Basic Information
ID: ALA3705744
Type: Binding
Description: Radioligand Binding Assay: Compounds were dissolved in 100% DMSO at a concentration 100 times the desired highest assay concentration, serially diluted 1:3 in 100% DMSO, and 1.0 ul/well of each solution was dispensed to a Nunc polypropylene, round bottom, 384-well plate. 100% inhibition is defined with 1.0 ul/well of 10 mM desipramine dissolved in DMSO. 50 ul/well of a 2x membrane preparation (0.4 mg/ml in 50 mM Tris-Cl, pH 7.5, 120 mM NaCl, 5 mM KCl) and 50 ul/well of a 2x radioligand solution (4 nM [3H]nisoxetine in 50 mM Tris-Cl, pH 7.5, 120 mM NaCl, 5 mM KCl) were added to the well and the reaction incubated for 1 hour at room temperature. The contents of the assay plate were then transferred to a Millipore MultiscreenHTS GF/B filter plate which was pretreated with 0.5% PEI for at least one hour. The plate was vacuum filtered and washed with 7 washes of 100 ul/well 50 mM Tris-Cl, pH 7.5, 120 mM NaCl, 5 mM KCl chilled to 4 C.
Format: BAO_0000249
Organism: Homo sapiens
Target: Norepinephrine transporter(ALA222)
Document: ALA3639048
BindingDB Source: 6939
Activity Charts
Bioactivity
Activity Types for Assay ALA3705744
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 299.80 | 3.85 | 3.85 |
| 285.77 | 3.55 | 3.55 |
| 386.89 | 4.56 | 4.56 |
| 454.88 | 5.57 | 5.57 |
| 415.85 | 5.32 | 5.32 |
| 413.86 | 4.90 | 4.90 |
| 363.85 | 4.01 | 4.01 |
| 370.88 | 6.06 | 6.06 |
| 421.33 | 5.21 | 5.21 |
| 437.33 | 5.60 | 5.60 |
| 313.83 | 4.24 | 4.24 |
| 299.80 | 3.94 | 3.94 |
| 427.88 | 5.29 | 5.29 |
| 375.90 | 5.00 | 5.00 |
| 361.88 | 4.69 | 4.69 |
| 361.88 | 4.69 | 4.69 |
| 376.89 | 4.27 | 4.27 |
| 414.94 | 5.25 | 5.25 |
| 411.94 | 5.85 | 5.85 |
| 418.92 | 4.67 | 4.67 |
| 416.91 | 4.03 | 4.03 |
| 376.89 | 4.39 | 4.39 |
| 381.93 | 5.06 | 5.06 |
| 437.99 | 5.31 | 5.31 |
| 384.91 | 6.45 | 6.45 |
| 419.57 | 3.26 | 3.26 |
| 445.87 | 5.84 | 5.84 |
| 377.88 | 4.82 | 4.82 |
| 392.89 | 4.40 | 4.40 |
| 418.97 | 5.64 | 5.64 |
| 418.97 | 5.64 | 5.64 |
| 435.36 | 5.60 | 5.60 |
| 451.35 | 5.99 | 5.99 |
| 396.32 | 5.35 | 5.35 |
| 426.35 | 5.35 | 5.35 |
| 412.32 | 5.05 | 5.05 |
| 411.34 | 4.93 | 4.93 |
| 449.39 | 5.91 | 5.91 |
| 412.32 | 5.47 | 5.47 |
| 480.32 | 6.49 | 6.49 |
| 384.25 | 5.49 | 5.49 |
| 463.86 | 5.98 | 5.98 |
| 463.86 | 5.98 | 5.98 |
| 445.87 | 5.84 | 5.84 |
| 479.42 | 6.20 | 6.20 |
| 447.41 | 5.46 | 5.46 |
| 429.42 | 5.32 | 5.32 |
| 447.86 | 5.85 | 5.85 |
| 418.90 | 5.08 | 5.08 |
| 404.88 | 4.69 | 4.69 |
| 433.84 | 5.46 | 5.46 |
| 368.91 | 4.07 | 4.07 |
| 460.04 | 3.71 | 3.71 |
| 601.84 | 2.53 | 2.53 |
| 423.97 | 4.62 | 4.62 |