Basic Information
ID: ALA3887361
Type: Functional
Description: Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
Organism: Homo sapiens
Cell type: HTLA
Activity Charts
Bioactivity
Activity Types for Assay ALA3887361
EC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 409.53 | 3.56 | 3.56 |
| 450.44 | 5.97 | 5.97 |
| 434.37 | 5.20 | 5.20 |
| 405.33 | 4.46 | 4.46 |
| 434.37 | 3.87 | 3.87 |
| 448.39 | 4.26 | 4.26 |
| 463.41 | 4.64 | 4.64 |
| 460.41 | 5.21 | 5.21 |
| 462.42 | 5.25 | 5.25 |
| 444.36 | 4.08 | 4.08 |
| 482.41 | 5.99 | 5.99 |
| 482.41 | 5.99 | 5.99 |
| 448.39 | 4.26 | 4.26 |
| 419.36 | 4.85 | 4.85 |
| 435.36 | 4.14 | 4.14 |
| 436.41 | 5.58 | 5.58 |
| 435.42 | 6.64 | 6.64 |
| 421.39 | 6.25 | 6.25 |
| 422.38 | 5.19 | 5.19 |
| 436.41 | 5.58 | 5.58 |
| 437.58 | 4.34 | 4.34 |
| 446.38 | 4.64 | 4.64 |
| 447.41 | 5.32 | 5.32 |
| 450.41 | 5.24 | 5.24 |
| 502.49 | 5.89 | 5.89 |
| 438.53 | 2.72 | 2.72 |
| 435.36 | 4.14 | 4.14 |
| 446.38 | 4.82 | 4.82 |
| 448.39 | 4.86 | 4.86 |
| 449.60 | 4.69 | 4.69 |
| 424.55 | 3.35 | 3.35 |
| 421.33 | 3.75 | 3.75 |
| 438.57 | 3.74 | 3.74 |
| 410.52 | 2.96 | 2.96 |
| 462.42 | 4.65 | 4.65 |
| 435.57 | 4.30 | 4.30 |
| 451.61 | 4.73 | 4.73 |
| 421.54 | 3.91 | 3.91 |
| 435.52 | 3.28 | 3.28 |
| 423.56 | 3.95 | 3.95 |
| 452.60 | 4.12 | 4.12 |
| 437.54 | 3.32 | 3.32 |
| 450.54 | 2.88 | 2.88 |