Assay Detail
Binding
CHEMBL4479310
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human P2X7 receptor in LPS/IFN-gamma-differentiated human THP-1 cells assessed as suppression of BzATP-stimulated IL-1beta release per-incubated for 30 mins before BzATP addition and measured after 30 mins by ELISA
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | THP-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Potent Suppressive Effects of 1-Piperidinylimidazole Based Novel P2X7 Receptor Antagonists on Cancer Cell Migration and Invasion.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 7.85 | 10.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3415305 | — | — | 1 | 10.22 |
| CHEMBL4521847 | — | — | 1 | 9.49 |
| CHEMBL4582650 | — | — | 1 | 8.99 |
| CHEMBL4561852 | — | — | 1 | 8.88 |
| CHEMBL4560935 | — | — | 1 | 8.75 |
| CHEMBL4165149 | — | — | 1 | 8.66 |
| CHEMBL4529050 | — | — | 1 | 8.37 |
| CHEMBL4573595 | — | — | 1 | 8.33 |
| CHEMBL4584526 | — | — | 1 | 8.08 |
| CHEMBL4531777 | — | — | 1 | 8.00 |
| CHEMBL4570660 | — | — | 1 | 7.89 |
| CHEMBL4542014 | — | — | 1 | 7.77 |
| CHEMBL3741159 | — | — | 1 | 7.75 |
| CHEMBL4526937 | — | — | 1 | 7.66 |
| CHEMBL4559257 | — | — | 1 | 7.66 |
| CHEMBL4585050 | — | — | 1 | 7.58 |
| CHEMBL4534068 | — | — | 1 | 7.50 |
| CHEMBL4586600 | — | — | 1 | 7.43 |
| CHEMBL4594110 | — | — | 1 | 7.37 |
| CHEMBL4582804 | — | — | 1 | 7.30 |
| CHEMBL3415342 | — | — | 1 | 7.27 |
| CHEMBL4536033 | — | — | 1 | 7.24 |
| CHEMBL4513283 | — | — | 1 | 7.19 |
| CHEMBL4529842 | — | — | 1 | 6.92 |
| CHEMBL4535840 | — | — | 1 | 6.84 |
| CHEMBL4592534 | — | — | 1 | 6.68 |
| CHEMBL4537806 | — | — | 1 | 6.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3415305 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL4521847 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL4582650 | — | IC50 | = | 1.03 | nM | 8.99 |
| CHEMBL4561852 | — | IC50 | = | 1.33 | nM | 8.88 |
| CHEMBL4560935 | — | IC50 | = | 1.76 | nM | 8.75 |
| CHEMBL4165149 | — | IC50 | = | 2.19 | nM | 8.66 |
| CHEMBL4529050 | — | IC50 | = | 4.28 | nM | 8.37 |
| CHEMBL4573595 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL4584526 | — | IC50 | = | 8.29 | nM | 8.08 |
| CHEMBL4531777 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4570660 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4542014 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3741159 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4526937 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4559257 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4585050 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4534068 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4586600 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4594110 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4582804 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3415342 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4536033 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4513283 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL4529842 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL4535840 | — | IC50 | = | 143.0 | nM | 6.84 |
| CHEMBL4592534 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4537806 | — | IC50 | = | 552.0 | nM | 6.26 |