Assay Detail
Binding
CHEMBL654079
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In vitro inhibitory activity against recombinant human calpain 1
36
Total Activities
34
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 alpha-ketoamide analogues as potent calpain I inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 6.99 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL269384 | — | — | 1 | 8.15 |
| CHEMBL8605 | — | — | 1 | 8.15 |
| CHEMBL269333 | — | — | 1 | 8.10 |
| CHEMBL8486 | MDL-28170 | — | 1 | 7.96 |
| CHEMBL8703 | — | — | 1 | 7.70 |
| CHEMBL268950 | — | — | 1 | 7.70 |
| CHEMBL8294 | — | — | 1 | 7.54 |
| CHEMBL267888 | — | — | 1 | 7.46 |
| CHEMBL8858 | — | — | 1 | 7.40 |
| CHEMBL8104 | — | — | 1 | 7.33 |
| CHEMBL8651 | — | — | 2 | 7.30 |
| CHEMBL8757 | — | — | 1 | 7.30 |
| CHEMBL276726 | — | — | 1 | 7.30 |
| CHEMBL8391 | — | — | 1 | 7.25 |
| CHEMBL8641 | — | — | 1 | 7.25 |
| CHEMBL268737 | — | — | 1 | 7.20 |
| CHEMBL8686 | — | — | 1 | 7.12 |
| CHEMBL8459 | — | — | 1 | 7.09 |
| CHEMBL418150 | — | — | 1 | 7.05 |
| CHEMBL8741 | — | — | 1 | 6.82 |
| CHEMBL269383 | — | — | 1 | 6.81 |
| CHEMBL8621 | — | — | 1 | 6.77 |
| CHEMBL8728 | — | — | 1 | 6.71 |
| CHEMBL8733 | — | — | 1 | 6.70 |
| CHEMBL436925 | — | — | 1 | 6.70 |
| CHEMBL266807 | — | — | 1 | 6.69 |
| CHEMBL262694 | — | — | 1 | 6.62 |
| CHEMBL8535 | — | — | 1 | 6.54 |
| CHEMBL8673 | — | — | 1 | 6.47 |
| CHEMBL8688 | — | — | 1 | 6.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL269384 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL8605 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL269333 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL8486 | MDL-28170 | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL8703 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL268950 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL8294 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL267888 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL8858 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL8104 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL8757 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL276726 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL8651 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL8641 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL8391 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL268737 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL8686 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL8459 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL418150 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL8741 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL269383 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL8621 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL8728 | — | IC50 | = | 195.0 | nM | 6.71 |
| CHEMBL8733 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL436925 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL266807 | — | IC50 | = | 205.0 | nM | 6.69 |
| CHEMBL262694 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL8535 | — | IC50 | = | 286.0 | nM | 6.54 |
| CHEMBL8651 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL8673 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL8688 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL1793864 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL1793864 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL266784 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL8860 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL274356 | — | IC50 | = | 5000.0 | nM | 5.30 |