Assay Detail
Binding
CHEMBL987751
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Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in HEK293 cells
35
Total Activities
35
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 | 35 | 6.20 | 7.98 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL508786 | — | — | 1 | 7.98 |
| CHEMBL457573 | — | — | 1 | 7.19 |
| CHEMBL469488 | — | — | 1 | 7.19 |
| CHEMBL521082 | — | — | 1 | 7.16 |
| CHEMBL482011 | — | — | 1 | 7.04 |
| CHEMBL446738 | — | — | 1 | 6.90 |
| CHEMBL480443 | — | — | 1 | 6.82 |
| CHEMBL458224 | — | — | 1 | 6.79 |
| CHEMBL510696 | — | — | 1 | 6.69 |
| CHEMBL521081 | — | — | 1 | 6.67 |
| CHEMBL456051 | — | — | 1 | 6.65 |
| CHEMBL516168 | — | — | 1 | 6.50 |
| CHEMBL456287 | — | — | 1 | 6.49 |
| CHEMBL456068 | — | — | 1 | 6.49 |
| CHEMBL456069 | — | — | 1 | 6.45 |
| CHEMBL455848 | — | — | 1 | 6.45 |
| CHEMBL455849 | — | — | 1 | 6.21 |
| CHEMBL515992 | — | — | 1 | 6.04 |
| CHEMBL480444 | — | — | 1 | 6.02 |
| CHEMBL456073 | — | — | 1 | 5.98 |
| CHEMBL481817 | — | — | 1 | 5.89 |
| CHEMBL515344 | — | — | 1 | 5.81 |
| CHEMBL458232 | — | — | 1 | 5.79 |
| CHEMBL482213 | — | — | 1 | 5.61 |
| CHEMBL515190 | — | — | 1 | 5.53 |
| CHEMBL457578 | — | — | 1 | 5.47 |
| CHEMBL456271 | — | — | 1 | 5.38 |
| CHEMBL445755 | — | — | 1 | 5.35 |
| CHEMBL515192 | — | — | 1 | 5.35 |
| CHEMBL515218 | — | — | 1 | 5.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL508786 | — | Ki | = | 10.5 | nM | 7.98 |
| CHEMBL457573 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL469488 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL521082 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL482011 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL446738 | — | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL480443 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL458224 | — | Ki | = | 162.0 | nM | 6.79 |
| CHEMBL510696 | — | Ki | = | 203.0 | nM | 6.69 |
| CHEMBL521081 | — | Ki | = | 215.0 | nM | 6.67 |
| CHEMBL456051 | — | Ki | = | 222.0 | nM | 6.65 |
| CHEMBL516168 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL456287 | — | Ki | = | 323.0 | nM | 6.49 |
| CHEMBL456068 | — | Ki | = | 325.0 | nM | 6.49 |
| CHEMBL455848 | — | Ki | = | 352.0 | nM | 6.45 |
| CHEMBL456069 | — | Ki | = | 354.0 | nM | 6.45 |
| CHEMBL455849 | — | Ki | = | 620.0 | nM | 6.21 |
| CHEMBL515992 | — | Ki | = | 913.0 | nM | 6.04 |
| CHEMBL480444 | — | Ki | = | 960.0 | nM | 6.02 |
| CHEMBL456073 | — | Ki | = | 1037.0 | nM | 5.98 |
| CHEMBL481817 | — | Ki | = | 1283.0 | nM | 5.89 |
| CHEMBL515344 | — | Ki | = | 1533.0 | nM | 5.81 |
| CHEMBL458232 | — | Ki | = | 1640.0 | nM | 5.79 |
| CHEMBL482213 | — | Ki | = | 2473.0 | nM | 5.61 |
| CHEMBL515190 | — | Ki | = | 2934.0 | nM | 5.53 |
| CHEMBL457578 | — | Ki | = | 3364.3 | nM | 5.47 |
| CHEMBL456271 | — | Ki | = | 4186.0 | nM | 5.38 |
| CHEMBL445755 | — | Ki | = | 4466.0 | nM | 5.35 |
| CHEMBL515192 | — | Ki | = | 4468.0 | nM | 5.35 |
| CHEMBL515218 | — | Ki | = | 4695.0 | nM | 5.33 |
| CHEMBL519952 | — | Ki | = | 4954.0 | nM | 5.30 |
| CHEMBL457579 | — | Ki | = | 8124.0 | nM | 5.09 |
| CHEMBL459098 | — | Ki | = | 12100.0 | nM | 4.92 |
| CHEMBL457580 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL456264 | — | Ki | - | — | - |