Assay Detail
Binding
CHEMBL2345601
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant MMP14 catalytic domain using Mca-Lys-Pro- Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 as substrate incubated for 2 hrs prior to substrate addition measured every 15 secs for 15 mins by fluorometric analysis
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
Arylsulfonamide inhibitors of aggrecanases as potential therapeutic agents for osteoarthritis: synthesis and biological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.18 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL198778 | — | — | 1 | 8.40 |
| CHEMBL19611 | ILOMASTAT | 2.0 | 1 | 8.33 |
| CHEMBL2337697 | — | — | 1 | 7.62 |
| CHEMBL197842 | — | — | 1 | 7.15 |
| CHEMBL2337690 | — | — | 1 | 7.09 |
| CHEMBL2337696 | — | — | 1 | 6.87 |
| CHEMBL2337691 | — | — | 1 | 6.51 |
| CHEMBL2337698 | — | — | 1 | 5.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL198778 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL19611 | ILOMASTAT | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL2337697 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL197842 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL2337690 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL2337696 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL2337691 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL2337698 | — | IC50 | = | 3700.0 | nM | 5.43 |