Assay Detail
Functional
CHEMBL5039191
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Partial agonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as intrinsic activity by measuring cell index change within 60 mins by Label-Free Impedance-Based Assay
7
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Crystal Structure and Subsequent Ligand Design of a Nonriboside Partial Agonist Bound to the Adenosine A<sub>2A</sub> Receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 6 | 7.11 | 8.85 |
| pEC50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL331372 | CGS-21680 | — | 1 | 8.85 |
| CHEMBL124345 | — | — | 1 | 8.01 |
| CHEMBL5093654 | — | — | 1 | 7.35 |
| CHEMBL5078507 | — | — | 1 | 6.57 |
| CHEMBL5091876 | — | — | 1 | 6.09 |
| CHEMBL5088305 | — | — | 1 | 5.78 |
| CHEMBL5093743 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL331372 | CGS-21680 | EC50 | = | 1.413 | nM | 8.85 |
| CHEMBL124345 | — | EC50 | = | 9.772 | nM | 8.01 |
| CHEMBL5093654 | — | EC50 | = | 44.67 | nM | 7.35 |
| CHEMBL5078507 | — | EC50 | = | 269.15 | nM | 6.57 |
| CHEMBL5091876 | — | EC50 | = | 812.83 | nM | 6.09 |
| CHEMBL5088305 | — | EC50 | = | 1659.59 | nM | 5.78 |
| CHEMBL5093743 | — | pEC50 | - | — | - |