Assay Detail
Binding
CHEMBL5032900
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]MSX-2 from human recombinant adenosine A2A receptor expressed in CHO cells by liquid scintillation counting analysis
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Adenosine A<sub>2A</sub>R/A<sub>1</sub>R Antagonists Enabling Additional H<sub>3</sub>R Antagonism for the Treatment of Parkinson's Disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 7.53 | 9.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL240624 | PRELADENANT | 3.0 | 1 | 9.06 |
| CHEMBL5082650 | — | — | 1 | 8.40 |
| CHEMBL5084903 | — | — | 1 | 8.31 |
| CHEMBL5082920 | — | — | 1 | 8.21 |
| CHEMBL5088622 | — | — | 1 | 8.14 |
| CHEMBL1095488 | — | — | 1 | 8.12 |
| CHEMBL5089580 | — | — | 1 | 7.45 |
| CHEMBL5081556 | — | — | 1 | 6.98 |
| CHEMBL5087059 | — | — | 1 | 6.85 |
| CHEMBL5093850 | — | — | 1 | 6.69 |
| CHEMBL5072724 | — | — | 1 | 6.14 |
| CHEMBL5093935 | — | — | 1 | 6.03 |
| CHEMBL5094263 | — | — | 1 | - |
| CHEMBL5094415 | — | — | 1 | - |
| CHEMBL2297871 | — | — | 1 | - |
| CHEMBL14638 | CIPROXIFAN | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL240624 | PRELADENANT | Ki | = | 0.88 | nM | 9.06 |
| CHEMBL5082650 | — | Ki | = | 4.01 | nM | 8.40 |
| CHEMBL5084903 | — | Ki | = | 4.85 | nM | 8.31 |
| CHEMBL5082920 | — | Ki | = | 6.24 | nM | 8.21 |
| CHEMBL5088622 | — | Ki | = | 7.25 | nM | 8.14 |
| CHEMBL1095488 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL5089580 | — | Ki | = | 35.5 | nM | 7.45 |
| CHEMBL5081556 | — | Ki | = | 104.0 | nM | 6.98 |
| CHEMBL5087059 | — | Ki | = | 142.0 | nM | 6.85 |
| CHEMBL5093850 | — | Ki | = | 203.0 | nM | 6.69 |
| CHEMBL5072724 | — | Ki | = | 717.0 | nM | 6.14 |
| CHEMBL5093935 | — | Ki | = | 941.0 | nM | 6.03 |
| CHEMBL5094263 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5094415 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL2297871 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL14638 | CIPROXIFAN | Ki | > | 1000.0 | nM | - |