Assay Detail
Binding
CHEMBL4835175
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant ADAMTS-4 (AA1 to 520) assessed as cleavage of fluorescent substrate using as TBIS-1 substrate incubated for 180 mins by biochemical assay
14
Total Activities
14
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 4 (CHEMBL2318) ↗| 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 | 14 | 6.92 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4868710 | — | — | 1 | 7.92 |
| CHEMBL4856943 | — | — | 1 | 7.82 |
| CHEMBL4874034 | — | — | 1 | 7.75 |
| CHEMBL4877087 | — | — | 1 | 7.60 |
| CHEMBL4846457 | — | — | 1 | 7.52 |
| CHEMBL4877662 | — | — | 1 | 7.27 |
| CHEMBL4650334 | ALDUMASTAT | 2.0 | 1 | 6.81 |
| CHEMBL4876618 | — | — | 1 | 6.43 |
| CHEMBL4854306 | — | — | 1 | 6.37 |
| CHEMBL4873384 | — | — | 1 | 6.35 |
| CHEMBL4876864 | — | — | 1 | 6.32 |
| CHEMBL4856883 | — | — | 1 | 6.30 |
| CHEMBL4859812 | — | — | 1 | 6.20 |
| CHEMBL4850670 | — | — | 1 | 6.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4868710 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4856943 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4874034 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4877087 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4846457 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4877662 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4650334 | ALDUMASTAT | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL4876618 | — | IC50 | = | 368.0 | nM | 6.43 |
| CHEMBL4854306 | — | IC50 | = | 428.0 | nM | 6.37 |
| CHEMBL4873384 | — | IC50 | = | 448.0 | nM | 6.35 |
| CHEMBL4876864 | — | IC50 | = | 478.0 | nM | 6.32 |
| CHEMBL4856883 | — | IC50 | = | 506.0 | nM | 6.30 |
| CHEMBL4859812 | — | IC50 | = | 635.0 | nM | 6.20 |
| CHEMBL4850670 | — | IC50 | = | 715.0 | nM | 6.15 |