Assay Detail
Binding
CHEMBL952340
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]ZM241685 from human adenosine A2A 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 | 8.57 | 9.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL487569 | — | — | 1 | 9.72 |
| CHEMBL485765 | — | — | 1 | 9.59 |
| CHEMBL487553 | — | — | 1 | 9.36 |
| CHEMBL487554 | — | — | 1 | 9.33 |
| CHEMBL521356 | — | — | 1 | 9.25 |
| CHEMBL486745 | — | — | 1 | 9.22 |
| CHEMBL487572 | — | — | 1 | 9.21 |
| CHEMBL486162 | — | — | 1 | 9.15 |
| CHEMBL485972 | — | — | 1 | 9.14 |
| CHEMBL520229 | — | — | 1 | 9.08 |
| CHEMBL486950 | — | — | 1 | 9.04 |
| CHEMBL486140 | — | — | 1 | 8.74 |
| CHEMBL521223 | — | — | 1 | 8.72 |
| CHEMBL458242 | — | — | 1 | 8.64 |
| CHEMBL520036 | — | — | 1 | 8.64 |
| CHEMBL486130 | — | — | 1 | 8.54 |
| CHEMBL521029 | — | — | 1 | 8.52 |
| CHEMBL519383 | — | — | 1 | 8.51 |
| CHEMBL486131 | — | — | 1 | 8.40 |
| CHEMBL519549 | — | — | 1 | 8.13 |
| CHEMBL485752 | — | — | 1 | 8.11 |
| CHEMBL487372 | — | — | 1 | 8.10 |
| CHEMBL487371 | — | — | 1 | 7.92 |
| CHEMBL520238 | — | — | 1 | 7.40 |
| CHEMBL487765 | — | — | 1 | 7.06 |
| CHEMBL485950 | — | — | 1 | 7.06 |
| CHEMBL487766 | — | — | 1 | 6.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL487569 | — | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL485765 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL487553 | — | Ki | = | 0.44 | nM | 9.36 |
| CHEMBL487554 | — | Ki | = | 0.47 | nM | 9.33 |
| CHEMBL521356 | — | Ki | = | 0.56 | nM | 9.25 |
| CHEMBL486745 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL487572 | — | Ki | = | 0.61 | nM | 9.21 |
| CHEMBL486162 | — | Ki | = | 0.71 | nM | 9.15 |
| CHEMBL485972 | — | Ki | = | 0.72 | nM | 9.14 |
| CHEMBL520229 | — | Ki | = | 0.83 | nM | 9.08 |
| CHEMBL486950 | — | Ki | = | 0.92 | nM | 9.04 |
| CHEMBL486140 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL521223 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL458242 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL520036 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL486130 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL521029 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL519383 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL486131 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL519549 | — | Ki | = | 7.4 | nM | 8.13 |
| CHEMBL485752 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL487372 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL487371 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL520238 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL487765 | — | Ki | = | 87.0 | nM | 7.06 |
| CHEMBL485950 | — | Ki | = | 87.0 | nM | 7.06 |
| CHEMBL487766 | — | Ki | = | 120.0 | nM | 6.92 |