Assay Detail
Binding
CHEMBL640365
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Displacement of [3H]-(R)-PIA from Adenosine A1 receptor of rat cerebral cortex membranes
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 6.75 | 7.95 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL95811 | — | — | 1 | 7.95 |
| CHEMBL313422 | — | — | 1 | 7.54 |
| CHEMBL319971 | — | — | 1 | 7.49 |
| CHEMBL318251 | — | — | 1 | 7.28 |
| CHEMBL100195 | — | — | 1 | 7.04 |
| CHEMBL96041 | — | — | 1 | 6.72 |
| CHEMBL93932 | — | — | 1 | 6.70 |
| CHEMBL317310 | — | — | 1 | 6.69 |
| CHEMBL329722 | — | — | 1 | 6.55 |
| CHEMBL88147 | — | — | 1 | 6.52 |
| CHEMBL317382 | — | — | 1 | 6.17 |
| CHEMBL97383 | — | — | 1 | 5.73 |
| CHEMBL414023 | — | — | 1 | 5.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL95811 | — | Ki | = | 11.3 | nM | 7.95 |
| CHEMBL313422 | — | Ki | = | 28.9 | nM | 7.54 |
| CHEMBL319971 | — | Ki | = | 32.5 | nM | 7.49 |
| CHEMBL318251 | — | Ki | = | 52.2 | nM | 7.28 |
| CHEMBL100195 | — | Ki | = | 91.3 | nM | 7.04 |
| CHEMBL96041 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL93932 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL317310 | — | Ki | = | 205.0 | nM | 6.69 |
| CHEMBL329722 | — | Ki | = | 283.0 | nM | 6.55 |
| CHEMBL88147 | — | Ki | = | 305.0 | nM | 6.52 |
| CHEMBL317382 | — | Ki | = | 680.0 | nM | 6.17 |
| CHEMBL97383 | — | Ki | = | 1850.0 | nM | 5.73 |
| CHEMBL414023 | — | Ki | = | 3950.0 | nM | 5.40 |