Assay Detail
Binding
CHEMBL639749
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Tested for the binding affinity of A1 receptor by displacing the [3H]-PIA in rat brain membranes
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Brain membranes |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
2-Substitution of N6-benzyladenosine-5'-uronamides enhances selectivity for A3 adenosine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 7.31 | 9.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 1 | 9.23 |
| CHEMBL284969 | — | — | 1 | 9.22 |
| CHEMBL609534 | — | — | 1 | 8.68 |
| CHEMBL285819 | — | — | 1 | 8.03 |
| CHEMBL1256714 | — | — | 1 | 7.85 |
| CHEMBL133566 | — | — | 1 | 7.75 |
| CHEMBL307199 | — | — | 1 | 7.73 |
| CHEMBL66393 | — | — | 1 | 7.70 |
| CHEMBL119709 | IB-MECA | — | 1 | 7.27 |
| CHEMBL2113561 | — | — | 1 | 7.20 |
| CHEMBL1950647 | — | — | 1 | 6.40 |
| CHEMBL431733 | NAMODENOSON | 3.0 | 1 | 6.09 |
| CHEMBL2113557 | — | — | 1 | 5.67 |
| CHEMBL331372 | CGS-21680 | — | 1 | 5.58 |
| CHEMBL2113562 | — | — | 1 | 5.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | = | 0.59 | nM | 9.23 |
| CHEMBL284969 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL609534 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL285819 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL1256714 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL133566 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL307199 | — | Ki | = | 18.5 | nM | 7.73 |
| CHEMBL66393 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL119709 | IB-MECA | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL2113561 | — | Ki | = | 63.8 | nM | 7.20 |
| CHEMBL1950647 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL431733 | NAMODENOSON | Ki | = | 820.0 | nM | 6.09 |
| CHEMBL2113557 | — | Ki | = | 2140.0 | nM | 5.67 |
| CHEMBL331372 | CGS-21680 | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL2113562 | — | Ki | = | 4890.0 | nM | 5.31 |