Assay Detail
Binding
CHEMBL653673
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Inhibition of Calpain 1 by [3H]acetyl-casein assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Expert |
Publication
Characterization of a continuous fluorogenic assay for calpain I. Kinetic evaluation of peptide aldehydes, halomethyl ketones and (acyloxy)methyl ketones as inhibitors of the enzyme
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.10 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL341222 | — | — | 1 | 7.70 |
| CHEMBL340020 | — | — | 1 | 7.60 |
| CHEMBL338859 | — | — | 1 | 7.52 |
| CHEMBL341014 | — | — | 1 | 7.46 |
| CHEMBL286722 | — | — | 1 | 7.40 |
| CHEMBL423112 | — | — | 1 | 7.40 |
| CHEMBL419423 | — | — | 1 | 7.26 |
| CHEMBL129657 | — | — | 1 | 7.00 |
| CHEMBL339000 | — | — | 1 | 7.00 |
| CHEMBL127613 | — | — | 1 | 7.00 |
| CHEMBL128775 | — | — | 1 | 7.00 |
| CHEMBL128776 | — | — | 1 | 6.85 |
| CHEMBL129458 | — | — | 1 | 6.57 |
| CHEMBL128135 | — | — | 1 | 6.40 |
| CHEMBL129823 | — | — | 1 | 6.30 |
| CHEMBL127663 | — | — | 1 | - |
| CHEMBL2370670 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL341222 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL340020 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL338859 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL341014 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL286722 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL423112 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL419423 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL129657 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL339000 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL127613 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL128775 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL128776 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL129458 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL128135 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL129823 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL127663 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2370670 | — | IC50 | > | 1000.0 | nM | - |