Assay Detail
Binding
CHEMBL866588
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Inhibition of recombinant human cathepsin K by fluorescence assay
28
Total Activities
28
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
Novel, potent P2-P3 pyrrolidine derivatives of ketoamide-based cathepsin K inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 8.18 | 9.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL205659 | — | — | 1 | 9.38 |
| CHEMBL206515 | — | — | 1 | 9.09 |
| CHEMBL383211 | — | — | 1 | 9.00 |
| CHEMBL205759 | — | — | 1 | 8.80 |
| CHEMBL426859 | — | — | 1 | 8.77 |
| CHEMBL206559 | — | — | 1 | 8.68 |
| CHEMBL436747 | — | — | 1 | 8.68 |
| CHEMBL202685 | — | — | 1 | 8.55 |
| CHEMBL196896 | — | — | 1 | 8.52 |
| CHEMBL204284 | — | — | 1 | 8.52 |
| CHEMBL382990 | — | — | 1 | 8.42 |
| CHEMBL206482 | — | — | 1 | 8.37 |
| CHEMBL205517 | — | — | 1 | 8.30 |
| CHEMBL206740 | — | — | 1 | 8.18 |
| CHEMBL380300 | — | — | 1 | 8.16 |
| CHEMBL439517 | — | — | 1 | 8.08 |
| CHEMBL383687 | — | — | 1 | 8.05 |
| CHEMBL202723 | — | — | 1 | 7.85 |
| CHEMBL381394 | — | — | 1 | 7.82 |
| CHEMBL206191 | — | — | 1 | 7.80 |
| CHEMBL203027 | — | — | 1 | 7.77 |
| CHEMBL203466 | — | — | 1 | 7.68 |
| CHEMBL383238 | — | — | 1 | 7.62 |
| CHEMBL382832 | — | — | 1 | 7.57 |
| CHEMBL206532 | — | — | 1 | 7.54 |
| CHEMBL425236 | — | — | 1 | 7.50 |
| CHEMBL204509 | — | — | 1 | 7.24 |
| CHEMBL206160 | — | — | 1 | 7.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL205659 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL206515 | — | IC50 | = | 0.81 | nM | 9.09 |
| CHEMBL383211 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL205759 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL426859 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL206559 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL436747 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL202685 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL196896 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL204284 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL382990 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL206482 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL205517 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL206740 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL380300 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL439517 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL383687 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL202723 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL381394 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL206191 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL203027 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL203466 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL383238 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL382832 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL206532 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL425236 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL204509 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL206160 | — | IC50 | = | 65.0 | nM | 7.19 |