Assay Detail
Functional
CHEMBL5037231
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Antagonist activity at human adenosine A1 receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay
20
Total Activities
11
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | Flp-In-CHO |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development of Covalent, Clickable Probes for Adenosine A<sub>1</sub> and A<sub>3</sub> Receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| pKb | 11 | - | - |
| Ki | 9 | 8.37 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4204703 | — | — | 2 | 9.40 |
| CHEMBL5080823 | — | — | 2 | 8.55 |
| CHEMBL5088372 | — | — | 2 | 8.48 |
| CHEMBL5074992 | — | — | 2 | 8.46 |
| CHEMBL5089483 | — | — | 2 | 8.41 |
| CHEMBL5092788 | — | — | 2 | 8.41 |
| CHEMBL5073669 | — | — | 2 | 8.09 |
| CHEMBL5076192 | — | — | 2 | 7.99 |
| CHEMBL5089727 | — | — | 2 | 7.51 |
| CHEMBL5087305 | — | — | 1 | - |
| CHEMBL5076572 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4204703 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL5080823 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL5088372 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL5074992 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL5089483 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL5092788 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL5073669 | — | Ki | = | 8.1 | nM | 8.09 |
| CHEMBL5076192 | — | Ki | = | 10.2 | nM | 7.99 |
| CHEMBL5089727 | — | Ki | = | 30.9 | nM | 7.51 |
| CHEMBL5087305 | — | pKb | = | 8.4 | — | - |
| CHEMBL5073669 | — | pKb | = | 8.09 | — | - |
| CHEMBL5080823 | — | pKb | = | 8.56 | — | - |
| CHEMBL5089483 | — | pKb | = | 8.41 | — | - |
| CHEMBL5076192 | — | pKb | = | 7.99 | — | - |
| CHEMBL5074992 | — | pKb | = | 8.45 | — | - |
| CHEMBL5088372 | — | pKb | = | 8.48 | — | - |
| CHEMBL5076572 | — | pKb | = | 7.01 | — | - |
| CHEMBL5089727 | — | pKb | = | 7.51 | — | - |
| CHEMBL4204703 | — | pKb | = | 9.44 | — | - |
| CHEMBL5092788 | — | pKb | = | 8.41 | — | - |