Assay Detail
Binding
CHEMBL5254890
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Inhibition of HIV-1 protease using Abz-NF-6 as substrate assessed as inhibition constant measured every 2 mins for 20 mins by fluorescence based ELISA analysis
15
Total Activities
15
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
Evaluation of darunavir-derived HIV-1 protease inhibitors incorporating P2' amide-derivatives: Synthesis, biological evaluation and structural studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 8.86 | 10.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5274743 | — | — | 1 | 10.89 |
| CHEMBL1323 | DARUNAVIR | 4.0 | 1 | 10.80 |
| CHEMBL5287711 | — | — | 1 | 10.04 |
| CHEMBL5271083 | — | — | 1 | 9.52 |
| CHEMBL5288746 | — | — | 1 | 9.41 |
| CHEMBL5284706 | — | — | 1 | 9.35 |
| CHEMBL5268648 | — | — | 1 | 6.75 |
| CHEMBL5281851 | — | — | 1 | 6.51 |
| CHEMBL5278603 | — | — | 1 | 6.47 |
| CHEMBL5271223 | — | — | 1 | - |
| CHEMBL5287201 | — | — | 1 | - |
| CHEMBL5291125 | — | — | 1 | - |
| CHEMBL5280093 | — | — | 1 | - |
| CHEMBL5267260 | — | — | 1 | - |
| CHEMBL5266228 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5274743 | — | Ki | = | 0.0129 | nM | 10.89 |
| CHEMBL1323 | DARUNAVIR | Ki | = | 0.016 | nM | 10.80 |
| CHEMBL5287711 | — | Ki | = | 0.0921 | nM | 10.04 |
| CHEMBL5271083 | — | Ki | = | 0.302 | nM | 9.52 |
| CHEMBL5288746 | — | Ki | = | 0.388 | nM | 9.41 |
| CHEMBL5284706 | — | Ki | = | 0.445 | nM | 9.35 |
| CHEMBL5268648 | — | Ki | = | 177.8 | nM | 6.75 |
| CHEMBL5281851 | — | Ki | = | 310.37 | nM | 6.51 |
| CHEMBL5278603 | — | Ki | = | 337.3 | nM | 6.47 |
| CHEMBL5271223 | — | Ki | = | 0.0089 | nM | - |
| CHEMBL5287201 | — | Ki | = | 0.0044 | nM | - |
| CHEMBL5291125 | — | Ki | = | 0.0006 | nM | - |
| CHEMBL5280093 | — | Ki | = | 0.0091 | nM | - |
| CHEMBL5267260 | — | Ki | = | 0.0053 | nM | - |
| CHEMBL5266228 | — | Ki | = | 0.0015 | nM | - |