Basic Information
ID: ALA3705425
Type: Binding
Description: Enzyme Inhibtion Assay: To determine Aurora B activity of representative compounds of the invention, Active Aurora B enzyme (recombinant residues 1-344) and INCENP (recombinant GST fusion protein (Upstate)) were incubated in wells of a 384 well plate with biotinylted histone H3 peptide residues 1-21 (Upstate), 1 mM ATP, and various concentrations of inhibitors in a HEPES buffer, pH 7.4 containing MgCl2, sodium othrovanadate, and Triton X-100. After 1 hour, the reaction was stopped with EDTA and anti-phospho-histone H3 Europium Cryptate (Cis-Bio) and SA-APC (Phycolink, Prozyme) were added to detect the phosphopeptide. The amount of phosphorylation was determined by the time-resolved fluorescence ratio of signals at 665 nm and 615 nm.
Organism: Homo sapiens
Activity Charts
Bioactivity
Activity Types for Assay ALA3705425
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 440.53 | 5.89 | 5.89 |
| 488.55 | 5.18 | 5.18 |
| 528.64 | 5.83 | 5.83 |
| 498.61 | 5.74 | 5.74 |
| 530.61 | 4.41 | 4.41 |