Assay Detail
Functional
CHEMBL932847
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human recombinant P2X7 receptor assessed as inhibition of calcium flux by FLIPR assay
29
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and in vitro activity of N'-cyano-4-(2-phenylacetyl)-N-o-tolylpiperazine-1-carboximidamide P2X7 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 6.92 | 7.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL255578 | — | — | 1 | 7.44 |
| CHEMBL437403 | — | — | 1 | 7.40 |
| CHEMBL403965 | — | — | 1 | 7.40 |
| CHEMBL255787 | — | — | 1 | 7.36 |
| CHEMBL413070 | — | — | 1 | 7.34 |
| CHEMBL402614 | — | — | 1 | 7.34 |
| CHEMBL272934 | — | — | 1 | 7.29 |
| CHEMBL257273 | — | — | 1 | 7.24 |
| CHEMBL402832 | — | — | 2 | 7.24 |
| CHEMBL403410 | — | — | 1 | 7.23 |
| CHEMBL271213 | — | — | 1 | 7.22 |
| CHEMBL255784 | — | — | 1 | 7.16 |
| CHEMBL257092 | — | — | 1 | 7.15 |
| CHEMBL404528 | — | — | 1 | 7.06 |
| CHEMBL257275 | — | — | 1 | 7.03 |
| CHEMBL257635 | — | — | 1 | 7.00 |
| CHEMBL403916 | — | — | 1 | 6.96 |
| CHEMBL255536 | — | — | 1 | 6.92 |
| CHEMBL272275 | — | — | 1 | 6.85 |
| CHEMBL402243 | — | — | 1 | 6.72 |
| CHEMBL272579 | — | — | 1 | 6.66 |
| CHEMBL255788 | — | — | 1 | 6.51 |
| CHEMBL255980 | — | — | 1 | 6.39 |
| CHEMBL255742 | — | — | 1 | 6.37 |
| CHEMBL257216 | — | — | 1 | 6.34 |
| CHEMBL257838 | — | — | 1 | 6.00 |
| CHEMBL409534 | — | — | 1 | 5.89 |
| CHEMBL255534 | — | — | 1 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL255578 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL403965 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL437403 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL255787 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL402614 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL413070 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL272934 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL257273 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL402832 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL402832 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL403410 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL271213 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL255784 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL257092 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL404528 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL257275 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL257635 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL403916 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL255536 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL272275 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL402243 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL272579 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL255788 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL255980 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL255742 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL257216 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL257838 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL409534 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL255534 | — | IC50 | = | 1500.0 | nM | 5.82 |