Assay Detail
Binding
CHEMBL640695
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Binding affinity to adenosine A1 receptor of rat brain membranes without NaCl by inhibition of [125-I]-labeled aminobenzyl adenosine binding
9
Total Activities
9
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
125I-labeled 8-phenylxanthine derivatives: antagonist radioligands for adenosine A1 receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.96 | 9.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 1 | 9.46 |
| CHEMBL605469 | — | — | 1 | 9.05 |
| CHEMBL464859 | NECA | — | 1 | 8.62 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | — | 1 | 7.75 |
| CHEMBL355370 | — | — | 1 | 7.43 |
| CHEMBL351481 | — | — | 1 | 7.43 |
| CHEMBL163574 | — | — | 1 | 7.36 |
| CHEMBL11348 | — | — | 1 | 7.32 |
| CHEMBL349519 | — | — | 1 | 7.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | IC50 | = | 0.35 | nM | 9.46 |
| CHEMBL605469 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL464859 | NECA | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL355370 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL351481 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL163574 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL11348 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL349519 | — | IC50 | = | 64.0 | nM | 7.19 |