Assay Detail
Binding
CHEMBL640350
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Inhibition of N6-[3H]cyclohexyladenosine binding to guinea pig forebrain membrane Adenosine A1 receptor
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
8-Polycycloalkyl-1,3-dipropylxanthines as potent and selective antagonists for A1-adenosine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 7.91 | 9.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 1 | 9.49 |
| CHEMBL489640 | — | — | 1 | 9.15 |
| CHEMBL605856 | — | — | 1 | 9.12 |
| CHEMBL2093942 | — | — | 1 | 9.10 |
| CHEMBL2094076 | — | — | 1 | 8.89 |
| CHEMBL415321 | — | — | 1 | 8.36 |
| CHEMBL172950 | — | — | 1 | 8.25 |
| CHEMBL321507 | — | — | 1 | 7.82 |
| CHEMBL605066 | — | — | 1 | 7.80 |
| CHEMBL320147 | — | — | 1 | 6.43 |
| CHEMBL157655 | — | — | 1 | 5.85 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 4.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL489640 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL605856 | — | Ki | = | 0.75 | nM | 9.12 |
| CHEMBL2093942 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL2094076 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL415321 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL172950 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL321507 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL605066 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL320147 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL157655 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 23000.0 | nM | 4.64 |