Assay Detail
Binding
CHEMBL895983
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HIV1 Protease M2 variant by FRET based assay
12
Total Activities
12
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 and synthesis of HIV-1 protease inhibitors incorporating oxazolidinones as P2/P2' ligands in pseudosymmetric dipeptide isosteres.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 8.63 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL729 | LOPINAVIR | 4.0 | 1 | 10.40 |
| CHEMBL116 | AMPRENAVIR | 4.0 | 1 | 9.68 |
| CHEMBL163 | RITONAVIR | 4.0 | 1 | 9.34 |
| CHEMBL114 | SAQUINAVIR | 4.0 | 1 | 8.99 |
| CHEMBL388901 | — | — | 1 | 8.78 |
| CHEMBL388680 | — | — | 1 | 8.51 |
| CHEMBL245003 | — | — | 1 | 8.41 |
| CHEMBL245221 | — | — | 1 | 7.86 |
| CHEMBL230771 | — | — | 1 | 7.85 |
| CHEMBL388689 | — | — | 1 | 7.74 |
| CHEMBL395064 | — | — | 1 | 7.41 |
| CHEMBL1163 | ATAZANAVIR | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL729 | LOPINAVIR | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL116 | AMPRENAVIR | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL163 | RITONAVIR | Ki | = | 0.46 | nM | 9.34 |
| CHEMBL114 | SAQUINAVIR | Ki | = | 1.03 | nM | 8.99 |
| CHEMBL388901 | — | Ki | = | 1.67 | nM | 8.78 |
| CHEMBL388680 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL245003 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL245221 | — | Ki | = | 13.9 | nM | 7.86 |
| CHEMBL230771 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL388689 | — | Ki | = | 18.3 | nM | 7.74 |
| CHEMBL395064 | — | Ki | = | 39.2 | nM | 7.41 |
| CHEMBL1163 | ATAZANAVIR | Ki | = | 0.009 | nM | - |