Assay Detail
Functional
CHEMBL2049237
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Antagonist activity at human P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced IL8 release pretreated for 30 mins before bzATP challenge measured after 30 mins by ELISA
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | THP-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-activity relationships and optimization of 3,5-dichloropyridine derivatives as novel P2X(7) receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.41 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2048437 | — | — | 1 | 8.89 |
| CHEMBL2048438 | — | — | 1 | 8.04 |
| CHEMBL2048286 | — | — | 1 | 7.38 |
| CHEMBL2048285 | — | — | 1 | 7.25 |
| CHEMBL28324 | — | — | 1 | 6.92 |
| CHEMBL2048436 | — | — | 1 | 6.89 |
| CHEMBL2048251 | — | — | 1 | 6.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2048437 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL2048438 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL2048286 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL2048285 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL28324 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2048436 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL2048251 | — | IC50 | = | 320.0 | nM | 6.50 |