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Information on EC 2.7.10.1 - receptor protein-tyrosine kinase and Organism(s) Homo sapiens and UniProt Accession P00533

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IUBMB Comments
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 . In the human genome, 58 receptor-type protein-tyrosine kinases have been identified and these are distributed into 20 subfamilies.
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Select one or more organisms in this record:
This record set is specific for:
Homo sapiens
UNIPROT: P00533
Word Map
The taxonomic range for the selected organisms is: Homo sapiens
The enzyme appears in selected viruses and cellular organisms
Synonyms
tyrosine kinase, epidermal growth factor receptor, insulin receptor, c-kit, erlotinib, c-met, egf receptor, erbb2, her-2, receptor tyrosine kinase, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
A-type platelet-derived growth factor receptor
265516
-
Adhesion-related kinase
-
-
-
-
ALK
247
-
ALK tyrosine kinase receptor
265731
-
alpha platelet-derived growth factor receptor
265516
-
Anaplastic lymphoma kinase
angiopoietin 1 receptor
265630
-
AXL oncogene
-
-
-
-
basic-FGF receptor
265496
-
BDNF/NT-3 growth factors receptor
265665
-
beta platelet-derived growth factor receptor
265489
-
Brain-specific kinase
-
-
-
-
Breathless protein
-
-
-
-
Brt
247
-
c-erbB3
-
-
-
-
c-fgr
-
-
-
-
c-fms
c-kit
c-Kit receptor protein-tyrosine kinase
265493
-
c-Kit receptor tyrosine kinase
247
-
c-Kit RTK
247
-
c-Kit tyrosine kinase
-
-
-
-
c-kitR tyrosine kinase
265493
-
C-mer
c-met
c-Met receptor tyrosine kinase
c-Met RTK
247
-
C-ret
-
-
-
-
C-SRC
247
-
C14
-
-
-
-
Cadherin 96Ca
-
-
-
-
CD115 antigen
-
-
-
-
CD117
247
-
CD117 antigen
-
-
-
-
CD135 antigen
-
-
-
-
CD136 antigen
-
-
-
-
CD140a antigen
-
-
-
-
CD140b antigen
-
-
-
-
CD167a antigen
-
-
-
-
CD202b antigen
-
-
-
-
CD220 antigen
-
-
-
-
CD221 antigen
-
-
-
-
CD246 antigen
-
-
-
-
CDW136
-
-
-
-
CEK4
-
-
-
-
Cell adhesion kinase
-
-
-
-
cKit
247
-
CLD1
247
-
CLD2
247
-
colony-stimulating factor-1 receptor
247
-
CSF-1 receptor
247
also known as c-fms and CD115
CSF-1R
247
-
DDR1
265656
-
Derailed protein
-
-
-
-
DFGF-R1
-
-
-
-
discoidin domain receptor 1
265656
-
discoidin domain receptor 2
265666
-
discoidin domain receptor tyrosine kinase 1
265656
-
Discoidin receptor tyrosine kinase
Doughnut protein
-
-
-
-
Dror
-
-
-
-
Drosophila relative of ERBB
-
-
-
-
DRT
-
-
-
-
DTK
247
-
DTK receptor tyrosine kinase
265646
-
EBK
-
-
-
-
EGF receptor
247
-
EGF receptor protein-tyrosine kinase
247
-
EGF receptor tyrosine kinase
EGF RTK
247
-
EGF TK
247
-
EGF-R
247
-
EGFR kinase
247
-
EGFR protein tyrosine kinase
247
-
EGFr TK
-
-
-
-
EGFR tyrosine kinase
EGFR-TK
247
-
Egg laying defective protein 15
-
-
-
-
ELK
-
-
-
-
Embryonic brain kinase
-
-
-
-
embryonic receptor kinase
265571
-
EmRK2
265571
-
Endothelial kinase receptor EK1
-
-
-
-
Eph receptor tyrosine kinase
265615
-
EPH-and ELK-related kinase
-
-
-
-
EphA1
EphA1 receptor
247
-
EPHA1 receptor tyrosine kinase
265527
-
EphA2
EPHA4
265615
-
EphB3
265606
-
ephrin type-A receptor 1
265527
-
ephrin type-A receptor 2
265549
-
ephrin type-A receptor 3
265552
-
ephrin type-A receptor 4
265615
-
ephrin type-A receptor 5
265609
-
ephrin type-A receptor 7
265663
-
ephrin type-A receptor 8
265553
-
ephrin type-B receptor 1
265614
-
ephrin type-B receptor 2
265554
-
ephrin type-B receptor 3
265606
-
ephrin type-B receptor 4
265612
-
ephrine receptor
247
-
epidermal growth factor receptor
epidermal growth factor receptor 2
247
-
epidermal growth factor receptor 4
265662
-
epidermal growth factor receptor kinase
247
-
epidermal growth factor receptor tyrosine kinase
epidermal growth factor receptor tyrosine kinase inhibitor
247
-
Epidermal growth factor receptor-related protein
-
-
-
-
epidermal growth factor type II receptor
247
-
epidermal growth factor-receptor
247
-
epidermal growth-factor receptor tyrosine kinase
247
-
Epithelial cell kinase
epithelial discoidin domain receptor 1
265656
-
erb-B1
265729
-
ErbB receptor protein-tyrosine kinase
247
-
erbB tyrosine kinase
-
-
-
-
ErbB-1
265729
-
ErbB-2
265467
-
ErbB-4 receptor
265662
-
ErbB-4 tyrosine kinase
247
-
ERBB1
ErbB1 tyrosine kinase
247
-
ErbB2 kinase
-
-
-
-
erbB2 receptor tyrosine kinase
ErbB2 tyrosine kinase
247
-
ErbB4 receptor
247
-
ERK
-
-
-
-
erlotinib
247
-
erythropoietin-producing hepatocellular receptor tyrosine kinase subtype A2
247
-
erythropoietin-producing human hepatocellular carcinoma B3
265606
-
ETK
-
-
-
-
FGF receptor
265496
-
FGF receptor tyrosine kinase
247
-
FGFR-4
265533
-
FGFR1K
265496
-
FGFR2
FGFR3
FGFR4
247
-
fibroblast growth factor receptor
247
-
fibroblast growth factor receptor 1
265496
-
fibroblast growth factor receptor 4
265533
-
fibroblast growth factor receptor BFR-2
265528
-
Flk-1
247
-
Flt-1
247
-
FLT3 receptor protein
247
-
FLT4
265568
-
FLT4 receptor tyrosine kinase
265568
-
Fms proto-oncogene
-
-
-
-
fms-like tyrosine kinase 3
247
-
GCTK
-
-
-
-
GHR
247
-
GP145-TrkB
-
-
-
-
GP145-TrkB/GP95-TrkB
-
-
-
-
GP145-TrkC
-
-
-
-
growth hormone receptor
247
-
Gurken receptor
-
-
-
-
Heartless protein
-
-
-
-
HEK 2
265606
-
HEK3
-
-
-
-
HEK4
-
-
-
-
HEK6
-
-
-
-
Heparin-binding growth factor receptor
-
-
-
-
hepatocyte growth factor receptor
HER receptor protein-tyrosine kinase
247
-
HER-1
265729
-
Her-2
265467
-
Her1 tyrosine kinase
247
-
HER2neu
247
-
HER3
265531
-
HER3/ERRB3
265531
-
HER4
247
-
HGF receptor
-
-
-
-
HGF-SF receptor
-
-
-
-
high affinity nerve growth factor receptor
265714
-
HTK
265612
-
human epidermal growth factor receptor2
247
-
hydroxyaryl-protein kinase
-
-
-
-
HYK
-
-
-
-
IGF-1 receptor
247
-
IGF-1R
IGF-IR
247
-
IGFR tyrosine kinase
247
-
ILP receptor
-
-
-
-
insulin receptor
insulin receptor kinase
247
-
insulin receptor protein tyrosine kinase
247
-
insulin receptor protein-tyrosine kinase
-
-
-
-
insulin receptor tyrosine kinase
247
-
insulin receptor-beta subunit
247
-
insulin receptor-related protein
265508
-
insulin-growth factor-1 receptor
247
-
insulin-like growth factor 1 receptor
265479
-
insulin-like growth factor I receptor
265479
-
insulin-like growth factor receptor
247
-
insulin-like growth factor type I receptor
247
-
Insulin-like growth factor-1 receptor
247
-
Insulin-like Growth Factor-1 receptor tyrosine kinase
247
-
IR kinase
247
-
iR-beta subunit
247
-
IR-PTK
247
-
IR-related receptor
-
-
-
-
KDR/fetal liver kinase-1
247
-
KDR/Flk-1
247
-
Keratinocyte growth factor receptor
KGF receptor
247
-
KGFR
247
-
Kinase insert domain receptor
-
-
-
-
Kinase NYK
-
-
-
-
Kinase VIK
-
-
-
-
Kit protein-tyrosine kinase
247
-
KIT receptor tyrosine kinase
247
-
leukocyte tyrosine kinase receptor
265555
-
Linotte protein
-
-
-
-
M-CSF receptor
247
-
macrophage colony stimulating factor I receptor
265476
-
macrophage colony-stimulating factor receptor
247
-
macrophage stimulating 1 receptor
247
-
macrophage stimulating 1-receptor
247
-
macrophage-colony stimulating factor receptor
247
-
macrophage-stimulating protein receptor
265642
-
mast/stem cell growth factor receptor
265493
-
MEK4
-
-
-
-
Met proto-oncogene tyrosine kinase
-
-
-
-
Met receptor-tyrosine kinase
247
-
Met RTK
247
-
Met-related kinase
-
-
-
-
Met/hepatocyte growth factor receptor tyrosine kinase
265481
-
MFR
-
-
-
-
MIR
-
-
-
-
MLN 19
-
-
-
-
mROR1
-
-
-
-
mROR2
-
-
-
-
MSP receptor
-
-
-
-
muscle-specific receptor tyrosine kinase
247
-
muscle-specific receptor-tyrosine kinase
247
-
nerve growth factor receptor
247
-
NEU proto-oncogene
-
-
-
-
neuregulin receptor ErbB-4
265662
-
Neurospecific receptor tyrosine kinase
-
-
-
-
neurotrophin tyrosine receptor kinase
247
-
non-receptor protein tyrosine kinase
247
-
NRTK
-
-
-
-
NT-3 growth factor receptor
265664
-
NUK
-
-
-
-
orphan receptor tyrosine kinase
247
-
P140 TEK
-
-
-
-
p140-TrkA
-
-
-
-
p145c-kit
265493
-
p180erbB4
-
-
-
-
p185-Ron
-
-
-
-
p185erbB2
-
-
-
-
p190MET kinase
265481
-
p75 neurotrophin receptor
247
-
p75NTR
247
-
Pagliaccio
-
-
-
-
PDGF beta-receptor
265489
-
PDGF receptor
247
-
PDGF receptor tyrosine kinase
247
-
PDGF-alpha receptor
247
-
PDGF-beta receptor
247
-
PDGF-R-alpha
-
-
-
-
PDGF-R-beta
-
-
-
-
PDGFR
247
-
PDGFR kinase
-
-
-
-
PDGFR-alpha
PDGFR-beta
PDGFRalpha
247
-
PDGFRB
265489
-
PDGFRbeta
platelet derived growth factor receptor-beta
265489
-
platelet-derived growth factor receptor
247
-
platelet-derived growth factor receptor alpha
platelet-derived growth factor receptor-beta
247
-
proline-rich tyrosinekinase
247
-
protein kinase eck
265549
-
protein receptor tyrosine kinase RTK 6
265656
-
Protein-tyrosine kinase byk
-
-
-
-
Protein-tyrosine kinase receptor MPK-11
-
-
-
-
Proto-oncogene tyrosine-protein kinase Kit
-
-
-
-
proto-oncogene tyrosine-protein kinase MER
265660
-
proto-oncogene tyrosine-protein kinase receptor ret
265715
-
proto-oncogene tyrosine-protein kinase ROS
265484
-
Pyk-2
247
-
recepteur d'origine nantais
recepteur d'origine nantais receptor tyrosine kinase
247
-
Recepteur d’Origine Nantais
265642
-
receptor for macrophage colony-stimulating factor
247
-
receptor for stem cell factor
247
-
receptor protein tyrosine kinase
247
-
receptor protein tyrosine kinase RTK
265666
-
receptor protein-tyrosine kinase erbB-2
265467
-
receptor protein-tyrosine kinase erbB-3
265531
-
receptor protein-tyrosine kinase erbB-4
265662
-
Receptor protein-tyrosine kinase HEK11
-
-
-
-
Receptor protein-tyrosine kinase HEK5
-
-
-
-
Receptor protein-tyrosine kinase HEK7
-
-
-
-
Receptor protein-tyrosine kinase HEK8
-
-
-
-
Receptor protein-tyrosine kinase TKT
-
-
-
-
receptor tyrosine kinase
receptor tyrosine kinase c-Kit
247
-
receptor tyrosine kinase EphA1
247
-
receptor tyrosine kinase EphA2
265549
-
Receptor tyrosine kinase MerTK
-
-
-
-
receptor tyrosine kinase RET
247
-
receptor tyrosine kinase RON
247
-
receptor tyrosine kinase ROR1
265628
-
receptor tyrosine kinase Ror2
265629
-
receptor tyrosine kinase Sky
265646
-
receptor tyrosine kinase vascular endothelial growth factor receptor-2
247
-
Receptor-activated Janus kinase
-
-
-
-
receptor-like protein-tyrosine kinase TK14
265528
-
receptor-type tyrosine kinase termed Rse
265646
-
receptor-type tyrosine-protein kinase FLT3
265573
-
Ret receptor tyrosine kinase
247
-
Ret51
247
-
Ret9
247
-
RON receptor tyrosine kinase
Ron tyrosine kinase receptor
265642
-
RPTK
247
-
Rse
247
-
RTKs
247
-
SCFR
-
-
-
-
sFlt-1
247
-
Sky
247
-
Slow nerve growth factor receptor
-
-
-
-
soluble fms-like tyrosine kinase 1
247
-
Srcasm
265573
-
stem cell factor receptor
247
-
stem cell receptor
247
-
stem cell tyrosine kinase 1
265573
-
Stem cell-derived tyrosine kinase
STK
247
-
STK-1
265573
-
subclass III receptor tyrosine kinase
247
-
TAM receptor
247
-
Tif
247
-
Torpedo protein
-
-
-
-
TRK1 transforming tyrosine kinase protein
-
-
-
-
TrkB tyrosine kinase
-
-
-
-
TrkC tyrosine kinase
-
-
-
-
Tunica interna endothelial cell kinase
-
-
-
-
Tyro 3
247
-
TYRO3
265646
-
Tyrosine kinase CEK6 receptor
-
-
-
-
Tyrosine kinase DDR
-
-
-
-
tyrosine kinase p59fyn
265573
-
Tyrosine kinase receptor HD-14
-
-
-
-
tyrosine kinase receptor RON
247
-
tyrosine kinase receptor trkE
265656
-
Tyrosine kinase-type cell surface receptor HER2
-
-
-
-
Tyrosine kinase-type cell surface receptor HER3
-
-
-
-
Tyrosine kinase-type cell surface receptor HER4
-
-
-
-
Tyrosine-protein kinase CAK
-
-
-
-
Tyrosine-protein kinase CEK9
-
-
-
-
Tyrosine-protein kinase DTK
-
-
-
-
Tyrosine-protein kinase FLT3
-
-
-
-
Tyrosine-protein kinase FRT
-
-
-
-
Tyrosine-protein kinase receptor CEK10
-
-
-
-
Tyrosine-protein kinase receptor CEK11
-
-
-
-
Tyrosine-protein kinase receptor CEK5
-
-
-
-
Tyrosine-protein kinase receptor CEK7
-
-
-
-
Tyrosine-protein kinase receptor CEK8
-
-
-
-
Tyrosine-protein kinase receptor CEPHA7
-
-
-
-
Tyrosine-protein kinase receptor ECK
-
-
-
-
Tyrosine-protein kinase receptor EEK
-
-
-
-
Tyrosine-protein kinase receptor EPH
-
-
-
-
Tyrosine-protein kinase receptor ESK
-
-
-
-
Tyrosine-protein kinase receptor ETK1
-
-
-
-
Tyrosine-protein kinase receptor FLT
-
-
-
-
Tyrosine-protein kinase receptor FLT3
-
-
-
-
Tyrosine-protein kinase receptor FLT4
-
-
-
-
Tyrosine-protein kinase receptor HTK
-
-
-
-
Tyrosine-protein kinase receptor PAG
-
-
-
-
Tyrosine-protein kinase receptor QEK5
-
-
-
-
Tyrosine-protein kinase receptor REK4
-
-
-
-
Tyrosine-protein kinase receptor SEK
-
-
-
-
Tyrosine-protein kinase receptor TCK
-
-
-
-
Tyrosine-protein kinase receptor TEK
-
-
-
-
tyrosine-protein kinase receptor Tie-1
265566
-
tyrosine-protein kinase receptor TYRO3
265646
-
tyrosine-protein kinase receptor UFO
265557
-
Tyrosine-protein kinase receptor XEK
-
-
-
-
Tyrosine-protein kinase receptor XELK
-
-
-
-
Tyrosine-protein kinase receptor ZEK1
-
-
-
-
Tyrosine-protein kinase receptor ZEK2
-
-
-
-
Tyrosine-protein kinase receptor ZEK3
-
-
-
-
Tyrosine-protein kinase RSE
-
-
-
-
tyrosine-protein kinase RYK
265564
-
Tyrosine-protein kinase SKY
-
-
-
-
tyrosine-protein kinase transmembrane receptor ROR1
265628
-
tyrosine-protein kinase transmembrane receptor ROR2
265629
-
vascular endothelial growth factor
247
-
vascular endothelial growth factor 2
247
-
vascular endothelial growth factor receptor
vascular endothelial growth factor receptor 1
265713
-
vascular endothelial growth factor receptor 2
vascular endothelial growth factor receptor 3
265568
-
vascular endothelial growth factor receptor tyrosine kinase
247
-
vascular endothelial growth factor receptor-1
265571
-
vascular endothelial growth-factor receptor-1 tyrosine kinase
247
-
Vascular permeability factor receptor
-
-
-
-
VDR
247
-
VEGF factor receptor tyrosine kinase
247
-
VEGF receptor
265571
-
VEGF receptor tyrosine kinase
247
-
VEGF receptor-1
265571
-
VEGFR
247
-
VEGFR tyrosine kinase
247
-
VEGFR-1
247
-
VEGFR-1 tyrosine kinase
247
-
VEGFR-2
VEGFR-2 tyrosine kinase
265571
-
VEGFR-3
247
-
VEGFR1
VEGFR1-3
247
-
VEGFR2
VEGFR2/kinase domain region
247
-
VEGFR3
247
isoform
vitamin D receptor
247
-
additional information
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.
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 + NAEYLRV
ADP + NAE-phospho-Y-LRV
show the reaction diagram
-
-
-
-
?
ATP + VPEYINQ
ADP + VPE-phosphoY-INQ
show the reaction diagram
-
-
-
-
?
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 + 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 + poly-Ala-Glu-Lys-Tyr
ADP * poly-Ala-L-Glu-L-Lys-L-tyrosine phosphate
show the reaction diagram
-
substrate used for c-Met
-
-
?
ATP + poly-Glu-Tyr
ADP + poly-L-Glu-L-tyrosine phosphate
show the reaction diagram
-
substrate used for EGFR
-
-
?
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 + [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
-
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 SUBSTRATE
NATURAL 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 + 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
-
-
?
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
Ca2+
ligand-binding induced dimerization enables transautophosphorylation of ErbB1 which results in enhanced intracellular cytoplasmic Ca2+ concentration activating calmodulin which reverses autoinhibition by net charge changes in the juxtamembranes
Mg2+
-
required
Ca2+
-
L-type Ca2+ channel activity is induced by enzyme activity regulating the Ca2+ flux and intracellular Ca2+ concentration, capacitative Ca2+ entry measurements using a fluorescent method
Cr3+
-
activates insulin receptor tyrosine phosphorylation in vivo
hydrogen peroxide
-
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
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1-(4-aminophenyl)-3-[3-(1,3-benzodioxol-5-yl)-4-oxo-2,4-dihydroindeno[1,2-c]pyrazol-5-yl]urea
-
61% inhibition of EGFR
1-(4-aminophenyl)-3-[3-(3,4-dihydroxyphenyl)-4-oxo-2,4-dihydroindeno[1,2-c]pyrazol-5-yl]urea
-
50% inhibition of EGFR
1-(4-aminophenyl)-3-[3-(4-hydroxyphenyl)-4-oxo-2,4-dihydroindeno[1,2-c]pyrazol-5-yl]urea
-
65% inhibition of EGFR
1-(4-aminophenyl)-3-[3-(4-methoxyphenyl)-4-oxo-2,4-dihydroindeno[1,2-c]pyrazol-5-yl]urea
-
3% inhibition of EGFR
1-(4-hydroxyphenyl)-3-[3-(4-methoxyphenyl)-4-oxo-2,4-dihydroindeno[1,2-c]pyrazol-5-yl]urea
-
7% inhibition of EGFR
1-[3-(1,3-benzodioxol-5-yl)-4-oxo-2,4-dihydroindeno[1,2-c]pyrazol-5-yl]-3-(4-hydroxyphenyl)urea
-
4% inhibition of EGFR
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
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
-
-
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-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]-6-(methylamino)pyrimidine-5-carbaldehyde O-methyloxime
-
48% inhibition of EGFR at 0.002 mM
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-[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
-
30% inhibition of EGFR
AG1478
-
specific tyrosine kinase inhibitor of EGFR, whifh decreases EGFR phosphorylation through the inhibition of EGFR/HER3 dimerization
erlotinib
-
-
herceptin
-
combined therapy with herceptin and iressa exerts a greater suppression in EGFR activation
-
Iressa
-
gefitinib, specific tyrosine kinase inhibitor of EGFR, does not abolish basal HER2 phosphorylation, but decreases EGFR and HER3 phosphorylation through the inhibition of EGFR/HER3 dimerization. Combined therapy with herceptin and iressa exerts a greater suppression in EGFR activation
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
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
Tarceva
-
81% inhibition of EGFR
(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)-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-[[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-(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
-
-
(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)-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-[[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
-
(2S)-N,N-dimethyl-2-[(4-[[1-(1,3-thiazol-4-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
-
(2S)-N,N-dimethyl-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
-
(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
-
-
(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
-
-
-
(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-diamino-2,3-dicyano-1,4-bis(2-aminophenylthio)-butadiene
-
-
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
-
88% inhibition of KDR
1-(4-aminophenyl)-3-[3-(3,4-dihydroxyphenyl)-4-oxo-2,4-dihydroindeno[1,2-c]pyrazol-5-yl]urea
-
58% inhibition of KDR
1-(4-aminophenyl)-3-[3-(4-hydroxyphenyl)-4-oxo-2,4-dihydroindeno[1,2-c]pyrazol-5-yl]urea
-
73% inhibition of KDR
1-(4-aminophenyl)-3-[3-(4-methoxyphenyl)-4-oxo-2,4-dihydroindeno[1,2-c]pyrazol-5-yl]urea
-
42% inhibition of KDR
1-(4-hydroxyphenyl)-3-[3-(4-methoxyphenyl)-4-oxo-2,4-dihydroindeno[1,2-c]pyrazol-5-yl]urea
-
44% inhibition of KDR
1-[3-(1,3-benzodioxol-5-yl)-4-oxo-2,4-dihydroindeno[1,2-c]pyrazol-5-yl]-3-(4-hydroxyphenyl)urea
-
70% inhibition of KDR
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-[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-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
-
39% inhibition of ErbB-2 at 0.01 mM
5,7-dihydroxyisoflavone derivatives
-
diverse derivatives, analysis of inhibitory effect on EGFR tyrosine kinase activity, overview
-
5-(2-morpholin-4-yl-2-oxoethoxy)-N-[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
-
-
5-(4-(dihydroxyboranyl)benzylamino)-2-hydroxybenzoic acid
-
inhibition of EGFR tyrosine kinase
-
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
-
-
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
-
95% inhibition of KDR
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,N-dimethyl-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]acetamide
-
-
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-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-[1-(3-fluorobenzyl)-1H-indazol-5-yl]-5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine
-
-
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
-
-
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
nakijiquinone C
-
IC50 of 0.125 mg/ml for EGFR, IC50 of 0.103 mg/ml for HER2
neratinib
-
-
NVP-BBT594
-
-
NVP-BEZ235
-
-
NVP-BGJ398
-
-
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
PD-173074
-
-
PD153035
-
specific inhibition of EGFR-TK, IC50 is 0.00329 mM with 1 U of purified EGFR-TK from A431 cells
PD168393
PD184352
-
-
PD325901
-
-
PD98059
-
-
PF-2341066
-
IC50: 0.002 mM
PHA-665752
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
-
PIK-90
-
-
PI_103
-
-
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
regorafenib
-
-
siRNA
-
sorafenib
Spry protein
-
-
-
staurosporine
-
-
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
-
38% inhibition of KDR
tert-butyl 2-([[4-(3-bromoanilino)-6-methoxyquinazolin-7-yl]oxy]methyl)morpholine-4-carboxylate
-
-
tert-butyl 2-([[4-(3-chloroanilino)-6-methoxyquinazolin-7-yl]oxy]methyl)morpholine-4-carboxylate
-
-
tert-butyl 2-([[4-(4-bromoanilino)-6-methoxyquinazolin-7-yl]oxy]methyl)morpholine-4-carboxylate
-
-
trastuzumab
-
-
-
trichostatin A
-
the ability of RON to inhibit HIV-1 transcription is sensitive to a histone deacetylase inhibitor
tyrphostin
-
-
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%
varlitinib
-
-
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
ZSTK474
-
-
[7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-yl](1H-indazol-3-yl)methanone
-
-
-
additional information
-