Assay Detail
Binding
CHEMBL5134928
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Antagonist activity at human P2X2 receptor expressed in human 1321N1 cells assessed as reduction in intracellular Ca2+ influx incubated for 30 mins by Fura-2 AM based fluorescence assay
10
Total Activities
10
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
Design and synthesis of adamantane-1-carbonyl thiourea derivatives as potent and selective inhibitors of h-P2X4 and h-P2X7 receptors: An Emerging therapeutic tool for treatment of inflammation and neurological disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 5.60 | 6.13 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5200337 | — | — | 1 | 6.13 |
| CHEMBL5187239 | — | — | 1 | 6.05 |
| CHEMBL5174645 | — | — | 1 | 5.97 |
| CHEMBL1615626 | — | — | 1 | 5.85 |
| CHEMBL5183204 | — | — | 1 | 5.64 |
| CHEMBL5175938 | — | — | 1 | 5.34 |
| CHEMBL5172961 | — | — | 1 | 5.31 |
| CHEMBL5186040 | — | — | 1 | 5.28 |
| CHEMBL265502 | SURAMIN | 3.0 | 1 | 4.87 |
| CHEMBL1532400 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5200337 | — | IC50 | = | 732.0 | nM | 6.13 |
| CHEMBL5187239 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL5174645 | — | IC50 | = | 1061.0 | nM | 5.97 |
| CHEMBL1615626 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL5183204 | — | IC50 | = | 2306.0 | nM | 5.64 |
| CHEMBL5175938 | — | IC50 | = | 4576.0 | nM | 5.34 |
| CHEMBL5172961 | — | IC50 | = | 4852.0 | nM | 5.31 |
| CHEMBL5186040 | — | IC50 | = | 5242.0 | nM | 5.28 |
| CHEMBL265502 | SURAMIN | IC50 | = | 13450.0 | nM | 4.87 |
| CHEMBL1532400 | — | IC50 | - | — | - |