Assay Detail
Binding
CHEMBL949243
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Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in HEK293 cells
16
Total Activities
16
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
2-Amino-N-pyrimidin-4-ylacetamides as A2A receptor antagonists: 1. Structure-activity relationships and optimization of heterocyclic substituents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 6.03 | 6.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL398272 | — | — | 1 | 6.66 |
| CHEMBL251975 | — | — | 1 | 6.57 |
| CHEMBL270136 | — | — | 1 | 6.41 |
| CHEMBL272825 | — | — | 1 | 6.41 |
| CHEMBL272669 | — | — | 1 | 6.14 |
| CHEMBL271377 | — | — | 1 | 6.07 |
| CHEMBL270467 | — | — | 1 | 6.07 |
| CHEMBL409112 | — | — | 1 | 6.07 |
| CHEMBL409934 | — | — | 1 | 6.03 |
| CHEMBL270761 | — | — | 1 | 5.77 |
| CHEMBL252171 | — | — | 1 | 5.77 |
| CHEMBL271202 | — | — | 1 | 5.70 |
| CHEMBL270715 | — | — | 1 | 5.38 |
| CHEMBL409711 | — | — | 1 | 5.36 |
| CHEMBL272889 | — | — | 1 | - |
| CHEMBL407711 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL398272 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL251975 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL270136 | — | Ki | = | 389.0 | nM | 6.41 |
| CHEMBL272825 | — | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL272669 | — | Ki | = | 720.0 | nM | 6.14 |
| CHEMBL271377 | — | Ki | = | 850.0 | nM | 6.07 |
| CHEMBL270467 | — | Ki | = | 850.0 | nM | 6.07 |
| CHEMBL409112 | — | Ki | = | 850.0 | nM | 6.07 |
| CHEMBL409934 | — | Ki | = | 930.0 | nM | 6.03 |
| CHEMBL270761 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL252171 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL271202 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL270715 | — | Ki | = | 4200.0 | nM | 5.38 |
| CHEMBL409711 | — | Ki | = | 4400.0 | nM | 5.36 |
| CHEMBL272889 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL407711 | — | Ki | > | 10000.0 | nM | - |