Basic Information
ID: ALA3705783
Type: Binding
Description: Biochemical Assay: The inhibitory activity of putative kinase inhibitors and the potency of selected compounds were determined using a trans-phosphorylation assay.Specific peptide or protein substrates are trans-phosphorylated by their specific serine-threonine or tyrosine kinase, in the presence of ATP traced with 33P-gamma-ATP, and in the presence of their own optimal buffer and cofactors.At the end of the phosphorylation reaction, more than 98% cold ATP and radioactive ATP is captured by an excess of the ion exchange dowex resin; the resin then settles down to the bottom of the reaction plate by gravity.Supernatant, containing the phosphorylated substrate, is subsequently withdrawn and transferred into a counting plate, then evaluated by beta-counting.Reagents/Assay Conditions i. Dowex Resin Preparation500 g of wet resin (SIGMA, custom prepared resin DOWEX 1x8 200-400 mesh, 2.5 Kg) are weighed out and diluted to 2 L in 150 mM sodium formate, pH 3.00.The resin is allowed to settle down.
Format: BAO_0000357
Organism: Homo sapiens
Target: Serine/threonine-protein kinase PLK1(ALA3024)
Document: ALA3638516
BindingDB Source: 6558
Activity Charts
Bioactivity
Activity Types for Assay ALA3705783
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 334.38 | 2.13 | 2.13 |
| 448.53 | 1.58 | 1.58 |
| 488.47 | 2.13 | 2.13 |
| 502.50 | 2.47 | 2.47 |
| 532.53 | 1.92 | 1.92 |
| 499.50 | 3.44 | 3.44 |
| 534.52 | 2.90 | 2.90 |
| 550.97 | 3.17 | 3.17 |
| 514.51 | 3.03 | 3.03 |
| 503.49 | 3.07 | 3.07 |
| 462.56 | 1.84 | 1.84 |
| 436.37 | 3.15 | 3.15 |
| 433.52 | 2.48 | 2.48 |
| 573.62 | 2.79 | 2.79 |
| 380.41 | 1.32 | 1.32 |