PIK3CA (H1047R)/PIK3R1 NanoBRET Kinase Assay

PIK3CA (H1047R)/PIK3R1 NanoBRET Target Engagement Intracellular Kinase Assay for screening of compounds binding to the target.

Target Overview


PIK3CA (H1047R)/PIK3R1

HGNC Symbol

PIK3CA (H1047R)-PIK3R1


MGC142161, MGC142163, p110-alpha, PI3K, PI3K-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(H1047R) fusion and PIK3R1 expression vectors were seeded into the wells of 384-well plates. The cells were pre-treated with the 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.


Binding of compound to target kinase

Reference Compound IC50s
Compounds IC50 (M)
PI-103 7.235e-008

Screening Location

Malvern, USA

Reference compound IC50 for PIK3CA(H1047R)/PIK3R1