Assay Detail
Binding
CHEMBL5320640
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Inhibition of human cathepsin K using Z-LR-AMC as substrate preincubated for 20 mins followed by pre-activated enzyme addition and measured after 15 mins by fluorescence based microplate reader analysis
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Dipeptide-Derived Alkynes as Potent and Selective Irreversible Inhibitors of Cysteine Cathepsins.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 4.89 | 5.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5405909 | — | — | 1 | 5.68 |
| CHEMBL5395533 | — | — | 1 | 5.40 |
| CHEMBL5411088 | — | — | 1 | 5.05 |
| CHEMBL5401219 | — | — | 1 | 4.72 |
| CHEMBL5413230 | — | — | 1 | 4.60 |
| CHEMBL134083 | — | — | 1 | 4.59 |
| CHEMBL5409217 | — | — | 1 | 4.58 |
| CHEMBL5432531 | — | — | 1 | 4.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5405909 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL5395533 | — | Ki | = | 4000.0 | nM | 5.40 |
| CHEMBL5411088 | — | Ki | = | 8810.0 | nM | 5.05 |
| CHEMBL5401219 | — | Ki | = | 19100.0 | nM | 4.72 |
| CHEMBL5413230 | — | Ki | = | 25000.0 | nM | 4.60 |
| CHEMBL134083 | — | Ki | = | 25940.0 | nM | 4.59 |
| CHEMBL5409217 | — | Ki | = | 26000.0 | nM | 4.58 |
| CHEMBL5432531 | — | Ki | = | 30000.0 | nM | 4.52 |