Assay Detail
Binding
CHEMBL992195
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Inhibition of humanized rabbit cathepsin K
27
Total Activities
25
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
Investigation of ketone warheads as alternatives to the nitrile for preparation of potent and selective cathepsin K inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 8.12 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL474438 | — | — | 1 | 9.80 |
| CHEMBL481611 | ODANACATIB | 3.0 | 1 | 9.70 |
| CHEMBL443434 | — | — | 1 | 8.80 |
| CHEMBL503774 | — | — | 3 | 8.74 |
| CHEMBL448605 | — | — | 1 | 8.59 |
| CHEMBL449314 | — | — | 1 | 8.54 |
| CHEMBL452219 | — | — | 1 | 8.41 |
| CHEMBL481743 | — | — | 1 | 8.38 |
| CHEMBL480922 | — | — | 1 | 8.37 |
| CHEMBL446544 | — | — | 1 | 8.24 |
| CHEMBL500567 | — | — | 1 | 8.16 |
| CHEMBL481744 | — | — | 1 | 8.14 |
| CHEMBL501877 | — | — | 1 | 8.14 |
| CHEMBL500545 | — | — | 1 | 8.08 |
| CHEMBL499380 | — | — | 1 | 8.05 |
| CHEMBL481814 | — | — | 1 | 8.01 |
| CHEMBL499527 | — | — | 1 | 7.82 |
| CHEMBL443209 | — | — | 1 | 7.80 |
| CHEMBL515238 | — | — | 1 | 7.57 |
| CHEMBL472831 | — | — | 1 | 7.48 |
| CHEMBL475434 | — | — | 1 | 7.35 |
| CHEMBL499218 | — | — | 1 | 7.27 |
| CHEMBL443960 | — | — | 1 | 7.17 |
| CHEMBL454826 | — | — | 1 | 7.07 |
| CHEMBL448681 | — | — | 1 | 6.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL474438 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL481611 | ODANACATIB | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL443434 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL503774 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL503774 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL448605 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL449314 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL452219 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL481743 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL480922 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL446544 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL500567 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL481744 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL501877 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL500545 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL499380 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL481814 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL503774 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL499527 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL443209 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL515238 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL472831 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL475434 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL499218 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL443960 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL454826 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL448681 | — | IC50 | = | 159.0 | nM | 6.80 |