Assay Detail
Binding
CHEMBL1064297
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to rat adenosine A1 receptor
8
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| 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 | 7 | 7.84 | 9.72 |
| IC50 | 1 | 7.76 | 7.76 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL52333 | ROLOFYLLINE | 3.0 | 1 | 9.72 |
| CHEMBL414157 | TONAPOFYLLINE | 3.0 | 1 | 8.89 |
| CHEMBL592435 | DERENOFYLLINE | 2.0 | 1 | 8.60 |
| CHEMBL292917 | — | — | 1 | 8.18 |
| CHEMBL440115 | FK453 | 1.0 | 1 | 7.76 |
| CHEMBL305322 | — | — | 1 | 7.50 |
| CHEMBL60156 | — | — | 1 | 7.12 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 4.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL52333 | ROLOFYLLINE | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL414157 | TONAPOFYLLINE | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL592435 | DERENOFYLLINE | Ki | = | 2.51 | nM | 8.60 |
| CHEMBL292917 | — | Ki | = | 6.61 | nM | 8.18 |
| CHEMBL440115 | FK453 | IC50 | = | 17.2 | nM | 7.76 |
| CHEMBL305322 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL60156 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 14000.0 | nM | 4.85 |