Assay Detail
Binding
CHEMBL4153246
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Antagonist activity at human P2X7 receptor in expressed in HEK293 cells assessed as inhibition of BzATP-induced EtBr uptake
8
Total Activities
8
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
Synthesis and structure-activity relationships of quinolinone and quinoline-based P2X7 receptor antagonists and their anti-sphere formation activities in glioblastoma cells.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.84 | 9.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4165149 | — | — | 1 | 9.96 |
| CHEMBL4171354 | — | — | 1 | 8.82 |
| CHEMBL1823817 | CE-224535 | 2.0 | 1 | 8.40 |
| CHEMBL2048438 | — | — | 1 | 7.89 |
| CHEMBL4173050 | — | — | 1 | 7.27 |
| CHEMBL4169645 | — | — | 1 | 7.07 |
| CHEMBL28324 | — | — | 1 | 6.80 |
| CHEMBL377219 | — | — | 1 | 6.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4165149 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL4171354 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL1823817 | CE-224535 | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2048438 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4173050 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4169645 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL28324 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL377219 | — | IC50 | = | 300.0 | nM | 6.52 |