Assay Detail
Binding
CHEMBL2174885
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Displacement of [125I]I-AB-MECA from human A3 adenosine receptor expressed in CHO cells after 60 min Packard Cobra 2 gamma-counter
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structural sweet spot for A1 adenosine receptor activation by truncated (N)-methanocarba nucleosides: receptor docking and potent anticonvulsant activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 6.47 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2012684 | — | — | 1 | 8.05 |
| CHEMBL1512545 | — | — | 1 | 7.91 |
| CHEMBL2170795 | — | — | 1 | 7.77 |
| CHEMBL2170797 | — | — | 1 | 7.16 |
| CHEMBL2012685 | — | — | 1 | 6.96 |
| CHEMBL2170785 | — | — | 1 | 6.82 |
| CHEMBL2012672 | — | — | 1 | 6.80 |
| CHEMBL2170796 | — | — | 1 | 6.74 |
| CHEMBL2012686 | — | — | 1 | 6.33 |
| CHEMBL2170798 | — | — | 1 | 6.31 |
| CHEMBL2170792 | — | — | 1 | 6.26 |
| CHEMBL2012680 | — | — | 1 | 6.22 |
| CHEMBL2170799 | — | — | 1 | 6.19 |
| CHEMBL2170800 | — | — | 1 | 6.17 |
| CHEMBL2170787 | — | — | 1 | 6.11 |
| CHEMBL2170786 | — | — | 1 | 6.11 |
| CHEMBL2170793 | — | — | 1 | 6.10 |
| CHEMBL2170788 | — | — | 1 | 5.76 |
| CHEMBL2170791 | — | — | 1 | 5.75 |
| CHEMBL2170794 | — | — | 1 | 5.66 |
| CHEMBL2170790 | — | — | 1 | 5.55 |
| CHEMBL2170789 | — | — | 1 | 5.53 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2012684 | — | Ki | = | 8.9 | nM | 8.05 |
| CHEMBL1512545 | — | Ki | = | 12.4 | nM | 7.91 |
| CHEMBL2170795 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL2170797 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL2012685 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL2170785 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL2012672 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL2170796 | — | Ki | = | 182.0 | nM | 6.74 |
| CHEMBL2012686 | — | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL2170798 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL2170792 | — | Ki | = | 550.0 | nM | 6.26 |
| CHEMBL2012680 | — | Ki | = | 606.0 | nM | 6.22 |
| CHEMBL2170799 | — | Ki | = | 640.0 | nM | 6.19 |
| CHEMBL2170800 | — | Ki | = | 670.0 | nM | 6.17 |
| CHEMBL2170787 | — | Ki | = | 780.0 | nM | 6.11 |
| CHEMBL2170786 | — | Ki | = | 780.0 | nM | 6.11 |
| CHEMBL2170793 | — | Ki | = | 790.0 | nM | 6.10 |
| CHEMBL2170788 | — | Ki | = | 1720.0 | nM | 5.76 |
| CHEMBL2170791 | — | Ki | = | 1760.0 | nM | 5.75 |
| CHEMBL2170794 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL2170790 | — | Ki | = | 2790.0 | nM | 5.55 |
| CHEMBL2170789 | — | Ki | = | 2930.0 | nM | 5.53 |