Assay Detail
Functional
CHEMBL1780668
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at P2X7 receptor in human LPS-stimulated monocytes assessed as inhibition of ATP-induced IL1-beta release by ELISA in presence of human blood
10
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct 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 | 7 | 7.21 | 9.10 |
| IC90 | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1823817 | CE-224535 | 2.0 | 2 | 9.10 |
| CHEMBL1779511 | — | — | 1 | 7.15 |
| CHEMBL1779509 | — | — | 1 | 6.73 |
| CHEMBL1779510 | — | — | 1 | 6.70 |
| CHEMBL560423 | — | — | 2 | 6.35 |
| CHEMBL559968 | — | — | 2 | - |
| CHEMBL1779508 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1823817 | CE-224535 | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL1779511 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL1779509 | — | IC50 | = | 185.0 | nM | 6.73 |
| CHEMBL1779510 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL560423 | — | IC50 | = | 447.0 | nM | 6.35 |
| CHEMBL559968 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1779508 | — | IC50 | - | — | - | |
| CHEMBL559968 | — | IC90 | > | 10000.0 | nM | - |
| CHEMBL560423 | — | IC90 | = | 1000.0 | nM | - |
| CHEMBL1823817 | CE-224535 | IC90 | = | 4.7 | nM | - |