Assay Detail
Functional
CHEMBL1026413
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Antiviral activity against multidrug-resistant HIV1 with protease L10I, K14R, R41K, M46L, I54V, L63P, A71V, V82A, L90M, I93L mutation in phytohemagglutininin-activated PBMC assessed as inhibition of p24Gag protein production
6
Total Activities
6
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
Flexible cyclic ethers/polyethers as novel P2-ligands for HIV-1 protease inhibitors: design, synthesis, biological evaluation, and protein-ligand X-ray studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 7.20 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1323 | DARUNAVIR | 4.0 | 1 | 8.40 |
| CHEMBL523528 | — | — | 1 | 7.19 |
| CHEMBL492254 | — | — | 1 | 6.66 |
| CHEMBL116 | AMPRENAVIR | 4.0 | 1 | 6.54 |
| CHEMBL5483011 | INDINAVIR | 3.0 | 1 | - |
| CHEMBL163 | RITONAVIR | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1323 | DARUNAVIR | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL523528 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL492254 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL116 | AMPRENAVIR | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL5483011 | INDINAVIR | IC50 | > | 1000.0 | nM | - |
| CHEMBL163 | RITONAVIR | IC50 | > | 1000.0 | nM | - |