Assay Report Card

Basic Information

ID: ALA3706286

Type: Binding

Description: Fluorescence Quenching Assay: CADD and biological testing to identify compounds that interact with novel ERK substrate docking sites. The known ERK2 docking sites include the DRS (site 1) and FRS (site 5) regions, whereas predicted docking sites are labeled sites 2-4 (Table 6). One compound, 76, that targets the DRS is being marketed by Calbiochem/EMD Biosciences (Cat#328006) as an ERK inhibitor. Successful inhibitor identification to date has been based on a combination of fluorescence quenching (FQ) of ERK2 wild type and docking site mutants in the presence of test compound.

Organism: Mus musculus

Activity Charts

Compound Summary

Parent Molecular WeightALogPPolar Surface Area
308.432.252.25
290.412.402.40
308.381.581.58
324.431.861.86
274.320.700.70
442.563.773.77
456.383.893.89
435.963.553.55