Assay Detail
Binding
CHEMBL863709
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Inhibition of rat cathepsin K
13
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Structure activity relationships of 5-, 6-, and 7-methyl-substituted azepan-3-one cathepsin K inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 6.75 | 8.10 |
| Ki app | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL203665 | RELACATIB | 2.0 | 1 | 8.10 |
| CHEMBL286364 | — | — | 1 | 7.22 |
| CHEMBL205172 | — | — | 1 | 7.14 |
| CHEMBL203224 | — | — | 1 | 6.37 |
| CHEMBL440574 | — | — | 1 | 6.18 |
| CHEMBL377713 | — | — | 1 | 6.17 |
| CHEMBL202991 | — | — | 1 | 6.10 |
| CHEMBL203845 | — | — | 1 | - |
| CHEMBL205068 | — | — | 1 | - |
| CHEMBL203556 | — | — | 1 | - |
| CHEMBL204169 | — | — | 1 | - |
| CHEMBL438435 | — | — | 1 | - |
| CHEMBL202668 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL203665 | RELACATIB | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL286364 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL205172 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL203224 | — | Ki | = | 430.0 | nM | 6.37 |
| CHEMBL440574 | — | Ki | = | 660.0 | nM | 6.18 |
| CHEMBL377713 | — | Ki | = | 680.0 | nM | 6.17 |
| CHEMBL202991 | — | Ki | = | 790.0 | nM | 6.10 |
| CHEMBL203845 | — | Ki app | - | — | - | |
| CHEMBL205068 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL203556 | — | Ki app | - | — | - | |
| CHEMBL204169 | — | Ki app | - | — | - | |
| CHEMBL438435 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL202668 | — | Ki app | - | — | - |