Assay Detail
Binding
CHEMBL949242
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]ZM241385 from human adenosine A2A 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 | 7.61 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL398272 | — | — | 1 | 9.05 |
| CHEMBL252171 | — | — | 1 | 8.70 |
| CHEMBL251975 | — | — | 1 | 8.57 |
| CHEMBL271202 | — | — | 1 | 8.05 |
| CHEMBL270467 | — | — | 1 | 7.92 |
| CHEMBL272825 | — | — | 1 | 7.85 |
| CHEMBL271377 | — | — | 1 | 7.77 |
| CHEMBL270136 | — | — | 1 | 7.62 |
| CHEMBL409711 | — | — | 1 | 7.59 |
| CHEMBL270761 | — | — | 1 | 7.57 |
| CHEMBL272669 | — | — | 1 | 7.29 |
| CHEMBL409934 | — | — | 1 | 7.27 |
| CHEMBL270715 | — | — | 1 | 6.88 |
| CHEMBL409112 | — | — | 1 | 6.87 |
| CHEMBL272889 | — | — | 1 | 6.72 |
| CHEMBL407711 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL398272 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL252171 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL251975 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL271202 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL270467 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL272825 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL271377 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL270136 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL409711 | — | Ki | = | 25.5 | nM | 7.59 |
| CHEMBL270761 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL272669 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL409934 | — | Ki | = | 53.4 | nM | 7.27 |
| CHEMBL270715 | — | Ki | = | 131.0 | nM | 6.88 |
| CHEMBL409112 | — | Ki | = | 135.0 | nM | 6.87 |
| CHEMBL272889 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL407711 | — | Ki | = | 1000.0 | nM | 6.00 |