Assay Detail
Binding
CHEMBL642893
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Displacement of [3H]R-PIA from adenosine A1 receptor of Wistar rat forebrain
13
Total Activities
13
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
N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 7.62 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 1 | 8.92 |
| CHEMBL139000 | (R)-PIA | — | 1 | 8.59 |
| CHEMBL116903 | — | — | 1 | 8.51 |
| CHEMBL117974 | — | — | 1 | 8.44 |
| CHEMBL423315 | — | — | 1 | 8.33 |
| CHEMBL2112564 | — | — | 1 | 8.00 |
| CHEMBL327073 | — | — | 1 | 7.82 |
| CHEMBL115471 | — | — | 1 | 7.37 |
| CHEMBL117904 | — | — | 1 | 7.12 |
| CHEMBL331382 | METRIFUDIL | 2.0 | 1 | 7.01 |
| CHEMBL326838 | — | — | 1 | 7.00 |
| CHEMBL411732 | — | — | 1 | 6.90 |
| CHEMBL331372 | CGS-21680 | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL139000 | (R)-PIA | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL116903 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL117974 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL423315 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL2112564 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL327073 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL115471 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL117904 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL331382 | METRIFUDIL | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL326838 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL411732 | — | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL331372 | CGS-21680 | Ki | = | 9900.0 | nM | 5.00 |