Basic Information
ID: ALA3888292
Type: Binding
Description: Functional Assay: IC50(10′): The functional properties of the ligands were determined by 86Rb+ efflux assays in cells expressing α3β4 and α4β2 nAChR subtypes. The functional activity of each ligand was measured for its agonism, antagonism and desensitization ability. Agonist activity for each of the ligands was tested at eight different concentrations. The responses were compared to that stimulated by 100 μM (−)-nicotine, a near maximally effective concentration. The potency (IC50(0′)) of each ligand as an antagonist was derived from the full concentration-effect curves. We determined the desensitization potency of each ligand by pre-treating cells with the test compound for 10 minutes before 100 μM (−)-nicotine was applied. The potency of a ligand to desensitize the receptor after a 10 minute exposure (IC50(10′) was obtained with full concentration-effect curves using at least 8 concentrations of the ligand.
Activity Charts
Bioactivity
Activity Types for Assay ALA3888292
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 162.24 | 1.85 | 1.85 |
| 211.27 | 1.80 | 1.80 |
| 260.34 | 1.34 | 1.34 |
| 258.36 | 2.67 | 2.67 |
| 272.39 | 3.06 | 3.06 |
| 242.32 | 1.89 | 1.89 |
| 274.36 | 1.64 | 1.64 |
| 276.35 | 2.62 | 2.62 |
| 292.81 | 2.89 | 2.89 |