Information on EC 2.7.10.1 - receptor protein-tyrosine kinase and Organism(s) Homo sapiens and UniProt Accession P04626

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UNIPROT: P04626
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The taxonomic range for the selected organisms is: Homo sapiens

The enzyme appears in selected viruses and cellular organisms

EC NUMBER
COMMENTARY hide
2.7.10.1
-
RECOMMENDED NAME
GeneOntology No.
receptor protein-tyrosine kinase
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
ATP + a [protein]-L-tyrosine = ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
active site structure, activation mechanism
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phospho group transfer
-
-
-
-
SYSTEMATIC NAME
IUBMB Comments
ATP:[protein]-L-tyrosine O-phosphotransferase (receptor-type)
The receptor protein-tyrosine kinases, which can be defined as having a transmembrane domain, are a large and diverse multigene family found only in Metazoans [1]. In the human genome, 58 receptor-type protein-tyrosine kinases have been identified and these are distributed into 20 subfamilies.
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
metabolism
physiological function
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
ATP + Ac-DYFE-6-chloro-W-NHMe
ADP + Ac-DYpFE-6-chloro-W-NHMe
show the reaction diagram
substrate identified by substrate-activity-screening methodology based on optimization of substrate YFEW in a modular manner
-
-
?
ATP + Ac-DYFGW-NHMe
ADP + Ac-DYpFGW-NHMe
show the reaction diagram
substrate identified by substrate-activity-screening methodology based on optimization of substrate YFEW in a modular manner
-
-
?
ATP + G protein-coupled receptor kinase-2
ADP + phosphorylated G protein-coupled receptor kinase-2
show the reaction diagram
ATP + insulin receptor substrate 1-L-tyrosine
ADP + insulin receptor substrate 1-L-tyrosine phosphate
show the reaction diagram
-
peptide derived from the regulatory domain of insulin receptor
-
-
?
ATP + KKHTDDGYMPMSPGVA
ADP + KKHTDDGY-phosphate-MPMSPGVA
show the reaction diagram
-
commercial peptide substrate
-
-
?
ATP + KKSRGDYMTMQIG
ADP + KKSRGDY-phosphate-MTMQIG
show the reaction diagram
-
commercial peptide substrate
-
-
?
ATP + phosphatidylinositol 3-kinase
ADP + phosphorylated phosphatidylinositol 3-kinase
show the reaction diagram
-
binding of c-kit ligand, stem cell factor SCF to c-kit receptor c-kitR is known to activate c-kitR tyrosine kinase, thereby leading to autophosphorylation of c-kitR on Tyr and to association of c-kitR with substrates such as phosphatidylinositol 3-kinase
-
-
?
ATP + phosphoinositide-dependent kinase-1-L-tyrosine
ADP + phosphoinositide-dependent kinase-1-L-tyrosine phosphate
show the reaction diagram
-
insulin-like growth factor-1 receptor directly interacts with and activates phosphoinositide-dependent kinase-1
-
-
?
ATP + phospholipase C gamma
ADP + phosphorylated phospholipase C gamma
show the reaction diagram
ATP + poly(Glu-Ala-Tyr)
ADP + poly(Glu-Ala-Tyr)-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + poly(Glu:Tyr)
ADP + poly(Glu:Tyr) phosphate
show the reaction diagram
-
-
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
show the reaction diagram
ATP + YFEW
ADP + YpFEW
show the reaction diagram
tetrapeptide identified by substrate profiling
-
-
?
ATP + [beta-catenin]-Tyr142
ADP + [beta-catenin]-Tyr142 phosphate
show the reaction diagram
-
isoforms FGFR2, FGFR3, EGFR and TRKA directly phosphorylate beta-catenin at Tyr142, which increases cytoplasmic beta-catenin concentration via release of beta-catenin from membranous cadherin complexes
-
-
?
ATP + [endothelial growth-factor]-L-tyrosine
ADP + [endothelial growth-factor]-L-tyrosine phosphate
show the reaction diagram
-
EGFR tyrosine kinase
-
-
?
ATP + [poly-(Glu,Tyr)1:4]
ADP + [poly-(Glu,Tyr)1:4]-tyrosine phosphate
show the reaction diagram
-
synthetic substrate
-
-
?
ATP + [vascular endothelial growth-factor-1]-L-tyrosine
ADP + [vascular endothelial growth-factor-1]-L-tyrosine phosphate
show the reaction diagram
-
VEGFR-1 tyrosine kinase
-
-
?
poly(Glu:Tyr) + ATP
ADP + poly(Glu:Tyr) phosphate
show the reaction diagram
-
-
-
-
?
additional information
?
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
ATP + G protein-coupled receptor kinase-2
ADP + phosphorylated G protein-coupled receptor kinase-2
show the reaction diagram
-
GRK2 activation also increases GRK2 degradation and downregulation, independent of Gbetagamma subunits and phosphoinositide 3-kinase
-
-
?
ATP + phospholipase C gamma
ADP + phosphorylated phospholipase C gamma
show the reaction diagram
-
growth factor-induced tyrosine phosphorylation of PLC gamma is essential for stimulation of phosphatidylinositol hydrolysis in vitro and in vivo
-
-
ATP + poly(Glu:Tyr)
ADP + poly(Glu:Tyr) phosphate
show the reaction diagram
-
-
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
show the reaction diagram
P29320
autophosphorylated on tyrosine and also mediated tyrosine phosphorylation of casein
-
-
?
ATP + [beta-catenin]-Tyr142
ADP + [beta-catenin]-Tyr142 phosphate
show the reaction diagram
-
isoforms FGFR2, FGFR3, EGFR and TRKA directly phosphorylate beta-catenin at Tyr142, which increases cytoplasmic beta-catenin concentration via release of beta-catenin from membranous cadherin complexes
-
-
?
ATP + [endothelial growth-factor]-L-tyrosine
ADP + [endothelial growth-factor]-L-tyrosine phosphate
show the reaction diagram
-
EGFR tyrosine kinase
-
-
?
ATP + [vascular endothelial growth-factor-1]-L-tyrosine
ADP + [vascular endothelial growth-factor-1]-L-tyrosine phosphate
show the reaction diagram
-
VEGFR-1 tyrosine kinase
-
-
?
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Cr3+
-
activates insulin receptor tyrosine phosphorylation in vivo
hydrogen peroxide
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insulin-induced ROS production, limited exposure enhances insulin-induced autophosphorylation of the insulin receptor, while prolonged exposure impairs the action of insulin
Zn2+
-
presence of Zn2+ at 0.1 mM rapidly activates isoform ALK. This activation is dependent of ALK tyrosine kinase activity and dimerization of the receptor but is independent of Src family kinase activity. Addition of sodium pyrithione, a zinc ionophore, leads to a further activation of ALK. This stronger activation is dependent of Src family kinase but independent of ALK activity and dimerization
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(2R)-2-[(4-[[1-(1,3-thiazol-4-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
-
(2R)-2-[(4-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]-N,N-dimethylpropanamide
-
-
(2R)-2-[(4-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]-N-methylpropanamide
-
-
(2R)-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
-
(2R)-N,N-dimethyl-2-[(4-[[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
-
(2R)-N,N-dimethyl-2-[(4-[[1-(1,3-thiazol-4-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
-
(2R)-N,N-dimethyl-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
-
(2R)-N,N-dimethyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
-
-
(2R)-N-methyl-2-[(4-[[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
-
(2R)-N-methyl-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
-
(2S)-2-[(4-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]-N,N-dimethylpropanamide
-
-
(2S)-N,N-dimethyl-2-[(4-[[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
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-
(2S)-N,N-dimethyl-2-[(4-[[1-(1,3-thiazol-4-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
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-
(2S)-N,N-dimethyl-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
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3-[[5-([6-amino-5-[(E)-(methoxyimino)methyl]pyrimidin-4-yl]amino)-1H-indazol-1-yl]methyl]benzonitrile
-
-
4-amino-6-(1H-indazol-5-ylamino)pyrimidine-5-carbaldehyde O-methyloxime
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4-amino-6-([3-chloro-4-[(3,5-difluorobenzyl)oxy]phenyl]amino)pyrimidine-5-carbaldehyde O-methyloxime
-
-
4-amino-6-([3-chloro-4-[(3-fluorobenzyl)oxy]phenyl]amino)pyrimidine-5-carbaldehyde O-methyloxime
-
-
4-amino-6-[(1-benzyl-1H-indazol-5-yl)amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
4-amino-6-[(3-bromophenyl)amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
4-amino-6-[(3-chloro-4-fluorobenzyl)amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
4-amino-6-[(3-chloro-4-fluorophenyl)amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
4-amino-6-[[1-(3-chlorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(1-methylethyl)oxime
-
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(2-methoxybenzyl)oxime
-
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(2-methoxyethyl)oxime
-
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(2-methylpropyl)oxime
-
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-benzyloxime
-
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-ethyloxime
-
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde oxime
-
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
4-amino-6-[[1-(3-fluorobenzyl)-2,3-dihydro-1H-indol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
4-amino-6-[[1-(3-methoxybenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
4-amino-6-[[1-(4-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
4-amino-6-[[2-(3-fluorobenzyl)-1H-benzimidazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
4-amino-6-[[4-(benzyloxy)-3-chlorophenyl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
4-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]-6-(methylamino)pyrimidine-5-carbaldehyde O-methyloxime
-
39% inhibition of ErbB-2 at 0.01 mM
5-(2-morpholin-4-yl-2-oxoethoxy)-N-[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
-
-
5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
-
-
5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(1,3-thiazol-4-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
-
-
5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
-
-
5-[(1R)-1-methyl-2-oxo-2-pyrrolidin-1-ylethoxy]-N-[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
-
-
5-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
-
-
5-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
-
-
AG1478
-
specific tyrosine kinase inhibitor of EGFR, does not inhibit epidermal growth factor-induced or heregulin beta-induced HER2 phosphorylation. Cleavage of HER4 and dimerization of HER4/HER2 occur together with reactivation of HER3 via HER2/HER3, leading to persistent HER2 phosphorylation in the now resistant, surviving cells
herceptin
-
combined therapy with herceptin and iressa exerts a greater suppression in HER2 activation
-
Iressa
-
gefitinib, specific tyrosine kinase inhibitor of EGFR, does not abolish basal HER2 phosphorylation. Cleavage of HER4 and dimerization of HER4/HER2 occur together with reactivation of HER3 via HER2/HER3, leading to persistent HER2 phosphorylation in the now resistant, surviving cells. Combined therapy with herceptin and iressa exerts a greater suppression in HER2 activation
N,N-dimethyl-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]acetamide
-
-
N-[1-(3-fluorobenzyl)-1H-indazol-5-yl]-5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine
-
-
(2R)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N,N-dimethylpropanamide
-
-
(2R)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N-(2-hydroxyethyl)-N-methylpropanamide
-
-
(2R)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N-methylpropanamide
-
-
(2R)-N,N-dimethyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
-
-
(2R)-N-(2-hydroxyethyl)-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
-
-
(2R)-N-(2-hydroxyethyl)-N-methyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
-
-
(2R)-N-(2-methoxyethyl)-N-methyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
-
-
(2S)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N,N-dimethylpropanamide
-
-
(2S)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N-(2-hydroxyethyl)-N-methylpropanamide
-
-
(2S)-N,N-dimethyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
-
-
(2S)-N-(2-hydroxyethyl)-N-methyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
-
-
(Z)-5-[6-[3-(4-methoxyphenyl)-ureido]-2-oxo-1,2-dihydroindol-3-ylidene-methyl]-4-methyl-1H-pyrrole-3-carboxylic acid
potent inhibitor against tyrosine kinases, including VEGFR and PDGFR families, as well as Aurora kinases
1-(4-(1H-pyrazol-1-yl)phenyl)-3-(2-aminoquinazolin-6-yl)-4-methylpyridin-2(1H)-one
-
-
1-(4-acetylphenyl)-3-(2-aminoquinazolin-6-yl)-4-methylpyridin-2(1H)-one
-
-
1-(4-aminophenyl)-3-[3-(1,3-benzodioxol-5-yl)-4-oxo-2,4-dihydroindeno[1,2-c]pyrazol-5-yl]urea
1-(4-aminophenyl)-3-[3-(3,4-dihydroxyphenyl)-4-oxo-2,4-dihydroindeno[1,2-c]pyrazol-5-yl]urea
1-(4-aminophenyl)-3-[3-(4-hydroxyphenyl)-4-oxo-2,4-dihydroindeno[1,2-c]pyrazol-5-yl]urea
1-(4-aminophenyl)-3-[3-(4-methoxyphenyl)-4-oxo-2,4-dihydroindeno[1,2-c]pyrazol-5-yl]urea
1-(4-hydroxyphenyl)-3-[3-(4-methoxyphenyl)-4-oxo-2,4-dihydroindeno[1,2-c]pyrazol-5-yl]urea
1-[3-(1,3-benzodioxol-5-yl)-4-oxo-2,4-dihydroindeno[1,2-c]pyrazol-5-yl]-3-(4-hydroxyphenyl)urea
2,4,6-trihydroxydeoxybenzoin derivatives
-
diverse derivatives, analysis of inhibitory effect on EGFR tyrosine kinase activity, overview
-
2-[(2-cyanobenzyl)oxy]-N-(3-hydroxyphenyl)-4-[3-(pyrrolidin-1-yl)propoxy]benzamide
most potent inhibitor in a series of benzanilides. Effect depends on the 3'-OH-Ph and 2''-CN-benzyl working co-operatively to deliver maximum inhibition. Modeling studies suggest a novel binding mode, incorporating a water molecule bound between these two groups and concomitant binding to the hinge
2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N-(2-hydroxyethyl)-N-methylacetamide
-
-
2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]acetamide
-
-
2-[5-(benzylthio)-1,3,4-oxadiazol-2-yl]-N-[4-[5-(benzylthio)-1,3,4-oxadiazol-2-yl]phenyl]aniline
49% inhibition at 0.01 mM, antiproliferative activity on human breast cancer cell line MCF-7, IC50 value 0.00073 mM
2-[7-(4-[[4-(imidazo[1,2-a]pyridin-3-yl)pyrimidin-2-yl]amino]-3-methoxyphenyl)-9-oxa-3,7-diazabicyclo[3.3.1]non-3-yl]ethanol
-
compound shows good IGF-1R inhibitory activity in a cellular assay and a high free fraction in human plasma. However this compound shows a higher affinity for the hERG channel
3-(2-aminoquinazolin-6-yl)-1-(2-cyclopentylethyl)-4-methylpyridin-2(1H)-one
-
cyclopentylethyl
3-(2-aminoquinazolin-6-yl)-1-(3,3-dimethylindolin-6-yl)-4-methylpyridin-2(1H)-one
-
pyridone, nonselective inhibitor of c-Kit
3-(2-aminoquinazolin-6-yl)-1-(3-fluoro-4-methylphenyl)-4-methylpyridin-2(1H)-one
-
-
3-(2-aminoquinazolin-6-yl)-1-(3-methoxyphenyl)-4-methylpyridin-2(1H)-one
-
-
3-(2-aminoquinazolin-6-yl)-1-(4-chloro-3-fluorophenyl)-4-methylpyridin-2(1H)-one
-
-
3-(2-aminoquinazolin-6-yl)-1-(4-chlorophenyl)-4-methylpyridin-2(1H)-one
-
-
3-(2-aminoquinazolin-6-yl)-1-(4-fluoro-3-methylphenyl)-4-methylpyridin-2(1H)-one
-
-
3-(2-aminoquinazolin-6-yl)-1-(4-methoxyphenyl)-4-methylpyridin-2(1H)-one
-
-
3-(2-aminoquinazolin-6-yl)-1-(4-tert-butylphenyl)-4-methylpyridin-2(1H)-one
-
exhibits poor selectivity
3-(2-aminoquinazolin-6-yl)-4-methyl-1-(3-(trifluoromethyl)phenyl)pyridin-2(1H)-one
-
-
3-(2-aminoquinazolin-6-yl)-4-methyl-1-(4-(oxazol-2-yl)phenyl)pyridin-2(1H)-one
-
exhibits potent inhibition of c-Kit, greater than 200fold selectivity against KDR, p38, Lck, and Src, and desirable pharmacokinetic properties
3-(2-aminoquinazolin-6-yl)-4-methyl-1-(4-(trifluoromethyl)phenyl)pyridin-2(1H)-one
-
-
3-(2-aminoquinazolin-6-yl)-4-methyl-1-(4-morpholinophenyl)pyridin-2(1H)-one
-
-
3-(2-aminoquinazolin-6-yl)-4-methyl-1-phenylpyridin-2(1H)-one
-
-
3-(N-3-carboxyphenylaminomethyl)-2-phenylboronic acid
-
inhibition of EGFR tyrosine kinase
-
3-[[5-([6-amino-5-[(E)-(methoxyimino)methyl]pyrimidin-4-yl]amino)-1H-indazol-1-yl]methyl]benzonitrile
-
-
4-(2',5'-dihydroxybenzylamino)phenylboronic acid
-
inhibition of EGFR tyrosine kinase
-
4-(3-chloroanilino)-6,7-dimethoxyquinazoline
-
-
4-(5-((2-methoxyethyl)carbamoyl)naphthalen-2-yloxy)-7-methoxyquinoline-6-carboxamide
-
-
4-(5-((4-chlorophenyl)carbamoyl)naphthalen-2-yloxy)-7-methoxyquinoline-6-carboxamide
-
-
4-(5-((4-chlorophenyl)carbamoyl)naphthalen-2-yloxy)-N-methylpicolinamide
-
-
4-(5-(cyclopropylcarbamoyl)naphthalen-2-yloxy)-7-methoxyquinoline-6-carboxamide
-
-
4-(5-bromoindole-3-yl)-6,7-dimethoxyquinazoline
-
relatively potent inhibitor of EGFR-TK activity
4-(5-carbamoylnaphthalen-2-yloxy)-7-methoxyquinoline-6-carboxamide
-
-
4-(5-chloro-6-fluoro-indole-3-yl)-6,7-di-(2-methoxyethoxy)quinazoline
-
relatively potent inhibitor of EGFR-TK activity
4-(5-chloro-6-fluoroindole-3-yl)-6,7-dimethoxyquinazoline
-
relatively potent inhibitor of EGFR-TK activity, is a dual EGFR-TK and HER-2-TK inhibitor
4-(5-chloro-6-fluoroindole-3-yl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazoline
-
relatively potent inhibitor of EGFR-TK activity, is a dual EGFR-TK and HER-2-TK inhibitor
4-(6-fluoro-5-methylindole-3-yl)-6,7-dimethoxyquinazoline
-
relatively potent inhibitor of EGFR-TK activity
4-(imidazo[1,2-a]pyridin-3-yl)-N-[2-methoxyphenyl-4-(4-piperidinyl)]pyrimidin-2-amine
-
-
4-(imidazo[2-methoxy-4-(9-oxa-3,7-diazabicyclo[3.3.1]non-3-yl)phenyl])pyrimidin-2-amine
-
-
4-(N-3-carboxyphenylaminomethyl)-2-phenylboronic acid
-
inhibition of EGFR tyrosine kinase
-
4-amino-1-tert-butyl-3-(1'-naphthyl)pyrazolo[3,4-d]pyrimidine
-
-
4-amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine
4-amino-6-(1H-indazol-5-ylamino)pyrimidine-5-carbaldehyde O-methyloxime
-
-
4-amino-6-([3-chloro-4-[(3,5-difluorobenzyl)oxy]phenyl]amino)pyrimidine-5-carbaldehyde O-methyloxime
-
-
4-amino-6-([3-chloro-4-[(3-fluorobenzyl)oxy]phenyl]amino)pyrimidine-5-carbaldehyde O-methyloxime
-
-
4-amino-6-[(1-benzyl-1H-indazol-5-yl)amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
4-amino-6-[(3-bromophenyl)amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
4-amino-6-[(3-chloro-4-fluorobenzyl)amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
4-amino-6-[(3-chloro-4-fluorophenyl)amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
4-amino-6-[[1-(3-chlorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(1-methylethyl)oxime
-
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(2-methoxybenzyl)oxime
-
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(2-methoxyethyl)oxime
-
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(2-methylpropyl)oxime
-
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-benzyloxime
-
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-ethyloxime
-
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde oxime
-
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
4-amino-6-[[1-(3-fluorobenzyl)-2,3-dihydro-1H-indol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
4-amino-6-[[1-(3-methoxybenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
4-amino-6-[[1-(4-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
4-amino-6-[[2-(3-fluorobenzyl)-1H-benzimidazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
4-amino-6-[[4-(benzyloxy)-3-chlorophenyl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
4-ethyl-3-[2-[4-(4-ethyl-5-thioxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenylamino]phenyl]-1H-1,2,4-triazole-5(4H)-thione
52% inhibition at 0.01 mM, antiproliferative activity on human breast cancer cell line MCF-7, IC50 value 0.00238 mM
4-methoxy-3-((2'-methoxybenzylamino)methyl)phenylboronic acid
-
inhibition of EGFR tyrosine kinase
-
4-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]-6-(methylamino)pyrimidine-5-carbaldehyde O-methyloxime
-
48% inhibition of EGFR at 0.002 mM
5,7-dihydroxyisoflavone derivatives
-
diverse derivatives, analysis of inhibitory effect on EGFR tyrosine kinase activity, overview
-
5-(4-(dihydroxyboranyl)benzylamino)-2-hydroxybenzoic acid
-
inhibition of EGFR tyrosine kinase
-
6-(1H-indol-5-ylmethyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
-
6-(1H-indol-5-ylmethyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
-
6-(3-bromobenzyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
-
6-(3-bromobenzyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
-
6-(6,7-dimethoxyquinazolin-4-yloxy)-1-naphthamide
-
-
6-(6,7-dimethoxyquinazolin-4-yloxy)-N-(2-methoxyethyl)-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide methanesulfonate
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(1-methylcyclopropyl)-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(2,2,2-trifluoroethyl)-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(2-fluorophenyl)-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(2-methoxyethyl)-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(3-(trifluoromethyl)phenyl)-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(3-fluorophenyl)-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(3-methoxypropyl)-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(3-methylisoxazol-5-yl)-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(4-(trifluoromethyl)phenyl)-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(4-fluorophenyl)-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(5-methylisoxazol-3-yl)-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(isoxazol-3-yl)-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(pyridin-2-yl)-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(pyridin-3-yl)-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(pyridin-4-yl)-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(thiazol-2-yl)-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-ethyl-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-isopropyl-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-methyl-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-p-tolyl-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-phenyl-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-propyl-1-naphthamide
-
-
6-(7-methoxyquinolin-4-yloxy)-1-naphthamide
-
-
6-(7H-pyrrolo[2,3-d]pyrimidin-4-yloxy)-N-(4-chlorophenyl)-1-naphthamide
-
-
6-[4-fluoro-3-(trifluoromethyl)benzyl]-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
-
6-[4-fluoro-3-(trifluoromethyl)benzyl]-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
-
AAL 993
AbI kinase
-
activated Abl kinase phosphorylates the EGFR at specific sites and uncouples the receptor from ligand-mediated internalization
-
active pharmacophore 1
-
derivative of lavendustin A, inhibition of EGFR tyrosine kinase
AG1296
-
FLT-3 inhibitor treatment results in formation of larger amounts of the mature 150 kDa form of mutant FLT-3 ITD
AG1478
AG556
-
highly selective EGFR kinase inhibitor, 0.01 mM inhibits human ether-a-go-go-related gene channel current and the effect is significantly countered by the protein tyrosine phosphatase inhibitor orthovanadate (1 mM)
Antibody
-
monoclonal antibodies for inhibition of IGF-IR alter receptor trafficking by high affinity binding, promoting receptor degradation and consequently preventing human tumor growth in vivo
-
AZD2171
-
inhibits VEGFR2
CEP-7055
-
inhibits VEGFR1-3
CEP701
-
inhibits FLT3
cisplatin
-
anti-cancer drug inhibiting receptor tyrosine kinases
cycloheximide
-
depletes the synthetic pool of Met receptor
doxorubicin
dynamin K44A
-
reduces EGFR internalization to 40%
-
erlotinib
ethyl 4-(3-(2-aminoquinazolin-6-yl)-4-methyl-2-oxopyridin-1(2H)-yl)benzoate
-
-
G protein-coupled receptor kinase-2
-
platelet-derived growth factor-dependent GRK2 phosphorylation desensitizes the PDGF receptor-beta
-
ganglioside GM3
-
0.062 mM, significant inhibition
gefinitib
-
i.e. ZD1839, highly specific inhibitor of EGFR tyrosine kinase and of HER1 tyrosine kinase, clinical effects, overview
-
gefitinib
geldanamycin
-
-
gemcitabine
genistein
GM3
-
inhibitory effect on tyrosine phosphorylation of both mono- and dimeric EGFR
herceptin
-
humanized monoclonal antibody
-
blocks the interaction of Ron with hepatocyte growth factor-like protein and diminishes Ron phosphorylation and its downstream signaling
-
hydrogen peroxide
-
limited exposure enhances insulin-induced autophosphorylation of the insulin receptor, while prolonged exposure impairs the action of insulin
imatinib
imatinib mesylate
-
potent inhibitor
Iressa
lavendustin A
-
-
lipid mimetic of GM3
-
inhibitory effect on tyrosine phosphorylation of both mono- and dimeric EGFR
lipid mimetic of lyso-GM3 dimer
-
inhibitory effect on tyrosine phosphorylation of both mono- and dimeric EGFR
luteolin
LY294002
-
PI3K/AKT inhibitor, has no effects on RON-mediated cell spreading either with or without MSP, but completely abrogates the cell survival properties of RON and reduces MSP-induced Transwell migration by 60-80%
lyso-GM3 dimer
-
inhibitory effect on tyrosine phosphorylation of both mono- and dimeric EGFR. A lipid mimetic of lyso-GM3 dimer shows similar strong inhibitory effect on EGF-induced EGFR tyrosine kinase activity, and similar low cytotoxicity, as the authentic lyso-GM3 dimer. Inhibits more strongly than GM3 or a lipid mimetic of GM3
MFCD09840836
-
mithramycin
-
inhibits binding of Sp factors to GC-rich sites, dramatically reduces Axl promoter activity and Axl, Sp1 and Sp3 expression
MLN518
-
inhibits FLT3
mouse monoclonal blocking antibody
-
increases apoptosis by 32% as compared to gemcitabine alone
-
N-(2,4-dichlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
-
N-(2-hydroxyethyl)-N-methyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]acetamide
-
-
N-(2-methoxyethyl)-6-(7-methoxyquinolin-4-yloxy)-1-naphthamide
-
-
N-(3,5-dichlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
-
N-(3-chlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
-
N-(4-chloro-3-(trifluoromethyl)phenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
-
N-(4-chlorophenyl)-3-(6,7-dimethoxyquinolin-4-yloxy)isoquinoline-8-carboxamide
-
-
N-(4-chlorophenyl)-6-((6,7-dimethoxyquinolin-4-yl)(methyl)amino)-1-naphthamide
-
-
N-(4-chlorophenyl)-6-(2-(methylamino)pyridin-4-yloxy)-1-naphthamide
-
-
N-(4-chlorophenyl)-6-(2-(methylamino)pyrimidin-4-yloxy)-1-naphthamide
-
-
N-(4-chlorophenyl)-6-(3-fluoro-6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
-
N-(4-chlorophenyl)-6-(6,7-dimethoxyquinazolin-4-yloxy)-1-naphthamide
-
-
N-(4-chlorophenyl)-6-(6,7-dimethoxyquinolin-4-ylamino)-1-naphthamide
-
-
N-(4-chlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
has significant antitumor efficacy against established HT29 human colon adenocarcinoma xenografts implanted in athymic mice
N-(4-chlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-5-fluoro-1-naphthamide
-
-
N-(4-chlorophenyl)-6-(6-(methylamino)pyrimidin-4-yloxy)-1-naphthamide
-
-
N-(4-chlorophenyl)-6-(7-methoxyquinolin-4-yloxy)-1-naphthamide
-
-
N-(4-chlorophenyl)-6-(pyridin-4-yloxy)-1-naphthamide
-
-
N-(4-chlorophenyl)-6-(pyrimidin-4-yloxy)-1-naphthamide
-
-
N-(4-chlorophenyl)-6-(quinolin-4-yloxy)-1-naphthamide
-
-
N-(4-chlorophenyl)-7-(6,7-dimethoxyquinolin-4-yloxy)quinoline-4-carboxamide
-
-
N-(4-tert-butylphenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
-
N-(5-tert-butylisoxazol-3-yl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
-
N-(cyclopropylmethyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
-
N-cyclobutyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
-
N-cyclopentyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
-
N-cyclopropyl-6-(6,7-dimethoxyquinazolin-4-yloxy)-1-naphthamide
-
-
N-cyclopropyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
-
N-cyclopropyl-6-(7-methoxyquinolin-4-yloxy)-1-naphthamide
-
-
N-ethyl-5-[2-[4-(5-(ethylamino)-1,3,4-thiadiazol-2-yl)phenylamino]-phenyl]-1,3,4-thiadiazol-2-amine
97.7% inhibition at 0.01 mM, antiproliferative activity on human breast cancer cell line MCF-7, IC50 value 0.00094 mM
N-tert-butyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
-
N-[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]-5-(2-morpholin-4-yl-2-oxoethoxy)quinazolin-4-amine
-
-
N-[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]-5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine
-
-
N-[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]-5-[2-(4-methylpiperazin-1-yl)-2-oxoethoxy]quinazolin-4-amine
-
-
N-[3-chloro-4-[(6-methylpyridin-3-yl)oxy]phenyl]-5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine
-
-
N-[3-methoxy-4-[(6-methylpyridin-3-yl)oxy]phenyl]-5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine
-
-
N-[3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]-5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine
-
-
N-[3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]-5-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine
-
-
N3-(6-aminopyridin-3-yl)-N1-(2-cyclopentylethyl)-4-methylisophthalamide
-
bisamide
N4-(2-fluoro-4-chlorophenyl)-6-(2,5-dimethoxybenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
-
shows potent inhibition of VEGFR-2 over EGFR, platelet-derived growth factor receptor-beta and VEGFR-1
N4-(3-bromo,4-fluorophenyl)-6-(2-pyridin-2-yl-ethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
-
in an in vivo B16-F10 syngeneic mouse tumor model, compound exhibits significant reduction in tumor growth rate, in tumor vascular density and in metastases to the lung compared to the control
N4-(3-bromo-phenyl)-7-(3,4,5-trimethoxy-benzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
-
dual inhibitor of platelet derived growth factor recptor-beta and vascular endothelial growth factor receptor 2
N4-(3-bromophenyl)-7-(1-naphthylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
-
-
N4-(3-bromophenyl)-7-(2-chlorobenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
-
dual inhibitor of platelet derived growth factor recptor-beta and vascular endothelial growth factor receptor 2. In a COLO-205, in vivo tumor mouse model, compound demonstrates inhibition of tumor growth, metastasis, and tumor angiogenesis
N4-(4-chloro-2-fluorophenyl)-6-(1-naphthylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
-
shows potent inhibition of VEGFR-2 over EGFR, platelet-derived growth factor receptor-beta and VEGFR-1
N4-(4-chloro-2-fluorophenyl)-6-(2-methylbenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
-
potent, multiple receptor tyrosine kinase inhibitor
N4-(4-chlorophenyl)-6-(2,5-dimethoxybenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
-
potent, multiple receptor tyrosine kinase inhibitor
NVP-BBT594
-
-
OSI-774
-
i.e. erlotinib, inhibits EGF receptor protein tyrosine kinase, binding to EGF receptor kinase, structure overview, anticancer drug
pazopanib
-
i.e. 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulphonamide, potent inhibitor of vascular endothelial growth factor receotors 1, 2, and 3, platelet-derived growth factor receptor alpha, platelet-derived growth factor receptor beta, and KIT
PD153035
-
specific inhibition of EGFR-TK, IC50 is 0.00329 mM with 1 U of purified EGFR-TK from A431 cells
PD168393
PF-2341066
-
IC50: 0.002 mM
PHA-665752
-
IC50: 0.0009 mM
phosphotyrosyl phosphatase Shp1
-
Shp1 binds to c-Kit at Y570 and acts by dephosphorylating the receptor directly, or inhibits c-Kit signalling indirectly by dephosphorylating other receptor-associated protein-tyrosine kinases
-
PKC412
-
inhibits FLT3
PKI-166
-
-
Protein kinase C
-
subsequently phosphorylates c-Kit on specific serine residues leading to negative regulation of c-Kit activation
-
protein tyrosine phosphatase 1B
-
PTP1B, requirement for Y1234 and Y1235 in the Met receptor activation loop for interaction with PTP1B
-
quercetin
Rapamycin
-
IC50: 3 nM
siRNA
-
sorafenib
Spry protein
-
-
-
STI-571
STI571
-
commercial Gleevec/Glivec, specific inhibitor
SU 11248
-
inhibits VEGFR2
SU 6668
-
inhibits VEGFR2 and PDGF receptor beta
SU11248
SU5416
-
selective inhibitor
sunitinib
T-cell phosphatase
-
TCPTP, requirement for Y1234 and Y1235 in the Met receptor activation loop for interaction with TCPTP
-
Tarceva
trichostatin A
-
the ability of RON to inhibit HIV-1 transcription is sensitive to a histone deacetylase inhibitor
tyrphostin 51
-
-
tyrphostin A9
-
PDGF receptor-specific
tyrphostin AG 1478
-
inhibition of EGF receptor
tyrphostin AG 370
-
PDGF receptor-specific
-
tyrphostin AG1478
-
EGFR-specific antagonist
tyrphostin B56
-
i.e. AG 556, selective EGFR and ErbB-1 kinase inhibitor, reduces volume-sensitive chloride current in atrial myocytes, is antagonized by pretreatment with VO43-
U0126
-
MEK/ERK inhibitor, has no effects on RON-mediated cell spreading either with or without MSP, but completely abrogates the cell survival properties of RON and reduces MSP-induced Transwell migration by 60-80%
vatalanib
-
i.e. ZK 222584 or PTK 787, inhibits VEGFR1-3
wogonin
-
slight inhibitory effect on epidermal growth factor receptor tyrosine kinase
Wortmannin
-
-
ZD1839
-
i.e. gefitinib, reversible inhibition of ErbB1, competitive to ATP, binding to EGF receptor kinase, structure overview, anticancer drug
ZD6474
-
inhibits VEGFR2
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
AG1478
-
increases HER2 phosphorylation in the presence of heregulin. Phosphorylation of HER2 is greater by heregulin beta and heregulin beta-1 in the presence of AG 1478
betacellulin
-
activates HER3 and HER4 via HER2
-
Epidermal growth factor
-
induces phosphorylation
heregulin
-
activates HER3 and HER4 via HER2
-
Iressa
-
acute treatment with 0.001 mM iressa induces a significant increase in HER2 phosphorylation
5-aza-2'-deoxycytidine
-
demethylation by 5-aza-2'-deoxycytidine upregulates Axl and Sp3 expression in low-Axl-expressing Colo206f/WiDr cells, but not in high-Axl-expressing Rko cells
5-fluorouracil
-
-
angiopoietin-1
-
angiotensin II
betacellulin
-
brain-derived neurotrophic factor
-
activates TrkB
-
Calmodulin
ligand-binding induced dimerization enables transautophosphorylation of ErbB1 which results in enhanced intracellular Ca2+ concentration activating calmodulin which reverses autoinhibition by net charge changes in the juxtamembranes
cisplatin
-
AXL can be induced by chemotherapy drugs in acute myeloid leukemia U937 cells and this induction is dependent on the CCWGG methylation status of the AXL promoter
clathrin
-
EGFR is internalized classicaly through clathrin-dependent endocytosis
-
Collagen
-
250 kDa dimeric DDR1a entity is phosphorylated upon ligand stimulation
Dok-7
-
a cytoplasmic post-synaptic protein coactivator of the muscle-specific receptor-tyrosine kinase MuSK
-
doxorubicin
-
AXL can be induced by chemotherapy drugs in acute myeloid leukemia U937 cells and this induction is dependent on the CCWGG methylation status of the AXL promoter
Epidermal growth factor
estrogen
-
induces Ret expression
Gas6
-
glial-derived neutrophic factor
-
triggers signaling pathway activation in breast tumor cell lines in a Ret-dependent manner. 10 ng/mL glial-derived neutrophic factor alone or in combination with 100ng/mL glial-derived neutrophic factor receptor alpha1 is the optimal concentration promoting activation of downstream signaling in breast cancer cell lines
-
heparin-binding EGF-like growth factor
-
activates
-
hepatocyte growth factor
-
-
-
hepatocyte growth factor-like protein
-
stimulates
-
heregulin
-
hydrogen peroxide
Insulin
-
macrophage stimulating protein
-
MSP, its only known ligand, both MSP-dependent and MSP-independent signaling by RON. RON exhibits MSP-independent tyrosine phosphorylation in MCF-10A cells. RON exhibits increased phosphorylation on Y1238/1239 and on the Y1360 docking site in the presence of exogenously added MSP. Similar levels of RON expression in NIH-3T3 cells do not lead to tyrosine phosphorylation of RON in the absence of ligand. MSP-independent tyrosine phosphorylation of RON also in HeLa cells
-
metformin
-
i.e. N,N-dimethylbiguanide or N,N-dimethylimidodicarbonimidic diamide, activates the insulin receptor tyrosine kinase by phosphorylation at Tyr1150 and Tyr1151, and indirectly via inhibition of protein tyrosine phosphatase 1B, metformin does not alter the order of substrate phosphorylation by the insulin receptor tyrosine kinase
nerve growth factor
-
activates TrkA, which leads to differentiation of neurons and neurobalstoma cells, whereas it induces proliferation of fibroblasts and apoptosis of medulloblastoma cells
-
neuregulins
-
activates
-
neurotrophin 3
-
activates TrkC
-
neurotrophin 4
-
activates TrkB
-
neurotrophin-3
-
activates
-
PMA/ionomycin
-
chronic lymphocytic leukemia cells and no