MAPK1+KRAS(G12C) NanoBRET Kinase Assay

MAPK1+KRAS(G12C) NanoBRET Target Engagement Intracellular Kinase Assay for screening of compounds binding to the target.

Target Overview

Target

MAPK1+KRAS(G12C)

HGNC Symbol

MAPK1+KRAS(G12C)

Synonyms

ERK2; ERT1; P42MAPK; PRKM1

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 co-expressing NanoLuc-MAPK1 Fusion Vector and KRAS(G12C) Vector were seeded into the wells of 384-well plates. The cells were pre-treated with the NanoBRET Tracer K-5 and then treated with reference compound CTx-0294885 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 program based on a sigmoidal dose response equation.

Readout

Binding of compound to target kinase

Reference Compound IC50s

Compounds	IC50 (M)
CTx-0294885	6.180e-007

Screening Location

Malvern, PA, USA

Further Information

More information can be found on our website NanoBRET Target Engagement Intracellular Kinase Assay Services

Reference compound IC50 for MAPK1+KRAS(G12C)

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