Assay Detail
Binding
CHEMBL908894
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]DPCPX from adenosine A1 receptor in rat cerebral cortex
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Tricyclic imidazoline derivatives as potent and selective adenosine A1 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 7.68 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL218458 | — | — | 1 | 9.22 |
| CHEMBL414157 | TONAPOFYLLINE | 3.0 | 1 | 9.00 |
| CHEMBL216269 | — | — | 1 | 8.40 |
| CHEMBL450341 | — | — | 1 | 8.22 |
| CHEMBL217268 | — | — | 1 | 8.08 |
| CHEMBL384279 | — | — | 1 | 8.00 |
| CHEMBL216200 | — | — | 1 | 7.98 |
| CHEMBL2113246 | — | — | 1 | 7.85 |
| CHEMBL217806 | — | — | 1 | 7.40 |
| CHEMBL217218 | — | — | 1 | 7.37 |
| CHEMBL386095 | — | — | 1 | 7.29 |
| CHEMBL217112 | — | — | 1 | 7.17 |
| CHEMBL439352 | — | — | 1 | 7.16 |
| CHEMBL218132 | — | — | 1 | 6.81 |
| CHEMBL387308 | — | — | 1 | 6.77 |
| CHEMBL216873 | — | — | 1 | 6.15 |
| CHEMBL216944 | — | — | 1 | - |
| CHEMBL217209 | — | — | 1 | - |
| CHEMBL216768 | — | — | 1 | - |
| CHEMBL217027 | — | — | 1 | - |
| CHEMBL218189 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL218458 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL414157 | TONAPOFYLLINE | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL216269 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL450341 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL217268 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL384279 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL216200 | — | Ki | = | 10.5 | nM | 7.98 |
| CHEMBL2113246 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL217806 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL217218 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL386095 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL217112 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL439352 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL218132 | — | Ki | = | 155.0 | nM | 6.81 |
| CHEMBL387308 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL216873 | — | Ki | = | 710.0 | nM | 6.15 |
| CHEMBL216944 | — | Ki | > | 100.0 | nM | - |
| CHEMBL217209 | — | Ki | > | 250.0 | nM | - |
| CHEMBL216768 | — | Ki | > | 250.0 | nM | - |
| CHEMBL217027 | — | Ki | > | 250.0 | nM | - |
| CHEMBL218189 | — | Ki | > | 100.0 | nM | - |