Assay Detail
Binding
CHEMBL4047804
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HIV-1 protease using fluorogenic substrate by fluorescence assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Human immunodeficiency virus 1 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Design, synthesis, X-ray studies, and biological evaluation of novel macrocyclic HIV-1 protease inhibitors involving the P1'-P2' ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 9.23 | 10.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4067478 | — | — | 1 | 10.85 |
| CHEMBL4095133 | — | — | 1 | 10.82 |
| CHEMBL1323 | DARUNAVIR | 4.0 | 1 | 10.80 |
| CHEMBL4079687 | — | — | 1 | 10.54 |
| CHEMBL4083439 | — | — | 1 | 10.21 |
| CHEMBL4076488 | — | — | 1 | 10.21 |
| CHEMBL4091175 | — | — | 1 | 9.34 |
| CHEMBL4070241 | — | — | 1 | 9.33 |
| CHEMBL4100548 | — | — | 1 | 9.26 |
| CHEMBL4073734 | — | — | 1 | 9.19 |
| CHEMBL4068907 | — | — | 1 | 8.38 |
| CHEMBL4096186 | — | — | 1 | 8.01 |
| CHEMBL4096469 | — | — | 1 | 7.88 |
| CHEMBL4074816 | — | — | 1 | 7.88 |
| CHEMBL4080889 | — | — | 1 | 7.57 |
| CHEMBL4095267 | — | — | 1 | 7.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4067478 | — | Ki | = | 0.014 | nM | 10.85 |
| CHEMBL4095133 | — | Ki | = | 0.015 | nM | 10.82 |
| CHEMBL1323 | DARUNAVIR | Ki | = | 0.016 | nM | 10.80 |
| CHEMBL4079687 | — | Ki | = | 0.029 | nM | 10.54 |
| CHEMBL4083439 | — | Ki | = | 0.062 | nM | 10.21 |
| CHEMBL4076488 | — | Ki | = | 0.062 | nM | 10.21 |
| CHEMBL4091175 | — | Ki | = | 0.46 | nM | 9.34 |
| CHEMBL4070241 | — | Ki | = | 0.47 | nM | 9.33 |
| CHEMBL4100548 | — | Ki | = | 0.55 | nM | 9.26 |
| CHEMBL4073734 | — | Ki | = | 0.64 | nM | 9.19 |
| CHEMBL4068907 | — | Ki | = | 4.21 | nM | 8.38 |
| CHEMBL4096186 | — | Ki | = | 9.85 | nM | 8.01 |
| CHEMBL4096469 | — | Ki | = | 13.2 | nM | 7.88 |
| CHEMBL4074816 | — | Ki | = | 13.3 | nM | 7.88 |
| CHEMBL4080889 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL4095267 | — | Ki | = | 33.3 | nM | 7.48 |