Assay Detail
Binding
CHEMBL5147056
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Inhibition of epimastigote form of Trypanosoma cruzi Tulahuen 2 cruzain assessed as reduction in 7-amino-4-methylcoumarin release incubated for 20 mins folllowed by Z-FR-AMC substrate addition and measured up to 45 mins by fluorometric assay
21
Total Activities
11
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
Thiosemicarbazone derivatives: Evaluation as cruzipain inhibitors and molecular modeling study of complexes with cruzain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 6.04 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL92099 | — | — | 2 | 7.16 |
| CHEMBL415311 | — | — | 2 | 7.09 |
| CHEMBL90512 | — | — | 2 | 6.83 |
| CHEMBL313679 | — | — | 2 | 6.82 |
| CHEMBL373586 | — | — | 2 | 6.12 |
| CHEMBL5169822 | — | — | 2 | 5.12 |
| CHEMBL90866 | — | — | 2 | 4.63 |
| CHEMBL5197613 | — | — | 2 | 4.52 |
| CHEMBL1269725 | — | — | 2 | - |
| CHEMBL92579 | — | — | 2 | - |
| CHEMBL4172404 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL92099 | — | IC50 | = | 69.5 | nM | 7.16 |
| CHEMBL92099 | — | IC50 | = | 69.18 | nM | 7.16 |
| CHEMBL415311 | — | IC50 | = | 81.28 | nM | 7.09 |
| CHEMBL415311 | — | IC50 | = | 81.6 | nM | 7.09 |
| CHEMBL90512 | — | IC50 | = | 147.0 | nM | 6.83 |
| CHEMBL90512 | — | IC50 | = | 147.91 | nM | 6.83 |
| CHEMBL313679 | — | IC50 | = | 151.36 | nM | 6.82 |
| CHEMBL313679 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL373586 | — | IC50 | = | 758.58 | nM | 6.12 |
| CHEMBL373586 | — | IC50 | = | 753.0 | nM | 6.12 |
| CHEMBL5169822 | — | IC50 | = | 7585.78 | nM | 5.12 |
| CHEMBL5169822 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL90866 | — | IC50 | = | 23442.29 | nM | 4.63 |
| CHEMBL90866 | — | IC50 | = | 23200.0 | nM | 4.63 |
| CHEMBL5197613 | — | IC50 | = | 30199.52 | nM | 4.52 |
| CHEMBL5197613 | — | IC50 | = | 29900.0 | nM | 4.52 |
| CHEMBL92579 | — | IC50 | = | 1479108.39 | nM | - |
| CHEMBL1269725 | — | IC50 | = | 104600.0 | nM | - |
| CHEMBL1269725 | — | IC50 | = | 104712.85 | nM | - |
| CHEMBL92579 | — | IC50 | = | 1470000.0 | nM | - |
| CHEMBL4172404 | — | IC50 | - | — | - |