Assay Detail
Binding
CHEMBL987748
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Displacement of [3H]ZM241385 from human adenosine A2A receptor expressed in HEK293 cells
37
Total Activities
37
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
N-[6-amino-2-(heteroaryl)pyrimidin-4-yl]acetamides as A2A receptor antagonists with improved drug like properties and in vivo efficacy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 37 | 7.41 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL515526 | — | — | 1 | 8.72 |
| CHEMBL458242 | — | — | 1 | 8.64 |
| CHEMBL508786 | — | — | 1 | 8.57 |
| CHEMBL456287 | — | — | 1 | 8.38 |
| CHEMBL458224 | — | — | 1 | 8.33 |
| CHEMBL469488 | — | — | 1 | 8.23 |
| CHEMBL455848 | — | — | 1 | 8.12 |
| CHEMBL516168 | — | — | 1 | 8.05 |
| CHEMBL515992 | — | — | 1 | 7.92 |
| CHEMBL456069 | — | — | 1 | 7.82 |
| CHEMBL480444 | — | — | 1 | 7.72 |
| CHEMBL480443 | — | — | 1 | 7.70 |
| CHEMBL455849 | — | — | 1 | 7.64 |
| CHEMBL515344 | — | — | 1 | 7.59 |
| CHEMBL456051 | — | — | 1 | 7.58 |
| CHEMBL456068 | — | — | 1 | 7.57 |
| CHEMBL456073 | — | — | 1 | 7.55 |
| CHEMBL457573 | — | — | 1 | 7.40 |
| CHEMBL481817 | — | — | 1 | 7.37 |
| CHEMBL521082 | — | — | 1 | 7.34 |
| CHEMBL458232 | — | — | 1 | 7.33 |
| CHEMBL510696 | — | — | 1 | 7.33 |
| CHEMBL446738 | — | — | 1 | 7.30 |
| CHEMBL482011 | — | — | 1 | 7.30 |
| CHEMBL457578 | — | — | 1 | 7.11 |
| CHEMBL445755 | — | — | 1 | 7.04 |
| CHEMBL519952 | — | — | 1 | 6.96 |
| CHEMBL521081 | — | — | 1 | 6.92 |
| CHEMBL515190 | — | — | 1 | 6.69 |
| CHEMBL482213 | — | — | 1 | 6.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL515526 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL458242 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL508786 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL456287 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL458224 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL469488 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL455848 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL516168 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL515992 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL456069 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL480444 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL480443 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL455849 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL515344 | — | Ki | = | 25.8 | nM | 7.59 |
| CHEMBL456051 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL456068 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL456073 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL457573 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL481817 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL521082 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL458232 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL510696 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL446738 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL482011 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL457578 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL445755 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL519952 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL521081 | — | Ki | = | 119.0 | nM | 6.92 |
| CHEMBL515190 | — | Ki | = | 205.0 | nM | 6.69 |
| CHEMBL482213 | — | Ki | = | 261.0 | nM | 6.58 |
| CHEMBL515218 | — | Ki | = | 275.0 | nM | 6.56 |
| CHEMBL457579 | — | Ki | = | 313.0 | nM | 6.50 |
| CHEMBL515192 | — | Ki | = | 324.0 | nM | 6.49 |
| CHEMBL459098 | — | Ki | = | 439.0 | nM | 6.36 |
| CHEMBL456271 | — | Ki | = | 455.0 | nM | 6.34 |
| CHEMBL457580 | — | Ki | = | 1867.0 | nM | 5.73 |
| CHEMBL456264 | — | Ki | > | 10000.0 | nM | - |