Assay Detail
Binding
CHEMBL5044913
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]SCH-58261 from A2A adenosine receptor (unknown origin) expressed in HEK cell membrane incubated for 60 mins at room temperature by NXT microplate scintillation counter analysis
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Optimization of 2-Amino-4,6-diarylpyrimidine-5-carbonitriles as Potent and Selective A<sub>1</sub> Antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 6.94 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL369573 | — | — | 1 | 8.96 |
| CHEMBL178584 | — | — | 1 | 7.95 |
| CHEMBL259319 | — | — | 1 | 6.80 |
| CHEMBL261185 | — | — | 1 | 6.39 |
| CHEMBL406788 | — | — | 1 | 6.34 |
| CHEMBL258834 | — | — | 1 | 6.25 |
| CHEMBL3937015 | — | — | 1 | 5.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL369573 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL178584 | — | Ki | = | 11.2 | nM | 7.95 |
| CHEMBL259319 | — | Ki | = | 159.0 | nM | 6.80 |
| CHEMBL261185 | — | Ki | = | 405.0 | nM | 6.39 |
| CHEMBL406788 | — | Ki | = | 459.0 | nM | 6.34 |
| CHEMBL258834 | — | Ki | = | 557.0 | nM | 6.25 |
| CHEMBL3937015 | — | Ki | = | 1369.0 | nM | 5.86 |