Assay Detail
Binding
CHEMBL1052240
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Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Functionalized congeners of A3 adenosine receptor-selective nucleosides containing a bicyclo[3.1.0]hexane ring system.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 5.71 | 6.56 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL583744 | — | — | 1 | 6.56 |
| CHEMBL582921 | — | — | 1 | 6.26 |
| CHEMBL583745 | — | — | 1 | 6.12 |
| CHEMBL583746 | — | — | 1 | 6.05 |
| CHEMBL574612 | — | — | 1 | 6.01 |
| CHEMBL490605 | — | — | 1 | 5.97 |
| CHEMBL490606 | — | — | 1 | 5.80 |
| CHEMBL576395 | — | — | 1 | 5.79 |
| CHEMBL567226 | — | — | 1 | 5.64 |
| CHEMBL573937 | — | — | 1 | 5.49 |
| CHEMBL573125 | — | — | 1 | 5.45 |
| CHEMBL568307 | — | — | 1 | 5.40 |
| CHEMBL523797 | — | — | 1 | 5.35 |
| CHEMBL567412 | — | — | 1 | 5.34 |
| CHEMBL583862 | — | — | 1 | 5.34 |
| CHEMBL574212 | — | — | 1 | 5.33 |
| CHEMBL583637 | — | — | 1 | 5.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL583744 | — | Ki | = | 277.0 | nM | 6.56 |
| CHEMBL582921 | — | Ki | = | 550.0 | nM | 6.26 |
| CHEMBL583745 | — | Ki | = | 766.0 | nM | 6.12 |
| CHEMBL583746 | — | Ki | = | 890.0 | nM | 6.05 |
| CHEMBL574612 | — | Ki | = | 979.0 | nM | 6.01 |
| CHEMBL490605 | — | Ki | = | 1080.0 | nM | 5.97 |
| CHEMBL490606 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL576395 | — | Ki | = | 1640.0 | nM | 5.79 |
| CHEMBL567226 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL573937 | — | Ki | = | 3250.0 | nM | 5.49 |
| CHEMBL573125 | — | Ki | = | 3540.0 | nM | 5.45 |
| CHEMBL568307 | — | Ki | = | 4000.0 | nM | 5.40 |
| CHEMBL523797 | — | Ki | = | 4510.0 | nM | 5.35 |
| CHEMBL567412 | — | Ki | = | 4520.0 | nM | 5.34 |
| CHEMBL583862 | — | Ki | = | 4520.0 | nM | 5.34 |
| CHEMBL574212 | — | Ki | = | 4730.0 | nM | 5.33 |
| CHEMBL583637 | — | Ki | = | 6200.0 | nM | 5.21 |