Assay Detail
Binding
CHEMBL5035309
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Time dependent inhibition of Trypanosoma cruzi cruzain using Cbz-Phe-Arg-AMC as substrate assessed as inhibition constant for EI complex measured for 0.5 to 1 hr by fluorescence based analysis
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Trypanosoma cruzi |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Self-Masked Aldehyde Inhibitors: A Novel Strategy for Inhibiting Cysteine Proteases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 7.69 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL91704 | K-777 | 2.0 | 1 | 9.70 |
| CHEMBL128135 | — | — | 1 | 9.36 |
| CHEMBL5079418 | — | — | 1 | 9.30 |
| CHEMBL5081709 | — | — | 1 | 7.75 |
| CHEMBL5079571 | — | — | 1 | 7.66 |
| CHEMBL5084365 | — | — | 1 | 7.33 |
| CHEMBL5080091 | — | — | 1 | 7.32 |
| CHEMBL5076256 | — | — | 1 | 7.31 |
| CHEMBL5082439 | — | — | 1 | 7.13 |
| CHEMBL5089591 | — | — | 1 | 6.99 |
| CHEMBL5079029 | — | — | 1 | 6.46 |
| CHEMBL5091908 | — | — | 1 | 6.00 |
| CHEMBL5072701 | — | — | 1 | - |
| CHEMBL5079046 | — | — | 1 | - |
| CHEMBL5092503 | — | — | 1 | - |
| CHEMBL5079476 | — | — | 1 | - |
| CHEMBL5082504 | — | — | 1 | - |
| CHEMBL5077312 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL91704 | K-777 | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL128135 | — | Ki | = | 0.44 | nM | 9.36 |
| CHEMBL5079418 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL5081709 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL5079571 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL5084365 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL5080091 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL5076256 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL5082439 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL5089591 | — | Ki | = | 103.0 | nM | 6.99 |
| CHEMBL5079029 | — | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL5091908 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL5072701 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL5079046 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL5092503 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL5079476 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL5082504 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL5077312 | — | Ki | > | 5000.0 | nM | - |