Assay Detail
Binding
CHEMBL718689
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of matrix metalloprotease-1
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 | 5.44 | 7.97 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL419751 | — | — | 1 | 7.97 |
| CHEMBL325048 | — | — | 1 | 7.09 |
| CHEMBL420487 | — | — | 1 | 6.02 |
| CHEMBL115712 | — | — | 1 | 5.96 |
| CHEMBL114804 | — | — | 1 | 5.93 |
| CHEMBL8943 | — | — | 1 | 4.51 |
| CHEMBL24398 | — | — | 1 | 4.48 |
| CHEMBL115082 | — | — | 1 | 4.30 |
| CHEMBL323874 | — | — | 1 | 4.12 |
| CHEMBL114357 | — | — | 1 | 4.02 |
| CHEMBL45483 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL419751 | — | Ki | = | 10.7 | nM | 7.97 |
| CHEMBL325048 | — | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL420487 | — | Ki | = | 946.0 | nM | 6.02 |
| CHEMBL115712 | — | Ki | = | 1087.0 | nM | 5.96 |
| CHEMBL114804 | — | Ki | = | 1163.0 | nM | 5.93 |
| CHEMBL8943 | — | Ki | = | 30953.0 | nM | 4.51 |
| CHEMBL24398 | — | Ki | = | 33160.0 | nM | 4.48 |
| CHEMBL115082 | — | Ki | = | 50000.0 | nM | 4.30 |
| CHEMBL323874 | — | Ki | = | 75000.0 | nM | 4.12 |
| CHEMBL114357 | — | Ki | = | 95500.0 | nM | 4.02 |
| CHEMBL45483 | — | Ki | < | 1.0 | nM | - |