Assay Detail
Binding
CHEMBL877099
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Inhibitory activity towards human calpain I
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
1,2-Benzothiazine 1,1-dioxide P(2)-P(3) peptide mimetic aldehyde calpain I inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 7.49 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL117553 | — | — | 1 | 8.30 |
| CHEMBL326161 | — | — | 1 | 8.22 |
| CHEMBL118688 | — | — | 1 | 8.15 |
| CHEMBL269384 | — | — | 1 | 8.15 |
| CHEMBL269333 | — | — | 1 | 8.10 |
| CHEMBL421043 | — | — | 1 | 7.82 |
| CHEMBL115954 | — | — | 1 | 7.62 |
| CHEMBL331414 | — | — | 1 | 7.55 |
| CHEMBL115963 | — | — | 1 | 7.55 |
| CHEMBL420698 | — | — | 1 | 7.55 |
| CHEMBL117006 | — | — | 1 | 7.52 |
| CHEMBL115573 | — | — | 1 | 7.52 |
| CHEMBL333622 | — | — | 1 | 7.44 |
| CHEMBL117694 | — | — | 1 | 7.43 |
| CHEMBL115572 | — | — | 1 | 7.43 |
| CHEMBL332683 | — | — | 1 | 7.42 |
| CHEMBL331649 | — | — | 1 | 7.29 |
| CHEMBL118817 | — | — | 1 | 7.08 |
| CHEMBL331733 | — | — | 1 | 6.89 |
| CHEMBL332638 | — | — | 1 | 6.82 |
| CHEMBL117729 | — | — | 1 | 6.70 |
| CHEMBL323656 | — | — | 1 | 6.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL117553 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL326161 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL118688 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL269384 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL269333 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL421043 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL115954 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL331414 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL115963 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL420698 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL117006 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL115573 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL333622 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL117694 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL115572 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL332683 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL331649 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL118817 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL331733 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL332638 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL117729 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL323656 | — | IC50 | = | 700.0 | nM | 6.16 |