Assay Detail
Binding
CHEMBL1023822
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Inhibition of humanized rabbit cathepsin K Tyr61Asp and Val157Leu mutant
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Identification of a nonbasic, nitrile-containing cathepsin K inhibitor (MK-1256) that is efficacious in a monkey model of osteoporosis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 9.20 | 9.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL201782 | — | — | 1 | 9.55 |
| CHEMBL492654 | — | — | 1 | 9.43 |
| CHEMBL523352 | — | — | 1 | 9.21 |
| CHEMBL495113 | — | — | 1 | 9.16 |
| CHEMBL523836 | — | — | 1 | 9.09 |
| CHEMBL492655 | — | — | 1 | 8.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL201782 | — | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL492654 | — | IC50 | = | 0.37 | nM | 9.43 |
| CHEMBL523352 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL495113 | — | IC50 | = | 0.69 | nM | 9.16 |
| CHEMBL523836 | — | IC50 | = | 0.81 | nM | 9.09 |
| CHEMBL492655 | — | IC50 | = | 1.8 | nM | 8.74 |