Assay Detail
Binding
CHEMBL828959
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Binding affinity against Adenosine A1 receptor from rat cerebral cortex was determined using [3H]DPCPX as radioligand
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Triamino derivatives of triazolotriazine and triazolopyrimidine as adenosine A2a receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 6.01 | 6.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL17127 | SCH-58261 | — | 1 | 6.41 |
| CHEMBL363660 | — | — | 1 | 6.12 |
| CHEMBL187071 | — | — | 1 | 6.10 |
| CHEMBL184309 | — | — | 1 | 6.09 |
| CHEMBL184061 | — | — | 1 | 5.96 |
| CHEMBL184678 | — | — | 1 | 5.82 |
| CHEMBL361687 | — | — | 1 | 5.58 |
| CHEMBL408465 | — | — | 1 | - |
| CHEMBL187810 | — | — | 1 | - |
| CHEMBL440381 | — | — | 1 | - |
| CHEMBL184655 | — | — | 1 | - |
| CHEMBL184641 | — | — | 1 | - |
| CHEMBL185107 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL17127 | SCH-58261 | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL363660 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL187071 | — | Ki | = | 790.0 | nM | 6.10 |
| CHEMBL184309 | — | Ki | = | 820.0 | nM | 6.09 |
| CHEMBL184061 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL184678 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL361687 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL408465 | — | Ki | > | 500.0 | nM | - |
| CHEMBL187810 | — | Ki | > | 500.0 | nM | - |
| CHEMBL440381 | — | Ki | > | 500.0 | nM | - |
| CHEMBL184655 | — | Ki | > | 500.0 | nM | - |
| CHEMBL184641 | — | Ki | > | 500.0 | nM | - |
| CHEMBL185107 | — | Ki | > | 500.0 | nM | - |