Assay Detail
Functional
CHEMBL5037232
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human adenosine A2A 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
22
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 | 11 | 7.63 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL136689 | — | — | 2 | 9.52 |
| CHEMBL5080823 | — | — | 2 | 7.58 |
| CHEMBL5074992 | — | — | 2 | 7.50 |
| CHEMBL5088372 | — | — | 2 | 7.44 |
| CHEMBL5073669 | — | — | 2 | 7.42 |
| CHEMBL5092788 | — | — | 2 | 7.15 |
| CHEMBL5089483 | — | — | 2 | 6.78 |
| CHEMBL5087305 | — | — | 2 | - |
| CHEMBL5076192 | — | — | 2 | - |
| CHEMBL5076572 | — | — | 2 | - |
| CHEMBL5089727 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL136689 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL5080823 | — | Ki | = | 26.3 | nM | 7.58 |
| CHEMBL5074992 | — | Ki | = | 31.6 | nM | 7.50 |
| CHEMBL5088372 | — | Ki | = | 36.3 | nM | 7.44 |
| CHEMBL5073669 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL5092788 | — | Ki | = | 70.8 | nM | 7.15 |
| CHEMBL5089483 | — | Ki | = | 166.0 | nM | 6.78 |
| CHEMBL5073669 | — | pKb | = | 7.42 | — | - |
| CHEMBL5080823 | — | pKb | = | 7.58 | — | - |
| CHEMBL5089483 | — | pKb | = | 6.78 | — | - |
| CHEMBL5076192 | — | pKb | - | — | - | |
| CHEMBL5074992 | — | pKb | = | 7.5 | — | - |
| CHEMBL5088372 | — | pKb | = | 7.44 | — | - |
| CHEMBL5076572 | — | pKb | - | — | - | |
| CHEMBL5089727 | — | pKb | - | — | - | |
| CHEMBL5092788 | — | pKb | = | 7.15 | — | - |
| CHEMBL136689 | — | pKb | = | 9.47 | — | - |
| CHEMBL5089727 | — | Ki | - | — | - | |
| CHEMBL5076572 | — | Ki | - | — | - | |
| CHEMBL5076192 | — | Ki | - | — | - | |
| CHEMBL5087305 | — | pKb | - | — | - | |
| CHEMBL5087305 | — | Ki | - | — | - |