Basic Information
ID: ALA3705800
Type: Binding
Description: Inhibition Assay: Enzymatic activity assay was performed in 96-well microtiter plates (Corning, catalog number #3686) using a total volume of 50 ul of an assay buffer composed of 50 mM HEPES pH 7.5, 10 mM MgCl2, 1.75 mM Na3VO4. Various concentrations of the test compound or vehicle controls were pre-incubated for one hour with 0.055 ug/ml of the human p38alfa (SAPKa) enzyme (obtained from University of Dundee). The reaction was started by addition of biotinylated ATF2 substrate and ATP in concentrations around their Km values (final concentration 0.62 uM and 60 uM respectively) and took place for one hour at 25 C. Addition of the detection reagents, streptavidin XL665 and anti-phosphoresidue antibody coupled to Europium cryptate, caused the juxtaposition of the cryptate and the XL665 fluorophore, resulting in fluorescence energy transfer (FRET). The FRET intensity depends on the amount of bounded cryptate antibody, which is proportional to the extent of substrate phosphorylation.
Format: BAO_0000357
Organism: Homo sapiens
Target: MAP kinase p38 alpha(ALA260)
Document: ALA3638430
BindingDB Source: 6390
Activity Charts
Bioactivity
Activity Types for Assay ALA3705800
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 374.48 | 4.71 | 4.71 |
| 397.48 | 5.07 | 5.07 |
| 387.44 | 4.67 | 4.67 |
| 346.43 | 3.93 | 3.93 |
| 360.46 | 4.32 | 4.32 |
| 378.45 | 4.46 | 4.46 |
| 320.39 | 3.52 | 3.52 |
| 362.47 | 4.56 | 4.56 |
| 389.50 | 3.47 | 3.47 |
| 471.55 | 2.94 | 2.94 |
| 376.46 | 3.55 | 3.55 |
| 403.44 | 3.90 | 3.90 |
| 424.52 | 2.95 | 2.95 |
| 410.46 | 4.95 | 4.95 |
| 361.45 | 3.71 | 3.71 |
| 361.45 | 3.71 | 3.71 |
| 377.44 | 2.95 | 2.95 |
| 335.41 | 3.18 | 3.18 |
| 362.43 | 3.11 | 3.11 |
| 359.43 | 4.78 | 4.78 |
| 358.45 | 4.52 | 4.52 |
| 374.44 | 3.76 | 3.76 |
| 344.42 | 4.21 | 4.21 |
| 344.42 | 4.13 | 4.13 |
| 408.45 | 5.15 | 5.15 |
| 451.55 | 3.00 | 3.00 |
| 294.35 | 2.99 | 2.99 |
| 348.45 | 4.03 | 4.03 |
| 361.40 | 4.13 | 4.13 |
| 390.48 | 3.68 | 3.68 |
| 404.51 | 4.07 | 4.07 |
| 459.59 | 4.02 | 4.02 |
| 392.43 | 3.89 | 3.89 |
| 420.49 | 4.41 | 4.41 |
| 409.44 | 5.42 | 5.42 |
| 389.46 | 4.15 | 4.15 |