Assay Detail
Binding
CHEMBL4427221
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Antagonist activity at human recombinant P2X7 receptor expressed in 1321N1 cells assessed as inhibition of BzATP-induced calcium mobilization incubated for 30 mins measured after 180 seconds by calcium-4 dye based FLIPR assay
11
Total Activities
11
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
The evolution of P2X7 antagonists with a focus on CNS indications.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 8.01 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4471289 | — | — | 1 | 8.62 |
| CHEMBL4442874 | — | — | 1 | 8.57 |
| CHEMBL4465051 | — | — | 1 | 8.35 |
| CHEMBL4546974 | — | — | 1 | 8.16 |
| CHEMBL4450832 | — | — | 1 | 8.07 |
| CHEMBL3674061 | — | — | 1 | 8.07 |
| CHEMBL4077415 | — | — | 1 | 8.06 |
| CHEMBL4567755 | — | — | 1 | 7.96 |
| CHEMBL3674077 | — | — | 1 | 7.96 |
| CHEMBL3674106 | — | — | 1 | 7.72 |
| CHEMBL3674060 | — | — | 1 | 6.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4471289 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4442874 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL4465051 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL4546974 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL4450832 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL3674061 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL4077415 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL4567755 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3674077 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3674106 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3674060 | — | IC50 | = | 240.0 | nM | 6.62 |