Assay Detail
Binding
CHEMBL644094
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Displacement of specific [125 I]AB-MECA binding at human Adenosine A3 receptor expressed in HEK cells
27
Total Activities
27
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, 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 | 27 | 7.06 | 8.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL164321 | — | — | 1 | 8.38 |
| CHEMBL111086 | — | — | 1 | 8.08 |
| CHEMBL422184 | — | — | 1 | 8.02 |
| CHEMBL163488 | — | — | 1 | 7.92 |
| CHEMBL2112931 | — | — | 1 | 7.74 |
| CHEMBL111545 | — | — | 1 | 7.72 |
| CHEMBL321845 | — | — | 1 | 7.70 |
| CHEMBL163126 | — | — | 1 | 7.64 |
| CHEMBL164302 | — | — | 1 | 7.54 |
| CHEMBL162706 | — | — | 1 | 7.51 |
| CHEMBL350988 | — | — | 1 | 7.29 |
| CHEMBL163743 | — | — | 1 | 7.26 |
| CHEMBL164210 | — | — | 1 | 7.22 |
| CHEMBL162630 | — | — | 1 | 7.08 |
| CHEMBL163626 | — | — | 1 | 6.96 |
| CHEMBL162665 | — | — | 1 | 6.91 |
| CHEMBL159631 | — | — | 1 | 6.77 |
| CHEMBL164039 | — | — | 1 | 6.71 |
| CHEMBL163813 | — | — | 1 | 6.66 |
| CHEMBL349191 | — | — | 1 | 6.61 |
| CHEMBL348766 | — | — | 1 | 6.61 |
| CHEMBL162666 | — | — | 1 | 6.58 |
| CHEMBL164200 | — | — | 1 | 6.35 |
| CHEMBL162991 | — | — | 1 | 6.29 |
| CHEMBL164312 | — | — | 1 | 5.70 |
| CHEMBL440720 | — | — | 1 | 5.70 |
| CHEMBL163634 | — | — | 1 | 5.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL164321 | — | Ki | = | 4.22 | nM | 8.38 |
| CHEMBL111086 | — | Ki | = | 8.29 | nM | 8.08 |
| CHEMBL422184 | — | Ki | = | 9.67 | nM | 8.02 |
| CHEMBL163488 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL2112931 | — | Ki | = | 18.1 | nM | 7.74 |
| CHEMBL111545 | — | Ki | = | 18.9 | nM | 7.72 |
| CHEMBL321845 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL163126 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL164302 | — | Ki | = | 28.9 | nM | 7.54 |
| CHEMBL162706 | — | Ki | = | 31.1 | nM | 7.51 |
| CHEMBL350988 | — | Ki | = | 51.1 | nM | 7.29 |
| CHEMBL163743 | — | Ki | = | 55.1 | nM | 7.26 |
| CHEMBL164210 | — | Ki | = | 59.9 | nM | 7.22 |
| CHEMBL162630 | — | Ki | = | 82.8 | nM | 7.08 |
| CHEMBL163626 | — | Ki | = | 109.0 | nM | 6.96 |
| CHEMBL162665 | — | Ki | = | 124.0 | nM | 6.91 |
| CHEMBL159631 | — | Ki | = | 169.0 | nM | 6.77 |
| CHEMBL164039 | — | Ki | = | 193.0 | nM | 6.71 |
| CHEMBL163813 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL349191 | — | Ki | = | 243.0 | nM | 6.61 |
| CHEMBL348766 | — | Ki | = | 248.0 | nM | 6.61 |
| CHEMBL162666 | — | Ki | = | 262.0 | nM | 6.58 |
| CHEMBL164200 | — | Ki | = | 446.0 | nM | 6.35 |
| CHEMBL162991 | — | Ki | = | 517.0 | nM | 6.29 |
| CHEMBL164312 | — | Ki | = | 1990.0 | nM | 5.70 |
| CHEMBL440720 | — | Ki | = | 2020.0 | nM | 5.70 |
| CHEMBL163634 | — | Ki | = | 2640.0 | nM | 5.58 |