Assay Detail
Functional
CHEMBL5126822
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Antagonist activity at adenosine A2A receptor (unknown origin)
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Adenosine receptor antagonists: Recent advances and therapeutic perspective.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 7.92 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL240624 | PRELADENANT | 3.0 | 1 | 9.30 |
| CHEMBL483688 | — | — | 1 | 9.26 |
| CHEMBL447664 | VIPADENANT | 2.0 | 1 | 8.89 |
| CHEMBL4740383 | ETRUMADENANT | 2.0 | 1 | 8.82 |
| CHEMBL113142 | ZM-241385 | — | 1 | 8.80 |
| CHEMBL4594442 | IMARADENANT | 2.0 | 1 | 8.77 |
| CHEMBL273807 | — | — | 1 | 8.71 |
| CHEMBL4297184 | CIFORADENANT | 2.0 | 1 | 8.47 |
| CHEMBL2105747 | TOZADENANT | 3.0 | 1 | 8.30 |
| CHEMBL260331 | — | — | 1 | 8.26 |
| CHEMBL404168 | — | — | 1 | 8.22 |
| CHEMBL431770 | ISTRADEFYLLINE | 4.0 | 1 | 7.92 |
| CHEMBL3694769 | PBF-509 | 1.0 | 1 | 7.30 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 5.77 |
| CHEMBL279898 | ENPROFYLLINE | 2.0 | 1 | 5.33 |
| CHEMBL113 | CAFFEINE | 4.0 | 1 | 4.63 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL240624 | PRELADENANT | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL483688 | — | Ki | = | 0.553 | nM | 9.26 |
| CHEMBL447664 | VIPADENANT | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL4740383 | ETRUMADENANT | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL113142 | ZM-241385 | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL4594442 | IMARADENANT | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL273807 | — | Ki | = | 1.97 | nM | 8.71 |
| CHEMBL4297184 | CIFORADENANT | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL2105747 | TOZADENANT | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL260331 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL404168 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL431770 | ISTRADEFYLLINE | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL3694769 | PBF-509 | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 1710.0 | nM | 5.77 |
| CHEMBL279898 | ENPROFYLLINE | Ki | = | 4730.0 | nM | 5.33 |
| CHEMBL113 | CAFFEINE | Ki | = | 23400.0 | nM | 4.63 |