Assay Detail
Binding
CHEMBL943937
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]ZM241385 from rat recombinant adenosine A2A receptor expressed in CHO cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Identification of novel, water-soluble, 2-amino-N-pyrimidin-4-yl acetamides as A2A receptor antagonists with in vivo efficacy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 8.02 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL431770 | ISTRADEFYLLINE | 4.0 | 1 | 8.70 |
| CHEMBL398272 | — | — | 1 | 7.96 |
| CHEMBL252171 | — | — | 1 | 7.85 |
| CHEMBL251975 | — | — | 1 | 7.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL431770 | ISTRADEFYLLINE | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL398272 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL252171 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL251975 | — | Ki | = | 26.0 | nM | 7.58 |