Information on EC 2.7.10.1 - receptor protein-tyrosine kinase

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The enzyme appears in viruses and cellular organisms

EC NUMBER
COMMENTARY
2.7.10.1
-
RECOMMENDED NAME
GeneOntology No.
receptor protein-tyrosine kinase
REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT ACCESSION NO.
LITERATURE
ATP + a [protein]-L-tyrosine = ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
ATP + a [protein]-L-tyrosine = ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
reaction mechanism; regulation of enzyme activity involves the activation loop, a polypeptide region outside the active site cleft, which is reversibly phosphorylated
-
ATP + a [protein]-L-tyrosine = ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
active site structure, activation mechanism
-
REACTION TYPE
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
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.
SYNONYMS
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
A-type platelet-derived growth factor receptor
P16234
-
Adhesion-related kinase
-
-
-
-
Adhesion-related kinase
Q00993
-
ALK receptor tyrosine kinase
-
-
ALK tyrosine kinase receptor
Q9UM73
-
ALK tyrosine kinase receptor
P97793
-
alpha platelet-derived growth factor receptor
P16234
-
alpha platelet-derived growth factor receptor
P26618
-
alpha platelet-derived growth factor receptor
P20786
-
alpha platelet-derived growth factor receptor
P26619
-
Anaplastic lymphoma kinase
-
-
-
-
Anaplastic lymphoma kinase
-
-
Anaplastic lymphoma kinase
-
-
Anaplastic lymphoma kinase
-
-
angiopoietin 1 receptor
Q06807
-
angiopoietin 1 receptor
O73791
-
angiopoietin 1 receptor
Q02763
-
angiopoietin 1 receptor
Q02858
-
ark
Q00993
-
Axl
P30530
-
AXL oncogene
-
-
-
-
basic fibroblast growth factor receptor 1
P21804
-
basic fibroblast growth factor receptor 1
P16092
-
basic fibroblast growth factor receptor 1
Q04589
-
basic-FGF receptor
P11362
-
BDNF/NT-3 growth factors receptor
Q9v6k3
-
BDNF/NT-3 growth factors receptor
Q91987
-
BDNF/NT-3 growth factors receptor
Q16620
-
BDNF/NT-3 growth factors receptor
P15209
-
BDNF/NT-3 growth factors receptor
Q63604
-
BEK/FGFR-2 receptor
P21803
-
beta platelet-derived growth factor receptor
P09619
-
beta platelet-derived growth factor receptor
P05622
-
brain specific kinase
Q60629
-
Brain-specific kinase
-
-
-
-
Breathless protein
-
-
-
-
c-erbB3
-
-
-
-
c-fgr
-
-
-
-
c-fms
-
-
-
-
c-kit
-
-
-
-
c-kit
-
-
c-kit
P05532
-
c-kit receptor
-
-
c-Kit receptor protein-tyrosine kinase
P10721
-
c-Kit receptor tyrosine kinase
-
-
c-Kit receptor tyrosine kinase
-
-
c-Kit RTK
-
-
c-Kit tyrosine kinase
-
-
-
-
c-kitR tyrosine kinase
P10721
-
C-mer
-
-
-
-
C-mer
-
-
c-met
-
-
-
-
c-met
Q2IBA6
-
c-met
P97523
-
c-Met receptor tyrosine kinase
-
-
c-Met receptor tyrosine kinase
P08581
-
c-Met RTK
-
-
C-ret
-
-
-
-
C-SRC
-
-
C14
-
-
-
-
Cadherin 96Ca
-
-
-
-
Cak I receptor
Q03146
-
CD115 antigen
-
-
-
-
CD117
-
-
CD117 antigen
-
-
-
-
CD135 antigen
-
-
-
-
CD136 antigen
-
-
-
-
CD140a antigen
-
-
-
-
CD140b antigen
-
-
-
-
CD167a antigen
-
-
-
-
CD202b antigen
-
-
-
-
CD220 antigen
-
-
-
-
CD221 antigen
-
-
-
-
CD246 antigen
-
-
-
-
CDW136
-
-
-
-
CEK4
-
-
-
-
Cek5
P28693
-
Cell adhesion kinase
-
-
-
-
chicken embryo kinase 5
P28693
-
cKit
-
-
class II receptor tyrosine kinase
P42159
-
colony-stimulating factor-1 receptor
-
-
CSF-1 receptor
-
also known as c-fms and CD115
DDR1
Q08345
-
DDR2
Q62371
-
Derailed protein
-
-
-
-
DFGF-R1
-
-
-
-
discoidin domain receptor 1
Q08345
-
discoidin domain receptor 2
Q16832
-
discoidin domain receptor 2
Q62371
-
discoidin domain receptor tyrosine kinase 1
Q08345
-
Discoidin receptor tyrosine kinase
-
-
-
-
Discoidin receptor tyrosine kinase
Q08345
-
Doughnut protein
-
-
-
-
Drl RTK
Q27324
-
Dror
-
-
-
-
Dror protein
Q24488
-
Drosophila relative of ERBB
-
-
-
-
DRT
-
-
-
-
DTK
P55144
-
DTK receptor tyrosine kinase
Q06418
-
EBK
-
-
-
-
EBK
Q61772
-
Eek receptor
O09127
-
EGF receptor
P24348
-
EGF receptor
-
-
EGF receptor protein-tyrosine kinase
-
-
EGF receptor tyrosine kinase
-
-
-
-
EGF receptor tyrosine kinase
-
-
EGF receptor tyrosine kinase
-
-
EGF receptor tyrosine kinase
-
-
EGF RPTK
-
-
EGF RTK
-
-
EGF TK
-
-
EGF-R
-
-
EGF-R
Q01279
-
EGF-receptor
-
-
Egfr
-
-
-
-
Egfr
-
-
Egfr
Q01279
-
EGFR protein tyrosine kinase
-
-
EGFR protein tyrosine kinase
-
-
EGFr TK
-
-
-
-
EGFR tyrosine kinase
P00533
-
EGFR tyrosine kinase
-
-
EGFR-tyrosine kinase
-
-
Egg laying defective protein 15
-
-
-
-
ELK
-
-
-
-
Elk tyrosine kinase
P09759
-
embryo brain kinase
Q61772
-
Embryonic brain kinase
-
-
-
-
embryonic receptor kinase
P35968
-
EmRK2
P35968
-
Endothelial kinase receptor EK1
-
-
-
-
Eph homologous kinase 3
P54759
-
Eph receptor tyrosine kinase
P54764
-
EPH-and ELK-related kinase
-
-
-
-
Eph-like kinase1
O13146
-
Eph-related receptor tyrosine kinase Cek9
Q07497
-
EphA1
-
-
EphA1 receptor
-
-
EPHA1 receptor tyrosine kinase
P21709
-
EphA2
P29317
-
EphA2
Q03145
-
EPHA4
P54764
-
ephrin receptor 1
O61460
-
ephrin type-A receptor 1
P21709
-
ephrin type-A receptor 2
P29317
-
ephrin type-A receptor 2
Q03145
-
ephrin type-A receptor 3
O13146
-
ephrin type-A receptor 3
P29318
-
ephrin type-A receptor 3
P29320
-
ephrin type-A receptor 3
P29319
-
ephrin type-A receptor 3
O08680
-
ephrin type-A receptor 4
Q07496
-
ephrin type-A receptor 4
P54764
-
ephrin type-A receptor 4
Q03137
-
ephrin type-A receptor 4A
Q91845
-
ephrin type-A receptor 4B
Q91694
-
ephrin type-A receptor 5
P54755
-
ephrin type-A receptor 5
P54756
-
ephrin type-A receptor 5
Q60629
-
ephrin type-A receptor 5
P54757
-
ephrin type-A receptor 6
Q62413
-
ephrin type-A receptor 7
O42422
-
ephrin type-A receptor 7
Q15375
-
ephrin type-A receptor 7
Q61772
-
ephrin type-A receptor 7
P54759
-
ephrin type-A receptor 8
P29322
-
ephrin type-A receptor 8
O09127
-
ephrin type-B receptor 1
P54762
-
ephrin type-B receptor 1
P09759
-
ephrin type-B receptor 1A
Q91571
-
ephrin type-B receptor 2
Q90344
-
ephrin type-B receptor 2
P28693
-
ephrin type-B receptor 2
P29323
-
ephrin type-B receptor 3
P54753
-
ephrin type-B receptor 3
P54754
-
ephrin type-B receptor 4
P54760
-
ephrin type-B receptor 4
P54761
-
ephrin type-B receptor 5
Q07497
-
ephrine receptor
-
-
epidermal growth factor receptor
-
-
epidermal growth factor receptor
P04412
-
epidermal growth factor receptor
-
-
epidermal growth factor receptor
P00533
-
epidermal growth factor receptor
-
-
epidermal growth factor receptor
Q01279
-
epidermal growth factor receptor
-
-
epidermal growth factor receptor 2
-
-
epidermal growth factor receptor 4
Q15303
-
epidermal growth factor receptor kinase
-
-
epidermal growth factor receptor tyrosine kinase
-
-
epidermal growth factor receptor tyrosine kinase
P00533
-
epidermal growth factor receptor tyrosine kinase
-
-
epidermal growth factor receptor tyrosine kinase inhibitor
-
-
Epidermal growth factor receptor-related protein
-
-
-
-
epidermal growth factor type II receptor
-
-
epidermal growth factor tyrosine protein kinase
-
-
epidermal growth factor-receptor
-
-
epidermal growth-factor receptor tyrosine kinase
-
-
Epithelial cell kinase
-
-
-
-
Epithelial cell kinase
P29317
-
epithelial discoidin domain receptor 1
Q08345
-
epithelial discoidin domain receptor 1
Q03146
-
epithelial discoidin domain receptor 1
Q63474
-
erb-B1
P00533
-
ErbB receptor protein-tyrosine kinase
-
-
erbB tyrosine kinase
-
-
-
-
ErbB-1
P00533
-
ErbB-2
P04626
-
ErbB-2
P70424
-
ErbB-4 receptor
Q15303
-
ErbB-4 tyrosine kinase
-
-
ERBB1
P00533
-
ErbB1 tyrosine kinase
-
-
ErbB2
Q61526
-
ErbB2
P06494
-
ErbB2 kinase
-
-
-
-
erbB2 receptor tyrosine kinase
-
-
erbB2 receptor tyrosine kinase
P04626
-
erbB2 receptor tyrosine kinase
-
-
erbB2 receptor tyrosine kinase
-
-
ErbB2 tyrosine kinase
-
-
ErbB3
Q61526
-
ErbB3 receptor tyrosine kinase
Q61526
-
ErbB4
-
-
ErbB4 receptor
-
-
ERK
-
-
-
-
erlotinib
-
-
ETK
-
-
-
-
fetal liver kinase 1
P35918
-
FGF receptor
P11362
-
FGF receptor tyrosine kinase
-
-
FGFR
-
-
FGFR
-
-
FGFR-4
P22455
-
FGFR1K
P11362
-
FGFR2
-
-
FGFR2
P21802
-
FGFR3
Q61851
-
FGFR4
-
-
FGFR4
Q03142
-
fibroblast growth factor receptor
-
-
fibroblast growth factor receptor
-
-
fibroblast growth factor receptor
-
-
fibroblast growth factor receptor 1
P11362
-
fibroblast growth factor receptor 1
P22182
-
fibroblast growth factor receptor 2
P21803
-
fibroblast growth factor receptor 2
Q01279
-
fibroblast growth factor receptor 2
Q03364
-
fibroblast growth factor receptor 3
Q61851
-
fibroblast growth factor receptor 4
P22455
-
fibroblast growth factor receptor 4
Q03142
-
fibroblast growth factor receptor 4
Q91742
-
fibroblast growth factor receptor BFR-2
P21802
-
fibroblast growth factor receptor homolog 1
Q07407
-
fibroblast growth factor receptor homolog 2
Q09147
-
FL cytokine receptor
Q00342
-
Flk-1
P52583
-
Flk-1
-
-
Flt-1
-
-
FLT3
P36888
-
FLT3 receptor protein
-
-
FLT3/FLK2 receptor tyrosine kinase
Q00342
-
FLT4
P35916
-
FLT4 receptor tyrosine kinase
P35916
-
Fms proto-oncogene
-
-
-
-
fms-like tyrosine kinase 3
-
-
GCTK
-
-
-
-
GCTK
P42159
-
GP145-TrkB
-
-
-
-
GP145-TrkB/GP95-TrkB
-
-
-
-
GP145-TrkC
-
-
-
-
gp145trkC
P24786
-
growth hormone receptor
-
-
Gurken receptor
-
-
-
-
Heartless protein
-
-
-
-
HEK
-
-
-
-
HEK
P29320
-
HEK 2
P54753
-
HEK3
-
-
-
-
HEK4
-
-
-
-
HEK6
-
-
-
-
Heparin-binding growth factor receptor
-
-
-
-
hepatocyte growth factor receptor
Q2IBA6
-
hepatocyte growth factor receptor
-
-
hepatocyte growth factor receptor
P08581
-
hepatocyte growth factor receptor
-
-
hepatocyte growth factor receptor
P16056
-
hepatocyte growth factor receptor
P97523
-
HER receptor protein-tyrosine kinase
-
-
HER-1
P00533
-
Her-2
P04626
-
Her1 tyrosine kinase
-
-
HER2
-
-
HER2
P04626
-
HER2
P70424
-
HER2neu
-
-
HER3
P21860
-
HER3/ERRB3
P21860
-
HGF receptor
-
-
-
-
HGF-SF receptor
-
-
-
-
high affinity nerve growth factor receptor
P04629
-
high affinity nerve growth factor receptor
P35739
-
HTK
P54760
-
HTL protein
Q07407
-
hydroxyaryl-protein kinase
-
-
-
-
HYK
-
-
-
-
HYK
Q02858
-
IGF-1 receptor
-
-
IGF-1R
P08069
-
IGF-1R
-
-
IGF-1R tyrosine kinase
-
-
IGFR tyrosine kinase
-
-
ILP receptor
-
-
-
-
ILP receptor
O02466
-
InRK
-
-
insulin receptor
-
-
insulin receptor
-
-
insulin receptor
P06213
-
insulin receptor
-
-
insulin receptor
P15208
-
insulin receptor
-
-
insulin receptor
P15127
-
insulin receptor kinase
-
-
insulin receptor kinase
-
-
insulin receptor kinase
-
-
insulin receptor protein tyrosine kinase
-
-
insulin receptor protein-tyrosine kinase
-
-
-
-
insulin receptor tyrosine kinase
-
-
insulin receptor tyrosine kinase
-
-
insulin receptor-beta subunit
-
-
insulin receptor-related protein
P14617
-
insulin receptor-related protein
P14616
-
insulin receptor-related protein
Q9wtl4
-
insulin receptor-related receptor
P24062
-
insulin RTK
P09208
-
insulin-growth factor-1 receptor
-
-
insulin-like growth factor 1 receptor
P08069
-
insulin-like growth factor I receptor
P08069
-
insulin-like growth factor I receptor
Q60751
-
insulin-like growth factor I receptor
P24062
-
insulin-like growth factor receptor
-
-
insulin-like growth factor type I receptor
-
-
Insulin-like growth factor-1 receptor
-
-
insulin-like growth factor-1 receptor kinase
-
-
Insulin-like Growth Factor-1 receptor tyrosine kinase
-
-
insulin-like peptide receptor
O02466
-
insulin-like receptor
Q93105
-
insulin-like receptor
P09208
-
insulin-receptor tyrosine kinase
-
-
IR kinase
-
-
iR-beta subunit
-
-
IR-PTK
-
-
IR-related receptor
-
-
-
-
IRK
-
-
-
-
IRR
-
-
-
-
IRR
P14616
-
IRR-protein tyrosine kinase
Q9wtl4
-
KDR
P35918
-
KDR
O08775
-
KDR/fetal liver kinase-1
-
-
KDR/Flk-1
-
-
Keratinocyte growth factor receptor
-
-
-
-
Keratinocyte growth factor receptor
-
-
Keratinocyte growth factor receptor
P21803
-
KGF receptor
-
-
KGF receptor
P21803
-
KGFR
-
-
Kinase insert domain receptor
-
-
-
-
Kinase NYK
-
-
-
-
Kinase VIK
-
-
-
-
Kit protein
Q08156
-
Kit protein-tyrosine kinase
-
-
Kit protein-tyrosine kinase
-
-
KIT receptor tyrosine kinase
-
-
leptin receptor
-
-
Let-23 receptor protein-tyrosine kinase
P24348
-
leukocyte tyrosine kinase receptor
P29376
-
leukocyte tyrosine kinase receptor
P08923
-
Linotte protein
-
-
-
-
ltk receptor tyrosine kinase
P08923
-
M-CSF receptor
-
-
macrophage colony stimulating factor I receptor
P13369
-
macrophage colony stimulating factor I receptor
P07333
-
macrophage colony stimulating factor I receptor
P09581
-
macrophage colony stimulating factor I receptor
Q00495
-
macrophage colony-stimulating factor receptor
-
-
macrophage colony-stimulating factor receptor
P09581
-
macrophage stimulating 1-receptor
-
-
macrophage-colony stimulating factor receptor
-
-
macrophage-stimulating protein receptor
Q04912
-
macrophage-stimulating protein receptor
Q62190
-
mast/stem cell growth factor receptor
P43481
-
mast/stem cell growth factor receptor
O97799
-
mast/stem cell growth factor receptor
Q28317
-
mast/stem cell growth factor receptor
Q28889
-
mast/stem cell growth factor receptor
Q08156
-
mast/stem cell growth factor receptor
P10721
-
mast/stem cell growth factor receptor
P05532
-
MDK1
Q61772
-
MEK4
-
-
-
-
melanoma receptor protein-tyrosine kinase
P13388
-
Mer receptor tyrosine kinase
Q60805
-
Mertk
Q60805
-
MET
-
-
MET
P08581
-
Met proto-oncogene tyrosine kinase
-
-
-
-
Met receptor-tyrosine kinase
-
-
Met-related kinase
-
-
-
-
Met/hepatocyte growth factor receptor tyrosine kinase
P08581
-
MFR
-
-
-
-
MIR
-
-
-
-
mouse developmental kinase 1
Q61772
-
mROR1
-
-
-
-
mROR2
-
-
-
-
MSP receptor
-
-
-
-
MST1R
-
-
muscle-specific receptor tyrosine kinase
-
-
muscle-specific receptor tyrosine kinase
Q61006
-
muscle-specific receptor-tyrosine kinase
-
-
MuSK
-
-
MuSK
Q61006
-
myoblast growth factor receptor egl-15
Q10656
-
nerve growth factor receptor
-
-
NET
-
-
-
-
NET
P54762
-
Neu
P06494
-
NEU proto-oncogene
-
-
-
-
neuregulin receptor ErbB-4
Q15303
-
Neurospecific receptor tyrosine kinase
-
-
-
-
neurotrophin tyrosine receptor kinase
-
-
neurotrophin tyrosine receptor kinase
P35739
-
NGF RPTK
-
-
non-receptor protein tyrosine kinase
-
-
NRTK
-
-
-
-
NT-3 growth factor receptor
Q91044
-
NT-3 growth factor receptor
Q16288
-
NT-3 growth factor receptor
Q03351
-
NT-3 growth factor receptor
P24786
-
nuclear growth factor tyrosine protein kinase
-
-
NUK
-
-
-
-
NYK/FLK-1
P35918
-
orphan receptor tyrosine kinase
-
-
P140 TEK
-
-
-
-
p140-TrkA
-
-
-
-
p145c-kit
P10721
-
p180erbB4
-
-
-
-
p185-Ron
-
-
-
-
p185erbB2
-
-
-
-
p190MET kinase
P08581
-
p72ITK/EMT
Q03526
-
p75 neurotrophin receptor
-
-
p75NTR
-
-
PAG
Q91694
-
Pagliaccio
-
-
-
-
PDGF A
P26619
-
PDGF beta-receptor
P09619
-
PDGF receptor
-
-
PDGF receptor
-
-
PDGF receptor tyrosine kinase
-
-
PDGF receptor tyrosine kinase
-
-
PDGF-alpha receptor
-
-
PDGF-beta receptor
-
-
PDGF-R-alpha
-
-
-
-
PDGF-R-beta
-
-
-
-
PDGFR
-
-
PDGFR kinase
-
-
-
-
PDGFR-alpha
-
-
PDGFR-alpha
-
isoform
PDGFR-beta
-
-
PDGFR-beta
-
isoform
PDGFR-beta
-
-
PDGFRB
P09619
-
PDGFRbeta
P09619
-
PKCdelta
-
-
platelet derived growth factor receptor-beta
P09619
-
platelet-derived growth factor receptor
-
-
platelet-derived growth factor receptor
-
-
platelet-derived growth factor receptor
-
-
platelet-derived growth factor receptor
-
-
platelet-derived growth factor receptor alpha
-
-
platelet-derived growth factor receptor alpha
P16234
-
platelet-derived growth factor receptor kinase
-
-
platelet-derived growth factor receptor-beta
-
-
platelet-derived growth factor RPTK
-
-
proline-rich tyrosinekinase
-
-
protein kinase Cdelta
-
-
protein kinase eck
P29317
-
protein receptor tyrosine kinase RTK 6
Q08345
-
Protein tyrosine kinase
-
-
Protein tyrosine kinase
-
-
Protein-tyrosine kinase byk
-
-
-
-
protein-tyrosine kinase ITK/EMT
Q03526
-
Protein-tyrosine kinase receptor MPK-11
-
-
-
-
Proto-oncogene tyrosine-protein kinase Kit
-
-
-
-
proto-oncogene tyrosine-protein kinase MER
Q12866
-
proto-oncogene tyrosine-protein kinase MER
Q60805
-
proto-oncogene tyrosine-protein kinase MER
P57097
-
proto-oncogene tyrosine-protein kinase receptor ret
P07949
-
proto-oncogene tyrosine-protein kinase receptor ret
P35546
-
proto-oncogene tyrosine-protein kinase ROS
P08922
-
Pyk-2
-
-
Quek2
P52583
-
rceptor protein-tyrosine kinase erbB-4
Q62956
-
recepteur d'origine nantais
-
-
recepteur d'origine nantais receptor tyrosine kinase
-
-
recepteur d'origine nantais receptor tyrosine kinase
-
-
Recepteur d’Origine Nantais
Q04912
-
receptor for macrophage colony-stimulating factor
-
-
receptor for stem cell factor
-
-
receptor protein tyrosine kinase
-
-
receptor protein tyrosine kinase RTK
Q16832
-
receptor protein-tyrosine kinase erbB-2
P04626
-
receptor protein-tyrosine kinase erbB-2
Q60553
-
receptor protein-tyrosine kinase erbB-2
P06494
-
receptor protein-tyrosine kinase erbB-3
P21860
-
receptor protein-tyrosine kinase erbB-3
Q62799
-
receptor protein-tyrosine kinase erbB-4
Q15303
-
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 PTK
-
-
receptor tyrosine kinase
O97799
-
receptor tyrosine kinase
-
-
receptor tyrosine kinase
P09208
-
receptor tyrosine kinase
-
-
receptor tyrosine kinase
P30530
-
receptor tyrosine kinase
P35590, Q02763
-
receptor tyrosine kinase
Q08345
-
receptor tyrosine kinase
-
-
receptor tyrosine kinase
-
-
receptor tyrosine kinase
P35739
-
receptor tyrosine kinase c-Kit
-
-
receptor tyrosine kinase c-Kit
P05532
-
receptor tyrosine kinase Cek8
Q07496
-
receptor tyrosine kinase EphA1
-
-
receptor tyrosine kinase EphA2
P29317
-
receptor tyrosine kinase EphA2
Q03145
-
Receptor tyrosine kinase MerTK
-
-
-
-
receptor tyrosine kinase RET
-
-
receptor tyrosine kinase RON
-
-
receptor tyrosine kinase ROR1
Q01973
-
receptor tyrosine kinase Ror2
Q01974
-
receptor tyrosine kinase Ror2
-
-
receptor tyrosine kinase Sek
Q03137
-
receptor tyrosine kinase Sky
Q06418
-
receptor tyrosine-protein kinase erbB-2
P06494
-
Receptor-activated Janus kinase
-
-
-
-
receptor-like protein tyrosine kinase bsk
Q60629
-
receptor-like protein-tyrosine kinase TK14
P21802
-
receptor-like tyrosine-protein kinase kin-15
P34891
-
receptor-like tyrosine-protein kinase kin-16
P34892
-
receptor-type tyrosine kinase termed Rse
Q06418
-
receptor-type tyrosine-protein kinase FLT3
P36888
-
recptor tyrosine kinase
-
-
RET oncogene protein
Q9vie4
-
Ret receptor tyrosine kinase
-
-
Ret receptor tyrosine kinase
-
-
Ret51
-
-
Ret9
-
-
RON receptor
Q62190
-
RON receptor tyrosine kinase
-
-
RON receptor tyrosine kinase
-
-
RON receptor tyrosine kinase
Q04912
-
RON receptor tyrosine kinase
-
-
RON receptor tyrosine kinase
-
-
RON receptor tyrosine kinase
Q62190
-
Ron tyrosine kinase receptor
Q04912
-
Ron/Stk receptor tyrosine kinase
Q62190
-
ROR1
-
-
ROR1
Q01973
-
RPTK
-
-
RPTK
-
-
RTK
-
-
-
-
RTK
Q02858
-
RTK
P35739
-
sam3 protein
Q61851
-
SCFR
-
-
-
-
sea receptor
-
-
Sek-1 receptor tyrosine kinase
Q91845
-
sevenless protein
P20806
-
sevenless receptor tyrosine kinase
-
-
sFlt-1
-
-
Sky receptor
P55146
-
sky receptor tyrosine kinase
P55146
-
Slow nerve growth factor receptor
-
-
-
-
soluble fms-like tyrosine kinase 1
-
-
sponge receptor tyrosine kinase
Q27656
-
Srcasm
P36888
-
stem cell derived tyrosine kinase
-
-
stem cell factor receptor
-
-
stem cell receptor
-
-
stem cell tyrosine kinase 1
P36888
-
Stem cell-derived tyrosine kinase
-
-
-
-
Stem cell-derived tyrosine kinase
-
-
STK-1
P36888
-
subclass III receptor tyrosine kinase
-
-
T-cell-specific kinase
Q03526
-
Tec family kinase EMT/ITK/TSK
Q03526
-
Tek receptor tyrosine kinase
Q02858
-
Tie-2
-
-
Tie1
-
-
Tie1
P35590
-
Tie2
Q02858
-
Torpedo protein
-
-
-
-
TRK1 transforming tyrosine kinase protein
-
-
-
-
TrkA
-
-
TrkA
Q16288
-
trkB
-
-
trkB
Q16288
-
trkB
Q63604
-
TrkB receptor
-
-
TrkB receptor
Q63604
-
TrkB tyrosine kinase
-
-
-
-
TrkC
-
-
TrkC
Q16288
-
TrkC
Q03351
-
TrkC receptor tyrosine kinases
Q03351
-
TrkC tyrosine kinase
-
-
-
-
Tsk
Q03526
-
Tunica interna endothelial cell kinase
-
-
-
-
Tyro 10 receptor tyrosine kinase
Q62371
-
Tyro 3
-
-
Tyrosine kinase
-
-
Tyrosine kinase CEK6 receptor
-
-
-
-
Tyrosine kinase DDR
-
-
-
-
tyrosine kinase domain of the insulin receptor
-
-
tyrosine kinase Emt/Itk
Q03526
-
tyrosine kinase p59fyn
P36888
-
tyrosine kinase QEK5
Q90344
-
tyrosine kinase receptor
-
-
tyrosine kinase receptor CEK2
P18460
-
tyrosine kinase receptor CEK3
P18461
-
Tyrosine kinase receptor HD-14
-
-
-
-
tyrosine kinase receptor HER2
P70424
-
tyrosine kinase receptor RON
-
-
tyrosine kinase receptor trkE
Q08345
-
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 Dnt
Q9v422
-
tyrosine-protein kinase Drl
Q27324
-
Tyrosine-protein kinase DTK
-
-
-
-
tyrosine-protein kinase Etk
P38134
-
tyrosine-protein kinase Etk
P58764
-
tyrosine-protein kinase Etk
Q8XC28
-
Tyrosine-protein kinase FLT3
-
-
-
-
Tyrosine-protein kinase FRT
-
-
-
-
tyrosine-protein kinase ITK/TSK
Q03526
-
tyrosine-protein kinase Ptk
O52788
-
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
Q06805
-
tyrosine-protein kinase receptor Tie-1
P35590
-
tyrosine-protein kinase receptor Tie-1
Q06806
-
tyrosine-protein kinase receptor torso
P18475
-
tyrosine-protein kinase receptor TYRO3
Q06418
-
tyrosine-protein kinase receptor TYRO3
P55144
-
tyrosine-protein kinase receptor TYRO3
P55146
-
tyrosine-protein kinase receptor UFO
P30530
-
tyrosine-protein kinase receptor UFO
Q00993
-
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
P34925
-
tyrosine-protein kinase RYK
Q01887
-
Tyrosine-protein kinase SKY
-
-
-
-
tyrosine-protein kinase transforming protein erbB
P00535
-
tyrosine-protein kinase transforming protein erbB
P11273
-
tyrosine-protein kinase transforming protein erbB
Avian erythroblastosis virus ES4
P00535
;
-
tyrosine-protein kinase transforming protein erbB
Avian erythroblastosis virus ts167
P11273
-
-
tyrosine-protein kinase transforming protein erbB
P00534
-
tyrosine-protein kinase transforming protein kit
P04048
-
tyrosine-protein kinase transforming protein kit
Feline sarcoma virus Hardy-Zuckerman 4
P04048
-
-
tyrosine-protein kinase transforming protein RYK
P33497
-
tyrosine-protein kinase transmembrane receptor Ror
Q24488
-
tyrosine-protein kinase transmembrane receptor ROR1
Q01973
-
tyrosine-protein kinase transmembrane receptor ROR1
Q9z139
-
tyrosine-protein kinase transmembrane receptor ROR2
Q01974
-
tyrosine-protein kinase transmembrane receptor ROR2
Q9z138
-
tyrosine-protein kinase Wzc
P76387
-
tyrosine-protein kinase Wzc
Q8X7L9
-
tyrosine-protein kinase Wzc
Q8X7L9
-
-
VAB-1 Eph receptor tyrosine kinase
O61460
-
vascular endothelial growth factor
-
-
vascular endothelial growth factor 2
-
-
vascular endothelial growth factor receptor
-
-
vascular endothelial growth factor receptor
P35968
-
vascular endothelial growth factor receptor
-
-
vascular endothelial growth factor receptor
P35918
-
vascular endothelial growth factor receptor
-
-
vascular endothelial growth factor receptor
O08775
-
vascular endothelial growth factor receptor 1
P17948
-
vascular endothelial growth factor receptor 1
P53767
-
vascular endothelial growth factor receptor 2
P52583
-
vascular endothelial growth factor receptor 2
-
-
vascular endothelial growth factor receptor 2
-
-
vascular endothelial growth factor receptor 2
P35968
-
vascular endothelial growth factor receptor 2
P35918
-
vascular endothelial growth factor receptor 2
O08775
-
vascular endothelial growth factor receptor 3
P35916
-
vascular endothelial growth factor receptor 3
P35917
-
vascular endothelial growth factor receptor tyrosine kinase
-
-
vascular endothelial growth factor receptor-1
P35968
-
vascular endothelial growth-factor receptor-1 tyrosine kinase
-
-
Vascular permeability factor receptor
-
-
-
-
VEGF factor receptor tyrosine kinase
-
-
VEGF receptor
P35968
-
VEGF receptor
P35918
-
VEGF receptor
O08775
-
VEGF receptor 2
P52583
-
VEGF receptor tyrosine kinase
-
-
VEGF receptor-1
P35968
-
VEGF-receptor
-
-
VEGFR
-
-
VEGFR tyrosine kinase
-
-
VEGFR-1
-
-
VEGFR-1 tyrosine kinase
-
-
VEGFR-2
P35968
-
VEGFR-2
P35918
-
VEGFR-2
O08775
-
VEGFR-2 tyrosine kinase
P35968
-
VEGFR-3
-
-
VEGFR1
-
-
VEGFR1
-
isoform
VEGFR1-3
-
-
VEGFR2
-
-
VEGFR2
-
-
VEGFR2
-
isoform
VEGFR2/kinase domain region
-
-
VEGFR3
-
isoform
vitamin D receptor
-
-
Xek
Q91571
-
Xenopus Elk-like kinase
Q91571
-
MLN 19
-
-
-
-
additional information
-
EGFR tyrosine kinase, Her1 tyrosine kinase, ErbB1 tyrosine kinase are part of the plasma membrane receptor tyrosine kinase family
additional information
-
epidermal growth factor receptor is a member of the Erb family
additional information
-
Kit receptor is a type III protein-tyrosine kinase
additional information
-
the enzyme is a member of receptor-mediated PTK family
additional information
-
the enzyme is a member of the FGFR family
additional information
-
WebB and HER receptor protein-tyrosine kinase, as well as epidermal growth factor receptor belong to the ErbB family, overview
additional information
P00533
the enzymes belong to the epidermal growth factor receptor family, i.e. EGFR/ErbB family
ORGANISM
COMMENTARY
LITERATURE
SEQUENCE CODE
SEQUENCE DB
SOURCE
strain ts167
SwissProt
Manually annotated by BRENDA team
Avian erythroblastosis virus ES4
strain ES4
SwissProt
Manually annotated by BRENDA team
Avian erythroblastosis virus ts167
strain ts167
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
grown in bovine BM and HCT-8 cells, parasite contains membrane proteins with EGF-like extracellular domains
-
-
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
strain O157
SwissProt
Manually annotated by BRENDA team
strain O157
SwissProt
Manually annotated by BRENDA team
strain Hardy-Zuckerman 4
SwissProt
Manually annotated by BRENDA team
Feline sarcoma virus Hardy-Zuckerman 4
strain Hardy-Zuckerman 4
SwissProt
Manually annotated by BRENDA team
ssp. catus
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
2 enzyme forms FGFR1 and FGFR2
-
-
Manually annotated by BRENDA team
2 isozymes PDGF-alpha receptor and PDGF-beta receptor, 4 isozymes FGFR-1, FGFR-2, FGFR-3, and FGFR-4
-
-
Manually annotated by BRENDA team
4 isozymes FGFR1-4
-
-
Manually annotated by BRENDA team
c-Met kinase
SwissProt
Manually annotated by BRENDA team
DDR1
SwissProt
Manually annotated by BRENDA team
EPHA4
SwissProt
Manually annotated by BRENDA team
epidermal growth factor receptor tyrosine kinase
SwissProt
Manually annotated by BRENDA team
ErbB1
SwissProt
Manually annotated by BRENDA team
IGF-1R
SwissProt
Manually annotated by BRENDA team
insulin-like growth factor 1 receptor
SwissProt
Manually annotated by BRENDA team
juxtamembrane domain and catalytic domains of c-Kit receptor protein-tyrosine kinase, residues 544-935
SwissProt
Manually annotated by BRENDA team
macrophage-stimulating protein receptor
SwissProt
Manually annotated by BRENDA team
MET
SwissProt
Manually annotated by BRENDA team
patients with chronic myelogenous leukemia
SwissProt
Manually annotated by BRENDA team
PDGFR-beta
SwissProt
Manually annotated by BRENDA team
PDGFRalpha
SwissProt
Manually annotated by BRENDA team
receptor-type tyrosine-protein kinase FLT3
SwissProt
Manually annotated by BRENDA team
several isozymes of both ErbB receptor protein-tyrosine kinase and HER receptor protein-tyrosine kinase
-
-
Manually annotated by BRENDA team
Southeast Asian acute myeloid leukemia patients
-
-
Manually annotated by BRENDA team
Mongolian gerbil
-
-
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
Balb/c female mice
SwissProt
Manually annotated by BRENDA team
C57BL/6 mice
SwissProt
Manually annotated by BRENDA team
CD-1 mice, BALB/cJ mice and C57BL/6 mice
SwissProt
Manually annotated by BRENDA team
male ddY mice
-
-
Manually annotated by BRENDA team
strains C3H/HeJ and C57BL/6
-
-
Manually annotated by BRENDA team
wild-type 129/P3J mice and 129/SvJ SR-A-/- mice
SwissProt
Manually annotated by BRENDA team
grown in bovine BM and HCT-8 cells, parasite contains membrane proteins with EGF-like extracellular domains
-
-
Manually annotated by BRENDA team
New Zealand white rabbits
-
-
Manually annotated by BRENDA team
female Sprague-Dawley rats
SwissProt
Manually annotated by BRENDA team
female Wistar rats
-
-
Manually annotated by BRENDA team
male sprague-dawley rats
-
-
Manually annotated by BRENDA team
male Wistar rats
-
-
Manually annotated by BRENDA team
grown in bovine BM and HCT-8 cells, parasite contains membrane proteins with EGF-like extracellular domains
-
-
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
metabolism
P54764
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
metabolism
-
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
-
PKCeltad is strongly associated with apoptosis induced by stearylamine-liposomes
physiological function
-
Kruppel-like factor 11 inhibits prostaglandin E2 synthesis via transcriptional silencing of the promoter of cytosolic phospholipase A2, this function of Kruppel-like factor 11 can be reversed by epidermal growth factor receptor-AKT-mediated post-translational modification of threonine 56
physiological function
-
brain-derived neurotrophic factor and TrkB signaling activates Narp expression alone
physiological function
-
VEGFR1 and VEGFR2 are the most important receptors involved in neovascularization
physiological function
Q08345
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
physiological function
-
Sevenless receptor tyrosine kinase binds directly to either the suppressor of cytokine signalling SOCS36E or the adaptor protein Drk, i.e. downstream of receptor kinase. In a mechanistic model, the competition between these two proteins for binding to the same docking site results in either attenuation of the Sevenless receptor tyrosine kinase transduction in cells that should not develop R7 photoreceptors or amplification of the Ras-MAPK signal only in the R7 precursor
physiological function
-
longterm exposure to different growth factors results in receptor tyrosine kinase-specific regulation of relatively small subproteomes, and implies that the strength and longevity of receptor tyrosine kinase-specific signals are critical in defining the composition and functional activity of the resulting proteome
physiological function
P08581
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
physiological function
-
potent activation of WNT/beta-catenin signaling by isoforms FGFR2, FGFR3, EGFR and TRKA kinases, which is independent of the PI3K/AKT pathway. Instead, this phenotype depends on ERK MAP kinase-mediated phosphorylation of WNT co-receptor LRP6 at Ser1490 and Thr1572 during its Golgi network-based maturation process. This phosphorylation dramatically increases the cellular response to WNT. FGFR2, FGFR3, EGFR and TRKA directly phosphorylate beta-catenin at Tyr142, which is known to increase cytoplasmic beta-catenin concentration via release of beta-catenin from membranous cadherin complexes
SUBSTRATE
PRODUCT                      
REACTION DIAGRAM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
(Substrate)
LITERATURE
(Substrate)
COMMENTARY
(Product)
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
-
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
FLT-3 is involved in signal transduction, mechanisms
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
phosphorylation of downstream signalling proteins
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
regulation mechanisms and ligand binding, ligand binding induces a conformational change, overview
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
stem cell factor and Kit receptor are essential playing important roles in e.g. gametogenesis, hematopoiesis, mast cell development and function, and melanogenesis, complete absence is lethal, enzyme deficiencies lead to defects in white and red blood cell production, to hypopigmentation, and to sterility, Kit receptor signaling regulation by autophosphorylation and dephosphorylation via a phosphatase, regulation mechanism, overview
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
stem cell factor and Kit receptor are essential playing important roles in gametogenesis, hematopoiesis, mast cell development and function, and melanogenesis, complete absence is lethal, enzyme deficiencies lead to defects in white and red blood cell production, to hypopigmentation, and to sterility
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
stem cell factor and Kit receptor are essential playing important roles in gametogenesis, hematopoiesis, mast cell development and function, and melanogenesis, complete absence is lethal, enzyme deficiencies lead to defects in white and red blood cell production, to hypopigmentation, and to sterility, Kit receptor signaling regulation by autophosphorylation and dephosphorylation via a phosphatase
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
P10721
substrate binding and active structure
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
substrates are membrane and cytosolic proteins
-
-
?
ATP + Ac-DYFE-6-chloro-W-NHMe
ADP + Ac-DYpFE-6-chloro-W-NHMe
show the reaction diagram
P08069
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
P08069
substrate identified by substrate-activity-screening methodology based on optimization of substrate YFEW in a modular manner
-
-
?
ATP + cortactin-L-tyrosine
ADP + cortactin-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, activates GRK2 by tyrosine phosphorylation at Y13, Y86, and Y92, the wild-type PDGFRbeta is 60fold more active with GRK2 than PDGFRbeta mutant Y857F, independent of Gbetagamma subunits and phosphoinositide 3-kinase
-
-
?
ATP + insulin receptor substrate 1-L-tyrosine
ADP + insulin receptor substrate 1-L-tyrosine phosphate
show the reaction diagram
-
-
tyrosine phosphorylation of insulin receptor substrate-1 by insulin receptor is decreased when insulin receptor substrate-1 is contained in high-molecular mass complexes prepared from 3T3-L1 adipocytes treated with tumor necrosis factor-alpha. Cytokine/hormone-induced formation of high-molecular mass complexes modulates availability of insulin receptor substrates to receptor tyrosine kinases
-
?
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 + insulin receptor substrate 2-L-tyrosine
ADP + insulin receptor substrate 2-L-tyrosine phosphate
show the reaction diagram
-
-
tyrosine phosphorylation of insulin receptor substrate-2 by insulin-like growth factor IGF-I receptor is increased when insulin receptor substrate-2 is contained in high-molecular-mass complexes prepared from FRTL-5 thyrocytes treated with dibutyryl cAMP. Cytokine/hormone-induced formation of high-molecular mass complexes modulates availability of insulin receptor substrates to receptor tyrosine kinases
-
?
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 + p130Cas-L-tyrosine
ADP + p130Cas-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + paxillin-L-tyrosine
ADP + paxillin-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
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 + phospholipase C gamma
ADP + phosphorylated phospholipase C gamma
show the reaction diagram
-
-
-
?
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 + phospholipase C gamma-L-tyrosine
ADP + phospholipase C gamma-L-tyrosine phosphate
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 + phosphorylated poly(Glu:Tyr)
show the reaction diagram
P58764
-
-
-
?
ATP + poly(Glu:Tyr)
ADP + poly(Glu:Tyr) phosphate
show the reaction diagram
-
-
-
-
?
ATP + poly-(Glu-Tyr)
ADP + poly-(Glu-Tyr) phosphate
show the reaction diagram
-
-
Tyr-phosphate
-
?
ATP + protein
ADP + protein tyrosine phosphate
show the reaction diagram
-
autophosphorylation
-
-
?
ATP + protein
ADP + protein tyrosine phosphate
show the reaction diagram
-
Y602 is a major site of in vitro autophosphorylation in Sek, Y596 is phosphorylated to a lower stoichiometry
-
-
?
ATP + protein
ADP + protein tyrosine phosphate
show the reaction diagram
-
intrinsic autophosphorylation activity
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
show the reaction diagram
-
autophosphorylation
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
show the reaction diagram
Q60553
autophosphorylation
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
show the reaction diagram
-
autophosphorylation
-
-
-
ATP + protein tyrosine
ADP + protein tyrosine phosphate
show the reaction diagram
-
protein kinase activity with specificity for tyrosine residues
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
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 + protein tyrosine
ADP + protein tyrosine phosphate
show the reaction diagram
-
specific for tyrosine
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
show the reaction diagram
P15208
insulin stimulates sequential autophosphorylation of Tyr1148, Tyr1152 and Tyr1153. Transition from the doubly to the triply phosphorylated forms is primarily responsible for the activation of substrate phosphorylation
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
show the reaction diagram
Q9wtl4
IRS-1 and IRS-2 proteins serve as substrates
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
show the reaction diagram
-
phospholipase C-gamma 1 is directly phosphorylated by TrkB
-
-
-
ATP + protein tyrosine
ADP + protein tyrosine phosphate
show the reaction diagram
-
phospholipase C-gamma 1 is directly phosphorylated by TrkB
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
show the reaction diagram
-
major sites of autophosphorylation are in the region containing Tyr670, Tyr674, and Tyr675
-
-
-
ATP + protein tyrosine
ADP + protein tyrosine phosphate
show the reaction diagram
P29320
autophosphorylated on tyrosine and also mediated tyrosine phosphorylation of casein
-
-
?
ATP + tyrosine-protein kinase Etp
ADP + phosphotyrosine-protein kinase Etp
show the reaction diagram
-
-
-
-
?
ATP + tyrosine-protein kinase Wcz
ADP + phosphotyrosine-protein kinase Wcz
show the reaction diagram
-
autophosphorylation
-
-
?
ATP + tyrosine-protein kinase Wcz
ADP + phosphotyrosine-protein kinase Wcz
show the reaction diagram
P58764
autophosphorylation
-
-
?
ATP + tyrosine-protein kinase Wcz
ADP + phosphotyrosine-protein kinase Wcz
show the reaction diagram
O52788
autophosphorylation
-
-
?
ATP + tyrosine-protein kinase Wcz
ADP + phosphotyrosine-protein kinase Wcz
show the reaction diagram
-
autophosphorylation
-
-
?
ATP + tyrosine-protein kinase Wcz
ADP + phosphotyrosine-protein kinase Wcz
show the reaction diagram
P76387
The C-terminal domain alone can undergo autophosphorylation and thus appears to harbor the protein-tyrosine kinase activity. By contrast, the N-terminal domain is not phosphorylated when incubated either alone or in the presence of the C-domain, and does not influence the extent of phosphorylation of the C-domain. The C-domain contains six different sites of phosphorylation. Among these, five are located at the C-terminal end of the molecule in the form of a tyrosine cluster Tyr708, Tyr710, Tyr711, Tyr713, and Tyr715, and one site is located upstream, at Tyr569. The Tyr569 residue can autophosphorylate through an intramolecular process, whereas the tyrosine cluster cannot. The phosphorylation of Tyr569 results in an increased protein kinase activity of Wzc, which can, in turn, phosphorylate the five terminal tyrosines through an intermolecular process. It is concluded that protein Wzc autophosphorylates by using a cooperative two-step mechanism that involves both intraphosphorylation and interphosphorylation
-
-
?
ATP + tyrosine-protein kinase Wcz
ADP + phosphotyrosine-protein kinase Wcz
show the reaction diagram
-
autophosphorylation at several tyrosine residues
-
-
?
ATP + tyrosine-protein kinase Wcz
ADP + phosphotyrosine-protein kinase Wcz
show the reaction diagram
-
efficient autophosphorylation in presence of ATP
-
-
?
ATP + tyrosine-protein kinase Wcz
ADP + phosphotyrosine-protein kinase Wcz
show the reaction diagram
-
presence of at least five isoforms, all phosphorylated exclusively at tyrosine supports the concept that autophosphorylation occurs at multiple sites within the protein
-
-
?
ATP + YFEW
ADP + YpFEW
show the reaction diagram
P08069
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 + [flagellin]-L-tyrosine
ADP + [flagellin]-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
-
-
?
poly(Glu:Tyr) + ATP
ADP + ?
show the reaction diagram
-
-
-
-
?
poly(Glu:Tyr) + ATP
ADP + poly(Glu:Tyr) phosphate
show the reaction diagram
-
-
-
-
?
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
?
-
-
-
-
-
-
additional information
?
-
Q62799
-
-
-
-
additional information
?
-
O02466
autophosphorylation
-
-
-
additional information
?
-
-
autophosphorylation
-
-
-
additional information
?
-
-
no phosphorylation of synthetic substrates such as poly(Glu80 Tyr20) or angiotensin II
-
-
-
additional information
?
-
O13146
generalized function of the Zek1 receptor in neuronal cell ontogeny
-
-
-
additional information
?
-
-
N-terminal portion of the enzyme is sufficient for the transformation of fibroblasts, one-third of the carboxy-terminal domain has a key role for the transformation of erythroid cells
-
-
-
additional information
?
-
O61460
functions in neural and epithelial morphogenesis
-
-
-
additional information
?
-
-
alternative splicing of the FGFR2 gene in the region encoding the carboxyl-terminal half of the third immunoglobulin domain determines the ligand specificity of this group of receptors
-
-
-
additional information
?
-
P76387
enzyme is involved in signal transduction
-
-
-
additional information
?
-
-
possible involvement of the enzyme in cell recognition and bacterial pathogenicity
-
-
-
additional information
?
-
P58764
involved in exopolysaccharide production and virulence
-
-
-
additional information
?
-
-
phosphotyrosine-protein phosphatase Wzb is able to dephosphorylate previously autophosphorylated Wzc. Reversible protein phosphorylation on tyrosine may be part of the cascade of reactions that determine the pathogenicity of bacteria
-
-
-
additional information
?
-
-
phosphorylation of Wzc, as regulated by Wzb, is directly connected with the production of a particular capsular polysaccharide, colanic acid. Thus, when Wzc is phosphorylated on tyrosine, no colanic acid is synthesised by bacteria, but when dephosphorylated by Wzb, colanic acid is produced
-
-
-
additional information
?
-
-
enzyme is involved in the production of the extracellular polysaccharide colanic acid
-
-
-
additional information
?
-
Q91845
Sek-1, perhaps with other Eph-related receptors, is required for interactions that regulate the segmental identity or movement of cells
-
-
-
additional information
?
-
Q60805
tyrosine kinase may play an important function in the developing mouse
-
-
-
additional information
?
-
Q61772
important role in the formation of neuronal structures and possibly other morphogenic processes
-
-
-
additional information
?
-
-
important role in neurogenesis
-
-
-
additional information
?
-
-
the neurotrophic receptor may function during early stages of neural development
-
-
-
additional information
?
-
Q63474
may play an important role in the generation of the mammalian nervous system
-
-
-
additional information
?
-
-
Dnrk may play an important role in neural development during Drosophila embryogenesis
-
-
-
additional information
?
-
Q91694
Pag may play a role in the differentiation of cranial neural crest and other tissues
-
-
-
additional information
?
-
Q9wtl4
receptor may play a role in the regulation of beta-cell mass
-
-
-
additional information
?
-
-
role for DDR2 in critical events during wound repair
-
-
-
additional information
?
-
-
essential for migration of tracheal and specific midline glial cells
-
-
-
additional information
?
-
Q9z138
required for cartilage and growth plate development
-
-
-
additional information
?
-
-
receptor of neuregulin
-
-
-
additional information
?
-
Q91571
may play a role in the development or function of the central nervous system
-
-
-
additional information
?
-
Q90344
may play a role in cell-cell interactions involved in retinotectal projections and differentiation of the central nervous system
-
-
-
additional information
?
-
-
required for directed tracheal cell extension
-
-
-
additional information
?
-
-
part of a novel signal transduction cascade involved in learning and memory
-
-
-
additional information
?
-
-
involved in cell-cell interactions
-
-
-
additional information
?
-
-
mutations in MERTK, the human orthologue of the RCS rat retinal dystrophy gene, cause retinitis pigmentosa
-
-
-
additional information
?
-
-
receptor protein-tyrosine kinase involvement in key aspects of neuronal pathway recognition
-
-
-
additional information
?
-
-
essential for the pathfinding ability of expressing neurons, participates in a mechanism required for muscle attachment site selection
-
-
-
additional information
?
-
Q62799
expression of neuregulins and their putative receptor ErbB3, is induced during Wallerian degeneration
-
-
-
additional information
?
-
-
amplification of the c-erb-B-2 gene in a salivary adenocarcinoma and a gastric cancer cell line MKN-7 suggests that its over-expression is sometimes involved in the neoplastic process
-
-
-
additional information
?
-
-
transformation of fibroblasts and transformation of erythroid cells
-
-
-
additional information
?
-
P00535
the erB oncogene efficiently transforms erythroblasts
-
-
-
additional information
?
-
P08069
plays an important role in cell growth control
-
-
-
additional information
?
-
P07333, P10721
implicated in the control of cell growth and differentiation
-
-
-
additional information
?
-
-
enzyme functions as the cell surface receptor for the macrophage colony stimulating factor
-
-
-
additional information
?
-
-
cell-surface receptor for an as-yet-unknown ligand
-
-
-
additional information
?
-
-
missense mutations located in the MET proto-oncogene lead to constitutive activation of the MET protein and papillary renal carcinomas
-
-
-
additional information
?
-
-
the proto-oncogene c-kit is involved in signal transduction
-
-
-
additional information
?
-
P06494
receptor for an as yet unidentified growth factor
-
-
-
additional information
?
-
-
functions as a cell surface receptor for an as yet unidentified ligand
-
-
-
additional information
?
-
-
human ltk gene maps to chromosome 15, bands q13-21, a region containing the breakpoint of a recurring chromosomal abnormality in B-cell non-Hodgkin lymphomas
-
-
-
additional information
?
-
-
Elk tyrosine kinase may be involved in cell-cell interactions in the nervous system
-
-
-
additional information
?
-
-
piebaldism results from mutations of the KIT proto-oncogene, which encodes the cellular receptor transmembrane tyrosine kinase for mast/stem cell growth factor
-
-
-
additional information
?
-
-
human piebald trait resulting from a dominant negative mutant allele of the c-kit membrane receptor gene
-
-
-
additional information
?
-
-
Ltk is expressed at a very low level in only a few cell lines and tissues and may be the receptor for a pre-B lymphocyte growth or differentiation factor
-
-
-
additional information
?
-
P09208
activity of inr gene appears to be required in the embryonic epidermis and nervous system among others, since development of the cuticle, as well as the peripheral and central nervous systems are affected by inr mutations
-
-
-
additional information
?
-
-
mutations in the coding sequence of the proto-oncogene c-kit in a human mast cell leukemia cell line causing ligand-independent activation of c-kit product
-
-
-
additional information
?
-
-
mutations in the fibroblast growth factor receptor-1 gene, which maps to 8p, cause one form of familial Pfeiffer syndrome. A C to G transversion in exon 5, predicting a proline to arginine substitution in the putative extracellular domain, is identified in all affected members of five unrelated PS families but not in any unaffected individuals
-
-
-
additional information
?
-
-
determination of anterior and posterior terminal structures of Drosophila embryos requires activation of two genes encoding putative protein kinases, torso and D-raf
-
-
-
additional information
?
-
-
Jackson-Weiss syndrome and Crouzon syndrome are allelic with mutations in fibroblast growth factor receptor 2
-
-
-
additional information
?
-
P20806
enzyme is required for normal eye development
-
-
-
additional information
?
-
-
IR-related protein is a receptor for insulin, IGF-I, IGF-II, or an as yet unidentified peptide hormone or growth factor belonging to the insulin family
-
-
-
additional information
?
-
P14617
IR-related protein is a receptor for insulin, IGF-I, IGF-II, or an as yet unidentified peptide hormone or growth factor belonging to the insulin family
-
-
-
additional information
?
-
-
FGFR2 mutations in Pfeiffer syndrome
-
-
-
additional information
?
-
-
trkB may code for a cell surface receptor involved in neurogenesis
-
-
-
additional information
?
-
-
enzyme is involved in glial cell generation
-
-
-
additional information
?
-
-
sevenless gene determines the fate of a single photoreceptor cell type in the eye of Drosophila
-
-
-
additional information
?
-
P13388
malignant melanoma in Xiphophorus fish hybrids is caused by the activity of a dominant oncogene Tu which codes for a receptor tyrosine kinase
-
-
-
additional information
?
-
P21709
ephrin type-A receptor 1 may be involved in the neoplastic process of some tumors
-
-
-
additional information
?
-
-
high affinity receptor for both acidic and basic fibroblast growth factor but not for keratinocyte growth factor
-
-
-
additional information
?
-
-
FGFR-4 binds acidic fibroblast growth factor with high affinity but does not bind basic fibroblast growth factor
-
-
-
additional information
?
-
-
receptor tyrosine kinase is necessary for the induction of a vulva, survival past the L1 stage, hermaphrodite fertility and for male spicule development
-
-
-
additional information
?
-
P24786
gp145trkC may play an important role in mediating the neurotrophic effects of NT-3
-
-
-
additional information
?
-
P29376
tk gene product likely functions as a cell surface receptor for an unidentified cellular growth factor
-
-
-
additional information
?
-
P35916
receptors for at least two hematopoietic growth factors: the stem cell factor and the colony-stimulating factor 1
-
-
-
additional information
?
-
-
may play a role in vascular development and regulation of vascular permeability
-
-
-
additional information
?
-
-
gene plays important role in embryonic development and carcinogenesis of the stomach
-
-
-
additional information
?
-
-
Flk-1 as a major regulator of vasculogenesis and angiogenesis
-
-
-
additional information
?
-
-
may be involved in tumor progression of epithelial ovarian cancer
-
-
-
additional information
?
-
P34891, P34892
may be specifically involved in cell-cell interactions regulating cell fusions that generate the hypodermis during postembryonic development
-
-
-
additional information
?
-
P26618
possibility that overexpression of PDGF-alpha receptor in high-metastatic clones may contribute to an increase in the capacity of tumor cells to generate metastases in the lung
-
-
-
additional information
?
-
P35739
signal transducing receptor for nerve growth factor
-
-
-
additional information
?
-
P15127
increased ERBB3 expression may play a role in some human malignancies
-
-
-
additional information
?
-
P26619
ectodermally produced PDGF A may act on the mesoderm during gastrulation and mesoderm induction establishes the tissue pattern of ligand and receptor expression
-
-
-
additional information
?
-
P24348
receptor for the inductive signal required for vulval development
-
-
-
additional information
?
-
-
enzyme is a receptor for vascular endothelial cell growth factor
-
-
-
additional information
?
-
-
plays a part in human neurogenesis, DRT gene may play a part in neuroblastoma and SCLC tumorigenesis
-
-
-
additional information
?
-
P29318
may play an important role during development and in signal transduction pathways
-
-
-
additional information
?
-
P29319
may play an important role during development and in signal transduction pathways
-
-
-
additional information
?
-
-
acts through a conserved Ras/MAP kinase signaling pathway to induce vulval differentiation
-
-
-
additional information
?
-
-
element of the complex signaling network involved in the control of cell proliferation and differentiation
-
-
-
additional information
?
-
-
inhibition of vascular smooth muscle cell growth through antisense transcription of a rat insulin-like growth factor I receptor cDNA
-
-
-
additional information
?
-
P29320
may have a role in tumorigenesis
-
-
-
additional information
?
-
-
involved in the proliferation of early progenitor/stem cells
-
-
-
additional information
?
-
-
receptor may be a key signal transducing component in the totipotent hematopoietic stem cell and its immediate self-renewing progeny
-
-
-
additional information
?
-
-
possible role for repulsive B-class Eph receptor/ligand interactions in constraining the orientation of longitudinal axon projections at the ventral midline
-
-
-
additional information
?
-
-
tyro3 may function as a novel neurotrophic factor receptor
-
-
-
additional information
?
-
P54761
important role in gestational growth and differentiation
-
-
-
additional information
?
-
-
Srcasm may help promote Src family kinase signaling in cells
-
-
-
additional information
?
-
P97523
tyrosine kinase receptor for hepatocyte growth factor
-
-
-
additional information
?
-
-
increased c-met expression indicates that this gene may participate in the healing process of gastric mucosa after injury
-
-
-
additional information
?
-
-
enzyme is implicated in control of cell growth
-
-
-
additional information
?
-
-
NET potentially plays important roles in human neurogenesis
-
-
-
additional information
?
-
P97793
ALK plays an important role in the development of the brain
-
-
-
additional information
?
-
-
important role for this kinase in CD2 co-stimulation of T cell responses
-
-
-
additional information
?
-
Q04912
role for the Ron receptor in progression toward malignancy
-
-
-
additional information
?
-
-
primary function is likely to be in developmental regulation
-
-
-
additional information
?
-
-
distinct mutations in the receptor tyrosine kinase gene ROR2 cause brachydactyly type B
-
-
-
additional information
?
-
-
recessive Robinow syndrome, allelic to dominant brachydactyly type B, is caused by loss of ROR2 activity
-
-
-
additional information
?
-
-
Cek9 plays an active role in embryonic signal transduction pathways
-
-
-
additional information
?
-
-
role for Tsk in early T-lymphocyte differentiation
-
-
-
additional information
?
-
-
rat trkC locus encodes multiple neurogenic receptors that exhibit differential response to neurotrophin-3 in PC12 cells
-
-
-
additional information
?
-
-
dominant mutations in ROR2, encoding an orphan receptor tyrosine kinase, cause brachydactyly type B
-
-
-
additional information
?
-
-
the mouse waved-2 phenotype results from a point mutation in the EGF receptor tyrosine kinase
-
-
-
additional information
?
-
Q00993
ufo may function as a signal transducer between specific cell types of mesodermal origin
-
-
-
additional information
?
-
-
Cek8 suggests its involvement in cellular survival or cell-cell interactions for specific subpopulations of developing motoneurons
-
-
-
additional information
?
-
-
tek receptor tyrosine kinase may be critically involved in the determination and/or maintenance of cells of the endothelial lineage
-
-
-
additional information
?
-
-
itk functions in a signal transduction pathway unique to T lymphocytes
-
-
-
additional information
?
-
-
ron gene product is a specific cell-surface receptor for macrophage-stimulating protein
-
-
-
additional information
?
-
-
mutation of the gene encoding the ROR2 tyrosine kinase causes autosomal recessive Robinow syndrome
-
-
-
additional information
?
-
-
vascular dysmorphogenesis caused by an activating mutation in the receptor tyrosine kinase TIE2
-
-
-
additional information
?
-
-
Sky may be involved in cell adhesion processes, particularly in the central nervous system
-
-
-
additional information
?
-
-
expression of the EGF-R gene in mouse blastocysts is tightly regulated by maternal steroid hormonal status
-
-
-
additional information
?
-
-
Emt/Itk is a protein tyrosine kinase required for T cell Ag receptor TCR-induced activation and development
-
-
-
additional information
?
-
Q00495
mrfms gene products may play a role in the normal and neoplastic growth of muscular cells
-
-
-
additional information
?
-
-
activating mutations of the fibroblast growth factor receptor 3 cause skeletal dysplasias including achondroplasia, and the neonatal lethal syndromes thanatophoric dysplasia types I and II, the mutations are also involved in cancer development, e.g. in multiple myeloma, bladder carcinoma, and cervical cancer
-
-
-
additional information
?
-
-
activation of PDGF receptor growth factor results in increased intracellular Ca2+ flux and cytoplasmic pH changes, enzyme stimulates generation of reactive oxygen species, such as O2.- and H2O2, which function as mitogenic mediators of activated growth-factor-receptor signaling, overview, the EGFR signaling pathway functions in many cellular processes, including proliferation, cell migration, and apoptosis, signaling pathways, overview
-
-
-
additional information
?
-
-
activation of PDGF receptor growth factor results in increased intracellular Ca2+ flux and cytoplasmic pH changes, enzyme stimulates generation of reactive oxygen species, which function as mitogenic mediators of activated growth-factor-receptor signaling, overview, the EGFR signaling pathway functions in many cellular processes, including proliferation, cell migration, and apoptosis, signaling pathways, overview
-
-
-
additional information
?
-
-
antagonistic regulation of swelling-activated Cl- current in rabbit ventricle by Src and EGFR protein tyrosine kinases, overview
-
-
-
additional information
?
-
-
deoxycholic acid and taurodeoxycholic acid activate insulin receptor kinase and ERBB1 kinase and subsequent ERK1/2 and AKT signaling pathways activation via induction of reactive oxygen species ROS production in mitochondria, ROS activation can be blocked by scavengers N-acetyl cysteine and Trolox, as well as cyclosporine A and bongkrekic acid
-
-
-
additional information
?
-
-
downregulation of endogenous Syk non-receptor tyrosine protein kinase expression in mammary endothelial cells enhances the ligand-induced activity of the epidermal growth factor receptor, but not of closely related human epidermal growth factor receptors HER2 and HER3, EGFR has a regulatory feedback effect on Syk, enzyme deregulation is associated with pathophysiological disorders such as cancer, regulation in vivo overview
-
-
-
additional information
?
-
-
EGF-like peptides bind as ligands to the extracellular domain of host cell EGFR leading to an activation of the intracellular tyrosine kinase domain which initiates downstream signaling pathways, e.g. the mitogen-activated protein kinase cascade
-
-
-
additional information
?
-
-
EGF-like peptides on the surface of coccidial parasites Sarcocystis neurona, Neospora caninum, and Cryptosporidium parvum bind as ligands to the extracellular domain of the gerbils' host cells' EGFR leading to an activation of the intracellular tyrosine kinase domain which initiates downstream signaling pathways, e.g. the mitogen-activated protein kinase cascade
-
-
-
additional information
?
-
P00533
enzyme regulation via reversible autophosphorylation, binding to plasma membrane of enzyme and enzyme-derived peptides, overview
-
-
-
additional information
?
-
-
enzyme transactivation stimulates cell migration and the subsequent activation of downstream signaling pathways
-
-
-
additional information
?
-
-
ErbB family enzymes are absolutely required for viability of embryos
-
-
-
additional information
?
-
-
insulin receptor tyrosine kinase is activated via autophosphorylation, the receptor plays a role in signalling which is redox autoregulated by insulin-induced reactive oxygen species involving an autoregulatory loop, redundant mechanisms, overview, physiologic implications for diabetes and hyperglycemia
-
-
-
additional information
?
-
-
insulin- or H2O2-induced activation by autophosphorylation of the insulin receptor initiates the IR signaling pathway which includes phosphorylation of extracellular signal-regulated kinases 1 and 2, i.e. ERK1 and ERK2, protein kinase B, and glycogen synthase kinase 3-beta
-
-
-
additional information
?
-
-
mutations in the glycine-riche loop of MET can cause papillary renal-cell carcinomas
-
-
-
additional information
?
-
-
PDGFRbeta wild-type and mutant Y857F activate c-Src kinase
-
-
-
additional information
?
-
-
platelet-derived growth factor receptor or epidermal growth factor receptor transactivation via recombinant dopamine D2 receptor is required for activation of extracellular signal-regulated kinases, i.e. ERKs
-
-
-
additional information
?
-
-
protein kinases and protein phosphatases regulate enzyme activities in the cell, regulation mechanisms, overview
-
-
-
additional information
?
-
-
receptor tyrosine kinases are key regulators of cellular homeostasis, regulation of enzyme signaling by protein tyrosine phosphatase-1B, defects in this regulation result in increased phosphorylation of epidermal growth factor receptor and platelet-derived growth factor which can be compensated by other signaling mechanisms, overview
-
-
-
additional information
?
-
-
the activated, tyrosine-phosphorylated Kit receptor is a docking site for signal transduction molecules containing SH2 domains, diverse proteins bind to the different tyrosine phosphates of the receptor, e.g. the adaptor protein APS, Src family kinases, Shp2 tyrosyl phosphatase, adaptor proteins Grb2 and Grb7, phosphatidylinositol 3-kinase, and the adaptor protein Shc, analysis of interactions, functions, and biological effects, binding of APS leads to Kit degradation, overview
-
-
-
additional information
?
-
-
the enzyme epidermal growth factor receptor tyrosine kinase is involved in signal transduction in cardiac preconditioning, mechanisms, enzyme inhibition is cardioprotective
-
-
-
additional information
?
-
-
the enzyme is regulated in balance with protein tyrosine phosphatase, complex regulation mechanism, overview, the enzyme has increasing effect, opposing to soluble protein kinase Src, on volume-sensitive chloride current in atrial myocytes
-
-
-
additional information
?
-
-
the enzyme is responsible for induction of calcium influx in corneal endothelial cells, FGF receptor tyrosine kinase activity is linked to L-type Ca2+ channel activity, overview
-
-
-
additional information
?
-
-
the insulin receptor tyrosine kinase performs insulin-induced autophosphorylation, regulatory dephosphorylation by protein tyrosine phosphatase PTP1B
-
-
-
additional information
?
-
-
the receptor protein tyrosine kinases are involved in cell signaling processes and signal transduction pathways in regulation of cell growth, differentiation, migration and metabolism by catalyzing protein phosphorylation and dephosphorylation, overview, EGFR tyrosine kinase regulates cell proliferation, IGFR tyrosine kinase regulates cell survival, VEGFR tyrosine kinase regulates tumor angiogenesis, mechanisms, overexpression of receptor protein tyrosine kinases in cancers
-
-
-
additional information
?
-
-
autophosphorylation of the insulin receptor via its protein tyrosine kinase activity, regulation mechanism
-
-
-
additional information
?
-
-
EGFR performs autophosphorylation
-
-
-
additional information
?
-
-
poor activity on free amino acids, consensus sequence of InRK is YM-MM, and of EGFR E-EEYF
-
-
-
additional information
?
-
-
serotonin 5-HT2c receptor signaling is largely independent from receptor tyrosine kinase activity
-
-
-
additional information
?
-
-
substrate recognition and binding structure, the enzyme depends on basic residues for substrate recognition, substrate specificity determinants in substrates
-
-
-
additional information
?
-
-
ErbB1 receptor shows three phosphorylation sites (Y1110, Y1172 and Y1192)
-
-
-
additional information
?
-
Avian erythroblastosis virus ES4
P00535
the erB oncogene efficiently transforms erythroblasts
-
-
-
additional information
?
-
Avian erythroblastosis virus ES4
-
N-terminal portion of the enzyme is sufficient for the transformation of fibroblasts, one-third of the carboxy-terminal domain has a key role for the transformation of erythroid cells, transformation of fibroblasts and transformation of erythroid cells
-
-
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
(Substrate)
LITERATURE
(Substrate)
COMMENTARY
(Product)
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
-
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
FLT-3 is involved in signal transduction, mechanisms
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
phosphorylation of downstream signalling proteins
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
regulation mechanisms and ligand binding, ligand binding induces a conformational change, overview
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
stem cell factor and Kit receptor are essential playing important roles in e.g. gametogenesis, hematopoiesis, mast cell development and function, and melanogenesis, complete absence is lethal, enzyme deficiencies lead to defects in white and red blood cell production, to hypopigmentation, and to sterility, Kit receptor signaling regulation by autophosphorylation and dephosphorylation via a phosphatase, regulation mechanism, overview
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
stem cell factor and Kit receptor are essential playing important roles in gametogenesis, hematopoiesis, mast cell development and function, and melanogenesis, complete absence is lethal, enzyme deficiencies lead to defects in white and red blood cell production, to hypopigmentation, and to sterility
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
stem cell factor and Kit receptor are essential playing important roles in gametogenesis, hematopoiesis, mast cell development and function, and melanogenesis, complete absence is lethal, enzyme deficiencies lead to defects in white and red blood cell production, to hypopigmentation, and to sterility, Kit receptor signaling regulation by autophosphorylation and dephosphorylation via a phosphatase
-
-
?
ATP + cortactin-L-tyrosine
ADP + cortactin-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 + p130Cas-L-tyrosine
ADP + p130Cas-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + paxillin-L-tyrosine
ADP + paxillin-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
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 + phospholipase C gamma-L-tyrosine
ADP + phospholipase C gamma-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + poly(Glu:Tyr)
ADP + poly(Glu:Tyr) phosphate
show the reaction diagram
-
-
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
show the reaction diagram
-
phospholipase C-gamma 1 is directly phosphorylated by TrkB
-
?
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
?
-
-
-
-
-
-
additional information
?
-
Q62799
-
-
-
-
additional information
?
-
P76387
enzyme is involved in signal transduction
-
-
-
additional information
?
-
-
possible involvement of the enzyme in cell recognition and bacterial pathogenicity
-
-
-
additional information
?
-
P58764
involved in exopolysaccharide production and virulence
-
-
-
additional information
?
-
-
phosphotyrosine-protein phosphatase Wzb is able to dephosphorylate previously autophosphorylated Wzc. Reversible protein phosphorylation on tyrosine may be part of the cascade of reactions that determine the pathogenicity of bacteria
-
-
-
additional information
?
-
-
phosphorylation of Wzc, as regulated by Wzb, is directly connected with the production of a particular capsular polysaccharide, colanic acid. Thus, when Wzc is phosphorylated on tyrosine, no colanic acid is synthesised by bacteria, but when dephosphorylated by Wzb, colanic acid is produced
-
-
-
additional information
?
-
-
enzyme is involved in the production of the extracellular polysaccharide colanic acid
-
-
-
additional information
?
-
Q91845
Sek-1, perhaps with other Eph-related receptors, is required for interactions that regulate the segmental identity or movement of cells
-
-
-
additional information
?
-
Q60805
tyrosine kinase may play an important function in the developing mouse
-
-
-
additional information
?
-
Q61772
important role in the formation of neuronal structures and possibly other morphogenic processes
-
-
-
additional information
?
-
-
important role in neurogenesis
-
-
-
additional information
?
-
-
the neurotrophic receptor may function during early stages of neural development
-
-
-
additional information
?
-
Q63474
may play an important role in the generation of the mammalian nervous system
-
-
-
additional information
?
-
-
Dnrk may play an important role in neural development during Drosophila embryogenesis
-
-
-
additional information
?
-
Q91694
Pag may play a role in the differentiation of cranial neural crest and other tissues
-
-
-
additional information
?
-
Q9wtl4
receptor may play a role in the regulation of beta-cell mass
-
-
-
additional information
?
-
-
role for DDR2 in critical events during wound repair
-
-
-
additional information
?
-
-
essential for migration of tracheal and specific midline glial cells
-
-
-
additional information
?
-
Q9z138
required for cartilage and growth plate development
-
-
-
additional information
?
-
-
receptor of neuregulin
-
-
-
additional information
?
-
Q91571
may play a role in the development or function of the central nervous system
-
-
-
additional information
?
-
Q90344
may play a role in cell-cell interactions involved in retinotectal projections and differentiation of the central nervous system
-
-
-
additional information
?
-
-
required for directed tracheal cell extension
-
-
-
additional information
?
-
-
part of a novel signal transduction cascade involved in learning and memory
-
-
-
additional information
?
-
-
involved in cell-cell interactions
-
-
-
additional information
?
-
-
mutations in MERTK, the human orthologue of the RCS rat retinal dystrophy gene, cause retinitis pigmentosa
-
-
-
additional information
?
-
-
receptor protein-tyrosine kinase involvement in key aspects of neuronal pathway recognition
-
-
-
additional information
?
-
-
essential for the pathfinding ability of expressing neurons, participates in a mechanism required for muscle attachment site selection
-
-
-
additional information
?
-
Q62799
expression of neuregulins and their putative receptor ErbB3, is induced during Wallerian degeneration
-
-
-
additional information
?
-
-
amplification of the c-erb-B-2 gene in a salivary adenocarcinoma and a gastric cancer cell line MKN-7 suggests that its over-expression is sometimes involved in the neoplastic process
-
-
-
additional information
?
-
-
transformation of fibroblasts and transformation of erythroid cells
-
-
-
additional information
?
-
P00535
the erB oncogene efficiently transforms erythroblasts
-
-
-
additional information
?
-
P08069
plays an important role in cell growth control
-
-
-
additional information
?
-
P07333, P10721
implicated in the control of cell growth and differentiation
-
-
-
additional information
?
-
-
enzyme functions as the cell surface receptor for the macrophage colony stimulating factor
-
-
-
additional information
?
-
-
cell-surface receptor for an as-yet-unknown ligand
-
-
-
additional information
?
-
-
missense mutations located in the MET proto-oncogene lead to constitutive activation of the MET protein and papillary renal carcinomas
-
-
-
additional information
?
-
-
the proto-oncogene c-kit is involved in signal transduction
-
-
-
additional information
?
-
P06494
receptor for an as yet unidentified growth factor
-
-
-
additional information
?
-
-
functions as a cell surface receptor for an as yet unidentified ligand
-
-
-
additional information
?
-
-
human ltk gene maps to chromosome 15, bands q13-21, a region containing the breakpoint of a recurring chromosomal abnormality in B-cell non-Hodgkin lymphomas
-
-
-
additional information
?
-
-
Elk tyrosine kinase may be involved in cell-cell interactions in the nervous system
-
-
-
additional information
?
-
-
piebaldism results from mutations of the KIT proto-oncogene, which encodes the cellular receptor transmembrane tyrosine kinase for mast/stem cell growth factor
-
-
-
additional information
?
-
-
human piebald trait resulting from a dominant negative mutant allele of the c-kit membrane receptor gene
-
-
-
additional information
?
-
-
Ltk is expressed at a very low level in only a few cell lines and tissues and may be the receptor for a pre-B lymphocyte growth or differentiation factor
-
-
-
additional information
?
-
P09208
activity of inr gene appears to be required in the embryonic epidermis and nervous system among others, since development of the cuticle, as well as the peripheral and central nervous systems are affected by inr mutations
-
-
-
additional information
?
-
-
mutations in the coding sequence of the proto-oncogene c-kit in a human mast cell leukemia cell line causing ligand-independent activation of c-kit product
-
-
-
additional information
?
-
-
mutations in the fibroblast growth factor receptor-1 gene, which maps to 8p, cause one form of familial Pfeiffer syndrome. A C to G transversion in exon 5, predicting a proline to arginine substitution in the putative extracellular domain, is identified in all affected members of five unrelated PS families but not in any unaffected individuals
-
-
-
additional information
?
-
-
determination of anterior and posterior terminal structures of Drosophila embryos requires activation of two genes encoding putative protein kinases, torso and D-raf
-
-
-
additional information
?
-
-
Jackson-Weiss syndrome and Crouzon syndrome are allelic with mutations in fibroblast growth factor receptor 2
-
-
-
additional information
?
-
P20806
enzyme is required for normal eye development
-
-
-
additional information
?
-
-
IR-related protein is a receptor for insulin, IGF-I, IGF-II, or an as yet unidentified peptide hormone or growth factor belonging to the insulin family
-
-
-
additional information
?
-
P14617
IR-related protein is a receptor for insulin, IGF-I, IGF-II, or an as yet unidentified peptide hormone or growth factor belonging to the insulin family
-
-
-
additional information
?
-
-
FGFR2 mutations in Pfeiffer syndrome
-
-
-
additional information
?
-
-
trkB may code for a cell surface receptor involved in neurogenesis
-
-
-
additional information
?
-
-
enzyme is involved in glial cell generation
-
-
-
additional information
?
-
-
sevenless gene determines the fate of a single photoreceptor cell type in the eye of Drosophila
-
-
-
additional information
?
-
P13388
malignant melanoma in Xiphophorus fish hybrids is caused by the activity of a dominant oncogene Tu which codes for a receptor tyrosine kinase
-
-
-
additional information
?
-
P21709
ephrin type-A receptor 1 may be involved in the neoplastic process of some tumors
-
-
-
additional information
?
-
-
high affinity receptor for both acidic and basic fibroblast growth factor but not for keratinocyte growth factor
-
-
-
additional information
?
-
-
FGFR-4 binds acidic fibroblast growth factor with high affinity but does not bind basic fibroblast growth factor
-
-
-
additional information
?
-
-
receptor tyrosine kinase is necessary for the induction of a vulva, survival past the L1 stage, hermaphrodite fertility and for male spicule development
-
-
-
additional information
?
-
P24786
gp145trkC may play an important role in mediating the neurotrophic effects of NT-3
-
-
-
additional information
?
-
P29376
tk gene product likely functions as a cell surface receptor for an unidentified cellular growth factor
-
-
-
additional information
?
-
P35916
receptors for at least two hematopoietic growth factors: the stem cell factor and the colony-stimulating factor 1
-
-
-
additional information
?
-
-
may play a role in vascular development and regulation of vascular permeability
-
-
-
additional information
?
-
-
gene plays important role in embryonic development and carcinogenesis of the stomach
-
-
-
additional information
?
-
-
Flk-1 as a major regulator of vasculogenesis and angiogenesis
-
-
-
additional information
?
-
-
may be involved in tumor progression of epithelial ovarian cancer
-
-
-
additional information
?
-
P34891, P34892
may be specifically involved in cell-cell interactions regulating cell fusions that generate the hypodermis during postembryonic development
-
-
-
additional information
?
-
P26618
possibility that overexpression of PDGF-alpha receptor in high-metastatic clones may contribute to an increase in the capacity of tumor cells to generate metastases in the lung
-
-
-
additional information
?
-
P35739
signal transducing receptor for nerve growth factor
-
-
-
additional information
?
-
P15127
increased ERBB3 expression may play a role in some human malignancies
-
-
-
additional information
?
-
P26619
ectodermally produced PDGF A may act on the mesoderm during gastrulation and mesoderm induction establishes the tissue pattern of ligand and receptor expression
-
-
-
additional information
?
-
P24348
receptor for the inductive signal required for vulval development
-
-
-
additional information
?
-
-
enzyme is a receptor for vascular endothelial cell growth factor
-
-
-
additional information
?
-
-
plays a part in human neurogenesis, DRT gene may play a part in neuroblastoma and SCLC tumorigenesis
-
-
-
additional information
?
-
P29318
may play an important role during development and in signal transduction pathways
-
-
-
additional information
?
-
P29319
may play an important role during development and in signal transduction pathways
-
-
-
additional information
?
-
-
acts through a conserved Ras/MAP kinase signaling pathway to induce vulval differentiation
-
-
-
additional information
?
-
-
element of the complex signaling network involved in the control of cell proliferation and differentiation
-
-
-
additional information
?
-
-
inhibition of vascular smooth muscle cell growth through antisense transcription of a rat insulin-like growth factor I receptor cDNA
-
-
-
additional information
?
-
P29320
may have a role in tumorigenesis
-
-
-
additional information
?
-
-
involved in the proliferation of early progenitor/stem cells
-
-
-
additional information
?
-
-
receptor may be a key signal transducing component in the totipotent hematopoietic stem cell and its immediate self-renewing progeny
-
-
-
additional information
?
-
-
possible role for repulsive B-class Eph receptor/ligand interactions in constraining the orientation of longitudinal axon projections at the ventral midline
-
-
-
additional information
?
-
-
tyro3 may function as a novel neurotrophic factor receptor
-
-
-
additional information
?
-
P54761
important role in gestational growth and differentiation
-
-
-
additional information
?
-
-
Srcasm may help promote Src family kinase signaling in cells
-
-
-
additional information
?
-
P97523
tyrosine kinase receptor for hepatocyte growth factor
-
-
-
additional information
?
-
-
increased c-met expression indicates that this gene may participate in the healing process of gastric mucosa after injury
-
-
-
additional information
?
-
-
enzyme is implicated in control of cell growth
-
-
-
additional information
?
-
-
NET potentially plays important roles in human neurogenesis
-
-
-
additional information
?
-
P97793
ALK plays an important role in the development of the brain
-
-
-
additional information
?
-
-
important role for this kinase in CD2 co-stimulation of T cell responses
-
-
-
additional information
?
-
Q04912
role for the Ron receptor in progression toward malignancy
-
-
-
additional information
?
-
-
primary function is likely to be in developmental regulation
-
-
-
additional information
?
-
-
distinct mutations in the receptor tyrosine kinase gene ROR2 cause brachydactyly type B
-
-
-
additional information
?
-
-
recessive Robinow syndrome, allelic to dominant brachydactyly type B, is caused by loss of ROR2 activity
-
-
-
additional information
?
-
-
Cek9 plays an active role in embryonic signal transduction pathways
-
-
-
additional information
?
-
-
role for Tsk in early T-lymphocyte differentiation
-
-
-
additional information
?
-
-
rat trkC locus encodes multiple neurogenic receptors that exhibit differential response to neurotrophin-3 in PC12 cells
-
-
-
additional information
?
-
-
dominant mutations in ROR2, encoding an orphan receptor tyrosine kinase, cause brachydactyly type B
-
-
-
additional information
?
-
-
the mouse waved-2 phenotype results from a point mutation in the EGF receptor tyrosine kinase
-
-
-
additional information
?
-
Q00993
ufo may function as a signal transducer between specific cell types of mesodermal origin
-
-
-
additional information
?
-
-
Cek8 suggests its involvement in cellular survival or cell-cell interactions for specific subpopulations of developing motoneurons
-
-
-
additional information
?
-
-
tek receptor tyrosine kinase may be critically involved in the determination and/or maintenance of cells of the endothelial lineage
-
-
-
additional information
?
-
-
itk functions in a signal transduction pathway unique to T lymphocytes
-
-
-
additional information
?
-
-
ron gene product is a specific cell-surface receptor for macrophage-stimulating protein
-
-
-
additional information
?
-
-
mutation of the gene encoding the ROR2 tyrosine kinase causes autosomal recessive Robinow syndrome
-
-
-
additional information
?
-
-
vascular dysmorphogenesis caused by an activating mutation in the receptor tyrosine kinase TIE2
-
-
-
additional information
?
-
-
Sky may be involved in cell adhesion processes, particularly in the central nervous system
-
-
-
additional information
?
-
-
expression of the EGF-R gene in mouse blastocysts is tightly regulated by maternal steroid hormonal status
-
-
-
additional information
?
-
-
Emt/Itk is a protein tyrosine kinase required for T cell Ag receptor TCR-induced activation and development
-
-
-
additional information
?
-
Q00495
mrfms gene products may play a role in the normal and neoplastic growth of muscular cells
-
-
-
additional information
?
-
-
activating mutations of the fibroblast growth factor receptor 3 cause skeletal dysplasias including achondroplasia, and the neonatal lethal syndromes thanatophoric dysplasia types I and II, the mutations are also involved in cancer development, e.g. in multiple myeloma, bladder carcinoma, and cervical cancer
-
-
-
additional information
?
-
-
activation of PDGF receptor growth factor results in increased intracellular Ca2+ flux and cytoplasmic pH changes, enzyme stimulates generation of reactive oxygen species, such as O2.- and H2O2, which function as mitogenic mediators of activated growth-factor-receptor signaling, overview, the EGFR signaling pathway functions in many cellular processes, including proliferation, cell migration, and apoptosis, signaling pathways, overview
-
-
-
additional information
?
-
-
activation of PDGF receptor growth factor results in increased intracellular Ca2+ flux and cytoplasmic pH changes, enzyme stimulates generation of reactive oxygen species, which function as mitogenic mediators of activated growth-factor-receptor signaling, overview, the EGFR signaling pathway functions in many cellular processes, including proliferation, cell migration, and apoptosis, signaling pathways, overview
-
-
-
additional information
?
-
-
antagonistic regulation of swelling-activated Cl- current in rabbit ventricle by Src and EGFR protein tyrosine kinases, overview
-
-
-
additional information
?
-
-
deoxycholic acid and taurodeoxycholic acid activate insulin receptor kinase and ERBB1 kinase and subsequent ERK1/2 and AKT signaling pathways activation via induction of reactive oxygen species ROS production in mitochondria, ROS activation can be blocked by scavengers N-acetyl cysteine and Trolox, as well as cyclosporine A and bongkrekic acid
-
-
-
additional information
?
-
-
downregulation of endogenous Syk non-receptor tyrosine protein kinase expression in mammary endothelial cells enhances the ligand-induced activity of the epidermal growth factor receptor, but not of closely related human epidermal growth factor receptors HER2 and HER3, EGFR has a regulatory feedback effect on Syk, enzyme deregulation is associated with pathophysiological disorders such as cancer, regulation in vivo overview
-
-
-
additional information
?
-
-
EGF-like peptides bind as ligands to the extracellular domain of host cell EGFR leading to an activation of the intracellular tyrosine kinase domain which initiates downstream signaling pathways, e.g. the mitogen-activated protein kinase cascade
-
-
-
additional information
?
-
-
EGF-like peptides on the surface of coccidial parasites Sarcocystis neurona, Neospora caninum, and Cryptosporidium parvum bind as ligands to the extracellular domain of the gerbils' host cells' EGFR leading to an activation of the intracellular tyrosine kinase domain which initiates downstream signaling pathways, e.g. the mitogen-activated protein kinase cascade
-
-
-
additional information
?
-
P00533
enzyme regulation via reversible autophosphorylation, binding to plasma membrane of enzyme and enzyme-derived peptides, overview
-
-
-
additional information
?
-
-
enzyme transactivation stimulates cell migration and the subsequent activation of downstream signaling pathways
-
-
-
additional information
?
-
-
ErbB family enzymes are absolutely required for viability of embryos
-
-
-
additional information
?
-
-
insulin receptor tyrosine kinase is activated via autophosphorylation, the receptor plays a role in signalling which is redox autoregulated by insulin-induced reactive oxygen species involving an autoregulatory loop, redundant mechanisms, overview, physiologic implications for diabetes and hyperglycemia
-
-
-
additional information
?
-
-
insulin- or H2O2-induced activation by autophosphorylation of the insulin receptor initiates the IR signaling pathway which includes phosphorylation of extracellular signal-regulated kinases 1 and 2, i.e. ERK1 and ERK2, protein kinase B, and glycogen synthase kinase 3-beta
-
-
-
additional information
?
-
-
mutations in the glycine-riche loop of MET can cause papillary renal-cell carcinomas
-
-
-
additional information
?
-
-
PDGFRbeta wild-type and mutant Y857F activate c-Src kinase
-
-
-
additional information
?
-
-
platelet-derived growth factor receptor or epidermal growth factor receptor transactivation via recombinant dopamine D2 receptor is required for activation of extracellular signal-regulated kinases, i.e. ERKs
-
-
-
additional information
?
-
-
protein kinases and protein phosphatases regulate enzyme activities in the cell, regulation mechanisms, overview
-
-
-
additional information
?
-
-
receptor tyrosine kinases are key regulators of cellular homeostasis, regulation of enzyme signaling by protein tyrosine phosphatase-1B, defects in this regulation result in increased phosphorylation of epidermal growth factor receptor and platelet-derived growth factor which can be compensated by other signaling mechanisms, overview
-
-
-
additional information
?
-
-
the activated, tyrosine-phosphorylated Kit receptor is a docking site for signal transduction molecules containing SH2 domains, diverse proteins bind to the different tyrosine phosphates of the receptor, e.g. the adaptor protein APS, Src family kinases, Shp2 tyrosyl phosphatase, adaptor proteins Grb2 and Grb7, phosphatidylinositol 3-kinase, and the adaptor protein Shc, analysis of interactions, functions, and biological effects, binding of APS leads to Kit degradation, overview
-
-
-
additional information
?
-
-
the enzyme epidermal growth factor receptor tyrosine kinase is involved in signal transduction in cardiac preconditioning, mechanisms, enzyme inhibition is cardioprotective
-
-
-
additional information
?
-
-
the enzyme is regulated in balance with protein tyrosine phosphatase, complex regulation mechanism, overview, the enzyme has increasing effect, opposing to soluble protein kinase Src, on volume-sensitive chloride current in atrial myocytes
-
-
-
additional information
?
-
-
the enzyme is responsible for induction of calcium influx in corneal endothelial cells, FGF receptor tyrosine kinase activity is linked to L-type Ca2+ channel activity, overview
-
-
-
additional information
?
-
-
the insulin receptor tyrosine kinase performs insulin-induced autophosphorylation, regulatory dephosphorylation by protein tyrosine phosphatase PTP1B
-
-
-
additional information
?
-
-
the receptor protein tyrosine kinases are involved in cell signaling processes and signal transduction pathways in regulation of cell growth, differentiation, migration and metabolism by catalyzing protein phosphorylation and dephosphorylation, overview, EGFR tyrosine kinase regulates cell proliferation, IGFR tyrosine kinase regulates cell survival, VEGFR tyrosine kinase regulates tumor angiogenesis, mechanisms, overexpression of receptor protein tyrosine kinases in cancers
-
-
-
additional information
?
-
Avian erythroblastosis virus ES4
P00535
the erB oncogene efficiently transforms erythroblasts
-
-
-
additional information
?
-
Avian erythroblastosis virus ES4
-
transformation of fibroblasts and transformation of erythroid cells
-
-
-
COFACTOR
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
ATP
-
dependent on; the binding site is a deep pocket lined by hydrophobic residues, enzyme affinity of Tie-2 for ATP is not influenced by phosphorylation of the activation loop
ATP
-
as MgATP2-, binding structure of ATP and product ADP
METALS and IONS
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
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
Ca2+
P00533
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
Cd2+
-
can partially substitue Mg2+
Co2+
-
can partially substitue Mg2+
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
Mg2+
-
-
Mg2+
-
; dependent on, Mg2+ is the physiologic metal ion, other divalent cations are able to support nucleotide binding, but only Mn2+, Co2+, and Cd2+ can substitute Mg2+ in supporting the catalytic activity
Mg2+
-
MgATP-
Mg2+
-
as MgATP2-
Mg2+
P10721
coordinates with Asp810 within the c-Kit DFG motif, overview
Mn2+
-
can partially substitue Mg2+
Zn2+
-
presence of Zn2+ at 0.1 mM rapidly activates isoform ALK. This activation is dependent of ALK tyrosine kinase activity and dimerization of the receptor but is independent of Src family kinase activity. Addition of sodium pyrithione, a zinc ionophore, leads to a further activation of ALK. This stronger activation is dependent of Src family kinase but independent of ALK activity and dimerization
INHIBITORS
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
(2R)-2-[(4-[[1-(1,3-thiazol-4-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
-
(2R)-2-[(4-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]-N,N-dimethylpropanamide
-
-
(2R)-2-[(4-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]-N-methylpropanamide
-
-
(2R)-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
-
(2R)-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
-
-
(R)-2-(2-[[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]methyl]pyrrolidin-1-yl)-2-oxoethanol
-
IC50: 97 nM; IC50: less than 2 nM
(R)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-1-methylethyl]-2-hydroxyacetamide
-
IC50: 3 nM; IC50: less than 2 nM
(R)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]propyl]-2-hydroxyacetamide
-
IC50: 2 nM; IC50: less than 2 nM
(S)-2-(2-[[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]methyl]pyrrolidin-1-yl)-2-oxoethanol
-
IC50: 2 nM; IC50: 327 nM
(S)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-1-methylethyl]-2-hydroxyacetamide
-
IC50: 19 nM; IC50: 2580 nM
(S)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]propyl]-2-hydroxyacetamide
-
IC50: 191 nM; IC50: 22 nM
(Z)-5-[6-[3-(4-methoxyphenyl)-ureido]-2-oxo-1,2-dihydroindol-3-ylidene-methyl]-4-methyl-1H-pyrrole-3-carboxylic acid
P16234
potent inhibitor against tyrosine kinases, including VEGFR and PDGFR families, as well as Aurora kinases
1-(4-(1H-pyrazol-1-yl)phenyl)-3-(2-aminoquinazolin-6-yl)-4-methylpyridin-2(1H)-one
-
-
1-(4-acetylphenyl)-3-(2-aminoquinazolin-6-yl)-4-methylpyridin-2(1H)-one
-
-
1-(4-aminophenyl)-3-[3-(1,3-benzodioxol-5-yl)-4-oxo-2,4-dihydroindeno[1,2-c]pyrazol-5-yl]urea
-
61% inhibition of EGFR; 88% inhibition of KDR
1-(4-aminophenyl)-3-[3-(3,4-dihydroxyphenyl)-4-oxo-2,4-dihydroindeno[1,2-c]pyrazol-5-yl]urea
-
50% inhibition of EGFR; 58% inhibition of KDR
1-(4-aminophenyl)-3-[3-(4-hydroxyphenyl)-4-oxo-2,4-dihydroindeno[1,2-c]pyrazol-5-yl]urea
-
65% inhibition of EGFR; 73% inhibition of KDR
1-(4-aminophenyl)-3-[3-(4-methoxyphenyl)-4-oxo-2,4-dihydroindeno[1,2-c]pyrazol-5-yl]urea
-
3% inhibition of EGFR; 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; 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; 70% inhibition of KDR
2,4,6-trihydroxydeoxybenzoin derivatives
-
diverse derivatives, analysis of inhibitory effect on parasite infection of host cells BM and HCT-8, IC50 values, overview
-
2,4,6-trihydroxydeoxybenzoin derivatives
-
diverse derivatives, analysis of inhibitory effect on EGFR tyrosine kinase activity, overview
-
2,4,6-trihydroxydeoxybenzoin derivatives
-
diverse derivatives, analysis of inhibitory effect on parasite infection of host cells BM and HCT-8, IC50 values, overview
-
2-[(2-cyanobenzyl)oxy]-N-(3-hydroxyphenyl)-4-[3-(pyrrolidin-1-yl)propoxy]benzamide
P08581
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
P00533
49% inhibition at 0.01 mM, antiproliferative activity on human breast cancer cell line MCF-7, IC50 value 0.00073 mM
2-[7-(4-[[4-(imidazo[1,2-a]pyridin-3-yl)pyrimidin-2-yl]amino]-3-methoxyphenyl)-9-oxa-3,7-diazabicyclo[3.3.1]non-3-yl]ethanol
-
compound shows good IGF-1R inhibitory activity in a cellular assay and a high free fraction in human plasma. However this compound shows a higher affinity for the hERG channel
3-(2-aminoquinazolin-6-yl)-1-(2-cyclopentylethyl)-4-methylpyridin-2(1H)-one
-
cyclopentylethyl
3-(2-aminoquinazolin-6-yl)-1-(3,3-dimethylindolin-6-yl)-4-methylpyridin-2(1H)-one
-
pyridone, nonselective inhibitor of c-Kit
3-(2-aminoquinazolin-6-yl)-1-(3-fluoro-4-methylphenyl)-4-methylpyridin-2(1H)-one
-
-
3-(2-aminoquinazolin-6-yl)-1-(3-methoxyphenyl)-4-methylpyridin-2(1H)-one
-
-
3-(2-aminoquinazolin-6-yl)-1-(4-chloro-3-fluorophenyl)-4-methylpyridin-2(1H)-one
-
-
3-(2-aminoquinazolin-6-yl)-1-(4-chlorophenyl)-4-methylpyridin-2(1H)-one
-
-
3-(2-aminoquinazolin-6-yl)-1-(4-fluoro-3-methylphenyl)-4-methylpyridin-2(1H)-one
-
-
3-(2-aminoquinazolin-6-yl)-1-(4-methoxyphenyl)-4-methylpyridin-2(1H)-one
-
-
3-(2-aminoquinazolin-6-yl)-1-(4-tert-butylphenyl)-4-methylpyridin-2(1H)-one
-
exhibits poor selectivity
3-(2-aminoquinazolin-6-yl)-4-methyl-1-(3-(trifluoromethyl)phenyl)pyridin-2(1H)-one
-
-
3-(2-aminoquinazolin-6-yl)-4-methyl-1-(3-(trifluoromethyl)phenyl)pyridin-2(1H)-one
P05532
-
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-bromo-5-t-butyl-4-hydroxy-benzylidenemalonitrile
-
-
3-[[5-([6-amino-5-[(E)-(methoxyimino)methyl]pyrimidin-4-yl]amino)-1H-indazol-1-yl]methyl]benzonitrile
-
;
4-(2',5'-dihydroxybenzylamino)phenylboronic acid
-
inhibition of EGFR tyrosine kinase
-
4-(3-chloroanilino)-6,7-dimethoxyquinazoline
-
-
4-(5-((2-methoxyethyl)carbamoyl)naphthalen-2-yloxy)-7-methoxyquinoline-6-carboxamide
-
-
4-(5-((4-chlorophenyl)carbamoyl)naphthalen-2-yloxy)-7-methoxyquinoline-6-carboxamide
-
-
4-(5-((4-chlorophenyl)carbamoyl)naphthalen-2-yloxy)-N-methylpicolinamide
-
-
4-(5-(cyclopropylcarbamoyl)naphthalen-2-yloxy)-7-methoxyquinoline-6-carboxamide
-
-
4-(5-bromoindole-3-yl)-6,7-dimethoxyquinazoline
-
relatively potent inhibitor of EGFR-TK activity
4-(5-carbamoylnaphthalen-2-yloxy)-7-methoxyquinoline-6-carboxamide
-
-
4-(5-chloro-6-fluoro-indole-3-yl)-6,7-di-(2-methoxyethoxy)quinazoline
-
relatively potent inhibitor of EGFR-TK activity
4-(5-chloro-6-fluoroindole-3-yl)-6,7-dimethoxyquinazoline
-
relatively potent inhibitor of EGFR-TK activity, is a dual EGFR-TK and HER-2-TK inhibitor
4-(5-chloro-6-fluoroindole-3-yl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazoline
-
relatively potent inhibitor of EGFR-TK activity, is a dual EGFR-TK and HER-2-TK inhibitor
4-(6-fluoro-5-methylindole-3-yl)-6,7-dimethoxyquinazoline
-
relatively potent inhibitor of EGFR-TK activity
4-(imidazo[1,2-a]pyridin-3-yl)-N-[2-methoxyphenyl-4-(4-piperidinyl)]pyrimidin-2-amine
-
-
4-(imidazo[2-methoxy-4-(9-oxa-3,7-diazabicyclo[3.3.1]non-3-yl)phenyl])pyrimidin-2-amine
-
-
4-(N-3-carboxyphenylaminomethyl)-2-phenylboronic acid
-
inhibition of EGFR tyrosine kinase
-
4-amino-1-tert-butyl-3-(1'-naphthyl)pyrazolo[3,4-d]pyrimidine
-
-
4-amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine
-
-
4-amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine
-
PP2, combination of 5-fluorouracil-PP2 decreases the 5-fluorouracil-induced activation of EGFR-AKT pathway
4-amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine
-
PP2, completely abrogates RON-mediated cell spreading both in the absence and presence of MSP
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
P00533
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
-
39% inhibition of ErbB-2 at 0.01 mM; 48% inhibition of EGFR at 0.002 mM
5,7-dihydroxyisoflavone derivatives
-
diverse derivatives, analysis of inhibitory effect on parasite infection of host cells BM and HCT-8, IC50 values, overview
-
5,7-dihydroxyisoflavone derivatives
-
diverse derivatives, analysis of inhibitory effect on EGFR tyrosine kinase activity, overview
-
5,7-dihydroxyisoflavone derivatives
-
diverse derivatives, analysis of inhibitory effect on parasite infection of host cells BM and HCT-8, IC50 values, 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
-
-
6,7-dimethyl-2-phenylquinoxaline
-
-
6-(1H-indol-5-ylmethyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
P09619
-
6-(1H-indol-5-ylmethyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
P09619
-
6-(3-bromobenzyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
P09619
-
6-(3-bromobenzyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
P09619
-
6-(6,7-dimethoxyquinazolin-4-yloxy)-1-naphthamide
-
-
6-(6,7-dimethoxyquinazolin-4-yloxy)-N-(2-methoxyethyl)-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide methanesulfonate
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(1-methylcyclopropyl)-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(2,2,2-trifluoroethyl)-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(2-fluorophenyl)-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(2-methoxyethyl)-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(3-(trifluoromethyl)phenyl)-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(3-fluorophenyl)-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(3-methoxypropyl)-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(3-methylisoxazol-5-yl)-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(4-(trifluoromethyl)phenyl)-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(4-fluorophenyl)-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(5-methylisoxazol-3-yl)-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(isoxazol-3-yl)-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(pyridin-2-yl)-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(pyridin-3-yl)-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(pyridin-4-yl)-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(thiazol-2-yl)-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-ethyl-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-isopropyl-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-methyl-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-p-tolyl-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-phenyl-1-naphthamide
-
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-propyl-1-naphthamide
-
-
6-(7-methoxyquinolin-4-yloxy)-1-naphthamide
-
-
6-(7H-pyrrolo[2,3-d]pyrimidin-4-yloxy)-N-(4-chlorophenyl)-1-naphthamide
-
-
6-[4-fluoro-3-(trifluoromethyl)benzyl]-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
P09619
-
6-[4-fluoro-3-(trifluoromethyl)benzyl]-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
P09619
-
AAL 993
-
30% inhibition of EGFR; 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
AEE788
-
50 mg/kg AEE788 inhibits the autophosphorylation of both epidermal growth factor receptor andvascular endothelial growth factor receptor
AG1296
-
FLT-3 inhibitor treatment results in formation of larger amounts of the mature 150 kDa form of mutant FLT-3 ITD
AG1296
-
selective inhibitor
AG1478
-
inhibition of epidermal growth factor receptor tyrosine kinase
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; specific tyrosine kinase inhibitor of EGFR. It decreases HER3 phosphorylation through the inhibition of EGFR/HER3 dimerization. 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; specific tyrosine kinase inhibitor of EGFR, whifh decreases EGFR phosphorylation through the inhibition of EGFR/HER3 dimerization
AG556
-
highly selective EGFR kinase inhibitor, 0.01 mM inhibits human ether-a-go-go-related gene channel current and the effect is significantly countered by the protein tyrosine phosphatase inhibitor orthovanadate (1 mM)
Antibody
-
monoclonal antibodies for inhibition of IGF-IR alter receptor trafficking by high affinity binding, promoting receptor degradation and consequently preventing human tumor growth in vivo
-
AZD2171
-
inhibits VEGFR2
CEP-7055
-
inhibits VEGFR1-3
CEP701
-
inhibits FLT3
cisplatin
-
anti-cancer drug inhibiting receptor tyrosine kinases
cycloheximide
-
depletes the synthetic pool of Met receptor
Doxorubicin
-
anti-cancer drug inhibiting receptor tyrosine kinases
Doxorubicin
-
-
dynamin K44A
-
reduces EGFR internalization to 40%
-
dynamin K44A
Q61006
inhibits agrin-induced MuSK endocytosis
-
ebselen
-
-
erlotinib
-
anti-cancer drug inhibiting receptor tyrosine kinases
erlotinib
-
-
erlotinib
-
;
ethyl 4-(3-(2-aminoquinazolin-6-yl)-4-methyl-2-oxopyridin-1(2H)-yl)benzoate
-
-
FPT III
-
inhibition of epidermal growth factor receptor tyrosine kinase
-
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
-
specific inhibition of EGFR-TK
gefitinib
-
-
geldanamycin
-
-
gemcitabine
-
anti-cancer drug inhibiting receptor tyrosine kinases
gemcitabine
-
-
genistein
-
protein tyrosine kinase inhibitor
genistein
-
broad spectrum PTK inhibitor
genistein
-
-
genistein
-
inhibition of epidermal growth factor receptor tyrosine kinase
genistein
-
broad-spectrum protein tyrosine kinase inhibitor, 0.03 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)
genistein
-
-
GM3
-
inhibitory effect on tyrosine phosphorylation of both mono- and dimeric EGFR
Herbimycin
-
-
herceptin
-
-
-
herceptin
-
combined therapy with herceptin and iressa exerts a greater suppression in EGFR activation; combined therapy with herceptin and iressa exerts a greater suppression in HER2 activation
-
hexachlorobenzene
-
increases after in vivo administration the total epidermal growth factor receptor content and decreases the plasma membrane epidermal growth factor receptor content compared to untreated rats, higher enzyme activity at low doses of 1 mg per kg body weight, reduced enzyme activity at higher doses of 100 mg hexachlorobenzene per kg body weight and above, chronic treatment induces a down-regulation of epidermal growth factor receptor and increases the EGFR-tyrosine kinase activity in the microsomal fraction
HgCl2
-
0.2 mM, 51% inhibition
humanized monoclonal antibody
-
blocks the interaction of Ron with hepatocyte growth factor-like protein and diminishes Ron phosphorylation and its downstream signaling
-
humanized monoclonal antibody
-
significantly decreases tumor growth of murine xenografts from subcutaneously injected lung, colon, and pancreatic cancer cell lines in nude mice
-
hydrogen peroxide
-
limited exposure enhances insulin-induced autophosphorylation of the insulin receptor, while prolonged exposure impairs the action of insulin
imatinib
-
inhibits c-Kit receptor and PDGF receptor tyrosine kinases
imatinib
-
IC50: 30 nM
imatinib
-
inhibits c-Kit and PDGFR
imatinib
-
potently inhibits the tyrosine kinase activities of PDGFR and c-kit. Short postnatal imatinib exposure significantly reduces the litter size sired by the treated animals and leads to permanently slightly elevated serum levels of the gonadotropins. Testicular morphology and mRNA levels of ligands and receptors involved in stem cell factor/c-kit and PDGF signaling return to control levels, and the offsprings are born healthy
imatinib mesylate
-
potent inhibitor
Iressa
-
gefitinib, specific tyrosine kinase inhibitor of EGFR. Decreases HER3 phosphorylation through the inhibition of EGFR/HER3 dimerization. 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; 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; 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
K-252a
-
complete inhibition at 200 nM
KN93
-
inhibition of epidermal growth factor receptor tyrosine kinase
lavendustin A
-
-
lestaurinib
P36888
-
-
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
-
dietary flavonoid, transinactivation of epidermal growth factor receptor tyrosine kinase and blocking of downstream signaling pathways activation, and cell migration in MiaPaCa-2 cells
luteolin
P36888
luteolin is a potent receptor-type tyrosine-protein kinase FLT3 inhibitor. Luteolin suppresses cell proliferation in MV4,11 cells with constitutively activated FLT3
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
mithramycin
-
inhibits binding of Sp factors to GC-rich sites, dramatically reduces Axl promoter activity and Axl, Sp1 and Sp3 expression
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-(2,4-dichlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
-
N-(2-hydroxyethyl)-N-methyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]acetamide
-
-
N-(2-methoxyethyl)-6-(7-methoxyquinolin-4-yloxy)-1-naphthamide
-
-
N-(3,5-dichlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
-
N-(3-chlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
-
N-(4-chloro-3-(trifluoromethyl)phenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
-
N-(4-chlorophenyl)-3-(6,7-dimethoxyquinolin-4-yloxy)isoquinoline-8-carboxamide
-
-
N-(4-chlorophenyl)-6-((6,7-dimethoxyquinolin-4-yl)(methyl)amino)-1-naphthamide
-
-
N-(4-chlorophenyl)-6-(2-(methylamino)pyridin-4-yloxy)-1-naphthamide
-
-
N-(4-chlorophenyl)-6-(2-(methylamino)pyrimidin-4-yloxy)-1-naphthamide
-
-
N-(4-chlorophenyl)-6-(3-fluoro-6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
-
N-(4-chlorophenyl)-6-(6,7-dimethoxyquinazolin-4-yloxy)-1-naphthamide
-
-
N-(4-chlorophenyl)-6-(6,7-dimethoxyquinolin-4-ylamino)-1-naphthamide
-
-
N-(4-chlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
has significant antitumor efficacy against established HT29 human colon adenocarcinoma xenografts implanted in athymic mice
N-(4-chlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
P35918
dose dependent inhibition of Flk-1 phosphorylation
N-(4-chlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
O08775
shows in vivo inhibition of corneal angiogenesis
N-(4-chlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-5-fluoro-1-naphthamide
-
-
N-(4-chlorophenyl)-6-(6-(methylamino)pyrimidin-4-yloxy)-1-naphthamide
-
-
N-(4-chlorophenyl)-6-(7-methoxyquinolin-4-yloxy)-1-naphthamide
-
-
N-(4-chlorophenyl)-6-(pyridin-4-yloxy)-1-naphthamide
-
-
N-(4-chlorophenyl)-6-(pyrimidin-4-yloxy)-1-naphthamide
-
-
N-(4-chlorophenyl)-6-(quinolin-4-yloxy)-1-naphthamide
-
-
N-(4-chlorophenyl)-7-(6,7-dimethoxyquinolin-4-yloxy)quinoline-4-carboxamide
-
-
N-(4-tert-butylphenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
-
N-(5-tert-butylisoxazol-3-yl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
-
N-(cyclopropylmethyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
-
N-cyclobutyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
-
N-cyclopentyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
-
N-cyclopropyl-6-(6,7-dimethoxyquinazolin-4-yloxy)-1-naphthamide
-
-
N-cyclopropyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
-
N-cyclopropyl-6-(7-methoxyquinolin-4-yloxy)-1-naphthamide
-
-
N-ethyl-5-[2-[4-(5-(ethylamino)-1,3,4-thiadiazol-2-yl)phenylamino]-phenyl]-1,3,4-thiadiazol-2-amine
P00533
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-[1-(3-fluorobenzyl)-1H-indazol-5-yl]-5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine
-
-
N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]ethyl]-2-hydroxyacetamide
-
IC50: 35 nM, potent, orally active inhibitor when co-administered with the cytochrome P450 inhibitor 1-aminobenzotriazole; IC50: 4 nM, potent, orally active inhibitor when co-administered with the cytochrome P450 inhibitor 1-aminobenzotriazole
N-[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]-5-(2-morpholin-4-yl-2-oxoethoxy)quinazolin-4-amine
-
-
N-[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]-5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine
-
-
N-[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]-5-[2-(4-methylpiperazin-1-yl)-2-oxoethoxy]quinazolin-4-amine
-
-
N-[3-chloro-4-[(6-methylpyridin-3-yl)oxy]phenyl]-5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine
-
-
N-[3-methoxy-4-[(6-methylpyridin-3-yl)oxy]phenyl]-5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine
-
-
N-[3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]-5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine
-
-
N-[3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]-5-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine
-
-
N3-(6-aminopyridin-3-yl)-N1-(2-cyclopentylethyl)-4-methylisophthalamide
-
bisamide
N4-(2-fluoro-4-chlorophenyl)-6-(2,5-dimethoxybenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
-
shows potent inhibition of VEGFR-2 over EGFR, platelet-derived growth factor receptor-beta and VEGFR-1; 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; 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; 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; 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; 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; 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; 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; potent, multiple receptor tyrosine kinase inhibitor
N6-Dimethylaminopurine
-
unspecific inhibitor of protein kinases
NVP-BBT594
-
-
OSI-774
-
i.e. erlotinib, inhibits EGF receptor protein tyrosine kinase, binding to EGF receptor kinase, structure overview, anticancer drug
pazopanib
-
i.e. 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulphonamide, potent inhibitor of vascular endothelial growth factor receotors 1, 2, and 3, platelet-derived growth factor receptor alpha, platelet-derived growth factor receptor beta, and KIT
PD-153035
-
synthetic inhibitor, highly specific for the epidermal growth factor receptor
PD-153035
-
highly specific and potent inhibition of EGFR kinase
PD153035
-
specific inhibition of EGFR-TK, IC50 is 0.00329 mM with 1 U of purified EGFR-TK from A431 cells
PD153035
Q61526
inhibits tyrosine kinase activity of EGFR and whereby blocks cellular responses of activated ErbB3. It inhibits heregulin-induced VEGFA expression; inhibits tyrosine kinase activity of EGFR and whereby blocks cellular responses of activated ErbB3. It inhibits heregulin-induced VEGFA expression
PD168393
-
complete inhibition at 0.01 mM
PF-2341066
-
IC50: 0.002 mM
PHA-665752
-
IC50: 0.0009 mM
phosphotyrosyl phosphatase Shp1
-
Shp1 binds to c-Kit at Y570 and acts by dephosphorylating the receptor directly, or inhibits c-Kit signalling indirectly by dephosphorylating other receptor-associated protein-tyrosine kinases
-
PKC412
-
inhibits FLT3
PKI-166
-
0.5 mM/kg body weight
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
-
protein tyrosine phosphatase 1B
-
PTP1B, negative regulator of Met. Loss of protein tyrosine phosphatase 1B enhances heregulin-mediated phosphorylation of Met. Interaction with Met requires phosphorylation of twin tyrosines (Y1234/35) in the activation loop of the Met kinase domain
-
quercetin
-
dietary flavonoid, transinactivation of epidermal growth factor receptor tyrosine kinase and blocking of downstream signaling pathways activation, and cell migration in MiaPaCa-2 cells
quercetin
P36888
-
Rapamycin
-
IC50: 3 nM
RM-6427
-
inhibits parasite infection of host cells BM and HCT-8
-
RM-6428
-
inhibits parasite infection of host cells BM and HCT-8
-
rottlerin
-
specific inhibitor of PKCdelta
shRNA
Q61526
sh-ErbB3 cells normally metastasize to the lung, but the heregulin-induced increase in metastasis is completely abrogated. Inactivation of ErbB3 by shRNA does not directly influence the formation of metastatic colonies in the experimental metastasis model, although heregulin-induced enhancement is completely dependent on ErbB3. However, spontaneous metastasis by inoculating the cells without heregulin stimulation into the foot pad is significantly decreased
-
siRNA
-
significantly reduces cancer cell proliferation, motility, and increases apoptotic susceptibility of colorectal carcinoma cells
-
siRNA
-
use of Sp1/Sp3 siRNAs significantly reducs Axl promoter activity and protein levels in Rko and HeLa cells
-
siRNA
-
-
-
siRNA
Q61526
local injection of siRNA against ErbB3 with the atolocollagen results in a decrease in the tumor growth of parent B16-BL6 cells
-
siRNA
-
suppressed expression of Ror2, which results in impaired microtubule-organizing center reorientation following Wnt5a stimulation
-
siRNA
-
knocks down Ror2 expression, results in a drastic inhibition of Wnt5a CM- or purified Wnt5a-induced wound closure and no lamellipodia formation following Wnt5a stimulation. Wnt5a-induced microtubule-organizing center reorientation is also impaired in Ror2-depleted cells
-
siRNA
-
siRNA directed against Tie1 suppresses expression of the receptor by more than 90%. Ang1 inhibition of permeability is not affected by suppression of Tie1 expression. Ability of Ang1 to inhibit induction of apoptosis in response to serum deprivation is not diminished by suppression of Tie1 expression; siRNA directed against Tie2 suppresses expression of the receptor by more than 90%. Ang1 inhibits endothelial monolayer permeability, which is prevented by suppression of Tie2 expression. Ability of Ang1 to inhibit induction of apoptosis in response to serum deprivation is completely blocked by suppression of Tie2 expression
-
siRNA
-
blocks VEGF secretion by melanoma tumors
-
sorafenib
-
oral multikinase inhibitor, inhibits receptor tyrosine kinase autophosphorylation, implicated in tumorigenesis and tumor progression
sorafenib
-
oral multikinase inhibitor, inhibits receptor tyrosine kinase autophosphorylation
sorafenib
-
-
staurosporine
-
unspecific inhibitor of protein kinases
STI-571
-
specific protein-tyrosine kinase inhibitor binds to an inactive Kit receptor form, utilized in tumor treatment, binding structure
STI-571
P10721
-
STI571
-
commercial Gleevec/Glivec, specific inhibitor
SU 11248
-
inhibits VEGFR2
SU 6668
-
inhibits VEGFR2 and PDGF receptor beta
SU11248
-
FLT-3 inhibitor treatment results in formation of larger amounts of the mature 150 kDa form of mutant FLT-3 ITD
SU11248
-
inhibits FLT3
SU5416
-
selective inhibitor
sunitinib
-
VEGFR tyrosine kinase inhibitor
sunitinib
-
-
sunitinib
-
effects of Src kinase inhibitor saracatinib and multiple receptor tyrosine kinase inhibitor sunitinib on renal cell carcinoma cell line ACHN and Caki-1. Saracatinib alone or in combination with sunitinib inhibits the migration of ACHN and Caki-1 cells in vitro. Combined treatment results in improved growth inhibition, greater loss of the S phase cell population and decreased clonogenic colony formation compared to sunitinib alone in the metastatic Caki-1 line. Saracatinib alone and in combination with sunitinib inhibits phosphorylation of the cell progression regulator c-Myc in a dose-dependent manner. Sunitinib alone or in combination suppresses cyclin-D1 expression with the combination showing greater dose-dependent effect. Sunitinib inhibits vascular endothelial growth factor secretion through the inhibition of STAT3 signaling and VEGF biosynthesis. HIF1-alpha expression in normoxic and hypoxic conditions in Caki-1 cells is inhibited by either saracatinib or sunitinib when administered alone, however, a greater reduction occurrs when these compounds are given in combination. Targeting Src kinase and RTK simultaneously with saracatinib and sunitinib results in 70-80% blockade of renal cell carcinoma cell migration, synergistic inhibition of cell growth and reduction of acquired drug resistance in Caki-1 cells
T-cell phosphatase
-
TCPTP, requirement for Y1234 and Y1235 in the Met receptor activation loop for interaction with TCPTP
-
Tarceva
-
38% inhibition of KDR; 81% inhibition of EGFR
trichostatin A
-
the ability of RON to inhibit HIV-1 transcription is sensitive to a histone deacetylase inhibitor
tyrphostin 51
-
-
tyrphostin A9
-
PDGF receptor-specific
tyrphostin AG 1478
-
inhibition of EGF receptor
tyrphostin AG 370
-
PDGF receptor-specific
-
tyrphostin AG1478
-
EGFR-specific antagonist
tyrphostin B56
-
i.e. AG 556, selective EGFR and ErbB-1 kinase inhibitor, reduces volume-sensitive chloride current in atrial myocytes, is antagonized by pretreatment with VO43-
U0126
-
MEK/ERK inhibitor, has no effects on RON-mediated cell spreading either with or without MSP, but completely abrogates the cell survival properties of RON and reduces MSP-induced Transwell migration by 60-80%
vanadate
-
-
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
ZD1839
-
selective inhibitor
ZD6474
-
inhibits VEGFR2
MLN518
-
inhibits FLT3
additional information
-
no inhibition by daidzein
-
additional information
-
no inhibition by genistein
-
additional information
-
inhibitory role for the KIT juxtamembrane region in controlling the receptor kinase activity
-
additional information
-
inhibitors based on an oxindole core, indolinones. Oxindole occupies the site in which theATP binds, whereas the moieties that extend from the oxindole contact residues in the hinge region between the two kinase lobes. The more specific inhibitor of FGFR1 induces a conformational change in the nucleotide-binding loop
-
additional information
-
autoregulation by a pseudosubstrate mechanism, overview
-
additional information
-
proto-oncogene Cbl binds to Kit and is activated by parallel binding of adaptor protein APS leading to inactivation and degradation of the Kit receptor
-
additional information
-
enzyme inhibition by the juxtamembrane domain in cis by maintaining the control alphaC-helix and the activation loop in their active conformations, the juxtamembrane also inhibits receptor dimerization
-
additional information
-
inhibition of the insulin receptor tyrosine kinase and insulin action by dephosphorylation at Tyr1150 and Tyr1151 via protein tyrosine phosphatase 1B
-
additional information
-
inhibition of the insulin receptor tyrosine kinase and insulin action by dephosphorylation
-
additional information
-
inhibitory potency of diverse aminoboronic acids, e.g. no inhibition of EGFR tyrosine kinase by 3-(2,5-dihydroxybenzylamino)phenylboronic acid, overview
-
additional information
-
clinical effects of enzyme inhibitors as anti-cancer drugs, overview, inhibitory antibodies, overview
-
additional information
-
enzyme inhibition leads to a reduction of capacitative calcium entry CCE in SV-40 transfected endothelial cells
-
additional information
P10721
enzyme performs autoinhibition via its juxtamembrane domain, structure and mechanism, overview
-
additional information
P00533
autoinhibition mechanism based on a structural model including the 2 juxtamembranes and the protein tyrosine kinase domain binding electrostatically to acidic lipids in the plasma membrane restricting access to the substrate tyrosines, reversible by ligand-binding induced dimerization and subsequent transautophosphorylation and Ca2+/calmodulin induced net charge changes in the juxtamembranes
-
additional information
Q60805
soluble anti-scavenger receptor A substantially inhibits apoptotic cell-induced phosphorylation of Mertk and of phospholipase Cgamma2, essential steps in apoptotic cell ingestion. Relative to macrophage tissue of wild-type mice, apoptotic cell-induced Mertk phosphorylation is reduced and delayed in macrophage tissue of SR-A-/- mice, as is in vitro apoptotic cell ingestion at early time-points
-
additional information
-
blocking internalization of the IGF-IR results in an attenuation of ERK activation, with no affect on the activation of the PI-3K/Akt pathway
-
additional information
-
blocking internalization of the EGFR expressed in HeLa cells decreases ERK activity but also increases protein kinase C activity
-
additional information
Q61006
suppression of N-ethylmaleimide sensitive factor expression or N-ethylmaleimide sensitive factor mutation attenuate MuSK downstream signaling
-
additional information
-
selective elimination of unmyelinated C-fibers by neonatal capsaicin treatment results in marked reduction of the c-kit receptor and calcitonin gene-related peptide expression in the superficial layer of the spinal cord. C-kit receptor expression is significantly down-regulated in medium-sized dorsal root ganglia neurons after nerve injury
-
additional information
-
loading of fluoresceinated-C43 (fluorescein isothiocyanate (FITC)-C43) into MCF-7 cells significantly reduces insulin-like growth factor-1 receptor/phosphoinositide-dependent kinase-1 interaction
-
additional information
-
VEGFR-2 may be a responsible target of LYG-202 leading to interruption of VEGF-stimulated signal transduction
-
additional information
P09619
the inclusion of a 2-amino group in pyrrolo[2,3-d]pyrimidines improves multiple receptor tyrosine kinase inhibition and antiangiogenic activity. The 2-amino analogs are better against epidermal growth factor receptor EGFR and platelet derived growth factor PDGFR-beta in whole cell inhibition assays and in the A-431 cytotoxicity assay compared to the 2-deamino analogs. The 2-deamino analogs are more potent inhibitors against vascular endothelial growth factor VEGFR-2 than the corresponding 2-amino compounds; the inclusion of a 2-amino group in pyrrolo[2,3-d]pyrimidines improves multiple receptor tyrosine kinase inhibition and antiangiogenic activity. The 2-amino analogs are better against epidermal growth factor receptor EGFR and platelet derived growth factor PDGFR-beta in whole cell inhibition assays and in the A-431 cytotoxicity assay compared to the 2-deamino analogs. The 2-deamino analogs are more potent inhibitors against vascular endothelial growth factor VEGFR-2 than the corresponding 2-amino compounds; the inclusion of a 2-amino group in pyrrolo[2,3-d]pyrimidines improves multiple receptor tyrosine kinase inhibition and antiangiogenic activity. The 2-amino analogs are better against epidermal growth factor receptor EGFR and platelet derived growth factor PDGFR-beta in whole cell inhibition assays and in the A-431 cytotoxicity assay compared to the 2-deamino analogs. The 2-deamino analogs are more potent inhibitors against vascular endothelial growth factor VEGFR-2 than the corresponding 2-amino compounds; the inclusion of a 2-amino group in pyrrolo[2,3-d]pyrimidines improves multiple receptor tyrosine kinase inhibition and antiangiogenic activity. The 2-amino analogs are better against epidermal growth factor receptor EGFR and platelet derived growth factor PDGFR-beta in whole cell inhibition assays and in the A-431 cytotoxicity assay compared to the 2-deamino analogs. The 2-deamino analogs are more potent inhibitors against vascular endothelial growth factor VEGFR-2 than the corresponding 2-amino compounds
-
additional information
P08069
identification of inhibitors by translation of structure-efficiency relationships of the substrates into structure-activity relationships of the inhibitors upon replacement of the phosphorylation warhead by an inactive mimetic
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
(B1-Thr)ILP
O02466
autophosphorylation of the expressed ILP receptor is half-maximally stimulated by a synthetic ILP analog, (B1-Thr)ILP, at a concentration of about 0.0005 mM
-
12-O-tetradecanoylphorbol-13-acetate
-
upregulates Ron protein expression
5-aza-2'-deoxycytidine
-
demethylation by 5-aza-2'-deoxycytidine upregulates Axl and Sp3 expression in low-Axl-expressing Colo206f/WiDr cells, but not in high-Axl-expressing Rko cells
5-Fluorouracil
-
-
AG1478
-
increases HER2 phosphorylation in the presence of heregulin. Phosphorylation of HER2 is greater by heregulin beta and heregulin beta-1 in the presence of AG 1478
agrin
Q61006
MuSK becomes rapidly internalized in response to agrin, which appears to be required for induced acetylcholine receptor clustering
-
angiopoietin-1
-
-
-
angiopoietin-1
-
activates; activates
-
angiotensin II
-
induces transactivation of epidermal growth factor receptor, mechanism
angiotensin II
-
-
betacellulin
-
activates
-
betacellulin
-
activates HER3 and HER4 via HER2; activates HER3 via HER2
-
brain-derived neurotrophic factor
-
activates TrkB
-
Calmodulin
P00533
ligand-binding induced dimerization enables transautophosphorylation of ErbB1 which results in enhanced intracellular Ca2+ concentration activating calmodulin which reverses autoinhibition by net charge changes in the juxtamembranes
capsaicin
-
c-kit receptor expression is significantly up-regulated in medium-sized dorsal root ganglia neurons after neonatal capsaicin treatment
chicken macrophage stimulating-protein
-
MSP, activates
-
cisplatin
-
AXL can be induced by chemotherapy drugs in acute myeloid leukemia U937 cells and this induction is dependent on the CCWGG methylation status of the AXL promoter
clathrin
-
EGFR is internalized classicaly through clathrin-dependent endocytosis
-
Collagen
-
250 kDa dimeric DDR1a entity is phosphorylated upon ligand stimulation
dibutyryl cAMP
-
tyrosine phosphorylation of insulin receptor substrate-2 by insulin-like growth factor IGF-I receptor is increased when insulin receptor substrate-2 is contained in high-molecular-mass complexes prepared from FRTL-5 thyrocytes treated with dibutyryl cAMP. Cytokine/hormone-induced formation of high-molecular mass complexes modulates availability of insulin receptor substrates to receptor tyrosine kinases
Dok-7
-
a cytoplasmic post-synaptic protein coactivator of the muscle-specific receptor-tyrosine kinase MuSK
-
Doxorubicin
-
AXL can be induced by chemotherapy drugs in acute myeloid leukemia U937 cells and this induction is dependent on the CCWGG methylation status of the AXL promoter
Epidermal growth factor
-
activates the tyrosine kinase activity of the epidermal growth factor receptor promoting cell growth
Epidermal growth factor
-
EGFR dimer is formed by activation
Epidermal growth factor
-
high-doses stimulate ubiquitination and endocytosis of EGFR through caveolae in HeLa cells
Epidermal growth factor
-
induces phosphorylation; induces phosphorylation; induces phosphorylation
Estrogen
-
induces Ret expression
fibroblast growth factor
-
activation occurs by phosphorylation on residues 653 and 654
-
Gas6
-
in U937 cells ectopically overexpressing AXL, addition of exogenous Gas6 induces AXL phosphorylation and activation of the Akt and ERK1/2 survival pathways. The Gas6-AXL activation pathway of drug resistance is associated with increased expression of Bcl-2 and Twist
-
glial-derived neutrophic factor
-
triggers signaling pathway activation in breast tumor cell lines in a Ret-dependent manner. 10 ng/mL glial-derived neutrophic factor alone or in combination with 100ng/mL glial-derived neutrophic factor receptor alpha1 is the optimal concentration promoting activation of downstream signaling in breast cancer cell lines
-
heparin-binding EGF-like growth factor
-
activates
-
hepatocyte growth factor
-
-
-
hepatocyte growth factor
Q2IBA6
activation of c-MET occurs in response to binding the physiological ligand hepatocyte growth factor
-
hepatocyte growth factor-like protein
-
stimulates
-
heregulin
Q61526
induces phosphorylation of ErbB3 and metastatic properties including MMP-9 expression, invasion, adhesion and experimental lung metastasis in vivo; rapidly induces phosphorylation of EGFR
-
heregulin
-
loss of tyrosine phosphorylation of the receptor is detectable as early as 15 min post-chase, whereas Met itself is stable, demonstrating that under these conditions Met is significantly dephosphorylated prior to degradation
-
heregulin
-
ligand for the Met receptor
-
heregulin
-
activates HER3 and HER4 via HER2; activates HER3 via HER2
-
hexachlorobenzene
-
increases after in vivo administration the total epidermal growth factor receptor content and decreases the plasma membrane epidermal growth factor receptor content compared to untreated rats, higher enzyme activity at low doses, reduced enzyme activity at higher doses of hexachlorobenzene
hydrogen peroxide
-
activates the autophosphorylation and protein tyrosine phosphorylation activities of the insulin receptor, and thus the insulin receptor signaling pathway, overview
hydrogen peroxide
-
limited exposure enhances insulin-induced autophosphorylation of the insulin receptor, while prolonged exposure impairs the action of insulin, acts by direct oxidation of the receptor tyrosine kinase or indirectly by oxidation of protein tyrosine phosphatase
hydrogen peroxide
-
-
hydrogen peroxide
-
-
IGF-I
O02466
stimulates autophosphorylation of the ILP receptor
-
Insulin
-
induces receptor activation by autophosphorylation
-
Insulin
-
activates enzyme tyrosine autophosphorylation
-
internalin B
Q2IBA6
activation of c-MET occurs in response to binding the internalin B protein of Listeria monocytogenes
-
Iressa
-
acute treatment with 0.001 mM iressa induces a significant increase in HER2 phosphorylation
macrophage stimulating protein
-
MSP, its only known ligand, both MSP-dependent and MSP-independent signaling by RON. RON exhibits MSP-independent tyrosine phosphorylation in MCF-10A cells. RON exhibits increased phosphorylation on Y1238/1239 and on the Y1360 docking site in the presence of exogenously added MSP. Similar levels of RON expression in NIH-3T3 cells do not lead to tyrosine phosphorylation of RON in the absence of ligand. MSP-independent tyrosine phosphorylation of RON also in HeLa cells
-
macrophage-stimulating protein
Q62190
the ligand for RON, inhibits IFN-gamma-induced STAT1 phosphorylation and CIITA expression, resulting in reduced surface levels of MHC class II
-
metformin
-
i.e. N,N-dimethylbiguanide or N,N-dimethylimidodicarbonimidic diamide, activates the insulin receptor tyrosine kinase by phosphorylation at Tyr1150 and Tyr1151, and indirectly via inhibition of protein tyrosine phosphatase 1B, metformin does not alter the order of substrate phosphorylation by the insulin receptor tyrosine kinase
N-ethylmaleimide sensitive factor
Q61006
an appropriate level of N-ethylmaleimide sensitive factor and its ATPase activity may be required for MuSK endocytosis and subsequent activation
-
nerve growth factor
-
activates TrkA, which leads to differentiation of neurons and neurobalstoma cells, whereas it induces proliferation of fibroblasts and apoptosis of medulloblastoma cells
-
neuregulins
-
activates
-
neurotrophin 3
-
activates TrkC
-
neurotrophin 4
-
activates TrkB
-
neurotrophin-3
-
activates
-
PMA/ionomycin
-
chronic lymphocytic leukemia cells and normal tonsil B cells, which constitutively express Ror1 mRNA, can not be further activated. In contrast, a 15 to 25fold increase in the ROR1 mRNA expression was observed in in vitro activated normal B and T cells
-
PorB
-
PorB from Neisseria meningitidis is able to induce protein tyrosine kinase activity
-
reactive oxygen species
-
deoxycholic acid and taurodeoxycholic acid activate insulin receptor kinase and ERBB1 kinase and subsequent signaling pathway activation via induction of reactive oxygen species ROS production in mitochondria, ROS activation can be blocked by scavengers N-acetyl cysteine and Trolox, as well as cyclosporine A and bongkrekic acid
-
reactive oxygen species
-
-
-
stem cell factor
-
soluble and membrane-bound glycoprotein, activating ligand of the stem cell receptor i.e. the Kit protein-tyrosine kinase
-
stem cell factor
-
soluble and membrane-bound glycoprotein, activating ligand of the stem cell receptor i.e. the Kit protein-tyrosine kinase, stem cell factor ligand binding induces receptor dimerization and tyrosine kinase activation
-
thiol/disulfide
-
regulation of insulin receptor tyrosine kinase activity by shifts in the redox status
-
tumor necrosis factor-alpha
-
tyrosine phosphorylation of insulin receptor substrate-1 by insulin receptor is decreased when insulin receptor substrate-1 is contained in high-molecular mass complexes prepared from 3T3-L1 adipocytes treated with tumor necrosis factor-alpha.Cytokine/hormone-induced formation of high-molecular mass complexes modulates availability of insulin receptor substrates to receptor tyrosine kinases
-
VP16
-
AXL can be induced by chemotherapy drugs in acute myeloid leukemia U937 cells and this induction is dependent on the CCWGG methylation status of the AXL promoter
metformin
-
i.e. N,N-dimethylbiguanide or N,N-dimethylimidodicarbonimidic diamide, activates the insulin receptor tyrosine kinase by phosphorylation, and indirectly via inhibition of protein tyrosine phosphatase, metformin does not alter the order of substrate phosphorylation by the insulin receptor tyrosine kinase
additional information
O09127
the Eek receptor can be activated by at least three different GPI-linked ligands
-
additional information
-
the BEK receptor, like FLG, also requires an interaction with heparan sulfate proteoglycans to facilitate binding to its ligands
-
additional information
-
protein-tyrosine kinase ITK/EMT is associated with CD28 and becomes tyrosine-phosphorylated and activated within seconds of CD28 ligation
-
additional information
-
one activation process in vertebrates involves activation and translocation to the plasma membrane of Ras, and/or autophosphorylation
-
additional information
-
autoregulation by a pseudosubstrate mechanism, overview
-
additional information
-
activation mechanism
-
additional information
-
reactive oxygen species, such as O2.- and H2O2, function as mitogenic mediators of activated growth-factor-receptor signaling
-
additional information
-
activation mechanism, overview
-
additional information
-
activation of the insulin receptor by phosphorylation via its tyrosine kinase activity
-
additional information
-
downregulation of endogenous Syk non-receptor tyrosine protein kinase expression in mammary endothelial cells enhances the ligand-induced activity of the epidermal growth factor receptor, but not of closely related human epidermal growth factor receptors HER2 and HER3, autophosphorylation inhibits EGFR, which is activated by Syk
-
additional information
-
deoxycholic acid and taurodeoxycholic acid enhance enzyme activity by inhibition of protein tyrosine phosphatases PTPases
-
additional information
-
FGFR2 and FGFR3 are activated by phosphorylation through non-receptor tyrosine kinase Pyk2
-
additional information
-
platelet-derived growth factor receptor or epidermal growth factor receptor transactivation via recombinant dopamine D2 receptor
-
additional information
Q2IBA6
ligand-dependent nonlinear increase in the level of c-MET phosphorylation in serum-starved Vero cells. c-MET activation response is sensitive to the dimer autophosphorylation rate. Stimulated monomeric c-MET, although clearly an active kinase molecule, is incapable of existing in an activated (i.e., phosphorylated, signaling competent) state due to synergistic effects of the biochemical properties associated with the c-MET monomeric state
-
additional information
-
exogenous expression of Sp1/Sp3 increases Axl promoter activity
-
additional information
-
two sites (Sp a and Sp b) proximal to the translation start site are indispensable for Axl promoter activity, whereas mutation of three additional upstream motifs (Sp c, Sp d and Sp e) is of additional relevance
-
additional information
-
constitutive activation of RTKs is provoked by several mechanisms including chromosomal translocations and various mutations involving their regulatory regions. Missense, insertion or deletion mutations in the regulatory regions, such as juxtamembrane domain, activation loop, and extracellular domain, also cause constitutive activation of RTKs mainly by preventing the auto-inhibitory regulation
-
additional information
-
FLT3 wild-type receptor protein is phosphorylated only upon stimulation with FLT3 ligand
-
additional information
-
EBV transformation does not induce ROR1 protein or ROR1 mRNA expression
-
additional information
-
overexpression of RET by electroporation in sacral neural crest cells, increases their ability to colonize the hindgut
-
additional information
-
sustained Ras activation in response to TrkA activation mediates differentiation, whereas transient activation results in proliferation
-
additional information
-
cysteines at position 303 and 348 are involved in covalent dimerization and/or ligand-induced receptor activation
-
additional information
-
local environment and membrane surface potential can modulate dimerization and activation of the receptor
-
additional information
-
Met tyrosine phosphorylation is elevated in cells in which the levels of either PTP1B or TCPTP are knocked down by specific siRNA, but not in cells transfected with scrambled siRNA. When both PTP1B and TCPTP are targeted together, up to 3fold higher tyrosine phosphorylation of Met is observed, suggesting an additive role for these phosphatases in the regulation of tyrosine phosphorylation of Met
-
additional information
Q60805
exposure to apoptotic cells induces a time-dependent increase in association of scavenger receptor A with Mertk in a direct or indirect manner
-
additional information
-
tyrosine phosphorylation of RON depends on the activity of Src family kinases
-
additional information
-
the activation of PKCdelta is strongly related to the glycosaminoglycans, especially chondroitin sulfate on the plasma membrane
-
additional information
-
insulin-like growth factor-1 treatment enhances phosphoinositide-dependent kinase-1 interaction with insulin-like growth factor-1 receptor in intact MCF-7 cells
-
KM VALUE [mM]
KM VALUE [mM] Maximum
SUBSTRATE
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
0.0051
-
Ac-DYFE-6-chloro-W-NHMe
P08069
pH 7.4, 25°C
-
0.07
-
Ac-DYFGW-NHMe
P08069
pH 7.4, 25°C
-
0.0011
-
ATP
-
mutant enzyme L861Q
0.005
-
ATP
-
wild type enzyme
0.0109
-
ATP
-
mutant enzyme L858R
0.232
-
YFEW
P08069
pH 7.4, 25°C
-
0.129
-
ATP
-
deletion mutant enzyme DELTA746-750
additional information
-
additional information
-
InRK: random kinetic mechanism, reaction kinetic can be influenced by the sort of substrate
-
additional information
-
additional information
-
enzyme dephosphorylation kinetics
-
additional information
-
additional information
P00533
lipid ligand-binding kinetics of ErbB1, plasma membrane binding kinetics of enzyme-derived peptides, overview
-
additional information
-
additional information
-
kinetics of wild-type EGFR-TK from A431 cells and recombinant EGFR-TK from Sf9 cells
-
Ki VALUE [mM]
Ki VALUE [mM] Maximum
INHIBITOR
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
2.7e-06
-
5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
-
inhibition versus erbB2 kinase
3.3e-06
-
erlotinib
-
deletion mutant enzyme DELTA746-750
6.25e-06
-
erlotinib
-
mutant enzyme L858R
1.75e-05
-
erlotinib
-
wild type enzyme
4.87e-05
-
erlotinib
-
mutant enzyme L861Q
additional information
-
additional information
-
-
-
IC50 VALUE [mM]
IC50 VALUE [mM] Maximum
INHIBITOR
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
0.00014
-
(2R)-2-[(4-[[1-(1,3-thiazol-4-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
8e-06
-
(2R)-2-[(4-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]-N,N-dimethylpropanamide
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
5.7e-05
-
(2R)-2-[(4-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]-N-methylpropanamide
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
3.2e-05
-
(2R)-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
3.4e-05
-
(2R)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N,N-dimethylpropanamide
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.0001
-
(2R)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N,N-dimethylpropanamide
-
inhibition of erbB2 in a mouse BT474C xenograft model
0.001
-
(2R)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N,N-dimethylpropanamide
-
inhibition of erbB2 in KB cells
3.1e-05
-
(2R)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N-(2-hydroxyethyl)-N-methylpropanamide
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
6.6e-05
-
(2R)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N-methylpropanamide
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
2.6e-05
-
(2R)-N,N-dimethyl-2-[(4-[[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.00023
-
(2R)-N,N-dimethyl-2-[(4-[[1-(1,3-thiazol-4-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
8e-06
-
(2R)-N,N-dimethyl-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
inhibition versus erbB2 kinase
9e-05
-
(2R)-N,N-dimethyl-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
2.3e-05
-
(2R)-N,N-dimethyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.00032
-
(2R)-N,N-dimethyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
-
inhibition of erbB2 in a mouse BT474C xenograft model
0.0027
-
(2R)-N,N-dimethyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
-
inhibition of erbB2 in KB cells
0.0002
-
(2R)-N-(2-hydroxyethyl)-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
6.9e-05
-
(2R)-N-(2-hydroxyethyl)-N-methyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.00027
-
(2R)-N-(2-hydroxyethyl)-N-methyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
-
inhibition of erbB2 in a mouse BT474C xenograft model
0.023
-
(2R)-N-(2-hydroxyethyl)-N-methyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
-
inhibition of erbB2 in KB cells
0.00012
-
(2R)-N-(2-methoxyethyl)-N-methyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.00024
-
(2R)-N-methyl-2-[(4-[[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
5.9e-05
-
(2R)-N-methyl-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
6e-06
-
(2S)-2-[(4-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]-N,N-dimethylpropanamide
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
4.3e-05
-
(2S)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N,N-dimethylpropanamide
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
7.9e-05
-
(2S)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N-(2-hydroxyethyl)-N-methylpropanamide
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
2.4e-05
-
(2S)-N,N-dimethyl-2-[(4-[[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.00013
-
(2S)-N,N-dimethyl-2-[(4-[[1-(1,3-thiazol-4-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
8e-05
-
(2S)-N,N-dimethyl-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
3e-05
-
(2S)-N,N-dimethyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
7.8e-05
-
(2S)-N-(2-hydroxyethyl)-N-methyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
2e-06
-
(R)-2-(2-[[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]methyl]pyrrolidin-1-yl)-2-oxoethanol
-
IC50: less than 2 nM
9.7e-05
-
(R)-2-(2-[[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]methyl]pyrrolidin-1-yl)-2-oxoethanol
-
IC50: 97 nM
2e-06
-
(R)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-1-methylethyl]-2-hydroxyacetamide
-
IC50: less than 2 nM
3e-06
-
(R)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-1-methylethyl]-2-hydroxyacetamide
-
IC50: 3 nM
2e-06
-
(R)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]propyl]-2-hydroxyacetamide
-
IC50: 2 nM; IC50: less than 2 nM
2e-06
-
(S)-2-(2-[[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]methyl]pyrrolidin-1-yl)-2-oxoethanol
-
IC50: 2 nM
0.000327
-
(S)-2-(2-[[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]methyl]pyrrolidin-1-yl)-2-oxoethanol
-
IC50: 327 nM
1.9e-05
-
(S)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-1-methylethyl]-2-hydroxyacetamide
-
IC50: 19 nM
0.00258
-
(S)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-1-methylethyl]-2-hydroxyacetamide
-
IC50: 2580 nM
2.2e-05
-
(S)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]propyl]-2-hydroxyacetamide
-
IC50: 22 nM
0.000191
-
(S)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]propyl]-2-hydroxyacetamide
-
IC50: 191 nM
9.8e-07
-
(Z)-5-[6-[3-(4-methoxyphenyl)-ureido]-2-oxo-1,2-dihydroindol-3-ylidene-methyl]-4-methyl-1H-pyrrole-3-carboxylic acid
P16234
pH 7.5, 22°C
1e-05
-
1-(4-(1H-pyrazol-1-yl)phenyl)-3-(2-aminoquinazolin-6-yl)-4-methylpyridin-2(1H)-one
-
c-Kit
0.0034
-
1-(4-(1H-pyrazol-1-yl)phenyl)-3-(2-aminoquinazolin-6-yl)-4-methylpyridin-2(1H)-one
-
KDR
2e-05
-
1-(4-acetylphenyl)-3-(2-aminoquinazolin-6-yl)-4-methylpyridin-2(1H)-one
-
c-Kit
0.005
-
1-(4-acetylphenyl)-3-(2-aminoquinazolin-6-yl)-4-methylpyridin-2(1H)-one
-
KDR
0.00012
-
2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N-(2-hydroxyethyl)-N-methylacetamide
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.00018
-
2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]acetamide
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
4e-06
-
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
-
pH not specified in the publication, temperature not specified in the publication
1e-06
-
3-(2-aminoquinazolin-6-yl)-1-(2-cyclopentylethyl)-4-methylpyridin-2(1H)-one
-
c-Kit
0.0014
-
3-(2-aminoquinazolin-6-yl)-1-(2-cyclopentylethyl)-4-methylpyridin-2(1H)-one
-
KDR
6.1e-06
-
3-(2-aminoquinazolin-6-yl)-1-(3,3-dimethylindolin-6-yl)-4-methylpyridin-2(1H)-one
-
c-Kit
4.8e-05
-
3-(2-aminoquinazolin-6-yl)-1-(3,3-dimethylindolin-6-yl)-4-methylpyridin-2(1H)-one
-
KDR
4e-05
-
3-(2-aminoquinazolin-6-yl)-1-(3-fluoro-4-methylphenyl)-4-methylpyridin-2(1H)-one
-
c-Kit
0.005
-
3-(2-aminoquinazolin-6-yl)-1-(3-fluoro-4-methylphenyl)-4-methylpyridin-2(1H)-one
-
KDR
6.5e-05
-
3-(2-aminoquinazolin-6-yl)-1-(3-methoxyphenyl)-4-methylpyridin-2(1H)-one
-
c-Kit
0.005
-
3-(2-aminoquinazolin-6-yl)-1-(3-methoxyphenyl)-4-methylpyridin-2(1H)-one
-
KDR
6e-05
-
3-(2-aminoquinazolin-6-yl)-1-(4-chloro-3-fluorophenyl)-4-methylpyridin-2(1H)-one
-
c-Kit
0.005
-
3-(2-aminoquinazolin-6-yl)-1-(4-chloro-3-fluorophenyl)-4-methylpyridin-2(1H)-one
-
KDR
2e-05
-
3-(2-aminoquinazolin-6-yl)-1-(4-chlorophenyl)-4-methylpyridin-2(1H)-one
-
c-Kit
0.005
-
3-(2-aminoquinazolin-6-yl)-1-(4-chlorophenyl)-4-methylpyridin-2(1H)-one
-
KDR
1.4e-05
-
3-(2-aminoquinazolin-6-yl)-1-(4-fluoro-3-methylphenyl)-4-methylpyridin-2(1H)-one
-
c-Kit
0.0043
-
3-(2-aminoquinazolin-6-yl)-1-(4-fluoro-3-methylphenyl)-4-methylpyridin-2(1H)-one
-
KDR
1.7e-05
-
3-(2-aminoquinazolin-6-yl)-1-(4-methoxyphenyl)-4-methylpyridin-2(1H)-one
-
c-Kit
0.005
-
3-(2-aminoquinazolin-6-yl)-1-(4-methoxyphenyl)-4-methylpyridin-2(1H)-one
-
KDR
2.1e-06
-
3-(2-aminoquinazolin-6-yl)-1-(4-tert-butylphenyl)-4-methylpyridin-2(1H)-one
-
c-Kit
1.1e-05
-
3-(2-aminoquinazolin-6-yl)-1-(4-tert-butylphenyl)-4-methylpyridin-2(1H)-one
-
KDR
1.4e-05
-
3-(2-aminoquinazolin-6-yl)-4-methyl-1-(3-(trifluoromethyl)phenyl)pyridin-2(1H)-one
-
c-Kit
0.005
-
3-(2-aminoquinazolin-6-yl)-4-methyl-1-(3-(trifluoromethyl)phenyl)pyridin-2(1H)-one
-
KDR
2.2e-05
-
3-(2-aminoquinazolin-6-yl)-4-methyl-1-(4-(oxazol-2-yl)phenyl)pyridin-2(1H)-one
-
c-Kit
0.005
-
3-(2-aminoquinazolin-6-yl)-4-methyl-1-(4-(oxazol-2-yl)phenyl)pyridin-2(1H)-one
-
KDR
7.9e-06
-
3-(2-aminoquinazolin-6-yl)-4-methyl-1-(4-(trifluoromethyl)phenyl)pyridin-2(1H)-one
-
c-Kit
0.0018
-
3-(2-aminoquinazolin-6-yl)-4-methyl-1-(4-(trifluoromethyl)phenyl)pyridin-2(1H)-one
-
KDR
1.3e-05
-
3-(2-aminoquinazolin-6-yl)-4-methyl-1-(4-morpholinophenyl)pyridin-2(1H)-one
-
c-Kit
0.0044
-
3-(2-aminoquinazolin-6-yl)-4-methyl-1-(4-morpholinophenyl)pyridin-2(1H)-one
-
KDR
0.00021
-
3-(2-aminoquinazolin-6-yl)-4-methyl-1-phenylpyridin-2(1H)-one
-
c-Kit
0.001
-
3-(2-aminoquinazolin-6-yl)-4-methyl-1-phenylpyridin-2(1H)-one
-
KDR
2e-05
-
3-[[5-([6-amino-5-[(E)-(methoxyimino)methyl]pyrimidin-4-yl]amino)-1H-indazol-1-yl]methyl]benzonitrile
-
-
4.4e-05
-
3-[[5-([6-amino-5-[(E)-(methoxyimino)methyl]pyrimidin-4-yl]amino)-1H-indazol-1-yl]methyl]benzonitrile
-
-
2.2e-05
-
4-(5-((2-methoxyethyl)carbamoyl)naphthalen-2-yloxy)-7-methoxyquinoline-6-carboxamide
-
-
2e-07
-
4-(5-((4-chlorophenyl)carbamoyl)naphthalen-2-yloxy)-7-methoxyquinoline-6-carboxamide
-
KDR enzyme
3e-06
-
4-(5-((4-chlorophenyl)carbamoyl)naphthalen-2-yloxy)-7-methoxyquinoline-6-carboxamide
-
VEGF driven proliferation of HUVEC cell
3e-06
-
4-(5-((4-chlorophenyl)carbamoyl)naphthalen-2-yloxy)-N-methylpicolinamide
-
KDR enzyme
0.00021
-
4-(5-((4-chlorophenyl)carbamoyl)naphthalen-2-yloxy)-N-methylpicolinamide
-
VEGF driven proliferation of HUVEC cell
3.7e-07
-
4-(5-(cyclopropylcarbamoyl)naphthalen-2-yloxy)-7-methoxyquinoline-6-carboxamide
-
-
0.000131
-
4-(5-bromoindole-3-yl)-6,7-dimethoxyquinazoline
-
-
1.3e-06
-
4-(5-carbamoylnaphthalen-2-yloxy)-7-methoxyquinoline-6-carboxamide
-
-
0.000472
-
4-(5-chloro-6-fluoro-indole-3-yl)-6,7-di-(2-methoxyethoxy)quinazoline
-
-
0.000209
-
4-(5-chloro-6-fluoroindole-3-yl)-6,7-dimethoxyquinazoline
-
-
0.000333
-
4-(5-chloro-6-fluoroindole-3-yl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazoline
-
-
0.000533
-
4-(6-fluoro-5-methylindole-3-yl)-6,7-dimethoxyquinazoline
-
-
5e-06
-
4-(imidazo[1,2-a]pyridin-3-yl)-N-[2-methoxyphenyl-4-(4-piperidinyl)]pyrimidin-2-amine
-
pH not specified in the publication, temperature not specified in the publication
4e-06
-
4-(imidazo[2-methoxy-4-(9-oxa-3,7-diazabicyclo[3.3.1]non-3-yl)phenyl])pyrimidin-2-amine
-
pH not specified in the publication, temperature not specified in the publication
0.000306
-
4-amino-6-(1H-indazol-5-ylamino)pyrimidine-5-carbaldehyde O-methyloxime
-
-
0.004123
-
4-amino-6-(1H-indazol-5-ylamino)pyrimidine-5-carbaldehyde O-methyloxime
-
-
3.3e-05
-
4-amino-6-([3-chloro-4-[(3,5-difluorobenzyl)oxy]phenyl]amino)pyrimidine-5-carbaldehyde O-methyloxime
-
-
1.2e-05
-
4-amino-6-([3-chloro-4-[(3-fluorobenzyl)oxy]phenyl]amino)pyrimidine-5-carbaldehyde O-methyloxime
-
-
1.8e-05
-
4-amino-6-([3-chloro-4-[(3-fluorobenzyl)oxy]phenyl]amino)pyrimidine-5-carbaldehyde O-methyloxime
-
-
2.2e-05
-
4-amino-6-[(1-benzyl-1H-indazol-5-yl)amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
4.4e-05
-
4-amino-6-[(1-benzyl-1H-indazol-5-yl)amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
0.001123
-
4-amino-6-[(3-chloro-4-fluorobenzyl)amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
0.00522
-
4-amino-6-[(3-chloro-4-fluorobenzyl)amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
2.3e-05
-
4-amino-6-[[1-(3-chlorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
3e-05
-
4-amino-6-[[1-(3-chlorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
1.4e-05
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(1-methylethyl)oxime
-
-
2.5e-05
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(1-methylethyl)oxime
-
-
4.7e-05
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(2-methoxybenzyl)oxime
-
-
0.000435
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(2-methoxybenzyl)oxime
-
-
6e-06
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(2-methoxyethyl)oxime
-
-
1.4e-05
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(2-methoxyethyl)oxime
-
-
3.2e-05
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(2-methylpropyl)oxime
-
-
0.000173
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(2-methylpropyl)oxime
-
-
2.3e-05
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-benzyloxime
-
-
9.5e-05
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-benzyloxime
-
-
5e-06
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-ethyloxime
-
-
7e-06
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-ethyloxime
-
-
1.2e-05
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde oxime
-
-
4.2e-05
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde oxime
-
-
1.3e-05
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
2.7e-05
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
5.7e-05
-
4-amino-6-[[1-(3-fluorobenzyl)-2,3-dihydro-1H-indol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
0.000255
-
4-amino-6-[[1-(3-fluorobenzyl)-2,3-dihydro-1H-indol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
0.000267
-
4-amino-6-[[1-(3-methoxybenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
0.000104
-
4-amino-6-[[1-(4-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
0.000189
-
4-amino-6-[[1-(4-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
4.8e-05
-
4-amino-6-[[2-(3-fluorobenzyl)-1H-benzimidazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
7.6e-05
-
4-amino-6-[[2-(3-fluorobenzyl)-1H-benzimidazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
1.6e-05
-
4-amino-6-[[4-(benzyloxy)-3-chlorophenyl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
0.000153
-
4-amino-6-[[4-(benzyloxy)-3-chlorophenyl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
-
4.3e-05
-
5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.00016
-
5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(1,3-thiazol-4-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
5.1e-05
-
5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
1.2e-05
-
5-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.00014
-
5-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.025
-
6-(1H-indol-5-ylmethyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
P09619
pH not specified in the publication, temperature not specified in the publication
0.077
-
6-(1H-indol-5-ylmethyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
P09619
pH not specified in the publication, temperature not specified in the publication
0.2
-
6-(1H-indol-5-ylmethyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
P09619
pH not specified in the publication, temperature not specified in the publication; pH not specified in the publication, temperature not specified in the publication
0.031
-
6-(1H-indol-5-ylmethyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
P09619
pH not specified in the publication, temperature not specified in the publication
0.056
-
6-(1H-indol-5-ylmethyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
P09619
pH not specified in the publication, temperature not specified in the publication
0.104
-
6-(1H-indol-5-ylmethyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
P09619
pH not specified in the publication, temperature not specified in the publication
0.223
-
6-(1H-indol-5-ylmethyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
P09619
pH not specified in the publication, temperature not specified in the publication
0.0003
-
6-(3-bromobenzyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
P09619
pH not specified in the publication, temperature not specified in the publication
0.0118
-
6-(3-bromobenzyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
P09619
pH not specified in the publication, temperature not specified in the publication
0.0451
-
6-(3-bromobenzyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
P09619
pH not specified in the publication, temperature not specified in the publication
0.05
-
6-(3-bromobenzyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
P09619
pH not specified in the publication, temperature not specified in the publication
0.0085
-
6-(3-bromobenzyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
P09619
pH not specified in the publication, temperature not specified in the publication
0.112
-
6-(3-bromobenzyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
P09619
pH not specified in the publication, temperature not specified in the publication
0.129
-
6-(3-bromobenzyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
P09619
pH not specified in the publication, temperature not specified in the publication
0.2
-
6-(3-bromobenzyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
P09619
pH not specified in the publication, temperature not specified in the publication
1.3e-06
-
6-(6,7-dimethoxyquinazolin-4-yloxy)-1-naphthamide
-
-
0.000314
-
6-(6,7-dimethoxyquinazolin-4-yloxy)-N-(2-methoxyethyl)-1-naphthamide
-
-
9e-07
-
6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide methanesulfonate
-
-
1.5e-05
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(1-methylcyclopropyl)-1-naphthamide
-
-
3.8e-06
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(2,2,2-trifluoroethyl)-1-naphthamide
-
-
2e-06
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(2-fluorophenyl)-1-naphthamide
-
KDR enzyme
7e-06
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(2-fluorophenyl)-1-naphthamide
-
VEGF driven proliferation of HUVEC cell
1.2e-05
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(2-methoxyethyl)-1-naphthamide
-
-
5e-07
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(3-(trifluoromethyl)phenyl)-1-naphthamide
-
KDR enzyme
3.4e-05
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(3-(trifluoromethyl)phenyl)-1-naphthamide
-
VEGF driven proliferation of HUVEC cell
6e-07
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(3-fluorophenyl)-1-naphthamide
-
KDR enzyme
3e-06
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(3-fluorophenyl)-1-naphthamide
-
VEGF driven proliferation of HUVEC cell
4.2e-06
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(3-methoxypropyl)-1-naphthamide
-
-
1e-06
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(3-methylisoxazol-5-yl)-1-naphthamide
-
KDR enzyme
7e-06
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(3-methylisoxazol-5-yl)-1-naphthamide
-
VEGF driven proliferation of HUVEC cell
5e-07
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(4-(trifluoromethyl)phenyl)-1-naphthamide
-
KDR enzyme
1.6e-05
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(4-(trifluoromethyl)phenyl)-1-naphthamide
-
VEGF driven proliferation of HUVEC cell
1e-06
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(4-fluorophenyl)-1-naphthamide
-
KDR enzyme
2e-06
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(4-fluorophenyl)-1-naphthamide
-
VEGF driven proliferation of HUVEC cell
6e-07
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(5-methylisoxazol-3-yl)-1-naphthamide
-
KDR enzyme
6e-06
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(5-methylisoxazol-3-yl)-1-naphthamide
-
VEGF driven proliferation of HUVEC cell
2e-07
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(isoxazol-3-yl)-1-naphthamide
-
KDR enzyme
4e-07
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(isoxazol-3-yl)-1-naphthamide
-
VEGF driven proliferation of HUVEC cell
8e-07
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(pyridin-2-yl)-1-naphthamide
-
KDR enzyme
2e-06
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(pyridin-2-yl)-1-naphthamide
-
VEGF driven proliferation of HUVEC cell
8e-07
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(pyridin-3-yl)-1-naphthamide
-
KDR enzyme
2e-06
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(pyridin-3-yl)-1-naphthamide
-
VEGF driven proliferation of HUVEC cell
2e-06
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(pyridin-4-yl)-1-naphthamide
-
KDR enzyme; VEGF driven proliferation of HUVEC cell
3e-07
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(thiazol-2-yl)-1-naphthamide
-
KDR enzyme
2e-06
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(thiazol-2-yl)-1-naphthamide
-
VEGF driven proliferation of HUVEC cell
1.3e-06
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-ethyl-1-naphthamide
-
-
4e-06
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-isopropyl-1-naphthamide
-
VEGF driven proliferat