Assay Detail
Binding
CHEMBL4835178
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant TACE (AA34 to 660) assessed as cleavage of fluorescent substrate using 5FAM-LAQAVRSSSRK-5TAMRA as substrate 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
Disintegrin and metalloproteinase domain-containing protein 17 (CHEMBL3706) ↗| 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 | 6.20 | 6.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4863614 | — | — | 1 | 6.77 |
| CHEMBL4856943 | — | — | 1 | 6.77 |
| CHEMBL4862188 | — | — | 1 | 6.62 |
| CHEMBL4846457 | — | — | 1 | 6.62 |
| CHEMBL4876618 | — | — | 1 | 6.43 |
| CHEMBL4868710 | — | — | 1 | 6.43 |
| CHEMBL4854306 | — | — | 1 | 6.19 |
| CHEMBL4856883 | — | — | 1 | 5.89 |
| CHEMBL4877662 | — | — | 1 | 5.89 |
| CHEMBL4873384 | — | — | 1 | 5.63 |
| CHEMBL4874226 | — | — | 1 | 5.57 |
| CHEMBL4876864 | — | — | 1 | 5.57 |
| CHEMBL4877087 | — | — | 1 | - |
| CHEMBL4650334 | ALDUMASTAT | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4863614 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4856943 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4862188 | — | IC50 | = | 242.0 | nM | 6.62 |
| CHEMBL4846457 | — | IC50 | = | 242.0 | nM | 6.62 |
| CHEMBL4876618 | — | IC50 | = | 368.0 | nM | 6.43 |
| CHEMBL4868710 | — | IC50 | = | 368.0 | nM | 6.43 |
| CHEMBL4854306 | — | IC50 | = | 651.0 | nM | 6.19 |
| CHEMBL4856883 | — | IC50 | = | 1275.0 | nM | 5.89 |
| CHEMBL4877662 | — | IC50 | = | 1275.0 | nM | 5.89 |
| CHEMBL4873384 | — | IC50 | = | 2316.0 | nM | 5.63 |
| CHEMBL4874226 | — | IC50 | = | 2709.0 | nM | 5.57 |
| CHEMBL4876864 | — | IC50 | = | 2709.0 | nM | 5.57 |
| CHEMBL4877087 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL4650334 | ALDUMASTAT | IC50 | > | 20000.0 | nM | - |