Assay Detail
Binding
CHEMBL4182207
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Inhibition of HCV genotype 1b Con1 NS3 protease infected in human HuH7 replicon cells assessed as reduction in viral replication after 4 days by luciferase reporter gene assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Hepatitis C virus (isolate Con1) |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
The discovery and optimization of naphthalene-linked P2-P4 Macrocycles as inhibitors of HCV NS3 protease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 22 | 8.03 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4215698 | — | — | 1 | 9.70 |
| CHEMBL4202696 | — | — | 1 | 9.52 |
| CHEMBL4205832 | — | — | 1 | 9.22 |
| CHEMBL4210795 | — | — | 1 | 9.00 |
| CHEMBL2105735 | ASUNAPREVIR | 4.0 | 1 | 8.92 |
| CHEMBL4204453 | — | — | 1 | 8.74 |
| CHEMBL4210743 | — | — | 1 | 8.52 |
| CHEMBL3933212 | — | — | 1 | 8.35 |
| CHEMBL4209552 | — | — | 1 | 8.30 |
| CHEMBL4211655 | — | — | 1 | 8.15 |
| CHEMBL4213684 | — | — | 1 | 8.10 |
| CHEMBL4207524 | — | — | 1 | 7.82 |
| CHEMBL4216353 | — | — | 1 | 7.80 |
| CHEMBL4211245 | — | — | 1 | 7.75 |
| CHEMBL4212349 | — | — | 1 | 7.47 |
| CHEMBL4211385 | — | — | 1 | 7.46 |
| CHEMBL4216640 | — | — | 1 | 7.46 |
| CHEMBL4215939 | — | — | 1 | 7.30 |
| CHEMBL4217267 | — | — | 1 | 7.16 |
| CHEMBL4207303 | — | — | 1 | 6.89 |
| CHEMBL4217305 | — | — | 1 | 6.60 |
| CHEMBL4212654 | — | — | 1 | 6.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4215698 | — | EC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4202696 | — | EC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4205832 | — | EC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4210795 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2105735 | ASUNAPREVIR | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4204453 | — | EC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4210743 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3933212 | — | EC50 | = | 4.5 | nM | 8.35 |
| CHEMBL4209552 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4211655 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4213684 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4207524 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4216353 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4211245 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4212349 | — | EC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4211385 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4216640 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4215939 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4217267 | — | EC50 | = | 69.0 | nM | 7.16 |
| CHEMBL4207303 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4217305 | — | EC50 | = | 253.0 | nM | 6.60 |
| CHEMBL4212654 | — | EC50 | = | 302.0 | nM | 6.52 |