Assay Detail
Binding
CHEMBL863704
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Inhibition of human cathepsin K
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 | 13 | 8.60 | 10.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL203665 | RELACATIB | 2.0 | 1 | 10.39 |
| CHEMBL205172 | — | — | 1 | 9.85 |
| CHEMBL286364 | — | — | 1 | 9.80 |
| CHEMBL203224 | — | — | 1 | 8.85 |
| CHEMBL203845 | — | — | 1 | 8.82 |
| CHEMBL377713 | — | — | 1 | 8.60 |
| CHEMBL202991 | — | — | 1 | 8.40 |
| CHEMBL440574 | — | — | 1 | 8.35 |
| CHEMBL204169 | — | — | 1 | 7.72 |
| CHEMBL438435 | — | — | 1 | 7.54 |
| CHEMBL205068 | — | — | 1 | 7.52 |
| CHEMBL203556 | — | — | 1 | 7.38 |
| CHEMBL202668 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL203665 | RELACATIB | Ki | = | 0.041 | nM | 10.39 |
| CHEMBL205172 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL286364 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL203224 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL203845 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL377713 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL202991 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL440574 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL204169 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL438435 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL205068 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL203556 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL202668 | — | Ki | = | 0.0099 | nM | - |