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

Trusted NanoBRET™ Target Engagement technology

Close collaboration with our scientists from start to finish

Cellular assay provides biologically relevant results

Technology Overview

How NanoBRET™ Target Engagement Works

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.

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.

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

Biochemical: 123 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.

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

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.

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.

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:

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.
Wells, C. et al. (2020) Quantifying CDK Inhibitor Selectivity in Live Cells. Nat. Commun. 11(1), 2743.
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.
Robers, M.B. et al. (2015) Target Engagement and Drug Residence Time Can Be Observed in Living Cells with BRET. Nat. Commun. 6, 10091
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!