Assay Detail
Functional
CHEMBL2184479
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human P2X4 receptor expressed in 1321N1 cells assessed as inhibition of ATP-induced cytosolic calcium influx compound preincubated for 30 mins before ATP treatment by Fluo-4 AM fluorescence method
58
Total Activities
58
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | 1321-N1 |
| 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 | 56 | 5.26 | 6.72 |
| EC50 | 2 | 5.50 | 6.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2180137 | — | — | 1 | 6.72 |
| CHEMBL2180179 | — | — | 1 | 6.30 |
| CHEMBL14249 | ADENOSINE TRIPHOSPHATE | 2.0 | 1 | 6.00 |
| CHEMBL2180139 | — | — | 1 | 5.99 |
| CHEMBL2180160 | — | — | 1 | 5.86 |
| CHEMBL2180171 | — | — | 1 | 5.75 |
| CHEMBL490 | PAROXETINE | 4.0 | 1 | 5.73 |
| CHEMBL2180138 | — | — | 1 | 5.64 |
| CHEMBL2180136 | — | — | 1 | 5.63 |
| CHEMBL2180149 | — | — | 1 | 5.61 |
| CHEMBL2180148 | — | — | 1 | 5.60 |
| CHEMBL2180141 | — | — | 1 | 5.58 |
| CHEMBL2180174 | — | — | 1 | 5.57 |
| CHEMBL2180151 | — | — | 1 | 5.47 |
| CHEMBL2180142 | — | — | 1 | 5.41 |
| CHEMBL2180183 | — | — | 1 | 5.39 |
| CHEMBL2180184 | — | — | 1 | 5.37 |
| CHEMBL2180185 | — | — | 1 | 5.28 |
| CHEMBL451082 | — | — | 1 | 5.22 |
| CHEMBL2180169 | — | — | 1 | 5.02 |
| CHEMBL336208 | — | — | 1 | 5.00 |
| CHEMBL484675 | — | — | 1 | 4.99 |
| CHEMBL2180158 | — | — | 1 | 4.97 |
| CHEMBL2180177 | — | — | 1 | 4.97 |
| CHEMBL2180147 | — | — | 1 | 4.93 |
| CHEMBL2180175 | — | — | 1 | 4.91 |
| CHEMBL1163419 | TNP-ATP | — | 1 | 4.82 |
| CHEMBL2180173 | — | — | 1 | 4.76 |
| CHEMBL2180181 | — | — | 1 | 4.63 |
| CHEMBL2180172 | — | — | 1 | 4.61 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2180137 | — | IC50 | = | 189.0 | nM | 6.72 |
| CHEMBL2180179 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL14249 | ADENOSINE TRIPHOSPHATE | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2180139 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL2180160 | — | IC50 | = | 1380.0 | nM | 5.86 |
| CHEMBL2180171 | — | IC50 | = | 1780.0 | nM | 5.75 |
| CHEMBL490 | PAROXETINE | IC50 | = | 1870.0 | nM | 5.73 |
| CHEMBL2180138 | — | IC50 | = | 2280.0 | nM | 5.64 |
| CHEMBL2180136 | — | IC50 | = | 2350.0 | nM | 5.63 |
| CHEMBL2180149 | — | IC50 | = | 2440.0 | nM | 5.61 |
| CHEMBL2180148 | — | IC50 | = | 2490.0 | nM | 5.60 |
| CHEMBL2180141 | — | IC50 | = | 2640.0 | nM | 5.58 |
| CHEMBL2180174 | — | IC50 | = | 2690.0 | nM | 5.57 |
| CHEMBL2180151 | — | IC50 | = | 3390.0 | nM | 5.47 |
| CHEMBL2180142 | — | IC50 | = | 3930.0 | nM | 5.41 |
| CHEMBL2180183 | — | IC50 | = | 4110.0 | nM | 5.39 |
| CHEMBL2180184 | — | IC50 | = | 4290.0 | nM | 5.37 |
| CHEMBL2180185 | — | IC50 | = | 5290.0 | nM | 5.28 |
| CHEMBL451082 | — | IC50 | = | 5970.0 | nM | 5.22 |
| CHEMBL2180169 | — | IC50 | = | 9540.0 | nM | 5.02 |
| CHEMBL336208 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL484675 | — | IC50 | = | 10300.0 | nM | 4.99 |
| CHEMBL2180158 | — | IC50 | = | 10800.0 | nM | 4.97 |
| CHEMBL2180177 | — | IC50 | = | 10700.0 | nM | 4.97 |
| CHEMBL2180147 | — | IC50 | = | 11800.0 | nM | 4.93 |
| CHEMBL2180175 | — | IC50 | = | 12400.0 | nM | 4.91 |
| CHEMBL1163419 | TNP-ATP | IC50 | = | 15200.0 | nM | 4.82 |
| CHEMBL2180173 | — | IC50 | = | 17400.0 | nM | 4.76 |
| CHEMBL2180181 | — | IC50 | = | 23200.0 | nM | 4.63 |
| CHEMBL2180172 | — | IC50 | = | 24600.0 | nM | 4.61 |
| CHEMBL2180145 | — | IC50 | = | 26900.0 | nM | 4.57 |
| CHEMBL2180146 | — | IC50 | = | 39100.0 | nM | 4.41 |
| CHEMBL2180167 | — | IC50 | = | 45800.0 | nM | 4.34 |
| CHEMBL2180135 | — | IC50 | = | 52300.0 | nM | 4.28 |
| CHEMBL2180165 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180164 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180163 | — | IC50 | >= | 10000.0 | nM | - |
| CHEMBL2180162 | — | IC50 | >= | 10000.0 | nM | - |
| CHEMBL2180161 | — | IC50 | >= | 10000.0 | nM | - |
| CHEMBL2180156 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180159 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180178 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180150 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL229357 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180152 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180182 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180155 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180154 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180180 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180153 | — | IC50 | > | 10000.0 | nM | - |