Assay Detail
Binding
CHEMBL949248
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-DPCPX from human adenosine A1 receptor expressed in HEK293 cell membrane
22
Total Activities
22
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: 2. Reduction of hERG activity, observed species selectivity, and structure-activity relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 6.22 | 7.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL409460 | — | — | 1 | 7.15 |
| CHEMBL410234 | — | — | 1 | 6.68 |
| CHEMBL272637 | — | — | 1 | 6.66 |
| CHEMBL270355 | — | — | 1 | 6.58 |
| CHEMBL259038 | — | — | 1 | 6.57 |
| CHEMBL406397 | — | — | 1 | 6.46 |
| CHEMBL409229 | — | — | 1 | 6.43 |
| CHEMBL409459 | — | — | 1 | 6.42 |
| CHEMBL261176 | — | — | 1 | 6.30 |
| CHEMBL261177 | — | — | 1 | 6.27 |
| CHEMBL429761 | — | — | 1 | 6.26 |
| CHEMBL270314 | — | — | 1 | 6.20 |
| CHEMBL406921 | — | — | 1 | 6.20 |
| CHEMBL270467 | — | — | 1 | 6.07 |
| CHEMBL429428 | — | — | 1 | 6.05 |
| CHEMBL271606 | — | — | 1 | 6.03 |
| CHEMBL272679 | — | — | 1 | 5.99 |
| CHEMBL271786 | — | — | 1 | 5.92 |
| CHEMBL409420 | — | — | 1 | 5.73 |
| CHEMBL409419 | — | — | 1 | 5.68 |
| CHEMBL409230 | — | — | 1 | 5.64 |
| CHEMBL429575 | — | — | 1 | 5.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL409460 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL410234 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL272637 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL270355 | — | Ki | = | 262.0 | nM | 6.58 |
| CHEMBL259038 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL406397 | — | Ki | = | 347.0 | nM | 6.46 |
| CHEMBL409229 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL409459 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL261176 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL261177 | — | Ki | = | 540.0 | nM | 6.27 |
| CHEMBL429761 | — | Ki | = | 550.0 | nM | 6.26 |
| CHEMBL270314 | — | Ki | = | 630.0 | nM | 6.20 |
| CHEMBL406921 | — | Ki | = | 630.0 | nM | 6.20 |
| CHEMBL270467 | — | Ki | = | 850.0 | nM | 6.07 |
| CHEMBL429428 | — | Ki | = | 890.0 | nM | 6.05 |
| CHEMBL271606 | — | Ki | = | 940.0 | nM | 6.03 |
| CHEMBL272679 | — | Ki | = | 1020.0 | nM | 5.99 |
| CHEMBL271786 | — | Ki | = | 1210.0 | nM | 5.92 |
| CHEMBL409420 | — | Ki | = | 1880.0 | nM | 5.73 |
| CHEMBL409419 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL409230 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL429575 | — | Ki | = | 2600.0 | nM | 5.58 |