Assay Detail
Binding
CHEMBL5140236
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against human P2X7R stably transfected in human 1321N1 cells incubated for 30 mins by Fura-2 AM staining based calcium influx assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | 1321N1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Therapeutic potentials and structure-activity relationship of 1,3-benzodioxole N-carbamothioyl carboxamide derivatives as selective and potent antagonists of P2X4 and P2X7 receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.43 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL497967 | — | — | 1 | 8.00 |
| CHEMBL2048438 | — | — | 1 | 7.89 |
| CHEMBL5178892 | — | — | 1 | 7.75 |
| CHEMBL5205239 | — | — | 1 | 7.47 |
| CHEMBL5174305 | — | — | 1 | 7.35 |
| CHEMBL5194724 | — | — | 1 | 6.96 |
| CHEMBL5186938 | — | — | 1 | 6.04 |
| CHEMBL5172890 | — | — | 1 | 5.90 |
| CHEMBL5184613 | — | — | 1 | 5.79 |
| CHEMBL5208562 | — | — | 1 | 5.72 |
| CHEMBL5200114 | — | — | 1 | 5.45 |
| CHEMBL5206892 | — | — | 1 | 4.88 |
| CHEMBL265502 | SURAMIN | 3.0 | 1 | 4.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL497967 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2048438 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5178892 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5205239 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5174305 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL5194724 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5186938 | — | IC50 | = | 902.0 | nM | 6.04 |
| CHEMBL5172890 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL5184613 | — | IC50 | = | 1642.0 | nM | 5.79 |
| CHEMBL5208562 | — | IC50 | = | 1886.0 | nM | 5.72 |
| CHEMBL5200114 | — | IC50 | = | 3563.0 | nM | 5.45 |
| CHEMBL5206892 | — | IC50 | = | 13105.0 | nM | 4.88 |
| CHEMBL265502 | SURAMIN | IC50 | = | 35190.0 | nM | 4.45 |