Assay Detail
Binding
CHEMBL3868487
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HCV genotype 1b NS3/4A protease assessed as substrate cleavage using Ac-C(Eu)DDMEEAbu(COO)ASK(QSY7)-amide as substrate incubated for 30 mins prior to substrate addition measured after 2.5 hrs by time-resolved fluorescence assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Hepatitis C virus subtype 1b |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Design and Synthesis of P2-P4 Macrocycles Containing a Unique Spirocyclic Proline: A New Class of HCV NS3/4A Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 10.74 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2063090 | GRAZOPREVIR ANHYDROUS | 4.0 | 1 | 11.00 |
| CHEMBL3785323 | — | — | 1 | 11.00 |
| CHEMBL3928647 | — | — | 1 | 11.00 |
| CHEMBL3924454 | — | — | 1 | 11.00 |
| CHEMBL3943429 | — | — | 1 | 10.70 |
| CHEMBL3915464 | — | — | 1 | 10.70 |
| CHEMBL3956226 | — | — | 1 | 10.52 |
| CHEMBL3962860 | — | — | 1 | 10.52 |
| CHEMBL3893915 | — | — | 1 | 10.52 |
| CHEMBL3952146 | — | — | 1 | 10.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2063090 | GRAZOPREVIR ANHYDROUS | IC50 | = | 0.01 | nM | 11.00 |
| CHEMBL3785323 | — | IC50 | = | 0.01 | nM | 11.00 |
| CHEMBL3928647 | — | IC50 | = | 0.01 | nM | 11.00 |
| CHEMBL3924454 | — | IC50 | = | 0.01 | nM | 11.00 |
| CHEMBL3943429 | — | IC50 | = | 0.02 | nM | 10.70 |
| CHEMBL3915464 | — | IC50 | = | 0.02 | nM | 10.70 |
| CHEMBL3956226 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL3962860 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL3893915 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL3952146 | — | IC50 | = | 0.04 | nM | 10.40 |