Assay Detail
Binding
CHEMBL4153217
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human P2X3 receptor expressed in 1321N1 cells assessed as inhibition of ATP-induced calcium flux measured for 30 secs at 0.4 secs intervals by Flou-4-AM dye based fluorescence assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 | 5.71 | 5.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4160315 | — | — | 1 | 5.80 |
| CHEMBL103 | PROGESTERONE | 4.0 | 1 | 5.80 |
| CHEMBL4159276 | — | — | 1 | 5.52 |
| CHEMBL1672104 | — | — | 1 | - |
| CHEMBL265502 | SURAMIN | 3.0 | 1 | - |
| CHEMBL4175875 | — | — | 1 | - |
| CHEMBL2180179 | — | — | 1 | - |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4160315 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL103 | PROGESTERONE | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4159276 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL1672104 | — | IC50 | - | — | - | |
| CHEMBL265502 | SURAMIN | IC50 | - | — | - | |
| CHEMBL4175875 | — | IC50 | - | — | - | |
| CHEMBL2180179 | — | IC50 | - | — | - | |
| CHEMBL1355736 | THEOPHYLLINE | IC50 | - | — | - |