Assay Detail
Binding
CHEMBL4835207
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant ADAMTS-5 assessed as cleavage of fluorescent substrate using FAM-TBIS-1 in presence of 2% HSA by biochemical assay
3
Total Activities
3
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 |
Target
A disintegrin and metalloproteinase with thrombospondin motifs 5 (CHEMBL2285) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of GLPG1972/S201086, a Potent, Selective, and Orally Bioavailable ADAMTS-5 Inhibitor for the Treatment of Osteoarthritis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 6.56 | 6.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4864100 | — | — | 1 | 6.92 |
| CHEMBL4877087 | — | — | 1 | 6.86 |
| CHEMBL4878543 | — | — | 1 | 5.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4864100 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4877087 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL4878543 | — | IC50 | = | 1224.0 | nM | 5.91 |