Assay Detail
Binding
CHEMBL642256
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Displacement of [3H]CPX from Adenosine A1 receptor of bovine brain cerebral cortex membranes
12
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Tissue | Cerebral cortex |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
A1 adenosine receptor antagonists as ligands for positron emission tomography (PET) and single-photon emission tomography (SPET).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 9.34 | 10.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL152026 | — | — | 1 | 10.03 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 2 | 9.81 |
| CHEMBL148589 | — | — | 1 | 9.74 |
| CHEMBL152058 | — | — | 1 | 9.67 |
| CHEMBL152488 | — | — | 1 | 9.62 |
| CHEMBL152294 | — | — | 1 | 9.54 |
| CHEMBL284578 | — | — | 1 | 9.51 |
| CHEMBL357346 | — | — | 1 | 9.31 |
| CHEMBL34004 | — | — | 1 | 9.28 |
| CHEMBL346676 | — | — | 1 | 8.91 |
| CHEMBL356239 | — | — | 1 | 6.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL152026 | — | Ki | = | 0.094 | nM | 10.03 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 0.155 | nM | 9.81 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL148589 | — | Ki | = | 0.183 | nM | 9.74 |
| CHEMBL152058 | — | Ki | = | 0.216 | nM | 9.67 |
| CHEMBL152488 | — | Ki | = | 0.237 | nM | 9.62 |
| CHEMBL152294 | — | Ki | = | 0.286 | nM | 9.54 |
| CHEMBL284578 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL357346 | — | Ki | = | 0.493 | nM | 9.31 |
| CHEMBL34004 | — | Ki | = | 0.526 | nM | 9.28 |
| CHEMBL346676 | — | Ki | = | 1.23 | nM | 8.91 |
| CHEMBL356239 | — | Ki | = | 149.0 | nM | 6.83 |