CHEK2

NanoBRET Target Engagement Intracellular Kinase Assay, Competitive binding assay format

Target

CHEK2

HGNC Symbol

CHEK2

Synonyms

CHK2; CDS1; HuCds1; PP1425; RAD53

Cell Line

HEK293 human epithelial cell line from ATCC

Assay Format

384-well plate format using Promega’s NanoBRET TE Intracellular Kinase Assay

Assay Protocol

HEK293 cells transiently expressing NanoLuc-CHEK2 Fusion Vector were seeded into the wells of 384-well plates. The cells were pre-treated with the NanoBRET Tracer K-10 and then treated with reference compound staurosporine 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)
Staurosporine 8.135e-007
Screening Location

Malvern, USA

Reference compound IC50 for CHEK2