Assay Detail
Binding
CHEMBL645214
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Binding affinity against Adenosine A1 receptor from guinea pig forebrain membranes by N6-[3H]- cyclohexyladenosine displacement.
19
Total Activities
19
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
Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine- or N6-((R)-phenylisopropyl)adenosine-induced cognitive disturbance.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 7.60 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL82589 | — | — | 1 | 8.89 |
| CHEMBL312857 | — | — | 1 | 8.62 |
| CHEMBL116486 | — | — | 1 | 8.57 |
| CHEMBL84363 | — | — | 1 | 8.52 |
| CHEMBL84144 | — | — | 1 | 8.46 |
| CHEMBL310557 | — | — | 1 | 8.25 |
| CHEMBL312352 | — | — | 1 | 8.24 |
| CHEMBL82417 | — | — | 1 | 8.21 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 8.19 |
| CHEMBL292904 | — | — | 1 | 8.18 |
| CHEMBL313780 | — | — | 1 | 7.92 |
| CHEMBL418101 | — | — | 1 | 7.89 |
| CHEMBL84545 | — | — | 1 | 7.82 |
| CHEMBL83822 | — | — | 1 | 7.64 |
| CHEMBL120350 | — | — | 1 | 6.92 |
| CHEMBL27508 | — | — | 1 | 5.82 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 4.64 |
| CHEMBL113 | CAFFEINE | 4.0 | 1 | 4.00 |
| CHEMBL27203 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL82589 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL312857 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL116486 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL84363 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL84144 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL310557 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL312352 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL82417 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL292904 | — | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL313780 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL418101 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL84545 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL83822 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL120350 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL27508 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 23000.0 | nM | 4.64 |
| CHEMBL113 | CAFFEINE | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL27203 | — | Ki | > | 100000.0 | nM | - |