Assay Detail
Binding
CHEMBL641515
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Binding affinity against human adenosine A3 receptor in HEK293 cells using [125I]AB-MECA 21680 radioligand.
38
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| 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 | 38 | 5.07 | 6.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL76273 | — | — | 1 | 6.50 |
| CHEMBL72862 | — | — | 1 | 6.44 |
| CHEMBL307459 | — | — | 1 | 6.25 |
| CHEMBL449090 | — | — | 1 | 6.13 |
| CHEMBL309566 | — | — | 1 | 6.13 |
| CHEMBL76874 | — | — | 1 | 5.94 |
| CHEMBL75772 | — | — | 1 | 5.92 |
| CHEMBL75169 | — | — | 1 | 5.58 |
| CHEMBL309490 | GALANGIN | — | 1 | 5.50 |
| CHEMBL74852 | — | — | 1 | 5.47 |
| CHEMBL76128 | — | — | 1 | 5.40 |
| CHEMBL72617 | ARTOCARPIN | — | 1 | 5.34 |
| CHEMBL73648 | MORIN PENTAETHYL ETHER | — | 1 | 5.32 |
| CHEMBL74248 | — | — | 1 | 5.28 |
| CHEMBL75897 | 2'-HYDROXY-FLAVANONE | — | 1 | 5.22 |
| CHEMBL74505 | — | — | 1 | 5.14 |
| CHEMBL74328 | — | — | 2 | 5.09 |
| CHEMBL75590 | — | — | 1 | 5.08 |
| CHEMBL74489 | — | — | 1 | 5.04 |
| CHEMBL74975 | — | — | 1 | 4.94 |
| CHEMBL75126 | — | — | 1 | 4.89 |
| CHEMBL275638 | FLAVONE | 2.0 | 1 | 4.77 |
| CHEMBL305858 | — | — | 1 | 4.72 |
| CHEMBL74330 | — | — | 1 | 4.68 |
| CHEMBL72166 | — | — | 1 | 4.66 |
| CHEMBL75141 | — | — | 1 | 4.64 |
| CHEMBL75773 | — | — | 1 | 4.60 |
| CHEMBL74430 | — | — | 1 | 4.55 |
| CHEMBL293478 | 6-CHLOROFLAVONE | — | 1 | 4.50 |
| CHEMBL28626 | MORIN | — | 1 | 4.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL76273 | — | Ki | = | 317.0 | nM | 6.50 |
| CHEMBL72862 | — | Ki | = | 364.0 | nM | 6.44 |
| CHEMBL307459 | — | Ki | = | 561.0 | nM | 6.25 |
| CHEMBL309566 | — | Ki | = | 741.0 | nM | 6.13 |
| CHEMBL449090 | — | Ki | = | 748.0 | nM | 6.13 |
| CHEMBL76874 | — | Ki | = | 1160.0 | nM | 5.94 |
| CHEMBL75772 | — | Ki | = | 1210.0 | nM | 5.92 |
| CHEMBL75169 | — | Ki | = | 2650.0 | nM | 5.58 |
| CHEMBL309490 | GALANGIN | Ki | = | 3150.0 | nM | 5.50 |
| CHEMBL74852 | — | Ki | = | 3400.0 | nM | 5.47 |
| CHEMBL76128 | — | Ki | = | 3950.0 | nM | 5.40 |
| CHEMBL72617 | ARTOCARPIN | Ki | = | 4590.0 | nM | 5.34 |
| CHEMBL73648 | MORIN PENTAETHYL ETHER | Ki | = | 4830.0 | nM | 5.32 |
| CHEMBL74248 | — | Ki | = | 5240.0 | nM | 5.28 |
| CHEMBL75897 | 2'-HYDROXY-FLAVANONE | Ki | = | 6070.0 | nM | 5.22 |
| CHEMBL74505 | — | Ki | = | 7270.0 | nM | 5.14 |
| CHEMBL74328 | — | Ki | = | 8170.0 | nM | 5.09 |
| CHEMBL75590 | — | Ki | = | 8280.0 | nM | 5.08 |
| CHEMBL74489 | — | Ki | = | 9180.0 | nM | 5.04 |
| CHEMBL74975 | — | Ki | = | 11500.0 | nM | 4.94 |
| CHEMBL75126 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL275638 | FLAVONE | Ki | = | 16900.0 | nM | 4.77 |
| CHEMBL305858 | — | Ki | = | 19000.0 | nM | 4.72 |
| CHEMBL74330 | — | Ki | = | 21100.0 | nM | 4.68 |
| CHEMBL72166 | — | Ki | = | 22000.0 | nM | 4.66 |
| CHEMBL75141 | — | Ki | = | 23000.0 | nM | 4.64 |
| CHEMBL74328 | — | Ki | = | 24000.0 | nM | 4.62 |
| CHEMBL75773 | — | Ki | = | 25000.0 | nM | 4.60 |
| CHEMBL74430 | — | Ki | = | 28000.0 | nM | 4.55 |
| CHEMBL293478 | 6-CHLOROFLAVONE | Ki | = | 32000.0 | nM | 4.50 |
| CHEMBL28626 | MORIN | Ki | = | 34000.0 | nM | 4.47 |
| CHEMBL73933 | 4'-HYDROXY-FLAVANONE | Ki | = | 42800.0 | nM | 4.37 |
| CHEMBL78326 | — | Ki | = | 45500.0 | nM | 4.34 |
| CHEMBL75200 | — | Ki | = | 48000.0 | nM | 4.32 |
| CHEMBL76933 | — | Ki | = | 50100.0 | nM | 4.30 |
| CHEMBL274318 | FLAVANONE | Ki | = | 50100.0 | nM | 4.30 |
| CHEMBL45176 | VISNAGIN | Ki | = | 60000.0 | nM | 4.22 |
| CHEMBL75514 | — | Ki | = | 88900.0 | nM | 4.05 |