Assay Detail
Binding
CHEMBL2014359
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Displacement of [3H]R-PIA from human recombinant adenosine receptor-1 expressed in CHO cell membrane after 60 mins by liquid scintillation counting
19
Total Activities
19
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
Truncated (N)-Methanocarba Nucleosides as A(1) Adenosine Receptor Agonists and Partial Agonists: Overcoming Lack of a Recognition Element.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 6.59 | 7.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2012686 | — | — | 1 | 7.32 |
| CHEMBL2012674 | — | — | 1 | 7.29 |
| CHEMBL2012684 | — | — | 1 | 7.17 |
| CHEMBL2012682 | — | — | 1 | 7.14 |
| CHEMBL2012681 | — | — | 1 | 7.14 |
| CHEMBL2012683 | — | — | 1 | 7.10 |
| CHEMBL2012678 | — | — | 1 | 7.08 |
| CHEMBL2012685 | — | — | 1 | 7.06 |
| CHEMBL2012675 | — | — | 1 | 6.85 |
| CHEMBL2012679 | — | — | 1 | 6.70 |
| CHEMBL2012673 | — | — | 1 | 6.68 |
| CHEMBL2012676 | — | — | 1 | 6.64 |
| CHEMBL2012672 | — | — | 1 | 6.46 |
| CHEMBL2012677 | — | — | 1 | 6.12 |
| CHEMBL2012680 | — | — | 1 | 6.03 |
| CHEMBL2012691 | — | — | 1 | 5.90 |
| CHEMBL2012693 | — | — | 1 | 5.72 |
| CHEMBL2012690 | — | — | 1 | 5.45 |
| CHEMBL2012687 | — | — | 1 | 5.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2012686 | — | Ki | = | 47.9 | nM | 7.32 |
| CHEMBL2012674 | — | Ki | = | 51.6 | nM | 7.29 |
| CHEMBL2012684 | — | Ki | = | 68.4 | nM | 7.17 |
| CHEMBL2012682 | — | Ki | = | 72.2 | nM | 7.14 |
| CHEMBL2012681 | — | Ki | = | 72.7 | nM | 7.14 |
| CHEMBL2012683 | — | Ki | = | 78.8 | nM | 7.10 |
| CHEMBL2012678 | — | Ki | = | 82.6 | nM | 7.08 |
| CHEMBL2012685 | — | Ki | = | 86.8 | nM | 7.06 |
| CHEMBL2012675 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL2012679 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL2012673 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL2012676 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL2012672 | — | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL2012677 | — | Ki | = | 760.0 | nM | 6.12 |
| CHEMBL2012680 | — | Ki | = | 930.0 | nM | 6.03 |
| CHEMBL2012691 | — | Ki | = | 1260.0 | nM | 5.90 |
| CHEMBL2012693 | — | Ki | = | 1910.0 | nM | 5.72 |
| CHEMBL2012690 | — | Ki | = | 3580.0 | nM | 5.45 |
| CHEMBL2012687 | — | Ki | = | 4790.0 | nM | 5.32 |