Assay Detail
Binding
CHEMBL4153210
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Antagonist activity at P2X7 in LPS/IFN gamma differentiated human THP-1 cells assessed as inhibition of BzATP-induced IL-1beta release preincubated for 30 mins followed by BzATP stimulation for 30 mins by ELISA
18
Total Activities
18
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
Synthesis and structure-activity relationships of quinolinone and quinoline-based P2X7 receptor antagonists and their anti-sphere formation activities in glioblastoma cells.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.43 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4171354 | — | — | 1 | 8.52 |
| CHEMBL4175330 | — | — | 1 | 8.22 |
| CHEMBL4175875 | — | — | 1 | 8.15 |
| CHEMBL4159914 | — | — | 1 | 7.92 |
| CHEMBL4163225 | — | — | 1 | 7.72 |
| CHEMBL4169592 | — | — | 1 | 7.60 |
| CHEMBL4159276 | — | — | 1 | 7.54 |
| CHEMBL4159289 | — | — | 1 | 7.48 |
| CHEMBL4176511 | — | — | 1 | 6.95 |
| CHEMBL28324 | — | — | 1 | 6.89 |
| CHEMBL4165201 | — | — | 1 | 6.75 |
| CHEMBL4160756 | — | — | 1 | 6.47 |
| CHEMBL4167190 | — | — | 1 | 6.36 |
| CHEMBL4161406 | — | — | 1 | - |
| CHEMBL4167598 | — | — | 1 | - |
| CHEMBL4172722 | — | — | 1 | - |
| CHEMBL4168674 | — | — | 1 | - |
| CHEMBL4165253 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4171354 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4175330 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4175875 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4159914 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4163225 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4169592 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4159276 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4159289 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4176511 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL28324 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4165201 | — | IC50 | = | 178.0 | nM | 6.75 |
| CHEMBL4160756 | — | IC50 | = | 335.0 | nM | 6.47 |
| CHEMBL4167190 | — | IC50 | = | 434.0 | nM | 6.36 |
| CHEMBL4161406 | — | IC50 | - | — | - | |
| CHEMBL4167598 | — | IC50 | - | — | - | |
| CHEMBL4172722 | — | IC50 | - | — | - | |
| CHEMBL4168674 | — | IC50 | - | — | - | |
| CHEMBL4165253 | — | IC50 | - | — | - |