Assay Detail
Binding
CHEMBL4018933
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Displacement of [3H]CGS21680 from human A2A adenosine receptor expressed in HEK293 cell membranes after 60 mins by gamma counting method
11
Total Activities
11
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 | Autocuration |
Publication
Polypharmacology of N6-(3-Iodobenzyl)adenosine-5'-N-methyluronamide (IB-MECA) and Related A3 Adenosine Receptor Ligands: Peroxisome Proliferator Activated Receptor (PPAR) γ Partial Agonist and PPARδ Antagonist Activity Suggests Their Antidiabetic Potential.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 6.38 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL596014 | — | — | 1 | 7.82 |
| CHEMBL596042 | — | — | 1 | 7.24 |
| CHEMBL594625 | — | — | 1 | 6.91 |
| CHEMBL200732 | — | — | 1 | 6.65 |
| CHEMBL413686 | — | — | 1 | 6.47 |
| CHEMBL500569 | — | — | 1 | 6.36 |
| CHEMBL522152 | — | — | 1 | 6.32 |
| CHEMBL227279 | — | — | 1 | 5.80 |
| CHEMBL603424 | — | — | 1 | 5.80 |
| CHEMBL119709 | IB-MECA | — | 1 | 5.54 |
| CHEMBL431733 | NAMODENOSON | 3.0 | 1 | 5.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL596014 | — | Ki | = | 15.2 | nM | 7.82 |
| CHEMBL596042 | — | Ki | = | 57.6 | nM | 7.24 |
| CHEMBL594625 | — | Ki | = | 122.0 | nM | 6.91 |
| CHEMBL200732 | — | Ki | = | 223.0 | nM | 6.65 |
| CHEMBL413686 | — | Ki | = | 341.0 | nM | 6.47 |
| CHEMBL500569 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL522152 | — | Ki | = | 475.0 | nM | 6.32 |
| CHEMBL227279 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL603424 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL119709 | IB-MECA | Ki | = | 2910.0 | nM | 5.54 |
| CHEMBL431733 | NAMODENOSON | Ki | = | 5360.0 | nM | 5.27 |