Assay Detail
Binding
CHEMBL765047
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Inhibitory activity against purified HIV-1 protease expressed in Escherichia coli in sensitive fluorometric assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Human immunodeficiency virus 1 |
| 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
Design and synthesis of new potent C2-symmetric HIV-1 protease inhibitors. Use of L-mannaric acid as a peptidomimetic scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 7.21 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL431476 | — | — | 1 | 9.70 |
| CHEMBL105459 | — | — | 1 | 9.40 |
| CHEMBL419596 | — | — | 1 | 9.05 |
| CHEMBL124093 | — | — | 1 | 8.64 |
| CHEMBL333286 | — | — | 1 | 7.09 |
| CHEMBL124770 | — | — | 1 | 6.85 |
| CHEMBL339112 | — | — | 1 | 6.30 |
| CHEMBL330858 | — | — | 1 | 6.18 |
| CHEMBL124877 | — | — | 1 | 5.70 |
| CHEMBL332554 | — | — | 1 | 5.30 |
| CHEMBL124684 | — | — | 1 | 5.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL431476 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL105459 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL419596 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL124093 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL333286 | — | Ki | = | 81.0 | nM | 7.09 |
| CHEMBL124770 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL339112 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL330858 | — | Ki | = | 660.0 | nM | 6.18 |
| CHEMBL124877 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL332554 | — | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL124684 | — | Ki | = | 7100.0 | nM | 5.15 |