Basic Information
ID: ALA3705727
Type: Binding
Description: Kinase Assay: Inhibition of PDGFR-beta kinase activity by compounds disclosed herein was quantified by measuring the amount of [33P] incorporated into the substrate in the presence of a test compound. Briefly, a reaction mixture of 25 uL final volume containing 55 ng of PDGFR-beta kinase (obtained by purifying recombinant N-terminal 6xHis-tagged PDGFR-beta kinase domain construct expressed by baculovirus), 2.5 ug of the substrate [Poly (Glu-Tyr, 4:1), Sigma], kinase reaction buffer (20 mM MOPS pH 7.0, 1 mM EDTA, 5% glycerol, 0.01% Brij-35, 0.1% beta-mercaptoethanol, 1 mg/mL BSA, 2 mM MnCl2, 30 nM ATP, 0.1 uCi per well [33P]-gamma-ATP (2,500-3,000 Ci/mmol)), and a test compound (diluted from 9 uM to the desired final concentration by 4% DMSO) or DMSO (as the control) was incubated at 30C. for 30 minutes. The reaction was stopped by adding 5 uL of 3% phosphoric acid solution. The resultant solution (30 uL) was later harvested by a UniFilter Plate GF/B (PerkinElmer).
Organism: Homo sapiens
Activity Charts
Bioactivity
Activity Types for Assay ALA3705727
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 253.33 | 3.29 | 3.29 |
| 344.44 | 5.01 | 5.01 |
| 374.46 | 5.39 | 5.39 |
| 345.43 | 4.78 | 4.78 |
| 360.44 | 4.36 | 4.36 |
| 471.59 | 4.81 | 4.81 |