Assay Detail
Functional
CHEMBL1780666
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
17
Total Activities
17
Compounds Tested
1
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 | 17 | 6.64 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1823817 | CE-224535 | 2.0 | 1 | 8.85 |
| CHEMBL1779511 | — | — | 1 | 7.72 |
| CHEMBL1779510 | — | — | 1 | 7.47 |
| CHEMBL1779508 | — | — | 1 | 7.38 |
| CHEMBL560423 | — | — | 1 | 7.08 |
| CHEMBL1779509 | — | — | 1 | 7.07 |
| CHEMBL559968 | — | — | 1 | 6.54 |
| CHEMBL559079 | — | — | 1 | 6.40 |
| CHEMBL1779513 | — | — | 1 | 6.16 |
| CHEMBL559078 | — | — | 1 | 6.10 |
| CHEMBL1779503 | — | — | 1 | 6.03 |
| CHEMBL1779493 | — | — | 1 | 5.96 |
| CHEMBL1779497 | — | — | 1 | 5.89 |
| CHEMBL1779495 | — | — | 1 | 5.55 |
| CHEMBL1779494 | — | — | 1 | 5.44 |
| CHEMBL1779501 | — | — | 1 | - |
| CHEMBL1779500 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1823817 | CE-224535 | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL1779511 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1779510 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL1779508 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL560423 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL1779509 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL559968 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL559079 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL1779513 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL559078 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL1779503 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL1779493 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1779497 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1779495 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL1779494 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL1779501 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL1779500 | — | IC50 | > | 5000.0 | nM | - |