tkELECT^SM - Personalized Screening & Profiling

Customized compound profiling using our expanding menu of tyrosine kinase assays. Choose from a large collection of whole cell, functional assays that monitor the activity of a specific receptor tyrosine kinase (RTK) or cytosolic tyrosine kinase (CTK) by measuring the tyrosine phosphorylation status of proteins in their natural cellular environment. tkELECT is a flexible solution with multiple applications including, primary HTS & lead discovery and ongoing lead optimization & SAR and is ideal for identifying novel receptor tyrosine kinase inhibitors, allosteric modulators or antibody therapeutics.

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Panel Features & Benefits

Customized screening and profiling - choose from 34 RTK and CTK assays
High quality reproducible data
Flexible - standardized or custom panels
Inhibitor and agonist mode – identify small molecule inhibitors and/or antibody therapeutics
Broad applications – including specificity and compound liability

How it Works

Receptor Tyrosine Kinases - Ideal for Small Molecule and Antibody Discovery

Unlike biochemical assays that commonly use a truncated version of the receptor, our cell-based kinase assays utilize wild-type, full length proteins that allow all steps in receptor activation to be monitored. This whole cell assay platform is ideal for identifying novel receptor tyrosine kinase inhibitors, allosteric modulators or antibody therapeutics.

A serious of commercially available anti-receptor antibodies (neutralizing antibodies) were tested with cells expressing the ErbB1 receptor and dose dependent inhibition was observed (left panel). Cells expressing TrkA, TrkB, or TrkC were used to identify, screen or profile small molecule inhibitors (right panel).

tkELECT Assay Panel

Listed below are the assays currently available for screening and profiling.

Gene Symbol ▲	Kinase Name	Entrez Gene Symbol
AXL	AXL receptor tyrosine kinase (AXL)	AXL
BLK	B lymphoid tyrosine kinase (BLK)	BLK
BTK	Bruton agammaglobulinemia tyrosine kinase (BTK)	BTK
cINSRa	Insulin receptor, isoform A (INSR)	cINSRa
cINSRb	Insulin receptor, isoform B (INSR)	cINSRb
c-KIT	v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog (KIT)	c-KIT
CLK1	CDC-Like Kinase 1 (CLK1)	CLK1
CLK2	CDC-Like Kinase 2 (CLK2)	CLK2
c-Ret-GFRα1	Proto-oncogene tyrosine-protein kinase receptor Ret (RET)	c-Ret-GFRα1
c-Ret-GFRα2	Proto-oncogene tyrosine-protein kinase receptor Ret (RET)	c-Ret-GFRα2
CSF1R	colony-stimulating factor 1 receptor (CSF1R)	CSF1R
CSF3R-JAK1	colony stimulating factor 3 receptor (CSF3R-JAK1)	CSF3R-JAK1
CSNK1D	casein kinase 1, delta (CSNK1D)	CSNK1D
DDR1	Discoidin domain receptor 1 (CD167a)	DDR1
EGFR/ErbB3	Epidermal growth factor receptor	EGFR
EphA4	EPH receptor A4 (EphA4)	EphA4
EphA5	Ephrin type-A receptor 5 (EphA5)	EphA5
EphA7	Ephrin type-A receptor 7 (EphA7)	EphA7
EphB1	Ephrin type-B receptor 1 (EphB1)	EphB1
EphB2	Ephrin type-B receptor 2 (EphB2)	EphB2
EphB3	Ephrin type-B receptor 3 (EphB3)	EphB3
EphB4	Ephrin type-B receptor 4 (EphB4)	EphB4
EpoR-JAK2	Erythropoietin receptor (EpoR)	EpoR-JAK2
ErbB1	v-erb-b2 erythroblastic leukemia viral oncogene homolog 1 (EGFR)	ErbB1
ErbB2-ErbB3	v-erb-b2 erythroblastic leukemia viral oncogene homolog 2 (HER2)	ErbB2-ErbB3
ErbB4	erb-b2 receptor tyrosine kinase 4	ErbB4
FGFR1	Fibroblast growth factor receptor 1 (FGFR1)	FGFR1
FGFR1-α-Klotho	Fibroblast Growth Factor Receptor 1 (FGFR1), α-Klotho	FGFR1-α-Klotho
FGFR1-β-Klotho	Fibroblast growth factor receptor 1 (FGFR1), β-Klotho	FGFR1-β-Klotho
FGFR4	Fibroblast growth factor receptor 4 (FGFR4)	FGFR4
FGFR4-α-Klotho	Fibroblast Growth Factor Receptor 4 (FGFR4), α-Klotho	FGFR4-α-Klotho
FGFR4-β-Klotho	Fibroblast growth factor receptor 4 (FGFR4), β-Klotho	FGFR4-β-Klotho
FGR	FGR proto-oncogene, Src family tyrosine kinase (FGR)	FGR
FLT4	fms-related tyrosine kinase 4 (FLT4)	FLT4
GHR-JAK1	Growth hormone receptor (GHR-JAK1)	GHR-JAK1
GHR-JAK2	Growth hormone receptor (GHR-JAK2)	GHR-JAK2
HCK	Hemopoietic cell kinase (HCK)	HCK
IGF1R	Insulin-like growth factor 1 receptor (IGF1R)	IGF1R
INSRa	Insulin receptor, isoform A (INSR)	INSRa
INSRb	Insulin receptor, isoform B (INSR)	INSRb
JAK3	Janus kinase 3 (JAK3)	JAK3
KDR	Kinase Insert Domain Receptor (VEGFR2)	KDR
MEK1	Mitogen-activated protein kinase kinase 1 (MAP2K1)	MEK1
mINSRa	Insulin receptor, isoform A (INSR)	mINSRa
mINSRb	Insulin receptor, isoform B (INSR)	mINSRb
PDGFRa	Platelet-derived growth factor receptor alpha (PDGFRa)	PDGFRa
PDGFRb	Platelet-derived growth factor receptor beta (PDGFRb)	PDGFRB
PI3Kδ	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit delta)	PI3Kδ
PIM1	Pim-1 oncogene (PIM1)	PIM1
PRLR-JAK1	Prolactin receptor (PRLR)	PRLR-JAK1
PRLR-JAK2	Prolactin receptor (PRLR)	PRLR-JAK2
PYK2	PTK2B protein tyrosine kinase 2 beta (PTK2B)	PYK2
rhTrkA-rhP75	Neurotrophic tyrosine kinase receptor type 1 (NTRK1)	rhTrkA-rhP75
RIPK1	Receptor (TNFRSF)-Interacting Serine-Threonine Kinase 1 (RIPK1)	RIPK1
RIPK2	Receptor-interacting serine-threonine kinase 2 (RIPK2)	RIPK2
RIPK3	Receptor-Interacting Serine-Threonine Kinase 3 (RIPK3)	RIPK3
rTrkA-rP75	Neurotrophic tyrosine kinase receptor type 1 (NTRK1)	rTrkA-rP75
SIK1	Salt-inducible kinase 1 (SIK1)	SIK1
SYK	Spleen tyrosine kinase (SYK)	SYK
Tie2	Angiopoietin-1 receptor (Tie2)	Tie2
TrkA	Neurotrophic tyrosine kinase receptor type 1 (NTRK1)	TrkA
TrkA-P75	Neurotrophic tyrosine kinase receptor type 1 (NTRK1)	TrkA-P75
TrkB	Neurotrophic tyrosine kinase receptor type 2 (NTRK2)	TrkB
TrkB-P75	Neurotrophic tyrosine kinase receptor type 2 (NTRK2)	TrkB-P75
TrkC	Neurotrophic tyrosine kinase receptor type 3 (NTRK3)	TrkC
TrkC-P75	Neurotrophic tyrosine kinase receptor type 3 (NTRK3)	TrkC-P75
TYK2	Tyrosine kinase 2 (TYK2)	TYK2
YES1	v-yes-1 Yamaguchi sarcoma viral oncogene homolog 1 (YES)	YES1

Data Analysis & Interpretation

Definitions

Percent Activity/Inhibition

The results for single concentration (primary screen) for tested compound(s) are reported in your study report and spreadsheets as '% Activity' or '% Inhibition' and are calculated in the following manner:

% Activity
(Agonist Mode) =
100% x

[

Mean RLU _{(test sample)}- Mean RLU_{(vehicle control)}

Mean MAX RLU _{(control ligand)}- Mean RLU _{(vehicle control)}

]

test sample = client supplied compound
vehicle control = DMSO (0% activity)
control ligand = control compound (100% activity)

% Inhibition
(Antagonist mode) =
100% x

[

Mean RLU _{(test sample)}- Mean RLU_{(vehicle control)}

Mean MAX RLU _{(control ligand)}- Mean RLU _{(vehicle control)}

]

test sample = client supplied compound
vehicle control = DMSO (0% activity)
EC80 control = control compound (80% activity)

Dose Response Curve (EC50/IC50)

The results for 10-point dose response curve compound/target interactions are reported in the study report and spreadsheets as EC50/IC50, which are values derived using the Hill equation:

tkELECTSM - Personalized Screening & Profiling