Assay Detail
Binding
CHEMBL947856
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Binding affinity to human adenosine A2B receptor
14
Total Activities
14
Compounds Tested
2
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 | 7.69 | 9.39 |
| Kd | 4 | 8.68 | 9.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL500634 | — | — | 1 | 9.77 |
| CHEMBL485862 | — | — | 1 | 9.39 |
| CHEMBL1628266 | — | — | 1 | 8.95 |
| CHEMBL490262 | — | — | 1 | 8.92 |
| CHEMBL506685 | — | — | 1 | 8.78 |
| CHEMBL273807 | — | — | 1 | 8.71 |
| CHEMBL212625 | — | — | 1 | 8.44 |
| CHEMBL260331 | — | — | 1 | 8.26 |
| CHEMBL450826 | — | — | 1 | 7.96 |
| CHEMBL260933 | GS 6201 | 1.0 | 1 | 7.66 |
| CHEMBL452924 | — | — | 1 | 7.27 |
| CHEMBL521280 | — | — | 1 | 7.22 |
| CHEMBL279898 | ENPROFYLLINE | 2.0 | 1 | 5.19 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 5.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL500634 | — | Kd | = | 0.17 | nM | 9.77 |
| CHEMBL485862 | — | Ki | = | 0.41 | nM | 9.39 |
| CHEMBL1628266 | — | Kd | = | 1.13 | nM | 8.95 |
| CHEMBL490262 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL506685 | — | Kd | = | 1.65 | nM | 8.78 |
| CHEMBL273807 | — | Ki | = | 1.97 | nM | 8.71 |
| CHEMBL212625 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL260331 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL450826 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL260933 | GS 6201 | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL452924 | — | Ki | = | 53.4 | nM | 7.27 |
| CHEMBL521280 | — | Kd | = | 60.0 | nM | 7.22 |
| CHEMBL279898 | ENPROFYLLINE | Ki | = | 6400.0 | nM | 5.19 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 7850.0 | nM | 5.11 |