Assay Detail
Binding
CHEMBL642021
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Tested for the binding affinity of A3 receptor by displacing N6-[[125I]-4-amino-3-iodobenzyl]-adenosine-5''-N-methyluronamide from membranes of CHO cells transfected with rat A3-cDNA
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| 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 | 7.69 | 9.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL431733 | NAMODENOSON | 3.0 | 1 | 9.48 |
| CHEMBL119709 | IB-MECA | — | 1 | 8.96 |
| CHEMBL133566 | — | — | 1 | 8.89 |
| CHEMBL307199 | — | — | 1 | 8.85 |
| CHEMBL2113557 | — | — | 1 | 8.64 |
| CHEMBL2113562 | — | — | 1 | 8.51 |
| CHEMBL66393 | — | — | 1 | 8.02 |
| CHEMBL609534 | — | — | 1 | 7.81 |
| CHEMBL1950647 | — | — | 1 | 7.30 |
| CHEMBL1256714 | — | — | 1 | 6.94 |
| CHEMBL2113561 | — | — | 1 | 6.74 |
| CHEMBL284969 | — | — | 1 | 6.62 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 1 | 6.62 |
| CHEMBL331372 | CGS-21680 | — | 1 | 6.23 |
| CHEMBL285819 | — | — | 1 | 5.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL431733 | NAMODENOSON | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL119709 | IB-MECA | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL133566 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL307199 | — | Ki | = | 1.41 | nM | 8.85 |
| CHEMBL2113557 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL2113562 | — | Ki | = | 3.12 | nM | 8.51 |
| CHEMBL66393 | — | Ki | = | 9.5 | nM | 8.02 |
| CHEMBL609534 | — | Ki | = | 15.5 | nM | 7.81 |
| CHEMBL1950647 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL1256714 | — | Ki | = | 116.0 | nM | 6.94 |
| CHEMBL2113561 | — | Ki | = | 181.0 | nM | 6.74 |
| CHEMBL284969 | — | Ki | = | 237.0 | nM | 6.62 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL331372 | CGS-21680 | Ki | = | 584.0 | nM | 6.23 |
| CHEMBL285819 | — | Ki | = | 1890.0 | nM | 5.72 |