Assay Detail
Binding
CHEMBL1036412
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Displacement of [3H]CGS21680 from human adenosine A2A receptor
28
Total Activities
28
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 | 28 | 7.85 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL564473 | — | — | 1 | 8.77 |
| CHEMBL551368 | — | — | 1 | 8.66 |
| CHEMBL560904 | — | — | 1 | 8.59 |
| CHEMBL553449 | — | — | 1 | 8.59 |
| CHEMBL557084 | — | — | 1 | 8.46 |
| CHEMBL556083 | — | — | 1 | 8.46 |
| CHEMBL554623 | — | — | 1 | 8.43 |
| CHEMBL549885 | — | — | 1 | 8.37 |
| CHEMBL550636 | — | — | 1 | 8.32 |
| CHEMBL549477 | — | — | 1 | 8.21 |
| CHEMBL551373 | — | — | 1 | 8.15 |
| CHEMBL538629 | — | — | 1 | 8.12 |
| CHEMBL571672 | — | — | 1 | 8.03 |
| CHEMBL538949 | — | — | 1 | 8.03 |
| CHEMBL557696 | — | — | 1 | 8.02 |
| CHEMBL564224 | — | — | 1 | 8.00 |
| CHEMBL558291 | — | — | 1 | 7.85 |
| CHEMBL561163 | — | — | 1 | 7.80 |
| CHEMBL552511 | — | — | 1 | 7.76 |
| CHEMBL561244 | — | — | 1 | 7.70 |
| CHEMBL562421 | — | — | 1 | 7.64 |
| CHEMBL431770 | ISTRADEFYLLINE | 4.0 | 1 | 7.44 |
| CHEMBL561645 | — | — | 1 | 7.10 |
| CHEMBL540156 | — | — | 1 | 6.82 |
| CHEMBL563034 | — | — | 1 | 6.77 |
| CHEMBL551177 | — | — | 1 | 6.66 |
| CHEMBL557624 | — | — | 1 | 6.51 |
| CHEMBL564142 | — | — | 1 | 6.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL564473 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL551368 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL560904 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL553449 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL557084 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL556083 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL554623 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL549885 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL550636 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL549477 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL551373 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL538629 | — | Ki | = | 7.6 | nM | 8.12 |
| CHEMBL571672 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL538949 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL557696 | — | Ki | = | 9.5 | nM | 8.02 |
| CHEMBL564224 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL558291 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL561163 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL552511 | — | Ki | = | 17.5 | nM | 7.76 |
| CHEMBL561244 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL562421 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL431770 | ISTRADEFYLLINE | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL561645 | — | Ki | = | 79.0 | nM | 7.10 |
| CHEMBL540156 | — | Ki | = | 153.0 | nM | 6.82 |
| CHEMBL563034 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL551177 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL557624 | — | Ki | = | 308.0 | nM | 6.51 |
| CHEMBL564142 | — | Ki | = | 388.0 | nM | 6.41 |