Assay Detail
Binding
CHEMBL643930
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Binding affinity towards adenosine A3 receptor expressed in HEK293 cells versus [125I]AB-MECA
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
2-Alkynyl-8-aryl-9-methyladenines as novel adenosine receptor antagonists: their synthesis and structure-activity relationships toward hepatic glucose production induced via agonism of the A(2B) receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 6.20 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL52735 | — | — | 1 | 7.89 |
| CHEMBL51192 | — | — | 1 | 6.48 |
| CHEMBL48153 | — | — | 1 | 6.27 |
| CHEMBL297685 | — | — | 1 | 5.96 |
| CHEMBL300624 | — | — | 1 | 5.68 |
| CHEMBL27508 | — | — | 1 | 5.60 |
| CHEMBL440115 | FK453 | 1.0 | 1 | 5.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL52735 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL51192 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL48153 | — | Ki | = | 540.0 | nM | 6.27 |
| CHEMBL297685 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL300624 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL27508 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL440115 | FK453 | Ki | = | 2800.0 | nM | 5.55 |