Assay Detail
Binding
CHEMBL4223222
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Inhibition of human cathepsin K
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Peptidomimetic nitrile inhibitors of malarial protease falcipain-2 with high selectivity against human cathepsins.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.28 | 9.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4228926 | — | — | 1 | 9.96 |
| CHEMBL1215628 | — | — | 1 | 9.70 |
| CHEMBL4228143 | — | — | 1 | 9.00 |
| CHEMBL4227295 | — | — | 1 | 8.89 |
| CHEMBL4228861 | — | — | 1 | 6.70 |
| CHEMBL4226767 | — | — | 1 | 6.67 |
| CHEMBL4224829 | — | — | 1 | 6.36 |
| CHEMBL4228604 | — | — | 1 | 6.06 |
| CHEMBL4227965 | — | — | 1 | 5.73 |
| CHEMBL4225367 | — | — | 1 | 5.57 |
| CHEMBL4225099 | — | — | 1 | 5.42 |
| CHEMBL4228800 | — | — | 1 | - |
| CHEMBL4227619 | — | — | 1 | - |
| CHEMBL4227566 | — | — | 1 | - |
| CHEMBL4228399 | — | — | 1 | - |
| CHEMBL4228343 | — | — | 1 | - |
| CHEMBL4229174 | — | — | 1 | - |
| CHEMBL4228081 | — | — | 1 | - |
| CHEMBL4228920 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4228926 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL1215628 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4228143 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4227295 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4228861 | — | IC50 | = | 202.0 | nM | 6.70 |
| CHEMBL4226767 | — | IC50 | = | 213.0 | nM | 6.67 |
| CHEMBL4224829 | — | IC50 | = | 435.0 | nM | 6.36 |
| CHEMBL4228604 | — | IC50 | = | 867.0 | nM | 6.06 |
| CHEMBL4227965 | — | IC50 | = | 1870.0 | nM | 5.73 |
| CHEMBL4225367 | — | IC50 | = | 2690.0 | nM | 5.57 |
| CHEMBL4225099 | — | IC50 | = | 3828.0 | nM | 5.42 |
| CHEMBL4228800 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4227619 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4227566 | — | IC50 | - | — | - | |
| CHEMBL4228399 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4228343 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4229174 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4228081 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4228920 | — | IC50 | > | 5000.0 | nM | - |