Assay Detail
Binding
CHEMBL3388950
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ADAMTS-4 using VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG peptide substrate by AlphaScreen assay
9
Total Activities
9
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
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 | 7.92 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL187092 | — | — | 1 | 9.00 |
| CHEMBL3358158 | — | — | 1 | 8.40 |
| CHEMBL3358156 | — | — | 1 | 8.30 |
| CHEMBL3358155 | — | — | 1 | 8.10 |
| CHEMBL3358153 | — | — | 1 | 7.92 |
| CHEMBL3358154 | — | — | 1 | 7.77 |
| CHEMBL3358157 | — | — | 1 | 7.66 |
| CHEMBL3358151 | — | — | 1 | 7.13 |
| CHEMBL3358152 | — | — | 1 | 6.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL187092 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3358158 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3358156 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3358155 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3358153 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3358154 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3358157 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3358151 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL3358152 | — | IC50 | = | 110.0 | nM | 6.96 |