Assay Detail
Functional
CHEMBL4193732
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Potent and Selective A2A Antagonists with Efficacy in Animal Models of Parkinson's Disease and Depression.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 25 | 9.40 | 10.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4217582 | — | — | 1 | 10.22 |
| CHEMBL4217248 | — | — | 1 | 10.15 |
| CHEMBL4203542 | — | — | 1 | 9.82 |
| CHEMBL4213177 | — | — | 1 | 9.68 |
| CHEMBL4212821 | — | — | 1 | 9.66 |
| CHEMBL4205884 | — | — | 1 | 9.60 |
| CHEMBL4207914 | — | — | 1 | 9.59 |
| CHEMBL4217668 | — | — | 1 | 9.57 |
| CHEMBL4212278 | — | — | 1 | 9.52 |
| CHEMBL4215754 | — | — | 1 | 9.40 |
| CHEMBL4217235 | — | — | 1 | 9.40 |
| CHEMBL4207104 | — | — | 1 | 9.40 |
| CHEMBL4205341 | — | — | 1 | 9.38 |
| CHEMBL4210241 | — | — | 1 | 9.30 |
| CHEMBL4212810 | — | — | 1 | 9.05 |
| CHEMBL4218105 | — | — | 1 | 8.96 |
| CHEMBL4205030 | — | — | 1 | 8.92 |
| CHEMBL4208426 | — | — | 1 | 8.92 |
| CHEMBL4209408 | — | — | 1 | 8.82 |
| CHEMBL4204531 | — | — | 1 | 8.68 |
| CHEMBL4216716 | — | — | 1 | - |
| CHEMBL4212740 | — | — | 1 | - |
| CHEMBL4207839 | — | — | 1 | - |
| CHEMBL4212260 | — | — | 1 | - |
| CHEMBL4207902 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4217582 | — | Ki | = | 0.06 | nM | 10.22 |
| CHEMBL4217248 | — | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL4203542 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL4213177 | — | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL4212821 | — | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL4205884 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL4207914 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL4217668 | — | Ki | = | 0.27 | nM | 9.57 |
| CHEMBL4212278 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL4215754 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL4217235 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL4207104 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL4205341 | — | Ki | = | 0.42 | nM | 9.38 |
| CHEMBL4210241 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL4212810 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL4218105 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL4205030 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL4208426 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL4209408 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL4204531 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL4216716 | — | Ki | - | — | - | |
| CHEMBL4212740 | — | Ki | - | — | - | |
| CHEMBL4207839 | — | Ki | - | — | - | |
| CHEMBL4212260 | — | Ki | - | — | - | |
| CHEMBL4207902 | — | Ki | - | — | - |