Assay Detail
Binding
CHEMBL4615161
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Antagonist activity at human P2X4 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
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and Structure Relationships of Salicylanilide Derivatives as Potent, Non-acidic P2X1 Receptor Antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.64 | 7.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4640175 | — | — | 1 | 7.37 |
| CHEMBL2338695 | — | — | 1 | 7.31 |
| CHEMBL2088011 | — | — | 1 | 6.87 |
| CHEMBL536151 | IMD-0354 | 1.0 | 1 | 6.81 |
| CHEMBL461542 | — | — | 1 | 6.81 |
| CHEMBL2179174 | — | — | 1 | 6.81 |
| CHEMBL2338696 | — | — | 1 | 6.68 |
| CHEMBL589733 | — | — | 1 | 6.27 |
| CHEMBL2179173 | — | — | 1 | 6.15 |
| CHEMBL2338686 | — | — | 1 | 6.14 |
| CHEMBL2088014 | — | — | 1 | 5.82 |
| CHEMBL4644398 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4640175 | — | IC50 | = | 42.6 | nM | 7.37 |
| CHEMBL2338695 | — | IC50 | = | 48.8 | nM | 7.31 |
| CHEMBL2088011 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL536151 | IMD-0354 | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL461542 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL2179174 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL2338696 | — | IC50 | = | 209.0 | nM | 6.68 |
| CHEMBL589733 | — | IC50 | = | 537.0 | nM | 6.27 |
| CHEMBL2179173 | — | IC50 | = | 712.0 | nM | 6.15 |
| CHEMBL2338686 | — | IC50 | = | 729.0 | nM | 6.14 |
| CHEMBL2088014 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4644398 | — | IC50 | >= | 10000.0 | nM | - |