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 300 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 K300 (300 full-length kinases) panels.

Click to see full list of kinases on panel

AAK1	CDK14 + Cyclin Y	DCLK3	HCK	MAP3K9	NIM1K	PRKCG	STK26
ABL1	CDK15 + Cyclin Y	DDR1	HIPK2	MAP4K1	NLK	PRKCH	STK3
ABL2	CDK16 + Cyclin Y	DDR2	HIPK3	MAP4K2	NTRK1	PRKCQ	STK32A
ACVR1	CDK17 + Cyclin Y	DYRK1A	HIPK4	MAP4K3	NTRK2	PRKG2	STK32B
ACVR1B	CDK18 + Cyclin Y	DYRK1B	HUNK	MAP4K5	NTRK3	PRKX	STK33
ACVRL1	CDK19 + Cyclin C	DYRK2	ICK	MAPK1	NUAK1	PTK2	STK35
ADK	CDK2 + Cyclin A1	EGFR	IGF1R	MAPK11	NUAK2	PTK2B	STK36
AKT1	CDK2 + Cyclin E1	EIF2AK4 k2 domain	IKBKE	MAPK14	PAK4	PTK6	STK38
AKT2	CDK20 + Cyclin H	EPHA1	INSR	MAPK15	PAK6	RET	STK38L
ALK	CDK3 + Cyclin E1	EPHA10	IRAK1	MAPK3	PDPK1	RIOK2	STK4
ARAF	CDK4 + Cyclin D3	EPHA2	IRAK3	MAPK4	PHKG1	RIPK1	TBK1
AURKA	CDK5 + CDK5R1	EPHA3	IRAK4	MAPK6	PHKG2	RIPK2	TEC
AURKB	CDK6 + Cyclin D1	EPHA4	ITK	MAPK8	PIK3C3	RIPK3	TEK
AURKC	CDK7	EPHA5	JAK2	MAPK9	PIK3CA + PIK3R1	ROCK1	TESK1
AXL	CDK8 + Cyclin C	EPHA6	JAK2 (V617F)	MARK1	PIK3CB + PIK3R1	ROCK2	TGFBR1
BLK	CDK9 + Cyclin K	EPHA7	JAK3	MARK2	PIK3CD + PIK3R1	RON	TGFBR2
BMP2K	CDKL1	EPHA8	JNK3	MARK3	PIKFYVE	RPS6KA1	TIE1
BMPR1A	CDKL2	EPHB1	KIT	MARK4	PIM1	RPS6KA2	TLK1
BMX	CDKL3	EPHB2	LATS1	MAST3	PIM2	RPS6KA3	TLK2
BRAF (V600E)	CDKL5	EPHB3	LATS2	MAST4	PIM3	RPS6KA4	TNK1
BRAF	CHEK1	EPHB4	LCK	MELK	PIP4K2C	RPS6KA6	TNK2
BRSK1	CHEK2	ERN1	LIMK1	MERTK	PIP5K1B	SBK3	TNNI3K
BRSK2	CIT	ERN2	LIMK2	MET	PKMYT1	SGK1	TSSK1B
BTK	CLK1	FER	LRRK2	MKNK2	PKN1	SGK2	TTK
CAMK1	CLK2	FES	LTK	MLTK	PKN2	SGK3	TXK
CAMK1D	CLK4	FGFR1	LYN	MOK	PKN3	SIK1	TYK2
CAMK1G	COQ8B	FGFR2	MAP2K5	MUSK	PLK1	SIK2	TYRO3
CAMK2A	CRAF	FGFR3	MAP2K6	MYLK2	PLK2	SIK3	ULK1
CAMK2B	CSF1R	FGFR4	MAP3K10	MYLK3	PLK3	SLK	ULK2
CAMK2D	CSK	FGR	MAP3K11	MYLK4	PLK4	SNRK	ULK3
CAMK2G	CSNK1A1L	FLT1	MAP3K12	NEK1	PRKAA1	SRC	VRK2
CASK	CSNK1D	FLT3	MAP3K13	NEK11	PRKAA2	SRMS	WEE1
CDK1 + Cyclin B1	CSNK1E	FRK	MAP3K19	NEK2	PRKACA	STK10	WEE2
CDK10 + Cyclin L2	CSNK1G2	FYN	MAP3K2	NEK3	PRKACB	STK11	YES1
CDK11A + Cyclin K	CSNK2A1	GAK	MAP3K21	NEK4	PRKCA	STK16
CDK11B + Cyclin B	CSNK2A2	GRK7	MAP3K3	NEK5	PRKCB	STK17A
CDK12	DAPK2	GSK3A	MAP3K4	NEK6	PRKCD	STK17B
CDK13	DCLK1	GSK3B	MAP3K7/TAB1	NEK9	PRKCE	STK24

(click to expand)

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 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.

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