Assay Detail
Binding
CHEMBL713837
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Inhibition of matrix metalloprotease-8
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Design and synthesis of a series of (2R)-N(4)-hydroxy-2-(3-hydroxybenzyl)-N(1)- [(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]butanediamide derivatives as potent, selective, and orally bioavailable aggrecanase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 6.78 | 9.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL419751 | — | — | 1 | 9.35 |
| CHEMBL45483 | — | — | 1 | 9.15 |
| CHEMBL114804 | — | — | 1 | 8.04 |
| CHEMBL325048 | — | — | 1 | 7.43 |
| CHEMBL420487 | — | — | 1 | 7.16 |
| CHEMBL24398 | — | — | 1 | 6.77 |
| CHEMBL115712 | — | — | 1 | 6.52 |
| CHEMBL114357 | — | — | 1 | 5.92 |
| CHEMBL8943 | — | — | 1 | 5.07 |
| CHEMBL323874 | — | — | 1 | 4.82 |
| CHEMBL115082 | — | — | 1 | 4.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL419751 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL45483 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL114804 | — | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL325048 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL420487 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL24398 | — | Ki | = | 171.0 | nM | 6.77 |
| CHEMBL115712 | — | Ki | = | 303.0 | nM | 6.52 |
| CHEMBL114357 | — | Ki | = | 1192.0 | nM | 5.92 |
| CHEMBL8943 | — | Ki | = | 8600.0 | nM | 5.07 |
| CHEMBL323874 | — | Ki | = | 15300.0 | nM | 4.82 |
| CHEMBL115082 | — | Ki | = | 40000.0 | nM | 4.40 |