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Kinase Selectivity Profiling Services

Accelerate your drug discovery workflow with our kinase selectivity profiling services. You can count on expert support from start to finish—and beyond. We help you succeed with our collaborative approach, innovative technology and commitment to high quality standards.
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Service Overview

Our Assay

Our kinase selectivity profiling services use NanoBRET™ Target Engagement Intracellular Kinase Assays to test your supplied compounds. It includes a diverse panel of 192 or 240 full-length kinases transiently expressed in HEK293 cells.

Your Data

  • Quantitative measurement of compound affinity and occupancy in live cells
  • Includes cellular selectivity and off-target activity
  • Ratiometric BRET data provide reproducibility with low error rates
  • Both single point and dose response data with technical duplicates

Service Schedule

Monthly or on-demand runs

Turnaround Time

2–3 weeks

Why Choose Us

  • Close collaboration with our scientists from start to finish
  • Cellular assay provides biologically relevant results

Technology Overview

How NanoBRET™ Target Engagement Works

18708maimageoptim
NanoBRET™ TE technology is a bioluminescence resonance energy transfer (BRET) method. In this method, a target is expressed in mammalian cells as a target-NanoLuc® fusion protein. BRET is achieved by luminescent energy transfer from NanoLuc® luciferase to a cell-permeable NanoBRET™ TE Tracer that is bound to the target-NanoLuc® fusion protein. A test compound that is cell-permeable and competes with the tracer for target binding will result in a loss of NanoBRET™ signal. Using the optimized assay conditions provided for each target, the assay yields quantitative intracellular compound affinity and occupancy. Compound occupancy is quantified using controls that allow the BRET signal to be normalized.

Advantages of Cellular vs. Biochemical Kinase Assays

Cellular kinase assays, compared to biochemical assays, provide a more physiologically relevant environment, reflecting real cellular complexities. They enable assessment of drug permeability and can detect off-target effects in a natural context. While biochemical assays are precise, they may not capture the full spectrum of cellular interactions, making cellular assays a more holistic choice for evaluating kinase inhibitors.
cellular-vs-biochemical-kinase-assay
Visual comparison between cellular and biochemical kinase assays. Left: Biochemical kinase assays are done in a simplified environment with the kinase target. Right: Cellular kinase assays incorporate a complex cellular setting with multiple proteins and interactions to provide more relevant data.
compound-concentration-occupancy

Various cellular conditions can result in right- or left-shifted occupancy:

  • Protein complexes
  • Target activation state
  • Compartmentalization
  • Plasma membrane
  • Efflux
  • Unpredictable metabolites (e.g., nucleotides)

Improved Kinase Selectivity Profile Using Cellular Method

These dendrograms show the target occupancy obtained with 10µM dabrafenib using the live-cell NanoBRET™ TE K240 Kinase Selectivity Panel compared to a biochemical cell-free approach. The kinases with an occupancy >50% are marked with red dots. The results showed an improved spectrum of activity in cells, with 50 targets engaged by dabrafenib using the NanoBRET™ TE method, compared to 123 kinases engaged using the biochemical approach.

NanoBRET™ TE: 50 Hits

dabrafenib-nanobret-kinase-tree-hits

Biochemical: 123 Hits

dabrafenib-ambit-kinase-tree-hits

Kinase Panel

Our panels include kinases spread broadly across the kinome. Click below for a full list of kinases included in our K192 (192 full-length kinases) and K240 (240 full-length kinases) panels.

k192-k240-panel-key
Click to see full list of kinases on panel
AAK1 CDK2 + Cyclin E1 DYRK1A HIPK4 MAP3K4 NEK3 PTK6 STK3
ABL1 CDK20 + Cyclin H DYRK1B HUNK MAP3K9 NEK4 RET STK32A
ABL2 CDK3 + Cyclin E1 EIF2AK4 k2 domain ICK MAP4K1 NEK5 RIOK2 STK32B
AKT2 CDK4 + Cyclin D3 EPHA1 IGF1R MAP4K2 NEK6 RIPK1 STK33
AURKA CDK5 + CDK5R1 EPHA2 IKBKE MAP4K3 NEK9 RIPK2 STK35
AURKB CDK6 + Cyclin D1 EPHA4 INSR MAP4K5 NIM1K RIPK3 STK36
AURKC CDK7 EPHA5 IRAK3 MAPK11 NLK ROCK1 STK38
AXL CDK8 + Cyclin C EPHA6 IRAK4 MAPK14 NTRK1 ROCK2 STK38L
BLK CDK9 + Cyclin K EPHA7 ITK MAPK4 NTRK2 RON STK4
BMP2K CDKL1 EPHA8 JAK2 (V617F) MAPK6 NUAK1 RPS6KA1 TBK1
BMX CDKL2 EPHB1 JAK3 MAPK8 PAK4 RPS6KA2 TEC
BRAF (V600E) CDKL3 EPHB3 JNK3 MAPK9 PAK6 RPS6KA3 TEK
BRSK1 CDKL5 EPHB4 KIT MARK2 PHKG1 RPS6KA4 TESK1
BRSK2 CHEK1 ERN1 LATS1 MARK3 PHKG2 RPS6KA6 TIE1
BTK CHEK2 ERN2 LATS2 MARK4 PIK3C3 SBK3 TLK1
CAMK1 CLK1 FER LCK MAST3 PIKFYVE SGK1 TLK2
CAMK1D CLK2 FES LIMK1 MAST4 PIP4K2C SGK2 TNK1
CAMK1G CLK4 FGFR1 LIMK2 MELK PIP5K1B SIK1 TNK2
CAMK2A CSF1R FGFR2 LRRK2 MERTK PKMYT1 SIK2 TNNI3K
CAMK2D CSK FGFR3 LTK MET PLK2 SIK3 TSSK1B
CASK CSNK1A1L FGFR4 LYN MKNK2 PLK3 SLK TTK
CDK1 + Cyclin B1 CSNK1D FGR MAP2K5 MLTK PLK4 SNRK TXK
CDK10 + Cyclin L2 CSNK1E FLT3 MAP3K10 MOK PRKAA1 SRC TYK2
CDK14 + Cyclin Y CSNK1G2 FRK MAP3K11 MUSK PRKAA2 SRMS TYRO3
CDK15 + Cyclin Y CSNK2A1 FYN MAP3K12 MYLK2 PRKACA STK10 ULK1
CDK16 + Cyclin Y CSNK2A2 GAK MAP3K13 MYLK3 PRKACB STK11 ULK2
CDK17 + Cyclin Y DAPK2 GSK3A MAP3K19 MYLK4 PRKCE STK16 ULK3
CDK18 + Cyclin Y DCLK3 GSK3B MAP3K2 NEK1 PRKX STK17B WEE1
CDK19 + Cyclin C DDR1 HIPK2 MAP3K21 NEK11 PTK2 STK24 WEE2
CDK2 + Cyclin A1 DDR2 HIPK3 MAP3K3 NEK2 PTK2B STK26 YES1

 

k240-k192-kinase-tree
Can't find your kinase on the panel?
See the Kinase Target Engagement Assay Selection Table for a full list of kinase vectors available for use with NanoBRET™ TE Intracellular Kinase Assays. Tell us which kinase you are looking for and we can help!
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Want to run the kinase selectivity assay yourself?
We offer the NanoBRET™ Target Engagement (TE) K192 Kinase Selectivity System that can be run in your lab to quantitatively measure intracellular compound occupancy against a panel of 192 kinases in a single experiment.

Data

Easily Follow-up Your Hits with Compound IC50 Determinations

Our service can help you determine compound affinity for kinase hits. Example data below shows the IC50 kinase profiles for individual kinase hits identified from selectivity profiling data. 

ic50s-dabrafenib-nbte-9-kinases
The selectivity profile for 156nM dabrafenib and was obtained using the NanoBRET™ TE K240 Kinase Selectivity Panel. Individual NanoBRET™ TE Kinase Assays for each of the nine kinase hits identified from dabrafenib K240 profile were used to determine the affinity of dabrafenib for each kinase.
cellchemicalbiologypaper
Learn how NanoBRET™ TE could be used to quantitatively profile compound occupancy against hundreds of kinases in live cells.
Read Paper

Publications

The NanoBRET™ TE Kinase Selectivity System is the chosen method in a variety of peer-reviewed publications. See details in the following publications:  

  1. Vasta, J.D. et al. (2018) Quantitative, Wide-Spectrum Kinase Profiling in Live Cells for Assessing the Effect of Cellular ATP on Target Engagement. Cell Chem. Biol. 25, 206.
  2. Wells, C. et al. (2020) Quantifying CDK Inhibitor Selectivity in Live Cells. Nat. Commun. 11(1), 2743.
  3. Ong, L.L. et al. (2020) A High-Throughput BRET Cellular Target Engagement Assay Links Biochemical to Cellular Activity for Bruton’s Tyrosine Kinase. SLAS Discov. 25(2), 176.
  4. Robers, M.B. et al. (2015) Target Engagement and Drug Residence Time Can Be Observed in Living Cells with BRET. Nat. Commun. 6, 10091
  5. Jin, H.Y. et al. (2020) High-Throughput Implementation of the NanoBRET Target Engagement Intracellular Kinase Assay to Reveal Differential Compound Engagement by SIK2/3 Isoforms. SLAS Discov. 25(2), 215.

Have questions about our kinase profiling services? We're here to help!