Assay Detail
Binding
CHEMBL744606
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Inhibition of calpain, using human mu-calpain isolated from erythrocytes and Suc-Leu-Tyr-AMC as the fluorogenic substrate
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Discovery of phenyl alanine derived ketoamides carrying benzoyl residues as novel calpain inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 7.01 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL280587 | — | — | 1 | 8.22 |
| CHEMBL423112 | — | — | 1 | 7.82 |
| CHEMBL280654 | — | — | 1 | 7.82 |
| CHEMBL284866 | — | — | 1 | 7.40 |
| CHEMBL282979 | — | — | 1 | 7.40 |
| CHEMBL28203 | — | — | 1 | 7.30 |
| CHEMBL27036 | — | — | 1 | 7.30 |
| CHEMBL441599 | — | — | 1 | 7.10 |
| CHEMBL283475 | — | — | 1 | 7.05 |
| CHEMBL26631 | — | — | 1 | 6.85 |
| CHEMBL281731 | — | — | 1 | 6.70 |
| CHEMBL28444 | — | — | 1 | 6.64 |
| CHEMBL26870 | — | — | 1 | 6.55 |
| CHEMBL26381 | — | — | 1 | 6.43 |
| CHEMBL280652 | — | — | 1 | 6.35 |
| CHEMBL27250 | — | — | 1 | 6.35 |
| CHEMBL281874 | — | — | 1 | 5.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL280587 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL423112 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL280654 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL284866 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL282979 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL28203 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL27036 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL441599 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL283475 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL26631 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL281731 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL28444 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL26870 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL26381 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL280652 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL27250 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL281874 | — | Ki | = | 1080.0 | nM | 5.97 |