Assay Detail
Binding
CHEMBL3388955
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Inhibition of human MMP13 using Mca-PQG1 peptide substrate assessed as substrate cleavage after 2 to 4 hrs
9
Total Activities
9
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
Identification of potent and selective hydantoin inhibitors of aggrecanase-1 and aggrecanase-2 that are efficacious in both chemical and surgical models of osteoarthritis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 5.88 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL187092 | — | — | 1 | 9.00 |
| CHEMBL3358153 | — | — | 1 | 6.14 |
| CHEMBL3358155 | — | — | 1 | 6.03 |
| CHEMBL3358154 | — | — | 1 | 5.51 |
| CHEMBL3358156 | — | — | 1 | 5.38 |
| CHEMBL3358157 | — | — | 1 | 5.33 |
| CHEMBL3358151 | — | — | 1 | 5.16 |
| CHEMBL3358158 | — | — | 1 | 4.52 |
| CHEMBL3358152 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL187092 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3358153 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL3358155 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL3358154 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL3358156 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL3358157 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL3358151 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL3358158 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL3358152 | — | IC50 | - | — | - |