Assay Detail
Binding
CHEMBL873043
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding ability of adenosine A2a receptor by using [3H]-CGS- as radioligand in rat striatal homogenate
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 | 14 | 8.28 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL278906 | — | — | 1 | 8.92 |
| CHEMBL16867 | — | — | 1 | 8.85 |
| CHEMBL315150 | — | — | 1 | 8.72 |
| CHEMBL17127 | SCH-58261 | — | 1 | 8.64 |
| CHEMBL16894 | — | — | 1 | 8.62 |
| CHEMBL315562 | — | — | 1 | 8.60 |
| CHEMBL82901 | — | — | 1 | 8.34 |
| CHEMBL83574 | — | — | 1 | 8.31 |
| CHEMBL85864 | — | — | 1 | 8.16 |
| CHEMBL17094 | — | — | 1 | 8.05 |
| CHEMBL85973 | — | — | 1 | 7.98 |
| CHEMBL86186 | — | — | 1 | 7.92 |
| CHEMBL83235 | — | — | 1 | 7.86 |
| CHEMBL277589 | — | — | 1 | 7.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL278906 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL16867 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL315150 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL17127 | SCH-58261 | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL16894 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL315562 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL82901 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL83574 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL85864 | — | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL17094 | — | Ki | = | 8.9 | nM | 8.05 |
| CHEMBL85973 | — | Ki | = | 10.4 | nM | 7.98 |
| CHEMBL86186 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL83235 | — | Ki | = | 13.7 | nM | 7.86 |
| CHEMBL277589 | — | Ki | = | 101.0 | nM | 7.00 |