Assay Detail
Binding
CHEMBL827192
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Binding affinity against Adenosine A2a receptor determined using [3H]ZM-241385 as radioligand
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| 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 | 15 | 7.61 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL173941 | — | — | 1 | 8.52 |
| CHEMBL184309 | — | — | 1 | 8.40 |
| CHEMBL363660 | — | — | 1 | 8.19 |
| CHEMBL184061 | — | — | 1 | 8.15 |
| CHEMBL184678 | — | — | 1 | 7.96 |
| CHEMBL408465 | — | — | 1 | 7.66 |
| CHEMBL440381 | — | — | 1 | 7.62 |
| CHEMBL187071 | — | — | 1 | 7.62 |
| CHEMBL360619 | — | — | 1 | 7.54 |
| CHEMBL17127 | SCH-58261 | — | 1 | 7.43 |
| CHEMBL361687 | — | — | 1 | 7.26 |
| CHEMBL185107 | — | — | 1 | 7.04 |
| CHEMBL184641 | — | — | 1 | 7.03 |
| CHEMBL184655 | — | — | 1 | 7.00 |
| CHEMBL187810 | — | — | 1 | 6.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL173941 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL184309 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL363660 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL184061 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL184678 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL408465 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL440381 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL187071 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL360619 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL17127 | SCH-58261 | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL361687 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL185107 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL184641 | — | Ki | = | 93.0 | nM | 7.03 |
| CHEMBL184655 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL187810 | — | Ki | = | 190.0 | nM | 6.72 |