Assay Detail
Binding
CHEMBL647736
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In vitro binding affinity against Adenosine A2a receptor in rat forebrain membranes by [3H]NECA (+CPA) displacement.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Forebrain |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Adenosine A2A antagonists with potent anti-cataleptic activity
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 7.99 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL77691 | — | — | 1 | 8.80 |
| CHEMBL77698 | — | — | 1 | 8.70 |
| CHEMBL78317 | — | — | 1 | 8.41 |
| CHEMBL77699 | — | — | 1 | 8.41 |
| CHEMBL27215 | — | — | 1 | 8.21 |
| CHEMBL422399 | — | — | 1 | 8.21 |
| CHEMBL283937 | — | — | 1 | 8.17 |
| CHEMBL78211 | — | — | 1 | 8.13 |
| CHEMBL27508 | — | — | 1 | 8.11 |
| CHEMBL76931 | — | — | 1 | 8.09 |
| CHEMBL431770 | ISTRADEFYLLINE | 4.0 | 1 | 7.89 |
| CHEMBL306313 | — | — | 1 | 7.85 |
| CHEMBL312079 | — | — | 1 | 7.82 |
| CHEMBL306633 | — | — | 1 | 7.75 |
| CHEMBL75093 | — | — | 1 | 7.31 |
| CHEMBL73827 | — | — | 1 | 7.24 |
| CHEMBL283847 | — | — | 1 | 6.77 |
| CHEMBL306945 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL77691 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL77698 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL78317 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL77699 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL27215 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL422399 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL283937 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL78211 | — | Ki | = | 7.4 | nM | 8.13 |
| CHEMBL27508 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL76931 | — | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL431770 | ISTRADEFYLLINE | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL306313 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL312079 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL306633 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL75093 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL73827 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL283847 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL306945 | — | Ki | > | 100000.0 | nM | - |