Assay Detail
Binding
CHEMBL642197
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Binding affinity against adenosine A1 receptor in rat cortex by using [3H]- PIA as a radioligand
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cortex |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
N6,9-disubstituted adenines: potent, selective antagonists at the A1 adenosine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 25 | 5.36 | 6.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL301574 | — | — | 1 | 6.36 |
| CHEMBL88788 | — | — | 1 | 6.28 |
| CHEMBL48278 | — | — | 1 | 6.27 |
| CHEMBL95332 | — | — | 1 | 6.03 |
| CHEMBL95617 | — | — | 1 | 5.92 |
| CHEMBL95913 | — | — | 1 | 5.77 |
| CHEMBL294590 | — | — | 1 | 5.75 |
| CHEMBL321753 | — | — | 1 | 5.70 |
| CHEMBL1202925 | — | — | 1 | 5.60 |
| CHEMBL99407 | — | — | 1 | 5.55 |
| CHEMBL318453 | — | — | 1 | 5.48 |
| CHEMBL320370 | — | — | 1 | 5.48 |
| CHEMBL95936 | — | — | 1 | 5.33 |
| CHEMBL98779 | — | — | 1 | 5.16 |
| CHEMBL96015 | — | — | 1 | 5.16 |
| CHEMBL321749 | — | — | 1 | 5.16 |
| CHEMBL96014 | — | — | 1 | 5.14 |
| CHEMBL319010 | — | — | 1 | 5.06 |
| CHEMBL1202924 | — | — | 1 | 4.96 |
| CHEMBL62756 | — | — | 1 | 4.72 |
| CHEMBL317398 | — | — | 1 | 4.64 |
| CHEMBL64239 | — | — | 1 | 4.55 |
| CHEMBL304009 | — | — | 1 | 4.34 |
| CHEMBL65976 | — | — | 1 | 4.16 |
| CHEMBL95897 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL301574 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL88788 | — | Ki | = | 530.0 | nM | 6.28 |
| CHEMBL48278 | — | Ki | = | 540.0 | nM | 6.27 |
| CHEMBL95332 | — | Ki | = | 940.0 | nM | 6.03 |
| CHEMBL95617 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL95913 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL294590 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL321753 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL1202925 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL99407 | — | Ki | = | 2800.0 | nM | 5.55 |
| CHEMBL318453 | — | Ki | = | 3300.0 | nM | 5.48 |
| CHEMBL320370 | — | Ki | = | 3300.0 | nM | 5.48 |
| CHEMBL95936 | — | Ki | = | 4700.0 | nM | 5.33 |
| CHEMBL98779 | — | Ki | = | 7000.0 | nM | 5.16 |
| CHEMBL96015 | — | Ki | = | 6900.0 | nM | 5.16 |
| CHEMBL321749 | — | Ki | = | 6900.0 | nM | 5.16 |
| CHEMBL96014 | — | Ki | = | 7200.0 | nM | 5.14 |
| CHEMBL319010 | — | Ki | = | 8700.0 | nM | 5.06 |
| CHEMBL1202924 | — | Ki | = | 11000.0 | nM | 4.96 |
| CHEMBL62756 | — | Ki | = | 19000.0 | nM | 4.72 |
| CHEMBL317398 | — | Ki | = | 23000.0 | nM | 4.64 |
| CHEMBL64239 | — | Ki | = | 28000.0 | nM | 4.55 |
| CHEMBL304009 | — | Ki | = | 46000.0 | nM | 4.34 |
| CHEMBL65976 | — | Ki | = | 69000.0 | nM | 4.16 |
| CHEMBL95897 | — | Ki | > | 100000.0 | nM | - |