Basic Information
ID: ALA3705892
Type: Binding
Description: Radioligand Binding: The TAAR1 radioligand 3[H](S)-4-[(ethyl-phenyl-amino)-methyl]-4,5-dihydro-oxazol-2-ylamine (described in WO 2008/098857) was used at a concentration equal to the calculated Kd value, that was usually around 2.3 nM, resulting in the binding of approximately 0.2% of the radioligand and a specific binding representing approximately 85% of the total binding. Nonspecific binding was defined as the amount of 3-[H]-(S)-4-[(ethyl-phenyl-amino)-methyl]-4,5-dihydro-oxazol-2-ylamine bound in the presence of 10 uM unlabeled ligand. All compounds were tested at a broad range of concentrations (10 pM to 10 uM) in duplicates. The test compounds (20 ul/well) were transferred into a 96 deep well plate (TreffLab), and 180 ul of HEPES-NaOH (20 mM, pH 7.4) containing MgCl2 (10 mM) and CaCl2 (2 mM) (binding buffer), 300 ul of the radioligand 3[H](S)-4-[(ethyl-phenyl-amino)-methyl]-4,5-dihydro-oxazol-2-ylamine at a concentration of 3.3Kd in nM.
Organism: Rattus norvegicus
Activity Charts
Bioactivity
Activity Types for Assay ALA3705892
Ki
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 348.41 | 2.99 | 2.99 |
| 382.85 | 3.64 | 3.64 |
| 366.40 | 3.13 | 3.13 |
| 378.43 | 3.00 | 3.00 |
| 362.43 | 3.00 | 3.00 |
| 362.43 | 3.30 | 3.30 |
| 378.43 | 3.00 | 3.00 |
| 366.40 | 3.13 | 3.13 |
| 378.43 | 3.00 | 3.00 |
| 382.85 | 3.64 | 3.64 |
| 408.46 | 3.01 | 3.01 |
| 382.85 | 3.64 | 3.64 |
| 382.85 | 3.64 | 3.64 |
| 382.85 | 3.64 | 3.64 |
| 382.85 | 3.64 | 3.64 |
| 378.43 | 3.00 | 3.00 |
| 396.88 | 3.65 | 3.65 |
| 362.43 | 3.00 | 3.00 |
| 362.43 | 3.00 | 3.00 |
| 373.42 | 3.54 | 3.54 |
| 387.44 | 3.55 | 3.55 |
| 380.42 | 3.14 | 3.14 |
| 392.46 | 3.01 | 3.01 |
| 387.44 | 2.87 | 2.87 |
| 401.47 | 3.35 | 3.35 |
| 401.47 | 4.03 | 4.03 |
| 387.44 | 3.17 | 3.17 |
| 391.41 | 3.00 | 3.00 |
| 366.40 | 2.92 | 2.92 |
| 348.41 | 2.79 | 2.79 |
| 366.40 | 2.92 | 2.92 |
| 383.84 | 2.83 | 2.83 |
| 417.39 | 3.20 | 3.20 |
| 373.42 | 2.66 | 2.66 |
| 417.39 | 3.20 | 3.20 |
| 371.44 | 3.67 | 3.67 |
| 371.44 | 3.67 | 3.67 |
| 357.42 | 3.28 | 3.28 |
| 391.41 | 3.00 | 3.00 |
| 414.41 | 3.59 | 3.59 |
| 442.47 | 4.08 | 4.08 |
| 442.47 | 4.08 | 4.08 |
| 391.41 | 3.00 | 3.00 |
| 428.44 | 3.60 | 3.60 |
| 414.41 | 3.39 | 3.39 |
| 414.41 | 3.39 | 3.39 |
| 418.38 | 2.59 | 2.59 |
| 384.83 | 2.23 | 2.23 |
| 384.83 | 2.23 | 2.23 |
| 384.83 | 2.23 | 2.23 |
| 418.38 | 2.59 | 2.59 |
| 418.38 | 2.59 | 2.59 |
| 375.39 | 1.45 | 1.45 |
| 418.38 | 2.59 | 2.59 |