Assay Detail
Binding
CHEMBL763236
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In vitro enzyme inhibitory activity against HIV-1 protease.
20
Total Activities
20
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
Synthesis and antiviral activity of a series of HIV-1 protease inhibitors with functionality tethered to the P1 or P1' phenyl substituents: X-ray crystal structure assisted design.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 9.48 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL295414 | — | — | 1 | 10.40 |
| CHEMBL295442 | — | — | 1 | 10.15 |
| CHEMBL416082 | — | — | 1 | 10.10 |
| CHEMBL295549 | — | — | 1 | 10.05 |
| CHEMBL295470 | — | — | 1 | 9.82 |
| CHEMBL298316 | — | — | 1 | 9.80 |
| CHEMBL45451 | — | — | 1 | 9.74 |
| CHEMBL44578 | — | — | 1 | 9.70 |
| CHEMBL46274 | — | — | 1 | 9.70 |
| CHEMBL297673 | — | — | 1 | 9.70 |
| CHEMBL297045 | — | — | 1 | 9.46 |
| CHEMBL296115 | — | — | 1 | 9.46 |
| CHEMBL47712 | — | — | 1 | 9.33 |
| CHEMBL45457 | — | — | 1 | 9.26 |
| CHEMBL295482 | — | — | 1 | 9.05 |
| CHEMBL46062 | — | — | 1 | 9.00 |
| CHEMBL291203 | — | — | 1 | 8.80 |
| CHEMBL295609 | — | — | 1 | 8.74 |
| CHEMBL295013 | — | — | 1 | 8.72 |
| CHEMBL45474 | — | — | 1 | 8.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL295414 | — | IC50 | = | 0.04 | nM | 10.40 |
| CHEMBL295442 | — | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL416082 | — | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL295549 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL295470 | — | IC50 | = | 0.15 | nM | 9.82 |
| CHEMBL298316 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL45451 | — | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL44578 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL46274 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL297673 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL297045 | — | IC50 | = | 0.35 | nM | 9.46 |
| CHEMBL296115 | — | IC50 | = | 0.35 | nM | 9.46 |
| CHEMBL47712 | — | IC50 | = | 0.47 | nM | 9.33 |
| CHEMBL45457 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL295482 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL46062 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL291203 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL295609 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL295013 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL45474 | — | IC50 | = | 2.0 | nM | 8.70 |