Assay Detail
Binding
CHEMBL887888
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Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortical membrane
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
N9-benzyl-substituted 1,3-dimethyl- and 1,3-dipropyl-pyrimido[2,1-f]purinediones: synthesis and structure-activity relationships at adenosine A1 and A2A receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 5.95 | 7.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL400620 | — | — | 1 | 7.05 |
| CHEMBL240507 | — | — | 1 | 6.75 |
| CHEMBL431770 | ISTRADEFYLLINE | 4.0 | 1 | 6.64 |
| CHEMBL400619 | — | — | 1 | 6.64 |
| CHEMBL240296 | — | — | 1 | 6.32 |
| CHEMBL398593 | — | — | 1 | 6.15 |
| CHEMBL240295 | — | — | 1 | 6.00 |
| CHEMBL241618 | — | — | 1 | 5.85 |
| CHEMBL399618 | — | — | 1 | 5.60 |
| CHEMBL240294 | — | — | 1 | 5.46 |
| CHEMBL401440 | — | — | 1 | 5.45 |
| CHEMBL240083 | — | — | 1 | 4.75 |
| CHEMBL113 | CAFFEINE | 4.0 | 1 | 4.73 |
| CHEMBL399414 | — | — | 1 | - |
| CHEMBL238418 | — | — | 1 | - |
| CHEMBL238417 | — | — | 1 | - |
| CHEMBL238636 | — | — | 1 | - |
| CHEMBL398385 | — | — | 1 | - |
| CHEMBL241617 | — | — | 1 | - |
| CHEMBL241616 | — | — | 1 | - |
| CHEMBL266451 | — | — | 1 | - |
| CHEMBL238419 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL400620 | — | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL240507 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL431770 | ISTRADEFYLLINE | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL400619 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL240296 | — | Ki | = | 480.0 | nM | 6.32 |
| CHEMBL398593 | — | Ki | = | 710.0 | nM | 6.15 |
| CHEMBL240295 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL241618 | — | Ki | = | 1420.0 | nM | 5.85 |
| CHEMBL399618 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL240294 | — | Ki | = | 3430.0 | nM | 5.46 |
| CHEMBL401440 | — | Ki | = | 3580.0 | nM | 5.45 |
| CHEMBL240083 | — | Ki | = | 17800.0 | nM | 4.75 |
| CHEMBL113 | CAFFEINE | Ki | = | 18800.0 | nM | 4.73 |
| CHEMBL399414 | — | Ki | > | 25000.0 | nM | - |
| CHEMBL238418 | — | Ki | > | 25000.0 | nM | - |
| CHEMBL238417 | — | Ki | >= | 25000.0 | nM | - |
| CHEMBL238636 | — | Ki | > | 2500.0 | nM | - |
| CHEMBL398385 | — | Ki | > | 2500.0 | nM | - |
| CHEMBL241617 | — | Ki | >= | 2500.0 | nM | - |
| CHEMBL241616 | — | Ki | > | 2500.0 | nM | - |
| CHEMBL266451 | — | Ki | >= | 25000.0 | nM | - |
| CHEMBL238419 | — | Ki | > | 25000.0 | nM | - |