Assay Detail
Binding
CHEMBL4133148
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at P2X7 receptor in Swiss mouse peritoneal macrophages assessed as inhibition of ATP-induced propidium iodide uptake after 25 mins by flow cytometric analysis
16
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
1-Aryl-1H- and 2-aryl-2H-1,2,3-triazole derivatives blockade P2X7 receptor in vitro and inflammatory response in vivo.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Inhibition | 8 | - | - |
| IC50 | 8 | 6.70 | 7.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4162056 | — | — | 2 | 7.08 |
| CHEMBL4176461 | — | — | 2 | 7.02 |
| CHEMBL4161422 | — | — | 2 | 6.97 |
| CHEMBL1823297 | — | — | 2 | 6.78 |
| CHEMBL4166558 | — | — | 2 | 6.50 |
| CHEMBL4173394 | BRILLIANT BLUE G | 4.0 | 2 | 6.46 |
| CHEMBL4161877 | — | — | 2 | 6.46 |
| CHEMBL1823287 | — | — | 2 | 6.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4162056 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL4176461 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL4161422 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL1823297 | — | IC50 | = | 167.0 | nM | 6.78 |
| CHEMBL4166558 | — | IC50 | = | 317.0 | nM | 6.50 |
| CHEMBL4173394 | BRILLIANT BLUE G | IC50 | = | 343.0 | nM | 6.46 |
| CHEMBL4161877 | — | IC50 | = | 349.0 | nM | 6.46 |
| CHEMBL1823287 | — | IC50 | = | 488.0 | nM | 6.31 |
| CHEMBL4161422 | — | Inhibition | - | % | - | |
| CHEMBL4173394 | BRILLIANT BLUE G | Inhibition | - | % | - | |
| CHEMBL1823287 | — | Inhibition | - | % | - | |
| CHEMBL4176461 | — | Inhibition | - | % | - | |
| CHEMBL1823297 | — | Inhibition | - | % | - | |
| CHEMBL4161877 | — | Inhibition | - | % | - | |
| CHEMBL4162056 | — | Inhibition | - | % | - | |
| CHEMBL4166558 | — | Inhibition | - | % | - |