Assay Detail
Binding
CHEMBL657758
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The calpain inhibitory activity(I 50) was measured as ability to enter the platelet to inhibit calpain after cell lysis(assay 2)
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Ester and amide derivatives of E64c as inhibitors of platelet calpains.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 5.65 | 6.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL302897 | — | — | 1 | 6.52 |
| CHEMBL61010 | — | — | 1 | 6.00 |
| CHEMBL64174 | — | — | 1 | 5.70 |
| CHEMBL63494 | — | — | 1 | 5.70 |
| CHEMBL303315 | — | — | 1 | 5.70 |
| CHEMBL418130 | — | — | 1 | 5.70 |
| CHEMBL294046 | — | — | 1 | 5.52 |
| CHEMBL63440 | ALOXISTATIN | 2.0 | 1 | 5.40 |
| CHEMBL60482 | — | — | 1 | 5.40 |
| CHEMBL302443 | — | — | 1 | 5.30 |
| CHEMBL64647 | — | — | 1 | 5.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL302897 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL61010 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL64174 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL63494 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL303315 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL418130 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL294046 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL63440 | ALOXISTATIN | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL60482 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL302443 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL64647 | — | IC50 | = | 6000.0 | nM | 5.22 |