Assay Detail
Binding
CHEMBL4625022
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]DPCPX from Sprague-Dawley rat whole brain membrane A1AR in presence of GTP by radioligand binding assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
C2-substituted quinazolinone derivatives exhibit A<sub>1</sub> and/or A<sub>2A</sub> adenosine receptor affinities in the low micromolar range.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 5.34 | 6.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL113142 | ZM-241385 | — | 1 | 6.29 |
| CHEMBL3289109 | — | — | 1 | 5.53 |
| CHEMBL127066 | — | — | 1 | 5.42 |
| CHEMBL4634217 | — | — | 1 | 5.24 |
| CHEMBL4068369 | — | — | 1 | 5.23 |
| CHEMBL24449 | — | — | 1 | 5.16 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 1 | 4.53 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL113142 | ZM-241385 | Ki | = | 510.0 | nM | 6.29 |
| CHEMBL3289109 | — | Ki | = | 2950.0 | nM | 5.53 |
| CHEMBL127066 | — | Ki | = | 3770.0 | nM | 5.42 |
| CHEMBL4634217 | — | Ki | = | 5720.0 | nM | 5.24 |
| CHEMBL4068369 | — | Ki | = | 5890.0 | nM | 5.23 |
| CHEMBL24449 | — | Ki | = | 6920.0 | nM | 5.16 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | = | 29500.0 | nM | 4.53 |