Assay Detail
Functional
CHEMBL1659967
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Antiviral activity against HIV1 expressing protease L10F/M46L/I50V/A71Vmutant infected in human MT4 cells selected at 1 uM of GRL-286 by MTT assay
10
Total Activities
10
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 | Autocuration |
Target
Human immunodeficiency virus 1 (CHEMBL378) ↗| Type | ORGANISM |
| Organism | Human immunodeficiency virus 1 |
Publication
Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 10 | 7.06 | 7.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1163 | ATAZANAVIR | 4.0 | 1 | 7.68 |
| CHEMBL222559 | TIPRANAVIR | 4.0 | 1 | 7.43 |
| CHEMBL1323 | DARUNAVIR | 4.0 | 1 | 6.70 |
| CHEMBL584 | NELFINAVIR | 4.0 | 1 | 6.43 |
| CHEMBL116 | AMPRENAVIR | 4.0 | 1 | - |
| CHEMBL729 | LOPINAVIR | 4.0 | 1 | - |
| CHEMBL571882 | — | — | 1 | - |
| CHEMBL571982 | — | — | 1 | - |
| CHEMBL577560 | — | — | 1 | - |
| CHEMBL1650599 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1163 | ATAZANAVIR | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL222559 | TIPRANAVIR | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL1323 | DARUNAVIR | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL584 | NELFINAVIR | EC50 | = | 370.0 | nM | 6.43 |
| CHEMBL116 | AMPRENAVIR | EC50 | > | 1000.0 | nM | - |
| CHEMBL729 | LOPINAVIR | EC50 | > | 1000.0 | nM | - |
| CHEMBL571882 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL571982 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL577560 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL1650599 | — | EC50 | > | 1000.0 | nM | - |