Assay Detail
Binding
CHEMBL657292
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Inhibitory concentration against recombinant human cathepsin B was determined in a fluorescence assay using 10 uM Cbz-Phe-Arg-AMC as substrate
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Exploration of the P2-P3 SAR of aldehyde cathepsin K inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 6.00 | 7.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL114462 | — | — | 1 | 7.14 |
| CHEMBL116402 | — | — | 1 | 6.40 |
| CHEMBL114161 | — | — | 1 | 6.34 |
| CHEMBL117658 | — | — | 1 | 6.09 |
| CHEMBL116779 | — | — | 1 | 5.66 |
| CHEMBL116724 | — | — | 1 | 5.47 |
| CHEMBL117144 | — | — | 1 | 4.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL114462 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL116402 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL114161 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL117658 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL116779 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL116724 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL117144 | — | IC50 | = | 12000.0 | nM | 4.92 |