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A-type platelet-derived growth factor receptor
-
ALK receptor tyrosine kinase
-
-
ALK tyrosine kinase receptor
alpha platelet-derived growth factor receptor
Anaplastic lymphoma kinase
basic fibroblast growth factor receptor 1
BDNF/NT-3 growth factors receptor
beta platelet-derived growth factor receptor
Brain-specific kinase
-
-
-
-
Breathless protein
-
-
-
-
c-Kit receptor protein-tyrosine kinase
-
c-Kit receptor tyrosine kinase
c-Kit tyrosine kinase
-
-
-
-
c-Met receptor tyrosine kinase
Cell adhesion kinase
-
-
-
-
chicken embryo kinase 5
-
class II receptor tyrosine kinase
-
colony-stimulating factor-1 receptor
-
-
CSF-1 receptor
-
also known as c-fms and CD115
discoidin domain receptor 1
-
discoidin domain receptor 2
discoidin domain receptor tyrosine kinase 1
-
Discoidin receptor tyrosine kinase
Drosophila relative of ERBB
-
-
-
-
DTK receptor tyrosine kinase
-
EC 2.7.1.112
-
-
formerly, part transferred
-
EGF receptor protein-tyrosine kinase
-
-
EGF receptor tyrosine kinase
EGFR protein tyrosine kinase
Egg laying defective protein 15
-
-
-
-
Embryonic brain kinase
-
-
-
-
embryonic receptor kinase
-
Endothelial kinase receptor EK1
-
-
-
-
Eph homologous kinase 3
-
Eph receptor tyrosine kinase
-
EPH-and ELK-related kinase
-
-
-
-
Eph-related receptor tyrosine kinase Cek9
-
EPHA1 receptor tyrosine kinase
-
ephrin type-A receptor 1
-
ephrin type-A receptor 4A
-
ephrin type-A receptor 4B
-
ephrin type-A receptor 6
-
ephrin type-B receptor 1A
-
ephrin type-B receptor 5
-
epidermal growth factor receptor
epidermal growth factor receptor 2
-
-
epidermal growth factor receptor 4
-
epidermal growth factor receptor kinase
-
-
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 discoidin domain receptor 1
ErbB receptor protein-tyrosine kinase
-
-
erbB tyrosine kinase
-
-
-
-
ErbB1 tyrosine kinase
-
-
erbB2 receptor tyrosine kinase
ErbB2 tyrosine kinase
-
-
ErbB3 receptor tyrosine kinase
-
erythropoietin-producing hepatocellular receptor tyrosine kinase subtype A2
-
-
erythropoietin-producing human hepatocellular carcinoma B3
-
FGF receptor tyrosine kinase
-
-
fibroblast growth factor receptor
fibroblast growth factor receptor 1
fibroblast growth factor receptor 2
fibroblast growth factor receptor 3
fibroblast growth factor receptor 4
fibroblast growth factor receptor BFR-2
-
fibroblast growth factor receptor homolog 1
-
fibroblast growth factor receptor homolog 2
-
FLT3 receptor protein
-
-
FLT3/FLK2 receptor tyrosine kinase
-
FLT4 receptor tyrosine kinase
-
Fms proto-oncogene
-
-
-
-
fms-like tyrosine kinase 3
-
-
GP145-TrkB/GP95-TrkB
-
-
-
-
growth hormone receptor
-
-
Heartless protein
-
-
-
-
Heparin-binding growth factor receptor
-
-
-
-
hepatocyte growth factor receptor
HER receptor protein-tyrosine kinase
-
-
high affinity nerve growth factor receptor
human epidermal growth factor receptor2
-
-
hydroxyaryl-protein kinase
-
-
-
-
IGF-1R tyrosine kinase
-
-
insulin receptor protein tyrosine kinase
-
-
insulin receptor protein-tyrosine kinase
-
-
-
-
insulin receptor tyrosine kinase
insulin receptor-beta subunit
-
-
insulin receptor-related protein
insulin receptor-related receptor
-
insulin-growth factor-1 receptor
-
-
insulin-like growth factor 1 receptor
-
insulin-like growth factor I receptor
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
-
insulin-receptor tyrosine kinase
-
-
IR-related receptor
-
-
-
-
IRR-protein tyrosine kinase
-
KDR/fetal liver kinase-1
-
-
Keratinocyte growth factor receptor
Kinase insert domain receptor
-
-
-
-
Kit protein-tyrosine kinase
KIT receptor tyrosine kinase
-
-
Let-23 receptor protein-tyrosine kinase
-
leukocyte tyrosine kinase receptor
ltk receptor tyrosine kinase
-
macrophage colony stimulating factor I receptor
macrophage colony-stimulating factor receptor
macrophage stimulating 1 receptor
-
-
macrophage stimulating 1-receptor
-
-
macrophage-colony stimulating factor receptor
-
-
macrophage-stimulating protein receptor
mast/stem cell growth factor receptor
melanoma receptor protein-tyrosine kinase
-
Mer receptor tyrosine kinase
-
Met proto-oncogene tyrosine kinase
-
-
-
-
Met receptor-tyrosine kinase
Met-related kinase
-
-
-
-
Met/hepatocyte growth factor receptor tyrosine kinase
-
mouse developmental kinase 1
-
muscle-specific receptor tyrosine kinase
muscle-specific receptor-tyrosine kinase
-
-
myoblast growth factor receptor egl-15
-
nerve growth factor receptor
-
-
NEU proto-oncogene
-
-
-
-
neuregulin receptor ErbB-4
-
Neurospecific receptor tyrosine kinase
-
-
-
-
neurotrophin tyrosine receptor kinase
non-receptor protein tyrosine kinase
-
-
NT-3 growth factor receptor
nuclear growth factor tyrosine protein kinase
-
-
orphan receptor tyrosine kinase
-
-
p75 neurotrophin receptor
-
-
PDGF receptor tyrosine kinase
platelet derived growth factor receptor-beta
-
platelet-derived growth factor receptor
platelet-derived growth factor receptor alpha
platelet-derived growth factor receptor kinase
-
-
platelet-derived growth factor receptor-beta
-
-
platelet-derived growth factor RPTK
-
-
proline-rich tyrosinekinase
-
-
protein kinase Cdelta
-
-
protein receptor tyrosine kinase RTK 6
-
Protein-tyrosine kinase byk
-
-
-
-
protein-tyrosine kinase ITK/EMT
-
Protein-tyrosine kinase receptor MPK-11
-
-
-
-
Proto-oncogene tyrosine-protein kinase Kit
-
-
-
-
proto-oncogene tyrosine-protein kinase MER
proto-oncogene tyrosine-protein kinase receptor
-
proto-oncogene tyrosine-protein kinase receptor ret
proto-oncogene tyrosine-protein kinase ROS
-
rceptor protein-tyrosine kinase erbB-4
-
recepteur d'origine nantais
recepteur d'origine nantais receptor tyrosine kinase
Recepteur dOrigine Nantais
-
receptor for macrophage colony-stimulating factor
-
-
receptor for stem cell factor
-
-
receptor protein tyrosine kinase
-
-
receptor protein tyrosine kinase RTK
-
receptor protein-tyrosine kinase erbB-2
receptor protein-tyrosine kinase erbB-3
receptor protein-tyrosine kinase erbB-4
-
Receptor protein-tyrosine kinase HEK11
-
-
-
-
Receptor protein-tyrosine kinase HEK5
-
-
-
-
Receptor protein-tyrosine kinase HEK7
-
-
-
-
Receptor protein-tyrosine kinase HEK8
-
-
-
-
Receptor protein-tyrosine kinase TKT
-
-
-
-
receptor tyrosine kinase c-Kit
receptor tyrosine kinase Cek8
-
receptor tyrosine kinase EphA1
-
-
receptor tyrosine kinase EphA2
receptor tyrosine kinase Mer
-
Receptor tyrosine kinase MerTK
-
-
-
-
receptor tyrosine kinase RET
receptor tyrosine kinase RON
-
-
receptor tyrosine kinase ROR1
-
receptor tyrosine kinase Ror2
receptor tyrosine kinase Sek
-
receptor tyrosine kinase Sky
-
receptor tyrosine kinase vascular endothelial growth factor receptor-2
-
-
receptor tyrosine-protein kinase erbB-2
-
Receptor-activated Janus kinase
-
-
-
-
receptor-like protein tyrosine kinase bsk
-
receptor-like protein-tyrosine kinase TK14
-
receptor-like tyrosine-protein kinase kin-15
-
receptor-like tyrosine-protein kinase kin-16
-
receptor-type tyrosine kinase termed Rse
-
receptor-type tyrosine-protein kinase FLT3
-
Ret receptor tyrosine kinase
RON receptor tyrosine kinase
Ron tyrosine kinase receptor
-
Ron/Stk receptor tyrosine kinase
-
Sek-1 receptor tyrosine kinase
-
sevenless receptor tyrosine kinase
-
-
sky receptor tyrosine kinase
-
Slow nerve growth factor receptor
-
-
-
-
soluble fms-like tyrosine kinase 1
-
-
sponge receptor tyrosine kinase
-
stem cell derived tyrosine kinase
-
-
stem cell factor receptor
-
-
stem cell tyrosine kinase 1
-
Stem cell-derived tyrosine kinase
subclass III receptor tyrosine kinase
-
-
Tec family kinase EMT/ITK/TSK
-
Tek receptor tyrosine kinase
-
TRK1 transforming tyrosine kinase protein
-
-
-
-
TrkB tyrosine kinase
-
-
-
-
TrkC receptor tyrosine kinase
-
TrkC tyrosine kinase
-
-
-
-
Tunica interna endothelial cell kinase
-
-
-
-
Tyro 10 receptor tyrosine kinase
-
Tyrosine kinase CEK6 receptor
-
-
-
-
Tyrosine kinase DDR
-
-
-
-
tyrosine kinase domain of the insulin receptor
-
-
tyrosine kinase Emt/Itk
-
tyrosine kinase receptor
-
-
tyrosine kinase receptor CEK2
-
tyrosine kinase receptor CEK3
-
Tyrosine kinase receptor HD-14
-
-
-
-
tyrosine kinase receptor HER2
-
tyrosine kinase receptor RON
-
-
tyrosine kinase receptor trkE
-
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
-
tyrosine-protein kinase Drl
-
Tyrosine-protein kinase DTK
-
-
-
-
tyrosine-protein kinase Etk
Tyrosine-protein kinase FLT3
-
-
-
-
Tyrosine-protein kinase FRT
-
-
-
-
tyrosine-protein kinase ITK/TSK
-
tyrosine-protein kinase Ptk
-
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
tyrosine-protein kinase receptor torso
-
tyrosine-protein kinase receptor TYRO3
tyrosine-protein kinase receptor UFO
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
Tyrosine-protein kinase SKY
-
-
-
-
tyrosine-protein kinase transforming protein erbB
tyrosine-protein kinase transforming protein kit
tyrosine-protein kinase transforming protein RYK
-
tyrosine-protein kinase transmembrane receptor Ror
-
tyrosine-protein kinase transmembrane receptor ROR1
tyrosine-protein kinase transmembrane receptor ROR2
tyrosine-protein kinase Wzc
VAB-1 Eph receptor tyrosine kinase
-
vascular endothelial growth factor
-
-
vascular endothelial growth factor 2
-
-
vascular endothelial growth factor receptor
vascular endothelial growth factor receptor 1
vascular endothelial growth factor receptor 2
vascular endothelial growth factor receptor 3
vascular endothelial growth factor receptor tyrosine kinase
-
-
vascular endothelial growth factor receptor-1
-
vascular endothelial growth-factor receptor-1 tyrosine kinase
-
-
Vascular permeability factor receptor
-
-
-
-
VEGF factor receptor tyrosine kinase
-
-
VEGF receptor tyrosine kinase
VEGFR tyrosine kinase
-
-
VEGFR-1 tyrosine kinase
-
-
VEGFR-2 tyrosine kinase
-
VEGFR2/kinase domain region
-
-
Xenopus Elk-like kinase
-
Adhesion-related kinase
-
-
-
-
Adhesion-related kinase
-
ALK
-
-
ALK tyrosine kinase receptor
-
ALK tyrosine kinase receptor
-
alpha platelet-derived growth factor receptor
-
alpha platelet-derived growth factor receptor
-
alpha platelet-derived growth factor receptor
-
alpha platelet-derived growth factor receptor
-
Anaplastic lymphoma kinase
-
-
-
-
Anaplastic lymphoma kinase
-
-
Anaplastic lymphoma kinase
-
-
Anaplastic lymphoma kinase
-
-
angiopoietin 1 receptor
-
angiopoietin 1 receptor
-
angiopoietin 1 receptor
-
angiopoietin 1 receptor
-
Axl
Drosophila sp. (in: flies)
-
-
basic fibroblast growth factor receptor 1
-
basic fibroblast growth factor receptor 1
-
490167, 490218, 490219, 490220, 490221, 490222, 490223, 490225, 490226, 490227, 490228, 490229, 490230, 490231
basic fibroblast growth factor receptor 1
-
basic fibroblast growth factor receptor 1
-
BDNF/NT-3 growth factors receptor
-
BDNF/NT-3 growth factors receptor
-
BDNF/NT-3 growth factors receptor
-
BDNF/NT-3 growth factors receptor
-
BDNF/NT-3 growth factors receptor
-
beta platelet-derived growth factor receptor
-
beta platelet-derived growth factor receptor
-
c-fms
-
-
-
-
c-kit
-
-
-
-
c-Kit receptor tyrosine kinase
-
-
c-Kit receptor tyrosine kinase
-
-
C-mer
-
-
-
-
c-met
-
-
-
-
c-Met receptor tyrosine kinase
-
-
c-Met receptor tyrosine kinase
-
discoidin domain receptor 2
-
discoidin domain receptor 2
-
Discoidin receptor tyrosine kinase
-
-
-
-
Discoidin receptor tyrosine kinase
-
DTK
-
-
EBK
-
-
-
-
EGF receptor
-
EGF receptor tyrosine kinase
-
-
-
-
EGF receptor tyrosine kinase
-
-
EGF receptor tyrosine kinase
-
-
EGF receptor tyrosine kinase
-
-
EGF-R
-
-
Egfr
-
-
-
-
Egfr
-
-
660727, 660873, 661457, 662678, 672910, 672957, 674681, 676837, 677234, 691067, 693346, 693727, 694498, 703259, 704651, 705802, 737815, 737831, 737992, 738710, 738744
EGFR protein tyrosine kinase
-
-
EGFR protein tyrosine kinase
-
-
EGFR protein tyrosine kinase
-
-
EGFR tyrosine kinase
-
-
EGFR-TK
-
-
EphA1
-
-
EphA2
-
-
ephrin type-A receptor 2
-
ephrin type-A receptor 2
-
ephrin type-A receptor 3
-
ephrin type-A receptor 3
-
ephrin type-A receptor 3
-
ephrin type-A receptor 3
-
ephrin type-A receptor 3
-
ephrin type-A receptor 4
-
ephrin type-A receptor 4
-
ephrin type-A receptor 4
-
ephrin type-A receptor 5
-
ephrin type-A receptor 5
-
ephrin type-A receptor 5
-
ephrin type-A receptor 5
-
ephrin type-A receptor 7
-
ephrin type-A receptor 7
-
ephrin type-A receptor 7
-
ephrin type-A receptor 7
-
ephrin type-A receptor 8
-
ephrin type-A receptor 8
-
ephrin type-B receptor 1
-
ephrin type-B receptor 1
-
ephrin type-B receptor 2
-
ephrin type-B receptor 2
-
ephrin type-B receptor 2
-
ephrin type-B receptor 3
-
ephrin type-B receptor 3
-
ephrin type-B receptor 4
-
ephrin type-B receptor 4
-
epidermal growth factor receptor
-
-
epidermal growth factor receptor
-
epidermal growth factor receptor
-
-
epidermal growth factor receptor
-
-
660727, 660873, 661457, 661551, 662556, 662679, 674681, 677234, 691067, 691636, 693727, 694498, 702950, 703259, 704651, 705802, 737815
epidermal growth factor receptor
-
epidermal growth factor receptor
-
-
epidermal growth factor receptor
-
epidermal growth factor receptor
-
-
epidermal growth factor receptor tyrosine kinase
-
-
epidermal growth factor receptor tyrosine kinase
-
epidermal growth factor receptor tyrosine kinase
-
-
Epithelial cell kinase
-
-
-
-
epithelial discoidin domain receptor 1
-
epithelial discoidin domain receptor 1
-
epithelial discoidin domain receptor 1
-
ErbB-2
-
ErbB-4 tyrosine kinase
-
-
ErbB-4 tyrosine kinase
-
-
ERBB1
-
-
ErbB2
-
-
erbB2 receptor tyrosine kinase
-
-
erbB2 receptor tyrosine kinase
-
erbB2 receptor tyrosine kinase
-
-
erbB2 receptor tyrosine kinase
-
-
ERK
-
-
-
-
FGFR
-
-
FGFR2
-
-
FGFR3
-
-
FGFR4
-
-
fibroblast growth factor receptor
-
-
fibroblast growth factor receptor
-
-
fibroblast growth factor receptor
-
-
fibroblast growth factor receptor 1
-
fibroblast growth factor receptor 1
-
fibroblast growth factor receptor 2
-
490218, 490288, 490289, 490290, 490291, 490292, 490293, 490294, 490295, 490296, 490297, 490298, 490299, 490300, 490301, 490302, 490303, 490304, 490305, 490306
fibroblast growth factor receptor 2
-
fibroblast growth factor receptor 2
-
fibroblast growth factor receptor 2
-
fibroblast growth factor receptor 3
-
490320, 490323, 490324, 490325, 490326, 490327, 490328, 490329, 490330, 490331, 490332, 490333, 490335, 490336, 490337, 490338, 490339, 721711
fibroblast growth factor receptor 3
-
fibroblast growth factor receptor 4
-
fibroblast growth factor receptor 4
-
fibroblast growth factor receptor 4
-
FL cytokine receptor
-
Flk-1
-
FLT3
-
-
GCTK
-
-
-
-
HEK
-
-
-
-
hepatocyte growth factor receptor
-
hepatocyte growth factor receptor
-
-
hepatocyte growth factor receptor
-
hepatocyte growth factor receptor
-
-
hepatocyte growth factor receptor
-
hepatocyte growth factor receptor
-
HER2
-
-
high affinity nerve growth factor receptor
-
high affinity nerve growth factor receptor
-
HYK
-
-
-
-
IGF-1R
-
-
IGF-IR
-
-
ILP receptor
-
-
-
-
insulin receptor
-
-
insulin receptor kinase
-
-
insulin receptor kinase
-
-
insulin receptor kinase
-
-
insulin receptor tyrosine kinase
-
-
insulin receptor tyrosine kinase
-
-
insulin receptor-related protein
-
insulin receptor-related protein
-
insulin receptor-related protein
-
insulin-like growth factor I receptor
-
insulin-like growth factor I receptor
-
insulin-like growth factor I receptor
-
insulin-like growth factor type I receptor
-
-
insulin-like growth factor type I receptor
-
-
insulin-like receptor
-
IRK
-
-
-
-
IRR
-
-
-
-
KDR
-
Keratinocyte growth factor receptor
-
-
-
-
Keratinocyte growth factor receptor
-
-
Keratinocyte growth factor receptor
-
KGF receptor
-
-
KIT
-
Kit protein-tyrosine kinase
-
-
Kit protein-tyrosine kinase
-
-
leukocyte tyrosine kinase receptor
-
leukocyte tyrosine kinase receptor
-
macrophage colony stimulating factor I receptor
-
macrophage colony stimulating factor I receptor
-
macrophage colony stimulating factor I receptor
-
macrophage colony stimulating factor I receptor
-
macrophage colony-stimulating factor receptor
-
-
macrophage colony-stimulating factor receptor
-
macrophage-stimulating protein receptor
-
macrophage-stimulating protein receptor
-
mast/stem cell growth factor receptor
-
mast/stem cell growth factor receptor
-
mast/stem cell growth factor receptor
-
mast/stem cell growth factor receptor
-
mast/stem cell growth factor receptor
-
mast/stem cell growth factor receptor
-
mast/stem cell growth factor receptor
-
MET
-
-
Met receptor-tyrosine kinase
-
-
Met receptor-tyrosine kinase
-
-
Met RTK
-
-
muscle-specific receptor tyrosine kinase
-
-
muscle-specific receptor tyrosine kinase
-
-
muscle-specific receptor tyrosine kinase
-
MuSK
-
-
NET
-
-
-
-
neurotrophin tyrosine receptor kinase
-
-
neurotrophin tyrosine receptor kinase
-
NT-3 growth factor receptor
-
NT-3 growth factor receptor
-
NT-3 growth factor receptor
-
NT-3 growth factor receptor
-
PDGF receptor
-
-
PDGF receptor tyrosine kinase
-
-
PDGF receptor tyrosine kinase
-
-
PDGF receptor tyrosine kinase
-
-
PDGFR
-
-
PDGFR-alpha
-
-
PDGFR-beta
-
-
PDGFRbeta
-
-
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
-
Protein tyrosine kinase
-
-
Protein tyrosine kinase
-
-
proto-oncogene tyrosine-protein kinase MER
-
proto-oncogene tyrosine-protein kinase MER
-
proto-oncogene tyrosine-protein kinase MER
-
proto-oncogene tyrosine-protein kinase receptor ret
-
proto-oncogene tyrosine-protein kinase receptor ret
-
PTK
-
-
recepteur d'origine nantais
-
-
recepteur d'origine nantais
-
recepteur d'origine nantais receptor tyrosine kinase
-
-
recepteur d'origine nantais receptor tyrosine kinase
-
-
receptor protein-tyrosine kinase erbB-2
-
receptor protein-tyrosine kinase erbB-2
-
receptor protein-tyrosine kinase erbB-2
-
receptor protein-tyrosine kinase erbB-3
-
receptor protein-tyrosine kinase erbB-3
-
receptor tyrosine kinase
-
receptor tyrosine kinase
-
-
receptor tyrosine kinase
-
receptor tyrosine kinase
Drosophila sp. (in: flies)
-
-
receptor tyrosine kinase
-
-
660727, 661669, 662678, 662679, 662856, 672173, 672948, 673212, 673570, 674071, 690295, 690447, 691595, 691636, 692230, 693346, 693727, 737744, 760845, 761882
receptor tyrosine kinase
-
receptor tyrosine kinase
-
receptor tyrosine kinase
-
receptor tyrosine kinase
-
receptor tyrosine kinase
-
receptor tyrosine kinase
-
receptor tyrosine kinase
-
receptor tyrosine kinase
-
-
receptor tyrosine kinase
-
-
receptor tyrosine kinase
-
receptor tyrosine kinase c-Kit
-
receptor tyrosine kinase c-Kit
-
receptor tyrosine kinase c-Kit
-
-
receptor tyrosine kinase EphA2
-
receptor tyrosine kinase EphA2
-
receptor tyrosine kinase RET
-
-
receptor tyrosine kinase RET
-
-
receptor tyrosine kinase Ror2
-
receptor tyrosine kinase Ror2
-
-
RET
-
-
Ret receptor tyrosine kinase
-
-
Ret receptor tyrosine kinase
-
-
Ron
-
-
RON receptor tyrosine kinase
-
-
RON receptor tyrosine kinase
-
-
RON receptor tyrosine kinase
-
-
RON receptor tyrosine kinase
-
-
RON receptor tyrosine kinase
-
RON receptor tyrosine kinase
-
-
RON receptor tyrosine kinase
-
-
RON receptor tyrosine kinase
-
RON receptor tyrosine kinase
-
-
RON receptor tyrosine kinase
-
-
RON receptor tyrosine kinase
-
-
RPTK
-
-
RTK
-
-
-
-
RTK
-
-
661669, 662856, 672173, 672948, 673212, 692230, 693346, 693727, 737744, 737815, 737818, 737823, 738414, 738624, 738744, 739054, 739206, 760845, 761882
RTKs
-
sevenless protein
-
Stem cell-derived tyrosine kinase
-
-
-
-
Stem cell-derived tyrosine kinase
-
-
STK
-
-
Tie1
-
-
Tie2
-
TrkA
-
-
trkB
-
-
TrkB receptor
-
-
TrkC
-
-
tyrosine-protein kinase Etk
-
tyrosine-protein kinase Etk
-
tyrosine-protein kinase Etk
-
tyrosine-protein kinase receptor Tie-1
-
tyrosine-protein kinase receptor Tie-1
-
tyrosine-protein kinase receptor Tie-1
-
tyrosine-protein kinase receptor TYRO3
-
tyrosine-protein kinase receptor TYRO3
-
tyrosine-protein kinase receptor TYRO3
-
tyrosine-protein kinase receptor UFO
-
tyrosine-protein kinase receptor UFO
-
tyrosine-protein kinase RYK
-
tyrosine-protein kinase RYK
-
tyrosine-protein kinase transforming protein erbB
-
tyrosine-protein kinase transforming protein erbB
-
tyrosine-protein kinase transforming protein erbB
-
-
tyrosine-protein kinase transforming protein erbB
-
-
tyrosine-protein kinase transforming protein erbB
-
tyrosine-protein kinase transforming protein kit
-
tyrosine-protein kinase transforming protein kit
-
-
tyrosine-protein kinase transmembrane receptor ROR1
-
tyrosine-protein kinase transmembrane receptor ROR1
-
tyrosine-protein kinase transmembrane receptor ROR2
-
tyrosine-protein kinase transmembrane receptor ROR2
-
tyrosine-protein kinase Wzc
-
tyrosine-protein kinase Wzc
-
tyrosine-protein kinase Wzc
-
-
tyrosine-protein kinase Wzc
-
tyrosine-protein kinase Wzc
-
vascular endothelial growth factor receptor
-
-
vascular endothelial growth factor receptor
-
vascular endothelial growth factor receptor
-
-
vascular endothelial growth factor receptor
-
vascular endothelial growth factor receptor
-
-
vascular endothelial growth factor receptor
-
vascular endothelial growth factor receptor 1
-
vascular endothelial growth factor receptor 1
-
vascular endothelial growth factor receptor 2
-
vascular endothelial growth factor receptor 2
-
-
vascular endothelial growth factor receptor 2
-
-
vascular endothelial growth factor receptor 2
-
vascular endothelial growth factor receptor 2
-
vascular endothelial growth factor receptor 2
-
vascular endothelial growth factor receptor 3
-
vascular endothelial growth factor receptor 3
-
VEGF receptor
-
VEGF receptor tyrosine kinase
-
-
VEGF receptor tyrosine kinase
-
-
VEGFR
-
-
VEGFR-2
-
-
VEGFR1
-
-
VEGFR2
-
-
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
the enzymes belong to the epidermal growth factor receptor family, i.e. EGFR/ErbB family
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ATP + a protein
ADP + a phosphoprotein
ATP + a [macrophage-stimulating protein]-L-tyrosine
ADP + a [macrophage-stimulating protein]-L-tyrosine phosphate
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
ATP + Ac-DYFE-6-chloro-W-NHMe
ADP + Ac-DYpFE-6-chloro-W-NHMe
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
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
-
-
-
-
?
ATP + G protein-coupled receptor kinase-2
ADP + phosphorylated G protein-coupled receptor kinase-2
ATP + insulin receptor substrate 1-L-tyrosine
ADP + insulin receptor substrate 1-L-tyrosine phosphate
ATP + insulin receptor substrate 2-L-tyrosine
ADP + insulin receptor substrate 2-L-tyrosine phosphate
-
-
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
-
commercial peptide substrate
-
-
?
ATP + KKSRGDYMTMQIG
ADP + KKSRGDY-phosphate-MTMQIG
-
commercial peptide substrate
-
-
?
ATP + NAEYLRV
ADP + NAE-phospho-Y-LRV
-
-
-
?
ATP + p130Cas-L-tyrosine
ADP + p130Cas-L-tyrosine phosphate
-
-
-
-
?
ATP + paxillin-L-tyrosine
ADP + paxillin-L-tyrosine phosphate
-
-
-
-
?
ATP + phosphatidylinositol 3-kinase
ADP + phosphorylated phosphatidylinositol 3-kinase
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
-
insulin-like growth factor-1 receptor directly interacts with and activates phosphoinositide-dependent kinase-1
-
-
?
ATP + phospholipase C gamma
ADP + phosphorylated phospholipase C gamma
ATP + phospholipase C gamma-L-tyrosine
ADP + phospholipase C gamma-L-tyrosine phosphate
-
-
-
-
?
ATP + poly(Glu-Ala-Tyr)
ADP + poly(Glu-Ala-Tyr)-L-tyrosine phosphate
-
-
-
-
?
ATP + poly(Glu:Tyr)
ADP + phosphorylated poly(Glu:Tyr)
-
-
-
?
ATP + poly(Glu:Tyr)
ADP + poly(Glu:Tyr) phosphate
-
-
-
-
?
ATP + poly-(Glu-Tyr)
ADP + poly-(Glu-Tyr) phosphate
-
-
Tyr-phosphate
-
?
ATP + poly-Ala-Glu-Lys-Tyr
ADP * poly-Ala-L-Glu-L-Lys-L-tyrosine phosphate
-
substrate used for c-Met
-
-
?
ATP + poly-Glu-Tyr
ADP + poly-L-Glu-L-tyrosine phosphate
-
substrate used for EGFR
-
-
?
ATP + protein
ADP + protein tyrosine phosphate
ATP + protein tyrosine
ADP + protein tyrosine phosphate
ATP + tyrosine-protein kinase Etp
ADP + phosphotyrosine-protein kinase Etp
-
-
-
?
ATP + tyrosine-protein kinase Wcz
ADP + phosphotyrosine-protein kinase Wcz
ATP + VPEYINQ
ADP + VPE-phosphoY-INQ
-
-
-
?
ATP + YFEW
ADP + YpFEW
tetrapeptide identified by substrate profiling
-
-
?
ATP + [beta-catenin]-Tyr142
ADP + [beta-catenin]-Tyr142 phosphate
-
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
-
EGFR tyrosine kinase
-
-
?
ATP + [flagellin]-L-tyrosine
ADP + [flagellin]-L-tyrosine phosphate
-
-
-
-
?
ATP + [gastrin]-L-tyrosine
ADP + [gastrin]-L-tyrosine phosphate
-
-
-
-
?
ATP + [minigastrin]-L-tyrosine
ADP + [minigastrin]-L-tyrosine phosphate
-
-
-
-
?
ATP + [poly-(Glu,Tyr)1:4]
ADP + [poly-(Glu,Tyr)1:4]-tyrosine phosphate
-
synthetic substrate
-
-
?
ATP + [vascular endothelial growth-factor-1]-L-tyrosine
ADP + [vascular endothelial growth-factor-1]-L-tyrosine phosphate
-
VEGFR-1 tyrosine kinase
-
-
?
poly(Glu:Tyr) + ATP
ADP + ?
-
-
-
-
?
poly(Glu:Tyr) + ATP
ADP + poly(Glu:Tyr) phosphate
-
-
-
-
?
additional information
?
-
ATP + a protein
ADP + a phosphoprotein
-
-
-
-
?
ATP + a protein
ADP + a phosphoprotein
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
660725, 660873, 660919, 660921, 661030, 661457, 662724, 662856, 671353, 672917, 673212, 674028, 674071, 674681, 676130, 677222, 677234, 703980, 704074, 705866, 737744, 737815, 737818, 737820, 737823, 737831, 738624 -
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
FLT-3 is involved in signal transduction, mechanisms
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
phosphorylation of downstream signalling proteins
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
regulation mechanisms and ligand binding, ligand binding induces a conformational change, overview
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
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
-
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
substrate binding and active structure
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
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
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
substrates are membrane and cytosolic proteins
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + G protein-coupled receptor kinase-2
ADP + phosphorylated G protein-coupled receptor kinase-2
-
GRK2 activation also increases GRK2 degradation and downregulation, independent of Gbetagamma subunits and phosphoinositide 3-kinase
-
-
?
ATP + G protein-coupled receptor kinase-2
ADP + phosphorylated G protein-coupled receptor kinase-2
-
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
-
peptide derived from the regulatory domain of insulin receptor
-
-
?
ATP + insulin receptor substrate 1-L-tyrosine
ADP + insulin receptor substrate 1-L-tyrosine phosphate
-
-
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 + phospholipase C gamma
ADP + phosphorylated phospholipase C gamma
-
-
?
ATP + phospholipase C gamma
ADP + phosphorylated phospholipase C gamma
-
-
?
ATP + phospholipase C gamma
ADP + phosphorylated phospholipase C gamma
growth factor-induced tyrosine phosphorylation of PLC gamma is essential for stimulation of phosphatidylinositol hydrolysis in vitro and in vivo
-
?
ATP + protein
ADP + protein tyrosine phosphate
autophosphorylation
-
-
?
ATP + protein
ADP + protein tyrosine phosphate
Y602 is a major site of in vitro autophosphorylation in Sek, Y596 is phosphorylated to a lower stoichiometry
-
-
?
ATP + protein
ADP + protein tyrosine phosphate
intrinsic autophosphorylation activity
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
autophosphorylation
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
protein kinase activity with specificity for tyrosine residues
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
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
specific for tyrosine
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
autophosphorylated on tyrosine and also mediated tyrosine phosphorylation of casein
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
autophosphorylation
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
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
IRS-1 and IRS-2 proteins serve as substrates
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
autophosphorylation
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
phospholipase C-gamma 1 is directly phosphorylated by TrkB
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
major sites of autophosphorylation are in the region containing Tyr670, Tyr674, and Tyr675
-
-
?
ATP + tyrosine-protein kinase Wcz
ADP + phosphotyrosine-protein kinase Wcz
autophosphorylation
-
-
?
ATP + tyrosine-protein kinase Wcz
ADP + phosphotyrosine-protein kinase Wcz
-
autophosphorylation
-
-
?
ATP + tyrosine-protein kinase Wcz
ADP + phosphotyrosine-protein kinase Wcz
autophosphorylation at several tyrosine residues
-
-
?
ATP + tyrosine-protein kinase Wcz
ADP + phosphotyrosine-protein kinase Wcz
presence of at least five isoforms, all phosphorylated exclusively at tyrosine supports the concept that autophosphorylation occurs at multiple sites within the protein
-
-
?
ATP + tyrosine-protein kinase Wcz
ADP + phosphotyrosine-protein kinase Wcz
autophosphorylation
-
-
?
ATP + tyrosine-protein kinase Wcz
ADP + phosphotyrosine-protein kinase Wcz
autophosphorylation
-
-
?
ATP + tyrosine-protein kinase Wcz
ADP + phosphotyrosine-protein kinase Wcz
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
efficient autophosphorylation in presence of ATP
-
-
?
additional information
?
-
no phosphorylation of synthetic substrates such as poly(Glu80 Tyr20) or angiotensin II
-
-
?
additional information
?
-
-
no phosphorylation of synthetic substrates such as poly(Glu80 Tyr20) or angiotensin II
-
-
?
additional information
?
-
possible involvement of the enzyme in cell recognition and bacterial pathogenicity
-
-
?
additional information
?
-
-
possible involvement of the enzyme in cell recognition and bacterial pathogenicity
-
-
?
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
?
-
transformation of fibroblasts and transformation of erythroid cells
-
-
?
additional information
?
-
the erB oncogene efficiently transforms erythroblasts
-
-
?
additional information
?
-
-
the erB oncogene efficiently transforms erythroblasts
-
-
?
additional information
?
-
the erB oncogene efficiently transforms erythroblasts
-
-
?
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
?
-
transformation of fibroblasts and transformation of erythroid cells
-
-
?
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
?
-
autophosphorylation
-
-
?
additional information
?
-
-
autophosphorylation
-
-
?
additional information
?
-
functions in neural and epithelial morphogenesis
-
-
?
additional information
?
-
-
functions in neural and epithelial morphogenesis
-
-
?
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
?
-
-
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
?
-
may be specifically involved in cell-cell interactions regulating cell fusions that generate the hypodermis during postembryonic development
-
-
?
additional information
?
-
may be specifically involved in cell-cell interactions regulating cell fusions that generate the hypodermis during postembryonic development
-
-
?
additional information
?
-
receptor for the inductive signal required for vulval development
-
-
?
additional information
?
-
-
receptor for the inductive signal required for vulval development
-
-
?
additional information
?
-
acts through a conserved Ras/MAP kinase signaling pathway to induce vulval differentiation
-
-
?
additional information
?
-
-
acts through a conserved Ras/MAP kinase signaling pathway to induce vulval differentiation
-
-
?
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
?
-
-
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
?
-
may play a role in cell-cell interactions involved in retinotectal projections and differentiation of the central nervous system
-
-
?
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
?
-
generalized function of the Zek1 receptor in neuronal cell ontogeny
-
-
?
additional information
?
-
-
generalized function of the Zek1 receptor in neuronal cell ontogeny
-
-
?
additional information
?
-
important role in neurogenesis
-
-
?
additional information
?
-
the neurotrophic receptor may function during early stages of neural development
-
-
?
additional information
?
-
Dnrk may play an important role in neural development during Drosophila embryogenesis
-
-
?
additional information
?
-
essential for migration of tracheal and specific midline glial cells
-
-
?
additional information
?
-
required for directed tracheal cell extension
-
-
?
additional information
?
-
part of a novel signal transduction cascade involved in learning and memory
-
-
?
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
?
-
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
?
-
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
?
-
sevenless gene determines the fate of a single photoreceptor cell type in the eye of Drosophila
-
-
?
additional information
?
-
enzyme is required for normal eye development
-
-
?
additional information
?
-
-
enzyme is required for normal eye development
-
-
?
additional information
?
-
enzyme is involved in signal transduction
-
-
?
additional information
?
-
involved in exopolysaccharide production and virulence
-
-
?
additional information
?
-
-
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
?
-
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
?
-
-
mutations in the glycine-riche loop of MET can cause papillary renal-cell carcinomas
-
-
?
additional information
?
-
-
protein kinases and protein phosphatases regulate enzyme activities in the cell, regulation mechanisms, overview
-
-
?
additional information
?
-
-
poor activity on free amino acids, consensus sequence of InRK is YM-MM, and of EGFR E-EEYF
-
-
?
additional information
?
-
may play an important role during development and in signal transduction pathways
-
-
?
additional information
?
-
-
may play an important role during development and in signal transduction pathways
-
-
?
additional information
?
-
Cek9 plays an active role in embryonic signal transduction pathways
-
-
?
additional information
?
-
-
Cek9 plays an active role in embryonic signal transduction pathways
-
-
?
additional information
?
-
Cek8 suggests its involvement in cellular survival or cell-cell interactions for specific subpopulations of developing motoneurons
-
-
?
additional information
?
-
autophosphorylation
-
-
?
additional information
?
-
autophosphorylation
-
-
?
additional information
?
-
-
autophosphorylation
-
-
?
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
?
-
-
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
?
-
involved in cell-cell interactions
-
-
?
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
?
-
-
mutations in MERTK, the human orthologue of the RCS rat retinal dystrophy gene, cause retinitis pigmentosa
-
-
?
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
?
-
-
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
?
-
plays an important role in cell growth control
-
-
?
additional information
?
-
-
plays an important role in cell growth control
-
-
?
additional information
?
-
implicated in the control of cell growth and differentiation
-
-
?
additional information
?
-
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
?
-
-
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
?
-
-
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
?
-
-
missense mutations located in the MET proto-oncogene lead to constitutive activation of the MET protein and papillary renal carcinomas
-
-
?
additional information
?
-
functions as a cell surface receptor for an as yet unidentified ligand
-
-
?
additional information
?
-
-
functions as a cell surface receptor for an as yet unidentified ligand
-
-
?
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
?
-
-
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
?
-
-
human piebald trait resulting from a dominant negative mutant allele of the c-kit membrane receptor gene
-
-
?
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 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
?
-
Jackson-Weiss syndrome and Crouzon syndrome are allelic with mutations in fibroblast growth factor receptor 2
-
-
?
additional information
?
-
-
Jackson-Weiss syndrome and Crouzon syndrome are allelic with mutations in fibroblast growth factor receptor 2
-
-
?
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
?
-
-
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
?
-
ephrin type-A receptor 1 may be involved in the neoplastic process of some tumors
-
-
?
additional information
?
-
-
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
?
-
-
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
?
-
-
FGFR-4 binds acidic fibroblast growth factor with high affinity but does not bind basic fibroblast growth factor
-
-
?
additional information
?
-
tk gene product likely functions as a cell surface receptor for an unidentified cellular growth factor
-
-
?
additional information
?
-
-
tk gene product likely functions as a cell surface receptor for an unidentified cellular growth factor
-
-
?
additional information
?
-
receptors for at least two hematopoietic growth factors: the stem cell factor and the colony-stimulating factor 1
-
-
?
additional information
?
-
-
receptors for at least two hematopoietic growth factors: the stem cell factor and the colony-stimulating factor 1
-
-
?
additional information
?
-
gene plays important role in embryonic development and carcinogenesis of the stomach
-
-
?
additional information
?
-
-
gene plays important role in embryonic development and carcinogenesis of the stomach
-
-
?
additional information
?
-
may be involved in tumor progression of epithelial ovarian cancer
-
-
?
additional information
?
-
-
may be involved in tumor progression of epithelial ovarian cancer
-
-
?
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
?
-
-
plays a part in human neurogenesis, DRT gene may play a part in neuroblastoma and SCLC tumorigenesis
-
-
?
additional information
?
-
element of the complex signaling network involved in the control of cell proliferation and differentiation
-
-
?
additional information
?
-
-
element of the complex signaling network involved in the control of cell proliferation and differentiation
-
-
?
additional information
?
-
may have a role in tumorigenesis
-
-
?
additional information
?
-
-
may have a role in tumorigenesis
-
-
?
additional information
?
-
involved in the proliferation of early progenitor/stem cells
-
-
?
additional information
?
-
-
involved in the proliferation of early progenitor/stem cells
-
-
?
additional information
?
-
Srcasm may help promote Src family kinase signaling in cells
-
-
?
additional information
?
-
enzyme is implicated in control of cell growth
-
-
?
additional information
?
-
NET potentially plays important roles in human neurogenesis
-
-
?
additional information
?
-
-
NET potentially plays important roles in human neurogenesis
-
-
?
additional information
?
-
role for the Ron receptor in progression toward malignancy
-
-
?
additional information
?
-
-
role for the Ron receptor in progression toward malignancy
-
-
?
additional information
?
-
distinct mutations in the receptor tyrosine kinase gene ROR2 cause brachydactyly type B
-
-
?
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
?
-
-
recessive Robinow syndrome, allelic to dominant brachydactyly type B, is caused by loss of ROR2 activity
-
-
?
additional information
?
-
dominant mutations in ROR2, encoding an orphan receptor tyrosine kinase, cause brachydactyly type B
-
-
?
additional information
?
-
-
dominant mutations in ROR2, encoding an orphan receptor tyrosine kinase, cause brachydactyly type B
-
-
?
additional information
?
-
ron gene product is a specific cell-surface receptor for macrophage-stimulating protein
-
-
?
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
?
-
-
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
?
-
-
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
?
-
-
Sky may be involved in cell adhesion processes, particularly in the central nervous system
-
-
?
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
?
-
-
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
?
-
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
?
-
-
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
?
-
-
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 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
?
-
-
serotonin 5-HT2c receptor signaling is largely independent from receptor tyrosine kinase activity
-
-
?
additional information
?
-
ErbB1 receptor shows three phosphorylation sites (Y1110, Y1172 and Y1192)
-
-
?
additional information
?
-
-
ErbB1 receptor shows three phosphorylation sites (Y1110, Y1172 and Y1192)
-
-
?
additional information
?
-
protein tyrosine kinases select substrates with a glutamic acid at the P-1 position and a large hydrophobic amino acid at the P+1 position
-
-
?
additional information
?
-
-
substrate recognition and binding structure, the enzyme depends on basic residues for substrate recognition, substrate specificity determinants in substrates
-
-
?
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
?
-
-
-
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
tyrosine kinase may play an important function in the developing mouse
-
-
?
additional information
?
-
-
tyrosine kinase may play an important function in the developing mouse
-
-
?
additional information
?
-
important role in the formation of neuronal structures and possibly other morphogenic processes
-
-
?
additional information
?
-
-
important role in the formation of neuronal structures and possibly other morphogenic processes
-
-
?
additional information
?
-
receptor may play a role in the regulation of beta-cell mass
-
-
?
additional information
?
-
-
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
?
-
required for cartilage and growth plate development
-
-
?
additional information
?
-
-
required for cartilage and growth plate development
-
-
?
additional information
?
-
the proto-oncogene c-kit is involved in signal transduction
-
-
?
additional information
?
-
-
the proto-oncogene c-kit is involved in signal transduction
-
-
?
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
?
-
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
?
-
-
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
?
-
trkB may code for a cell surface receptor involved in neurogenesis
-
-
?
additional information
?
-
-
trkB may code for a cell surface receptor involved in neurogenesis
-
-
?
additional information
?
-
may play a role in vascular development and regulation of vascular permeability
-
-
?
additional information
?
-
-
may play a role in vascular development and regulation of vascular permeability
-
-
?
additional information
?
-
Flk-1 as a major regulator of vasculogenesis and angiogenesis
-
-
?
additional information
?
-
-
Flk-1 as a major regulator of vasculogenesis and angiogenesis
-
-
?
additional information
?
-
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
?
-
-
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
?
-
may play an important role during development and in signal transduction pathways
-
-
?
additional information
?
-
-
may play an important role during development and in signal transduction pathways
-
-
?
additional information
?
-
receptor may be a key signal transducing component in the totipotent hematopoietic stem cell and its immediate self-renewing progeny
-
-
?
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
?
-
-
tyro3 may function as a novel neurotrophic factor receptor
-
-
?
additional information
?
-
important role in gestational growth and differentiation
-
-
?
additional information
?
-
important role in gestational growth and differentiation
-
-
?
additional information
?
-
-
important role in gestational growth and differentiation
-
-
?
additional information
?
-
ALK plays an important role in the development of the brain
-
-
?
additional information
?
-
-
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
?
-
primary function is likely to be in developmental regulation
-
-
?
additional information
?
-
-
primary function is likely to be in developmental regulation
-
-
?
additional information
?
-
role for Tsk in early T-lymphocyte differentiation
-
-
?
additional information
?
-
-
role for Tsk in early T-lymphocyte differentiation
-
-
?
additional information
?
-
the mouse waved-2 phenotype results from a point mutation in the EGF receptor tyrosine kinase
-
-
?
additional information
?
-
-
the mouse waved-2 phenotype results from a point mutation in the EGF receptor tyrosine kinase
-
-
?
additional information
?
-
ufo may function as a signal transducer between specific cell types of mesodermal origin
-
-
?
additional information
?
-
-
ufo may function as a signal transducer between specific cell types of mesodermal origin
-
-
?
additional information
?
-
tek receptor tyrosine kinase may be critically involved in the determination and/or maintenance of cells of the endothelial lineage
-
-
?
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
?
-
-
itk functions in a signal transduction pathway unique to T lymphocytes
-
-
?
additional information
?
-
expression of the EGF-R gene in mouse blastocysts is tightly regulated by maternal steroid hormonal status
-
-
?
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
?
-
-
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
?
-
-
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
?
-
-
antagonistic regulation of swelling-activated Cl- current in rabbit ventricle by Src and EGFR protein tyrosine kinases, overview
-
-
?
additional information
?
-
-
-
-
?
additional information
?
-
-
-
-
?
additional information
?
-
may play an important role in the generation of the mammalian nervous system
-
-
?
additional information
?
-
receptor of neuregulin
-
-
?
additional information
?
-
expression of neuregulins and their putative receptor ErbB3, is induced during Wallerian degeneration
-
-
?
additional information
?
-
expression of neuregulins and their putative receptor ErbB3, is induced during Wallerian degeneration
-
-
?
additional information
?
-
receptor for an as yet unidentified growth factor
-
-
?
additional information
?
-
Elk tyrosine kinase may be involved in cell-cell interactions in the nervous system
-
-
?
additional information
?
-
enzyme is involved in glial cell generation
-
-
?
additional information
?
-
signal transducing receptor for nerve growth factor
-
-
?
additional information
?
-
increased ERBB3 expression may play a role in some human malignancies
-
-
?
additional information
?
-
inhibition of vascular smooth muscle cell growth through antisense transcription of a rat insulin-like growth factor I receptor cDNA
-
-
?
additional information
?
-
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
?
-
rat trkC locus encodes multiple neurogenic receptors that exhibit differential response to neurotrophin-3 in PC12 cells
-
-
?
additional information
?
-
mrfms gene products may play a role in the normal and neoplastic growth of muscular cells
-
-
?
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
?
-
-
the enzyme epidermal growth factor receptor tyrosine kinase is involved in signal transduction in cardiac preconditioning, mechanisms, enzyme inhibition is cardioprotective
-
-
?
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
?
-
gp145trkC may play an important role in mediating the neurotrophic effects of NT-3
-
-
?
additional information
?
-
Sek-1, perhaps with other Eph-related receptors, is required for interactions that regulate the segmental identity or movement of cells
-
-
?
additional information
?
-
Pag may play a role in the differentiation of cranial neural crest and other tissues
-
-
?
additional information
?
-
-
Pag may play a role in the differentiation of cranial neural crest and other tissues
-
-
?
additional information
?
-
may play a role in the development or function of the central nervous system
-
-
?
additional information
?
-
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
?
-
-
autophosphorylation of the insulin receptor via its protein tyrosine kinase activity, regulation mechanism
-
-
?
additional information
?
-
malignant melanoma in Xiphophorus fish hybrids is caused by the activity of a dominant oncogene Tu which codes for a receptor tyrosine kinase
-
-
?
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
ATP + a protein
ADP + a phosphoprotein
ATP + a [macrophage-stimulating protein]-L-tyrosine
ADP + a [macrophage-stimulating protein]-L-tyrosine phosphate
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
ATP + cortactin-L-tyrosine
ADP + cortactin-L-tyrosine phosphate
-
-
-
-
?
ATP + G protein-coupled receptor kinase-2
ADP + phosphorylated G protein-coupled receptor kinase-2
-
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
-
-
-
-
?
ATP + paxillin-L-tyrosine
ADP + paxillin-L-tyrosine phosphate
-
-
-
-
?
ATP + phospholipase C gamma
ADP + phosphorylated phospholipase C gamma
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
-
-
-
-
?
ATP + poly(Glu:Tyr)
ADP + poly(Glu:Tyr) phosphate
-
-
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
ATP + [beta-catenin]-Tyr142
ADP + [beta-catenin]-Tyr142 phosphate
-
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
-
EGFR tyrosine kinase
-
-
?
ATP + [vascular endothelial growth-factor-1]-L-tyrosine
ADP + [vascular endothelial growth-factor-1]-L-tyrosine phosphate
-
VEGFR-1 tyrosine kinase
-
-
?
additional information
?
-
ATP + a protein
ADP + a phosphoprotein
-
-
-
-
?
ATP + a protein
ADP + a phosphoprotein
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
660725, 661030, 662724, 671353, 672917, 673212, 674028, 674071, 674681, 676130, 677222, 677234, 703980, 704074, 705866, 737744, 737815, 737818, 737820, 737823, 737831, 738624 -
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
FLT-3 is involved in signal transduction, mechanisms
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
phosphorylation of downstream signalling proteins
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
regulation mechanisms and ligand binding, ligand binding induces a conformational change, overview
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
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
-
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
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
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
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
autophosphorylated on tyrosine and also mediated tyrosine phosphorylation of casein
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
phospholipase C-gamma 1 is directly phosphorylated by TrkB
-
?
additional information
?
-
possible involvement of the enzyme in cell recognition and bacterial pathogenicity
-
-
?
additional information
?
-
-
possible involvement of the enzyme in cell recognition and bacterial pathogenicity
-
-
?
additional information
?
-
transformation of fibroblasts and transformation of erythroid cells
-
-
?
additional information
?
-
the erB oncogene efficiently transforms erythroblasts
-
-
?
additional information
?
-
-
the erB oncogene efficiently transforms erythroblasts
-
-
?
additional information
?
-
the erB oncogene efficiently transforms erythroblasts
-
-
?
additional information
?
-
transformation of fibroblasts and transformation of erythroid cells
-
-
?
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
?
-
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
?
-
-
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
?
-
may be specifically involved in cell-cell interactions regulating cell fusions that generate the hypodermis during postembryonic development
-
-
?
additional information
?
-
may be specifically involved in cell-cell interactions regulating cell fusions that generate the hypodermis during postembryonic development
-
-
?
additional information
?
-
receptor for the inductive signal required for vulval development
-
-
?
additional information
?
-
-
receptor for the inductive signal required for vulval development
-
-
?
additional information
?
-
acts through a conserved Ras/MAP kinase signaling pathway to induce vulval differentiation
-
-
?
additional information
?
-
-
acts through a conserved Ras/MAP kinase signaling pathway to induce vulval differentiation
-
-
?
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
?
-
-
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
?
-
may play a role in cell-cell interactions involved in retinotectal projections and differentiation of the central nervous system
-
-
?
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
?
-
important role in neurogenesis
-
-
?
additional information
?
-
the neurotrophic receptor may function during early stages of neural development
-
-
?
additional information
?
-
Dnrk may play an important role in neural development during Drosophila embryogenesis
-
-
?
additional information
?
-
essential for migration of tracheal and specific midline glial cells
-
-
?
additional information
?
-
required for directed tracheal cell extension
-
-
?
additional information
?
-
part of a novel signal transduction cascade involved in learning and memory
-
-
?
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
?
-
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
?
-
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
?
-
sevenless gene determines the fate of a single photoreceptor cell type in the eye of Drosophila
-
-
?
additional information
?
-
enzyme is required for normal eye development
-
-
?
additional information
?
-
-
enzyme is required for normal eye development
-
-
?
additional information
?
-
enzyme is involved in signal transduction
-
-
?
additional information
?
-
involved in exopolysaccharide production and virulence
-
-
?
additional information
?
-
-
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
?
-
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
?
-
-
mutations in the glycine-riche loop of MET can cause papillary renal-cell carcinomas
-
-
?
additional information
?
-
-
protein kinases and protein phosphatases regulate enzyme activities in the cell, regulation mechanisms, overview
-
-
?
additional information
?
-
may play an important role during development and in signal transduction pathways
-
-
?
additional information
?
-
-
may play an important role during development and in signal transduction pathways
-
-
?
additional information
?
-
Cek9 plays an active role in embryonic signal transduction pathways
-
-
?
additional information
?
-
-
Cek9 plays an active role in embryonic signal transduction pathways
-
-
?
additional information
?
-
Cek8 suggests its involvement in cellular survival or cell-cell interactions for specific subpopulations of developing motoneurons
-
-
?
additional information
?
-
involved in cell-cell interactions
-
-
?
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
?
-
-
mutations in MERTK, the human orthologue of the RCS rat retinal dystrophy gene, cause retinitis pigmentosa
-
-
?
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
?
-
-
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
?
-
plays an important role in cell growth control
-
-
?
additional information
?
-
-
plays an important role in cell growth control
-
-
?
additional information
?
-
implicated in the control of cell growth and differentiation
-
-
?
additional information
?
-
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
?
-
-
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
?
-
-
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
?
-
-
missense mutations located in the MET proto-oncogene lead to constitutive activation of the MET protein and papillary renal carcinomas
-
-
?
additional information
?
-
functions as a cell surface receptor for an as yet unidentified ligand
-
-
?
additional information
?
-
-
functions as a cell surface receptor for an as yet unidentified ligand
-
-
?
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
?
-
-
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
?
-
-
human piebald trait resulting from a dominant negative mutant allele of the c-kit membrane receptor gene
-
-
?
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 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
?
-
Jackson-Weiss syndrome and Crouzon syndrome are allelic with mutations in fibroblast growth factor receptor 2
-
-
?
additional information
?
-
-
Jackson-Weiss syndrome and Crouzon syndrome are allelic with mutations in fibroblast growth factor receptor 2
-
-
?
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
?
-
-
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
?
-
ephrin type-A receptor 1 may be involved in the neoplastic process of some tumors
-
-
?
additional information
?
-
-
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
?
-
-
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
?
-
-
FGFR-4 binds acidic fibroblast growth factor with high affinity but does not bind basic fibroblast growth factor
-
-
?
additional information
?
-
tk gene product likely functions as a cell surface receptor for an unidentified cellular growth factor
-
-
?
additional information
?
-
-
tk gene product likely functions as a cell surface receptor for an unidentified cellular growth factor
-
-
?
additional information
?
-
receptors for at least two hematopoietic growth factors: the stem cell factor and the colony-stimulating factor 1
-
-
?
additional information
?
-
-
receptors for at least two hematopoietic growth factors: the stem cell factor and the colony-stimulating factor 1
-
-
?
additional information
?
-
gene plays important role in embryonic development and carcinogenesis of the stomach
-
-
?
additional information
?
-
-
gene plays important role in embryonic development and carcinogenesis of the stomach
-
-
?
additional information
?
-
may be involved in tumor progression of epithelial ovarian cancer
-
-
?
additional information
?
-
-
may be involved in tumor progression of epithelial ovarian cancer
-
-
?
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
?
-
-
plays a part in human neurogenesis, DRT gene may play a part in neuroblastoma and SCLC tumorigenesis
-
-
?
additional information
?
-
element of the complex signaling network involved in the control of cell proliferation and differentiation
-
-
?
additional information
?
-
-
element of the complex signaling network involved in the control of cell proliferation and differentiation
-
-
?
additional information
?
-
may have a role in tumorigenesis
-
-
?
additional information
?
-
-
may have a role in tumorigenesis
-
-
?
additional information
?
-
involved in the proliferation of early progenitor/stem cells
-
-
?
additional information
?
-
-
involved in the proliferation of early progenitor/stem cells
-
-
?
additional information
?
-
Srcasm may help promote Src family kinase signaling in cells
-
-
?
additional information
?
-
enzyme is implicated in control of cell growth
-
-
?
additional information
?
-
NET potentially plays important roles in human neurogenesis
-
-
?
additional information
?
-
-
NET potentially plays important roles in human neurogenesis
-
-
?
additional information
?
-
role for the Ron receptor in progression toward malignancy
-
-
?
additional information
?
-
-
role for the Ron receptor in progression toward malignancy
-
-
?
additional information
?
-
distinct mutations in the receptor tyrosine kinase gene ROR2 cause brachydactyly type B
-
-
?
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
?
-
-
recessive Robinow syndrome, allelic to dominant brachydactyly type B, is caused by loss of ROR2 activity
-
-
?
additional information
?
-
dominant mutations in ROR2, encoding an orphan receptor tyrosine kinase, cause brachydactyly type B
-
-
?
additional information
?
-
-
dominant mutations in ROR2, encoding an orphan receptor tyrosine kinase, cause brachydactyly type B
-
-
?
additional information
?
-
ron gene product is a specific cell-surface receptor for macrophage-stimulating protein
-
-
?
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
?
-
-
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
?
-
-
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
?
-
-
Sky may be involved in cell adhesion processes, particularly in the central nervous system
-
-
?
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
?
-
-
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
?
-
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
?
-
-
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
?
-
-
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 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
?
-
-
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
?
-
-
-
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
tyrosine kinase may play an important function in the developing mouse
-
-
?
additional information
?
-
-
tyrosine kinase may play an important function in the developing mouse
-
-
?
additional information
?
-
important role in the formation of neuronal structures and possibly other morphogenic processes
-
-
?
additional information
?
-
-
important role in the formation of neuronal structures and possibly other morphogenic processes
-
-
?
additional information
?
-
receptor may play a role in the regulation of beta-cell mass
-
-
?
additional information
?
-
-
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
?
-
required for cartilage and growth plate development
-
-
?
additional information
?
-
-
required for cartilage and growth plate development
-
-
?
additional information
?
-
the proto-oncogene c-kit is involved in signal transduction
-
-
?
additional information
?
-
-
the proto-oncogene c-kit is involved in signal transduction
-
-
?
additional information
?
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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
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?
additional information
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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
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?
additional information
?
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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
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?
additional information
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trkB may code for a cell surface receptor involved in neurogenesis
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?
additional information
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trkB may code for a cell surface receptor involved in neurogenesis
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?
additional information
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may play a role in vascular development and regulation of vascular permeability
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?
additional information
?
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may play a role in vascular development and regulation of vascular permeability
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?
additional information
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Flk-1 as a major regulator of vasculogenesis and angiogenesis
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?
additional information
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Flk-1 as a major regulator of vasculogenesis and angiogenesis
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?
additional information
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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
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?
additional information
?
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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
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?
additional information
?
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may play an important role during development and in signal transduction pathways
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?
additional information
?
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may play an important role during development and in signal transduction pathways
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?
additional information
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receptor may be a key signal transducing component in the totipotent hematopoietic stem cell and its immediate self-renewing progeny
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?
additional information
?
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receptor may be a key signal transducing component in the totipotent hematopoietic stem cell and its immediate self-renewing progeny
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?
additional information
?
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possible role for repulsive B-class Eph receptor/ligand interactions in constraining the orientation of longitudinal axon projections at the ventral midline
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?
additional information
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tyro3 may function as a novel neurotrophic factor receptor
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?
additional information
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tyro3 may function as a novel neurotrophic factor receptor
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?
additional information
?
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important role in gestational growth and differentiation
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?
additional information
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important role in gestational growth and differentiation
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?
additional information
?
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important role in gestational growth and differentiation
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?
additional information
?
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ALK plays an important role in the development of the brain
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?
additional information
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ALK plays an important role in the development of the brain
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?
additional information
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important role for this kinase in CD2 co-stimulation of T cell responses
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?
additional information
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primary function is likely to be in developmental regulation
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?
additional information
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primary function is likely to be in developmental regulation
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?
additional information
?
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role for Tsk in early T-lymphocyte differentiation
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?
additional information
?
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role for Tsk in early T-lymphocyte differentiation
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?
additional information
?
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the mouse waved-2 phenotype results from a point mutation in the EGF receptor tyrosine kinase
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?
additional information
?
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the mouse waved-2 phenotype results from a point mutation in the EGF receptor tyrosine kinase
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?
additional information
?
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ufo may function as a signal transducer between specific cell types of mesodermal origin
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?
additional information
?
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ufo may function as a signal transducer between specific cell types of mesodermal origin
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?
additional information
?
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tek receptor tyrosine kinase may be critically involved in the determination and/or maintenance of cells of the endothelial lineage
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?
additional information
?
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tek receptor tyrosine kinase may be critically involved in the determination and/or maintenance of cells of the endothelial lineage
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?
additional information
?
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itk functions in a signal transduction pathway unique to T lymphocytes
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?
additional information
?
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itk functions in a signal transduction pathway unique to T lymphocytes
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?
additional information
?
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expression of the EGF-R gene in mouse blastocysts is tightly regulated by maternal steroid hormonal status
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?
additional information
?
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expression of the EGF-R gene in mouse blastocysts is tightly regulated by maternal steroid hormonal status
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?
additional information
?
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Emt/Itk is a protein tyrosine kinase required for T cell Ag receptor TCR-induced activation and development
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?
additional information
?
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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
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?
additional information
?
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antagonistic regulation of swelling-activated Cl- current in rabbit ventricle by Src and EGFR protein tyrosine kinases, overview
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?
additional information
?
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?
additional information
?
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?
additional information
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may play an important role in the generation of the mammalian nervous system
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?
additional information
?
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receptor of neuregulin
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?
additional information
?
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expression of neuregulins and their putative receptor ErbB3, is induced during Wallerian degeneration
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?
additional information
?
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expression of neuregulins and their putative receptor ErbB3, is induced during Wallerian degeneration
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?
additional information
?
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receptor for an as yet unidentified growth factor
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?
additional information
?
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Elk tyrosine kinase may be involved in cell-cell interactions in the nervous system
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?
additional information
?
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enzyme is involved in glial cell generation
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?
additional information
?
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signal transducing receptor for nerve growth factor
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?
additional information
?
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increased ERBB3 expression may play a role in some human malignancies
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?
additional information
?
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inhibition of vascular smooth muscle cell growth through antisense transcription of a rat insulin-like growth factor I receptor cDNA
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?
additional information
?
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tyrosine kinase receptor for hepatocyte growth factor
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?
additional information
?
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increased c-met expression indicates that this gene may participate in the healing process of gastric mucosa after injury
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?
additional information
?
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rat trkC locus encodes multiple neurogenic receptors that exhibit differential response to neurotrophin-3 in PC12 cells
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?
additional information
?
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mrfms gene products may play a role in the normal and neoplastic growth of muscular cells
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?
additional information
?
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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
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?
additional information
?
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the enzyme epidermal growth factor receptor tyrosine kinase is involved in signal transduction in cardiac preconditioning, mechanisms, enzyme inhibition is cardioprotective
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?
additional information
?
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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
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?
additional information
?
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gp145trkC may play an important role in mediating the neurotrophic effects of NT-3
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?
additional information
?
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Sek-1, perhaps with other Eph-related receptors, is required for interactions that regulate the segmental identity or movement of cells
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?
additional information
?
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Pag may play a role in the differentiation of cranial neural crest and other tissues
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?
additional information
?
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Pag may play a role in the differentiation of cranial neural crest and other tissues
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?
additional information
?
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may play a role in the development or function of the central nervous system
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?
additional information
?
-
ectodermally produced PDGF A may act on the mesoderm during gastrulation and mesoderm induction establishes the tissue pattern of ligand and receptor expression
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?
additional information
?
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malignant melanoma in Xiphophorus fish hybrids is caused by the activity of a dominant oncogene Tu which codes for a receptor tyrosine kinase
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?
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(2R)-2-[(4-[[1-(1,3-thiazol-4-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
(2R)-2-[(4-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]-N,N-dimethylpropanamide
-
(2R)-2-[(4-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]-N-methylpropanamide
-
(2R)-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
(2R)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N,N-dimethylpropanamide
-
-
(2R)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N-(2-hydroxyethyl)-N-methylpropanamide
-
-
(2R)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N-methylpropanamide
-
-
(2R)-N,N-dimethyl-2-[(4-[[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
(2R)-N,N-dimethyl-2-[(4-[[1-(1,3-thiazol-4-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
(2R)-N,N-dimethyl-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
(2R)-N,N-dimethyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
(2R)-N-(2-hydroxyethyl)-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
-
-
(2R)-N-(2-hydroxyethyl)-N-methyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
-
-
(2R)-N-(2-methoxyethyl)-N-methyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
-
-
(2R)-N-methyl-2-[(4-[[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
(2R)-N-methyl-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
(2S)-2-[(4-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]-N,N-dimethylpropanamide
-
(2S)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N,N-dimethylpropanamide
-
-
(2S)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N-(2-hydroxyethyl)-N-methylpropanamide
-
-
(2S)-N,N-dimethyl-2-[(4-[[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
(2S)-N,N-dimethyl-2-[(4-[[1-(1,3-thiazol-4-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
(2S)-N,N-dimethyl-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
(2S)-N,N-dimethyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
-
-
(2S)-N-(2-hydroxyethyl)-N-methyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
-
-
(3Z)-3-[(3,5-dimethyl-1H-pyrrol-2-yl)methylidene]-1,3-dihydro-2H-indol-2-one
-
-
(3Z)-3-[3-([1,4'-bipiperidine]-1'-carbonyl)-2-methyl-1,4,5,6-tetrahydro-7H-indol-7-ylidene]-5-fluoro-1,3-dihydro-2H-indol-2-one
-
-
(3Z)-5-fluoro-3-(2-methyl-3-[(2S)-2-[(pyrrolidin-1-yl)methyl]pyrrolidine-1-carbonyl]-1,4,5,6-tetrahydro-7H-indol-7-ylidene)-1,3-dihydro-2H-indol-2-one
-
-
(3Z)-5-fluoro-3-[2-methyl-3-(morpholine-4-carbonyl)-1,4,5,6-tetrahydro-7H-indol-7-ylidene]-1,3-dihydro-2H-indol-2-one
-
-
(3Z)-5-[(1-ethylpiperidin-4-yl)amino]-3-[(5-methoxy-1H-benzimidazol-2-yl)(phenyl)methylidene]-1,3-dihydro-2H-indol-2-one
-
-
(7Z)-7-(5-bromo-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-N-[2-(diethylamino)ethyl]-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-7-(5-chloro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-N-[2-(diethylamino)ethyl]-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[2-(morpholin-4-yl)ethyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[2-(piperidin-1-yl)ethyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[2-(pyridin-2-yl)ethyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[2-(pyrrolidin-1-yl)ethyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[3-(pyrrolidin-1-yl)propyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-N-(2-hydroxyethyl)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-N-[2-(diethylamino)ethyl]-2-methyl-7-(2-oxo-1,2-dihydro-3H-indol-3-ylidene)-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-N-[2-(diethylamino)ethyl]-2-methyl-7-(5-methyl-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-N-[2-(diethylamino)ethyl]-2-methyl-7-(5-nitro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-N-[2-(diethylamino)ethyl]-7-(4-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-N-[2-(diethylamino)ethyl]-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-N-[2-(diethylamino)ethyl]-7-(5-methoxy-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-N-[2-(diethylamino)ethyl]-7-(5-[[(diethylamino)oxy]sulfinyl]-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-N-[2-(diethylamino)ethyl]-7-(7-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-N-[2-(dimethylamino)ethyl]-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-N-[3-(diethylamino)-2-hydroxypropyl]-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(7Z)-N-[3-(diethylamino)propyl]-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
-
-
(E)-methyl 3-(4-(phenylamino)quinazolin-7-yl)acrylate
-
(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
potent inhibitor against tyrosine kinases, including VEGFR and PDGFR families, as well as Aurora kinases
1,4-diamino-2,3-dicyano-1,4-bis(2-aminophenylthio)-butadiene
-
-
1-(4-((5-methyl-2-((4-morpholinophenyl)amino)pyrimidin-4-yl) amino)piperidin-1-yl)ethan-1-one
100 nM, 53.9% inhibition. 28°C, pH not specified in the publication
1-(4-(1H-pyrazol-1-yl)phenyl)-3-(2-aminoquinazolin-6-yl)-4-methylpyridin-2(1H)-one
-
1-(4-(5-methyl-2-((4-morpholinophenyl)amino)pyrimidin-4-yl) piperazin-1-yl)ethan-1-one
100 nM, 45.3% inhibition. 28°C, pH not specified in the publication
1-(4-(5-methyl-2-((4-morpholinophenyl)amino)pyrimidin-4-yl) piperazin-1-yl)pentane-1,4-dione
100 nM, 9.5% inhibition. 28°C, pH not specified in the publication
1-(4-(5-methyl-2-((4-morpholinophenyl)amino)pyrimidin-4-yl) piperazin-1-yl)propan-1-one
100 nM, 41.7% inhibition. 28°C, pH not specified in the publication
1-(4-(phenylamino)quinazolin-7-yl)ethanone
-
1-(4-acetylphenyl)-3-(1-(5-methyl-2-((4-morpholinophenyl) amino)pyrimidin-4-yl)azetidin-3-yl)urea
100 nM, 50.0% inhibition. 28°C, pH not specified in the publication
1-(4-acetylphenyl)-3-(1-(5-methyl-2-((4-morpholinophenyl) amino)pyrimidin-4-yl)pyrrolidin-3-yl)urea
100 nM, 75.7% inhibition. 28°C, pH not specified in the publication
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-(4-[5-[1-(cyclopentylmethyl)-6-(methylamino)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]pyridin-2-yl]piperazin-1-yl)-2,2-dimethylpropan-1-one
-
-
1-(cyclopentylmethyl)-3-[6-(4-ethylpiperazin-1-yl)pyridin-3-yl]-N-methyl-1H-pyrazolo[3,4-d]pyrimidin-6-amine
-
-
1-(cyclopentylmethyl)-N-methyl-3-[4-(4-methylpiperazin-1-yl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
-
-
1-(cyclopentylmethyl)-N-methyl-3-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
-
-
1-(cyclopentylmethyl)-N-methyl-3-[6-(piperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
-
1-[(1,3-dioxolan-2-yl)methyl]-3-(4-methoxyphenyl)-N-methyl-1H-pyrazolo[3,4-d]pyrimidin-6-amine
-
1-[(1,3-dioxolan-2-yl)methyl]-N-methyl-3-[6-(piperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
-
1-[(1-benzyl-1H-1,2,3-triazol-4-yl)methyl]-N-methyl-3-[6-(piperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
-
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
1-[4-(5-[1-[(1-benzyl-1H-1,2,3-triazol-4-yl)methyl]-6-(methylamino)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]pyridin-2-yl)piperazin-1-yl]-2,2-dimethylpropan-1-one
-
2,4,6-trihydroxydeoxybenzoin derivatives
-
2-(4-acetylphenyl)-1-(4-(2-((4-morpholinophenyl)amino)thieno[3,2-d]pyrimidin-4-yl)piperazin-1-yl)ethan-1-one
100 nM, 68.0% inhibition. 28°C, pH not specified in the publication
2-bromo-1-(4-(phenylamino)quinazolin-7-yl)ethanone
-
2-chloro-1-(4-(phenylamino)quinazolin-7-yl)ethanone
-
2-chloro-N-(4-((2-chloro-5-hydroxyphenyl)amino)-6-(prop-2-yn-1-yloxy)quinazolin-7-yl)acetamide
-
2-chloro-N-(4-((2-chloro-5-hydroxyphenyl)amino)quinazolin-7-yl)acetamide
-
2-chloro-N-(4-(phenylamino)quinazolin-7-yl)acetamide
-
2-fluoro-1-(4-(phenylamino)quinazolin-7-yl)ethanone
-
2-[(2-cyanobenzyl)oxy]-N-(3-hydroxyphenyl)-4-[3-(pyrrolidin-1-yl)propoxy]benzamide
most potent inhibitor in a series of benzanilides. Effect depends on the 3'-OH-Ph and 2''-CN-benzyl working co-operatively to deliver maximum inhibition. Modeling studies suggest a novel binding mode, incorporating a water molecule bound between these two groups and concomitant binding to the hinge
2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N-(2-hydroxyethyl)-N-methylacetamide
-
-
2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]acetamide
-
-
2-[5-(benzylthio)-1,3,4-oxadiazol-2-yl]-N-[4-[5-(benzylthio)-1,3,4-oxadiazol-2-yl]phenyl]aniline
49% inhibition at 0.01 mM, antiproliferative activity on human breast cancer cell line MCF-7, IC50 value 0.00073 mM
2-[7-(4-[[4-(imidazo[1,2-a]pyridin-3-yl)pyrimidin-2-yl]amino]-3-methoxyphenyl)-9-oxa-3,7-diazabicyclo[3.3.1]non-3-yl]ethanol
-
compound shows good IGF-1R inhibitory activity in a cellular assay and a high free fraction in human plasma. However this compound shows a higher affinity for the hERG channel
3-(2,4-dimethyl-5-[(Z)-[2-oxo-5-(2-phenylhydrazinecarbonyl)-1,2-dihydro-3H-indol-3-ylidene]methyl]-1H-pyrrol-3-yl)propanoic acid
-
-
3-(2-aminoquinazolin-6-yl)-1-(2-cyclopentylethyl)-4-methylpyridin-2(1H)-one
cyclopentylethyl
3-(2-aminoquinazolin-6-yl)-1-(3,3-dimethylindolin-6-yl)-4-methylpyridin-2(1H)-one
pyridone, nonselective inhibitor of c-Kit
3-(2-aminoquinazolin-6-yl)-1-(3-fluoro-4-methylphenyl)-4-methylpyridin-2(1H)-one
-
3-(2-aminoquinazolin-6-yl)-1-(3-methoxyphenyl)-4-methylpyridin-2(1H)-one
-
3-(2-aminoquinazolin-6-yl)-1-(4-chloro-3-fluorophenyl)-4-methylpyridin-2(1H)-one
-
3-(2-aminoquinazolin-6-yl)-1-(4-chlorophenyl)-4-methylpyridin-2(1H)-one
-
3-(2-aminoquinazolin-6-yl)-1-(4-fluoro-3-methylphenyl)-4-methylpyridin-2(1H)-one
-
3-(2-aminoquinazolin-6-yl)-1-(4-methoxyphenyl)-4-methylpyridin-2(1H)-one
-
3-(2-aminoquinazolin-6-yl)-1-(4-tert-butylphenyl)-4-methylpyridin-2(1H)-one
exhibits poor selectivity
3-(2-aminoquinazolin-6-yl)-4-methyl-1-(3-(trifluoromethyl)phenyl)pyridin-2(1H)-one
3-(2-aminoquinazolin-6-yl)-4-methyl-1-(4-(oxazol-2-yl)phenyl)pyridin-2(1H)-one
exhibits potent inhibition of c-Kit, greater than 200fold selectivity against KDR, p38, Lck, and Src, and desirable pharmacokinetic properties
3-(2-aminoquinazolin-6-yl)-4-methyl-1-(4-(trifluoromethyl)phenyl)pyridin-2(1H)-one
-
3-(2-aminoquinazolin-6-yl)-4-methyl-1-(4-morpholinophenyl)pyridin-2(1H)-one
-
3-(2-aminoquinazolin-6-yl)-4-methyl-1-phenylpyridin-2(1H)-one
-
3-(N-3-carboxyphenylaminomethyl)-phenylboronic acid
-
inhibition of EGFR tyrosine kinase
3-bromo-5-t-butyl-4-hydroxy-benzylidenemalonitrile
-
-
3-[2,4-dimethyl-5-[(Z)-(2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid
-
-
3-[2-[(Z)-(5-bromo-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-4,5,6,7-tetrahydro-1H-indol-3-yl]propanoic acid
-
-
3-[4-methyl-2-[(Z)-(2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid
-
-
3-[[5-([6-amino-5-[(E)-(methoxyimino)methyl]pyrimidin-4-yl]amino)-1H-indazol-1-yl]methyl]benzonitrile
-
4-(1H-indazol-3-yloxy)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidine
-
-
4-(2',5'-dihydroxybenzylamino)phenylboronic acid
-
inhibition of EGFR tyrosine kinase
4-(2-(4-(2-((4-morpholinophenyl)amino)thieno[3,2-d]pyrimidin-4-yl)piperazin-1-yl)-2-oxoethyl)benzonitrile
100 nM, 69.4% inhibition. 28°C, pH not specified in the publication
4-(3-chloroanilino)-6,7-dimethoxyquinazoline
-
-
4-(4-(cyclopropylsulfonyl)piperazin-1-yl)-5-methyl-N-(4-morpholinophenyl)pyrimidin-2-amine
100 nM, 51.7% inhibition. 28°C, pH not specified in the publication
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)-phenylboronic acid
-
inhibition of EGFR tyrosine kinase
4-amino-1-tert-butyl-3-(1'-naphthyl)pyrazolo[3,4-d]pyrimidine
-
-
4-amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine
4-amino-6-(1H-indazol-5-ylamino)pyrimidine-5-carbaldehyde O-methyloxime
-
4-amino-6-([3-chloro-4-[(3,5-difluorobenzyl)oxy]phenyl]amino)pyrimidine-5-carbaldehyde O-methyloxime
-
4-amino-6-([3-chloro-4-[(3-fluorobenzyl)oxy]phenyl]amino)pyrimidine-5-carbaldehyde O-methyloxime
-
4-amino-6-[(1-benzyl-1H-indazol-5-yl)amino]pyrimidine-5-carbaldehyde O-methyloxime
-
4-amino-6-[(3-bromophenyl)amino]pyrimidine-5-carbaldehyde O-methyloxime
-
4-amino-6-[(3-chloro-4-fluorobenzyl)amino]pyrimidine-5-carbaldehyde O-methyloxime
-
4-amino-6-[(3-chloro-4-fluorophenyl)amino]pyrimidine-5-carbaldehyde O-methyloxime
-
4-amino-6-[[1-(3-chlorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(1-methylethyl)oxime
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(2-methoxybenzyl)oxime
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(2-methoxyethyl)oxime
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(2-methylpropyl)oxime
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-benzyloxime
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-ethyloxime
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde oxime
-
4-amino-6-[[1-(3-fluorobenzyl)-1H-indol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
4-amino-6-[[1-(3-fluorobenzyl)-2,3-dihydro-1H-indol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
4-amino-6-[[1-(3-methoxybenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
4-amino-6-[[1-(4-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
4-amino-6-[[2-(3-fluorobenzyl)-1H-benzimidazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
4-amino-6-[[4-(benzyloxy)-3-chlorophenyl]amino]pyrimidine-5-carbaldehyde O-methyloxime
-
4-ethyl-3-[2-[4-(4-ethyl-5-thioxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenylamino]phenyl]-1H-1,2,4-triazole-5(4H)-thione
52% inhibition at 0.01 mM, antiproliferative activity on human breast cancer cell line MCF-7, IC50 value 0.00238 mM
4-methoxy-3-((2'-methoxybenzylamino)methyl)phenylboronic acid
-
inhibition of EGFR tyrosine kinase
4-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]-6-(methylamino)pyrimidine-5-carbaldehyde O-methyloxime
39% inhibition of ErbB-2 at 0.01 mM; 48% inhibition of EGFR at 0.002 mM
5,7-dihydroxyisoflavone derivatives
-
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-methyl-4-(4-(methylsulfonyl)piperazin-1-yl)-N-(4-morpholinophenyl)pyrimidin-2-amine
100 nM, 16.7% inhibition. 28°C, pH not specified in the publication
5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
-
5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(1,3-thiazol-4-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
-
5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
-
5-[(1R)-1-methyl-2-oxo-2-pyrrolidin-1-ylethoxy]-N-[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
-
5-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
-
5-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
-
5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-N-[(2S)-2-hydroxy-3-(morpholin-4-yl)propyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide
-
-
6,7-dimethyl-2-phenylquinoxaline
-
-
6-(1H-indol-5-ylmethyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
-
6-(1H-indol-5-ylmethyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
-
6-(3-bromobenzyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
-
6-(3-bromobenzyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
-
6-(6,7-dimethoxyquinazolin-4-yloxy)-1-naphthamide
-
6-(6,7-dimethoxyquinazolin-4-yloxy)-N-(2-methoxyethyl)-1-naphthamide
-
6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide methanesulfonate
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(1-methylcyclopropyl)-1-naphthamide
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(2,2,2-trifluoroethyl)-1-naphthamide
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(2-fluorophenyl)-1-naphthamide
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(2-methoxyethyl)-1-naphthamide
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(3-(trifluoromethyl)phenyl)-1-naphthamide
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(3-fluorophenyl)-1-naphthamide
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(3-methoxypropyl)-1-naphthamide
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(3-methylisoxazol-5-yl)-1-naphthamide
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(4-(trifluoromethyl)phenyl)-1-naphthamide
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(4-fluorophenyl)-1-naphthamide
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(5-methylisoxazol-3-yl)-1-naphthamide
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(isoxazol-3-yl)-1-naphthamide
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(pyridin-2-yl)-1-naphthamide
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(pyridin-3-yl)-1-naphthamide
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(pyridin-4-yl)-1-naphthamide
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(thiazol-2-yl)-1-naphthamide
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-ethyl-1-naphthamide
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-isopropyl-1-naphthamide
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-methyl-1-naphthamide
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-p-tolyl-1-naphthamide
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-phenyl-1-naphthamide
-
6-(6,7-dimethoxyquinolin-4-yloxy)-N-propyl-1-naphthamide
-
6-(7-methoxyquinolin-4-yloxy)-1-naphthamide
-
6-(7H-pyrrolo[2,3-d]pyrimidin-4-yloxy)-N-(4-chlorophenyl)-1-naphthamide
-
6-bromo-2-(4-chlorophenyl)-N-(2,4-difluorophenyl)quinazolin-4-amine
-
-
6-bromo-2-(4-chlorophenyl)-N-(2-fluorophenyl)quinazolin-4-amine
-
-
6-methoxy-7-[(morpholin-2-yl)methoxy]-N-(4-propylphenyl)quinazolin-4-amine
-
-
6-[4-fluoro-3-(trifluoromethyl)benzyl]-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
-
6-[4-fluoro-3-(trifluoromethyl)benzyl]-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
-
7,7-dimethyl-2-(1H-pyrazol-4-yl)-N-(4,5,6,7-tetrahydro-1H-indazol-3-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
7,7-dimethyl-2-(1H-pyrazol-4-yl)-N-[6-(trifluoromethyl)-1H-indazol-3-yl]-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
7,7-dimethyl-2-(1H-pyrazol-4-yl)-N-[7-(trifluoromethyl)-1H-indazol-3-yl]-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
7,7-dimethyl-N-(1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
7,7-dimethyl-N-(5-methyl-1H-pyrazol-3-yl)-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
8-(1-acetylpiperidin-4-yl)-2-((4-morpholinophenyl)amino)pteridin-7(8H)-one
100 nM, 16.7% inhibition. 28°C, pH not specified in the publication
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
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
BGB324
i.e. Bemcentinib; i.e. Bemcentinib; i.e. Bemcentinib; i.e. Bemcentinib; i.e. Bemcentinib; i.e. Bemcentinib; i.e. Bemcentinib; i.e. Bemcentinib
-
CEP-7055
-
inhibits VEGFR1-3
cisplatin
-
anti-cancer drug inhibiting receptor tyrosine kinases
cycloheximide
-
depletes the synthetic pool of Met receptor
cyclopropyl(4-(5-methyl-2-((4-morpholinophenyl)amino)pyrimidin-4-yl)piperazin-1-yl)methanone
100 nM, 31.4% inhibition. 28°C, pH not specified in the publication
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
GM3
-
inhibitory effect on tyrosine phosphorylation of both mono- and dimeric EGFR
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
-
hydrogen peroxide
-
limited exposure enhances insulin-induced autophosphorylation of the insulin receptor, while prolonged exposure impairs the action of insulin
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
LCRF-0004
-
potent and selective inhibitor
lipid mimetic of GM3
-
inhibitory effect on tyrosine phosphorylation of both mono- and dimeric EGFR
lipid mimetic of lyso-GM3 dimer
-
inhibitory effect on tyrosine phosphorylation of both mono- and dimeric EGFR
LY294002
-
PI3K/AKT inhibitor, has no effects on RON-mediated cell spreading either with or without MSP, but completely abrogates the cell survival properties of RON and reduces MSP-induced Transwell migration by 60-80%
lyso-GM3 dimer
-
inhibitory effect on tyrosine phosphorylation of both mono- and dimeric EGFR. A lipid mimetic of lyso-GM3 dimer shows similar strong inhibitory effect on EGF-induced EGFR tyrosine kinase activity, and similar low cytotoxicity, as the authentic lyso-GM3 dimer. Inhibits more strongly than GM3 or a lipid mimetic of GM3
methyl (3Z)-3-(3-[[2-(diethylamino)ethyl]carbamoyl]-2-methyl-1,4,5,6-tetrahydro-7H-indol-7-ylidene)-2-oxo-2,3-dihydro-1H-indole-5-carboxylate
-
-
methyl 3-[4-([6-(methylamino)-3-[4-(piperazin-1-yl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl]methyl)-1H-1,2,3-triazol-1-yl]thiophene-2-carboxylate
-
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,N-dimethyl-4-(5-methyl-2-((4-morpholinophenyl)amino)pyrimidin-4-yl)piperazine-1-carboxamide
100 nM, 68.0% inhibition. 28°C, pH not specified in the publication
N-(1,2-benzothiazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(1,3-benzothiazol-2-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(1H-indazol-3-yl)-7,7-dimethyl-2-(1,3-thiazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(1H-indazol-3-yl)-7,7-dimethyl-2-(1-methyl-1H-pyrazol-5-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(1H-indazol-3-yl)-7,7-dimethyl-2-(1H-1,2,3-triazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-3-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(1H-indazol-3-yl)-N,7,7-trimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(1H-indol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(2,4-dichlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
N-(2-hydroxyethyl)-N-methyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]acetamide
-
-
N-(2-methoxyethyl)-6-(7-methoxyquinolin-4-yloxy)-1-naphthamide
-
N-(3,5-dichlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
N-(3,5-dichlorophenyl)-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
-
-
N-(3-bromophenyl)-6-methoxy-7-[(4-methylmorpholin-2-yl)methoxy]quinazolin-4-amine
-
-
N-(3-bromophenyl)-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
-
-
N-(3-chloro-4-methylphenyl)-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
-
-
N-(3-chlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
N-(3-chlorophenyl)-6-methoxy-7-[(4-methylmorpholin-2-yl)methoxy]quinazolin-4-amine
-
-
N-(3-chlorophenyl)-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
-
-
N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)-1-benzothiophen-7-yl]oxy]phenyl)-1,3-diphenyl-1H-pyrazole-4-carboxamide
-
-
N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)-1-benzothiophen-7-yl]oxy]phenyl)-1,5-diphenyl-1H-pyrazole-4-carboxamide
-
-
N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)-1-benzothiophen-7-yl]oxy]phenyl)-1,5-diphenyl-1H-pyrrole-3-carboxamide
-
-
N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)-1-benzothiophen-7-yl]oxy]phenyl)-2,4-diphenyl-1,3-thiazole-5-carboxamide
-
-
N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-1-phenyl-5-(pyridin-2-yl)-1H-pyrazole-4-carboxamide
-
-
N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-1-phenyl-5-(pyridin-3-yl)-1H-pyrazole-4-carboxamide
-
-
N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-1-phenyl-5-(pyridin-4-yl)-1H-pyrazole-4-carboxamide
-
-
N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-1-phenyl-5-(thiophen-3-yl)-1H-pyrazole-4-carboxamide
-
-
N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-5-(2-fluorophenyl)-1-phenyl-1H-pyrazole-4-carboxamide
-
-
N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-5-(2-methoxyphenyl)-1-phenyl-1H-pyrazole-4-carboxamide
-
-
N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-5-(3-methoxyphenyl)-1-phenyl-1H-pyrazole-4-carboxamide
-
-
N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-5-(4-fluorophenyl)-1-phenyl-1H-pyrazole-4-carboxamide
-
-
N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-5-(4-methoxyphenyl)-1-phenyl-1H-pyrazole-4-carboxamide
-
-
N-(4,5-dichloro-1H-pyrazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(4-(phenylamino)quinazolin-7-yl)acrylamide
-
N-(4-(phenylamino)quinazolin-7-yl)ethenesulfonamide
-
N-(4-acetylphenyl)-1-(5-methyl-2-((4-morpholinophenyl) amino)pyrimidin-4-yl)piperidine-4-carboxamide
100 nM, 97.0% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-3-((5-methyl-2-((4-morpholinophenyl) amino)pyrimidin-4-yl)amino)azetidine-1-carboxamide
100 nM, 16.2% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-3-((5-methyl-2-((4-morpholinophenyl) amino)pyrimidin-4-yl)amino)pyrrolidine-1-carboxamide
100 nM, 57.3% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-((5-methyl-2-((4-morpholinophenyl) amino)pyrimidin-4-yl)amino)piperidine-1-carboxamide
100 nM, 78.6% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-(2-((4-morpholinophenyl)amino)-5-(trifluoromethyl)pyr-imidin-4-yl)piperazine-1-carboxamide
100 nM, 82.5% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-(2-((4-morpholinophenyl)amino)-5-nitropyrimidin-4-yl)piperazine-1-carboxamide
100 nM, 97.8 inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-(2-((4-morpholinophenyl)amino)-7-oxopteridin-8(7H)-yl)piperidine-1-carboxamide
100 nM, 35.9% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-(2-((4-morpholinophenyl)amino)quinazolin-4-yl)piperazine-1-carboxamide
100 nM, 36.0% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-(5-amino-2-((4-morpholinophenyl)amino) pyrimidin-4-yl)piperazine-1-carboxamide
100 nM, 67.9% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-(5-chloro-2-((4-morpholinophenyl)amino) pyrimidin-4-yl)piperazine-1-carboxamide
100 nM, 98.7% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-(5-fluoro-2-((4-morpholinophenyl)amino) pyrimidin-4-yl)piperazine-1-carboxamide
100 nM, 99.3% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-(5-methyl-2-((4-morpholinophenyl) amino)pyrimidin-4-yl)piperazine-1-sulfonamide
100 nM, 54.5% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-(5-methyl-2-((4-morpholinophenyl)amino)pyrimidin-4-yl)piperazine-1-carboxamide
2.9 nM, 81.8% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-(6-methyl-2-((4-morpholinophenyl)amino)pyrimidin-4-yl)piperazine-1-carboxamide
100 nM, 20.9% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-[2-[4-(morpholin-4-yl)anilino]pyrimidin-4-yl]piperazine-1-carboxamide
30 nM,0.7 % inhibition. 28°C, pH not specified in the publication
N-(4-bromo-2-chlorophenyl)-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
-
-
N-(4-bromo-2-fluorophenyl)-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
-
-
N-(4-bromo-3-methylphenyl)-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
-
-
N-(4-bromophenyl)-6-methoxy-7-[(4-methylmorpholin-2-yl)methoxy]quinazolin-4-amine
-
-
N-(4-bromophenyl)-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
-
-
N-(4-chloro-2-fluorophenyl)-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
-
-
N-(4-chloro-3-(trifluoromethyl)phenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
N-(4-chlorophenyl)-3-(6,7-dimethoxyquinolin-4-yloxy)isoquinoline-8-carboxamide
-
N-(4-chlorophenyl)-6-((6,7-dimethoxyquinolin-4-yl)(methyl)amino)-1-naphthamide
-
N-(4-chlorophenyl)-6-(2-(methylamino)pyridin-4-yloxy)-1-naphthamide
-
N-(4-chlorophenyl)-6-(2-(methylamino)pyrimidin-4-yloxy)-1-naphthamide
-
N-(4-chlorophenyl)-6-(3-fluoro-6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
N-(4-chlorophenyl)-6-(6,7-dimethoxyquinazolin-4-yloxy)-1-naphthamide
-
N-(4-chlorophenyl)-6-(6,7-dimethoxyquinolin-4-ylamino)-1-naphthamide
-
N-(4-chlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
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-cyanophenyl)-1-(5-methyl-2-((4-morpholinophenyl) amino)pyrimidin-4-yl)piperidine-4-carboxamide
100 nM, 94.3% inhibition. 28°C, pH not specified in the publication
N-(4-cyanophenyl)-4-(2-((4-morpholinophenyl)amino)quinazolin-4-yl)piperazine-1-carboxamide
100 nM, 40.5% inhibition. 28°C, pH not specified in the publication
N-(4-cyanophenyl)-4-(5-methyl-2-((4-morpholinophenyl)amino)pyrimidin-4-yl)piperazine-1-carboxamide
100 nM, 95.2% inhibition. 28°C, pH not specified in the publication
N-(4-cyanophenyl)-4-(6-methyl-2-((4-morpholinophenyl)amino)pyrimidin-4-yl)piperazine-1-carboxamide
100 nM, 15.8% inhibition. 28°C, pH not specified in the publication
N-(4-fluoro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(4-fluoro-2-methylphenyl)-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
-
-
N-(4-fluorophenyl)-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
-
-
N-(4-hydroxy-5-[(2E)-3-methyl-5-[(1R,2S)-1,2,3-trimethylcyclohex-3-en-1-yl]pent-2-en-1-yl]-3,6-dioxocyclohexa-1,4-dien-1-yl)glycine
-
IC50 of more than 0.2 mg/ml for EGFR, IC50 of 0.079 mg/ml for HER3
N-(4-tert-butylphenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
N-(5,7-difluoro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(5-fluoro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(5-tert-butylisoxazol-3-yl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
N-(5-[(2E)-5-[(1R)-1,3-dimethyl-2-methylidenecyclohex-3-en-1-yl]-3-methylpent-2-en-1-yl]-4-hydroxy-3,6-dioxocyclohexa-1,4-dien-1-yl)-D-serine
-
IC50 of more than 0.2 mg/ml for EGFR, IC50 of 0.022 mg/ml for HER3
N-(5-[(2E)-5-[(1R)-1,3-dimethyl-2-methylidenecyclohex-3-en-1-yl]-3-methylpent-2-en-1-yl]-4-hydroxy-3,6-dioxocyclohexa-1,4-dien-1-yl)-D-threonine
-
IC50 of more than 0.2 mg/ml for EGFR, IC50 of 0.027 mg/ml for HER3
N-(5-[(2E)-5-[(1R,3R)-1,3-dimethyl-2-methylidenecyclohexyl]-3-methylpent-2-en-1-yl]-4-hydroxy-3,6-dioxocyclohexa-1,4-dien-1-yl)-D-serine
-
IC50 of more than 0.2 mg/ml for EGFR, IC50 of 0.018 mg/ml for HER3
N-(5-[(2E)-5-[(1R,3R)-1,3-dimethyl-2-methylidenecyclohexyl]-3-methylpent-2-en-1-yl]-4-hydroxy-3,6-dioxocyclohexa-1,4-dien-1-yl)-D-threonine
-
IC50 of more than 0.2 mg/ml for EGFR, IC50 of 0.19 mg/ml for HER3
N-(5-[(2E)-5-[(1R,3R)-1,3-dimethyl-2-methylidenecyclohexyl]-3-methylpent-2-en-1-yl]-4-hydroxy-3,6-dioxocyclohexa-1,4-dien-1-yl)glycine
-
IC50 of 0.197 mg/ml for EGFR, IC50 of 0.125 mg/ml for HER2
N-(6-chloro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(6-fluoro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(7-chloro-1H-indazol-3-yl)-2-[5-(difluoromethyl)-1H-pyrazol-4-yl]-7,7-dimethyl-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(7-chloro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(7-chloro-5-fluoro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(7-chloro-6-fluoro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(7-fluoro-1-methyl-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(7-fluoro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
-
N-(cyclopropylmethyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
N-cyclobutyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
N-cyclopentyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
N-cyclopropyl-6-(6,7-dimethoxyquinazolin-4-yloxy)-1-naphthamide
-
N-cyclopropyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
N-cyclopropyl-6-(7-methoxyquinolin-4-yloxy)-1-naphthamide
-
N-ethyl-5-[2-[4-(5-(ethylamino)-1,3,4-thiadiazol-2-yl)phenylamino]-phenyl]-1,3,4-thiadiazol-2-amine
97.7% inhibition at 0.01 mM, antiproliferative activity on human breast cancer cell line MCF-7, IC50 value 0.00094 mM
N-tert-butyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
-
N-[(3Z)-2-oxo-3-[(1H-pyrrol-2-yl)methylidene]-2,3-dihydro-1H-indol-6-yl]-N'-phenylurea
-
-
N-[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
-
-
N-[4-chloro-3-(trifluoromethyl)phenyl]-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
-
-
N-[4-fluoro-3-(trifluoromethyl)phenyl]-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
-
-
N3-(6-aminopyridin-3-yl)-N1-(2-cyclopentylethyl)-4-methylisophthalamide
bisamide
N4-(2-fluoro-4-chlorophenyl)-6-(2,5-dimethoxybenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
shows potent inhibition of VEGFR-2 over EGFR, platelet-derived growth factor receptor-beta and VEGFR-1; 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
nakijiquinone C
-
IC50 of 0.125 mg/ml for EGFR, IC50 of 0.103 mg/ml for HER2
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
PF-2341066
-
IC50: 0.002 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
-
Protein kinase C
-
subsequently phosphorylates c-Kit on specific serine residues leading to negative regulation of c-Kit activation
-
protein tyrosine phosphatase 1B
-
rottlerin
-
specific inhibitor of PKCdelta
shRNA
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
-
STI571
-
commercial Gleevec/Glivec, specific inhibitor
SU 11248
-
inhibits VEGFR2
SU 6668
-
inhibits VEGFR2 and PDGF receptor beta
SU5416
-
selective inhibitor
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
tert-butyl 2-([[4-(3-bromoanilino)-6-methoxyquinazolin-7-yl]oxy]methyl)morpholine-4-carboxylate
-
-
tert-butyl 2-([[4-(3-chloroanilino)-6-methoxyquinazolin-7-yl]oxy]methyl)morpholine-4-carboxylate
-
-
tert-butyl 2-([[4-(4-bromoanilino)-6-methoxyquinazolin-7-yl]oxy]methyl)morpholine-4-carboxylate
-
-
trichostatin A
-
the ability of RON to inhibit HIV-1 transcription is sensitive to a histone deacetylase inhibitor
tyrphostin A9
-
PDGF receptor-specific
tyrphostin AG 1478
-
inhibition of EGF receptor
tyrphostin AG 370
-
PDGF receptor-specific
tyrphostin AG1478
-
EGFR-specific antagonist
tyrphostin B56
-
i.e. AG 556, selective EGFR and ErbB-1 kinase inhibitor, reduces volume-sensitive chloride current in atrial myocytes, is antagonized by pretreatment with VO43-
U0126
-
MEK/ERK inhibitor, has no effects on RON-mediated cell spreading either with or without MSP, but completely abrogates the cell survival properties of RON and reduces MSP-induced Transwell migration by 60-80%
vatalanib
-
i.e. ZK 222584 or PTK 787, inhibits VEGFR1-3
wogonin
-
slight inhibitory effect on epidermal growth factor receptor tyrosine kinase
[2-(4-chlorophenyl)-6-(4-fluorophenyl)quinazolin-4-yl]-2,4-difluorophenylamine
-
-
[7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-yl](1H-indazol-3-yl)methanone
-
-
(2R)-N,N-dimethyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]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
-
-
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
-
2,4,6-trihydroxydeoxybenzoin derivatives
-
diverse derivatives, analysis of inhibitory effect on parasite infection of host cells BM and HCT-8, IC50 values, overview
-
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
-
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
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
-
5,7-dihydroxyisoflavone derivatives
-
diverse derivatives, analysis of inhibitory effect on parasite infection of host cells BM and HCT-8, IC50 values, overview
-
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
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
AG1478
-
inhibition of epidermal growth factor receptor tyrosine kinase
doxorubicin
-
anti-cancer drug inhibiting receptor tyrosine kinases
dynamin K44A
-
reduces EGFR internalization to 40%
-
dynamin K44A
inhibits agrin-induced MuSK endocytosis
-
erlotinib
-
anti-cancer drug inhibiting receptor tyrosine kinases
gefitinib
-
i.e. ZD1839, highly specific inhibitor of EGFR tyrosine kinase and of HER1 tyrosine kinase, clinical effects, overview
gefitinib
-
specific inhibition of EGFR-TK
gemcitabine
-
anti-cancer drug inhibiting receptor tyrosine kinases
genistein
-
-
genistein
-
protein tyrosine kinase inhibitor
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
-
broad spectrum PTK inhibitor
genistein
-
inhibition of epidermal growth factor receptor tyrosine kinase
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
-
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
-
imatinib
-
inhibits c-Kit receptor and PDGF receptor tyrosine kinases
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
lapatinib
-
dual inhibitor of EGFR and ERBB2
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
luteolin is a potent receptor-type tyrosine-protein kinase FLT3 inhibitor. Luteolin suppresses cell proliferation in MV4,11 cells with constitutively activated FLT3
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
dose dependent inhibition of Flk-1 phosphorylation
N-(4-chlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
shows in vivo inhibition of corneal angiogenesis
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
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
-
-
PD168393
-
complete inhibition at 0.01 mM
PHA-665752
-
IC50: 0.0009 mM
PKI-166
-
-
PKI-166
-
0.5 mM/kg body weight
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
RM-6427
-
inhibits parasite infection of host cells BM and HCT-8
RM-6427
-
inhibits parasite infection of host cells BM and HCT-8
RM-6427
-
inhibits parasite infection of host cells BM and HCT-8
RM-6428
-
inhibits parasite infection of host cells BM and HCT-8
RM-6428
-
inhibits parasite infection of host cells BM and HCT-8
RM-6428
-
inhibits parasite infection of host cells BM and HCT-8
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
suppressed expression of Ror2, which results in impaired microtubule-organizing center reorientation following Wnt5a stimulation
-
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
-
siRNA
local injection of siRNA against ErbB3 with the atolocollagen results in a decrease in the tumor growth of parent B16-BL6 cells
-
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
-
sorafenib
-
oral multikinase inhibitor, inhibits receptor tyrosine kinase autophosphorylation, implicated in tumorigenesis and tumor progression
sorafenib
-
oral multikinase inhibitor, inhibits receptor tyrosine kinase autophosphorylation
Spry protein
-
-
-
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
SU11248
-
FLT-3 inhibitor treatment results in formation of larger amounts of the mature 150 kDa form of mutant FLT-3 ITD
sunitinib
-
VEGFR tyrosine kinase inhibitor
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
ZD1839
-
i.e. gefitinib, reversible inhibition of ErbB1, competitive to ATP, binding to EGF receptor kinase, structure overview, anticancer drug
ZD1839
-
selective inhibitor
additional information
no inhibition by genistein
-
additional information
-
no inhibition by genistein
-
additional information
inhibitory role for the KIT juxtamembrane region in controlling the receptor kinase activity
-
additional information
-
inhibitory role for the KIT juxtamembrane region in controlling the receptor kinase activity
-
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
-
no inhibition by daidzein
-
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
-
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
-
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
enzyme performs autoinhibition via its juxtamembrane domain, structure and mechanism, overview
-
additional information
-
enzyme performs autoinhibition via its juxtamembrane domain, structure and mechanism, overview
-
additional information
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
-
blocking internalization of the EGFR expressed in HeLa cells decreases ERK activity but also increases protein kinase C activity
-
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
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
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
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
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
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
-
additional information
development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening
-
additional information
development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening
-
additional information
development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening
-
additional information
development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening
-
additional information
development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening
-
additional information
development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening
-
additional information
development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening
-
additional information
development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening; development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening
-
additional information
-
autoregulation by a pseudosubstrate mechanism, overview
-
additional information
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
-
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
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
-
inhibition of the insulin receptor tyrosine kinase and insulin action by dephosphorylation
-
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0.00014
(2R)-2-[(4-[[1-(1,3-thiazol-4-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
Homo sapiens
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.000008
(2R)-2-[(4-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]-N,N-dimethylpropanamide
Homo sapiens
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.000057
(2R)-2-[(4-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]-N-methylpropanamide
Homo sapiens
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.000032
(2R)-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
Homo sapiens
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.000034 - 0.001
(2R)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N,N-dimethylpropanamide
0.000031
(2R)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N-(2-hydroxyethyl)-N-methylpropanamide
Homo sapiens
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.000066
(2R)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N-methylpropanamide
Homo sapiens
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.000026
(2R)-N,N-dimethyl-2-[(4-[[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
Homo sapiens
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
Homo sapiens
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.000008 - 0.00009
(2R)-N,N-dimethyl-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
0.000023 - 0.0027
(2R)-N,N-dimethyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
0.0002
(2R)-N-(2-hydroxyethyl)-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
Homo sapiens
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.000069 - 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
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
Homo sapiens
-
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
Homo sapiens
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.000059
(2R)-N-methyl-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
Homo sapiens
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.000006
(2S)-2-[(4-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]-N,N-dimethylpropanamide
Homo sapiens
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.000043
(2S)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N,N-dimethylpropanamide
Homo sapiens
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.000079
(2S)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N-(2-hydroxyethyl)-N-methylpropanamide
Homo sapiens
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.000024
(2S)-N,N-dimethyl-2-[(4-[[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
Homo sapiens
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
Homo sapiens
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.00008
(2S)-N,N-dimethyl-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
Homo sapiens
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.00003
(2S)-N,N-dimethyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
Homo sapiens
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.000078
(2S)-N-(2-hydroxyethyl)-N-methyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
Homo sapiens
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.0000078 - 0.0000407
(3Z)-3-[3-([1,4'-bipiperidine]-1'-carbonyl)-2-methyl-1,4,5,6-tetrahydro-7H-indol-7-ylidene]-5-fluoro-1,3-dihydro-2H-indol-2-one
0.0000085 - 0.0001184
(3Z)-5-fluoro-3-(2-methyl-3-[(2S)-2-[(pyrrolidin-1-yl)methyl]pyrrolidine-1-carbonyl]-1,4,5,6-tetrahydro-7H-indol-7-ylidene)-1,3-dihydro-2H-indol-2-one
0.0000011 - 0.0000401
(3Z)-5-fluoro-3-[2-methyl-3-(morpholine-4-carbonyl)-1,4,5,6-tetrahydro-7H-indol-7-ylidene]-1,3-dihydro-2H-indol-2-one
0.0000023 - 0.0000076
(7Z)-7-(5-bromo-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-N-[2-(diethylamino)ethyl]-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
0.0000026 - 0.0000121
(7Z)-7-(5-chloro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-N-[2-(diethylamino)ethyl]-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
0.0000016 - 0.0000132
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[2-(morpholin-4-yl)ethyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
0.0000043 - 0.0000194
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[2-(piperidin-1-yl)ethyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
0.0000114 - 0.0001606
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[2-(pyridin-2-yl)ethyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
0.0000074 - 0.0000416
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[2-(pyrrolidin-1-yl)ethyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
0.000001 - 0.000018
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
0.0000038 - 0.0000648
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[3-(pyrrolidin-1-yl)propyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
0.0000011 - 0.0000127
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-N-(2-hydroxyethyl)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
0.0000094 - 0.0000899
(7Z)-N-[2-(diethylamino)ethyl]-2-methyl-7-(2-oxo-1,2-dihydro-3H-indol-3-ylidene)-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
0.0000023 - 0.0000156
(7Z)-N-[2-(diethylamino)ethyl]-2-methyl-7-(5-methyl-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
0.0000069 - 0.0000257
(7Z)-N-[2-(diethylamino)ethyl]-2-methyl-7-(5-nitro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
0.000015 - 0.0000621
(7Z)-N-[2-(diethylamino)ethyl]-7-(4-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
0.0000023 - 0.0000101
(7Z)-N-[2-(diethylamino)ethyl]-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
0.0000246 - 0.0001014
(7Z)-N-[2-(diethylamino)ethyl]-7-(5-methoxy-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
0.0003303 - 0.0003976
(7Z)-N-[2-(diethylamino)ethyl]-7-(5-[[(diethylamino)oxy]sulfinyl]-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
0.0001124 - 0.0002603
(7Z)-N-[2-(diethylamino)ethyl]-7-(7-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
0.000003 - 0.0000227
(7Z)-N-[2-(dimethylamino)ethyl]-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
0.0000025 - 0.0000193
(7Z)-N-[3-(diethylamino)-2-hydroxypropyl]-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
0.0000027 - 0.0000213
(7Z)-N-[3-(diethylamino)propyl]-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
0.000002 - 0.000097
(R)-2-(2-[[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]methyl]pyrrolidin-1-yl)-2-oxoethanol
0.000002 - 0.000003
(R)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-1-methylethyl]-2-hydroxyacetamide
0.000002
(R)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]propyl]-2-hydroxyacetamide
0.000002 - 0.000327
(S)-2-(2-[[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]methyl]pyrrolidin-1-yl)-2-oxoethanol
0.000019 - 0.00258
(S)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-1-methylethyl]-2-hydroxyacetamide
0.000022 - 0.000191
(S)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]propyl]-2-hydroxyacetamide
0.00000098
(Z)-5-[6-[3-(4-methoxyphenyl)-ureido]-2-oxo-1,2-dihydroindol-3-ylidene-methyl]-4-methyl-1H-pyrrole-3-carboxylic acid
Homo sapiens
pH 7.5, 22°C
0.00001 - 0.0034
1-(4-(1H-pyrazol-1-yl)phenyl)-3-(2-aminoquinazolin-6-yl)-4-methylpyridin-2(1H)-one
0.01
1-(4-(phenylamino)quinazolin-7-yl)ethanone
Homo sapiens
IC50 above 0.01 mM, at pH 8.0, temperature not specified in the publication
0.00002 - 0.005
1-(4-acetylphenyl)-3-(2-aminoquinazolin-6-yl)-4-methylpyridin-2(1H)-one
0.0003 - 0.0072
1-(4-[5-[1-(cyclopentylmethyl)-6-(methylamino)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]pyridin-2-yl]piperazin-1-yl)-2,2-dimethylpropan-1-one
-
0.0001 - 0.0025
1-(cyclopentylmethyl)-3-[6-(4-ethylpiperazin-1-yl)pyridin-3-yl]-N-methyl-1H-pyrazolo[3,4-d]pyrimidin-6-amine
-
0.0000014 - 0.0006
1-(cyclopentylmethyl)-N-methyl-3-[4-(4-methylpiperazin-1-yl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
-
0.000008 - 0.00367
1-(cyclopentylmethyl)-N-methyl-3-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
-
0.00002 - 0.0021
1-(cyclopentylmethyl)-N-methyl-3-[6-(piperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
0.00025 - 0.0087
1-[(1,3-dioxolan-2-yl)methyl]-3-(4-methoxyphenyl)-N-methyl-1H-pyrazolo[3,4-d]pyrimidin-6-amine
0.00012 - 0.0075
1-[(1,3-dioxolan-2-yl)methyl]-N-methyl-3-[6-(piperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
0.00038 - 0.0076
1-[(1-benzyl-1H-1,2,3-triazol-4-yl)methyl]-N-methyl-3-[6-(piperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
0.00076 - 0.0054
1-[4-(5-[1-[(1-benzyl-1H-1,2,3-triazol-4-yl)methyl]-6-(methylamino)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]pyridin-2-yl)piperazin-1-yl]-2,2-dimethylpropan-1-one
0.000006
2-chloro-1-(4-(phenylamino)quinazolin-7-yl)ethanone
Homo sapiens
at pH 8.0, temperature not specified in the publication
0.000055
2-chloro-N-(4-(phenylamino)quinazolin-7-yl)acetamide
Homo sapiens
at pH 8.0, temperature not specified in the publication
0.000415
2-fluoro-1-(4-(phenylamino)quinazolin-7-yl)ethanone
Homo sapiens
at pH 8.0, temperature not specified in the publication
0.00012
2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N-(2-hydroxyethyl)-N-methylacetamide
Homo sapiens
-
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
Homo sapiens
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.000004
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
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000001 - 0.0014
3-(2-aminoquinazolin-6-yl)-1-(2-cyclopentylethyl)-4-methylpyridin-2(1H)-one
0.0000061 - 0.000048
3-(2-aminoquinazolin-6-yl)-1-(3,3-dimethylindolin-6-yl)-4-methylpyridin-2(1H)-one
0.00004 - 0.005
3-(2-aminoquinazolin-6-yl)-1-(3-fluoro-4-methylphenyl)-4-methylpyridin-2(1H)-one
0.000065 - 0.005
3-(2-aminoquinazolin-6-yl)-1-(3-methoxyphenyl)-4-methylpyridin-2(1H)-one
0.00006 - 0.005
3-(2-aminoquinazolin-6-yl)-1-(4-chloro-3-fluorophenyl)-4-methylpyridin-2(1H)-one
0.00002 - 0.005
3-(2-aminoquinazolin-6-yl)-1-(4-chlorophenyl)-4-methylpyridin-2(1H)-one
0.000014 - 0.0043
3-(2-aminoquinazolin-6-yl)-1-(4-fluoro-3-methylphenyl)-4-methylpyridin-2(1H)-one
0.000017 - 0.005
3-(2-aminoquinazolin-6-yl)-1-(4-methoxyphenyl)-4-methylpyridin-2(1H)-one
0.0000021 - 0.000011
3-(2-aminoquinazolin-6-yl)-1-(4-tert-butylphenyl)-4-methylpyridin-2(1H)-one
0.000014 - 0.005
3-(2-aminoquinazolin-6-yl)-4-methyl-1-(3-(trifluoromethyl)phenyl)pyridin-2(1H)-one
0.000022 - 0.005
3-(2-aminoquinazolin-6-yl)-4-methyl-1-(4-(oxazol-2-yl)phenyl)pyridin-2(1H)-one
0.0000079 - 0.0018
3-(2-aminoquinazolin-6-yl)-4-methyl-1-(4-(trifluoromethyl)phenyl)pyridin-2(1H)-one
0.000013 - 0.0044
3-(2-aminoquinazolin-6-yl)-4-methyl-1-(4-morpholinophenyl)pyridin-2(1H)-one
0.00021 - 0.001
3-(2-aminoquinazolin-6-yl)-4-methyl-1-phenylpyridin-2(1H)-one
0.00002 - 0.000044
3-[[5-([6-amino-5-[(E)-(methoxyimino)methyl]pyrimidin-4-yl]amino)-1H-indazol-1-yl]methyl]benzonitrile
0.000022
4-(5-((2-methoxyethyl)carbamoyl)naphthalen-2-yloxy)-7-methoxyquinoline-6-carboxamide
Homo sapiens
-
0.0000002 - 0.000003
4-(5-((4-chlorophenyl)carbamoyl)naphthalen-2-yloxy)-7-methoxyquinoline-6-carboxamide
0.000003 - 0.00021
4-(5-((4-chlorophenyl)carbamoyl)naphthalen-2-yloxy)-N-methylpicolinamide
0.00000037
4-(5-(cyclopropylcarbamoyl)naphthalen-2-yloxy)-7-methoxyquinoline-6-carboxamide
Homo sapiens
-
0.000131
4-(5-bromoindole-3-yl)-6,7-dimethoxyquinazoline
Homo sapiens
-
-
0.0000013
4-(5-carbamoylnaphthalen-2-yloxy)-7-methoxyquinoline-6-carboxamide
Homo sapiens
-
0.000472
4-(5-chloro-6-fluoro-indole-3-yl)-6,7-di-(2-methoxyethoxy)quinazoline
Homo sapiens
-
-
0.000209
4-(5-chloro-6-fluoroindole-3-yl)-6,7-dimethoxyquinazoline
Homo sapiens
-
-
0.000333
4-(5-chloro-6-fluoroindole-3-yl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazoline
Homo sapiens
-
-
0.000533
4-(6-fluoro-5-methylindole-3-yl)-6,7-dimethoxyquinazoline
Homo sapiens
-
-
0.000005
4-(imidazo[1,2-a]pyridin-3-yl)-N-[2-methoxyphenyl-4-(4-piperidinyl)]pyrimidin-2-amine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000004
4-(imidazo[2-methoxy-4-(9-oxa-3,7-diazabicyclo[3.3.1]non-3-yl)phenyl])pyrimidin-2-amine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000306 - 0.004123
4-amino-6-(1H-indazol-5-ylamino)pyrimidine-5-carbaldehyde O-methyloxime
0.000033
4-amino-6-([3-chloro-4-[(3,5-difluorobenzyl)oxy]phenyl]amino)pyrimidine-5-carbaldehyde O-methyloxime
Homo sapiens
-
0.000012 - 0.000018
4-amino-6-([3-chloro-4-[(3-fluorobenzyl)oxy]phenyl]amino)pyrimidine-5-carbaldehyde O-methyloxime
0.000022 - 0.000044
4-amino-6-[(1-benzyl-1H-indazol-5-yl)amino]pyrimidine-5-carbaldehyde O-methyloxime
0.001123 - 0.00522
4-amino-6-[(3-chloro-4-fluorobenzyl)amino]pyrimidine-5-carbaldehyde O-methyloxime
0.000023 - 0.00003
4-amino-6-[[1-(3-chlorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
0.000014 - 0.000025
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(1-methylethyl)oxime
0.000047 - 0.000435
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(2-methoxybenzyl)oxime
0.000006 - 0.000014
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(2-methoxyethyl)oxime
0.000032 - 0.000173
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(2-methylpropyl)oxime
0.000023 - 0.000095
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-benzyloxime
0.000005 - 0.000007
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-ethyloxime
0.000012 - 0.000042
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde oxime
0.000013 - 0.000027
4-amino-6-[[1-(3-fluorobenzyl)-1H-indol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
0.000057 - 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
Homo sapiens
-
0.000104 - 0.000189
4-amino-6-[[1-(4-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
0.000048 - 0.000076
4-amino-6-[[2-(3-fluorobenzyl)-1H-benzimidazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
0.000016 - 0.000153
4-amino-6-[[4-(benzyloxy)-3-chlorophenyl]amino]pyrimidine-5-carbaldehyde O-methyloxime
0.000043
5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
Homo sapiens
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
Homo sapiens
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.000051
5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
Homo sapiens
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.000012
5-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
Homo sapiens
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
Homo sapiens
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.025 - 0.2
6-(1H-indol-5-ylmethyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
0.031 - 0.223
6-(1H-indol-5-ylmethyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
0.0003 - 0.05
6-(3-bromobenzyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
0.0085 - 0.2
6-(3-bromobenzyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
0.0000013
6-(6,7-dimethoxyquinazolin-4-yloxy)-1-naphthamide
Homo sapiens
-
0.000314
6-(6,7-dimethoxyquinazolin-4-yloxy)-N-(2-methoxyethyl)-1-naphthamide
Homo sapiens
-
0.0000009
6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide methanesulfonate
Homo sapiens
-
0.000015
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(1-methylcyclopropyl)-1-naphthamide
Homo sapiens
-
0.0000038
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(2,2,2-trifluoroethyl)-1-naphthamide
Homo sapiens
-
0.000002 - 0.000007
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(2-fluorophenyl)-1-naphthamide
0.000012
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(2-methoxyethyl)-1-naphthamide
Homo sapiens
-
0.0000005 - 0.000034
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(3-(trifluoromethyl)phenyl)-1-naphthamide
0.0000006 - 0.000003
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(3-fluorophenyl)-1-naphthamide
0.0000042
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(3-methoxypropyl)-1-naphthamide
Homo sapiens
-
0.000001 - 0.000007
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(3-methylisoxazol-5-yl)-1-naphthamide
0.0000005 - 0.000016
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(4-(trifluoromethyl)phenyl)-1-naphthamide
0.000001 - 0.000002
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(4-fluorophenyl)-1-naphthamide
0.0000006 - 0.000006
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(5-methylisoxazol-3-yl)-1-naphthamide
0.0000002 - 0.0000004
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(isoxazol-3-yl)-1-naphthamide
0.0000008 - 0.000002
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(pyridin-2-yl)-1-naphthamide
0.0000008 - 0.000002
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(pyridin-3-yl)-1-naphthamide
0.000002
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(pyridin-4-yl)-1-naphthamide
0.0000003 - 0.000002
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(thiazol-2-yl)-1-naphthamide
0.0000013
6-(6,7-dimethoxyquinolin-4-yloxy)-N-ethyl-1-naphthamide
Homo sapiens
-
0.000004 - 0.0000059
6-(6,7-dimethoxyquinolin-4-yloxy)-N-isopropyl-1-naphthamide
0.0000038
6-(6,7-dimethoxyquinolin-4-yloxy)-N-methyl-1-naphthamide
Homo sapiens
-
0.0000005 - 0.000002
6-(6,7-dimethoxyquinolin-4-yloxy)-N-p-tolyl-1-naphthamide
0.0000002 - 0.0000008
6-(6,7-dimethoxyquinolin-4-yloxy)-N-phenyl-1-naphthamide
0.0000013 - 0.000007
6-(6,7-dimethoxyquinolin-4-yloxy)-N-propyl-1-naphthamide
0.0000012
6-(7-methoxyquinolin-4-yloxy)-1-naphthamide
Homo sapiens
-
0.000028 - 0.000037
6-(7H-pyrrolo[2,3-d]pyrimidin-4-yloxy)-N-(4-chlorophenyl)-1-naphthamide
0.09 - 0.2
6-[4-fluoro-3-(trifluoromethyl)benzyl]-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
0.057 - 0.5
6-[4-fluoro-3-(trifluoromethyl)benzyl]-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
0.0000007 - 0.0034
BGB324
-
0.000017 - 0.005
ethyl 4-(3-(2-aminoquinazolin-6-yl)-4-methyl-2-oxopyridin-1(2H)-yl)benzoate
0.000012
LCRF-0004
Homo sapiens
-
pH and temperature not specified in the publication
0.00083
luteolin
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000703 - 0.0002557
methyl (3Z)-3-(3-[[2-(diethylamino)ethyl]carbamoyl]-2-methyl-1,4,5,6-tetrahydro-7H-indol-7-ylidene)-2-oxo-2,3-dihydro-1H-indole-5-carboxylate
0.00043 - 0.0089
methyl 3-[4-([6-(methylamino)-3-[4-(piperazin-1-yl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl]methyl)-1H-1,2,3-triazol-1-yl]thiophene-2-carboxylate
0.0000082
MFCD09840836
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000002 - 0.000014
N-(2,4-dichlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
0.00013
N-(2-hydroxyethyl)-N-methyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]acetamide
Homo sapiens
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.000028
N-(2-methoxyethyl)-6-(7-methoxyquinolin-4-yloxy)-1-naphthamide
Homo sapiens
-
0.0000003 - 0.000028
N-(3,5-dichlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
0.00096
N-(3,5-dichlorophenyl)-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.00075
N-(3-bromophenyl)-6-methoxy-7-[(4-methylmorpholin-2-yl)methoxy]quinazolin-4-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.00073
N-(3-bromophenyl)-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.0003
N-(3-chloro-4-methylphenyl)-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.0000003 - 0.0000051
N-(3-chlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
0.00147
N-(3-chlorophenyl)-6-methoxy-7-[(4-methylmorpholin-2-yl)methoxy]quinazolin-4-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.00058
N-(3-chlorophenyl)-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.000032
N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)-1-benzothiophen-7-yl]oxy]phenyl)-1,3-diphenyl-1H-pyrazole-4-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000023
N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)-1-benzothiophen-7-yl]oxy]phenyl)-1,5-diphenyl-1H-pyrazole-4-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000101
N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)-1-benzothiophen-7-yl]oxy]phenyl)-1,5-diphenyl-1H-pyrrole-3-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000045
N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)-1-benzothiophen-7-yl]oxy]phenyl)-2,4-diphenyl-1,3-thiazole-5-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000023
N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-1-phenyl-5-(pyridin-2-yl)-1H-pyrazole-4-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000014
N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-1-phenyl-5-(pyridin-3-yl)-1H-pyrazole-4-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000025
N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-5-(2-fluorophenyl)-1-phenyl-1H-pyrazole-4-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000027
N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-5-(3-methoxyphenyl)-1-phenyl-1H-pyrazole-4-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00023
N-(4-bromo-2-chlorophenyl)-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.00045
N-(4-bromo-2-fluorophenyl)-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.00032
N-(4-bromo-3-methylphenyl)-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.00068
N-(4-bromophenyl)-6-methoxy-7-[(4-methylmorpholin-2-yl)methoxy]quinazolin-4-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.00072
N-(4-bromophenyl)-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.00016
N-(4-chloro-2-fluorophenyl)-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.000001 - 0.000247
N-(4-chloro-3-(trifluoromethyl)phenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
0.000023 - 0.000175
N-(4-chlorophenyl)-3-(6,7-dimethoxyquinolin-4-yloxy)isoquinoline-8-carboxamide
0.0014
N-(4-chlorophenyl)-6-((6,7-dimethoxyquinolin-4-yl)(methyl)amino)-1-naphthamide
Homo sapiens
KDR enzyme
0.000007 - 0.00014
N-(4-chlorophenyl)-6-(2-(methylamino)pyridin-4-yloxy)-1-naphthamide
0.000046 - 0.000296
N-(4-chlorophenyl)-6-(2-(methylamino)pyrimidin-4-yloxy)-1-naphthamide
0.00002 - 0.000069
N-(4-chlorophenyl)-6-(3-fluoro-6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
0.000002
N-(4-chlorophenyl)-6-(6,7-dimethoxyquinazolin-4-yloxy)-1-naphthamide
0.000008 - 0.000014
N-(4-chlorophenyl)-6-(6,7-dimethoxyquinolin-4-ylamino)-1-naphthamide
0.0000005 - 0.000008
N-(4-chlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
0.0000003 - 0.000002
N-(4-chlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-5-fluoro-1-naphthamide
0.00002 - 0.000106
N-(4-chlorophenyl)-6-(6-(methylamino)pyrimidin-4-yloxy)-1-naphthamide
0.000001 - 0.000008
N-(4-chlorophenyl)-6-(7-methoxyquinolin-4-yloxy)-1-naphthamide
0.000018 - 0.00022
N-(4-chlorophenyl)-6-(pyridin-4-yloxy)-1-naphthamide
0.00031
N-(4-chlorophenyl)-6-(pyrimidin-4-yloxy)-1-naphthamide
Homo sapiens
KDR enzyme
0.000004 - 0.000034
N-(4-chlorophenyl)-6-(quinolin-4-yloxy)-1-naphthamide
0.00001 - 0.000022
N-(4-chlorophenyl)-7-(6,7-dimethoxyquinolin-4-yloxy)quinoline-4-carboxamide
0.0002
N-(4-fluoro-2-methylphenyl)-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.00062
N-(4-fluorophenyl)-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.0000007 - 0.000063
N-(4-tert-butylphenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
0.0000008 - 0.000068
N-(5-tert-butylisoxazol-3-yl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
0.000011 - 0.00007
N-(cyclopropylmethyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
0.0000013 - 0.000007
N-cyclobutyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
0.000007 - 0.000015
N-cyclopentyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
0.0000029
N-cyclopropyl-6-(6,7-dimethoxyquinazolin-4-yloxy)-1-naphthamide
Homo sapiens
-
0.0000006 - 0.000001
N-cyclopropyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
0.00000045
N-cyclopropyl-6-(7-methoxyquinolin-4-yloxy)-1-naphthamide
Homo sapiens
-
0.0015
N-tert-butyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
Homo sapiens
-
0.000022
N-[1-(3-fluorobenzyl)-1H-indazol-5-yl]-5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine
Homo sapiens
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.000004 - 0.000035
N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]ethyl]-2-hydroxyacetamide
0.00014
N-[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]-5-(2-morpholin-4-yl-2-oxoethoxy)quinazolin-4-amine
Homo sapiens
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.000019
N-[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]-5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine
Homo sapiens
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.00035
N-[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]-5-[2-(4-methylpiperazin-1-yl)-2-oxoethoxy]quinazolin-4-amine
Homo sapiens
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.000027
N-[3-chloro-4-[(6-methylpyridin-3-yl)oxy]phenyl]-5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine
Homo sapiens
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.000023
N-[3-methoxy-4-[(6-methylpyridin-3-yl)oxy]phenyl]-5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine
Homo sapiens
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.000022
N-[3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]-5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine
Homo sapiens
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.000035
N-[3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]-5-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine
Homo sapiens
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.00017
N-[4-chloro-3-(trifluoromethyl)phenyl]-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.00321
N-[4-fluoro-3-(trifluoromethyl)phenyl]-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.000077 - 0.025
N3-(6-aminopyridin-3-yl)-N1-(2-cyclopentylethyl)-4-methylisophthalamide
0.0001 - 0.185
N4-(2-fluoro-4-chlorophenyl)-6-(2,5-dimethoxybenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
0.0241 - 0.0936
N4-(3-bromo,4-fluorophenyl)-6-(2-pyridin-2-yl-ethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
0.0018 - 0.0257
N4-(3-bromo-phenyl)-7-(3,4,5-trimethoxy-benzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
0.0149 - 0.129
N4-(3-bromophenyl)-7-(1-naphthylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
0.0015 - 0.0179
N4-(3-bromophenyl)-7-(2-chlorobenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
0.00048 - 0.2
N4-(4-chloro-2-fluorophenyl)-6-(1-naphthylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
0.016 - 0.0298
N4-(4-chloro-2-fluorophenyl)-6-(2-methylbenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
0.0152 - 0.0567
N4-(4-chlorophenyl)-6-(2,5-dimethoxybenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
0.00329
PD153035
Homo sapiens
-
specific inhibition of EGFR-TK, IC50 is 0.00329 mM with 1 U of purified EGFR-TK from A431 cells
0.002
PF-2341066
Homo sapiens
-
IC50: 0.002 mM
0.0009
PHA-665752
Homo sapiens
-
IC50: 0.0009 mM
0.00059
quercetin
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000003
Rapamycin
Homo sapiens
-
IC50: 3 nM
0.000004 - 0.0000106
sunitinib
0.0025
tert-butyl 2-([[4-(3-bromoanilino)-6-methoxyquinazolin-7-yl]oxy]methyl)morpholine-4-carboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.00119
tert-butyl 2-([[4-(3-chloroanilino)-6-methoxyquinazolin-7-yl]oxy]methyl)morpholine-4-carboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.00231
tert-butyl 2-([[4-(4-bromoanilino)-6-methoxyquinazolin-7-yl]oxy]methyl)morpholine-4-carboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.000034
(2R)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N,N-dimethylpropanamide
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
inhibition of erbB2 in KB cells
0.000008
(2R)-N,N-dimethyl-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
Homo sapiens
inhibition versus erbB2 kinase
0.00009
(2R)-N,N-dimethyl-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
Homo sapiens
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.000023
(2R)-N,N-dimethyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
Homo sapiens
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells
0.000023
(2R)-N,N-dimethyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
Homo sapiens
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
Homo sapiens
-
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
Homo sapiens
-
inhibition of erbB2 in KB cells
0.000069
(2R)-N-(2-hydroxyethyl)-N-methyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
inhibition of erbB2 in KB cells
0.0000078
(3Z)-3-[3-([1,4'-bipiperidine]-1'-carbonyl)-2-methyl-1,4,5,6-tetrahydro-7H-indol-7-ylidene]-5-fluoro-1,3-dihydro-2H-indol-2-one
Homo sapiens
-
c-Kit, pH and temperature not specified in the publication
0.000008
(3Z)-3-[3-([1,4'-bipiperidine]-1'-carbonyl)-2-methyl-1,4,5,6-tetrahydro-7H-indol-7-ylidene]-5-fluoro-1,3-dihydro-2H-indol-2-one
Homo sapiens
-
VEGFR-2, pH and temperature not specified in the publication
0.0000407
(3Z)-3-[3-([1,4'-bipiperidine]-1'-carbonyl)-2-methyl-1,4,5,6-tetrahydro-7H-indol-7-ylidene]-5-fluoro-1,3-dihydro-2H-indol-2-one
Homo sapiens
-
PDGFR-beta, pH and temperature not specified in the publication
0.0000085
(3Z)-5-fluoro-3-(2-methyl-3-[(2S)-2-[(pyrrolidin-1-yl)methyl]pyrrolidine-1-carbonyl]-1,4,5,6-tetrahydro-7H-indol-7-ylidene)-1,3-dihydro-2H-indol-2-one
Homo sapiens
-
c-Kit, pH and temperature not specified in the publication
0.0000118
(3Z)-5-fluoro-3-(2-methyl-3-[(2S)-2-[(pyrrolidin-1-yl)methyl]pyrrolidine-1-carbonyl]-1,4,5,6-tetrahydro-7H-indol-7-ylidene)-1,3-dihydro-2H-indol-2-one
Homo sapiens
-
VEGFR-2, pH and temperature not specified in the publication
0.0001184
(3Z)-5-fluoro-3-(2-methyl-3-[(2S)-2-[(pyrrolidin-1-yl)methyl]pyrrolidine-1-carbonyl]-1,4,5,6-tetrahydro-7H-indol-7-ylidene)-1,3-dihydro-2H-indol-2-one
Homo sapiens
-
PDGFR-beta, pH and temperature not specified in the publication
0.0000011
(3Z)-5-fluoro-3-[2-methyl-3-(morpholine-4-carbonyl)-1,4,5,6-tetrahydro-7H-indol-7-ylidene]-1,3-dihydro-2H-indol-2-one
Homo sapiens
-
VEGFR-2, pH and temperature not specified in the publication
0.0000021
(3Z)-5-fluoro-3-[2-methyl-3-(morpholine-4-carbonyl)-1,4,5,6-tetrahydro-7H-indol-7-ylidene]-1,3-dihydro-2H-indol-2-one
Homo sapiens
-
c-Kit, pH and temperature not specified in the publication
0.0000401
(3Z)-5-fluoro-3-[2-methyl-3-(morpholine-4-carbonyl)-1,4,5,6-tetrahydro-7H-indol-7-ylidene]-1,3-dihydro-2H-indol-2-one
Homo sapiens
-
PDGFR-beta, pH and temperature not specified in the publication
0.0000023
(7Z)-7-(5-bromo-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-N-[2-(diethylamino)ethyl]-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
c-Kit, pH and temperature not specified in the publication
0.0000039
(7Z)-7-(5-bromo-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-N-[2-(diethylamino)ethyl]-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
VEGFR-2, pH and temperature not specified in the publication
0.0000076
(7Z)-7-(5-bromo-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-N-[2-(diethylamino)ethyl]-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
PDGFR-beta, pH and temperature not specified in the publication
0.0000026
(7Z)-7-(5-chloro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-N-[2-(diethylamino)ethyl]-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
VEGFR-2, pH and temperature not specified in the publication
0.0000027
(7Z)-7-(5-chloro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-N-[2-(diethylamino)ethyl]-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
c-Kit, pH and temperature not specified in the publication
0.0000121
(7Z)-7-(5-chloro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-N-[2-(diethylamino)ethyl]-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
PDGFR-beta, pH and temperature not specified in the publication
0.0000016
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[2-(morpholin-4-yl)ethyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
VEGFR-2, pH and temperature not specified in the publication
0.000002
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[2-(morpholin-4-yl)ethyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
c-Kit, pH and temperature not specified in the publication
0.0000132
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[2-(morpholin-4-yl)ethyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
PDGFR-beta, pH and temperature not specified in the publication
0.0000043
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[2-(piperidin-1-yl)ethyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
VEGFR-2, pH and temperature not specified in the publication
0.0000058
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[2-(piperidin-1-yl)ethyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
c-Kit, pH and temperature not specified in the publication
0.0000194
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[2-(piperidin-1-yl)ethyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
PDGFR-beta, pH and temperature not specified in the publication
0.0000114
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[2-(pyridin-2-yl)ethyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
VEGFR-2, pH and temperature not specified in the publication
0.0000377
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[2-(pyridin-2-yl)ethyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
c-Kit, pH and temperature not specified in the publication
0.0001606
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[2-(pyridin-2-yl)ethyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
PDGFR-beta, pH and temperature not specified in the publication
0.0000074
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[2-(pyrrolidin-1-yl)ethyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
c-Kit, pH and temperature not specified in the publication
0.0000097
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[2-(pyrrolidin-1-yl)ethyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
VEGFR-2, pH and temperature not specified in the publication
0.0000416
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[2-(pyrrolidin-1-yl)ethyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
PDGFR-beta, pH and temperature not specified in the publication
0.000001
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
VEGFR-2, pH and temperature not specified in the publication
0.0000057
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
c-Kit, pH and temperature not specified in the publication
0.000018
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
PDGFR-beta, pH and temperature not specified in the publication
0.0000038
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[3-(pyrrolidin-1-yl)propyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
VEGFR-2, pH and temperature not specified in the publication
0.0000107
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[3-(pyrrolidin-1-yl)propyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
c-Kit, pH and temperature not specified in the publication
0.0000648
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[3-(pyrrolidin-1-yl)propyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
PDGFR-beta, pH and temperature not specified in the publication
0.0000011
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-N-(2-hydroxyethyl)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
VEGFR-2, pH and temperature not specified in the publication
0.0000014
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-N-(2-hydroxyethyl)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
c-Kit, pH and temperature not specified in the publication
0.0000127
(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-N-(2-hydroxyethyl)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
PDGFR-beta, pH and temperature not specified in the publication
0.0000094
(7Z)-N-[2-(diethylamino)ethyl]-2-methyl-7-(2-oxo-1,2-dihydro-3H-indol-3-ylidene)-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
VEGFR-2, pH and temperature not specified in the publication
0.0000899
(7Z)-N-[2-(diethylamino)ethyl]-2-methyl-7-(2-oxo-1,2-dihydro-3H-indol-3-ylidene)-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
PDGFR-beta, pH and temperature not specified in the publication
0.0000023
(7Z)-N-[2-(diethylamino)ethyl]-2-methyl-7-(5-methyl-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
VEGFR-2, pH and temperature not specified in the publication
0.0000041
(7Z)-N-[2-(diethylamino)ethyl]-2-methyl-7-(5-methyl-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
c-Kit, pH and temperature not specified in the publication
0.0000156
(7Z)-N-[2-(diethylamino)ethyl]-2-methyl-7-(5-methyl-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
PDGFR-beta, pH and temperature not specified in the publication
0.0000069
(7Z)-N-[2-(diethylamino)ethyl]-2-methyl-7-(5-nitro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
c-Kit, pH and temperature not specified in the publication
0.0000133
(7Z)-N-[2-(diethylamino)ethyl]-2-methyl-7-(5-nitro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
PDGFR-beta, pH and temperature not specified in the publication
0.0000257
(7Z)-N-[2-(diethylamino)ethyl]-2-methyl-7-(5-nitro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
VEGFR-2, pH and temperature not specified in the publication
0.000015
(7Z)-N-[2-(diethylamino)ethyl]-7-(4-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
VEGFR-2, pH and temperature not specified in the publication
0.0000431
(7Z)-N-[2-(diethylamino)ethyl]-7-(4-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
c-Kit, pH and temperature not specified in the publication
0.0000621
(7Z)-N-[2-(diethylamino)ethyl]-7-(4-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
PDGFR-beta, pH and temperature not specified in the publication
0.0000023
(7Z)-N-[2-(diethylamino)ethyl]-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
VEGFR-2, pH and temperature not specified in the publication
0.0000024
(7Z)-N-[2-(diethylamino)ethyl]-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
c-Kit, pH and temperature not specified in the publication
0.0000101
(7Z)-N-[2-(diethylamino)ethyl]-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
PDGFR-beta, pH and temperature not specified in the publication
0.0000246
(7Z)-N-[2-(diethylamino)ethyl]-7-(5-methoxy-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
VEGFR-2, pH and temperature not specified in the publication
0.0000355
(7Z)-N-[2-(diethylamino)ethyl]-7-(5-methoxy-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
c-Kit, pH and temperature not specified in the publication
0.0001014
(7Z)-N-[2-(diethylamino)ethyl]-7-(5-methoxy-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
PDGFR-beta, pH and temperature not specified in the publication
0.0003303
(7Z)-N-[2-(diethylamino)ethyl]-7-(5-[[(diethylamino)oxy]sulfinyl]-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
VEGFR-2, pH and temperature not specified in the publication
0.0003957
(7Z)-N-[2-(diethylamino)ethyl]-7-(5-[[(diethylamino)oxy]sulfinyl]-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
PDGFR-beta, pH and temperature not specified in the publication
0.0003976
(7Z)-N-[2-(diethylamino)ethyl]-7-(5-[[(diethylamino)oxy]sulfinyl]-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
c-Kit, pH and temperature not specified in the publication
0.0001124
(7Z)-N-[2-(diethylamino)ethyl]-7-(7-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
VEGFR-2, pH and temperature not specified in the publication
0.0001808
(7Z)-N-[2-(diethylamino)ethyl]-7-(7-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
c-Kit, pH and temperature not specified in the publication
0.0002603
(7Z)-N-[2-(diethylamino)ethyl]-7-(7-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
PDGFR-beta, pH and temperature not specified in the publication
0.000003
(7Z)-N-[2-(dimethylamino)ethyl]-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
VEGFR-2, pH and temperature not specified in the publication
0.0000066
(7Z)-N-[2-(dimethylamino)ethyl]-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
c-Kit, pH and temperature not specified in the publication
0.0000227
(7Z)-N-[2-(dimethylamino)ethyl]-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
PDGFR-beta, pH and temperature not specified in the publication
0.0000025
(7Z)-N-[3-(diethylamino)-2-hydroxypropyl]-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
VEGFR-2, pH and temperature not specified in the publication
0.0000041
(7Z)-N-[3-(diethylamino)-2-hydroxypropyl]-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
c-Kit, pH and temperature not specified in the publication
0.0000193
(7Z)-N-[3-(diethylamino)-2-hydroxypropyl]-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
PDGFR-beta, pH and temperature not specified in the publication
0.0000027
(7Z)-N-[3-(diethylamino)propyl]-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
VEGFR-2, pH and temperature not specified in the publication
0.0000099
(7Z)-N-[3-(diethylamino)propyl]-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
c-Kit, pH and temperature not specified in the publication
0.0000213
(7Z)-N-[3-(diethylamino)propyl]-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
Homo sapiens
-
PDGFR-beta, pH and temperature not specified in the publication
0.000002
(R)-2-(2-[[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]methyl]pyrrolidin-1-yl)-2-oxoethanol
Mus musculus
-
IC50: less than 2 nM
0.000097
(R)-2-(2-[[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]methyl]pyrrolidin-1-yl)-2-oxoethanol
Mus musculus
-
IC50: 97 nM
0.000002
(R)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-1-methylethyl]-2-hydroxyacetamide
Mus musculus
-
IC50: less than 2 nM
0.000003
(R)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-1-methylethyl]-2-hydroxyacetamide
Mus musculus
-
IC50: 3 nM
0.000002
(R)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]propyl]-2-hydroxyacetamide
Mus musculus
-
IC50: 2 nM
0.000002
(R)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]propyl]-2-hydroxyacetamide
Mus musculus
-
IC50: less than 2 nM
0.000002
(S)-2-(2-[[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]methyl]pyrrolidin-1-yl)-2-oxoethanol
Mus musculus
-
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
Mus musculus
-
IC50: 327 nM
0.000019
(S)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-1-methylethyl]-2-hydroxyacetamide
Mus musculus
-
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
Mus musculus
-
IC50: 2580 nM
0.000022
(S)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]propyl]-2-hydroxyacetamide
Mus musculus
-
IC50: 22 nM
0.000191
(S)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]propyl]-2-hydroxyacetamide
Mus musculus
-
IC50: 191 nM
0.00001
1-(4-(1H-pyrazol-1-yl)phenyl)-3-(2-aminoquinazolin-6-yl)-4-methylpyridin-2(1H)-one
Homo sapiens
c-Kit
0.0034
1-(4-(1H-pyrazol-1-yl)phenyl)-3-(2-aminoquinazolin-6-yl)-4-methylpyridin-2(1H)-one
Homo sapiens
KDR
0.00002
1-(4-acetylphenyl)-3-(2-aminoquinazolin-6-yl)-4-methylpyridin-2(1H)-one
Homo sapiens
c-Kit
0.005
1-(4-acetylphenyl)-3-(2-aminoquinazolin-6-yl)-4-methylpyridin-2(1H)-one
Homo sapiens
KDR
0.0003
1-(4-[5-[1-(cyclopentylmethyl)-6-(methylamino)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]pyridin-2-yl]piperazin-1-yl)-2,2-dimethylpropan-1-one
Homo sapiens
pH and temperature not specified in the publication
-
0.00061
1-(4-[5-[1-(cyclopentylmethyl)-6-(methylamino)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]pyridin-2-yl]piperazin-1-yl)-2,2-dimethylpropan-1-one
Homo sapiens
pH and temperature not specified in the publication
-
0.0072
1-(4-[5-[1-(cyclopentylmethyl)-6-(methylamino)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]pyridin-2-yl]piperazin-1-yl)-2,2-dimethylpropan-1-one
Homo sapiens
pH and temperature not specified in the publication
-
0.0001
1-(cyclopentylmethyl)-3-[6-(4-ethylpiperazin-1-yl)pyridin-3-yl]-N-methyl-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
-
0.00026
1-(cyclopentylmethyl)-3-[6-(4-ethylpiperazin-1-yl)pyridin-3-yl]-N-methyl-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
-
0.00028
1-(cyclopentylmethyl)-3-[6-(4-ethylpiperazin-1-yl)pyridin-3-yl]-N-methyl-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
-
0.00044
1-(cyclopentylmethyl)-3-[6-(4-ethylpiperazin-1-yl)pyridin-3-yl]-N-methyl-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
-
0.0018
1-(cyclopentylmethyl)-3-[6-(4-ethylpiperazin-1-yl)pyridin-3-yl]-N-methyl-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
-
0.0019
1-(cyclopentylmethyl)-3-[6-(4-ethylpiperazin-1-yl)pyridin-3-yl]-N-methyl-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
-
0.0025
1-(cyclopentylmethyl)-3-[6-(4-ethylpiperazin-1-yl)pyridin-3-yl]-N-methyl-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
-
0.0000014
1-(cyclopentylmethyl)-N-methyl-3-[4-(4-methylpiperazin-1-yl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
-
0.000006
1-(cyclopentylmethyl)-N-methyl-3-[4-(4-methylpiperazin-1-yl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
-
0.000013
1-(cyclopentylmethyl)-N-methyl-3-[4-(4-methylpiperazin-1-yl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
-
0.000066
1-(cyclopentylmethyl)-N-methyl-3-[4-(4-methylpiperazin-1-yl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
-
0.000068
1-(cyclopentylmethyl)-N-methyl-3-[4-(4-methylpiperazin-1-yl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
-
0.000092
1-(cyclopentylmethyl)-N-methyl-3-[4-(4-methylpiperazin-1-yl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
-
0.00042
1-(cyclopentylmethyl)-N-methyl-3-[4-(4-methylpiperazin-1-yl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
-
0.0006
1-(cyclopentylmethyl)-N-methyl-3-[4-(4-methylpiperazin-1-yl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
-
0.000008
1-(cyclopentylmethyl)-N-methyl-3-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
-
0.00003
1-(cyclopentylmethyl)-N-methyl-3-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
-
0.00006
1-(cyclopentylmethyl)-N-methyl-3-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
-
0.00007
1-(cyclopentylmethyl)-N-methyl-3-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
-
0.00036
1-(cyclopentylmethyl)-N-methyl-3-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
-
0.0004
1-(cyclopentylmethyl)-N-methyl-3-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
-
0.00048
1-(cyclopentylmethyl)-N-methyl-3-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
-
0.0035
1-(cyclopentylmethyl)-N-methyl-3-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
-
0.00367
1-(cyclopentylmethyl)-N-methyl-3-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
-
0.00002
1-(cyclopentylmethyl)-N-methyl-3-[6-(piperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
0.00005
1-(cyclopentylmethyl)-N-methyl-3-[6-(piperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
0.00012
1-(cyclopentylmethyl)-N-methyl-3-[6-(piperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
0.00064
1-(cyclopentylmethyl)-N-methyl-3-[6-(piperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
0.00069
1-(cyclopentylmethyl)-N-methyl-3-[6-(piperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
0.0011
1-(cyclopentylmethyl)-N-methyl-3-[6-(piperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
0.0021
1-(cyclopentylmethyl)-N-methyl-3-[6-(piperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
0.00025
1-[(1,3-dioxolan-2-yl)methyl]-3-(4-methoxyphenyl)-N-methyl-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
0.0012
1-[(1,3-dioxolan-2-yl)methyl]-3-(4-methoxyphenyl)-N-methyl-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
0.0013
1-[(1,3-dioxolan-2-yl)methyl]-3-(4-methoxyphenyl)-N-methyl-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
0.0075
1-[(1,3-dioxolan-2-yl)methyl]-3-(4-methoxyphenyl)-N-methyl-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
0.0087
1-[(1,3-dioxolan-2-yl)methyl]-3-(4-methoxyphenyl)-N-methyl-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
0.00012
1-[(1,3-dioxolan-2-yl)methyl]-N-methyl-3-[6-(piperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
0.00016
1-[(1,3-dioxolan-2-yl)methyl]-N-methyl-3-[6-(piperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
0.00053
1-[(1,3-dioxolan-2-yl)methyl]-N-methyl-3-[6-(piperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
0.0045
1-[(1,3-dioxolan-2-yl)methyl]-N-methyl-3-[6-(piperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
0.0062
1-[(1,3-dioxolan-2-yl)methyl]-N-methyl-3-[6-(piperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
0.0075
1-[(1,3-dioxolan-2-yl)methyl]-N-methyl-3-[6-(piperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
0.00038
1-[(1-benzyl-1H-1,2,3-triazol-4-yl)methyl]-N-methyl-3-[6-(piperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
0.0004
1-[(1-benzyl-1H-1,2,3-triazol-4-yl)methyl]-N-methyl-3-[6-(piperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
0.00053
1-[(1-benzyl-1H-1,2,3-triazol-4-yl)methyl]-N-methyl-3-[6-(piperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
0.0006
1-[(1-benzyl-1H-1,2,3-triazol-4-yl)methyl]-N-methyl-3-[6-(piperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
0.0007
1-[(1-benzyl-1H-1,2,3-triazol-4-yl)methyl]-N-methyl-3-[6-(piperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
0.00073
1-[(1-benzyl-1H-1,2,3-triazol-4-yl)methyl]-N-methyl-3-[6-(piperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
0.0009
1-[(1-benzyl-1H-1,2,3-triazol-4-yl)methyl]-N-methyl-3-[6-(piperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
0.0023
1-[(1-benzyl-1H-1,2,3-triazol-4-yl)methyl]-N-methyl-3-[6-(piperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
0.0076
1-[(1-benzyl-1H-1,2,3-triazol-4-yl)methyl]-N-methyl-3-[6-(piperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
Homo sapiens
pH and temperature not specified in the publication
0.00076
1-[4-(5-[1-[(1-benzyl-1H-1,2,3-triazol-4-yl)methyl]-6-(methylamino)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]pyridin-2-yl)piperazin-1-yl]-2,2-dimethylpropan-1-one
Homo sapiens
pH and temperature not specified in the publication
0.00084
1-[4-(5-[1-[(1-benzyl-1H-1,2,3-triazol-4-yl)methyl]-6-(methylamino)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]pyridin-2-yl)piperazin-1-yl]-2,2-dimethylpropan-1-one
Homo sapiens
pH and temperature not specified in the publication
0.0012
1-[4-(5-[1-[(1-benzyl-1H-1,2,3-triazol-4-yl)methyl]-6-(methylamino)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]pyridin-2-yl)piperazin-1-yl]-2,2-dimethylpropan-1-one
Homo sapiens
pH and temperature not specified in the publication
0.0045
1-[4-(5-[1-[(1-benzyl-1H-1,2,3-triazol-4-yl)methyl]-6-(methylamino)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]pyridin-2-yl)piperazin-1-yl]-2,2-dimethylpropan-1-one
Homo sapiens
pH and temperature not specified in the publication
0.0054
1-[4-(5-[1-[(1-benzyl-1H-1,2,3-triazol-4-yl)methyl]-6-(methylamino)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]pyridin-2-yl)piperazin-1-yl]-2,2-dimethylpropan-1-one
Homo sapiens
pH and temperature not specified in the publication
0.000001
3-(2-aminoquinazolin-6-yl)-1-(2-cyclopentylethyl)-4-methylpyridin-2(1H)-one
Homo sapiens
c-Kit
0.0014
3-(2-aminoquinazolin-6-yl)-1-(2-cyclopentylethyl)-4-methylpyridin-2(1H)-one
Homo sapiens
KDR
0.0000061
3-(2-aminoquinazolin-6-yl)-1-(3,3-dimethylindolin-6-yl)-4-methylpyridin-2(1H)-one
Homo sapiens
c-Kit
0.000048
3-(2-aminoquinazolin-6-yl)-1-(3,3-dimethylindolin-6-yl)-4-methylpyridin-2(1H)-one
Homo sapiens
KDR
0.00004
3-(2-aminoquinazolin-6-yl)-1-(3-fluoro-4-methylphenyl)-4-methylpyridin-2(1H)-one
Homo sapiens
c-Kit
0.005
3-(2-aminoquinazolin-6-yl)-1-(3-fluoro-4-methylphenyl)-4-methylpyridin-2(1H)-one
Homo sapiens
KDR
0.000065
3-(2-aminoquinazolin-6-yl)-1-(3-methoxyphenyl)-4-methylpyridin-2(1H)-one
Homo sapiens
c-Kit
0.005
3-(2-aminoquinazolin-6-yl)-1-(3-methoxyphenyl)-4-methylpyridin-2(1H)-one
Homo sapiens
KDR
0.00006
3-(2-aminoquinazolin-6-yl)-1-(4-chloro-3-fluorophenyl)-4-methylpyridin-2(1H)-one
Homo sapiens
c-Kit
0.005
3-(2-aminoquinazolin-6-yl)-1-(4-chloro-3-fluorophenyl)-4-methylpyridin-2(1H)-one
Homo sapiens
KDR
0.00002
3-(2-aminoquinazolin-6-yl)-1-(4-chlorophenyl)-4-methylpyridin-2(1H)-one
Homo sapiens
c-Kit
0.005
3-(2-aminoquinazolin-6-yl)-1-(4-chlorophenyl)-4-methylpyridin-2(1H)-one
Homo sapiens
KDR
0.000014
3-(2-aminoquinazolin-6-yl)-1-(4-fluoro-3-methylphenyl)-4-methylpyridin-2(1H)-one
Homo sapiens
c-Kit
0.0043
3-(2-aminoquinazolin-6-yl)-1-(4-fluoro-3-methylphenyl)-4-methylpyridin-2(1H)-one
Homo sapiens
KDR
0.000017
3-(2-aminoquinazolin-6-yl)-1-(4-methoxyphenyl)-4-methylpyridin-2(1H)-one
Homo sapiens
c-Kit
0.005
3-(2-aminoquinazolin-6-yl)-1-(4-methoxyphenyl)-4-methylpyridin-2(1H)-one
Homo sapiens
KDR
0.0000021
3-(2-aminoquinazolin-6-yl)-1-(4-tert-butylphenyl)-4-methylpyridin-2(1H)-one
Homo sapiens
c-Kit
0.000011
3-(2-aminoquinazolin-6-yl)-1-(4-tert-butylphenyl)-4-methylpyridin-2(1H)-one
Homo sapiens
KDR
0.000014
3-(2-aminoquinazolin-6-yl)-4-methyl-1-(3-(trifluoromethyl)phenyl)pyridin-2(1H)-one
Homo sapiens
c-Kit
0.005
3-(2-aminoquinazolin-6-yl)-4-methyl-1-(3-(trifluoromethyl)phenyl)pyridin-2(1H)-one
Homo sapiens
KDR
0.000022
3-(2-aminoquinazolin-6-yl)-4-methyl-1-(4-(oxazol-2-yl)phenyl)pyridin-2(1H)-one
Homo sapiens
c-Kit
0.005
3-(2-aminoquinazolin-6-yl)-4-methyl-1-(4-(oxazol-2-yl)phenyl)pyridin-2(1H)-one
Homo sapiens
KDR
0.0000079
3-(2-aminoquinazolin-6-yl)-4-methyl-1-(4-(trifluoromethyl)phenyl)pyridin-2(1H)-one
Homo sapiens
c-Kit
0.0018
3-(2-aminoquinazolin-6-yl)-4-methyl-1-(4-(trifluoromethyl)phenyl)pyridin-2(1H)-one
Homo sapiens
KDR
0.000013
3-(2-aminoquinazolin-6-yl)-4-methyl-1-(4-morpholinophenyl)pyridin-2(1H)-one
Homo sapiens
c-Kit
0.0044
3-(2-aminoquinazolin-6-yl)-4-methyl-1-(4-morpholinophenyl)pyridin-2(1H)-one
Homo sapiens
KDR
0.00021
3-(2-aminoquinazolin-6-yl)-4-methyl-1-phenylpyridin-2(1H)-one
Homo sapiens
c-Kit
0.001
3-(2-aminoquinazolin-6-yl)-4-methyl-1-phenylpyridin-2(1H)-one
Homo sapiens
KDR
0.00002
3-[[5-([6-amino-5-[(E)-(methoxyimino)methyl]pyrimidin-4-yl]amino)-1H-indazol-1-yl]methyl]benzonitrile
Homo sapiens
-
0.000044
3-[[5-([6-amino-5-[(E)-(methoxyimino)methyl]pyrimidin-4-yl]amino)-1H-indazol-1-yl]methyl]benzonitrile
Homo sapiens
-
0.0000002
4-(5-((4-chlorophenyl)carbamoyl)naphthalen-2-yloxy)-7-methoxyquinoline-6-carboxamide
Homo sapiens
KDR enzyme
0.000003
4-(5-((4-chlorophenyl)carbamoyl)naphthalen-2-yloxy)-7-methoxyquinoline-6-carboxamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.000003
4-(5-((4-chlorophenyl)carbamoyl)naphthalen-2-yloxy)-N-methylpicolinamide
Homo sapiens
KDR enzyme
0.00021
4-(5-((4-chlorophenyl)carbamoyl)naphthalen-2-yloxy)-N-methylpicolinamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.000306
4-amino-6-(1H-indazol-5-ylamino)pyrimidine-5-carbaldehyde O-methyloxime
Homo sapiens
-
0.004123
4-amino-6-(1H-indazol-5-ylamino)pyrimidine-5-carbaldehyde O-methyloxime
Homo sapiens
-
0.000012
4-amino-6-([3-chloro-4-[(3-fluorobenzyl)oxy]phenyl]amino)pyrimidine-5-carbaldehyde O-methyloxime
Homo sapiens
-
0.000018
4-amino-6-([3-chloro-4-[(3-fluorobenzyl)oxy]phenyl]amino)pyrimidine-5-carbaldehyde O-methyloxime
Homo sapiens
-
0.000022
4-amino-6-[(1-benzyl-1H-indazol-5-yl)amino]pyrimidine-5-carbaldehyde O-methyloxime
Homo sapiens
-
0.000044
4-amino-6-[(1-benzyl-1H-indazol-5-yl)amino]pyrimidine-5-carbaldehyde O-methyloxime
Homo sapiens
-
0.001123
4-amino-6-[(3-chloro-4-fluorobenzyl)amino]pyrimidine-5-carbaldehyde O-methyloxime
Homo sapiens
-
0.00522
4-amino-6-[(3-chloro-4-fluorobenzyl)amino]pyrimidine-5-carbaldehyde O-methyloxime
Homo sapiens
-
0.000023
4-amino-6-[[1-(3-chlorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
Homo sapiens
-
0.00003
4-amino-6-[[1-(3-chlorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
Homo sapiens
-
0.000014
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(1-methylethyl)oxime
Homo sapiens
-
0.000025
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(1-methylethyl)oxime
Homo sapiens
-
0.000047
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(2-methoxybenzyl)oxime
Homo sapiens
-
0.000435
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(2-methoxybenzyl)oxime
Homo sapiens
-
0.000006
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(2-methoxyethyl)oxime
Homo sapiens
-
0.000014
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(2-methoxyethyl)oxime
Homo sapiens
-
0.000032
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(2-methylpropyl)oxime
Homo sapiens
-
0.000173
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-(2-methylpropyl)oxime
Homo sapiens
-
0.000023
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-benzyloxime
Homo sapiens
-
0.000095
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-benzyloxime
Homo sapiens
-
0.000005
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-ethyloxime
Homo sapiens
-
0.000007
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-ethyloxime
Homo sapiens
-
0.000012
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde oxime
Homo sapiens
-
0.000042
4-amino-6-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde oxime
Homo sapiens
-
0.000013
4-amino-6-[[1-(3-fluorobenzyl)-1H-indol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
Homo sapiens
-
0.000027
4-amino-6-[[1-(3-fluorobenzyl)-1H-indol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
Homo sapiens
-
0.000057
4-amino-6-[[1-(3-fluorobenzyl)-2,3-dihydro-1H-indol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
Homo sapiens
-
0.000255
4-amino-6-[[1-(3-fluorobenzyl)-2,3-dihydro-1H-indol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
Homo sapiens
-
0.000104
4-amino-6-[[1-(4-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
Homo sapiens
-
0.000189
4-amino-6-[[1-(4-fluorobenzyl)-1H-indazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
Homo sapiens
-
0.000048
4-amino-6-[[2-(3-fluorobenzyl)-1H-benzimidazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
Homo sapiens
-
0.000076
4-amino-6-[[2-(3-fluorobenzyl)-1H-benzimidazol-5-yl]amino]pyrimidine-5-carbaldehyde O-methyloxime
Homo sapiens
-
0.000016
4-amino-6-[[4-(benzyloxy)-3-chlorophenyl]amino]pyrimidine-5-carbaldehyde O-methyloxime
Homo sapiens
-
0.000153
4-amino-6-[[4-(benzyloxy)-3-chlorophenyl]amino]pyrimidine-5-carbaldehyde O-methyloxime
Homo sapiens
-
0.025
6-(1H-indol-5-ylmethyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
Homo sapiens
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
Homo sapiens
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
Homo sapiens
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
Homo sapiens
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
Homo sapiens
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
Homo sapiens
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
Homo sapiens
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
Homo sapiens
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
Homo sapiens
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
Homo sapiens
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
Homo sapiens
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
Homo sapiens
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
Homo sapiens
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
Homo sapiens
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
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000002
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(2-fluorophenyl)-1-naphthamide
Homo sapiens
KDR enzyme
0.000007
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(2-fluorophenyl)-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.0000005
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(3-(trifluoromethyl)phenyl)-1-naphthamide
Homo sapiens
KDR enzyme
0.000034
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(3-(trifluoromethyl)phenyl)-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.0000006
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(3-fluorophenyl)-1-naphthamide
Homo sapiens
KDR enzyme
0.000003
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(3-fluorophenyl)-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.000001
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(3-methylisoxazol-5-yl)-1-naphthamide
Homo sapiens
KDR enzyme
0.000007
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(3-methylisoxazol-5-yl)-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.0000005
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(4-(trifluoromethyl)phenyl)-1-naphthamide
Homo sapiens
KDR enzyme
0.000016
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(4-(trifluoromethyl)phenyl)-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.000001
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(4-fluorophenyl)-1-naphthamide
Homo sapiens
KDR enzyme
0.000002
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(4-fluorophenyl)-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.0000006
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(5-methylisoxazol-3-yl)-1-naphthamide
Homo sapiens
KDR enzyme
0.000006
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(5-methylisoxazol-3-yl)-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.0000002
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(isoxazol-3-yl)-1-naphthamide
Homo sapiens
KDR enzyme
0.0000004
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(isoxazol-3-yl)-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.0000008
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(pyridin-2-yl)-1-naphthamide
Homo sapiens
KDR enzyme
0.000002
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(pyridin-2-yl)-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.0000008
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(pyridin-3-yl)-1-naphthamide
Homo sapiens
KDR enzyme
0.000002
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(pyridin-3-yl)-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.000002
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(pyridin-4-yl)-1-naphthamide
Homo sapiens
KDR enzyme
0.000002
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(pyridin-4-yl)-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.0000003
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(thiazol-2-yl)-1-naphthamide
Homo sapiens
KDR enzyme
0.000002
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(thiazol-2-yl)-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.000004
6-(6,7-dimethoxyquinolin-4-yloxy)-N-isopropyl-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.000005
6-(6,7-dimethoxyquinolin-4-yloxy)-N-isopropyl-1-naphthamide
Homo sapiens
KDR enzyme
0.0000059
6-(6,7-dimethoxyquinolin-4-yloxy)-N-isopropyl-1-naphthamide
Homo sapiens
-
0.0000005
6-(6,7-dimethoxyquinolin-4-yloxy)-N-p-tolyl-1-naphthamide
Homo sapiens
KDR enzyme
0.000002
6-(6,7-dimethoxyquinolin-4-yloxy)-N-p-tolyl-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.0000002
6-(6,7-dimethoxyquinolin-4-yloxy)-N-phenyl-1-naphthamide
Homo sapiens
KDR enzyme
0.0000008
6-(6,7-dimethoxyquinolin-4-yloxy)-N-phenyl-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.0000013
6-(6,7-dimethoxyquinolin-4-yloxy)-N-propyl-1-naphthamide
Homo sapiens
-
0.0000013
6-(6,7-dimethoxyquinolin-4-yloxy)-N-propyl-1-naphthamide
Homo sapiens
KDR enzyme
0.000007
6-(6,7-dimethoxyquinolin-4-yloxy)-N-propyl-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.000028
6-(7H-pyrrolo[2,3-d]pyrimidin-4-yloxy)-N-(4-chlorophenyl)-1-naphthamide
Homo sapiens
KDR enzyme
0.000037
6-(7H-pyrrolo[2,3-d]pyrimidin-4-yloxy)-N-(4-chlorophenyl)-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.09
6-[4-fluoro-3-(trifluoromethyl)benzyl]-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.122
6-[4-fluoro-3-(trifluoromethyl)benzyl]-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.2
6-[4-fluoro-3-(trifluoromethyl)benzyl]-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.057
6-[4-fluoro-3-(trifluoromethyl)benzyl]-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.164
6-[4-fluoro-3-(trifluoromethyl)benzyl]-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.2
6-[4-fluoro-3-(trifluoromethyl)benzyl]-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.5
6-[4-fluoro-3-(trifluoromethyl)benzyl]-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000007
BGB324
Homo sapiens
pH and temperature not specified in the publication
-
0.0000026
BGB324
Homo sapiens
pH and temperature not specified in the publication
-
0.000003
BGB324
Homo sapiens
pH and temperature not specified in the publication
-
0.000008
BGB324
Homo sapiens
pH and temperature not specified in the publication
-
0.000015
BGB324
Homo sapiens
pH and temperature not specified in the publication
-
0.000017
BGB324
Homo sapiens
pH and temperature not specified in the publication
-
0.001
BGB324
Homo sapiens
pH and temperature not specified in the publication
-
0.0034
BGB324
Homo sapiens
pH and temperature not specified in the publication
-
0.000017
ethyl 4-(3-(2-aminoquinazolin-6-yl)-4-methyl-2-oxopyridin-1(2H)-yl)benzoate
Homo sapiens
c-Kit
0.005
ethyl 4-(3-(2-aminoquinazolin-6-yl)-4-methyl-2-oxopyridin-1(2H)-yl)benzoate
Homo sapiens
KDR
0.00003
imatinib
Homo sapiens
-
IC50: 30 nM
0.000052
imatinib
Homo sapiens
c-Kit
0.025
imatinib
Homo sapiens
KDR
0.0000703
methyl (3Z)-3-(3-[[2-(diethylamino)ethyl]carbamoyl]-2-methyl-1,4,5,6-tetrahydro-7H-indol-7-ylidene)-2-oxo-2,3-dihydro-1H-indole-5-carboxylate
Homo sapiens
-
PDGFR-beta, pH and temperature not specified in the publication
0.0001672
methyl (3Z)-3-(3-[[2-(diethylamino)ethyl]carbamoyl]-2-methyl-1,4,5,6-tetrahydro-7H-indol-7-ylidene)-2-oxo-2,3-dihydro-1H-indole-5-carboxylate
Homo sapiens
-
VEGFR-2, pH and temperature not specified in the publication
0.0002557
methyl (3Z)-3-(3-[[2-(diethylamino)ethyl]carbamoyl]-2-methyl-1,4,5,6-tetrahydro-7H-indol-7-ylidene)-2-oxo-2,3-dihydro-1H-indole-5-carboxylate
Homo sapiens
-
c-Kit, pH and temperature not specified in the publication
0.00043
methyl 3-[4-([6-(methylamino)-3-[4-(piperazin-1-yl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl]methyl)-1H-1,2,3-triazol-1-yl]thiophene-2-carboxylate
Homo sapiens
pH and temperature not specified in the publication
0.00078
methyl 3-[4-([6-(methylamino)-3-[4-(piperazin-1-yl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl]methyl)-1H-1,2,3-triazol-1-yl]thiophene-2-carboxylate
Homo sapiens
pH and temperature not specified in the publication
0.00086
methyl 3-[4-([6-(methylamino)-3-[4-(piperazin-1-yl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl]methyl)-1H-1,2,3-triazol-1-yl]thiophene-2-carboxylate
Homo sapiens
pH and temperature not specified in the publication
0.0089
methyl 3-[4-([6-(methylamino)-3-[4-(piperazin-1-yl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl]methyl)-1H-1,2,3-triazol-1-yl]thiophene-2-carboxylate
Homo sapiens
pH and temperature not specified in the publication
0.000002
N-(2,4-dichlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
Homo sapiens
KDR enzyme
0.000014
N-(2,4-dichlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.0000003
N-(3,5-dichlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
Homo sapiens
KDR enzyme
0.000028
N-(3,5-dichlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.0000003
N-(3-chlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
Homo sapiens
KDR enzyme
0.0000051
N-(3-chlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.000001
N-(4-chloro-3-(trifluoromethyl)phenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
Homo sapiens
KDR enzyme
0.000247
N-(4-chloro-3-(trifluoromethyl)phenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.000023
N-(4-chlorophenyl)-3-(6,7-dimethoxyquinolin-4-yloxy)isoquinoline-8-carboxamide
Homo sapiens
KDR enzyme
0.000175
N-(4-chlorophenyl)-3-(6,7-dimethoxyquinolin-4-yloxy)isoquinoline-8-carboxamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.000007
N-(4-chlorophenyl)-6-(2-(methylamino)pyridin-4-yloxy)-1-naphthamide
Homo sapiens
KDR enzyme
0.00014
N-(4-chlorophenyl)-6-(2-(methylamino)pyridin-4-yloxy)-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.000046
N-(4-chlorophenyl)-6-(2-(methylamino)pyrimidin-4-yloxy)-1-naphthamide
Homo sapiens
KDR enzyme
0.000296
N-(4-chlorophenyl)-6-(2-(methylamino)pyrimidin-4-yloxy)-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.00002
N-(4-chlorophenyl)-6-(3-fluoro-6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
Homo sapiens
KDR enzyme
0.000069
N-(4-chlorophenyl)-6-(3-fluoro-6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.000002
N-(4-chlorophenyl)-6-(6,7-dimethoxyquinazolin-4-yloxy)-1-naphthamide
Homo sapiens
KDR enzyme
0.000002
N-(4-chlorophenyl)-6-(6,7-dimethoxyquinazolin-4-yloxy)-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.000008
N-(4-chlorophenyl)-6-(6,7-dimethoxyquinolin-4-ylamino)-1-naphthamide
Homo sapiens
KDR enzyme
0.000014
N-(4-chlorophenyl)-6-(6,7-dimethoxyquinolin-4-ylamino)-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.0000005
N-(4-chlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
Homo sapiens
KDR enzyme
0.000008
N-(4-chlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.0000003
N-(4-chlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-5-fluoro-1-naphthamide
Homo sapiens
KDR enzyme
0.000002
N-(4-chlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-5-fluoro-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.00002
N-(4-chlorophenyl)-6-(6-(methylamino)pyrimidin-4-yloxy)-1-naphthamide
Homo sapiens
KDR enzyme
0.000106
N-(4-chlorophenyl)-6-(6-(methylamino)pyrimidin-4-yloxy)-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.000001
N-(4-chlorophenyl)-6-(7-methoxyquinolin-4-yloxy)-1-naphthamide
Homo sapiens
KDR enzyme
0.000008
N-(4-chlorophenyl)-6-(7-methoxyquinolin-4-yloxy)-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.000018
N-(4-chlorophenyl)-6-(pyridin-4-yloxy)-1-naphthamide
Homo sapiens
KDR enzyme
0.00022
N-(4-chlorophenyl)-6-(pyridin-4-yloxy)-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.000004
N-(4-chlorophenyl)-6-(quinolin-4-yloxy)-1-naphthamide
Homo sapiens
KDR enzyme
0.000034
N-(4-chlorophenyl)-6-(quinolin-4-yloxy)-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.00001
N-(4-chlorophenyl)-7-(6,7-dimethoxyquinolin-4-yloxy)quinoline-4-carboxamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.000022
N-(4-chlorophenyl)-7-(6,7-dimethoxyquinolin-4-yloxy)quinoline-4-carboxamide
Homo sapiens
KDR enzyme
0.0000007
N-(4-tert-butylphenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
Homo sapiens
KDR enzyme
0.000063
N-(4-tert-butylphenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.0000008
N-(5-tert-butylisoxazol-3-yl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
Homo sapiens
KDR enzyme
0.000068
N-(5-tert-butylisoxazol-3-yl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.000011
N-(cyclopropylmethyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
Homo sapiens
-
0.000015
N-(cyclopropylmethyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
Homo sapiens
KDR enzyme
0.00007
N-(cyclopropylmethyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.0000013
N-cyclobutyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
Homo sapiens
-
0.000003
N-cyclobutyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
Homo sapiens
KDR enzyme
0.000007
N-cyclobutyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.000007
N-cyclopentyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.000009
N-cyclopentyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
Homo sapiens
KDR enzyme
0.000015
N-cyclopentyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
Homo sapiens
-
0.0000006
N-cyclopropyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
Homo sapiens
-
0.0000006
N-cyclopropyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
Homo sapiens
KDR enzyme
0.000001
N-cyclopropyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
Homo sapiens
VEGF driven proliferation of HUVEC cell
0.000004
N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]ethyl]-2-hydroxyacetamide
Mus musculus
-
IC50: 4 nM, potent, orally active inhibitor when co-administered with the cytochrome P450 inhibitor 1-aminobenzotriazole
0.000035
N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]ethyl]-2-hydroxyacetamide
Mus musculus
-
IC50: 35 nM, potent, orally active inhibitor when co-administered with the cytochrome P450 inhibitor 1-aminobenzotriazole
0.000077
N3-(6-aminopyridin-3-yl)-N1-(2-cyclopentylethyl)-4-methylisophthalamide
Homo sapiens
c-Kit
0.025
N3-(6-aminopyridin-3-yl)-N1-(2-cyclopentylethyl)-4-methylisophthalamide
Homo sapiens
KDR
0.0001
N4-(2-fluoro-4-chlorophenyl)-6-(2,5-dimethoxybenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.185
N4-(2-fluoro-4-chlorophenyl)-6-(2,5-dimethoxybenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0241
N4-(3-bromo,4-fluorophenyl)-6-(2-pyridin-2-yl-ethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0859
N4-(3-bromo,4-fluorophenyl)-6-(2-pyridin-2-yl-ethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0936
N4-(3-bromo,4-fluorophenyl)-6-(2-pyridin-2-yl-ethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0018
N4-(3-bromo-phenyl)-7-(3,4,5-trimethoxy-benzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0257
N4-(3-bromo-phenyl)-7-(3,4,5-trimethoxy-benzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0149
N4-(3-bromophenyl)-7-(1-naphthylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.129
N4-(3-bromophenyl)-7-(1-naphthylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0015
N4-(3-bromophenyl)-7-(2-chlorobenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0179
N4-(3-bromophenyl)-7-(2-chlorobenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00048
N4-(4-chloro-2-fluorophenyl)-6-(1-naphthylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.2
N4-(4-chloro-2-fluorophenyl)-6-(1-naphthylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.016
N4-(4-chloro-2-fluorophenyl)-6-(2-methylbenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0298
N4-(4-chloro-2-fluorophenyl)-6-(2-methylbenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0152
N4-(4-chlorophenyl)-6-(2,5-dimethoxybenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0567
N4-(4-chlorophenyl)-6-(2,5-dimethoxybenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000004
sunitinib
Homo sapiens
-
VEGFR-2, pH and temperature not specified in the publication
0.0000089
sunitinib
Homo sapiens
-
c-Kit, pH and temperature not specified in the publication
0.0000106
sunitinib
Homo sapiens
-
PDGFR, pH and temperature not specified in the publication
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C289S
strong ligand-triggered phosphorylation as for the wild-type DDR1. In the absence of beta-mercaptoethanol, forms dimers (250 kDa). Binds to immobilized collagen at comparable levels as the wild-type. DDR1b and C289S constructs bind to collagen-agarose beads equally well
C303S
no ligand-triggered phosphorylation. In the absence of beta-mercaptoethanol, does not form dimers. Has a significantly lower affinity to bind to immobilized collagen, relative to wild type DDR1. Shows no affinity to collagen-agarose beads
C348S
no ligand-triggered phosphorylation. In the absence of beta-mercaptoethanol, does not form dimers. Has a significantly lower affinity to bind to immobilized collagen, relative to wild type DDR1. Shows no affinity to collagen-agarose beads
C379R
-
the mutation is linked to osteoglophonic dysplasia
C717S
the mutant has activity comparable to that of the wild type enzyme and is poorly inhibited by the quinazolines
D816F
-
c-Kit mutant, in patients with aggressive mastocytosis or AML patients
D816H
-
c-Kit mutant, in patients with aggressive mastocytosis or AML patients
D816Y
-
c-Kit mutant, in patients with aggressive mastocytosis or AML patients
D835Y
-
FLT3 mutant, in 7% of AML patients
DELTA746-750
-
the in-frame deletion mutant is active but exhibits a higher KM for ATP and a lower Ki for erlotinib relative to the wild-type receptor
G370C
-
the mutation is linked to thanatophoric dysplasia I and bladder cancer
G375C
-
the mutation is linked to achondroplasia, the most common form of human dwarfism
G382D
-
the mutation is linked to multiple myeloma
G388R
-
the mutation is linked to tumor progression
I654V
-
the mutation is linked to increased risk of breast cancer
K1018A
-
construction of a defective-enzyme mutant CHO-1018 cell line which shows a loss in ATP-binding activity and thus in PTK function
K1110A
-
dead Met kinase, present at the plasma membrane
K1114M
-
kinase dead mutant of RON, which does not exhibit any tyrosine phosphorylation in HeLa cells
K634A
-
site-directed mutagenesis PDGFbeta receptor tyrosine kinase, results in impaired tyrosine autophosphorylation and maturation, as well as loss of kinase activity
K644A
-
site-directed mutagenesis of juxtamembrane tandem mutagenic construct of FLT-3 RTK and of wild-type FLT-3 RTK, maturation of the mutants by glycosylation and phosphorylation is impaired, altered localization compaired to the wild-type enzyme, overview
K758M
mutant shows no tyrosine kinase activity
L858R
-
mutant is active but exhibits a higher KM for ATP and a lower Ki for erlotinib relative to the wild-type receptor
L861Q
-
comparable activity to the wild-type receptor
R844C
-
less stable and active than the wild-type enzyme
S371C
-
the mutation is linked to thanatophoric dysplasia I
S372C
-
the mutation is linked to Beare-Stevenson cutis gyrata syndrome
T373C
-
the mutation is linked to thanatophoric dysplasia I and bladder cancer
T518M
ROR1 T518M polymorphism does not associate with prognostically distinct B-CLL subtypes
T670I
-
cKit mutant, that renders patients with gastrointestinal stromal tumor refractory to imatinib
V381E
-
the mutation is linked to hypochondroplasia
V560G
-
c-Kit mutant, juxtamembrane mutation
V916T
KDR mutant, which shares the majority of residues with c-Kit in the ATP binding pocket. Inhibitor 3-(2-aminoquinazolin-6-yl)-4-methyl-1-(3-(trifluoromethyl)phenyl)pyridin-2(1H)-one binds in the DFG-out conformation. Two nitrogens from the aminoquinazoline portion of the molecule form hydrogen bonding interactions with linker region of the enzyme at Cys673. The pyridone scaffold is further anchored by the hydrogen bond contacts between its carbonyl group and Asp810
Y1003F
-
coimmunoprecipitates with D/A mutants of PTP1B and TCPTP, although the interaction is decreased when compared to wild-type Met with TCPTP
Y1234/Y1235F
-
substitution of both tyrosine residues additionally decreases the ability of both TCPTP (D/A) and PTP1B (D/A) mutants to coimmunoprecipitate with Met
Y1234F
-
coimmunoprecipitation of tyrosine-phosphorylated Met with TCPTP (D/A) or PTP1B (D/A) decreases significantly
Y123F
-
coimmunoprecipitation of tyrosine-phosphorylated Met with TCPTP (D/A) or PTP1B (D/A) decreases significantly
Y1349F
-
no significant decrease in the ability of PTP1B D/A or TCPTP D/A mutants to coimmunoprecipitate
Y1349F/Y1356F
-
no significant decrease in the ability of PTP1B D/A or TCPTP D/A mutants to coimmunoprecipitate
Y1356F
-
no significant decrease in the ability of PTP1B D/A or TCPTP D/A mutants to coimmunoprecipitate
Y372C
-
the mutation is linked to osteoglophonic dysplasia
Y375C
-
the mutation is linked to Beare-Stevenson cutis gyrata syndrome
Y687F
mutation disrupts RET autophosphorylation
Y719F
-
c-Kit mutant, does not abolish kinase activity
Y740F/Y751F
-
site-directed mutagenesis, reduced activity with GRK2 compared to the wild-type enzyme, the mutant cannot recruit phosphoinositide 3-kinase
Y857F
-
site-directed mutagenesis, mutant shows reduced sensitivity to GRK2 inhibitory phosphorylation compared to the wild-type PDGFRbeta
Y900/905F
mutant shows significant lower levels of Y981 phosphorylation despite no effect on total phosphorylation
Y900F
mutation does not disrupt RET autophosphorylation
Y905F
mutation does not disrupt RET autophosphorylation
Y981F
mutation does not disrupt RET autophosphorylation
D1232V
-
is more active than the wild-type, produces tumors in nude mice and is highly metastatic
DELTA(T573-H579)
-
c-Kit mutant, juxtamembrane mutation
M1231T
-
equivalent tumor latency and 100% tumor formation as the wild-type
M1254T
-
is more active than the wild-type, produces tumors in nude mice and is highly metastatic
Y719F
-
c-Kit mutant, knock-in mouse, which does not show an apparent abnormality in hematopoiesis
V664E
oncogenic mutation in TM domain, mutation increases the dimerizing propensities of the transmembrane domains
A391E
-
the mutation is linked to Crouzon syndrome with acanthosis nigricans and bladder cancer
A391E
germ-line mutation in Crouzon syndrome with acanthosis nigricans. The transmembrane domains are able to dimerize, and mutation A391E increases the cross-linking propensities of the two domains
D816V
-
c-Kit mutant, in patients with aggressive mastocytosis or AML patients
D816V
-
FLT3 mutant, in 7% of AML patients
G380R
-
the mutation is linked to achondroplasia with acanthosis nigricans
G380R
-
the mutation is linked to achondroplasia, the most common form of human dwarfism
K650E
-
naturally occuring activating-mutation of the enzyme causing thanatophoric dysplasia
K650E
-
FGFR3 mutant, activating mutation
Y766F
the Y766F FGF receptor mutant is unable to associate with tyrosine-phosphorylate PLC gamma or to stimulate hydrolysis of phosphatidylinositol. Nevertheless, the Y766F FGF receptor mutant can be autophosphorylated, and can phosphorylate several cellular proteins and stimulate DNA synthesis
Y766F
fibroblast growth factor receptor with the single point mutation fails to associate with PLC gamma in response to FGF. The mutant receptor also fails to mediate PtdIns hydrolysis and Ca2+ mobilization after FGF stimulation. However, the mutant receptor phosphorylats itself and several other cellular proteins, and it mediats mitogenesis in response to FGF
additional information
mutations in the Caenorhabditis elegans let-23 EGFR-like gene
additional information
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mutations in the Caenorhabditis elegans let-23 EGFR-like gene
additional information
c-Kit mutant, juxtamembrane mutation
additional information
a single amino acid substitution in the ATP-binding site of the putative kinase domain results in the synthesis of an inactive sev protein unable to determine cell fate
additional information
integration of proviral DNA into the PDGF beta-receptor gene in HTLV-I-infected T-cells results in a novel tyrosine kinase product with transforming activity
additional information
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integration of proviral DNA into the PDGF beta-receptor gene in HTLV-I-infected T-cells results in a novel tyrosine kinase product with transforming activity
additional information
c-kit gene mutations in three patients with piebaldism: a missense substitution Phe584-Leu, within the tyrosine kinase domain, is associated with a severe piebald phenotype, whereas two different frameshifts, within codons 561 and 642, are both associated with a variable and relatively mild piebald phenotype
additional information
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c-kit gene mutations in three patients with piebaldism: a missense substitution Phe584-Leu, within the tyrosine kinase domain, is associated with a severe piebald phenotype, whereas two different frameshifts, within codons 561 and 642, are both associated with a variable and relatively mild piebald phenotype
additional information
conversion of Asp-816 to Val in human c-kitR may be an activating mutation and responsible for the constitutive activation of c-kitR in HMC-1 cells
additional information
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conversion of Asp-816 to Val in human c-kitR may be an activating mutation and responsible for the constitutive activation of c-kitR in HMC-1 cells
additional information
piebaldism is an autosomal dominant genetic disorder that results from Gly664Arg mutations within the tyrosine kinase domain of the c-Kit protooncogene
additional information
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piebaldism is an autosomal dominant genetic disorder that results from Gly664Arg mutations within the tyrosine kinase domain of the c-Kit protooncogene
additional information
human piebald trait resulting from a dominant negative mutant allele of the c-kit membrane receptor gene
additional information
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human piebald trait resulting from a dominant negative mutant allele of the c-kit membrane receptor gene
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
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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
FGFR2 exon IIIa and IIIc mutations in Crouzon, Jackson-Weiss, and Pfeiffer syndromes, missense changes, insertions, and a deletion due to alternative RNA splicing
additional information
mutations in the fibroblast growth factor receptor 2 gene cause Crouzon syndrome
additional information
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mutations in the fibroblast growth factor receptor 2 gene cause Crouzon syndrome
additional information
ephrin type-A receptor 1 may be involved in the neoplastic process of some tumors
additional information
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ephrin type-A receptor 1 may be involved in the neoplastic process of some tumors
additional information
the mutations in FGFR2-associated craniosynostoses are clustered in five structural elements of immunoglobulin-like domain III of the receptor
additional information
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the mutations in FGFR2-associated craniosynostoses are clustered in five structural elements of immunoglobulin-like domain III of the receptor
additional information
identical mutations in the FGFR2 gene cause both Pfeiffer and Crouzon syndrome phenotypes
additional information
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identical mutations in the FGFR2 gene cause both Pfeiffer and Crouzon syndrome phenotypes
additional information
A to G transition is found at position 886 in exon 5 of the fibroblast growth factor receptor 2 in members of a family with Crouzon phenotype and plagiocephaly
additional information
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A to G transition is found at position 886 in exon 5 of the fibroblast growth factor receptor 2 in members of a family with Crouzon phenotype and plagiocephaly
additional information
Jackson-Weiss syndrome and Crouzon syndrome are allelic with mutations in fibroblast growth factor receptor 2
additional information
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Jackson-Weiss syndrome and Crouzon syndrome are allelic with mutations in fibroblast growth factor receptor 2
additional information
Apert syndrome results from localized mutations of FGFR2 and is allelic with Crouzon syndrome
additional information
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Apert syndrome results from localized mutations of FGFR2 and is allelic with Crouzon syndrome
additional information
mutations in the third immunoglobulin domain of the fibroblast growth factor receptor-2 gene in Crouzon syndrome
additional information
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mutations in the third immunoglobulin domain of the fibroblast growth factor receptor-2 gene in Crouzon syndrome
additional information
FGFR2 mutations in Pfeiffer syndrome
additional information
FGFR2 mutations associated with a spectrum of craniosyostosis phenotypes: tyrosine 105 to cysteine, glycine 338 to glutamic acid, serine 351 to cysteine and glycine 384 to arginine
additional information
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FGFR2 mutations associated with a spectrum of craniosyostosis phenotypes: tyrosine 105 to cysteine, glycine 338 to glutamic acid, serine 351 to cysteine and glycine 384 to arginine
additional information
Crouzon syndrome: deletion, duplication, and point mutation within FGFR2 gene
additional information
Pfeiffer's syndrome results from an S351C mutation in the fibroblast growth factor receptor-2 gene
additional information
mutations 934C to G and 937C to G of fibroblast growth factor receptor 2 gene in Chinese patients with Apert syndrome
additional information
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mutations 934C to G and 937C to G of fibroblast growth factor receptor 2 gene in Chinese patients with Apert syndrome
additional information
Apert syndrome is characterised by syndactyly of the hands and feet, recurrent mutations of a serine-proline dipeptide, either Ser252Trp or Pro253Arg, in the linker between the IgII and IgIII extracellular immunoglobulin-like domains. A C to T mutation that predicts a Ser252Leu substitution, ascertained in a boy with mild Crouzon syndrome is also present in three clinically normal members of his family. A CG to TT mutation that predicts a Ser252Phe substitution results in a phenotype consistent with Apert syndrome. Finally, a CGC to TCT mutation that predicts a double amino acid substitution, Ser252Phe and Pro253Ser, causes a Pfeiffer syndrome variant with mild craniosynostosis, broad thumbs and big toes, fixed extension of several digits, and only minimal cutaneous syndactyly
additional information
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Apert syndrome is characterised by syndactyly of the hands and feet, recurrent mutations of a serine-proline dipeptide, either Ser252Trp or Pro253Arg, in the linker between the IgII and IgIII extracellular immunoglobulin-like domains. A C to T mutation that predicts a Ser252Leu substitution, ascertained in a boy with mild Crouzon syndrome is also present in three clinically normal members of his family. A CG to TT mutation that predicts a Ser252Phe substitution results in a phenotype consistent with Apert syndrome. Finally, a CGC to TCT mutation that predicts a double amino acid substitution, Ser252Phe and Pro253Ser, causes a Pfeiffer syndrome variant with mild craniosynostosis, broad thumbs and big toes, fixed extension of several digits, and only minimal cutaneous syndactyly
additional information
Trp290Cys mutation in exon IIIa of the fibroblast growth factor receptor 2 gene is associated with Pfeiffer syndrome
additional information
achondroplasia is defined by recurrent G380R mutations of FGFR3
additional information
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achondroplasia is defined by recurrent G380R mutations of FGFR3
additional information
frequent activating mutations of FGFR3 in human bladder and cervix carcinomas
additional information
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frequent activating mutations of FGFR3 in human bladder and cervix carcinomas
additional information
a sporadic mutation causing a Lys650Glu change in the tyrosine kinase domain of FGFR3 is found in 16 of 16 individuals with one type of thanatophoric dysplasia. Of 39 individuals with a second type of thanatophoric dysplasia, 22 have a mutation causing an Arg248Cys change and one has a Ser371Cys substitution, both in the extracellular region of the protein
additional information
FGFR3 is a possible candidate for the Huntington disease gene
additional information
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FGFR3 is a possible candidate for the Huntington disease gene
additional information
Asn540Thr substitution in the fibroblast growth factor receptor 3 tyrosine kinase domain causes hypochondroplasia
additional information
constitutive activation of fibroblast growth factor receptor 3 by the transmembrane domain point mutation found in achondroplasia
additional information
mutation that results in the substitution of an unpaired cysteine residue in the extracellular domain of FGFR3 in thanatophoric dysplasia type I
additional information
FGFR3 transmembrane domain mutation, Ala391Glu, in three unrelated families with Crouzon syndrome and acanthosis nigricans, a specific skin disorder of hyperkeratosis and hyperpigmentation
additional information
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FGFR3 transmembrane domain mutation, Ala391Glu, in three unrelated families with Crouzon syndrome and acanthosis nigricans, a specific skin disorder of hyperkeratosis and hyperpigmentation
additional information
mutations in the gene encoding fibroblast growth factor receptor-3 in achondroplasia
additional information
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mutations in the gene encoding fibroblast growth factor receptor-3 in achondroplasia
additional information
thanatophoric dwarfism (TD) is a sporadic lethal skeletal dysplasia with micromelic shortening of the limbs, macrocephaly, platyspondyly and reduced thoracic cavity. Identification of FGFR3 mutations in 25 of 26 thanatophoric dwarfism cases. Two novel missense mutations, Y373C and G370C, are detected in 8/26 and 1/26 thanatophoric dwarfism 1 cases respectively. Both mutations create cysteine residues in the juxta extramembrane domain of the receptor. Sixteen cases carry the previously reported R248C mutation - 9/26 cases, S249C - 2/26 cases, or stop codon FGFR3 mutations, 5/26 cases
additional information
a recurrent mutation in the tyrosine kinase domain of fibroblast growth factor receptor 3 causes hypochondroplasia. This mutation causes a C to A transversion at nucleotide 1620, resulting in an Asn540Lys substitution in the proximal tyrosine kinase domain
additional information
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a recurrent mutation in the tyrosine kinase domain of fibroblast growth factor receptor 3 causes hypochondroplasia. This mutation causes a C to A transversion at nucleotide 1620, resulting in an Asn540Lys substitution in the proximal tyrosine kinase domain
additional information
Gly375Cys substitution in the transmembrane domain of the fibroblast growth factor receptor-3 in a newborn with achondroplasia
additional information
G370C mutation in the FGFR3 gene in a Japanese patient with thanatophoric dysplasia
additional information
mutation of the gene encoding the ROR2 tyrosine kinase causes autosomal recessive Robinow syndrome
additional information
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mutation of the gene encoding the ROR2 tyrosine kinase causes autosomal recessive Robinow syndrome
additional information
dominant mutations in ROR2, encoding an orphan receptor tyrosine kinase, cause brachydactyly type B
additional information
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dominant mutations in ROR2, encoding an orphan receptor tyrosine kinase, cause brachydactyly type B
additional information
R849W or the Y897S: the receptors containing either mutation show ligand-independent hyperphosphorylation, resulting in dominantly inherited venous malformations
additional information
fetal and adult human CNS, in human leukemia, lymphoma cell lines, and a variety of human cancers derived from neuroectoderm express a truncated Ror1 receptor tyrosine kinase, lacking both extracellular and transmembrane domains
additional information
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fetal and adult human CNS, in human leukemia, lymphoma cell lines, and a variety of human cancers derived from neuroectoderm express a truncated Ror1 receptor tyrosine kinase, lacking both extracellular and transmembrane domains
additional information
recessive Robinow syndrome, allelic to dominant brachydactyly type B, is caused by loss of ROR2 activity. The identification of mutations in three distinct domains containing Frizzled-like, kringle and tyrosine kinase motifs indicates that these are all essential for ROR2 function
additional information
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recessive Robinow syndrome, allelic to dominant brachydactyly type B, is caused by loss of ROR2 activity. The identification of mutations in three distinct domains containing Frizzled-like, kringle and tyrosine kinase motifs indicates that these are all essential for ROR2 function
additional information
distinct mutations in the receptor tyrosine kinase gene ROR2 cause brachydactyly type B
additional information
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distinct mutations in the receptor tyrosine kinase gene ROR2 cause brachydactyly type B
additional information
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construction of FLT-3 with a tandem repeat of the juxtamembrane, termed FLT-3 ITD RTK, showing impaired maturation during recombinant expression in MV4-11 cells, the mutation alters enzyme interactions with other proteins, e.g. heat shock proteins, overview
additional information
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gain-of-function mutations of Kit receptor are associated with several neoplasms including acute myelogenous leukemia, gastrointestinal stromal tumors, and mastocytomas
additional information
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gain-of-function mutations of Kit receptor are associated with several neoplasms including acute myelogenous leukemia, gastrointestinal stromal tumors, mastocytomas, and nasal T-cell lymphomas, mutations and associated tumor types, overview
additional information
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null mutations of any of the ErbB family enzymes result in embryonic lethality
additional information
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a mutant FLT3 receptor protein with an internal tandem duplication (FLT3-ITD) accumulates in a perinuclear region and is not detectable at the plasma membrane. Mutant accumulation can neither be detected in the endoplasmic reticulum nor in the Golgi apparatus. The mutant protein resides most probably in an unidentified compartment of the secretory pathway between the endoplasmic reticulum and the Golgi apparatus. FLT3 mutant receptor protein is constitutively phosphorylated and therefore activated. FLT3 wild-type receptor protein expression level is higher than the expression level of the mutant FLT3 receptor protein
additional information
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c-Kit mutants harboring extracellular domain mutations are not constitutively active, whereas extracellular domain mutants of c-FMS are constitutively active and oncogenic. Extracellular domain mutation of FGFR disturbs the autoinhibitory mechanism, resulting in constitutive acitvation
additional information
DDR1 mutants lacking the stalk region fail to form dimers, whereas deletion of the discoidin domain does not prevent dimerization
additional information
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DDR1 mutants lacking the stalk region fail to form dimers, whereas deletion of the discoidin domain does not prevent dimerization
additional information
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FLT3 mutations affect more females than males (80% vs 20%) whereas KIT mutations have no significant effect on the gender distribution. KIT mutations are commonly found in patients aged between 41-60 years whereas FLT3 mutations are frequently found in patients aged between 21-40. Most mutant KIT cases belong to acute myeloid leukemia-M2 subtype (63.6%) whereas most mutant FLT3 cases belong to acute myeloid leukemiaL-M3 subtype (60%). KIT-mutated patients and demonstrate a high expression of myeloid antigens and CD56 lymphoid antigen. FLT3 mutation is coexistent with PML-RARalpha with markedly low or no CD11c and HLA-DR expression
additional information
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mutant insulin receptor, has increased binding to insulin in an acidic endosomal environment in a patient with severe insulin resistant diabetes. Receptor mutant is degraded rather than recycled to the plasma membrane
additional information
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mutating either Y1353, Y1360, or the kinase domain ablates the ability of Ron to repress HIV-1 transcription
additional information
mutation of all motifs abolishes binding of Sp1 and Sp3
additional information
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mutation of all motifs abolishes binding of Sp1 and Sp3
additional information
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mutations in RTK genes are uncommon in anaplastic thyroid cancer, but there are genomic copy number gains in many RTK genes with relatively high prevalences in these thyroid cancers. The prevalences of these copy gains are generally higher in anaplastic thyroid cancer than follicular thyroid cancer
additional information
no major genomic aberrations (mutations or truncation) of ROR1
additional information
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no major genomic aberrations (mutations or truncation) of ROR1
additional information
TrkA mutants defective in association sites for intracellular effector molecules in normal neuronal cells
additional information
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TrkA mutants defective in association sites for intracellular effector molecules in normal neuronal cells
additional information
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FokI vitamin D receptor gene polymorphisms affect bone mass indices
additional information
expression of the isolated transmembrane domain in HEK 293 and B104-1-1 cells and localization to the cell membrane. The transmembrane domains are able to dimerize, and mutation A391E increases the cross-linking propensities of the two domains
additional information
-
-
additional information
mutations at the W locus affect various aspects of hematopoiesis, the proliferation and migration of primordial germ cells and melanoblasts during development. The original W mutation and W37 are severe lethal mutations when homozygous. In the heterozygous state the W mutation has a weak phenotype while W37 has dominant characteristics. Wv and W41 are weak W mutations with dominant characteristics. W37, Wv and W41 are the result of missense mutations in the kinase domain of the c-kit coding sequence, E582K in W37, T660M in Wv, V831M in W41, which affect the c-kit associated tyrosine kinase to varying degrees
additional information
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mutations at the W locus affect various aspects of hematopoiesis, the proliferation and migration of primordial germ cells and melanoblasts during development. The original W mutation and W37 are severe lethal mutations when homozygous. In the heterozygous state the W mutation has a weak phenotype while W37 has dominant characteristics. Wv and W41 are weak W mutations with dominant characteristics. W37, Wv and W41 are the result of missense mutations in the kinase domain of the c-kit coding sequence, E582K in W37, T660M in Wv, V831M in W41, which affect the c-kit associated tyrosine kinase to varying degrees
additional information
the W42 mutation has a particularly severe effect in both the homozygous and the heterozygous states. The c-kit protein products in homozygous mutant mast cells are expressed normally but display a defective tyrosine kinase activity in vitro. Missense mutation D790N in the c-kit protein product, D790 is a conserved residue in all protein kinases
additional information
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the W42 mutation has a particularly severe effect in both the homozygous and the heterozygous states. The c-kit protein products in homozygous mutant mast cells are expressed normally but display a defective tyrosine kinase activity in vitro. Missense mutation D790N in the c-kit protein product, D790 is a conserved residue in all protein kinases
additional information
the mouse waved-2 phenotype results from a point mutation in the EGF receptor tyrosine kinase
additional information
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the mouse waved-2 phenotype results from a point mutation in the EGF receptor tyrosine kinase
additional information
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differences in Wnt5a-induced wound closure and microtubule-organizing center reorientation are not detectable in immortalized mouse embryonic fibroblasts from wild-type and Ror2-/- embryos
additional information
EphA2 deficiency impairs tumor progression in MMTV-Neu mice, but not MMTV-PyV-mT, transgenic models of mammary epithelial adenocarcinoma
additional information
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EphA2 deficiency impairs tumor progression in MMTV-Neu mice, but not MMTV-PyV-mT, transgenic models of mammary epithelial adenocarcinoma
additional information
mice with a targeted deletion of the Ron tyrosine kinase signaling domain (TK-/-), show a significant decrease in survival time after bacterial infection compared with controls, which is associated with a significant increase in bacterial colony-forming units in the blood and several end-organs. The increased bacterial load is associated with increased liver necrosis and serum alanine aminotransferase levels. Neutrophils from TK-/- mice exhibit decreased spontaneous oxidative burst capacity ex vivo, and a reduced level of neutrophil migration to and translocation within the liver. Loss of Ron signaling results in significantly reduced production of serum monocyte chemoattractant protein-1 and interleukin-6 levels following cecal ligation and puncture, and peritoneal macrophage isolated from TK-/- mice exhibit blunted production of monocyte chemoattractant protein-1, interleukin-6, and macrophage inflammatory protein-2 following stimulation with endotoxin ex vivo
additional information
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mice with a targeted deletion of the Ron tyrosine kinase signaling domain (TK-/-), show a significant decrease in survival time after bacterial infection compared with controls, which is associated with a significant increase in bacterial colony-forming units in the blood and several end-organs. The increased bacterial load is associated with increased liver necrosis and serum alanine aminotransferase levels. Neutrophils from TK-/- mice exhibit decreased spontaneous oxidative burst capacity ex vivo, and a reduced level of neutrophil migration to and translocation within the liver. Loss of Ron signaling results in significantly reduced production of serum monocyte chemoattractant protein-1 and interleukin-6 levels following cecal ligation and puncture, and peritoneal macrophage isolated from TK-/- mice exhibit blunted production of monocyte chemoattractant protein-1, interleukin-6, and macrophage inflammatory protein-2 following stimulation with endotoxin ex vivo
additional information
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mouse model with total loss of Ron protein, mice are lethal at an early stage of embryo development, mice hemizygous for the deletion of Ron are viable and fertile, but display an enhanced response to inflammation, are more susceptible to endotoxic shock and display an impaired ability to regulate nitric oxide. Mouse model in which the extracellular and transmembrane domains of Ron are preserved, along with eight amino acids of the intracellular domain, while ablation of the cytoplasmic domain results in complete loss of Ron intracellular signaling, homozygous mice with this germline deletion are viable, fertile and display no gross phenotypic abnormalities, but show an enhanced response to both acute and cell-mediated inflammatory stimuli. Mutant with insertion of beta-galactosidase gene into exon 1 of the mouse Ron gene, so that transcription of the reporter arises from the endogenous reporter and translates from its own start site. Homozygous mice with this mutation are viable and phenotypic normal, but show ablation of activity of Ron
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only MuSK deletion mutants containing the intact kinase domain can bind to N-ethylmaleimide sensitive factor. Deletion of the C terminus (13 amino acids) has no effect on MuSK binding to N-ethylmaleimide sensitive factor. Deletion of the middle 30 amino acids in the juxtamembrane, including Y556, a tyrosine implicated in agrin signaling, has no apparent effect on binding to N-ethylmaleimide sensitive factor. Deletion of any 30 amino acids in the kinase domain or in the region linking the juxtamembrane and kinase domains abolishes the binding activity, with the exception of one deletion mutant, DELTA739-768
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RON(-/-) mice harbor significantly increased systemic levels of IFN-gamma and IL-12p70 and increased levels of IL-12p40 transcript in their spleen. Enhanced susceptibility of RON(-/-) mice to endotoxin challenge is dependent on IFN-gamma-mediated signals
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inhibition of vascular smooth muscle cell growth through antisense transcription of a rat insulin-like growth factor I receptor cDNA
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mutation of the receptor tyrosine kinase gene Mertk in the retinal dystrophic RCS rat
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expression of the isolated transmembrane domain in HEK 293 and B104-1-1 cells and localization to the cell membrane. The transmembrane domains are able to dimerize, and mutation V664E increases the cross-linking propensities of the two domains. The transmembrane domain of mutant V664E specifically inhibits the phosphorylation of full-length mutant V664E, while the wild-type transmembrane domain does not. Mutant V664E transmembrane domain does not affect the phosphorylation levels of human full-length tyrosine kinase receptor FGFR3 mutant A391E
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