Assay Detail
Binding
CHEMBL639744
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Tested for binding affinity against Adenosine A1 receptor from rat forebrain membranes, using N6-[3H]- cyclohexyladenosine as radioligand
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
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 | 9 | 7.91 | 9.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL82589 | — | — | 1 | 9.72 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 9.34 |
| CHEMBL116486 | — | — | 1 | 9.25 |
| CHEMBL84144 | — | — | 1 | 9.12 |
| CHEMBL84363 | — | — | 1 | 9.00 |
| CHEMBL418101 | — | — | 1 | 8.82 |
| CHEMBL27508 | — | — | 1 | 6.37 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 5.07 |
| CHEMBL113 | CAFFEINE | 4.0 | 1 | 4.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL82589 | — | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 0.46 | nM | 9.34 |
| CHEMBL116486 | — | Ki | = | 0.56 | nM | 9.25 |
| CHEMBL84144 | — | Ki | = | 0.75 | nM | 9.12 |
| CHEMBL84363 | — | Ki | = | 0.99 | nM | 9.00 |
| CHEMBL418101 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL27508 | — | Ki | = | 430.0 | nM | 6.37 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 8470.0 | nM | 5.07 |
| CHEMBL113 | CAFFEINE | Ki | = | 29100.0 | nM | 4.54 |