Assay Detail
Binding
CHEMBL4193729
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Displacement of [3H]ZM241385 from human A2A receptor expressed in HEK293 cell membranes after 90 mins radioligand binding assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 | 9.04 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4212821 | — | — | 1 | 9.70 |
| CHEMBL4205884 | — | — | 1 | 9.52 |
| CHEMBL4207914 | — | — | 1 | 9.52 |
| CHEMBL4217582 | — | — | 1 | 9.40 |
| CHEMBL4203542 | — | — | 1 | 9.40 |
| CHEMBL4209408 | — | — | 1 | 9.40 |
| CHEMBL4210241 | — | — | 1 | 9.30 |
| CHEMBL4207104 | — | — | 1 | 9.30 |
| CHEMBL4204531 | — | — | 1 | 9.30 |
| CHEMBL4216716 | — | — | 1 | 9.22 |
| CHEMBL4212278 | — | — | 1 | 9.22 |
| CHEMBL4212740 | — | — | 1 | 9.15 |
| CHEMBL4205030 | — | — | 1 | 9.05 |
| CHEMBL4213177 | — | — | 1 | 9.00 |
| CHEMBL4217248 | — | — | 1 | 9.00 |
| CHEMBL4212810 | — | — | 1 | 8.92 |
| CHEMBL4218105 | — | — | 1 | 8.85 |
| CHEMBL4215754 | — | — | 1 | 8.82 |
| CHEMBL4217235 | — | — | 1 | 8.77 |
| CHEMBL4217668 | — | — | 1 | 8.72 |
| CHEMBL4207839 | — | — | 1 | 8.70 |
| CHEMBL4205341 | — | — | 1 | 8.70 |
| CHEMBL4212260 | — | — | 1 | 8.51 |
| CHEMBL4207902 | — | — | 1 | 8.35 |
| CHEMBL4208426 | — | — | 1 | 8.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4212821 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL4205884 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL4207914 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL4217582 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL4203542 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL4209408 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL4210241 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL4207104 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL4204531 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL4216716 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL4212278 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL4212740 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL4205030 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL4213177 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL4217248 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL4212810 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL4218105 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL4215754 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL4217235 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL4217668 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL4207839 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL4205341 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL4212260 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL4207902 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL4208426 | — | Ki | = | 6.4 | nM | 8.19 |