Assay Detail
Binding
CHEMBL829134
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Inhibition of 10 lM Cbz-Phe-Arg-AMC binding to human cathepsin B activity in fluorescence assay with 100 mM NaOAc
17
Total Activities
17
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 | 17 | 4.71 | 5.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL365822 | — | — | 1 | 5.28 |
| CHEMBL426617 | — | — | 1 | 5.21 |
| CHEMBL188438 | — | — | 1 | 5.01 |
| CHEMBL190053 | — | — | 1 | 5.00 |
| CHEMBL186778 | — | — | 1 | 4.92 |
| CHEMBL189417 | — | — | 1 | 4.75 |
| CHEMBL234367 | — | — | 1 | 4.70 |
| CHEMBL191584 | — | — | 1 | 4.57 |
| CHEMBL189604 | — | — | 1 | 4.51 |
| CHEMBL363773 | — | — | 1 | 4.50 |
| CHEMBL188400 | — | — | 1 | 4.35 |
| CHEMBL188563 | — | — | 1 | 4.25 |
| CHEMBL191178 | — | — | 1 | 4.22 |
| CHEMBL186149 | — | — | 1 | - |
| CHEMBL188929 | — | — | 1 | - |
| CHEMBL187864 | — | — | 1 | - |
| CHEMBL365049 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL365822 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL426617 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL188438 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL190053 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL186778 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL189417 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL234367 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL191584 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL189604 | — | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL363773 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL188400 | — | IC50 | = | 45000.0 | nM | 4.35 |
| CHEMBL188563 | — | IC50 | = | 56000.0 | nM | 4.25 |
| CHEMBL191178 | — | IC50 | = | 60000.0 | nM | 4.22 |
| CHEMBL186149 | — | IC50 | = | 3500000.0 | nM | - |
| CHEMBL188929 | — | IC50 | = | 107000.0 | nM | - |
| CHEMBL187864 | — | IC50 | = | 870000.0 | nM | - |
| CHEMBL365049 | — | IC50 | = | 870000.0 | nM | - |