Assay Detail
Binding
CHEMBL4835173
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of rat recombinant ADAMTS-5 assessed as cleavage of fluorescent substrate using FAM-TBIS-1 by biochemical assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
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 | 4 | 7.35 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4874034 | — | — | 1 | 8.30 |
| CHEMBL4650334 | ALDUMASTAT | 2.0 | 1 | 7.64 |
| CHEMBL4859812 | — | — | 1 | 7.51 |
| CHEMBL4850670 | — | — | 1 | 5.93 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4874034 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4650334 | ALDUMASTAT | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4859812 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4850670 | — | IC50 | = | 1167.0 | nM | 5.93 |