Assay Detail
Binding
CHEMBL769055
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Inhibitory activity against P2 site in HIV protease.
7
Total Activities
7
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 | Autocuration |
Target
Human immunodeficiency virus type 1 protease (CHEMBL243) ↗| Type | SINGLE PROTEIN |
| Organism | Human immunodeficiency virus 1 |
Publication
-Methanesulfonyl-L-valine as a novel, unnatural amino acid surrogate for P2 in the design of HIV protease inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 9.50 | 9.95 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL154519 | — | — | 1 | 9.95 |
| CHEMBL350243 | — | — | 1 | 9.82 |
| CHEMBL154692 | — | — | 1 | 9.79 |
| CHEMBL345187 | — | — | 1 | 9.76 |
| CHEMBL114 | SAQUINAVIR | 4.0 | 1 | 9.35 |
| CHEMBL75082 | — | — | 1 | 9.26 |
| CHEMBL154416 | — | — | 1 | 8.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL154519 | — | Ki | = | 0.113 | nM | 9.95 |
| CHEMBL350243 | — | Ki | = | 0.151 | nM | 9.82 |
| CHEMBL154692 | — | Ki | = | 0.162 | nM | 9.79 |
| CHEMBL345187 | — | Ki | = | 0.172 | nM | 9.76 |
| CHEMBL114 | SAQUINAVIR | Ki | = | 0.452 | nM | 9.35 |
| CHEMBL75082 | — | Ki | = | 0.55 | nM | 9.26 |
| CHEMBL154416 | — | Ki | = | 2.59 | nM | 8.59 |