Assay Detail
Binding
CHEMBL1811516
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Inhibition of human recombinant cathepsin S using Ac-KQLR-AMC as substrate by fluorescence assay
19
Total Activities
19
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
Azepanone-based inhibitors of human cathepsin S: optimization of selectivity via the P2 substituent.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 8.53 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1807698 | — | — | 1 | 9.30 |
| CHEMBL1807647 | — | — | 1 | 9.30 |
| CHEMBL1807700 | — | — | 1 | 9.24 |
| CHEMBL1807646 | — | — | 1 | 9.12 |
| CHEMBL1807699 | — | — | 1 | 8.92 |
| CHEMBL1807650 | — | — | 1 | 8.89 |
| CHEMBL1807703 | — | — | 1 | 8.82 |
| CHEMBL1807702 | — | — | 1 | 8.82 |
| CHEMBL1807697 | — | — | 1 | 8.72 |
| CHEMBL1807649 | — | — | 1 | 8.54 |
| CHEMBL1807645 | — | — | 1 | 8.31 |
| CHEMBL284939 | — | — | 1 | 8.08 |
| CHEMBL1807704 | — | — | 1 | 7.50 |
| CHEMBL1807696 | — | — | 1 | 7.43 |
| CHEMBL1807695 | — | — | 1 | 7.00 |
| CHEMBL1807701 | — | — | 1 | - |
| CHEMBL1807652 | — | — | 1 | - |
| CHEMBL1807651 | — | — | 1 | - |
| CHEMBL1807648 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1807698 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL1807647 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL1807700 | — | IC50 | = | 0.58 | nM | 9.24 |
| CHEMBL1807646 | — | IC50 | = | 0.76 | nM | 9.12 |
| CHEMBL1807699 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL1807650 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL1807703 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL1807702 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL1807697 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL1807649 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL1807645 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL284939 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL1807704 | — | IC50 | = | 31.6 | nM | 7.50 |
| CHEMBL1807696 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL1807695 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL1807701 | — | IC50 | < | 0.4 | nM | - |
| CHEMBL1807652 | — | IC50 | < | 0.4 | nM | - |
| CHEMBL1807651 | — | IC50 | < | 0.4 | nM | - |
| CHEMBL1807648 | — | IC50 | < | 0.4 | nM | - |