Assay Detail
Binding
CHEMBL4718383
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of cathepsin L (unknown origin) using Z-FR-AMC as substrate preincubated for 30 mins followed by substrate addition and further incubated for 30 mins under shaking condition by fluorescence assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Neuroprotective effect of synthetic chalcone derivatives as competitive dual inhibitors against μ-calpain and cathepsin B through the downregulation of tau phosphorylation and insoluble Aβ peptide formation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.32 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL423112 | — | — | 1 | 8.51 |
| CHEMBL92708 | CALPEPTIN | — | 1 | 7.14 |
| CHEMBL2368566 | — | — | 1 | 7.08 |
| CHEMBL63440 | ALOXISTATIN | 2.0 | 1 | 5.62 |
| CHEMBL4740912 | — | — | 1 | 4.83 |
| CHEMBL4746320 | — | — | 1 | 4.81 |
| CHEMBL4756611 | — | — | 1 | 4.79 |
| CHEMBL4743183 | — | — | 1 | 4.67 |
| CHEMBL4765091 | — | — | 1 | 4.59 |
| CHEMBL4786246 | — | — | 1 | 4.58 |
| CHEMBL4799634 | — | — | 1 | 4.57 |
| CHEMBL4740843 | — | — | 1 | 4.48 |
| CHEMBL4789024 | — | — | 1 | 4.45 |
| CHEMBL4764053 | — | — | 1 | 4.32 |
| CHEMBL490920 | — | — | 1 | - |
| CHEMBL4780290 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL423112 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL92708 | CALPEPTIN | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL2368566 | — | IC50 | = | 83.7 | nM | 7.08 |
| CHEMBL63440 | ALOXISTATIN | IC50 | = | 2410.0 | nM | 5.62 |
| CHEMBL4740912 | — | IC50 | = | 14870.0 | nM | 4.83 |
| CHEMBL4746320 | — | IC50 | = | 15610.0 | nM | 4.81 |
| CHEMBL4756611 | — | IC50 | = | 16040.0 | nM | 4.79 |
| CHEMBL4743183 | — | IC50 | = | 21590.0 | nM | 4.67 |
| CHEMBL4765091 | — | IC50 | = | 25790.0 | nM | 4.59 |
| CHEMBL4786246 | — | IC50 | = | 26120.0 | nM | 4.58 |
| CHEMBL4799634 | — | IC50 | = | 27010.0 | nM | 4.57 |
| CHEMBL4740843 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL4789024 | — | IC50 | = | 35370.0 | nM | 4.45 |
| CHEMBL4764053 | — | IC50 | = | 48410.0 | nM | 4.32 |
| CHEMBL490920 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4780290 | — | IC50 | > | 50000.0 | nM | - |