Basic Information
ID: ALA3705866
Type: Binding
Description: Kinase Inhibition Assay: Compounds of the invention were initially diluted to 10 mM in 100% DMSO (CALBIOCHEM) for storage and made into kinase buffer solution to create a compound concentration ranging from 1 uM and 10 uM. Serial dilutions of compounds of the invention were dispensed into a 96-well plate (GREINER BIOSCIENCES) at 6 uL each. Purified full-length human SYK, and KDR (CARNA BIOSCIENCES) were diluted in kinase buffer and added to the compound solutions and pre-incubated for 30 minutes at room temperature. Next, ATP (TEKNOVA) of Km (15 uM) and substrate solution (suggested manufacture substrates of PerkinElmer, for example, Ulight-TK peptide for SYK and Ulight-JAK1 for KDR (PERKINELMER)) was added (12 uL each) to the wells containing the compound solution and enzyme. The reaction mixture was incubated for 1 hour. Following the incubation, the stop solution made with EDTA, water, and Lance detection buffer (PERKINELMER) was added (12 uL each) to stop phosphorylation.
Organism: Homo sapiens
Activity Charts
Bioactivity
Activity Types for Assay ALA3705866
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 389.46 | 2.38 | 2.38 |
| 423.91 | 3.04 | 3.04 |
| 437.94 | 3.34 | 3.34 |
| 451.96 | 3.73 | 3.73 |
| 390.45 | 1.78 | 1.78 |
| 424.90 | 2.43 | 2.43 |
| 431.50 | 2.59 | 2.59 |
| 452.95 | 3.47 | 3.47 |
| 424.89 | 3.60 | 3.60 |
| 455.93 | 3.48 | 3.48 |
| 472.58 | 3.51 | 3.51 |
| 441.90 | 3.18 | 3.18 |
| 471.57 | 3.37 | 3.37 |
| 498.51 | 4.12 | 4.12 |
| 417.47 | 2.57 | 2.57 |
| 495.97 | 3.19 | 3.19 |
| 496.02 | 3.75 | 3.75 |
| 465.99 | 3.78 | 3.78 |
| 481.99 | 3.36 | 3.36 |
| 465.99 | 4.12 | 4.12 |
| 498.57 | 0.54 | 0.54 |
| 465.99 | 4.22 | 4.22 |