NanoBRET™ TE Intracellular Kinase Assay Services
Quantifying kinase inhibitor occupancy, selectivity, and affinity within the cellular environment, where engagement would naturally occur, is crucial to more accurately predict its engagement potencies against human kinases. In addition to equilibrium evaluation, it's also desirable to obtain kinetic parameters such as Residence Time enabling better compound optimization.
Quantitative and wide-spectrum kinase profiling services using the NanoBRET™ Target Engagement Intracellular Kinase Assay System (Promega) enable you to assess your compound's engagement for a selected intracellular target under physiological conditions. The platform also enables determination of compound Residence Time on the target while keeping the cells intact. Please submit your compound(s) of interest, and Carna will rapidly deliver cellular IC50 values and Residence Time analyses!
Investigate compound functions in intact cells expressing full-length kinases
One type of tracer covers a wide-range of kinase investigations
Please consult us for a targets not currently listed on our website or a request for custom assays.
● IC50 Determinations & Residence Time Analysis
（Half-log dilutions, in 8 conc. points)
(performed in duplicate based upon the IC50 evaluation result)
● Panel Services
- <Guide for Service Customers>
Improved selectivity under cellular environment
- Target occupancy with 1μM Crizotinib
- (Right)using intracellular kinases in HEK293
- (Left)using recombinant kinases assayed biochemically
at Km ATP on Carna's MSA
This proximity-based assay detects molecular interactions in live cells by measuring energy transfer from a bioluminescent protein donor (NanoLuc® luciferase) to a fluorescent probe (NanoBRET™ tracer). The NanoBRET™ TE Assay measures the apparent affinity of test compounds by competitive displacement of the NanoBRET™ tracer, reversibly bound to a NanoLuc® luciferase-kinase fusion protein expressed in live cells.