Assay Detail
Binding
CHEMBL3267349
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Inhibition of human recombinant adenosine A1 receptor
39
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Adenosine A2A receptor as a drug discovery target.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 39 | 6.44 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2165804 | — | — | 1 | 8.05 |
| CHEMBL401321 | — | — | 1 | 7.99 |
| CHEMBL261203 | — | — | 1 | 7.77 |
| CHEMBL2398482 | — | — | 1 | 7.62 |
| CHEMBL2024119 | — | — | 1 | 7.51 |
| CHEMBL401895 | — | — | 1 | 7.40 |
| CHEMBL564473 | — | — | 1 | 7.38 |
| CHEMBL447664 | VIPADENANT | 2.0 | 1 | 7.17 |
| CHEMBL487553 | — | — | 1 | 7.11 |
| CHEMBL197669 | ST1535 | 1.0 | 1 | 7.10 |
| CHEMBL609578 | — | — | 1 | 6.88 |
| CHEMBL259832 | — | — | 1 | 6.77 |
| CHEMBL2398486 | — | — | 1 | 6.72 |
| CHEMBL407307 | — | — | 1 | 6.68 |
| CHEMBL411329 | (R,S)-MEFLOQUINE | — | 1 | 6.61 |
| CHEMBL113142 | ZM-241385 | — | 1 | 6.59 |
| CHEMBL1370747 | — | — | 1 | 6.57 |
| CHEMBL513364 | — | — | 1 | 6.45 |
| CHEMBL520782 | — | — | 1 | 6.39 |
| CHEMBL17127 | SCH-58261 | — | 1 | 6.26 |
| CHEMBL395472 | — | — | 1 | 6.22 |
| CHEMBL482329 | — | — | 1 | 5.95 |
| CHEMBL2105747 | TOZADENANT | 3.0 | 1 | 5.87 |
| CHEMBL246675 | — | — | 1 | 5.87 |
| CHEMBL1762515 | — | — | 1 | 5.85 |
| CHEMBL1762513 | — | — | 1 | 5.85 |
| CHEMBL240624 | PRELADENANT | 3.0 | 2 | 5.83 |
| CHEMBL271202 | — | — | 1 | 5.70 |
| CHEMBL3260726 | — | — | 1 | 5.68 |
| CHEMBL431770 | ISTRADEFYLLINE | 4.0 | 1 | 5.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2165804 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL401321 | — | Ki | = | 10.2 | nM | 7.99 |
| CHEMBL261203 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL2398482 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL2024119 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL401895 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL564473 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL447664 | VIPADENANT | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL487553 | — | Ki | = | 77.2 | nM | 7.11 |
| CHEMBL197669 | ST1535 | Ki | = | 79.2 | nM | 7.10 |
| CHEMBL609578 | — | Ki | = | 133.0 | nM | 6.88 |
| CHEMBL259832 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL2398486 | — | Ki | = | 192.0 | nM | 6.72 |
| CHEMBL407307 | — | Ki | = | 207.0 | nM | 6.68 |
| CHEMBL411329 | (R,S)-MEFLOQUINE | Ki | = | 244.0 | nM | 6.61 |
| CHEMBL113142 | ZM-241385 | Ki | = | 255.0 | nM | 6.59 |
| CHEMBL1370747 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL513364 | — | Ki | = | 358.0 | nM | 6.45 |
| CHEMBL520782 | — | Ki | = | 406.0 | nM | 6.39 |
| CHEMBL17127 | SCH-58261 | Ki | = | 549.0 | nM | 6.26 |
| CHEMBL395472 | — | Ki | = | 602.0 | nM | 6.22 |
| CHEMBL482329 | — | Ki | = | 1116.0 | nM | 5.95 |
| CHEMBL2105747 | TOZADENANT | Ki | = | 1350.0 | nM | 5.87 |
| CHEMBL246675 | — | Ki | = | 1361.0 | nM | 5.87 |
| CHEMBL1762515 | — | Ki | = | 1405.0 | nM | 5.85 |
| CHEMBL1762513 | — | Ki | = | 1398.0 | nM | 5.85 |
| CHEMBL240624 | PRELADENANT | Ki | = | 1474.0 | nM | 5.83 |
| CHEMBL271202 | — | Ki | = | 1998.0 | nM | 5.70 |
| CHEMBL3260726 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL431770 | ISTRADEFYLLINE | Ki | = | 2830.0 | nM | 5.55 |
| CHEMBL3260725 | — | Ki | = | 8775.0 | nM | 5.06 |
| CHEMBL3260728 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL3260727 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL113 | CAFFEINE | Ki | = | 44900.0 | nM | 4.35 |
| CHEMBL598251 | — | Ki | - | — | - | |
| CHEMBL240624 | PRELADENANT | Ki | > | 996.0 | nM | - |
| CHEMBL3260731 | — | Ki | - | — | - | |
| CHEMBL3260730 | — | Ki | - | — | - | |
| CHEMBL3260729 | — | Ki | - | — | - |