Assay Detail
Binding
CHEMBL1074277
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Binding affinity to human adenosine A2A receptor
6
Total Activities
6
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
2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 6.17 | 7.92 |
| IC50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL457102 | — | — | 1 | 7.92 |
| CHEMBL592435 | DERENOFYLLINE | 2.0 | 1 | 6.40 |
| CHEMBL414157 | TONAPOFYLLINE | 3.0 | 1 | 5.19 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 5.17 |
| CHEMBL589080 | — | — | 1 | - |
| CHEMBL591235 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL457102 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL592435 | DERENOFYLLINE | Ki | = | 398.0 | nM | 6.40 |
| CHEMBL414157 | TONAPOFYLLINE | Ki | = | 6410.0 | nM | 5.19 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 6700.0 | nM | 5.17 |
| CHEMBL589080 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL591235 | — | IC50 | > | 100.0 | nM | - |