Assay Detail
Binding
CHEMBL4835176
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant MMP2 (AA34 to 660) assessed as cleavage of fluorescent substrate using 390 MMP FRET as substrate incubated for 30 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 |
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 | 5.86 | 6.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4877087 | — | — | 1 | 6.48 |
| CHEMBL4862188 | — | — | 1 | 6.20 |
| CHEMBL4650334 | ALDUMASTAT | 2.0 | 1 | 5.94 |
| CHEMBL4846457 | — | — | 1 | 5.55 |
| CHEMBL4876618 | — | — | 1 | 5.51 |
| CHEMBL4877662 | — | — | 1 | 5.47 |
| CHEMBL4854306 | — | — | 1 | - |
| CHEMBL4874226 | — | — | 1 | - |
| CHEMBL4863614 | — | — | 1 | - |
| CHEMBL4856883 | — | — | 1 | - |
| CHEMBL4876864 | — | — | 1 | - |
| CHEMBL4856943 | — | — | 1 | - |
| CHEMBL4868710 | — | — | 1 | - |
| CHEMBL4873384 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4877087 | — | IC50 | = | 328.0 | nM | 6.48 |
| CHEMBL4862188 | — | IC50 | = | 631.0 | nM | 6.20 |
| CHEMBL4650334 | ALDUMASTAT | IC50 | = | 1158.0 | nM | 5.94 |
| CHEMBL4846457 | — | IC50 | = | 2796.0 | nM | 5.55 |
| CHEMBL4876618 | — | IC50 | = | 3113.0 | nM | 5.51 |
| CHEMBL4877662 | — | IC50 | = | 3382.0 | nM | 5.47 |
| CHEMBL4854306 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL4874226 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4863614 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4856883 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL4876864 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL4856943 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL4868710 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL4873384 | — | IC50 | > | 20000.0 | nM | - |