GSK3B NanoBRET Target Engagement Intracellular Kinase Assay for screening of compounds binding to the target.
Target Overview
Target
GSK3B
HGNC Symbol
GSK3B
Synonyms
GSK3-beta
Cell Line
HEK293 human epithelial cell line from ATCC
Assay Properties
Assay Format
384-well plate format using Promega’s NanoBRET TE Intracellular Kinase Assay
Assay Protocol
HEK293 cells transiently expressing NanoLuc-GSK3B Fusion Vector were seeded into the wells of 384-well plates. The cells were pre-treated with the NanoBRET Tracer K-8 and then treated with reference compound CHIR-99021 for 1 hour. The BRET signal was measured on an Envision 2104 Multilabel Reader. IC50 value was calculated and IC50 curve was plotted using the GraphPad Prism 4 program based on a sigmoidal dose response equation.
Readout
Binding of compound to target kinase
Reference Compound IC50s
Compounds | IC50 (M) |
---|---|
CHIR-99021 | 1.528e-007 |
Screening Location
Malvern, USA
PDF