Assay Detail
Binding
CHEMBL4133156
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Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of ATP-induced IL-1beta release preincubated for 30 mins followed by ATP addition measured after 30 mins by ELISA
2
Total Activities
2
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 | 2 | 7.13 | 7.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4162056 | — | — | 1 | 7.17 |
| CHEMBL255787 | — | — | 1 | 7.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4162056 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL255787 | — | IC50 | = | 82.0 | nM | 7.09 |