Assay Detail
Binding
CHEMBL5055814
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Antagonist activity at rat P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by FLIPR analysis
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.04 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5086274 | — | — | 1 | 8.62 |
| CHEMBL255787 | — | — | 1 | 8.40 |
| CHEMBL3545108 | AZD9056 | 2.0 | 1 | 8.36 |
| CHEMBL2338352 | — | — | 1 | 8.33 |
| CHEMBL1628690 | — | — | 1 | 8.21 |
| CHEMBL437703 | — | — | 1 | 7.15 |
| CHEMBL5075634 | — | — | 1 | 7.02 |
| CHEMBL5498461 | E133 | — | 1 | 6.70 |
| CHEMBL3952549 | — | — | 1 | 6.58 |
| CHEMBL1823817 | CE-224535 | 2.0 | 1 | 6.33 |
| CHEMBL377219 | — | — | 1 | 6.04 |
| CHEMBL5087215 | — | — | 1 | 5.82 |
| CHEMBL1222883 | GSK1482160 | 1.0 | 1 | 5.72 |
| CHEMBL1094153 | — | — | 1 | 5.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5086274 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL255787 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3545108 | AZD9056 | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL2338352 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL1628690 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL437703 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL5075634 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL5498461 | E133 | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3952549 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL1823817 | CE-224535 | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL377219 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL5087215 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL1222883 | GSK1482160 | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL1094153 | — | IC50 | = | 5500.0 | nM | 5.26 |