Assay Detail
Binding
CHEMBL4718381
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human erythrocytes mu-calpain using Pep1 as substrate incubated for 30 mins under shaking condition in presence of CaCl2 by fluorescence assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Erythrocyte |
| 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 | 5.04 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL423112 | — | — | 1 | 7.00 |
| CHEMBL92708 | CALPEPTIN | — | 1 | 6.53 |
| CHEMBL2368566 | — | — | 1 | 6.40 |
| CHEMBL4765091 | — | — | 1 | 4.99 |
| CHEMBL4799634 | — | — | 1 | 4.89 |
| CHEMBL4786246 | — | — | 1 | 4.86 |
| CHEMBL4756611 | — | — | 1 | 4.77 |
| CHEMBL4764053 | — | — | 1 | 4.72 |
| CHEMBL4740912 | — | — | 1 | 4.72 |
| CHEMBL4746320 | — | — | 1 | 4.62 |
| CHEMBL4740843 | — | — | 1 | 4.39 |
| CHEMBL4780290 | — | — | 1 | 4.33 |
| CHEMBL63440 | ALOXISTATIN | 2.0 | 1 | 4.21 |
| CHEMBL4743183 | — | — | 1 | 4.16 |
| CHEMBL490920 | — | — | 1 | - |
| CHEMBL4789024 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL423112 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL92708 | CALPEPTIN | IC50 | = | 297.0 | nM | 6.53 |
| CHEMBL2368566 | — | IC50 | = | 397.1 | nM | 6.40 |
| CHEMBL4765091 | — | IC50 | = | 10230.0 | nM | 4.99 |
| CHEMBL4799634 | — | IC50 | = | 12980.0 | nM | 4.89 |
| CHEMBL4786246 | — | IC50 | = | 13700.0 | nM | 4.86 |
| CHEMBL4756611 | — | IC50 | = | 16810.0 | nM | 4.77 |
| CHEMBL4764053 | — | IC50 | = | 19060.0 | nM | 4.72 |
| CHEMBL4740912 | — | IC50 | = | 18830.0 | nM | 4.72 |
| CHEMBL4746320 | — | IC50 | = | 23820.0 | nM | 4.62 |
| CHEMBL4740843 | — | IC50 | = | 40870.0 | nM | 4.39 |
| CHEMBL4780290 | — | IC50 | = | 46570.0 | nM | 4.33 |
| CHEMBL63440 | ALOXISTATIN | IC50 | = | 62260.0 | nM | 4.21 |
| CHEMBL4743183 | — | IC50 | = | 69590.0 | nM | 4.16 |
| CHEMBL490920 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4789024 | — | IC50 | > | 50000.0 | nM | - |