Assay Detail
Binding
CHEMBL827846
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Inhibitory concentration against aggrecanase from porcine chondrocytes using [35S]-sulfate (5 mCi/ml) as radioligand and adding IL-1alpha (5 ng/ml) incubated for 10h
20
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Sus scrofa |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery of 3-OH-3-methylpipecolic hydroxamates: potent orally active inhibitors of aggrecanase and MMP-13.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 7.49 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL187092 | — | — | 1 | 8.82 |
| CHEMBL183474 | — | — | 1 | 8.43 |
| CHEMBL365283 | — | — | 1 | 8.33 |
| CHEMBL186663 | — | — | 1 | 8.16 |
| CHEMBL360854 | — | — | 1 | 8.10 |
| CHEMBL363126 | — | — | 1 | 7.96 |
| CHEMBL182306 | — | — | 1 | 7.85 |
| CHEMBL187474 | — | — | 1 | 7.82 |
| CHEMBL186500 | — | — | 1 | 7.82 |
| CHEMBL436277 | — | — | 1 | 7.77 |
| CHEMBL446697 | — | — | 1 | 7.72 |
| CHEMBL186743 | — | — | 1 | 7.29 |
| CHEMBL187245 | — | — | 1 | 7.11 |
| CHEMBL369115 | — | — | 1 | 7.07 |
| CHEMBL183995 | — | — | 2 | 6.92 |
| CHEMBL435102 | — | — | 1 | 6.31 |
| CHEMBL365658 | — | — | 1 | 6.30 |
| CHEMBL364643 | — | — | 1 | 5.70 |
| CHEMBL185168 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL187092 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL183474 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL365283 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL186663 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL360854 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL363126 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL182306 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL187474 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL186500 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL436277 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL446697 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL186743 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL187245 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL369115 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL183995 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL183995 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL435102 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL365658 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL364643 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL185168 | — | IC50 | > | 1000.0 | nM | - |