Assay Detail
Functional
CHEMBL4195359
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiviral activity against APV resistant HIV1 harboring protease L10F/M46I/I50V/I85V mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Human immunodeficiency virus 1 |
| Cell Type | MT4 |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Target
Human immunodeficiency virus 1 (CHEMBL378) ↗| Type | ORGANISM |
| Organism | Human immunodeficiency virus 1 |
Publication
Design and Synthesis of Highly Potent HIV-1 Protease Inhibitors Containing Tricyclic Fused Ring Systems as Novel P2 Ligands: Structure-Activity Studies, Biological and X-ray Structural Analysis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 6 | 7.86 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4214453 | — | — | 1 | 9.52 |
| CHEMBL4207145 | — | — | 1 | 9.49 |
| CHEMBL1163 | ATAZANAVIR | 4.0 | 1 | 7.16 |
| CHEMBL1323 | DARUNAVIR | 4.0 | 1 | 6.70 |
| CHEMBL729 | LOPINAVIR | 4.0 | 1 | 6.41 |
| CHEMBL116 | AMPRENAVIR | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4214453 | — | EC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4207145 | — | EC50 | = | 0.32 | nM | 9.49 |
| CHEMBL1163 | ATAZANAVIR | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL1323 | DARUNAVIR | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL729 | LOPINAVIR | EC50 | = | 390.0 | nM | 6.41 |
| CHEMBL116 | AMPRENAVIR | EC50 | > | 1000.0 | nM | - |