Assay Detail
Binding
CHEMBL3419484
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in CHO cell membranes incubated for 120 mins by scintillation counting method
40
Total Activities
40
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
Design, synthesis, and biological evaluation of novel 2-((2-(4-(substituted)phenylpiperazin-1-yl)ethyl)amino)-5'-N-ethylcarboxamidoadenosines as potent and selective agonists of the A2A adenosine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 40 | 7.29 | 8.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3416799 | — | — | 1 | 8.32 |
| CHEMBL3416798 | — | — | 1 | 8.26 |
| CHEMBL3416792 | — | — | 1 | 8.11 |
| CHEMBL464859 | NECA | — | 1 | 8.07 |
| CHEMBL331372 | CGS-21680 | — | 1 | 7.90 |
| CHEMBL3416810 | — | — | 1 | 7.79 |
| CHEMBL3416793 | — | — | 1 | 7.74 |
| CHEMBL3416790 | — | — | 1 | 7.64 |
| CHEMBL3416808 | — | — | 1 | 7.62 |
| CHEMBL3416800 | — | — | 1 | 7.62 |
| CHEMBL3416784 | — | — | 1 | 7.62 |
| CHEMBL3416780 | — | — | 1 | 7.60 |
| CHEMBL3414573 | — | — | 1 | 7.58 |
| CHEMBL3416781 | — | — | 1 | 7.54 |
| CHEMBL3416788 | — | — | 1 | 7.52 |
| CHEMBL3416806 | — | — | 1 | 7.48 |
| CHEMBL3416797 | — | — | 1 | 7.48 |
| CHEMBL3416796 | — | — | 1 | 7.47 |
| CHEMBL3416783 | — | — | 1 | 7.44 |
| CHEMBL3416786 | — | — | 1 | 7.37 |
| CHEMBL3416811 | — | — | 1 | 7.28 |
| CHEMBL3416775 | — | — | 1 | 7.26 |
| CHEMBL3416787 | — | — | 1 | 7.25 |
| CHEMBL3416791 | — | — | 1 | 7.14 |
| CHEMBL3416789 | — | — | 1 | 7.08 |
| CHEMBL3416785 | — | — | 1 | 7.06 |
| CHEMBL3416782 | — | — | 1 | 7.04 |
| CHEMBL3416794 | — | — | 1 | 7.02 |
| CHEMBL3416779 | — | — | 1 | 7.01 |
| CHEMBL3416807 | — | — | 1 | 6.63 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3416799 | — | Ki | = | 4.78 | nM | 8.32 |
| CHEMBL3416798 | — | Ki | = | 5.48 | nM | 8.26 |
| CHEMBL3416792 | — | Ki | = | 7.76 | nM | 8.11 |
| CHEMBL464859 | NECA | Ki | = | 8.41 | nM | 8.07 |
| CHEMBL331372 | CGS-21680 | Ki | = | 12.48 | nM | 7.90 |
| CHEMBL3416810 | — | Ki | = | 16.32 | nM | 7.79 |
| CHEMBL3416793 | — | Ki | = | 18.21 | nM | 7.74 |
| CHEMBL3416790 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL3416808 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL3416800 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL3416784 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL3416780 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL3414573 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL3416781 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL3416788 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL3416806 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL3416797 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL3416796 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL3416783 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL3416786 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL3416811 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL3416775 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL3416787 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL3416791 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL3416789 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL3416785 | — | Ki | = | 88.0 | nM | 7.06 |
| CHEMBL3416782 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL3416794 | — | Ki | = | 95.0 | nM | 7.02 |
| CHEMBL3416779 | — | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL3416807 | — | Ki | = | 235.0 | nM | 6.63 |
| CHEMBL3416776 | — | Ki | = | 237.0 | nM | 6.62 |
| CHEMBL3416795 | — | Ki | = | 277.0 | nM | 6.56 |
| CHEMBL3416777 | — | Ki | = | 659.0 | nM | 6.18 |
| CHEMBL3416804 | — | Ki | = | 682.0 | nM | 6.17 |
| CHEMBL3416805 | — | Ki | = | 745.0 | nM | 6.13 |
| CHEMBL3416778 | — | Ki | = | 967.0 | nM | 6.01 |
| CHEMBL3416803 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3416802 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3416801 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3416809 | — | Ki | > | 10000.0 | nM | - |