Assay Detail
Binding
CHEMBL3388952
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ADAMTS-5 using VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG peptide substrate by AlphaScreen assay in presence of 50% rat plasma
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Plasma |
| 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
Identification of potent and selective hydantoin inhibitors of aggrecanase-1 and aggrecanase-2 that are efficacious in both chemical and surgical models of osteoarthritis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.55 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL187092 | — | — | 1 | 7.75 |
| CHEMBL3358158 | — | — | 1 | 7.46 |
| CHEMBL3358156 | — | — | 1 | 6.96 |
| CHEMBL3358155 | — | — | 1 | 6.48 |
| CHEMBL3358153 | — | — | 1 | 6.38 |
| CHEMBL3358157 | — | — | 1 | 6.28 |
| CHEMBL3358151 | — | — | 1 | 6.21 |
| CHEMBL3358154 | — | — | 1 | 5.77 |
| CHEMBL3358152 | — | — | 1 | 5.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL187092 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3358158 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3358156 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3358155 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL3358153 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL3358157 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL3358151 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL3358154 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3358152 | — | IC50 | = | 2400.0 | nM | 5.62 |