PIK3CA (H1047R)/PIK3R1 NanoBRET Target Engagement Intracellular Kinase Assay for screening of compounds binding to the target.
PIK3CA (H1047R)/PIK3R1
PIK3CA (H1047R)-PIK3R1
MGC142161, MGC142163, p110-alpha, PI3K, PI3K-alpha
HEK293 human epithelial cell line from ATCC
384-well plate format using Promega’s NanoBRET TE Intracellular Kinase Assay
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
| Compounds | IC50 (M) |
|---|---|
| PI-103 | 7.235e-008 |
Malvern, USA
