Assay Detail
Binding
CHEMBL3831085
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Displacement of [3H]MSX2 from adenosine receptor A2a in rat brain striatal membranes
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Similarities and differences in affinity and binding modes of tricyclic pyrimido- and pyrazinoxanthines at human and rat adenosine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 37 | 5.94 | 6.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3827583 | — | — | 1 | 6.57 |
| CHEMBL3827859 | — | — | 1 | 6.47 |
| CHEMBL3828658 | — | — | 1 | 6.33 |
| CHEMBL3828002 | — | — | 1 | 6.29 |
| CHEMBL3827331 | — | — | 1 | 6.25 |
| CHEMBL3827016 | — | — | 1 | 6.23 |
| CHEMBL3828343 | — | — | 1 | 6.19 |
| CHEMBL3828401 | — | — | 1 | 6.18 |
| CHEMBL3828237 | — | — | 1 | 6.18 |
| CHEMBL3827301 | — | — | 1 | 6.13 |
| CHEMBL3828044 | — | — | 1 | 6.11 |
| CHEMBL3827365 | — | — | 1 | 6.07 |
| CHEMBL3093326 | — | — | 1 | 6.05 |
| CHEMBL3827074 | — | — | 1 | 6.00 |
| CHEMBL3827598 | — | — | 1 | 5.98 |
| CHEMBL3828555 | — | — | 1 | 5.86 |
| CHEMBL3827187 | — | — | 1 | 5.84 |
| CHEMBL3827201 | — | — | 1 | 5.83 |
| CHEMBL3827653 | — | — | 1 | 5.75 |
| CHEMBL3827175 | — | — | 1 | 5.71 |
| CHEMBL3827628 | — | — | 1 | 5.25 |
| CHEMBL3827216 | — | — | 1 | 5.19 |
| CHEMBL3827075 | — | — | 1 | 5.11 |
| CHEMBL3827031 | — | — | 1 | 4.94 |
| CHEMBL3827973 | — | — | 1 | - |
| CHEMBL3827920 | — | — | 1 | - |
| CHEMBL3827922 | — | — | 1 | - |
| CHEMBL3827544 | — | — | 1 | - |
| CHEMBL3828530 | — | — | 1 | - |
| CHEMBL3827298 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3827583 | — | Ki | = | 271.0 | nM | 6.57 |
| CHEMBL3827859 | — | Ki | = | 339.0 | nM | 6.47 |
| CHEMBL3828658 | — | Ki | = | 464.0 | nM | 6.33 |
| CHEMBL3828002 | — | Ki | = | 518.0 | nM | 6.29 |
| CHEMBL3827331 | — | Ki | = | 566.0 | nM | 6.25 |
| CHEMBL3827016 | — | Ki | = | 585.0 | nM | 6.23 |
| CHEMBL3828343 | — | Ki | = | 645.0 | nM | 6.19 |
| CHEMBL3828401 | — | Ki | = | 658.0 | nM | 6.18 |
| CHEMBL3828237 | — | Ki | = | 653.0 | nM | 6.18 |
| CHEMBL3827301 | — | Ki | = | 738.0 | nM | 6.13 |
| CHEMBL3828044 | — | Ki | = | 785.0 | nM | 6.11 |
| CHEMBL3827365 | — | Ki | = | 859.0 | nM | 6.07 |
| CHEMBL3093326 | — | Ki | = | 893.0 | nM | 6.05 |
| CHEMBL3827074 | — | Ki | = | 989.0 | nM | 6.00 |
| CHEMBL3827598 | — | Ki | = | 1050.0 | nM | 5.98 |
| CHEMBL3828555 | — | Ki | = | 1370.0 | nM | 5.86 |
| CHEMBL3827187 | — | Ki | = | 1460.0 | nM | 5.84 |
| CHEMBL3827201 | — | Ki | = | 1480.0 | nM | 5.83 |
| CHEMBL3827653 | — | Ki | = | 1790.0 | nM | 5.75 |
| CHEMBL3827175 | — | Ki | = | 1930.0 | nM | 5.71 |
| CHEMBL3827628 | — | Ki | = | 5640.0 | nM | 5.25 |
| CHEMBL3827216 | — | Ki | = | 6400.0 | nM | 5.19 |
| CHEMBL3827075 | — | Ki | = | 7850.0 | nM | 5.11 |
| CHEMBL3827031 | — | Ki | = | 11500.0 | nM | 4.94 |
| CHEMBL3828477 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL3828341 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL3827127 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL3827704 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL3827716 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL3827267 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL3827623 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL3827298 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL3828530 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL3827544 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL3827922 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL3827920 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL3827973 | — | Ki | > | 10000.0 | nM | - |