Assay Detail
Binding
CHEMBL949249
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Displacement of [3H]-ZM 241385 from rat adenosine A2A receptor expressed in CHO cell membrane
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
2-Amino-N-pyrimidin-4-ylacetamides as A2A receptor antagonists: 2. Reduction of hERG activity, observed species selectivity, and structure-activity relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 7.04 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL409460 | — | — | 1 | 7.85 |
| CHEMBL409459 | — | — | 1 | 7.60 |
| CHEMBL272637 | — | — | 1 | 7.56 |
| CHEMBL429761 | — | — | 1 | 7.47 |
| CHEMBL409229 | — | — | 1 | 7.43 |
| CHEMBL270314 | — | — | 1 | 7.39 |
| CHEMBL410234 | — | — | 1 | 7.37 |
| CHEMBL409419 | — | — | 1 | 7.33 |
| CHEMBL429428 | — | — | 1 | 7.06 |
| CHEMBL272679 | — | — | 1 | 6.99 |
| CHEMBL270467 | — | — | 1 | 6.88 |
| CHEMBL429575 | — | — | 1 | 6.81 |
| CHEMBL271606 | — | — | 1 | 6.80 |
| CHEMBL261177 | — | — | 1 | 6.77 |
| CHEMBL406921 | — | — | 1 | 6.64 |
| CHEMBL409420 | — | — | 1 | 6.57 |
| CHEMBL261176 | — | — | 1 | 6.37 |
| CHEMBL271786 | — | — | 1 | 5.80 |
| CHEMBL406397 | — | — | 1 | - |
| CHEMBL270355 | — | — | 1 | - |
| CHEMBL409230 | — | — | 1 | - |
| CHEMBL259038 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL409460 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL409459 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL272637 | — | Ki | = | 27.8 | nM | 7.56 |
| CHEMBL429761 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL409229 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL270314 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL410234 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL409419 | — | Ki | = | 46.7 | nM | 7.33 |
| CHEMBL429428 | — | Ki | = | 87.0 | nM | 7.06 |
| CHEMBL272679 | — | Ki | = | 103.0 | nM | 6.99 |
| CHEMBL270467 | — | Ki | = | 131.3 | nM | 6.88 |
| CHEMBL429575 | — | Ki | = | 155.0 | nM | 6.81 |
| CHEMBL271606 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL261177 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL406921 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL409420 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL261176 | — | Ki | = | 430.0 | nM | 6.37 |
| CHEMBL271786 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL406397 | — | Ki | - | — | - | |
| CHEMBL270355 | — | Ki | - | — | - | |
| CHEMBL409230 | — | Ki | - | — | - | |
| CHEMBL259038 | — | Ki | - | — | - |