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.

Services

● IC₅₀ Determinations & Residence Time Analysis

IC₅₀Determinations
（Half-log dilutions, in 8 conc. points)

Residence Time Analysis
(performed in duplicate based upon the IC₅₀ evaluation result)

● Panel Services

CDK Panel Assay Service

Discover the selectivity of your CDK inhibitors using our CDK panel consisting of 24 CDK targets.

Kinome-Wide Profiling Service
(192 Kinase Panel)

Collectively identify compound properties.Your compound is evaluated against 192 full-length kinases individually expressed in HEK293 cells under uniform assay conditions using the same tracer.

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

Biochemical Assay [ATP=Km] NanoBRET Assay

NanoBRET™ System

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.

A cell-permeable fluorescent NanoBRET™ tracer, a BRET acceptor, is added to HEK293 cells expressing a full length kinase/NanoLuc® fusion protein. Engagement of the tracer to the target protein generates a BRET signal

Binding of the test compound to the target protein results in a loss of BRET signal between the target protein and the tracer inside intact cells

Related Publications

Quantitative, Real-Time Measurements of Intracellular Target Engagement Using Energy Transfer
(Methods in Mol Biol. 2019;1888:45-71.Doi: 10.1007/978-1-4939-8891-4_3.)

IC₅₀ Determination Assay Services

Our IC₅₀ determinations are performed, using half-log dilutions and eight(8) compound concentrations in singlicate, duplicate, or triplicate, under physiological conditions.

Results are reported in two (2) weeks.

<Guide for Service Customers>

Service Flow

Compound Handling and Shipping

Application Form for NanoBRET™ Cell-based Assay