Assay Detail
Binding
CHEMBL948831
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Displacement of [3H]MSX-2 from human recombinant adenosine A2A receptor expressed in CHO cells
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 6.83 | 8.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL483261 | — | — | 1 | 8.19 |
| CHEMBL486478 | — | — | 1 | 7.64 |
| CHEMBL483487 | — | — | 1 | 7.32 |
| CHEMBL519390 | — | — | 1 | 7.16 |
| CHEMBL520297 | — | — | 1 | 7.04 |
| CHEMBL486282 | — | — | 1 | 7.03 |
| CHEMBL483065 | — | — | 1 | 6.99 |
| CHEMBL486893 | — | — | 1 | 6.95 |
| CHEMBL484899 | — | — | 1 | 6.84 |
| CHEMBL486479 | — | — | 1 | 6.84 |
| CHEMBL519813 | — | — | 1 | 6.82 |
| CHEMBL483469 | — | — | 1 | 6.79 |
| CHEMBL482648 | — | — | 1 | 6.63 |
| CHEMBL488541 | — | — | 1 | 6.57 |
| CHEMBL484900 | — | — | 1 | 6.56 |
| CHEMBL486688 | — | — | 1 | 6.51 |
| CHEMBL482436 | — | — | 1 | 6.48 |
| CHEMBL482855 | — | — | 1 | 6.48 |
| CHEMBL212625 | — | — | 1 | 6.32 |
| CHEMBL486481 | — | — | 1 | 5.43 |
| CHEMBL482638 | — | — | 1 | - |
| CHEMBL518972 | — | — | 1 | - |
| CHEMBL483688 | — | — | 1 | - |
| CHEMBL519253 | — | — | 1 | - |
| CHEMBL520899 | — | — | 1 | - |
| CHEMBL519556 | — | — | 1 | - |
| CHEMBL520617 | — | — | 1 | - |
| CHEMBL488542 | — | — | 1 | - |
| CHEMBL486281 | — | — | 1 | - |
| CHEMBL520830 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL483261 | — | Ki | = | 6.49 | nM | 8.19 |
| CHEMBL486478 | — | Ki | = | 22.7 | nM | 7.64 |
| CHEMBL483487 | — | Ki | = | 48.4 | nM | 7.32 |
| CHEMBL519390 | — | Ki | = | 69.4 | nM | 7.16 |
| CHEMBL520297 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL486282 | — | Ki | = | 94.5 | nM | 7.03 |
| CHEMBL483065 | — | Ki | = | 102.0 | nM | 6.99 |
| CHEMBL486893 | — | Ki | = | 112.0 | nM | 6.95 |
| CHEMBL484899 | — | Ki | = | 144.0 | nM | 6.84 |
| CHEMBL486479 | — | Ki | = | 145.0 | nM | 6.84 |
| CHEMBL519813 | — | Ki | = | 152.0 | nM | 6.82 |
| CHEMBL483469 | — | Ki | = | 161.0 | nM | 6.79 |
| CHEMBL482648 | — | Ki | = | 236.0 | nM | 6.63 |
| CHEMBL488541 | — | Ki | = | 271.0 | nM | 6.57 |
| CHEMBL484900 | — | Ki | = | 278.0 | nM | 6.56 |
| CHEMBL486688 | — | Ki | = | 306.0 | nM | 6.51 |
| CHEMBL482436 | — | Ki | = | 333.0 | nM | 6.48 |
| CHEMBL482855 | — | Ki | = | 328.0 | nM | 6.48 |
| CHEMBL212625 | — | Ki | = | 484.0 | nM | 6.32 |
| CHEMBL486481 | — | Ki | = | 3720.0 | nM | 5.43 |
| CHEMBL482638 | — | Ki | - | — | - | |
| CHEMBL518972 | — | Ki | - | — | - | |
| CHEMBL483688 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL519253 | — | Ki | - | — | - | |
| CHEMBL520899 | — | Ki | - | — | - | |
| CHEMBL519556 | — | Ki | - | — | - | |
| CHEMBL520617 | — | Ki | - | — | - | |
| CHEMBL488542 | — | Ki | - | — | - | |
| CHEMBL486281 | — | Ki | - | — | - | |
| CHEMBL520830 | — | Ki | - | — | - |