Assay Detail
Binding
CHEMBL4013271
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Inhibition of human MMP14 using Mca-PQGL-(3-[2, 4-dinitrophenyl]-L-2, 3-diaminopropionyl)-AR-OH as substrate after 2 to 4 hrs by fluorescence assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
A Highly Selective Hydantoin Inhibitor of Aggrecanase-1 and Aggrecanase-2 with a Low Projected Human Dose.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.39 | 6.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL187092 | — | — | 1 | 6.82 |
| CHEMBL4094455 | — | — | 1 | 5.80 |
| CHEMBL4102193 | — | — | 1 | 5.47 |
| CHEMBL4066965 | — | — | 1 | 5.41 |
| CHEMBL4072836 | — | — | 1 | 5.10 |
| CHEMBL3972836 | — | — | 1 | 4.82 |
| CHEMBL3980860 | — | — | 1 | 4.30 |
| CHEMBL3955404 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL187092 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4094455 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4102193 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL4066965 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL4072836 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL3972836 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL3980860 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL3955404 | — | IC50 | > | 100000.0 | nM | - |