Assay Detail
Binding
CHEMBL649107
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Ability to displace specific radioligand [3H]R-PIA binding at Adenosine A1 receptor in rat brain membrane
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
Ring-Constrained (N)-methanocarba nucleosides as adenosine receptor agonists: independent 5'-uronamide and 2'-deoxy modifications.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 6.56 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL27952 | — | — | 1 | 8.30 |
| CHEMBL284216 | — | — | 1 | 8.06 |
| CHEMBL27443 | — | — | 1 | 7.50 |
| CHEMBL280580 | — | — | 1 | 7.28 |
| CHEMBL417292 | — | — | 1 | 7.16 |
| CHEMBL27376 | — | — | 1 | 7.08 |
| CHEMBL27809 | — | — | 1 | 6.85 |
| CHEMBL26759 | — | — | 1 | 6.56 |
| CHEMBL283057 | — | — | 1 | 6.09 |
| CHEMBL286739 | — | — | 1 | 6.05 |
| CHEMBL27009 | — | — | 1 | 5.83 |
| CHEMBL287321 | — | — | 1 | 5.78 |
| CHEMBL27593 | — | — | 1 | 5.44 |
| CHEMBL27502 | — | — | 1 | 5.29 |
| CHEMBL28057 | — | — | 1 | 5.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL27952 | — | Ki | = | 5.06 | nM | 8.30 |
| CHEMBL284216 | — | Ki | = | 8.76 | nM | 8.06 |
| CHEMBL27443 | — | Ki | = | 31.8 | nM | 7.50 |
| CHEMBL280580 | — | Ki | = | 52.7 | nM | 7.28 |
| CHEMBL417292 | — | Ki | = | 69.2 | nM | 7.16 |
| CHEMBL27376 | — | Ki | = | 83.9 | nM | 7.08 |
| CHEMBL27809 | — | Ki | = | 141.0 | nM | 6.85 |
| CHEMBL26759 | — | Ki | = | 273.0 | nM | 6.56 |
| CHEMBL283057 | — | Ki | = | 805.0 | nM | 6.09 |
| CHEMBL286739 | — | Ki | = | 884.0 | nM | 6.05 |
| CHEMBL27009 | — | Ki | = | 1470.0 | nM | 5.83 |
| CHEMBL287321 | — | Ki | = | 1680.0 | nM | 5.78 |
| CHEMBL27593 | — | Ki | = | 3600.0 | nM | 5.44 |
| CHEMBL27502 | — | Ki | = | 5110.0 | nM | 5.29 |
| CHEMBL28057 | — | Ki | = | 8730.0 | nM | 5.06 |