Assay Detail
Binding
CHEMBL876556
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Ability to inhibit binding of [3H]R-PIA to Adenosine A1 receptor in rat brain cortical membranes
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis and structure-activity relationships of 3,7-dimethyl-1-propargylxanthine derivatives, A2A-selective adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 5.30 | 6.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL337373 | — | — | 1 | 6.92 |
| CHEMBL137438 | — | — | 1 | 6.60 |
| CHEMBL304455 | — | — | 1 | 6.09 |
| CHEMBL344678 | — | — | 1 | 5.68 |
| CHEMBL137471 | — | — | 1 | 5.60 |
| CHEMBL136836 | — | — | 1 | 5.57 |
| CHEMBL26897 | — | — | 1 | 5.41 |
| CHEMBL115940 | — | — | 1 | 5.21 |
| CHEMBL280982 | — | — | 1 | 4.86 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 4.85 |
| CHEMBL21053 | — | — | 1 | 4.82 |
| CHEMBL26138 | — | — | 1 | 4.55 |
| CHEMBL281811 | — | — | 1 | 4.55 |
| CHEMBL113 | CAFFEINE | 4.0 | 1 | 4.39 |
| CHEMBL282038 | — | — | 1 | 4.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL337373 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL137438 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL304455 | — | Ki | = | 820.0 | nM | 6.09 |
| CHEMBL344678 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL137471 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL136836 | — | Ki | = | 2700.0 | nM | 5.57 |
| CHEMBL26897 | — | Ki | = | 3890.0 | nM | 5.41 |
| CHEMBL115940 | — | Ki | = | 6100.0 | nM | 5.21 |
| CHEMBL280982 | — | Ki | = | 13800.0 | nM | 4.86 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 14000.0 | nM | 4.85 |
| CHEMBL21053 | — | Ki | = | 15000.0 | nM | 4.82 |
| CHEMBL26138 | — | Ki | = | 28000.0 | nM | 4.55 |
| CHEMBL281811 | — | Ki | = | 28000.0 | nM | 4.55 |
| CHEMBL113 | CAFFEINE | Ki | = | 41000.0 | nM | 4.39 |
| CHEMBL282038 | — | Ki | = | 45000.0 | nM | 4.35 |