Assay Detail
Functional
CHEMBL5037233
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human adenosine A2B 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
21
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 | 10 | 7.70 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL483688 | — | — | 2 | 8.89 |
| CHEMBL5076192 | — | — | 2 | 8.17 |
| CHEMBL5080823 | — | — | 2 | 7.75 |
| CHEMBL5074992 | — | — | 2 | 7.64 |
| CHEMBL5089483 | — | — | 2 | 7.58 |
| CHEMBL5092788 | — | — | 2 | 7.45 |
| CHEMBL5073669 | — | — | 2 | 7.10 |
| CHEMBL5088372 | — | — | 2 | 7.02 |
| CHEMBL5087305 | — | — | 1 | - |
| CHEMBL5076572 | — | — | 2 | - |
| CHEMBL5089727 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL483688 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL5076192 | — | Ki | = | 6.7 | nM | 8.17 |
| CHEMBL5080823 | — | Ki | = | 17.8 | nM | 7.75 |
| CHEMBL5074992 | — | Ki | = | 22.9 | nM | 7.64 |
| CHEMBL5089483 | — | Ki | = | 26.3 | nM | 7.58 |
| CHEMBL5092788 | — | Ki | = | 35.4 | nM | 7.45 |
| CHEMBL5073669 | — | Ki | = | 79.4 | nM | 7.10 |
| CHEMBL5088372 | — | Ki | = | 95.5 | nM | 7.02 |
| CHEMBL5073669 | — | pKb | = | 7.1 | — | - |
| CHEMBL5080823 | — | pKb | = | 7.75 | — | - |
| CHEMBL5089483 | — | pKb | = | 7.58 | — | - |
| CHEMBL5076192 | — | pKb | = | 8.17 | — | - |
| CHEMBL5074992 | — | pKb | = | 7.64 | — | - |
| CHEMBL5088372 | — | pKb | = | 7.02 | — | - |
| CHEMBL5076572 | — | pKb | - | — | - | |
| CHEMBL5089727 | — | pKb | - | — | - | |
| CHEMBL5092788 | — | pKb | = | 7.45 | — | - |
| CHEMBL5087305 | — | pKb | = | 7.73 | — | - |
| CHEMBL5089727 | — | Ki | - | — | - | |
| CHEMBL5076572 | — | Ki | - | — | - | |
| CHEMBL483688 | — | pKb | = | 8.87 | — | - |