Assay Detail
Binding
CHEMBL947857
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Binding affinity to human adenosine A3 receptor
10
Total Activities
10
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
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 | 10 | 5.84 | 6.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL490262 | — | — | 1 | 6.38 |
| CHEMBL485862 | — | — | 1 | 6.35 |
| CHEMBL273807 | — | — | 1 | 6.24 |
| CHEMBL260933 | GS 6201 | 1.0 | 1 | 5.97 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 4.28 |
| CHEMBL260331 | — | — | 1 | - |
| CHEMBL450826 | — | — | 1 | - |
| CHEMBL212625 | — | — | 1 | - |
| CHEMBL452924 | — | — | 1 | - |
| CHEMBL279898 | ENPROFYLLINE | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL490262 | — | Ki | = | 422.0 | nM | 6.38 |
| CHEMBL485862 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL273807 | — | Ki | = | 570.0 | nM | 6.24 |
| CHEMBL260933 | GS 6201 | Ki | = | 1070.0 | nM | 5.97 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 52300.0 | nM | 4.28 |
| CHEMBL260331 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL450826 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL212625 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL452924 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL279898 | ENPROFYLLINE | Ki | = | 158000.0 | nM | - |