Assay Detail
Binding
CHEMBL829135
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Inhibition of 10 lM Cbz-Phe-Arg-AMC binding to human cathepsin K in fluorescence assay with 100 mM NaOAc
18
Total Activities
18
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
P2-P3 conformationally constrained ketoamide-based inhibitors of cathepsin K.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.30 | 7.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL191584 | — | — | 1 | 7.58 |
| CHEMBL188400 | — | — | 1 | 7.54 |
| CHEMBL190053 | — | — | 1 | 7.50 |
| CHEMBL234367 | — | — | 1 | 7.14 |
| CHEMBL365822 | — | — | 1 | 6.89 |
| CHEMBL186778 | — | — | 1 | 6.62 |
| CHEMBL191178 | — | — | 1 | 6.47 |
| CHEMBL188438 | — | — | 1 | 6.43 |
| CHEMBL363773 | — | — | 1 | 6.39 |
| CHEMBL426617 | — | — | 1 | 6.19 |
| CHEMBL189604 | — | — | 1 | 6.08 |
| CHEMBL188563 | — | — | 1 | 5.82 |
| CHEMBL189417 | — | — | 1 | 5.55 |
| CHEMBL186149 | — | — | 1 | 5.31 |
| CHEMBL365049 | — | — | 1 | 5.24 |
| CHEMBL187864 | — | — | 1 | 5.24 |
| CHEMBL188929 | — | — | 1 | 5.09 |
| CHEMBL191588 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL191584 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL188400 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL190053 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL234367 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL365822 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL186778 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL191178 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL188438 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL363773 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL426617 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL189604 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL188563 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL189417 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL186149 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL365049 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL187864 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL188929 | — | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL191588 | — | IC50 | = | 460000.0 | nM | - |