Assay Detail
Binding
CHEMBL949247
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-ZM 241385 from human adenosine A2A 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 | 8.25 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL409460 | — | — | 1 | 8.82 |
| CHEMBL410234 | — | — | 1 | 8.68 |
| CHEMBL272637 | — | — | 1 | 8.68 |
| CHEMBL270314 | — | — | 1 | 8.62 |
| CHEMBL409229 | — | — | 1 | 8.60 |
| CHEMBL409459 | — | — | 1 | 8.54 |
| CHEMBL261177 | — | — | 1 | 8.44 |
| CHEMBL271606 | — | — | 1 | 8.43 |
| CHEMBL259038 | — | — | 1 | 8.42 |
| CHEMBL270355 | — | — | 1 | 8.40 |
| CHEMBL429575 | — | — | 1 | 8.36 |
| CHEMBL272679 | — | — | 1 | 8.27 |
| CHEMBL261176 | — | — | 1 | 8.24 |
| CHEMBL406921 | — | — | 1 | 8.22 |
| CHEMBL406397 | — | — | 1 | 8.07 |
| CHEMBL429428 | — | — | 1 | 8.00 |
| CHEMBL409419 | — | — | 1 | 8.00 |
| CHEMBL429761 | — | — | 1 | 7.96 |
| CHEMBL409420 | — | — | 1 | 7.96 |
| CHEMBL270467 | — | — | 1 | 7.92 |
| CHEMBL271786 | — | — | 1 | 7.82 |
| CHEMBL409230 | — | — | 1 | 7.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL409460 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL410234 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL272637 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL270314 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL409229 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL409459 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL261177 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL271606 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL259038 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL270355 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL429575 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL272679 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL261176 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL406921 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL406397 | — | Ki | = | 8.6 | nM | 8.07 |
| CHEMBL429428 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL409419 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL429761 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL409420 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL270467 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL271786 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL409230 | — | Ki | = | 86.0 | nM | 7.07 |