Assay Detail
Functional
CHEMBL2184470
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Antagonist activity at rat P2X4 receptor by cell-based calcium influx assay
11
Total Activities
11
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
N-substituted phenoxazine and acridone derivatives: structure-activity relationships of potent P2X4 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 5.54 | 6.03 |
| EC50 | 2 | 5.50 | 6.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2180160 | — | — | 1 | 6.03 |
| CHEMBL14249 | ADENOSINE TRIPHOSPHATE | 2.0 | 1 | 6.00 |
| CHEMBL2180137 | — | — | 1 | 5.68 |
| CHEMBL490 | PAROXETINE | 4.0 | 1 | 5.61 |
| CHEMBL2180149 | — | — | 1 | 5.39 |
| CHEMBL1163419 | TNP-ATP | — | 1 | 5.33 |
| CHEMBL2180136 | — | — | 1 | 5.22 |
| CHEMBL336208 | — | — | 1 | 5.00 |
| CHEMBL2180138 | — | — | 1 | - |
| CHEMBL2180174 | — | — | 1 | - |
| CHEMBL2180171 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2180160 | — | IC50 | = | 928.0 | nM | 6.03 |
| CHEMBL14249 | ADENOSINE TRIPHOSPHATE | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2180137 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL490 | PAROXETINE | IC50 | = | 2450.0 | nM | 5.61 |
| CHEMBL2180149 | — | IC50 | = | 4040.0 | nM | 5.39 |
| CHEMBL1163419 | TNP-ATP | IC50 | = | 4710.0 | nM | 5.33 |
| CHEMBL2180136 | — | IC50 | = | 6080.0 | nM | 5.22 |
| CHEMBL336208 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL2180138 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180174 | — | IC50 | >= | 10000.0 | nM | - |
| CHEMBL2180171 | — | IC50 | >= | 10000.0 | nM | - |