Assay Detail
Binding
CHEMBL642936
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Inhibition of bovine aggrecanase
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Potent and selective aggrecanase inhibitors containing cyclic P1 substituents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.67 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL24595 | — | — | 1 | 8.52 |
| CHEMBL24810 | — | — | 1 | 8.52 |
| CHEMBL283690 | — | — | 1 | 8.15 |
| CHEMBL281196 | — | — | 1 | 8.15 |
| CHEMBL24398 | — | — | 1 | 7.92 |
| CHEMBL283222 | — | — | 1 | 7.72 |
| CHEMBL24763 | — | — | 1 | 7.55 |
| CHEMBL26058 | — | — | 1 | 7.54 |
| CHEMBL26165 | — | — | 1 | 7.35 |
| CHEMBL26388 | — | — | 1 | 7.01 |
| CHEMBL281523 | — | — | 1 | 6.94 |
| CHEMBL24054 | — | — | 1 | 6.68 |
| CHEMBL26278 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL24595 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL24810 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL283690 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL281196 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL24398 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL283222 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL24763 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL26058 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL26165 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL26388 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL281523 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL24054 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL26278 | — | IC50 | > | 1000.0 | nM | - |