Assay Detail
Binding
CHEMBL2345166
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant ADAMTS5 using bovine nasal cartilage aggrecan as substrate assessed as inhibition of 1772-AGEG neuropeptide formation incubated for 2 hrs prior to substrate addition measured after 2 hrs by Western blot analysis
6
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Nasal cartilage |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
A disintegrin and metalloproteinase with thrombospondin motifs 5 (CHEMBL2285) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Arylsulfonamide inhibitors of aggrecanases as potential therapeutic agents for osteoarthritis: synthesis and biological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 3 | 5.96 | 7.11 |
| Inhibition | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2337698 | — | — | 2 | 7.11 |
| CHEMBL198778 | — | — | 2 | 6.08 |
| CHEMBL2337691 | — | — | 2 | 4.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2337698 | — | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL198778 | — | Ki | = | 840.0 | nM | 6.08 |
| CHEMBL2337691 | — | Ki | = | 21000.0 | nM | 4.68 |
| CHEMBL2337698 | — | Inhibition | - | % | - | |
| CHEMBL198778 | — | Inhibition | - | % | - | |
| CHEMBL2337691 | — | Inhibition | - | % | - |