Assay Detail
Binding
CHEMBL769378
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Inhibition of HIV-1 protease in vitro.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Human immunodeficiency virus type 1 protease (CHEMBL243) ↗| Type | SINGLE PROTEIN |
| Organism | Human immunodeficiency virus 1 |
Publication
Identification of MK-944a: a second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 9.41 | 9.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL113845 | — | — | 1 | 9.96 |
| CHEMBL96645 | — | — | 1 | 9.92 |
| CHEMBL325951 | — | — | 1 | 9.85 |
| CHEMBL408413 | — | — | 1 | 9.77 |
| CHEMBL1233940 | L 756423 | 2.0 | 1 | 9.74 |
| CHEMBL325013 | — | — | 1 | 9.72 |
| CHEMBL324025 | — | — | 1 | 9.66 |
| CHEMBL325181 | — | — | 1 | 9.60 |
| CHEMBL112257 | — | — | 1 | 9.59 |
| CHEMBL324516 | — | — | 1 | 9.49 |
| CHEMBL2062137 | — | — | 1 | 9.46 |
| CHEMBL325354 | — | — | 1 | 9.41 |
| CHEMBL1735 | INDINAVIR SULFATE | 4.0 | 1 | 9.39 |
| CHEMBL114834 | — | — | 1 | 9.33 |
| CHEMBL116107 | — | — | 1 | 9.31 |
| CHEMBL333607 | — | — | 1 | 9.21 |
| CHEMBL325946 | — | — | 1 | 9.17 |
| CHEMBL323882 | — | — | 1 | 8.96 |
| CHEMBL332498 | — | — | 1 | 8.77 |
| CHEMBL325395 | — | — | 1 | 8.77 |
| CHEMBL325267 | — | — | 1 | 8.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL113845 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL96645 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL325951 | — | IC50 | = | 0.14 | nM | 9.85 |
| CHEMBL408413 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL1233940 | L 756423 | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL325013 | — | IC50 | = | 0.19 | nM | 9.72 |
| CHEMBL324025 | — | IC50 | = | 0.22 | nM | 9.66 |
| CHEMBL325181 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL112257 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL324516 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL2062137 | — | IC50 | = | 0.35 | nM | 9.46 |
| CHEMBL325354 | — | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL1735 | INDINAVIR SULFATE | IC50 | = | 0.41 | nM | 9.39 |
| CHEMBL114834 | — | IC50 | = | 0.47 | nM | 9.33 |
| CHEMBL116107 | — | IC50 | = | 0.49 | nM | 9.31 |
| CHEMBL333607 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL325946 | — | IC50 | = | 0.68 | nM | 9.17 |
| CHEMBL323882 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL332498 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL325395 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL325267 | — | IC50 | = | 3.4 | nM | 8.47 |