Assay Detail
Binding
CHEMBL647734
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Binding affinity for adenosine A2a receptor as inhibition of 3[H]-CGS 21680 binding in rat striatum
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Striatum |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
The synthesis of new adenosine A3 selective ligands containing bioisosteric isoxazoles.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 6.00 | 7.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL431733 | NAMODENOSON | 3.0 | 1 | 7.25 |
| CHEMBL296135 | — | — | 1 | 5.72 |
| CHEMBL49843 | — | — | 1 | 5.68 |
| CHEMBL301169 | — | — | 1 | 5.33 |
| CHEMBL49513 | — | — | 1 | - |
| CHEMBL50982 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL431733 | NAMODENOSON | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL296135 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL49843 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL301169 | — | Ki | = | 4650.0 | nM | 5.33 |
| CHEMBL49513 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL50982 | — | Ki | > | 10000.0 | nM | - |