Assay Detail
Binding
CHEMBL868692
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Inhibitory activity against rabbit cathepsin K
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Oryctolagus cuniculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 8.10 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL426819 | — | — | 1 | 9.30 |
| CHEMBL371064 | BALICATIB | 2.0 | 1 | 8.57 |
| CHEMBL199358 | — | — | 1 | 8.02 |
| CHEMBL184514 | — | — | 1 | 7.48 |
| CHEMBL200301 | — | — | 1 | 7.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL426819 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL371064 | BALICATIB | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL199358 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL184514 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL200301 | — | IC50 | = | 72.0 | nM | 7.14 |