Assay Detail
Binding
CHEMBL646352
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Ability to inhibit binding of [3H]-CGS- 21680 to adenosine A2A receptor in rat brain striatal membranes.
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis and structure-activity relationships of 3,7-dimethyl-1-propargylxanthine derivatives, A2A-selective adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 32 | 6.70 | 8.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL342188 | — | — | 1 | 8.29 |
| CHEMBL136047 | — | — | 1 | 8.09 |
| CHEMBL27508 | — | — | 1 | 8.07 |
| CHEMBL137471 | — | — | 1 | 7.89 |
| CHEMBL137199 | — | — | 1 | 7.82 |
| CHEMBL136394 | — | — | 1 | 7.82 |
| CHEMBL280982 | — | — | 1 | 7.75 |
| CHEMBL334873 | — | — | 1 | 7.62 |
| CHEMBL136836 | — | — | 1 | 7.57 |
| CHEMBL138950 | — | — | 1 | 7.51 |
| CHEMBL342229 | — | — | 1 | 7.46 |
| CHEMBL26138 | — | — | 1 | 7.44 |
| CHEMBL138833 | — | — | 1 | 7.34 |
| CHEMBL343395 | — | — | 1 | 7.21 |
| CHEMBL137508 | — | — | 1 | 7.20 |
| CHEMBL136364 | — | — | 1 | 7.17 |
| CHEMBL26897 | — | — | 1 | 7.03 |
| CHEMBL343527 | — | — | 1 | 6.77 |
| CHEMBL345060 | — | — | 1 | 6.60 |
| CHEMBL344678 | — | — | 1 | 6.51 |
| CHEMBL344026 | — | — | 1 | 6.47 |
| CHEMBL337373 | — | — | 1 | 6.25 |
| CHEMBL137944 | — | — | 1 | 6.06 |
| CHEMBL422110 | — | — | 1 | 5.75 |
| CHEMBL115940 | — | — | 1 | 5.48 |
| CHEMBL139013 | — | — | 1 | 5.46 |
| CHEMBL136199 | — | — | 1 | 5.35 |
| CHEMBL282038 | — | — | 1 | 5.07 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 5.03 |
| CHEMBL342193 | — | — | 1 | 4.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL342188 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL136047 | — | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL27508 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL137471 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL137199 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL136394 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL280982 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL334873 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL136836 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL138950 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL342229 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL26138 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL138833 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL343395 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL137508 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL136364 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL26897 | — | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL343527 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL345060 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL344678 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL344026 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL337373 | — | Ki | = | 560.0 | nM | 6.25 |
| CHEMBL137944 | — | Ki | = | 880.0 | nM | 6.06 |
| CHEMBL422110 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL115940 | — | Ki | = | 3300.0 | nM | 5.48 |
| CHEMBL139013 | — | Ki | = | 3500.0 | nM | 5.46 |
| CHEMBL136199 | — | Ki | = | 4500.0 | nM | 5.35 |
| CHEMBL282038 | — | Ki | = | 8600.0 | nM | 5.07 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 9400.0 | nM | 5.03 |
| CHEMBL342193 | — | Ki | = | 14000.0 | nM | 4.85 |
| CHEMBL21053 | — | Ki | = | 19000.0 | nM | 4.72 |
| CHEMBL113 | CAFFEINE | Ki | = | 22000.0 | nM | 4.66 |