Assay Report Card

Basic Information

ID: ALA3707826

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

Compound Summary

Parent Molecular WeightALogPPolar Surface Area
389.462.382.38
423.913.043.04
437.943.343.34
451.963.733.73
390.451.781.78
424.902.432.43
431.502.592.59
452.953.473.47
424.893.603.60
455.933.483.48
472.583.513.51
441.903.183.18
471.573.373.37
498.514.124.12
417.472.572.57
495.973.193.19
496.023.753.75
465.993.783.78
481.993.363.36
465.994.124.12
498.570.540.54
465.994.224.22