Assay Detail
Binding
CHEMBL715008
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In vitro inhibitory activity against the catalytic domain of the human matrix metalloprotease-2
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Structure-based design and synthesis of potent matrix metalloproteinase inhibitors derived from a 6H-1,3,4-thiadiazine scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 6.47 | 7.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL109806 | — | — | 1 | 7.10 |
| CHEMBL111179 | — | — | 1 | 7.05 |
| CHEMBL111257 | — | — | 1 | 6.85 |
| CHEMBL110970 | — | — | 1 | 6.82 |
| CHEMBL111450 | — | — | 1 | 6.68 |
| CHEMBL422250 | — | — | 1 | 6.62 |
| CHEMBL110750 | — | — | 1 | 6.57 |
| CHEMBL321213 | — | — | 1 | 6.52 |
| CHEMBL322795 | — | — | 1 | 6.47 |
| CHEMBL109655 | — | — | 1 | 6.39 |
| CHEMBL109214 | — | — | 1 | 6.36 |
| CHEMBL109579 | — | — | 1 | 6.35 |
| CHEMBL109353 | — | — | 1 | 6.30 |
| CHEMBL419750 | — | — | 1 | 6.28 |
| CHEMBL109861 | — | — | 1 | 6.26 |
| CHEMBL422251 | — | — | 1 | 6.07 |
| CHEMBL109603 | — | — | 1 | 6.06 |
| CHEMBL111678 | — | — | 1 | 5.73 |
| CHEMBL108494 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL109806 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL111179 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL111257 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL110970 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL111450 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL422250 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL110750 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL321213 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL322795 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL109655 | — | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL109214 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL109579 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL109353 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL419750 | — | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL109861 | — | Ki | = | 550.0 | nM | 6.26 |
| CHEMBL422251 | — | Ki | = | 850.0 | nM | 6.07 |
| CHEMBL109603 | — | Ki | = | 880.0 | nM | 6.06 |
| CHEMBL111678 | — | Ki | = | 1870.0 | nM | 5.73 |
| CHEMBL108494 | — | Ki | > | 15000.0 | nM | - |