Assay Detail
Binding
CHEMBL950426
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 cells
27
Total Activities
27
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
Lead optimization of 4-acetylamino-2-(3,5-dimethylpyrazol-1-yl)-6-pyridylpyrimidines as A2A adenosine receptor antagonists for the treatment of Parkinson's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 6.74 | 8.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL485765 | — | — | 1 | 8.14 |
| CHEMBL487569 | — | — | 1 | 7.66 |
| CHEMBL521356 | — | — | 1 | 7.51 |
| CHEMBL487554 | — | — | 1 | 7.47 |
| CHEMBL485972 | — | — | 1 | 7.26 |
| CHEMBL486950 | — | — | 1 | 7.19 |
| CHEMBL486140 | — | — | 1 | 7.16 |
| CHEMBL487572 | — | — | 1 | 7.09 |
| CHEMBL487553 | — | — | 1 | 7.07 |
| CHEMBL486745 | — | — | 1 | 6.96 |
| CHEMBL519383 | — | — | 1 | 6.96 |
| CHEMBL486162 | — | — | 1 | 6.92 |
| CHEMBL520229 | — | — | 1 | 6.89 |
| CHEMBL458242 | — | — | 1 | 6.72 |
| CHEMBL486130 | — | — | 1 | 6.71 |
| CHEMBL521029 | — | — | 1 | 6.66 |
| CHEMBL520036 | — | — | 1 | 6.55 |
| CHEMBL487765 | — | — | 1 | 6.54 |
| CHEMBL487372 | — | — | 1 | 6.36 |
| CHEMBL521223 | — | — | 1 | 6.33 |
| CHEMBL487371 | — | — | 1 | 6.24 |
| CHEMBL485752 | — | — | 1 | 6.21 |
| CHEMBL519549 | — | — | 1 | 6.11 |
| CHEMBL520238 | — | — | 1 | 6.09 |
| CHEMBL486131 | — | — | 1 | 6.03 |
| CHEMBL487766 | — | — | 1 | 5.68 |
| CHEMBL485950 | — | — | 1 | 5.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL485765 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL487569 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL521356 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL487554 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL485972 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL486950 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL486140 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL487572 | — | Ki | = | 81.0 | nM | 7.09 |
| CHEMBL487553 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL486745 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL519383 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL486162 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL520229 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL458242 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL486130 | — | Ki | = | 195.0 | nM | 6.71 |
| CHEMBL521029 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL520036 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL487765 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL487372 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL521223 | — | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL487371 | — | Ki | = | 580.0 | nM | 6.24 |
| CHEMBL485752 | — | Ki | = | 620.0 | nM | 6.21 |
| CHEMBL519549 | — | Ki | = | 780.0 | nM | 6.11 |
| CHEMBL520238 | — | Ki | = | 820.0 | nM | 6.09 |
| CHEMBL486131 | — | Ki | = | 940.0 | nM | 6.03 |
| CHEMBL487766 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL485950 | — | Ki | = | 4600.0 | nM | 5.34 |