Assay Detail
Binding
CHEMBL642187
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Displacement of specific [3H]-CGS- 21680R-PIA binding to Adenosine A1 receptor in rat brain membranes.
29
Total Activities
29
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, CoMFA analysis, and receptor docking of 3,5-diacyl-2, 4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 29 | 5.12 | 7.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL321845 | — | — | 1 | 7.39 |
| CHEMBL349191 | — | — | 1 | 6.31 |
| CHEMBL350201 | — | — | 1 | 5.28 |
| CHEMBL164200 | — | — | 1 | 5.25 |
| CHEMBL163634 | — | — | 1 | 5.24 |
| CHEMBL164312 | — | — | 1 | 5.24 |
| CHEMBL352083 | — | — | 1 | 5.23 |
| CHEMBL422184 | — | — | 1 | 5.22 |
| CHEMBL111086 | — | — | 1 | 5.11 |
| CHEMBL164302 | — | — | 1 | 5.09 |
| CHEMBL164210 | — | — | 1 | 5.09 |
| CHEMBL2112931 | — | — | 1 | 5.08 |
| CHEMBL163743 | — | — | 1 | 5.08 |
| CHEMBL162666 | — | — | 1 | 5.04 |
| CHEMBL159631 | — | — | 1 | 5.04 |
| CHEMBL162665 | — | — | 1 | 5.01 |
| CHEMBL350988 | — | — | 1 | 4.97 |
| CHEMBL350419 | — | — | 1 | 4.95 |
| CHEMBL164321 | — | — | 1 | 4.94 |
| CHEMBL162630 | — | — | 1 | 4.90 |
| CHEMBL164039 | — | — | 1 | 4.88 |
| CHEMBL163126 | — | — | 1 | 4.87 |
| CHEMBL111545 | — | — | 1 | 4.81 |
| CHEMBL163626 | — | — | 1 | 4.80 |
| CHEMBL348766 | — | — | 1 | 4.78 |
| CHEMBL347423 | — | — | 1 | 4.70 |
| CHEMBL163488 | — | — | 1 | 4.60 |
| CHEMBL162706 | — | — | 1 | 4.39 |
| CHEMBL163813 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL321845 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL349191 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL350201 | — | Ki | = | 5240.0 | nM | 5.28 |
| CHEMBL164200 | — | Ki | = | 5680.0 | nM | 5.25 |
| CHEMBL163634 | — | Ki | = | 5710.0 | nM | 5.24 |
| CHEMBL164312 | — | Ki | = | 5790.0 | nM | 5.24 |
| CHEMBL352083 | — | Ki | = | 5940.0 | nM | 5.23 |
| CHEMBL422184 | — | Ki | = | 6050.0 | nM | 5.22 |
| CHEMBL111086 | — | Ki | = | 7770.0 | nM | 5.11 |
| CHEMBL164302 | — | Ki | = | 8200.0 | nM | 5.09 |
| CHEMBL164210 | — | Ki | = | 8090.0 | nM | 5.09 |
| CHEMBL2112931 | — | Ki | = | 8290.0 | nM | 5.08 |
| CHEMBL163743 | — | Ki | = | 8220.0 | nM | 5.08 |
| CHEMBL162666 | — | Ki | = | 9040.0 | nM | 5.04 |
| CHEMBL159631 | — | Ki | = | 9060.0 | nM | 5.04 |
| CHEMBL162665 | — | Ki | = | 9800.0 | nM | 5.01 |
| CHEMBL350988 | — | Ki | = | 10800.0 | nM | 4.97 |
| CHEMBL350419 | — | Ki | = | 11200.0 | nM | 4.95 |
| CHEMBL164321 | — | Ki | = | 11500.0 | nM | 4.94 |
| CHEMBL162630 | — | Ki | = | 12600.0 | nM | 4.90 |
| CHEMBL164039 | — | Ki | = | 13200.0 | nM | 4.88 |
| CHEMBL163126 | — | Ki | = | 13500.0 | nM | 4.87 |
| CHEMBL111545 | — | Ki | = | 15600.0 | nM | 4.81 |
| CHEMBL163626 | — | Ki | = | 16000.0 | nM | 4.80 |
| CHEMBL348766 | — | Ki | = | 16500.0 | nM | 4.78 |
| CHEMBL347423 | — | Ki | = | 19800.0 | nM | 4.70 |
| CHEMBL163488 | — | Ki | = | 25100.0 | nM | 4.60 |
| CHEMBL162706 | — | Ki | = | 41000.0 | nM | 4.39 |
| CHEMBL163813 | — | Ki | = | 113000.0 | nM | - |