Assay Detail
Binding
CHEMBL4425558
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ADAMTS5 using 43-mer-VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG as substrate in presence of Lewis rat plasma measured after 3 hrs by AlphaScreen assay
8
Total Activities
8
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
Use of Osmotic Pumps to Establish the Pharmacokinetic-Pharmacodynamic Relationship and Define Desirable Human Performance Characteristics for Aggrecanase Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.05 | 7.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3358158 | — | — | 1 | 7.46 |
| CHEMBL4436740 | — | — | 1 | 7.20 |
| CHEMBL4097165 | — | — | 1 | 7.20 |
| CHEMBL4450729 | — | — | 1 | 7.17 |
| CHEMBL3358156 | — | — | 1 | 7.10 |
| CHEMBL4587825 | — | — | 1 | 6.96 |
| CHEMBL4589438 | — | — | 1 | 6.85 |
| CHEMBL3358155 | — | — | 1 | 6.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3358158 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4436740 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL4097165 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL4450729 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL3358156 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4587825 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4589438 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3358155 | — | IC50 | = | 330.0 | nM | 6.48 |