Assay Detail
Binding
CHEMBL4133151
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Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of ATP-induced ethidium iodide uptake preincubated for 10 mins followed by ATP addition measured after 20 mins by spectrofluorometric analysis
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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 | 9 | 6.61 | 8.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4162056 | — | — | 1 | 8.28 |
| CHEMBL255787 | — | — | 1 | 7.07 |
| CHEMBL4161422 | — | — | 1 | 6.97 |
| CHEMBL1823297 | — | — | 1 | 6.32 |
| CHEMBL4176461 | — | — | 1 | 6.28 |
| CHEMBL4173394 | BRILLIANT BLUE G | 4.0 | 1 | 6.26 |
| CHEMBL4166558 | — | — | 1 | 6.21 |
| CHEMBL4161877 | — | — | 1 | 6.05 |
| CHEMBL1823287 | — | — | 1 | 6.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4162056 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL255787 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL4161422 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL1823297 | — | IC50 | = | 478.0 | nM | 6.32 |
| CHEMBL4176461 | — | IC50 | = | 522.0 | nM | 6.28 |
| CHEMBL4173394 | BRILLIANT BLUE G | IC50 | = | 552.0 | nM | 6.26 |
| CHEMBL4166558 | — | IC50 | = | 621.0 | nM | 6.21 |
| CHEMBL4161877 | — | IC50 | = | 897.0 | nM | 6.05 |
| CHEMBL1823287 | — | IC50 | = | 932.0 | nM | 6.03 |