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

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Homo sapiens
UNIPROT: P04626


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
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-
-
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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
physiological function
hepatocyte growth factor expression leads to autocrine activation of its receptor tyrosine kinase, MET, in nearly half of the acute myeloid leukemia cell lines and clinical samples studied. Genetic depletion of hepatocyte growth factor or MET potently inhibits the growth and survival of hepatocyte growth factor-expressing acute myeloid leukemia cells. Leukemic cells treated with the specific MET kinase inhibitor crizotinib develop resistance due to compensatory upregulation of hepatocyte growth factor expression, leading to restoration of MET signaling. In cases of acute myeloid leukemia where MET is coactivated with other tyrosine kinases, such as fibroblast growth factor receptor 1, concomitant inhibition of FGFR1 and MET blocks compensatory hepatocyte growth factor upregulation, resulting in sustained logarithmic cell kill both in vitro and in xenograft models in vivo
metabolism
Eph receptor tyrosine kinases are activated upon ephrin binding via a sequential and ordered autophosphorylation process where residue YJM2 is phosphorylated first, followed by YJM1, and, finally by Yact. The Eph kinase activity most closely correlates with the phosphorylation status of the juxtamembrane region and not that of the activation loop. Eph kinase activity is primarily correlated with phosphorylation of residue YJM2 and not of the adjacent YJM1
physiological function
Notch1 protein is an interacting partner of receptor tyrosine kinase DDR1. Upon ligand-mediated DDR1 kinase activation, Notch1 is activated, binds to DDR1, and activates canonical Notch1 targets, including Hes1 and Hey2. DDR1 ligand collagen I treatment significantly increases the active form of Notch1 receptor in the nuclear fraction, whereas DDR1 knockdown cells show little or no increase of the active form of Notch1 in the nuclear fraction. DDR1 activation suppresses genotoxic-mediated cell death. The DDR1 knockdown cancer cells show the reduced transformed phenotypes in vitro and in vivo xenograft studies
metabolism
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phosphorylation of the protein chaperone small glutamine-rich tetratricopeptide repeat-containing protein alpha at Ser305 is essential for isoform platelet-derived growth factor receptor PDGFRalpha stabilization and cell survival in PDGFRalpha-dependent cancer cells
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 [macrophage-stimulating protein]-L-tyrosine
ADP + a [macrophage-stimulating protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
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 + NAEYLRV
ADP + NAE-phospho-Y-LRV
show the reaction diagram
-
-
-
-
?
ATP + phosphatidylinositol 3-kinase
ADP + phosphorylated phosphatidylinositol 3-kinase
show the reaction diagram
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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
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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 + poly-Ala-Glu-Lys-Tyr
ADP * poly-Ala-L-Glu-L-Lys-L-tyrosine phosphate
show the reaction diagram
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substrate used for c-Met
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-
?
ATP + poly-Glu-Tyr
ADP + poly-L-Glu-L-tyrosine phosphate
show the reaction diagram
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substrate used for EGFR
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-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
show the reaction diagram
ATP + VPEYINQ
ADP + VPE-phosphoY-INQ
show the reaction diagram
-
-
-
-
?
ATP + YFEW
ADP + YpFEW
show the reaction diagram
tetrapeptide identified by substrate profiling
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-
?
ATP + [beta-catenin]-Tyr142
ADP + [beta-catenin]-Tyr142 phosphate
show the reaction diagram
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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
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-
?
ATP + [endothelial growth-factor]-L-tyrosine
ADP + [endothelial growth-factor]-L-tyrosine phosphate
show the reaction diagram
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EGFR tyrosine kinase
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-
?
ATP + [gastrin]-L-tyrosine
ADP + [gastrin]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [minigastrin]-L-tyrosine
ADP + [minigastrin]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [poly-(Glu,Tyr)1:4]
ADP + [poly-(Glu,Tyr)1:4]-tyrosine phosphate
show the reaction diagram
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synthetic substrate
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-
?
ATP + [vascular endothelial growth-factor-1]-L-tyrosine
ADP + [vascular endothelial growth-factor-1]-L-tyrosine phosphate
show the reaction diagram
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VEGFR-1 tyrosine kinase
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-
?
poly(Glu:Tyr) + ATP
ADP + poly(Glu:Tyr) phosphate
show the reaction diagram
-
-
-
-
?
additional information
?
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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 [macrophage-stimulating protein]-L-tyrosine
ADP + a [macrophage-stimulating protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
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
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-
?
ATP + phospholipase C gamma
ADP + phosphorylated phospholipase C gamma
show the reaction diagram
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growth factor-induced tyrosine phosphorylation of PLC gamma is essential for stimulation of phosphatidylinositol hydrolysis in vitro and in vivo
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ATP + poly(Glu:Tyr)
ADP + poly(Glu:Tyr) phosphate
show the reaction diagram
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-
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
show the reaction diagram
P29320
autophosphorylated on tyrosine and also mediated tyrosine phosphorylation of casein
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-
?
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
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EGFR tyrosine kinase
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-
?
ATP + [vascular endothelial growth-factor-1]-L-tyrosine
ADP + [vascular endothelial growth-factor-1]-L-tyrosine phosphate
show the reaction diagram
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VEGFR-1 tyrosine kinase
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-
?
additional information
?
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COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Cr3+
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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+
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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
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(2R)-2-[(4-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]-N,N-dimethylpropanamide
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(2R)-2-[(4-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]-N-methylpropanamide
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(2R)-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
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(2R)-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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(2R)-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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(2R)-N,N-dimethyl-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
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(2R)-N,N-dimethyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
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(2R)-N-methyl-2-[(4-[[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
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(2R)-N-methyl-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
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(2S)-2-[(4-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]-N,N-dimethylpropanamide
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(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
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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
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4-amino-6-([3-chloro-4-[(3-fluorobenzyl)oxy]phenyl]amino)pyrimidine-5-carbaldehyde O-methyloxime
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4-amino-6-[(1-benzyl-1H-indazol-5-yl)amino]pyrimidine-5-carbaldehyde O-methyloxime
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4-amino-6-[(3-bromophenyl)amino]pyrimidine-5-carbaldehyde O-methyloxime
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4-amino-6-[(3-chloro-4-fluorobenzyl)amino]pyrimidine-5-carbaldehyde O-methyloxime
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4-amino-6-[(3-chloro-4-fluorophenyl)amino]pyrimidine-5-carbaldehyde O-methyloxime
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4-amino-6-[[1-(3-chlorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
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4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(1-methylethyl)oxime
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4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(2-methoxybenzyl)oxime
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4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(2-methoxyethyl)oxime
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4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(2-methylpropyl)oxime
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4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-benzyloxime
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4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-ethyloxime
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4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
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4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde oxime
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4-amino-6-[[1-(3-fluorobenzyl)-1H-indol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
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4-amino-6-[[1-(3-fluorobenzyl)-2,3-dihydro-1H-indol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
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4-amino-6-[[1-(3-methoxybenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
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4-amino-6-[[1-(4-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
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4-amino-6-[[2-(3-fluorobenzyl)-1H-benzimidazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
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4-amino-6-[[4-(benzyloxy)-3-chlorophenyl]amino]pyrimidine-5-carbaldehyde O-methyloxime
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4-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]-6-(methylamino)pyrimidine-5-carbaldehyde O-methyloxime
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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
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5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
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5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(1,3-thiazol-4-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
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5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
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5-[(1R)-1-methyl-2-oxo-2-pyrrolidin-1-ylethoxy]-N-[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
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5-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
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5-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
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-
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
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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
-
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(2R)-N-(2-methoxyethyl)-N-methyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
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-
(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
-
-
(3Z)-3-[(3,5-dimethyl-1H-pyrrol-2-yl)methylidene]-1,3-dihydro-2H-indol-2-one
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-
(3Z)-3-[3-([1,4'-bipiperidine]-1'-carbonyl)-2-methyl-1,4,5,6-tetrahydro-7H-indol-7-ylidene]-5-fluoro-1,3-dihydro-2H-indol-2-one
-
-
(3Z)-5-fluoro-3-(2-methyl-3-[(2S)-2-[(pyrrolidin-1-yl)methyl]pyrrolidine-1-carbonyl]-1,4,5,6-tetrahydro-7H-indol-7-ylidene)-1,3-dihydro-2H-indol-2-one
-
-
(3Z)-5-fluoro-3-[2-methyl-3-(morpholine-4-carbonyl)-1,4,5,6-tetrahydro-7H-indol-7-ylidene]-1,3-dihydro-2H-indol-2-one
-
-
(3Z)-5-[(1-ethylpiperidin-4-yl)amino]-3-[(5-methoxy-1H-benzimidazol-2-yl)(phenyl)methylidene]-1,3-dihydro-2H-indol-2-one
-
-
(7Z)-7-(5-bromo-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-N-[2-(diethylamino)ethyl]-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-7-(5-chloro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-N-[2-(diethylamino)ethyl]-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[2-(morpholin-4-yl)ethyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[2-(piperidin-1-yl)ethyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[2-(pyridin-2-yl)ethyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[2-(pyrrolidin-1-yl)ethyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[3-(pyrrolidin-1-yl)propyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-N-(2-hydroxyethyl)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
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(7Z)-N-[2-(diethylamino)ethyl]-2-methyl-7-(2-oxo-1,2-dihydro-3H-indol-3-ylidene)-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-N-[2-(diethylamino)ethyl]-2-methyl-7-(5-methyl-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-N-[2-(diethylamino)ethyl]-2-methyl-7-(5-nitro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-N-[2-(diethylamino)ethyl]-7-(4-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-N-[2-(diethylamino)ethyl]-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-N-[2-(diethylamino)ethyl]-7-(5-methoxy-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-N-[2-(diethylamino)ethyl]-7-(5-[[(diethylamino)oxy]sulfinyl]-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-N-[2-(diethylamino)ethyl]-7-(7-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-N-[2-(dimethylamino)ethyl]-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-N-[3-(diethylamino)-2-hydroxypropyl]-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-N-[3-(diethylamino)propyl]-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(E)-methyl 3-(4-(phenylamino)quinazolin-7-yl)acrylate
-
-
-
(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-(phenylamino)quinazolin-7-yl)ethanone
-
-
-
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-bromo-1-(4-(phenylamino)quinazolin-7-yl)ethanone
-
-
-
2-chloro-1-(4-(phenylamino)quinazolin-7-yl)ethanone
-
-
-
2-chloro-N-(4-((2-chloro-5-hydroxyphenyl)amino)-6-(prop-2-yn-1-yloxy)quinazolin-7-yl)acetamide
-
-
-
2-chloro-N-(4-((2-chloro-5-hydroxyphenyl)amino)quinazolin-7-yl)acetamide
-
-
-
2-chloro-N-(4-(phenylamino)quinazolin-7-yl)acetamide
-
-
-
2-fluoro-1-(4-(phenylamino)quinazolin-7-yl)ethanone
-
-
-
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-(2,4-dimethyl-5-[(Z)-[2-oxo-5-(2-phenylhydrazinecarbonyl)-1,2-dihydro-3H-indol-3-ylidene]methyl]-1H-pyrrol-3-yl)propanoic acid
-
-
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-[2,4-dimethyl-5-[(Z)-(2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid
-
-
3-[2-[(Z)-(5-bromo-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-4,5,6,7-tetrahydro-1H-indol-3-yl]propanoic acid
-
-
3-[4-methyl-2-[(Z)-(2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid
-
-
3-[[5-([6-amino-5-[(E)-(methoxyimino)methyl]pyrimidin-4-yl]amino)-1H-indazol-1-yl]methyl]benzonitrile
-
-
4-(1H-indazol-3-yloxy)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidine
-
-
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
-
5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-N-[(2S)-2-hydroxy-3-(morpholin-4-yl)propyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide
-
-
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-methoxy-7-[(morpholin-2-yl)methoxy]-N-(4-propylphenyl)quinazolin-4-amine
-
-
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
-
7,7-dimethyl-2-(1H-pyrazol-4-yl)-N-(4,5,6,7-tetrahydro-1H-indazol-3-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
7,7-dimethyl-2-(1H-pyrazol-4-yl)-N-[6-(trifluoromethyl)-1H-indazol-3-yl]-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
7,7-dimethyl-2-(1H-pyrazol-4-yl)-N-[7-(trifluoromethyl)-1H-indazol-3-yl]-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
7,7-dimethyl-N-(1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
7,7-dimethyl-N-(5-methyl-1H-pyrazol-3-yl)-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
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
afatinib
-
-
-
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
-
axitinib
-
-
-
AZD2171
-
inhibits VEGFR2
AZD4547
-
-
-
BI2536
-
-
cabozantinib
-
-
-
canertinib
-
-
-
CEP-7055
-
inhibits VEGFR1-3
CEP701
-
inhibits FLT3
cetuximab
-
-
-
cisplatin
-
anti-cancer drug inhibiting receptor tyrosine kinases
crizotinib
-
-
-
cycloheximide
-
depletes the synthetic pool of Met receptor
dacomitinib
-
-
-
dasatinib
-
-
doxorubicin
dynamin K44A
-
reduces EGFR internalization to 40%
-
erlotinib
ethyl 4-(3-(2-aminoquinazolin-6-yl)-4-methyl-2-oxopyridin-1(2H)-yl)benzoate
-
-
foretinib
-
-
-
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
Genentech 5D5Fab
-
-
-
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
KU55933
-
-
lapatinib
-
lavendustin A
-
-
LCRF-0004
-
potent and selective inhibitor
-
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
LY2874455
-
-
-
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
methyl (3Z)-3-(3-[[2-(diethylamino)ethyl]carbamoyl]-2-methyl-1,4,5,6-tetrahydro-7H-indol-7-ylidene)-2-oxo-2,3-dihydro-1H-indole-5-carboxylate
-
-
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-(1,2-benzothiazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(1,3-benzothiazol-2-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(1H-indazol-3-yl)-7,7-dimethyl-2-(1,3-thiazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(1H-indazol-3-yl)-7,7-dimethyl-2-(1-methyl-1H-pyrazol-5-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(1H-indazol-3-yl)-7,7-dimethyl-2-(1H-1,2,3-triazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-3-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(1H-indazol-3-yl)-N,7,7-trimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(1H-indol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
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-(3,5-dichlorophenyl)-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
-
-
N-(3-bromophenyl)-6-methoxy-7-[(4-methylmorpholin-2-yl)methoxy]quinazolin-4-amine
-
-
N-(3-bromophenyl)-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
-
-
N-(3-chloro-4-methylphenyl)-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
-
-
N-(3-chlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
-
N-(3-chlorophenyl)-6-methoxy-7-[(4-methylmorpholin-2-yl)methoxy]quinazolin-4-amine
-
-
N-(3-chlorophenyl)-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
-
-
N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)-1-benzothiophen-7-yl]oxy]phenyl)-1,3-diphenyl-1H-pyrazole-4-carboxamide
-
-
N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)-1-benzothiophen-7-yl]oxy]phenyl)-1,5-diphenyl-1H-pyrazole-4-carboxamide
-
-
N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)-1-benzothiophen-7-yl]oxy]phenyl)-1,5-diphenyl-1H-pyrrole-3-carboxamide
-
-
N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)-1-benzothiophen-7-yl]oxy]phenyl)-2,4-diphenyl-1,3-thiazole-5-carboxamide
-
-
N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-1-phenyl-5-(pyridin-2-yl)-1H-pyrazole-4-carboxamide
-
-
N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-1-phenyl-5-(pyridin-3-yl)-1H-pyrazole-4-carboxamide
-
-
N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-1-phenyl-5-(pyridin-4-yl)-1H-pyrazole-4-carboxamide
-
-
N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-1-phenyl-5-(thiophen-3-yl)-1H-pyrazole-4-carboxamide
-
-
N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-5-(2-fluorophenyl)-1-phenyl-1H-pyrazole-4-carboxamide
-
-
N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-5-(2-methoxyphenyl)-1-phenyl-1H-pyrazole-4-carboxamide
-
-
N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-5-(3-methoxyphenyl)-1-phenyl-1H-pyrazole-4-carboxamide
-
-
N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-5-(4-fluorophenyl)-1-phenyl-1H-pyrazole-4-carboxamide
-
-
N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-5-(4-methoxyphenyl)-1-phenyl-1H-pyrazole-4-carboxamide
-
-
N-(4,5-dichloro-1H-pyrazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(4-(phenylamino)quinazolin-7-yl)acrylamide
-
-
-
N-(4-(phenylamino)quinazolin-7-yl)ethenesulfonamide
-
-
-
N-(4-bromo-2-chlorophenyl)-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
-
-
N-(4-bromo-2-fluorophenyl)-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
-
-
N-(4-bromo-3-methylphenyl)-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
-
-
N-(4-bromophenyl)-6-methoxy-7-[(4-methylmorpholin-2-yl)methoxy]quinazolin-4-amine
-
-
N-(4-bromophenyl)-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
-
-
N-(4-chloro-2-fluorophenyl)-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
-
-
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-fluoro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(4-fluoro-2-methylphenyl)-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
-
-
N-(4-fluorophenyl)-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
-
-
N-(4-hydroxy-5-[(2E)-3-methyl-5-[(1R,2S)-1,2,3-trimethylcyclohex-3-en-1-yl]pent-2-en-1-yl]-3,6-dioxocyclohexa-1,4-dien-1-yl)glycine
-
IC50 of more than 0.2 mg/ml for EGFR, IC50 of 0.079 mg/ml for HER3
N-(4-tert-butylphenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
-
N-(5,7-difluoro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(5-fluoro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(5-tert-butylisoxazol-3-yl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
-
N-(5-[(2E)-5-[(1R)-1,3-dimethyl-2-methylidenecyclohex-3-en-1-yl]-3-methylpent-2-en-1-yl]-4-hydroxy-3,6-dioxocyclohexa-1,4-dien-1-yl)-D-serine
-
IC50 of more than 0.2 mg/ml for EGFR, IC50 of 0.022 mg/ml for HER3
N-(5-[(2E)-5-[(1R)-1,3-dimethyl-2-methylidenecyclohex-3-en-1-yl]-3-methylpent-2-en-1-yl]-4-hydroxy-3,6-dioxocyclohexa-1,4-dien-1-yl)-D-threonine
-
IC50 of more than 0.2 mg/ml for EGFR, IC50 of 0.027 mg/ml for HER3
N-(5-[(2E)-5-[(1R,3R)-1,3-dimethyl-2-methylidenecyclohexyl]-3-methylpent-2-en-1-yl]-4-hydroxy-3,6-dioxocyclohexa-1,4-dien-1-yl)-D-serine
-
IC50 of more than 0.2 mg/ml for EGFR, IC50 of 0.018 mg/ml for HER3
N-(5-[(2E)-5-[(1R,3R)-1,3-dimethyl-2-methylidenecyclohexyl]-3-methylpent-2-en-1-yl]-4-hydroxy-3,6-dioxocyclohexa-1,4-dien-1-yl)-D-threonine
-
IC50 of more than 0.2 mg/ml for EGFR, IC50 of 0.19 mg/ml for HER3
N-(5-[(2E)-5-[(1R,3R)-1,3-dimethyl-2-methylidenecyclohexyl]-3-methylpent-2-en-1-yl]-4-hydroxy-3,6-dioxocyclohexa-1,4-dien-1-yl)glycine
-
IC50 of 0.197 mg/ml for EGFR, IC50 of 0.125 mg/ml for HER2
N-(6-chloro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(6-fluoro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(7-chloro-1H-indazol-3-yl)-2-[5-(difluoromethyl)-1H-pyrazol-4-yl]-7,7-dimethyl-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(7-chloro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(7-chloro-5-fluoro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(7-chloro-6-fluoro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(7-fluoro-1-methyl-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(7-fluoro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
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-[(3Z)-2-oxo-3-[(1H-pyrrol-2-yl)methylidene]-2,3-dihydro-1H-indol-6-yl]-N'-phenylurea
-
-
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
-
-
N-[4-chloro-3-(trifluoromethyl)phenyl]-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
-
-
N-[4-fluoro-3-(trifluoromethyl)phenyl]-6-methoxy-7-[(morpholin-2-yl)methoxy]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