Assay Detail
Binding
CHEMBL2213245
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Inhibition of cathepsin L using FR-aminoluciferin as substrate preincubated for 15 mins before substrate addition measured after 1 hr by luminescence assay
17
Total Activities
17
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 cathepsin S inhibitors characterized by a triazole P1-P2 amide replacement.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.26 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2207571 | — | — | 1 | 7.30 |
| CHEMBL251327 | — | — | 1 | 7.21 |
| CHEMBL2207570 | — | — | 1 | 6.89 |
| CHEMBL2207560 | — | — | 1 | 6.70 |
| CHEMBL249915 | — | — | 1 | 6.64 |
| CHEMBL2207564 | — | — | 1 | 6.40 |
| CHEMBL2207569 | — | — | 1 | 6.30 |
| CHEMBL2207562 | — | — | 1 | 6.22 |
| CHEMBL1236882 | — | — | 1 | 6.00 |
| CHEMBL2207565 | — | — | 1 | 6.00 |
| CHEMBL2207568 | — | — | 1 | 5.89 |
| CHEMBL2207567 | — | — | 1 | 5.05 |
| CHEMBL2207563 | — | — | 1 | 4.75 |
| CHEMBL387191 | — | — | 1 | - |
| CHEMBL2207561 | — | — | 1 | - |
| CHEMBL2207566 | — | — | 1 | - |
| CHEMBL2207559 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2207571 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL251327 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL2207570 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL2207560 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL249915 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL2207564 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL2207569 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL2207562 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL1236882 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL2207565 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2207568 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL2207567 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL2207563 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL387191 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL2207561 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL2207566 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL2207559 | — | IC50 | > | 20000.0 | nM | - |