Assay Detail
Binding
CHEMBL5046688
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Antagonist activity at human P2X7R expressed in HEK293 cells assessed as reduction in YO-PRO-1 iodide dye uptake preincubated for 30 mins followed by YO-PRO-1 iodide addition and measured after 2 hrs by fluorescence plate reader analysis
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Piperazine squaric acid diamides, a novel class of allosteric P2X7 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 6.40 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2338352 | — | — | 1 | 7.80 |
| CHEMBL5079389 | — | — | 1 | 7.62 |
| CHEMBL5093653 | — | — | 1 | 7.19 |
| CHEMBL5089768 | — | — | 1 | 7.13 |
| CHEMBL5094161 | — | — | 1 | 7.06 |
| CHEMBL5075280 | — | — | 1 | 6.99 |
| CHEMBL5072113 | — | — | 1 | 6.96 |
| CHEMBL5076450 | — | — | 1 | 6.87 |
| CHEMBL5093681 | — | — | 1 | 6.82 |
| CHEMBL5079624 | — | — | 1 | 6.80 |
| CHEMBL5094084 | — | — | 1 | 6.65 |
| CHEMBL5092737 | — | — | 1 | 6.52 |
| CHEMBL5073035 | — | — | 1 | 6.51 |
| CHEMBL5081860 | — | — | 1 | 6.42 |
| CHEMBL5076226 | — | — | 1 | 6.31 |
| CHEMBL5082947 | — | — | 1 | 6.26 |
| CHEMBL5090437 | — | — | 1 | 6.13 |
| CHEMBL5084591 | — | — | 1 | 6.12 |
| CHEMBL5075398 | — | — | 1 | 6.00 |
| CHEMBL5074653 | — | — | 1 | 4.31 |
| CHEMBL5092738 | — | — | 1 | 4.31 |
| CHEMBL5088972 | — | — | 1 | 4.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2338352 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL5079389 | — | IC50 | = | 23.99 | nM | 7.62 |
| CHEMBL5093653 | — | IC50 | = | 64.57 | nM | 7.19 |
| CHEMBL5089768 | — | IC50 | = | 74.13 | nM | 7.13 |
| CHEMBL5094161 | — | IC50 | = | 87.1 | nM | 7.06 |
| CHEMBL5075280 | — | IC50 | = | 102.33 | nM | 6.99 |
| CHEMBL5072113 | — | IC50 | = | 109.65 | nM | 6.96 |
| CHEMBL5076450 | — | IC50 | = | 134.9 | nM | 6.87 |
| CHEMBL5093681 | — | IC50 | = | 151.36 | nM | 6.82 |
| CHEMBL5079624 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL5094084 | — | IC50 | = | 223.87 | nM | 6.65 |
| CHEMBL5092737 | — | IC50 | = | 302.0 | nM | 6.52 |
| CHEMBL5073035 | — | IC50 | = | 309.03 | nM | 6.51 |
| CHEMBL5081860 | — | IC50 | = | 380.19 | nM | 6.42 |
| CHEMBL5076226 | — | IC50 | = | 489.78 | nM | 6.31 |
| CHEMBL5082947 | — | IC50 | = | 549.54 | nM | 6.26 |
| CHEMBL5090437 | — | IC50 | = | 741.31 | nM | 6.13 |
| CHEMBL5084591 | — | IC50 | = | 758.58 | nM | 6.12 |
| CHEMBL5075398 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL5074653 | — | IC50 | = | 48977.88 | nM | 4.31 |
| CHEMBL5092738 | — | IC50 | = | 48977.88 | nM | 4.31 |
| CHEMBL5088972 | — | IC50 | = | 83176.38 | nM | 4.08 |