Assay Detail
Functional
CHEMBL684614
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HIV-1 protease in a cell culture assay using HIV-1 IIIB infected H9 cells.
33
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Human immunodeficiency virus 1 |
| Cell Type | H9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Human immunodeficiency virus type 1 protease (CHEMBL243) ↗| Type | SINGLE PROTEIN |
| Organism | Human immunodeficiency virus 1 |
Publication
Tipranavir (PNU-140690): a potent, orally bioavailable nonpeptidic HIV protease inhibitor of the 5,6-dihydro-4-hydroxy-2-pyrone sulfonamide class.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 6.34 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL222559 | TIPRANAVIR | 4.0 | 1 | 7.52 |
| CHEMBL2112565 | — | — | 1 | 7.40 |
| CHEMBL2092977 | — | — | 1 | 6.96 |
| CHEMBL2112562 | — | — | 1 | 6.89 |
| CHEMBL21405 | — | — | 1 | 6.89 |
| CHEMBL325454 | — | — | 1 | 6.85 |
| CHEMBL332684 | — | — | 1 | 6.85 |
| CHEMBL421230 | — | — | 1 | 6.82 |
| CHEMBL116068 | — | — | 1 | 6.64 |
| CHEMBL2111768 | — | — | 2 | 6.39 |
| CHEMBL2111769 | — | — | 1 | 6.31 |
| CHEMBL21188 | — | — | 1 | 6.30 |
| CHEMBL117389 | — | — | 1 | 6.28 |
| CHEMBL2112566 | — | — | 1 | 6.24 |
| CHEMBL117719 | — | — | 1 | 6.22 |
| CHEMBL116965 | — | — | 1 | 6.19 |
| CHEMBL117500 | — | — | 1 | 6.16 |
| CHEMBL118006 | — | — | 1 | 6.10 |
| CHEMBL116265 | — | — | 1 | 6.00 |
| CHEMBL20846 | — | — | 1 | 6.00 |
| CHEMBL21281 | — | — | 1 | 5.96 |
| CHEMBL117856 | — | — | 1 | 5.92 |
| CHEMBL326566 | — | — | 1 | 5.92 |
| CHEMBL115743 | — | — | 1 | 5.80 |
| CHEMBL116798 | — | — | 1 | 5.75 |
| CHEMBL332043 | — | — | 1 | 5.75 |
| CHEMBL119906 | — | — | 1 | 5.64 |
| CHEMBL117638 | — | — | 1 | - |
| CHEMBL2111770 | — | — | 1 | - |
| CHEMBL2111771 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL222559 | TIPRANAVIR | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2112565 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2092977 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL2112562 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL21405 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL325454 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL332684 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL421230 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL116068 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL2111768 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL2111769 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL21188 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL117389 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL2112566 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL117719 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL116965 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL117500 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL118006 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL116265 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL20846 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL21281 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL117856 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL326566 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL115743 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL2111768 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL116798 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL332043 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL119906 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL2111770 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL117638 | — | IC50 | < | 1000.0 | nM | - |
| CHEMBL2111771 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2092978 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL324579 | — | IC50 | > | 1000.0 | nM | - |