Assay Detail
Binding
CHEMBL643132
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Binding affinity for recombinant rat A3-adenosine receptor by the displacement of specific [125I]APNEA or [125I]-N6-(4-amino-3-iodobenzyl)-adenosine-5'-N-methyluronamide
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Structure-activity relationships of N6-benzyladenosine-5'-uronamides as A3-selective adenosine agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 26 | 7.24 | 9.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2113613 | — | — | 1 | 9.06 |
| CHEMBL2113565 | — | — | 1 | 8.96 |
| CHEMBL2113567 | — | — | 1 | 8.92 |
| CHEMBL2113570 | — | — | 1 | 8.55 |
| CHEMBL2113611 | — | — | 1 | 8.37 |
| CHEMBL2113614 | — | — | 1 | 8.17 |
| CHEMBL2113612 | — | — | 1 | 8.15 |
| CHEMBL2113638 | — | — | 1 | 8.06 |
| CHEMBL2113571 | — | — | 1 | 8.05 |
| CHEMBL2113569 | — | — | 1 | 7.97 |
| CHEMBL2113610 | — | — | 1 | 7.96 |
| CHEMBL49843 | — | — | 1 | 7.80 |
| CHEMBL2113617 | — | — | 1 | 7.66 |
| CHEMBL3351031 | — | — | 1 | 7.57 |
| CHEMBL3351032 | — | — | 1 | 7.22 |
| CHEMBL519809 | — | — | 1 | 7.14 |
| CHEMBL610710 | — | — | 1 | 6.99 |
| CHEMBL464859 | NECA | — | 1 | 6.95 |
| CHEMBL2113618 | — | — | 1 | 6.61 |
| CHEMBL608761 | — | — | 1 | 6.33 |
| CHEMBL605866 | — | — | 1 | 5.85 |
| CHEMBL261482 | — | — | 1 | 5.80 |
| CHEMBL609834 | — | — | 1 | 5.30 |
| CHEMBL2113568 | — | — | 1 | 5.21 |
| CHEMBL129903 | — | — | 1 | 4.83 |
| CHEMBL2113566 | — | — | 1 | 4.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2113613 | — | Ki | = | 0.88 | nM | 9.06 |
| CHEMBL2113565 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL2113567 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL2113570 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL2113611 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL2113614 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL2113612 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL2113638 | — | Ki | = | 8.7 | nM | 8.06 |
| CHEMBL2113571 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL2113569 | — | Ki | = | 10.7 | nM | 7.97 |
| CHEMBL2113610 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL49843 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL2113617 | — | Ki | = | 21.9 | nM | 7.66 |
| CHEMBL3351031 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL3351032 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL519809 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL610710 | — | Ki | = | 103.0 | nM | 6.99 |
| CHEMBL464859 | NECA | Ki | = | 113.0 | nM | 6.95 |
| CHEMBL2113618 | — | Ki | = | 246.0 | nM | 6.61 |
| CHEMBL608761 | — | Ki | = | 468.0 | nM | 6.33 |
| CHEMBL605866 | — | Ki | = | 1410.0 | nM | 5.85 |
| CHEMBL261482 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL609834 | — | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL2113568 | — | Ki | = | 6220.0 | nM | 5.21 |
| CHEMBL129903 | — | Ki | = | 14700.0 | nM | 4.83 |
| CHEMBL2113566 | — | Ki | = | 18000.0 | nM | 4.75 |