Assay Detail
Functional
CHEMBL950440
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Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP production
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| 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 |
|---|---|---|---|
| IC50 | 15 | 7.34 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL486162 | — | — | 1 | 8.15 |
| CHEMBL520229 | — | — | 1 | 7.89 |
| CHEMBL487569 | — | — | 1 | 7.77 |
| CHEMBL487554 | — | — | 1 | 7.75 |
| CHEMBL521223 | — | — | 1 | 7.66 |
| CHEMBL486140 | — | — | 1 | 7.51 |
| CHEMBL486745 | — | — | 1 | 7.50 |
| CHEMBL486131 | — | — | 1 | 7.31 |
| CHEMBL458242 | — | — | 1 | 7.24 |
| CHEMBL486130 | — | — | 1 | 7.19 |
| CHEMBL485972 | — | — | 1 | 7.16 |
| CHEMBL487572 | — | — | 1 | 6.81 |
| CHEMBL519549 | — | — | 1 | 6.78 |
| CHEMBL485752 | — | — | 1 | 6.71 |
| CHEMBL521029 | — | — | 1 | 6.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL486162 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL520229 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL487569 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL487554 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL521223 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL486140 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL486745 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL486131 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL458242 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL486130 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL485972 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL487572 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL519549 | — | IC50 | = | 167.0 | nM | 6.78 |
| CHEMBL485752 | — | IC50 | = | 196.0 | nM | 6.71 |
| CHEMBL521029 | — | IC50 | = | 213.0 | nM | 6.67 |