Assay Detail
Functional
CHEMBL5099262
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Agonist activity at human adenosine A2A 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
3
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 | 17 | 5.60 | 7.95 |
| pEC50 | 7 | - | - |
| Activity | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL464859 | NECA | — | 1 | 7.95 |
| CHEMBL477 | ADENOSINE | 4.0 | 1 | 7.60 |
| CHEMBL5205907 | — | — | 1 | 6.26 |
| CHEMBL5197358 | — | — | 1 | 5.96 |
| CHEMBL5174429 | — | — | 1 | 5.86 |
| CHEMBL5208245 | — | — | 1 | 5.68 |
| CHEMBL5195714 | — | — | 1 | 5.67 |
| CHEMBL5171042 | — | — | 1 | 5.48 |
| CHEMBL5201013 | — | — | 1 | 5.24 |
| CHEMBL5187330 | — | — | 1 | 5.20 |
| CHEMBL5199871 | — | — | 1 | 5.17 |
| CHEMBL5184828 | — | — | 1 | 5.04 |
| CHEMBL3771208 | — | — | 1 | 4.95 |
| CHEMBL5191989 | — | — | 1 | 4.86 |
| CHEMBL5186981 | — | — | 1 | 4.86 |
| CHEMBL5188601 | — | — | 1 | 4.84 |
| CHEMBL5203632 | — | — | 1 | 4.58 |
| CHEMBL5171285 | — | — | 1 | - |
| CHEMBL5174052 | — | — | 1 | - |
| CHEMBL5186757 | — | — | 1 | - |
| CHEMBL5206687 | — | — | 1 | - |
| CHEMBL5172389 | — | — | 1 | - |
| CHEMBL5170857 | — | — | 1 | - |
| CHEMBL5209222 | — | — | 1 | - |
| CHEMBL5182056 | — | — | 1 | - |
| CHEMBL5179726 | — | — | 1 | - |
| CHEMBL5187478 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL464859 | NECA | EC50 | = | 11.22 | nM | 7.95 |
| CHEMBL477 | ADENOSINE | EC50 | = | 25.12 | nM | 7.60 |
| CHEMBL5205907 | — | EC50 | = | 549.54 | nM | 6.26 |
| CHEMBL5197358 | — | EC50 | = | 1096.48 | nM | 5.96 |
| CHEMBL5174429 | — | EC50 | = | 1380.38 | nM | 5.86 |
| CHEMBL5208245 | — | EC50 | = | 2089.3 | nM | 5.68 |
| CHEMBL5195714 | — | EC50 | = | 2137.96 | nM | 5.67 |
| CHEMBL5171042 | — | EC50 | = | 3311.31 | nM | 5.48 |
| CHEMBL5201013 | — | EC50 | = | 5754.4 | nM | 5.24 |
| CHEMBL5187330 | — | EC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL5199871 | — | EC50 | = | 6760.83 | nM | 5.17 |
| CHEMBL5184828 | — | EC50 | = | 9120.11 | nM | 5.04 |
| CHEMBL3771208 | — | EC50 | = | 11220.18 | nM | 4.95 |
| CHEMBL5191989 | — | EC50 | = | 13803.84 | nM | 4.86 |
| CHEMBL5186981 | — | EC50 | = | 13803.84 | nM | 4.86 |
| CHEMBL5188601 | — | EC50 | = | 14454.4 | nM | 4.84 |
| CHEMBL5203632 | — | EC50 | = | 26302.68 | nM | 4.58 |
| CHEMBL5171285 | — | pEC50 | - | — | - | |
| CHEMBL5174052 | — | pEC50 | - | — | - | |
| CHEMBL5186757 | — | pEC50 | - | — | - | |
| CHEMBL5206687 | — | pEC50 | - | — | - | |
| CHEMBL5172389 | — | Activity | - | — | - | |
| CHEMBL5170857 | — | Activity | - | — | - | |
| CHEMBL5209222 | — | pEC50 | - | — | - | |
| CHEMBL5182056 | — | pEC50 | - | — | - | |
| CHEMBL5179726 | — | Activity | - | — | - | |
| CHEMBL5187478 | — | pEC50 | - | — | - |