Assay Detail
Binding
CHEMBL1036413
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Displacement of [3H]CGS21680 from human adenosine A1 receptor
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Antagonists of the human A(2A) receptor. Part 5: Highly bio-available pyrimidine-4-carboxamides.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 6.79 | 7.91 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL554623 | — | — | 1 | 7.91 |
| CHEMBL556083 | — | — | 1 | 7.46 |
| CHEMBL553449 | — | — | 1 | 7.42 |
| CHEMBL550636 | — | — | 1 | 7.41 |
| CHEMBL564473 | — | — | 1 | 7.38 |
| CHEMBL549477 | — | — | 1 | 7.33 |
| CHEMBL557084 | — | — | 1 | 7.27 |
| CHEMBL538629 | — | — | 1 | 7.24 |
| CHEMBL551368 | — | — | 1 | 7.14 |
| CHEMBL560904 | — | — | 1 | 7.14 |
| CHEMBL552511 | — | — | 1 | 7.10 |
| CHEMBL557696 | — | — | 1 | 6.99 |
| CHEMBL571672 | — | — | 1 | 6.91 |
| CHEMBL549885 | — | — | 1 | 6.91 |
| CHEMBL551373 | — | — | 1 | 6.88 |
| CHEMBL561244 | — | — | 1 | 6.85 |
| CHEMBL561645 | — | — | 1 | 6.80 |
| CHEMBL558291 | — | — | 1 | 6.67 |
| CHEMBL538949 | — | — | 1 | 6.58 |
| CHEMBL561163 | — | — | 1 | 6.53 |
| CHEMBL562421 | — | — | 1 | 6.51 |
| CHEMBL563034 | — | — | 1 | 6.11 |
| CHEMBL564224 | — | — | 1 | 6.05 |
| CHEMBL564142 | — | — | 1 | 5.87 |
| CHEMBL540156 | — | — | 1 | 5.70 |
| CHEMBL557624 | — | — | 1 | 5.69 |
| CHEMBL551177 | — | — | 1 | 5.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL554623 | — | Ki | = | 12.2 | nM | 7.91 |
| CHEMBL556083 | — | Ki | = | 34.5 | nM | 7.46 |
| CHEMBL553449 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL550636 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL564473 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL549477 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL557084 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL538629 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL551368 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL560904 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL552511 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL557696 | — | Ki | = | 102.0 | nM | 6.99 |
| CHEMBL571672 | — | Ki | = | 124.0 | nM | 6.91 |
| CHEMBL549885 | — | Ki | = | 122.0 | nM | 6.91 |
| CHEMBL551373 | — | Ki | = | 131.0 | nM | 6.88 |
| CHEMBL561244 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL561645 | — | Ki | = | 157.0 | nM | 6.80 |
| CHEMBL558291 | — | Ki | = | 214.0 | nM | 6.67 |
| CHEMBL538949 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL561163 | — | Ki | = | 298.0 | nM | 6.53 |
| CHEMBL562421 | — | Ki | = | 311.0 | nM | 6.51 |
| CHEMBL563034 | — | Ki | = | 770.0 | nM | 6.11 |
| CHEMBL564224 | — | Ki | = | 884.0 | nM | 6.05 |
| CHEMBL564142 | — | Ki | = | 1342.0 | nM | 5.87 |
| CHEMBL540156 | — | Ki | = | 2004.0 | nM | 5.70 |
| CHEMBL557624 | — | Ki | = | 2062.0 | nM | 5.69 |
| CHEMBL551177 | — | Ki | = | 3540.0 | nM | 5.45 |