Assay Detail
Binding
CHEMBL872559
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Inhibition of matrix metalloprotease-2
10
Total Activities
10
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
Discovery of macrocyclic hydroxamic acids containing biphenylmethyl derivatives at P1', a series of selective TNF-alpha converting enzyme inhibitors with potent cellular activity in the inhibition of TNF-alpha release.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 7.38 | 9.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL432990 | — | — | 1 | 9.19 |
| CHEMBL91636 | — | — | 1 | 8.96 |
| CHEMBL325421 | — | — | 1 | 7.96 |
| CHEMBL324550 | — | — | 1 | 7.30 |
| CHEMBL323929 | — | — | 1 | 6.35 |
| CHEMBL431680 | — | — | 1 | 6.16 |
| CHEMBL115263 | — | — | 1 | 5.73 |
| CHEMBL324549 | — | — | 1 | - |
| CHEMBL325163 | — | — | 1 | - |
| CHEMBL114878 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL432990 | — | Ki | = | 0.64 | nM | 9.19 |
| CHEMBL91636 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL325421 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL324550 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL323929 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL431680 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL115263 | — | Ki | = | 1867.0 | nM | 5.73 |
| CHEMBL324549 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL325163 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL114878 | — | Ki | > | 2000.0 | nM | - |