Assay Detail
Binding
CHEMBL642989
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Binding affinity towards adenosine A1 receptor using [3H]N-cyclohexyladenosine in rat whole brain membranes.
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Brain membranes |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
[1,2,4]Triazolo[4,3-a]quinoxalin-4-amines: a new class of A1 receptor selective adenosine antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 6.86 | 8.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL268071 | — | — | 1 | 8.14 |
| CHEMBL7271 | — | — | 1 | 7.55 |
| CHEMBL267400 | — | — | 1 | 7.47 |
| CHEMBL266978 | — | — | 1 | 7.41 |
| CHEMBL268801 | — | — | 1 | 7.36 |
| CHEMBL7454 | — | — | 1 | 7.26 |
| CHEMBL414401 | — | — | 1 | 7.24 |
| CHEMBL7472 | — | — | 1 | 7.10 |
| CHEMBL269044 | — | — | 1 | 6.74 |
| CHEMBL6958 | — | — | 1 | 6.62 |
| CHEMBL6890 | — | — | 1 | 6.58 |
| CHEMBL7219 | — | — | 1 | 6.48 |
| CHEMBL7325 | — | — | 1 | 6.20 |
| CHEMBL269318 | — | — | 1 | 5.64 |
| CHEMBL7033 | — | — | 1 | 5.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL268071 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL7271 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL267400 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL266978 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL268801 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL7454 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL414401 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL7472 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL269044 | — | Ki | = | 181.0 | nM | 6.74 |
| CHEMBL6958 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL6890 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL7219 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL7325 | — | Ki | = | 630.0 | nM | 6.20 |
| CHEMBL269318 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL7033 | — | Ki | = | 8900.0 | nM | 5.05 |