KIT(D816V) NanoBRET Kinase Assay

KIT(D816V) NanoBRET Target Engagement Intracellular Kinase Assay for screening of compounds binding to the target.

Target Overview

Target

KIT (D816V)

HGNC Symbol

KIT (D816V)

Synonyms

C-Kit, PBT, CD117, SCFR

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- KIT(D816V) Fusion Vector were seeded into the wells of 384-well plates. The cells were pre-treated with the NanoBRET Tracer K-9 and then treated with reference compound Dasatinib 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)
Dasatinib	3.491e-008

Screening Location

Malvern, USA

Further information

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