Assay Detail
Binding
CHEMBL3887660
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Shift AlphaScreen Assay : The AlphaScreen Assay is modified to include the testing of inhibitors against ADAMTS-5 in the presence of 50% Lewis rat plasma in order to determine the effects of plasma protein binding on inhibitor potency. The ratio between the IC50 of the inhibitor against ADAMTS-5 in 50% Lewis rat plasma versus the IC50 of the inhibitor in buffer is calculated and is described as the plasma shift of the inhibitor. The assay is completed in the same manner using 10 nM ADAMTS-5 instead of 2.1 nM. A similar assay is used with dog ADAMTS-4 in the presence of 25% dog plasma.
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Plasma |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
A disintegrin-like and metallopeptidase (Reprolysin type) with thrombospondin type 1 motif, 5 (Aggrecanase-2) (CHEMBL3988600) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Aggrecanase inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.46 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4066965 | — | — | 1 | 7.82 |
| CHEMBL3980860 | — | — | 1 | 7.75 |
| CHEMBL4072836 | — | — | 1 | 7.70 |
| CHEMBL3972836 | — | — | 1 | 7.19 |
| CHEMBL3955404 | — | — | 1 | 6.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4066965 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3980860 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4072836 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3972836 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL3955404 | — | IC50 | = | 146.0 | nM | 6.84 |