Assay Detail
Binding
CHEMBL3119409
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-NECA from human adenosine A2A receptor expressed in CHO cells after 3 hrs by topcount scintillation counting analysis
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of simplified N²-substituted pyrazolo[3,4-d]pyrimidine derivatives as novel adenosine receptor antagonists: efficient synthetic approaches, biological evaluations and molecular docking studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 5.24 | 6.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3114160 | — | — | 1 | 6.10 |
| CHEMBL3114150 | — | — | 1 | 5.96 |
| CHEMBL3114148 | — | — | 1 | 5.80 |
| CHEMBL3114156 | — | — | 1 | 5.69 |
| CHEMBL3114154 | — | — | 1 | 5.68 |
| CHEMBL3114152 | — | — | 1 | 5.66 |
| CHEMBL3114149 | — | — | 1 | 5.57 |
| CHEMBL3114155 | — | — | 1 | 5.51 |
| CHEMBL3114140 | — | — | 1 | 5.48 |
| CHEMBL3114151 | — | — | 1 | 5.46 |
| CHEMBL3114142 | — | — | 1 | 5.43 |
| CHEMBL3114141 | — | — | 1 | 5.39 |
| CHEMBL3114147 | — | — | 1 | 5.34 |
| CHEMBL3114164 | — | — | 1 | 5.33 |
| CHEMBL3114162 | — | — | 1 | 5.27 |
| CHEMBL3114166 | — | — | 1 | 5.07 |
| CHEMBL3114139 | — | — | 1 | 5.04 |
| CHEMBL3114158 | — | — | 1 | 5.00 |
| CHEMBL3114146 | — | — | 1 | 4.92 |
| CHEMBL3114157 | — | — | 1 | 4.79 |
| CHEMBL3114159 | — | — | 1 | 4.76 |
| CHEMBL3114144 | — | — | 1 | 4.69 |
| CHEMBL3114165 | — | — | 1 | 4.63 |
| CHEMBL3114143 | — | — | 1 | 4.62 |
| CHEMBL3114145 | — | — | 1 | 4.59 |
| CHEMBL3114163 | — | — | 1 | 4.52 |
| CHEMBL3114161 | — | — | 1 | - |
| CHEMBL3114153 | — | — | 1 | - |
| CHEMBL3114167 | — | — | 1 | - |
| CHEMBL3114168 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3114160 | — | Ki | = | 800.0 | nM | 6.10 |
| CHEMBL3114150 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL3114148 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL3114156 | — | Ki | = | 2060.0 | nM | 5.69 |
| CHEMBL3114154 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL3114152 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL3114149 | — | Ki | = | 2700.0 | nM | 5.57 |
| CHEMBL3114155 | — | Ki | = | 3100.0 | nM | 5.51 |
| CHEMBL3114140 | — | Ki | = | 3300.0 | nM | 5.48 |
| CHEMBL3114151 | — | Ki | = | 3500.0 | nM | 5.46 |
| CHEMBL3114142 | — | Ki | = | 3700.0 | nM | 5.43 |
| CHEMBL3114141 | — | Ki | = | 4100.0 | nM | 5.39 |
| CHEMBL3114147 | — | Ki | = | 4600.0 | nM | 5.34 |
| CHEMBL3114164 | — | Ki | = | 4700.0 | nM | 5.33 |
| CHEMBL3114162 | — | Ki | = | 5400.0 | nM | 5.27 |
| CHEMBL3114166 | — | Ki | = | 8600.0 | nM | 5.07 |
| CHEMBL3114139 | — | Ki | = | 9100.0 | nM | 5.04 |
| CHEMBL3114158 | — | Ki | = | 9900.0 | nM | 5.00 |
| CHEMBL3114146 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL3114157 | — | Ki | = | 16400.0 | nM | 4.79 |
| CHEMBL3114159 | — | Ki | = | 17500.0 | nM | 4.76 |
| CHEMBL3114144 | — | Ki | = | 20500.0 | nM | 4.69 |
| CHEMBL3114165 | — | Ki | = | 23600.0 | nM | 4.63 |
| CHEMBL3114143 | — | Ki | = | 24200.0 | nM | 4.62 |
| CHEMBL3114145 | — | Ki | = | 25600.0 | nM | 4.59 |
| CHEMBL3114163 | — | Ki | = | 29900.0 | nM | 4.52 |
| CHEMBL3114161 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL3114153 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL3114167 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL3114168 | — | Ki | > | 100000.0 | nM | - |