Assay Detail
Binding
CHEMBL649881
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Binding affinity at adenosine A2 receptor from rat striatal membranes by [3H]NECA displacement.
17
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
N6-[2-(3,5-dimethoxyphenyl)-2-(2-methylphenyl)ethyl]adenosine and its uronamide derivatives. Novel adenosine agonists with both high affinity and high selectivity for the adenosine A2 receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 7.73 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2094089 | — | — | 3 | 8.51 |
| CHEMBL603366 | — | — | 1 | 8.22 |
| CHEMBL606507 | — | — | 1 | 8.21 |
| CHEMBL604402 | — | — | 1 | 8.19 |
| CHEMBL132960 | — | — | 1 | 8.03 |
| CHEMBL464859 | NECA | — | 1 | 7.92 |
| CHEMBL604607 | — | — | 1 | 7.73 |
| CHEMBL603579 | — | — | 1 | 7.72 |
| CHEMBL606506 | — | — | 1 | 7.71 |
| CHEMBL193692 | — | — | 1 | 7.60 |
| CHEMBL606505 | — | — | 1 | 7.52 |
| CHEMBL604404 | — | — | 1 | 7.21 |
| CHEMBL1256672 | — | — | 1 | 6.94 |
| CHEMBL139000 | (R)-PIA | — | 1 | 6.91 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 1 | 6.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2094089 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL2094089 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL603366 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL2094089 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL606507 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL604402 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL132960 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL464859 | NECA | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL604607 | — | Ki | = | 18.8 | nM | 7.73 |
| CHEMBL603579 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL606506 | — | Ki | = | 19.5 | nM | 7.71 |
| CHEMBL193692 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL606505 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL604404 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL1256672 | — | Ki | = | 116.0 | nM | 6.94 |
| CHEMBL139000 | (R)-PIA | Ki | = | 124.0 | nM | 6.91 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | = | 460.0 | nM | 6.34 |