Assay Detail
Binding
CHEMBL763311
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Inhibition of HIV protease
14
Total Activities
13
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 | Expert |
Target
Human immunodeficiency virus type 1 protease (CHEMBL243) ↗| Type | SINGLE PROTEIN |
| Organism | Human immunodeficiency virus 1 |
Publication
Novel inhibitors of HIV protease: design, synthesis and biological evaluation of picomolar inhibitors containing cyclic P1/P2 scaffolds.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 9.32 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL584 | NELFINAVIR | 4.0 | 1 | 11.00 |
| CHEMBL163 | RITONAVIR | 4.0 | 1 | 10.70 |
| CHEMBL114 | SAQUINAVIR | 4.0 | 1 | 10.40 |
| CHEMBL116 | AMPRENAVIR | 4.0 | 1 | 10.40 |
| CHEMBL279869 | — | — | 1 | 10.30 |
| CHEMBL263072 | — | — | 2 | 10.30 |
| CHEMBL5483011 | INDINAVIR | 3.0 | 1 | 10.15 |
| CHEMBL278928 | — | — | 1 | 9.10 |
| CHEMBL262204 | — | — | 1 | 8.92 |
| CHEMBL407895 | — | — | 1 | 7.80 |
| CHEMBL16167 | — | — | 1 | 6.48 |
| CHEMBL279397 | — | — | 1 | 5.32 |
| CHEMBL278174 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL584 | NELFINAVIR | Ki | = | 0.01 | nM | 11.00 |
| CHEMBL163 | RITONAVIR | Ki | = | 0.02 | nM | 10.70 |
| CHEMBL114 | SAQUINAVIR | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL116 | AMPRENAVIR | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL279869 | — | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL263072 | — | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL263072 | — | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL5483011 | INDINAVIR | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL278928 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL262204 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL407895 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL16167 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL279397 | — | Ki | = | 4800.0 | nM | 5.32 |
| CHEMBL278174 | — | Ki | > | 0.5 | nM | - |