Assay Detail
Binding
CHEMBL643470
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Binding affinity at adenosine A1 receptor from rat brain membranes by [3H]N6-cyclohexyladenosine displacement.
21
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
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 | 21 | 7.45 | 9.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 1 | 9.23 |
| CHEMBL139000 | (R)-PIA | — | 1 | 8.92 |
| CHEMBL603366 | — | — | 1 | 8.59 |
| CHEMBL2181971 | — | — | 1 | 8.28 |
| CHEMBL464859 | NECA | — | 1 | 8.20 |
| CHEMBL193692 | — | — | 1 | 8.17 |
| CHEMBL604607 | — | — | 1 | 8.03 |
| CHEMBL604402 | — | — | 1 | 7.74 |
| CHEMBL132960 | — | — | 1 | 7.62 |
| CHEMBL606507 | — | — | 1 | 7.52 |
| CHEMBL606505 | — | — | 1 | 7.43 |
| CHEMBL603579 | — | — | 1 | 7.21 |
| CHEMBL2094089 | — | — | 3 | 6.93 |
| CHEMBL606506 | — | — | 1 | 6.85 |
| CHEMBL604818 | — | — | 1 | 6.68 |
| CHEMBL604404 | — | — | 1 | 6.64 |
| CHEMBL603791 | — | — | 1 | 6.63 |
| CHEMBL1256672 | — | — | 1 | 6.22 |
| CHEMBL604819 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | = | 0.59 | nM | 9.23 |
| CHEMBL139000 | (R)-PIA | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL603366 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL2181971 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL464859 | NECA | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL193692 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL604607 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL604402 | — | Ki | = | 18.4 | nM | 7.74 |
| CHEMBL132960 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL606507 | — | Ki | = | 30.2 | nM | 7.52 |
| CHEMBL606505 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL603579 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL2094089 | — | Ki | = | 118.0 | nM | 6.93 |
| CHEMBL606506 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL2094089 | — | Ki | = | 142.0 | nM | 6.85 |
| CHEMBL2094089 | — | Ki | = | 188.0 | nM | 6.73 |
| CHEMBL604818 | — | Ki | = | 207.0 | nM | 6.68 |
| CHEMBL604404 | — | Ki | = | 229.0 | nM | 6.64 |
| CHEMBL603791 | — | Ki | = | 232.0 | nM | 6.63 |
| CHEMBL1256672 | — | Ki | = | 600.0 | nM | 6.22 |
| CHEMBL604819 | — | Ki | = | 1010.0 | nM | 6.00 |