Assay Detail
Binding
CHEMBL639432
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Binding affinity at Adenosine A1 receptor in rat brain membranes by [3H]PIA displacement.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Brain membranes |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 5.11 | 6.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL75772 | — | — | 1 | 6.29 |
| CHEMBL72862 | — | — | 1 | 6.22 |
| CHEMBL309490 | GALANGIN | — | 1 | 6.06 |
| CHEMBL76273 | — | — | 1 | 5.96 |
| CHEMBL449090 | — | — | 1 | 5.72 |
| CHEMBL74975 | — | — | 1 | 5.61 |
| CHEMBL75897 | 2'-HYDROXY-FLAVANONE | — | 1 | 5.58 |
| CHEMBL275638 | FLAVONE | 2.0 | 1 | 5.48 |
| CHEMBL76933 | — | — | 1 | 5.13 |
| CHEMBL74852 | — | — | 1 | 5.09 |
| CHEMBL72617 | ARTOCARPIN | — | 1 | 5.04 |
| CHEMBL73933 | 4'-HYDROXY-FLAVANONE | — | 1 | 4.94 |
| CHEMBL28626 | MORIN | — | 1 | 4.86 |
| CHEMBL75169 | — | — | 1 | 4.56 |
| CHEMBL274318 | FLAVANONE | — | 1 | 4.50 |
| CHEMBL75590 | — | — | 1 | 4.49 |
| CHEMBL74505 | — | — | 1 | 4.49 |
| CHEMBL76874 | — | — | 1 | 4.45 |
| CHEMBL76128 | — | — | 1 | 4.40 |
| CHEMBL74328 | — | — | 1 | 4.30 |
| CHEMBL75002 | — | — | 1 | 4.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL75772 | — | Ki | = | 509.0 | nM | 6.29 |
| CHEMBL72862 | — | Ki | = | 603.0 | nM | 6.22 |
| CHEMBL309490 | GALANGIN | Ki | = | 863.0 | nM | 6.06 |
| CHEMBL76273 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL449090 | — | Ki | = | 1890.0 | nM | 5.72 |
| CHEMBL74975 | — | Ki | = | 2480.0 | nM | 5.61 |
| CHEMBL75897 | 2'-HYDROXY-FLAVANONE | Ki | = | 2640.0 | nM | 5.58 |
| CHEMBL275638 | FLAVONE | Ki | = | 3280.0 | nM | 5.48 |
| CHEMBL76933 | — | Ki | = | 7320.0 | nM | 5.13 |
| CHEMBL74852 | — | Ki | = | 8180.0 | nM | 5.09 |
| CHEMBL72617 | ARTOCARPIN | Ki | = | 9090.0 | nM | 5.04 |
| CHEMBL73933 | 4'-HYDROXY-FLAVANONE | Ki | = | 11500.0 | nM | 4.94 |
| CHEMBL28626 | MORIN | Ki | = | 13800.0 | nM | 4.86 |
| CHEMBL75169 | — | Ki | = | 27600.0 | nM | 4.56 |
| CHEMBL274318 | FLAVANONE | Ki | = | 32000.0 | nM | 4.50 |
| CHEMBL75590 | — | Ki | = | 32600.0 | nM | 4.49 |
| CHEMBL74505 | — | Ki | = | 32300.0 | nM | 4.49 |
| CHEMBL76874 | — | Ki | = | 35600.0 | nM | 4.45 |
| CHEMBL76128 | — | Ki | = | 40000.0 | nM | 4.40 |
| CHEMBL74328 | — | Ki | = | 50300.0 | nM | 4.30 |
| CHEMBL75002 | — | Ki | = | 91900.0 | nM | 4.04 |