Assay Detail
Binding
CHEMBL3745028
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Antagonist activity at P2X7 receptor expressed in LPS/IFNgamma-differentiated human THP1 cells assessed as inhibition of BzATP-induced IL-1beta production after 4 hrs by ELISA
8
Total Activities
8
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
Structure-activity relationship studies of pyrimidine-2,4-dione derivatives as potent P2X7 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.55 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3740315 | — | — | 1 | 7.92 |
| CHEMBL3741159 | — | — | 1 | 7.85 |
| CHEMBL3742331 | — | — | 1 | 7.77 |
| CHEMBL3741837 | — | — | 1 | 7.64 |
| CHEMBL3742001 | — | — | 1 | 7.52 |
| CHEMBL3740602 | — | — | 1 | 7.50 |
| CHEMBL3741312 | — | — | 1 | 7.34 |
| CHEMBL28324 | — | — | 1 | 6.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3740315 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3741159 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3742331 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3741837 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3742001 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3740602 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3741312 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL28324 | — | IC50 | = | 129.0 | nM | 6.89 |