Assay Detail
Binding
CHEMBL4133154
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at P2X7 receptor in LPS/IFNc-differentiated human THP-1 cells assessed as inhibition of ATP-induced IL-1beta release preincubated for 30 mins followed by LPS stimulation for 4 hrs using cells treated with ATP for 30 mins by ELISA
3
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | THP-1 |
| 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 | 7.11 | 7.17 |
| Activity | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4162056 | — | — | 2 | 7.17 |
| CHEMBL255787 | — | — | 1 | 7.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4162056 | — | IC50 | = | 67.46 | nM | 7.17 |
| CHEMBL255787 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL4162056 | — | Activity | - | — | - |