Assay Detail
Binding
CHEMBL881506
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Inhibitory activity against cathepsin K using humanized rabbit enzyme
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Oryctolagus cuniculus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Trifluoroethylamines as amide isosteres in inhibitors of cathepsin K.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 8.16 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL371133 | — | — | 1 | 9.40 |
| CHEMBL426819 | — | — | 1 | 9.22 |
| CHEMBL182956 | — | — | 1 | 9.00 |
| CHEMBL372979 | — | — | 1 | 8.89 |
| CHEMBL372046 | — | — | 1 | 8.62 |
| CHEMBL193813 | — | — | 1 | 8.60 |
| CHEMBL195505 | — | — | 1 | 8.34 |
| CHEMBL194914 | — | — | 1 | 8.30 |
| CHEMBL184514 | — | — | 1 | 7.96 |
| CHEMBL197093 | — | — | 1 | 7.52 |
| CHEMBL433995 | — | — | 1 | 6.10 |
| CHEMBL195000 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL371133 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL426819 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL182956 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL372979 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL372046 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL193813 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL195505 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL194914 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL184514 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL197093 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL433995 | — | IC50 | = | 802.0 | nM | 6.10 |
| CHEMBL195000 | — | IC50 | = | 988.0 | nM | 6.00 |