Assay Detail
Binding
CHEMBL4018931
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Displacement of [125I]I-AB-MECA from human A3 adenosine receptor expressed in CHO cell membranes after 60 mins by gamma counting method
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 | 12 | 8.80 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL522152 | — | — | 1 | 9.52 |
| CHEMBL200732 | — | — | 1 | 9.42 |
| CHEMBL596042 | — | — | 1 | 9.38 |
| CHEMBL594625 | — | — | 1 | 8.93 |
| CHEMBL431733 | NAMODENOSON | 3.0 | 1 | 8.85 |
| CHEMBL500569 | — | — | 1 | 8.82 |
| CHEMBL387921 | — | — | 1 | 8.78 |
| CHEMBL119709 | IB-MECA | — | 1 | 8.74 |
| CHEMBL603424 | — | — | 1 | 8.67 |
| CHEMBL596014 | — | — | 1 | 8.52 |
| CHEMBL413686 | — | — | 1 | 8.38 |
| CHEMBL227279 | — | — | 1 | 7.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL522152 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL200732 | — | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL596042 | — | Ki | = | 0.42 | nM | 9.38 |
| CHEMBL594625 | — | Ki | = | 1.17 | nM | 8.93 |
| CHEMBL431733 | NAMODENOSON | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL500569 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL387921 | — | Ki | = | 1.66 | nM | 8.78 |
| CHEMBL119709 | IB-MECA | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL603424 | — | Ki | = | 2.16 | nM | 8.67 |
| CHEMBL596014 | — | Ki | = | 3.03 | nM | 8.52 |
| CHEMBL413686 | — | Ki | = | 4.16 | nM | 8.38 |
| CHEMBL227279 | — | Ki | = | 25.8 | nM | 7.59 |