Assay Detail
Binding
CHEMBL4263564
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Inhibition of calpain (unknown origin) using Suc-LY-AMC as fluorogenic substrate after 60 mins by spectrofluorometric analysis
12
Total Activities
12
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
Discovery of potent calpain inhibitors based on the azolo-imidazolidenone scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.59 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4277595 | — | — | 1 | 7.70 |
| CHEMBL92708 | CALPEPTIN | — | 1 | 7.28 |
| CHEMBL4281019 | — | — | 1 | 6.46 |
| CHEMBL4277940 | — | — | 1 | 6.42 |
| CHEMBL4285250 | — | — | 1 | 6.34 |
| CHEMBL4279497 | — | — | 1 | 5.99 |
| CHEMBL4293865 | — | — | 1 | 5.97 |
| CHEMBL4290527 | — | — | 1 | - |
| CHEMBL4285540 | — | — | 1 | - |
| CHEMBL4288918 | — | — | 1 | - |
| CHEMBL4287411 | — | — | 1 | - |
| CHEMBL4283272 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4277595 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL92708 | CALPEPTIN | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4281019 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4277940 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL4285250 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL4279497 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL4293865 | — | IC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL4290527 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4285540 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4288918 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4287411 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4283272 | — | IC50 | > | 1000.0 | nM | - |