Assay Detail
Functional
CHEMBL1780665
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Antagonist activity at P2X7 receptor expressed in HEK293 cells assessed as inhibition of ATP-induced YOPRO-1 uptake
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 7.18 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1823817 | CE-224535 | 2.0 | 1 | 8.40 |
| CHEMBL560423 | — | — | 1 | 7.82 |
| CHEMBL559968 | — | — | 1 | 6.52 |
| CHEMBL559078 | — | — | 1 | 5.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1823817 | CE-224535 | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL560423 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL559968 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL559078 | — | IC50 | = | 1100.0 | nM | 5.96 |