Assay Detail
Binding
CHEMBL895984
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Inhibition of HIV1 Protease M3 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 | 7.42 | 9.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1163 | ATAZANAVIR | 4.0 | 1 | 9.31 |
| CHEMBL729 | LOPINAVIR | 4.0 | 1 | 9.05 |
| CHEMBL116 | AMPRENAVIR | 4.0 | 1 | 8.85 |
| CHEMBL163 | RITONAVIR | 4.0 | 1 | 8.55 |
| CHEMBL114 | SAQUINAVIR | 4.0 | 1 | 7.11 |
| CHEMBL388680 | — | — | 1 | 6.95 |
| CHEMBL388901 | — | — | 1 | 6.91 |
| CHEMBL245221 | — | — | 1 | 6.73 |
| CHEMBL245003 | — | — | 1 | 6.55 |
| CHEMBL230771 | — | — | 1 | 6.41 |
| CHEMBL388689 | — | — | 1 | 6.35 |
| CHEMBL395064 | — | — | 1 | 6.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1163 | ATAZANAVIR | Ki | = | 0.49 | nM | 9.31 |
| CHEMBL729 | LOPINAVIR | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL116 | AMPRENAVIR | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL163 | RITONAVIR | Ki | = | 2.81 | nM | 8.55 |
| CHEMBL114 | SAQUINAVIR | Ki | = | 78.44 | nM | 7.11 |
| CHEMBL388680 | — | Ki | = | 112.0 | nM | 6.95 |
| CHEMBL388901 | — | Ki | = | 122.0 | nM | 6.91 |
| CHEMBL245221 | — | Ki | = | 185.0 | nM | 6.73 |
| CHEMBL245003 | — | Ki | = | 282.0 | nM | 6.55 |
| CHEMBL230771 | — | Ki | = | 392.0 | nM | 6.41 |
| CHEMBL388689 | — | Ki | = | 447.0 | nM | 6.35 |
| CHEMBL395064 | — | Ki | = | 549.0 | nM | 6.26 |