Assay Detail
Binding
CHEMBL5526115
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Positive allosteric modulation of human A3 adenosine receptor transfected in HEK293 cell membranes assessed as potentiation of 5-(2-chloro-6-((3-iodobenzyl)amino)-9H-purin-9-yl)-3,4-dihydroxy-N-methyltetrahydrofuran-2-carboxamide induced [35S]GTP-gammaS binding by measuring agonist pEC50 at 0.1 uM pretreated for 1 hr followed by agonist addition and measured after 2 hrs by liquid scintillation counting method (Rvb = 7.16 to 8.37 No_unit)
64
Total Activities
64
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Lipid Trolling to Optimize A<sub>3</sub> Adenosine Receptor-Positive Allosteric Modulators (PAMs).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 64 | 7.57 | 8.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5564885 | — | — | 1 | 8.12 |
| CHEMBL5555865 | — | — | 1 | 8.10 |
| CHEMBL5555988 | — | — | 1 | 8.04 |
| CHEMBL5562167 | — | — | 1 | 8.04 |
| CHEMBL5561940 | — | — | 1 | 8.01 |
| CHEMBL5568608 | — | — | 1 | 8.00 |
| CHEMBL5560918 | — | — | 1 | 7.97 |
| CHEMBL5568510 | — | — | 1 | 7.93 |
| CHEMBL5560102 | — | — | 1 | 7.92 |
| CHEMBL5562557 | — | — | 1 | 7.91 |
| CHEMBL5564854 | — | — | 1 | 7.89 |
| CHEMBL5567963 | — | — | 1 | 7.83 |
| CHEMBL5565378 | — | — | 1 | 7.82 |
| CHEMBL5564924 | — | — | 1 | 7.81 |
| CHEMBL5559455 | — | — | 1 | 7.77 |
| CHEMBL5564094 | — | — | 1 | 7.77 |
| CHEMBL5562368 | — | — | 1 | 7.76 |
| CHEMBL5563975 | — | — | 1 | 7.74 |
| CHEMBL5562872 | — | — | 1 | 7.73 |
| CHEMBL5566388 | — | — | 1 | 7.72 |
| CHEMBL5567642 | — | — | 1 | 7.71 |
| CHEMBL5567002 | — | — | 1 | 7.70 |
| CHEMBL5567428 | — | — | 1 | 7.69 |
| CHEMBL5527994 | — | — | 1 | 7.67 |
| CHEMBL5564886 | — | — | 1 | 7.67 |
| CHEMBL5566762 | — | — | 1 | 7.67 |
| CHEMBL5532494 | — | — | 1 | 7.64 |
| CHEMBL5532545 | — | — | 1 | 7.64 |
| CHEMBL5173661 | — | — | 1 | 7.64 |
| CHEMBL5567969 | — | — | 1 | 7.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5564885 | — | EC50 | = | 7.586 | nM | 8.12 |
| CHEMBL5555865 | — | EC50 | = | 7.943 | nM | 8.10 |
| CHEMBL5562167 | — | EC50 | = | 9.12 | nM | 8.04 |
| CHEMBL5555988 | — | EC50 | = | 9.12 | nM | 8.04 |
| CHEMBL5561940 | — | EC50 | = | 9.772 | nM | 8.01 |
| CHEMBL5568608 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5560918 | — | EC50 | = | 10.72 | nM | 7.97 |
| CHEMBL5568510 | — | EC50 | = | 11.75 | nM | 7.93 |
| CHEMBL5560102 | — | EC50 | = | 12.02 | nM | 7.92 |
| CHEMBL5562557 | — | EC50 | = | 12.3 | nM | 7.91 |
| CHEMBL5564854 | — | EC50 | = | 12.88 | nM | 7.89 |
| CHEMBL5567963 | — | EC50 | = | 14.79 | nM | 7.83 |
| CHEMBL5565378 | — | EC50 | = | 15.14 | nM | 7.82 |
| CHEMBL5564924 | — | EC50 | = | 15.49 | nM | 7.81 |
| CHEMBL5564094 | — | EC50 | = | 16.98 | nM | 7.77 |
| CHEMBL5559455 | — | EC50 | = | 16.98 | nM | 7.77 |
| CHEMBL5562368 | — | EC50 | = | 17.38 | nM | 7.76 |
| CHEMBL5563975 | — | EC50 | = | 18.2 | nM | 7.74 |
| CHEMBL5562872 | — | EC50 | = | 18.62 | nM | 7.73 |
| CHEMBL5566388 | — | EC50 | = | 19.05 | nM | 7.72 |
| CHEMBL5567642 | — | EC50 | = | 19.5 | nM | 7.71 |
| CHEMBL5567002 | — | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL5567428 | — | EC50 | = | 20.42 | nM | 7.69 |
| CHEMBL5566762 | — | EC50 | = | 21.38 | nM | 7.67 |
| CHEMBL5527994 | — | EC50 | = | 21.38 | nM | 7.67 |
| CHEMBL5564886 | — | EC50 | = | 21.38 | nM | 7.67 |
| CHEMBL5532494 | — | EC50 | = | 22.91 | nM | 7.64 |
| CHEMBL5532545 | — | EC50 | = | 22.91 | nM | 7.64 |
| CHEMBL5173661 | — | EC50 | = | 22.91 | nM | 7.64 |
| CHEMBL5567969 | — | EC50 | = | 23.99 | nM | 7.62 |
| CHEMBL5190388 | — | EC50 | = | 24.55 | nM | 7.61 |
| CHEMBL5565129 | — | EC50 | = | 26.3 | nM | 7.58 |
| CHEMBL5183188 | — | EC50 | = | 26.3 | nM | 7.58 |
| CHEMBL5561025 | — | EC50 | = | 26.92 | nM | 7.57 |
| CHEMBL5562056 | — | EC50 | = | 28.84 | nM | 7.54 |
| CHEMBL5555648 | — | EC50 | = | 30.2 | nM | 7.52 |
| CHEMBL5565518 | — | EC50 | = | 31.62 | nM | 7.50 |
| CHEMBL5564190 | — | EC50 | = | 32.36 | nM | 7.49 |
| CHEMBL5561663 | — | EC50 | = | 33.11 | nM | 7.48 |
| CHEMBL475346 | — | EC50 | = | 34.67 | nM | 7.46 |
| CHEMBL5558482 | — | EC50 | = | 34.67 | nM | 7.46 |
| CHEMBL5561575 | — | EC50 | = | 35.48 | nM | 7.45 |
| CHEMBL5561372 | — | EC50 | = | 38.02 | nM | 7.42 |
| CHEMBL5564279 | — | EC50 | = | 38.02 | nM | 7.42 |
| CHEMBL5556184 | — | EC50 | = | 38.02 | nM | 7.42 |
| CHEMBL5567863 | — | EC50 | = | 38.9 | nM | 7.41 |
| CHEMBL5562189 | — | EC50 | = | 41.69 | nM | 7.38 |
| CHEMBL5559920 | — | EC50 | = | 42.66 | nM | 7.37 |
| CHEMBL5170790 | — | EC50 | = | 44.67 | nM | 7.35 |
| CHEMBL5556136 | — | EC50 | = | 44.67 | nM | 7.35 |