Assay Detail
Binding
CHEMBL3108480
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Antagonist activity at human P2X1 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced cytosolic calcium influx preincubated for 30 mins followed by ATP addition by Fluo-4 AM dye-based fluorescence assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | 1321-N1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Carbamazepine derivatives with P2X4 receptor-blocking activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 4.70 | 5.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3103375 | — | — | 1 | 5.34 |
| CHEMBL3103385 | — | — | 1 | 5.27 |
| CHEMBL3103371 | — | — | 1 | 4.68 |
| CHEMBL1483754 | — | — | 1 | 4.60 |
| CHEMBL3103372 | — | — | 1 | 4.16 |
| CHEMBL3103369 | — | — | 1 | 4.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3103375 | — | IC50 | = | 4550.0 | nM | 5.34 |
| CHEMBL3103385 | — | IC50 | = | 5320.0 | nM | 5.27 |
| CHEMBL3103371 | — | IC50 | = | 20700.0 | nM | 4.68 |
| CHEMBL1483754 | — | IC50 | = | 25200.0 | nM | 4.60 |
| CHEMBL3103372 | — | IC50 | = | 68800.0 | nM | 4.16 |
| CHEMBL3103369 | — | IC50 | = | 69600.0 | nM | 4.16 |