ALK1

NanoBRET Target Engagement Intracellular Kinase Assay, Competitive binding assay format

Target

ALK1

HGNC Symbol

ACVRL1

Synonyms

ACVRLK1; HHT; HHT2; ORW2; SKR3

Cell Line

HEK293 human epithelial cell line from ATCC

Assay Format

384-well plate format using Promega’s NanoBRET TE Intracellular Kinase Assay

Assay Protocol

HEK293 cells transiently expressing NanoLuc-ALK1 Fusion Vector were seeded into the wells of 384-well plates. The cells were pre-treated with the NanoBRET Tracer K-11 and then treated with reference compound LDN-193189 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 4 program based on a sigmoidal dose response equation.

Readout

Binding of compound to target kinase

Reference Compound IC50s
Compounds IC50 (M)
LDN-193189 5.519e-007
Screening Location

Malvern, USA

Reference compound IC50 for ALK1