Assay Detail
Binding
CHEMBL640469
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Binding ability of adenosine A1 receptor by using [3H]CHA as radioligand in rat whole brain homogenate
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis of new pyrazolo[4,3-e]1,2,4-triazolo[1,5-c] pyrimidine and 1,2,3-triazolo[4,5-e]1,2,4-triazolo[1,5-c] pyrimidine displaying potent and selective activity as A2a adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 7.65 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL53737 | — | — | 1 | 8.82 |
| CHEMBL278906 | — | — | 1 | 8.48 |
| CHEMBL16867 | — | — | 1 | 8.33 |
| CHEMBL315150 | — | — | 1 | 8.25 |
| CHEMBL82901 | — | — | 1 | 8.21 |
| CHEMBL16687 | CGS-15943 | — | 1 | 8.19 |
| CHEMBL85973 | — | — | 1 | 7.86 |
| CHEMBL315562 | — | — | 1 | 7.74 |
| CHEMBL83574 | — | — | 1 | 7.72 |
| CHEMBL16894 | — | — | 1 | 7.52 |
| CHEMBL85864 | — | — | 1 | 7.37 |
| CHEMBL83235 | — | — | 1 | 7.21 |
| CHEMBL86186 | — | — | 1 | 6.94 |
| CHEMBL17127 | SCH-58261 | — | 1 | 6.92 |
| CHEMBL17094 | — | — | 1 | 6.63 |
| CHEMBL277589 | — | — | 1 | 6.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL53737 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL278906 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL16867 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL315150 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL82901 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL16687 | CGS-15943 | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL85973 | — | Ki | = | 13.7 | nM | 7.86 |
| CHEMBL315562 | — | Ki | = | 18.3 | nM | 7.74 |
| CHEMBL83574 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL16894 | — | Ki | = | 30.4 | nM | 7.52 |
| CHEMBL85864 | — | Ki | = | 42.4 | nM | 7.37 |
| CHEMBL83235 | — | Ki | = | 61.2 | nM | 7.21 |
| CHEMBL86186 | — | Ki | = | 116.0 | nM | 6.94 |
| CHEMBL17127 | SCH-58261 | Ki | = | 121.0 | nM | 6.92 |
| CHEMBL17094 | — | Ki | = | 236.0 | nM | 6.63 |
| CHEMBL277589 | — | Ki | = | 651.0 | nM | 6.19 |