Assay Detail
Binding
CHEMBL5055818
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Displacement of [3H]-A-804598 from rat P2X7 receptor expressed in HEK293 cell membrane by in vitro binding assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Subcellular | Membrane |
| 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 |
|---|---|---|---|
| Ki | 10 | 6.95 | 8.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1628690 | — | — | 1 | 8.41 |
| CHEMBL5086274 | — | — | 1 | 7.89 |
| CHEMBL437703 | — | — | 1 | 7.80 |
| CHEMBL255787 | — | — | 1 | 7.23 |
| CHEMBL2338352 | — | — | 1 | 7.01 |
| CHEMBL3545108 | AZD9056 | 2.0 | 1 | 6.89 |
| CHEMBL377219 | — | — | 1 | 6.70 |
| CHEMBL1222883 | GSK1482160 | 1.0 | 1 | 6.29 |
| CHEMBL5498461 | E133 | — | 1 | 6.00 |
| CHEMBL1094153 | — | — | 1 | 5.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1628690 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL5086274 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL437703 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL255787 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL2338352 | — | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL3545108 | AZD9056 | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL377219 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL1222883 | GSK1482160 | Ki | = | 510.0 | nM | 6.29 |
| CHEMBL5498461 | E133 | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL1094153 | — | Ki | = | 4800.0 | nM | 5.32 |