Assay Detail
Binding
CHEMBL942076
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Inhibition of cruzain
12
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Trypanosoma cruzi |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Dipeptidyl-alpha,beta-epoxyesters as potent irreversible inhibitors of the cysteine proteases cruzain and rhodesain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Inhibition | 7 | - | - |
| IC50 | 5 | 7.83 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL91704 | K-777 | 2.0 | 2 | 8.30 |
| CHEMBL330585 | — | — | 1 | 8.00 |
| CHEMBL249814 | — | — | 2 | 7.70 |
| CHEMBL249815 | — | — | 2 | 7.30 |
| CHEMBL249810 | — | — | 2 | - |
| CHEMBL274715 | — | — | 2 | - |
| CHEMBL420256 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL91704 | K-777 | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL330585 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL249814 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL249815 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL249810 | — | Inhibition | = | 5.0 | % | - |
| CHEMBL249810 | — | Inhibition | - | % | - | |
| CHEMBL274715 | — | Inhibition | = | 1.0 | % | - |
| CHEMBL274715 | — | Inhibition | - | % | - | |
| CHEMBL249814 | — | Inhibition | = | 93.0 | % | - |
| CHEMBL91704 | K-777 | Inhibition | = | 100.0 | % | - |
| CHEMBL249815 | — | Inhibition | = | 55.0 | % | - |
| CHEMBL420256 | — | IC50 | > | 1000.0 | nM | - |