Assay Detail
Binding
CHEMBL4133149
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 current at holding potential of -60 mV preincubated for 5 mins followed by ATP addition measured after 5 mins by Whole cell patch-clamp analysis
8
Total Activities
8
Compounds Tested
1
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 |
|---|---|---|---|
| IC50 | 8 | 6.81 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4162056 | — | — | 1 | 7.16 |
| CHEMBL4176461 | — | — | 1 | 7.09 |
| CHEMBL4161422 | — | — | 1 | 6.99 |
| CHEMBL1823297 | — | — | 1 | 6.99 |
| CHEMBL4173394 | BRILLIANT BLUE G | 4.0 | 1 | 6.96 |
| CHEMBL4166558 | — | — | 1 | 6.50 |
| CHEMBL1823287 | — | — | 1 | 6.47 |
| CHEMBL4161877 | — | — | 1 | 6.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4162056 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL4176461 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL4161422 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL1823297 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL4173394 | BRILLIANT BLUE G | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL4166558 | — | IC50 | = | 316.0 | nM | 6.50 |
| CHEMBL1823287 | — | IC50 | = | 341.0 | nM | 6.47 |
| CHEMBL4161877 | — | IC50 | = | 457.0 | nM | 6.34 |