Assay Detail
Binding
CHEMBL710802
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Inhibition of human matrix metalloprotease-9
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 | 5.91 | 8.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL419751 | — | — | 1 | 8.49 |
| CHEMBL325048 | — | — | 1 | 6.79 |
| CHEMBL420487 | — | — | 1 | 6.78 |
| CHEMBL114804 | — | — | 1 | 6.69 |
| CHEMBL8943 | — | — | 1 | 5.48 |
| CHEMBL115712 | — | — | 1 | 5.38 |
| CHEMBL24398 | — | — | 1 | 5.35 |
| CHEMBL114357 | — | — | 1 | 4.81 |
| CHEMBL323874 | — | — | 1 | 4.67 |
| CHEMBL115082 | — | — | 1 | 4.66 |
| CHEMBL45483 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL419751 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL325048 | — | Ki | = | 162.0 | nM | 6.79 |
| CHEMBL420487 | — | Ki | = | 166.0 | nM | 6.78 |
| CHEMBL114804 | — | Ki | = | 203.0 | nM | 6.69 |
| CHEMBL8943 | — | Ki | = | 3324.0 | nM | 5.48 |
| CHEMBL115712 | — | Ki | = | 4200.0 | nM | 5.38 |
| CHEMBL24398 | — | Ki | = | 4468.0 | nM | 5.35 |
| CHEMBL114357 | — | Ki | = | 15500.0 | nM | 4.81 |
| CHEMBL323874 | — | Ki | = | 21200.0 | nM | 4.67 |
| CHEMBL115082 | — | Ki | = | 22000.0 | nM | 4.66 |
| CHEMBL45483 | — | Ki | < | 1.0 | nM | - |