounds and methods of use thereof for the treatment of viral diseases
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 211 | 8.23 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3947223 | — | — | 2 | 9.15 |
| CHEMBL3905713 | — | — | 2 | 9.05 |
| CHEMBL3892379 | — | — | 2 | 9.05 |
| CHEMBL3935713 | — | — | 1 | 9.05 |
| CHEMBL3933586 | — | — | 1 | 9.00 |
| CHEMBL3915462 | — | — | 1 | 8.92 |
| CHEMBL3940812 | — | — | 1 | 8.92 |
| CHEMBL3909191 | — | — | 1 | 8.92 |
| CHEMBL3939023 | — | — | 1 | 8.89 |
| CHEMBL3921348 | — | — | 2 | 8.85 |
| CHEMBL3891479 | — | — | 1 | 8.80 |
| CHEMBL3949178 | — | — | 2 | 8.80 |
| CHEMBL3943078 | — | — | 1 | 8.77 |
| CHEMBL3971537 | — | — | 1 | 8.77 |
| CHEMBL3906025 | — | — | 1 | 8.77 |
| CHEMBL3899309 | — | — | 1 | 8.74 |
| CHEMBL3956983 | — | — | 1 | 8.74 |
| CHEMBL3918127 | — | — | 1 | 8.74 |
| CHEMBL3898617 | — | — | 1 | 8.74 |
| CHEMBL3980692 | — | — | 1 | 8.72 |
| CHEMBL3928375 | — | — | 1 | 8.72 |
| CHEMBL3943320 | — | — | 1 | 8.72 |
| CHEMBL3897404 | — | — | 2 | 8.72 |
| CHEMBL3896939 | — | — | 1 | 8.70 |
| CHEMBL3957086 | — | — | 1 | 8.68 |
| CHEMBL3892828 | — | — | 1 | 8.68 |
| CHEMBL3980606 | — | — | 1 | 8.68 |
| CHEMBL3906781 | — | — | 2 | 8.68 |
| CHEMBL3899764 | — | — | 1 | 8.68 |
| CHEMBL3944919 | — | — | 2 | 8.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3947223 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3892379 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3905713 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3935713 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3933586 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3915462 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3940812 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3909191 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3939023 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3921348 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3891479 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3949178 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3971537 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3906025 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3943078 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3899309 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3898617 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3956983 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3918127 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3980692 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3928375 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3897404 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3943320 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3896939 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3957086 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3980606 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3906781 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3899764 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3944919 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3971894 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3909804 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3978542 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3892828 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3944776 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3916219 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3905576 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3956781 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3971242 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3946017 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3968106 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3982221 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3979841 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3905713 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3892379 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3934354 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3951818 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3972569 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3957324 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3947223 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3953901 | — | IC50 | = | 2.6 | nM | 8.59 |