Assay Detail
Functional
CHEMBL2169616
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Agonist activity at human A1AR expressed in HEK293T/17 cells assessed as inhibition of isoproterenol-induced cAMP accumulation incubated for 10 mins by luciferase reporter assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK-293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Orally active adenosine A(1) receptor agonists with antinociceptive effects in mice.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 6.32 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL284969 | — | — | 1 | 7.85 |
| CHEMBL477 | ADENOSINE | 4.0 | 1 | 7.41 |
| CHEMBL2163560 | — | — | 1 | 7.14 |
| CHEMBL2163558 | — | — | 1 | 7.00 |
| CHEMBL576739 | — | — | 1 | 6.36 |
| CHEMBL57445 | — | — | 1 | 6.31 |
| CHEMBL752 | ADENOSINE PHOSPHATE | 4.0 | 1 | 6.30 |
| CHEMBL2163564 | — | — | 1 | 6.28 |
| CHEMBL2163565 | — | — | 1 | 6.26 |
| CHEMBL2163561 | — | — | 1 | 5.85 |
| CHEMBL2163566 | — | — | 1 | 5.82 |
| CHEMBL2163559 | — | — | 1 | 5.36 |
| CHEMBL2163567 | — | — | 1 | 5.27 |
| CHEMBL2163563 | — | — | 1 | 5.21 |
| CHEMBL2163562 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL284969 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL477 | ADENOSINE | EC50 | = | 39.0 | nM | 7.41 |
| CHEMBL2163560 | — | EC50 | = | 72.0 | nM | 7.14 |
| CHEMBL2163558 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL576739 | — | EC50 | = | 440.0 | nM | 6.36 |
| CHEMBL57445 | — | EC50 | = | 490.0 | nM | 6.31 |
| CHEMBL752 | ADENOSINE PHOSPHATE | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL2163564 | — | EC50 | = | 530.0 | nM | 6.28 |
| CHEMBL2163565 | — | EC50 | = | 550.0 | nM | 6.26 |
| CHEMBL2163561 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL2163566 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL2163559 | — | EC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL2163567 | — | EC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL2163563 | — | EC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL2163562 | — | EC50 | > | 10000.0 | nM | - |