Assay Detail
Binding
CHEMBL649104
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Ability to inhibit binding of [3H]CHA to adenosine A1 receptor in rat brain cortical membranes.
31
Total Activities
31
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 | 31 | 5.80 | 7.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL138833 | — | — | 1 | 7.08 |
| CHEMBL342188 | — | — | 1 | 6.99 |
| CHEMBL337373 | — | — | 1 | 6.75 |
| CHEMBL343395 | — | — | 1 | 6.70 |
| CHEMBL137199 | — | — | 1 | 6.62 |
| CHEMBL27508 | — | — | 1 | 6.58 |
| CHEMBL138950 | — | — | 1 | 6.27 |
| CHEMBL334873 | — | — | 1 | 6.12 |
| CHEMBL343527 | — | — | 1 | 6.08 |
| CHEMBL137944 | — | — | 1 | 6.07 |
| CHEMBL422110 | — | — | 1 | 6.02 |
| CHEMBL136836 | — | — | 1 | 5.96 |
| CHEMBL136047 | — | — | 1 | 5.92 |
| CHEMBL137471 | — | — | 1 | 5.89 |
| CHEMBL344678 | — | — | 1 | 5.89 |
| CHEMBL342229 | — | — | 1 | 5.82 |
| CHEMBL345060 | — | — | 1 | 5.72 |
| CHEMBL136364 | — | — | 1 | 5.64 |
| CHEMBL136394 | — | — | 1 | 5.60 |
| CHEMBL136199 | — | — | 1 | 5.55 |
| CHEMBL139013 | — | — | 1 | 5.55 |
| CHEMBL115940 | — | — | 1 | 5.50 |
| CHEMBL344026 | — | — | 1 | 5.39 |
| CHEMBL342193 | — | — | 1 | 5.36 |
| CHEMBL137508 | — | — | 1 | 5.04 |
| CHEMBL280982 | — | — | 1 | 5.02 |
| CHEMBL282038 | — | — | 1 | 4.92 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 4.77 |
| CHEMBL113 | CAFFEINE | 4.0 | 1 | 4.58 |
| CHEMBL21053 | — | — | 1 | 4.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL138833 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL342188 | — | Ki | = | 102.0 | nM | 6.99 |
| CHEMBL337373 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL343395 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL137199 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL27508 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL138950 | — | Ki | = | 540.0 | nM | 6.27 |
| CHEMBL334873 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL343527 | — | Ki | = | 840.0 | nM | 6.08 |
| CHEMBL137944 | — | Ki | = | 860.0 | nM | 6.07 |
| CHEMBL422110 | — | Ki | = | 950.0 | nM | 6.02 |
| CHEMBL136836 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL136047 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL137471 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL344678 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL342229 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL345060 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL136364 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL136394 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL136199 | — | Ki | = | 2800.0 | nM | 5.55 |
| CHEMBL139013 | — | Ki | = | 2800.0 | nM | 5.55 |
| CHEMBL115940 | — | Ki | = | 3200.0 | nM | 5.50 |
| CHEMBL344026 | — | Ki | = | 4100.0 | nM | 5.39 |
| CHEMBL342193 | — | Ki | = | 4400.0 | nM | 5.36 |
| CHEMBL137508 | — | Ki | = | 9200.0 | nM | 5.04 |
| CHEMBL280982 | — | Ki | = | 9600.0 | nM | 5.02 |
| CHEMBL282038 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 17000.0 | nM | 4.77 |
| CHEMBL113 | CAFFEINE | Ki | = | 26000.0 | nM | 4.58 |
| CHEMBL21053 | — | Ki | = | 33000.0 | nM | 4.48 |
| CHEMBL26138 | — | Ki | > | 1000.0 | nM | - |