Target Engagement
in Live Cells
The NanoBRET™ Target Engagement (TE)
Assay measures compound binding at select
target proteins in live cells, in real time. The
assay uses bioluminescence resonance
energy transfer (BRET), achieved by transfer-
ring the luminescent energy from NanoLuc
®
luciferase to the fl uor-tagged ligand bound
to the fused target protein. BRET makes
it possible to directly measure compound
permeability, binding affi nity and compound-
target residence time.
With the NanoBRET™ TE Assay you can:
• Measure Target Engagement in Live
Cells: Detect test compound binding
affi nity and permeability in live cells.
• Directly Measure Residence Time:
Compound and tracer compete directly for
the binding site.
• Use Full-Length Protein: Assays rely on
full-length proteins that are similar to the
native proteins.
• Assay HDACs, BET BRDs and kinases.
To learn more visit:
promega.com/ResidenceTime
©2016 Promega Corporation. All rights reserved. 29390100
Direct residence measurement of JQ1 at binding site on
NanoLuc
®
-BRD4 Fusion Protein.
13725MA
0
20
40
60
80
120
100
Time (minutes)
Tracer only
1,000nM JQ1 with washout
20,000nM JQ1, no washout
BRET
Ratio
(mBU)
0
10
20
30
40
Compound residence time measurement using
NanoLuc
®
-BRD4 Luciferase Fusion Protein.