Assay Detail
Binding
CHEMBL636731
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Evaluated for the binding affinity towards the Adenosine A1 receptor in cerebral cortices of Sprague-Dawley male rats using [3H]CHA as radioligand.
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
4-Amino[1,2,4]triazolo[4,3-a]quinoxalines. A novel class of potent adenosine receptor antagonists and potential rapid-onset antidepressants.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.08 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL139000 | (R)-PIA | — | 1 | 8.62 |
| CHEMBL262083 | N6-PHENYLADENOSINE | — | 1 | 8.19 |
| CHEMBL420705 | (S)-PIA | — | 1 | 6.98 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 1 | 6.19 |
| CHEMBL260167 | — | — | 1 | 5.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL139000 | (R)-PIA | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL262083 | N6-PHENYLADENOSINE | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL420705 | (S)-PIA | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL260167 | — | IC50 | = | 3700.0 | nM | 5.43 |