Assay Detail
Binding
CHEMBL5326511
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Inhibition of recombinant Trypanosoma cruzi Cruzipain using Z-FR-AMC as substrate preincubated for 20 mins followed by substrate addition and measured for 45 mins by fluorescence analysis
12
Total Activities
9
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
Design, synthesis and biological evaluation of novel thiosemicarbazones as cruzipain inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.32 | 8.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5437573 | — | — | 2 | 8.54 |
| CHEMBL5394366 | — | — | 2 | 8.48 |
| CHEMBL5403163 | — | — | 2 | 8.17 |
| CHEMBL181504 | — | — | 1 | 7.72 |
| CHEMBL89973 | — | — | 1 | 7.22 |
| CHEMBL183767 | — | — | 1 | 7.10 |
| CHEMBL313679 | — | — | 1 | 6.75 |
| CHEMBL91844 | — | — | 1 | 5.87 |
| CHEMBL108035 | — | — | 1 | 5.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5437573 | — | IC50 | = | 2.86 | nM | 8.54 |
| CHEMBL5394366 | — | IC50 | = | 3.34 | nM | 8.48 |
| CHEMBL5403163 | — | IC50 | = | 6.76 | nM | 8.17 |
| CHEMBL5437573 | — | IC50 | = | 8.54 | nM | 8.07 |
| CHEMBL5394366 | — | IC50 | = | 8.48 | nM | 8.07 |
| CHEMBL181504 | — | IC50 | = | 19.01 | nM | 7.72 |
| CHEMBL89973 | — | IC50 | = | 59.98 | nM | 7.22 |
| CHEMBL183767 | — | IC50 | = | 79.98 | nM | 7.10 |
| CHEMBL5403163 | — | IC50 | = | 175.0 | nM | 6.76 |
| CHEMBL313679 | — | IC50 | = | 176.2 | nM | 6.75 |
| CHEMBL91844 | — | IC50 | = | 1361.44 | nM | 5.87 |
| CHEMBL108035 | — | IC50 | = | 7998.34 | nM | 5.10 |