Assay Detail
Binding
CHEMBL5134929
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human P2X4 receptor expressed in human 1321N1 cells assessed as reduction in intracellular Ca2+ influx incubated for 30 mins by Fura-2 AM based fluorescence assay
12
Total Activities
12
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 | 12 | 5.57 | 5.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5174595 | — | — | 1 | 5.96 |
| CHEMBL5174645 | — | — | 1 | 5.89 |
| CHEMBL5175938 | — | — | 1 | 5.89 |
| CHEMBL5188202 | — | — | 1 | 5.89 |
| CHEMBL5172961 | — | — | 1 | 5.81 |
| CHEMBL5200337 | — | — | 1 | 5.46 |
| CHEMBL5184546 | — | — | 1 | 5.38 |
| CHEMBL5206955 | — | — | 1 | 5.34 |
| CHEMBL1615626 | — | — | 1 | 5.28 |
| CHEMBL265502 | SURAMIN | 3.0 | 1 | 5.25 |
| CHEMBL5181561 | — | — | 1 | 5.08 |
| CHEMBL5187239 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5174595 | — | IC50 | = | 1084.0 | nM | 5.96 |
| CHEMBL5174645 | — | IC50 | = | 1282.0 | nM | 5.89 |
| CHEMBL5175938 | — | IC50 | = | 1290.0 | nM | 5.89 |
| CHEMBL5188202 | — | IC50 | = | 1274.0 | nM | 5.89 |
| CHEMBL5172961 | — | IC50 | = | 1562.0 | nM | 5.81 |
| CHEMBL5200337 | — | IC50 | = | 3461.0 | nM | 5.46 |
| CHEMBL5184546 | — | IC50 | = | 4187.0 | nM | 5.38 |
| CHEMBL5206955 | — | IC50 | = | 4530.0 | nM | 5.34 |
| CHEMBL1615626 | — | IC50 | = | 5250.0 | nM | 5.28 |
| CHEMBL265502 | SURAMIN | IC50 | = | 5640.0 | nM | 5.25 |
| CHEMBL5181561 | — | IC50 | = | 8339.0 | nM | 5.08 |
| CHEMBL5187239 | — | IC50 | - | — | - |