Assay Detail
Functional
CHEMBL4052029
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiviral activity against darunavir-resistant HIV1 derived from 51 passages harboring protease L10I/I15V/K20R/L24I/V32I/L33F/M36I/M46L/I54M/L63P/K70Q/V82I/I84V/L89M mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Human immunodeficiency virus 1 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Target
Human immunodeficiency virus 1 (CHEMBL378) ↗| Type | ORGANISM |
| Organism | Human immunodeficiency virus 1 |
Publication
Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.43 | 7.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4098771 | — | — | 1 | 7.46 |
| CHEMBL4059839 | — | — | 1 | 6.32 |
| CHEMBL1323 | DARUNAVIR | 4.0 | 1 | 5.50 |
| CHEMBL4088111 | — | — | 1 | - |
| CHEMBL729 | LOPINAVIR | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4098771 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4059839 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL1323 | DARUNAVIR | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL4088111 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL729 | LOPINAVIR | IC50 | > | 1000.0 | nM | - |