Assay Detail
Binding
CHEMBL864511
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Inhibitory activity against human cathepsin L expressed in HepG2 cells
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HepG2 |
| 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 | 6 | 6.73 | 7.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL371064 | BALICATIB | 2.0 | 1 | 7.32 |
| CHEMBL200884 | — | — | 1 | 6.64 |
| CHEMBL184514 | — | — | 1 | 6.50 |
| CHEMBL426819 | — | — | 1 | 6.47 |
| CHEMBL199358 | — | — | 1 | - |
| CHEMBL200301 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL371064 | BALICATIB | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL200884 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL184514 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL426819 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL199358 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL200301 | — | IC50 | > | 10000.0 | nM | - |