Assay Detail
Functional
CHEMBL5099266
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Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
27
Total Activities
27
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and Structure-Activity Relationship Studies of Novel Adenosine A<sub>1</sub> Receptor-Selective Agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 20 | 6.35 | 7.87 |
| Activity | 7 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL477 | ADENOSINE | 4.0 | 1 | 7.87 |
| CHEMBL464859 | NECA | — | 1 | 7.83 |
| CHEMBL5171042 | — | — | 1 | 7.17 |
| CHEMBL5195714 | — | — | 1 | 7.00 |
| CHEMBL5191989 | — | — | 1 | 6.92 |
| CHEMBL5186981 | — | — | 1 | 6.88 |
| CHEMBL5205907 | — | — | 1 | 6.81 |
| CHEMBL5174429 | — | — | 1 | 6.79 |
| CHEMBL5197358 | — | — | 1 | 6.73 |
| CHEMBL5188601 | — | — | 1 | 6.63 |
| CHEMBL5187478 | — | — | 1 | 5.98 |
| CHEMBL5208245 | — | — | 1 | 5.85 |
| CHEMBL5184828 | — | — | 1 | 5.83 |
| CHEMBL5206687 | — | — | 1 | 5.82 |
| CHEMBL5186757 | — | — | 1 | 5.78 |
| CHEMBL5187330 | — | — | 1 | 5.56 |
| CHEMBL5172389 | — | — | 1 | 5.56 |
| CHEMBL5203632 | — | — | 1 | 5.52 |
| CHEMBL5170857 | — | — | 1 | 5.38 |
| CHEMBL5179726 | — | — | 1 | 5.08 |
| CHEMBL5174052 | — | — | 1 | - |
| CHEMBL3771208 | — | — | 1 | - |
| CHEMBL5199871 | — | — | 1 | - |
| CHEMBL5201013 | — | — | 1 | - |
| CHEMBL5171285 | — | — | 1 | - |
| CHEMBL5182056 | — | — | 1 | - |
| CHEMBL5209222 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL477 | ADENOSINE | EC50 | = | 13.49 | nM | 7.87 |
| CHEMBL464859 | NECA | EC50 | = | 14.79 | nM | 7.83 |
| CHEMBL5171042 | — | EC50 | = | 67.61 | nM | 7.17 |
| CHEMBL5195714 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5191989 | — | EC50 | = | 120.23 | nM | 6.92 |
| CHEMBL5186981 | — | EC50 | = | 131.83 | nM | 6.88 |
| CHEMBL5205907 | — | EC50 | = | 154.88 | nM | 6.81 |
| CHEMBL5174429 | — | EC50 | = | 162.18 | nM | 6.79 |
| CHEMBL5197358 | — | EC50 | = | 186.21 | nM | 6.73 |
| CHEMBL5188601 | — | EC50 | = | 234.42 | nM | 6.63 |
| CHEMBL5187478 | — | EC50 | = | 1047.13 | nM | 5.98 |
| CHEMBL5208245 | — | EC50 | = | 1412.54 | nM | 5.85 |
| CHEMBL5184828 | — | EC50 | = | 1479.11 | nM | 5.83 |
| CHEMBL5206687 | — | EC50 | = | 1513.56 | nM | 5.82 |
| CHEMBL5186757 | — | EC50 | = | 1659.59 | nM | 5.78 |
| CHEMBL5187330 | — | EC50 | = | 2754.23 | nM | 5.56 |
| CHEMBL5172389 | — | EC50 | = | 2754.23 | nM | 5.56 |
| CHEMBL5203632 | — | EC50 | = | 3019.95 | nM | 5.52 |
| CHEMBL5170857 | — | EC50 | = | 4168.69 | nM | 5.38 |
| CHEMBL5179726 | — | EC50 | = | 8317.64 | nM | 5.08 |
| CHEMBL5174052 | — | Activity | - | — | - | |
| CHEMBL3771208 | — | Activity | - | — | - | |
| CHEMBL5199871 | — | Activity | - | — | - | |
| CHEMBL5201013 | — | Activity | - | — | - | |
| CHEMBL5171285 | — | Activity | - | — | - | |
| CHEMBL5182056 | — | Activity | - | — | - | |
| CHEMBL5209222 | — | Activity | - | — | - |