Assay Detail
Binding
CHEMBL636642
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Inhibition of [3H]- PIA binding at adenosine A1 receptor on rat cerebral cortex membranes.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Xanthine functionalized congeners as potent ligands at A2-adenosine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 7.63 | 9.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL70059 | — | — | 1 | 9.06 |
| CHEMBL273094 | XANTHINE AMINE CONGENER | — | 1 | 8.92 |
| CHEMBL16866 | — | — | 1 | 8.03 |
| CHEMBL68756 | — | — | 1 | 8.03 |
| CHEMBL305765 | — | — | 1 | 7.92 |
| CHEMBL158507 | — | — | 1 | 7.89 |
| CHEMBL66207 | — | — | 1 | 7.89 |
| CHEMBL66523 | — | — | 1 | 7.89 |
| CHEMBL17141 | — | — | 1 | 7.60 |
| CHEMBL441598 | — | — | 1 | 7.57 |
| CHEMBL70188 | — | — | 1 | 7.38 |
| CHEMBL27041 | — | — | 1 | 7.30 |
| CHEMBL67389 | — | — | 1 | 7.24 |
| CHEMBL66053 | — | — | 1 | 7.24 |
| CHEMBL11348 | — | — | 1 | 7.19 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | — | 1 | 7.16 |
| CHEMBL305212 | — | — | 1 | 7.05 |
| CHEMBL307313 | — | — | 1 | 6.85 |
| CHEMBL66919 | — | — | 1 | 6.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL70059 | — | Ki | = | 0.87 | nM | 9.06 |
| CHEMBL273094 | XANTHINE AMINE CONGENER | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL16866 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL68756 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL305765 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL158507 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL66207 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL66523 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL17141 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL441598 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL70188 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL27041 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL67389 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL66053 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL11348 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL305212 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL307313 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL66919 | — | Ki | = | 180.0 | nM | 6.75 |