Assay Detail
Functional
CHEMBL4193733
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Antagonist activity at rat A2A receptor 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
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| 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 | 18 | 9.21 | 10.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4203542 | — | — | 1 | 10.30 |
| CHEMBL4217582 | — | — | 1 | 10.22 |
| CHEMBL4205341 | — | — | 1 | 9.55 |
| CHEMBL4209408 | — | — | 1 | 9.38 |
| CHEMBL4215754 | — | — | 1 | 9.36 |
| CHEMBL4213177 | — | — | 1 | 9.24 |
| CHEMBL4217235 | — | — | 1 | 9.19 |
| CHEMBL4204531 | — | — | 1 | 9.14 |
| CHEMBL4218105 | — | — | 1 | 9.13 |
| CHEMBL4217668 | — | — | 1 | 8.97 |
| CHEMBL4212278 | — | — | 1 | 8.94 |
| CHEMBL4210241 | — | — | 1 | 8.41 |
| CHEMBL4208426 | — | — | 1 | 7.96 |
| CHEMBL4216716 | — | — | 1 | - |
| CHEMBL4212740 | — | — | 1 | - |
| CHEMBL4212260 | — | — | 1 | - |
| CHEMBL4207839 | — | — | 1 | - |
| CHEMBL4207902 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4203542 | — | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL4217582 | — | Ki | = | 0.06 | nM | 10.22 |
| CHEMBL4205341 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL4209408 | — | Ki | = | 0.42 | nM | 9.38 |
| CHEMBL4215754 | — | Ki | = | 0.44 | nM | 9.36 |
| CHEMBL4213177 | — | Ki | = | 0.58 | nM | 9.24 |
| CHEMBL4217235 | — | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL4204531 | — | Ki | = | 0.72 | nM | 9.14 |
| CHEMBL4218105 | — | Ki | = | 0.74 | nM | 9.13 |
| CHEMBL4217668 | — | Ki | = | 1.07 | nM | 8.97 |
| CHEMBL4212278 | — | Ki | = | 1.15 | nM | 8.94 |
| CHEMBL4210241 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL4208426 | — | Ki | = | 11.1 | nM | 7.96 |
| CHEMBL4216716 | — | Ki | - | — | - | |
| CHEMBL4212740 | — | Ki | - | — | - | |
| CHEMBL4212260 | — | Ki | - | — | - | |
| CHEMBL4207839 | — | Ki | - | — | - | |
| CHEMBL4207902 | — | Ki | - | — | - |