NanoLuc-PIK3CA (C420R)/PIK3R1 NanoBRET Kinase Assay

NanoLuc-PIK3CA (C420R)/PIK3R1 NanoBRET Target Engagement Intracellular Kinase Assay for screening of compounds binding to the target.

Target Overview

Target

NanoLuc-PIK3CA (C420R)/PIK3R1

HGNC Symbol

NanoLuc-PIK3CA (C420R)-PIK3R1

Synonyms

CLAPO, CLOVE, CWS5, MCAP, MCM, MCMTC, PI3K, PI3K-alpha, p110-alpha

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-PIK3CA (C420R) Fusion Vector and PIK3R1 Expression Vector were seeded into the wells of 384-well plates. The cells were pre-treated with NanoBRET Tracer K-3 and then treated with reference compound PI-103 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

Reference Compound IC50s

Compounds	IC50 (M)
PI-103	4.213e-008

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 NanoLuc-PIK3CA (C420R)/PIK3R1

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