Information on EC 2.7.10.1 - receptor protein-tyrosine kinase and Organism(s) Homo sapiens and UniProt Accession P29323

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EC Tree 2 Transferases 2.7 Transferring phosphorus-containing groups 2.7.10 Protein-tyrosine kinases 2.7.10.1 receptor protein-tyrosine kinase

The receptor protein-tyrosine kinases, which can be defined as having a transmembrane domain, are a large and diverse multigene family found only in Metazoans . In the human genome, 58 receptor-type protein-tyrosine kinases have been identified and these are distributed into 20 subfamilies.

The taxonomic range for the selected organisms is: Homo sapiens
The enzyme appears in selected viruses and cellular organisms

Reaction Schemes

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+

a [protein]-L-tyrosine

=

+

a [protein]-L-tyrosine phosphate

+

=

+

Synonyms
tyrosine kinase, epidermal growth factor receptor, insulin receptor, c-kit, erlotinib, c-met, erbb2, egf receptor, receptor tyrosine kinase, her-2, more

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Go to Synonym Search

ephrin type-B receptor 2

-

490367, 490369, 490370, 490371, 490372, 490373

A-type platelet-derived growth factor receptor

-

490268, 490269, 490270

Adhesion-related kinase

-

-

-

-

ALK

-

-

ALK tyrosine kinase receptor

-

alpha platelet-derived growth factor receptor

-

Anaplastic lymphoma kinase

show

angiopoietin 1 receptor

-

490533, 490534, 490535

Axl

show

AXL kinase

-

AXL oncogene

-

-

-

-

basic fibroblast growth factor receptor 1

-

490167, 490218, 490219, 490220, 490221, 490222, 490223, 490225, 490226, 490227, 490228, 490229, 490230, 490231

basic-FGF receptor

-

BDNF/NT-3 growth factors receptor

-

490601, 490602, 490603, 490604

beta platelet-derived growth factor receptor

-

490194, 490195, 490196, 490197, 490198

Brain-specific kinase

-

-

-

-

Breathless protein

-

-

-

-

Brt

-

-

c-erbB3

-

-

-

-

c-fgr

-

-

-

-

c-fms

show

c-kit

show

c-Kit receptor protein-tyrosine kinase

-

c-Kit receptor tyrosine kinase

-

-

c-Kit RTK

-

-

c-Kit tyrosine kinase

-

-

-

-

c-kitR tyrosine kinase

-

C-mer

show

c-met

show

c-Met receptor tyrosine kinase

show

c-Met RTK

-

-

C-ret

-

-

-

-

C-SRC

-

-

C14

-

-

-

-

Cadherin 96Ca

-

-

-

-

CD115 antigen

-

-

-

-

CD117

-

-

CD117 antigen

-

-

-

-

CD135 antigen

-

-

-

-

CD136 antigen

-

-

-

-

CD140a antigen

-

-

-

-

CD140b antigen

-

-

-

-

CD167a antigen

-

-

-

-

CD202b antigen

-

-

-

-

CD220 antigen

-

-

-

-

CD221 antigen

-

-

-

-

CD246 antigen

-

-

-

-

CDW136

-

-

-

-

CEK4

-

-

-

-

Cell adhesion kinase

-

-

-

-

cKit

-

-

CLD1

-

-

CLD2

-

-

colony-stimulating factor-1 receptor

-

-

CSF-1 receptor

-

also known as c-fms and CD115

CSF-1R

-

-

DDR1

-

Derailed protein

-

-

-

-

DFGF-R1

-

-

-

-

discoidin domain receptor 1

-

discoidin domain receptor 2

-

discoidin domain receptor tyrosine kinase 1

-

Discoidin receptor tyrosine kinase

show

Doughnut protein

-

-

-

-

Dror

-

-

-

-

Drosophila relative of ERBB

-

-

-

-

DRT

-

-

-

-

DTK

-

-

DTK receptor tyrosine kinase

-

EBK

-

-

-

-

EGF receptor

show

EGF receptor protein-tyrosine kinase

-

-

EGF receptor tyrosine kinase

show

EGF RTK

-

EGF TK

-

-

EGF-R

-

-

Egfr

show

EGFR kinase

-

-

662556, 691714, 694546

EGFR protein tyrosine kinase

-

-

EGFr TK

-

-

-

-

EGFR tyrosine kinase

show

EGFR-TK

show

Egg laying defective protein 15

-

-

-

-

ELK

-

-

-

-

Embryonic brain kinase

-

-

-

-

embryonic receptor kinase

-

EmRK2

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Endothelial kinase receptor EK1

-

-

-

-

Eph receptor tyrosine kinase

-

EPH-and ELK-related kinase

-

-

-

-

EphA1

show

EphA1 receptor

-

-

EPHA1 receptor tyrosine kinase

-

EphA2

show

EPHA4

-

EphB3

-

ephrin type-A receptor 1

-

ephrin type-A receptor 2

-

ephrin type-A receptor 3

-

ephrin type-A receptor 4

-

ephrin type-A receptor 5

-

ephrin type-A receptor 7

-

ephrin type-A receptor 8

-

ephrin type-B receptor 1

-

ephrin type-B receptor 3

-

ephrin type-B receptor 4

-

ephrine receptor

-

-

epidermal growth factor receptor

show

epidermal growth factor receptor 2

-

-

epidermal growth factor receptor 4

-

490597, 490598, 490599

epidermal growth factor receptor kinase

-

-

epidermal growth factor receptor tyrosine kinase

show

epidermal growth factor receptor tyrosine kinase inhibitor

-

-

Epidermal growth factor receptor-related protein

-

-

-

-

epidermal growth factor type II receptor

-

-

epidermal growth factor-receptor

-

-

epidermal growth-factor receptor tyrosine kinase

-

-

Epithelial cell kinase

show

epithelial discoidin domain receptor 1

-

490201, 490547, 490580, 490581, 490582, 490583, 490584

erb-B1

-

ErbB receptor protein-tyrosine kinase

-

-

erbB tyrosine kinase

-

-

-

-

ErbB-1

-

ErbB-2

-

ErbB-4 receptor

-

ErbB-4 tyrosine kinase

-

-

ERBB1

show

ErbB1 tyrosine kinase

-

-

ErbB2

-

-

672173, 673212, 737992

ErbB2 kinase

-

-

-

-

erbB2 receptor tyrosine kinase

show

ErbB2 tyrosine kinase

-

-

ErbB4

-

-

ErbB4 receptor

-

-

ERK

-

-

-

-

erlotinib

-

-

erythropoietin-producing hepatocellular receptor tyrosine kinase subtype A2

-

-

erythropoietin-producing human hepatocellular carcinoma B3

-

ETK

-

-

-

-

FGF receptor

-

FGF receptor tyrosine kinase

-

-

FGFR

-

-

660727, 661669, 662236

FGFR-4

-

FGFR1

-

-

672173, 693727, 739206

FGFR1K

-

FGFR2

show

FGFR3

show

FGFR4

-

-

fibroblast growth factor receptor

-

-

660727, 661669, 662236, 691636, 693727, 739206

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 3

-

490320, 490323, 490324, 490325, 490326, 490327, 490328, 490329, 490330, 490331, 490332, 490333, 490335, 490336, 490337, 490338, 490339, 721711

fibroblast growth factor receptor 4

-

490319, 490320, 490321, 490322

fibroblast growth factor receptor BFR-2

-

FL cytokine receptor

-

490120, 490122, 490412, 490413, 490414, 490415, 490416, 490417, 490418

Flk-1

-

-

Flt-1

-

-

FLT-3

-

-

FLT3

show

FLT3 kinase

-

FLT3 receptor protein

-

-

FLT4

-

FLT4 receptor tyrosine kinase

-

Fms proto-oncogene

-

-

-

-

fms-like tyrosine kinase 3

-

-

GCTK

-

-

-

-

GHR

-

-

GP145-TrkB

-

-

-

-

GP145-TrkB/GP95-TrkB

-

-

-

-

GP145-TrkC

-

-

-

-

growth hormone receptor

-

-

Gurken receptor

-

-

-

-

Heartless protein

-

-

-

-

HEK

show

HEK 2

-

HEK3

-

-

-

-

HEK4

-

-

-

-

HEK6

-

-

-

-

Heparin-binding growth factor receptor

-

-

-

-

hepatocyte growth factor receptor

show

HER receptor protein-tyrosine kinase

-

-

HER-1

-

Her-2

-

Her1 tyrosine kinase

-

-

HER2

show

HER2neu

-

-

HER3

-

HER3/ERRB3

-

HER4

-

-

HGF receptor

-

-

-

-

HGF-SF receptor

-

-

-

-

high affinity nerve growth factor receptor

-

HTK

-

human epidermal growth factor receptor2

-

-

hydroxyaryl-protein kinase

-

-

-

-

HYK

-

-

-

-

IGF-1 receptor

-

-

IGF-1R

show

IGF-IR

-

-

IGFR tyrosine kinase

-

-

ILP receptor

-

-

-

-

insulin receptor

show

insulin receptor kinase

-

-

660729, 661030, 661206

insulin receptor protein tyrosine kinase

-

-

insulin receptor protein-tyrosine kinase

-

-

-

-

insulin receptor tyrosine kinase

-

-

insulin receptor-beta subunit

-

-

insulin receptor-related protein

-

insulin-growth factor-1 receptor

-

-

insulin-like growth factor 1 receptor

-

insulin-like growth factor I receptor

-

490147, 490148, 490149, 490150

insulin-like growth factor receptor

-

-

insulin-like growth factor type I receptor

-

-

Insulin-like growth factor-1 receptor

-

-

Insulin-like Growth Factor-1 receptor tyrosine kinase

-

-

IR kinase

-

-

iR-beta subunit

-

-

IR-PTK

-

-

IR-related receptor

-

-

-

-

IRK

show

IRR

show

KDR

-

691276, 693538, 693539, 693545

KDR/fetal liver kinase-1

-

-

KDR/Flk-1

-

-

Keratinocyte growth factor receptor

show

KGF receptor

-

-

KGFR

-

-

Kinase insert domain receptor

-

-

-

-

Kinase NYK

-

-

-

-

Kinase VIK

-

-

-

-

KIT

-

-

660921, 672784, 692230, 693346, 705866

KIT kinase

-

Kit protein-tyrosine kinase

-

-

KIT receptor tyrosine kinase

-

-

leukocyte tyrosine kinase receptor

-

490374, 490375, 490376

Linotte protein

-

-

-

-

M-CSF receptor

-

-

macrophage colony stimulating factor I receptor

-

490139, 490140, 490141, 490142, 490143

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

-

490139, 490207, 490208, 490209, 490210, 490211, 490212, 490213, 490214, 490215

MEK4

-

-

-

-

Mer

-

-

MER kinase

-

MET

show

MET kinase

-

Met proto-oncogene tyrosine kinase

-

-

-

-

Met receptor-tyrosine kinase

-

-

Met RTK

-

-

Met-related kinase

-

-

-

-

Met/hepatocyte growth factor receptor tyrosine kinase

-

MFR

-

-

-

-

MIR

-

-

-

-

MLN 19

-

-

-

-

mROR1

-

-

-

-

mROR2

-

-

-

-

MSP receptor

-

-

-

-

MST1R

-

-

muscle-specific receptor tyrosine kinase

-

-

muscle-specific receptor-tyrosine kinase

-

-

MuSK

-

-

nerve growth factor receptor

-

-

NET

show

NEU proto-oncogene

-

-

-

-

neuregulin receptor ErbB-4

-

Neurospecific receptor tyrosine kinase

-

-

-

-

neurotrophin tyrosine receptor kinase

-

-

non-receptor protein tyrosine kinase

-

-

NRTK

-

-

-

-

NT-3 growth factor receptor

-

NUK

-

-

-

-

orphan receptor tyrosine kinase

-

-

P140 TEK

-

-

-

-

p140-TrkA

-

-

-

-

p145c-kit

-

p180erbB4

-

-

-

-

p185-Ron

-

-

-

-

p185erbB2

-

-

-

-

p190MET kinase

-

p75 neurotrophin receptor

-

-

p75NTR

-

-

Pagliaccio

-

-

-

-

PDGF beta-receptor

-

PDGF receptor

-

-

PDGF receptor tyrosine kinase

-

-

PDGF-alpha receptor

-

-

PDGF-beta receptor

-

-

PDGF-R-alpha

-

-

-

-

PDGF-R-beta

-

-

-

-

PDGFR

-

-

PDGFR kinase

-

-

-

-

PDGFR-alpha

show

PDGFR-beta

show

PDGFRalpha

-

-

691636, 693346, 703031

PDGFRB

-

PDGFRbeta

show

platelet derived growth factor receptor-beta

-

platelet-derived growth factor receptor

-

-

660727, 662679, 691636, 693727, 694119, 705866

platelet-derived growth factor receptor alpha

show

platelet-derived growth factor receptor-beta

-

-

proline-rich tyrosinekinase

-

-

protein kinase eck

-

protein receptor tyrosine kinase RTK 6

-

Protein-tyrosine kinase byk

-

-

-

-

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

-

490174, 490175, 490176

Pyk-2

-

-

recepteur d'origine nantais

show

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

-

490102, 490103, 490104, 490105

receptor protein-tyrosine kinase erbB-3

-

490315, 490316, 490317

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

show

receptor tyrosine kinase c-Kit

-

receptor tyrosine kinase EphA1

-

-

receptor tyrosine kinase EphA2

-

Receptor tyrosine kinase MerTK

-

-

-

-

receptor tyrosine kinase RET

-

-

receptor tyrosine kinase RON

-

-

receptor tyrosine kinase ROR1

-

receptor tyrosine kinase Ror2

-

receptor tyrosine kinase Sky

-

receptor tyrosine kinase vascular endothelial growth factor receptor-2

-

-

Receptor-activated Janus kinase

-

-

-

-

receptor-like protein-tyrosine kinase TK14

-

receptor-type tyrosine kinase termed Rse

-

receptor-type tyrosine-protein kinase FLT3

-

RET

show

RET kinase

-

Ret receptor tyrosine kinase

-

-

Ret51

-

-

Ret9

-

-

Ron

show

RON receptor tyrosine kinase

show

Ron tyrosine kinase receptor

-

ROR1

-

RPTK

-

-

Rse

-

-

RTK

show

RTKs

-

-

SCFR

-

-

-

-

sFlt-1

-

-

Sky

-

-

Slow nerve growth factor receptor

-

-

-

-

soluble fms-like tyrosine kinase 1

-

-

Srcasm

-

stem cell factor receptor

-

-

stem cell receptor

-

-

stem cell tyrosine kinase 1

-

Stem cell-derived tyrosine kinase

show

STK

-

-

STK-1

-

subclass III receptor tyrosine kinase

-

-

TAM receptor

-

-

Tie1

show

Tie2

-

490533, 490534, 694051

Tif

-

-

Torpedo protein

-

-

-

-

TRK1 transforming tyrosine kinase protein

-

-

-

-

TrkA

show

trkB

show

TrkB tyrosine kinase

-

-

-

-

TrkC

show

TrkC tyrosine kinase

-

-

-

-

Tunica interna endothelial cell kinase

-

-

-

-

Tyro 3

-

-

TYRO3

-

TYRO3 kinase

-

Tyrosine kinase CEK6 receptor

-

-

-

-

Tyrosine kinase DDR

-

-

-

-

tyrosine kinase p59fyn

-

Tyrosine kinase receptor HD-14

-

-

-

-

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 DTK

-

-

-

-

Tyrosine-protein kinase FLT3

-

-

-

-

Tyrosine-protein kinase FRT

-

-

-

-

Tyrosine-protein kinase receptor CEK10

-

-

-

-

Tyrosine-protein kinase receptor CEK11

-

-

-

-

Tyrosine-protein kinase receptor CEK5

-

-

-

-

Tyrosine-protein kinase receptor CEK7

-

-

-

-

Tyrosine-protein kinase receptor CEK8

-

-

-

-

Tyrosine-protein kinase receptor CEPHA7

-

-

-

-

Tyrosine-protein kinase receptor ECK

-

-

-

-

Tyrosine-protein kinase receptor EEK

-

-

-

-

Tyrosine-protein kinase receptor EPH

-

-

-

-

Tyrosine-protein kinase receptor ESK

-

-

-

-

Tyrosine-protein kinase receptor ETK1

-

-

-

-

Tyrosine-protein kinase receptor FLT

-

-

-

-

Tyrosine-protein kinase receptor FLT3

-

-

-

-

Tyrosine-protein kinase receptor FLT4

-

-

-

-

Tyrosine-protein kinase receptor HTK

-

-

-

-

Tyrosine-protein kinase receptor PAG

-

-

-

-

Tyrosine-protein kinase receptor QEK5

-

-

-

-

Tyrosine-protein kinase receptor REK4

-

-

-

-

Tyrosine-protein kinase receptor SEK

-

-

-

-

Tyrosine-protein kinase receptor TCK

-

-

-

-

Tyrosine-protein kinase receptor TEK

-

-

-

-

tyrosine-protein kinase receptor Tie-1

-

tyrosine-protein kinase receptor TYRO3

-

490502, 490567, 490568, 490569, 490570

tyrosine-protein kinase receptor UFO

-

490149, 490379, 490380

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

-

490387, 490388, 490389

Tyrosine-protein kinase SKY

-

-

-

-

tyrosine-protein kinase transmembrane receptor ROR1

-

tyrosine-protein kinase transmembrane receptor ROR2

-

490527, 490529, 490530, 490531, 490532

vascular endothelial growth factor

-

-

vascular endothelial growth factor 2

-

-

vascular endothelial growth factor receptor

show

vascular endothelial growth factor receptor 1

-

vascular endothelial growth factor receptor 2

show

vascular endothelial growth factor receptor 3

-

490394, 490395, 490396

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

-

-

-

-

VDR

-

-

VEGF factor receptor tyrosine kinase

-

-

VEGF receptor

-

VEGF receptor tyrosine kinase

-

-

VEGF receptor-1

-

VEGFR

-

-

VEGFR tyrosine kinase

-

-

VEGFR-1

-

-

VEGFR-1 tyrosine kinase

-

-

VEGFR-2

show

VEGFR-2 tyrosine kinase

-

VEGFR-3

-

-

VEGFR1

show

VEGFR1-3

-

-

VEGFR2

show

VEGFR2 kinase

-

VEGFR2/kinase domain region

-

-

VEGFR3

-

isoform

vitamin D receptor

-

-

additional information

show

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Go to Reaction Search

ATP + a [protein]-L-tyrosine = ADP + a [protein]-L-tyrosine phosphate

show the reaction diagram

active site structure, activation mechanism

-

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Go to Reaction Type Search

phospho group transfer

-

-

-

-

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Go to Systematic Name Search

ATP:[protein]-L-tyrosine O-phosphotransferase (receptor-type)

The receptor protein-tyrosine kinases, which can be defined as having a transmembrane domain, are a large and diverse multigene family found only in Metazoans [1]. In the human genome, 58 receptor-type protein-tyrosine kinases have been identified and these are distributed into 20 subfamilies.

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Go to Substrate/Product Search

ATP + a [macrophage-stimulating protein]-L-tyrosine

ADP + a [macrophage-stimulating protein]-L-tyrosine phosphate

show the reaction diagram

Substrates: -
Products: -

?

ATP + a [protein]-L-tyrosine

ADP + a [protein]-L-tyrosine phosphate

show the reaction diagram

show

ATP + Ac-DYFE-6-chloro-W-NHMe

ADP + Ac-DYpFE-6-chloro-W-NHMe

show the reaction diagram

Substrates: substrate identified by substrate-activity-screening methodology based on optimization of substrate YFEW in a modular manner
Products: -

?

ATP + Ac-DYFGW-NHMe

ADP + Ac-DYpFGW-NHMe

show the reaction diagram

Substrates: substrate identified by substrate-activity-screening methodology based on optimization of substrate YFEW in a modular manner
Products: -

?

ATP + G protein-coupled receptor kinase-2

ADP + phosphorylated G protein-coupled receptor kinase-2

show the reaction diagram

show

ATP + insulin receptor substrate 1-L-tyrosine

ADP + insulin receptor substrate 1-L-tyrosine phosphate

show the reaction diagram

-

Substrates: peptide derived from the regulatory domain of insulin receptor
Products: -

?

ATP + KKHTDDGYMPMSPGVA

ADP + KKHTDDGY-phosphate-MPMSPGVA

show the reaction diagram

-

Substrates: commercial peptide substrate
Products: -

?

ATP + KKSRGDYMTMQIG

ADP + KKSRGDY-phosphate-MTMQIG

show the reaction diagram

-

Substrates: commercial peptide substrate
Products: -

?

ATP + NAEYLRV

ADP + NAE-phospho-Y-LRV

show the reaction diagram

Substrates: -
Products: -

?

ATP + phosphatidylinositol 3-kinase

ADP + phosphorylated phosphatidylinositol 3-kinase

show the reaction diagram

Substrates: 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
Products: -

?

ATP + phosphoinositide-dependent kinase-1-L-tyrosine

ADP + phosphoinositide-dependent kinase-1-L-tyrosine phosphate

show the reaction diagram

-

Substrates: insulin-like growth factor-1 receptor directly interacts with and activates phosphoinositide-dependent kinase-1
Products: -

?

ATP + phospholipase C gamma

ADP + phosphorylated phospholipase C gamma

show the reaction diagram

show

ATP + poly(Glu-Ala-Tyr)

ADP + poly(Glu-Ala-Tyr)-L-tyrosine phosphate

show the reaction diagram

-

Substrates: -
Products: -

?

ATP + poly(Glu:Tyr)

ADP + poly(Glu:Tyr) phosphate

show the reaction diagram

-

Substrates: -
Products: -

?

ATP + poly-Ala-Glu-Lys-Tyr

ADP * poly-Ala-L-Glu-L-Lys-L-tyrosine phosphate

show the reaction diagram

-

Substrates: substrate used for c-Met
Products: -

?

ATP + poly-Glu-Tyr

ADP + poly-L-Glu-L-tyrosine phosphate

show the reaction diagram

-

Substrates: substrate used for EGFR
Products: -

?

ATP + protein tyrosine

ADP + protein tyrosine phosphate

show the reaction diagram

show

ATP + VPEYINQ

ADP + VPE-phosphoY-INQ

show the reaction diagram

Substrates: -
Products: -

?

ATP + YFEW

ADP + YpFEW

show the reaction diagram

Substrates: tetrapeptide identified by substrate profiling
Products: -

?

ATP + [beta-catenin]-Tyr142

ADP + [beta-catenin]-Tyr142 phosphate

show the reaction diagram

-

Substrates: 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
Products: -

?

ATP + [endothelial growth-factor]-L-tyrosine

ADP + [endothelial growth-factor]-L-tyrosine phosphate

show the reaction diagram

-

Substrates: EGFR tyrosine kinase
Products: -

?

ATP + [gastrin]-L-tyrosine

ADP + [gastrin]-L-tyrosine phosphate

show the reaction diagram

-

Substrates: -
Products: -

?

ATP + [minigastrin]-L-tyrosine

ADP + [minigastrin]-L-tyrosine phosphate

show the reaction diagram

-

Substrates: -
Products: -

?

ATP + [poly-(Glu,Tyr)1:4]

ADP + [poly-(Glu,Tyr)1:4]-tyrosine phosphate

show the reaction diagram

-

Substrates: synthetic substrate
Products: -

?

ATP + [vascular endothelial growth-factor-1]-L-tyrosine

ADP + [vascular endothelial growth-factor-1]-L-tyrosine phosphate

show the reaction diagram

-

Substrates: VEGFR-1 tyrosine kinase
Products: -

?

poly(Glu:Tyr) + ATP

ADP + poly(Glu:Tyr) phosphate

show the reaction diagram

-

Substrates: -
Products: -

?

additional information

?

-

show

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Go to Natural Substrate Search

ATP + a [macrophage-stimulating protein]-L-tyrosine

ADP + a [macrophage-stimulating protein]-L-tyrosine phosphate

show the reaction diagram

Substrates: -
Products: -

?

ATP + a [protein]-L-tyrosine

ADP + a [protein]-L-tyrosine phosphate

show the reaction diagram

show

ATP + G protein-coupled receptor kinase-2

ADP + phosphorylated G protein-coupled receptor kinase-2

show the reaction diagram

-

Substrates: GRK2 activation also increases GRK2 degradation and downregulation, independent of Gbetagamma subunits and phosphoinositide 3-kinase
Products: -

?

ATP + phospholipase C gamma

ADP + phosphorylated phospholipase C gamma

show the reaction diagram

Substrates: growth factor-induced tyrosine phosphorylation of PLC gamma is essential for stimulation of phosphatidylinositol hydrolysis in vitro and in vivo
Products: -

?

ATP + poly(Glu:Tyr)

ADP + poly(Glu:Tyr) phosphate

show the reaction diagram

-

Substrates: -
Products: -

?

ATP + protein tyrosine

ADP + protein tyrosine phosphate

show the reaction diagram

Substrates: autophosphorylated on tyrosine and also mediated tyrosine phosphorylation of casein
Products: -

?

ATP + [beta-catenin]-Tyr142

ADP + [beta-catenin]-Tyr142 phosphate

show the reaction diagram

-

Substrates: 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
Products: -

?

ATP + [endothelial growth-factor]-L-tyrosine

ADP + [endothelial growth-factor]-L-tyrosine phosphate

show the reaction diagram

-

Substrates: EGFR tyrosine kinase
Products: -

?

ATP + [vascular endothelial growth-factor-1]-L-tyrosine

ADP + [vascular endothelial growth-factor-1]-L-tyrosine phosphate

show the reaction diagram

-

Substrates: VEGFR-1 tyrosine kinase
Products: -

?

additional information

?

-

show

back to the top

Go to Cofactor Search

ATP

show

back to the top

Go to Metals and Ions Search

Ca2+

show

Cr3+

-

activates insulin receptor tyrosine phosphorylation in vivo

hydrogen peroxide

-

insulin-induced ROS production, limited exposure enhances insulin-induced autophosphorylation of the insulin receptor, while prolonged exposure impairs the action of insulin

Mg2+

show

Mn2+

-

-

661483, 661030, 661163, 661206

Zn2+

-

presence of Zn2+ at 0.1 mM rapidly activates isoform ALK. This activation is dependent of ALK tyrosine kinase activity and dimerization of the receptor but is independent of Src family kinase activity. Addition of sodium pyrithione, a zinc ionophore, leads to a further activation of ALK. This stronger activation is dependent of Src family kinase but independent of ALK activity and dimerization

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Go to Inhibitor Search

(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

show

(2R)-N-(2-hydroxyethyl)-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide

-

-

(2R)-N-(2-hydroxyethyl)-N-methyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide

-

-

(2R)-N-(2-methoxyethyl)-N-methyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide

-

-

(2R)-N-methyl-2-[(4-[[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide

-

(2R)-N-methyl-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide

-

(2S)-2-[(4-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]-N,N-dimethylpropanamide

-

(2S)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N,N-dimethylpropanamide

-

-

(2S)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N-(2-hydroxyethyl)-N-methylpropanamide

-

-

(2S)-N,N-dimethyl-2-[(4-[[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide

-

(2S)-N,N-dimethyl-2-[(4-[[1-(1,3-thiazol-4-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide

-

(2S)-N,N-dimethyl-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide

-

(2S)-N,N-dimethyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide

-

-

(2S)-N-(2-hydroxyethyl)-N-methyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide

-

-

(3Z)-3-[(3,5-dimethyl-1H-pyrrol-2-yl)methylidene]-1,3-dihydro-2H-indol-2-one

-

-

(3Z)-3-[3-([1,4'-bipiperidine]-1'-carbonyl)-2-methyl-1,4,5,6-tetrahydro-7H-indol-7-ylidene]-5-fluoro-1,3-dihydro-2H-indol-2-one

-

-

(3Z)-5-fluoro-3-(2-methyl-3-[(2S)-2-[(pyrrolidin-1-yl)methyl]pyrrolidine-1-carbonyl]-1,4,5,6-tetrahydro-7H-indol-7-ylidene)-1,3-dihydro-2H-indol-2-one

-

-

(3Z)-5-fluoro-3-[2-methyl-3-(morpholine-4-carbonyl)-1,4,5,6-tetrahydro-7H-indol-7-ylidene]-1,3-dihydro-2H-indol-2-one

-

-

(3Z)-5-[(1-ethylpiperidin-4-yl)amino]-3-[(5-methoxy-1H-benzimidazol-2-yl)(phenyl)methylidene]-1,3-dihydro-2H-indol-2-one

-

-

(7Z)-7-(5-bromo-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-N-[2-(diethylamino)ethyl]-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide

-

-

(7Z)-7-(5-chloro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-N-[2-(diethylamino)ethyl]-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide

-

-

(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[2-(morpholin-4-yl)ethyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide

-

-

(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[2-(piperidin-1-yl)ethyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide

-

-

(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[2-(pyridin-2-yl)ethyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide

-

-

(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[2-(pyrrolidin-1-yl)ethyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide

-

-

(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide

-

-

(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-N-[3-(pyrrolidin-1-yl)propyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide

-

-

(7Z)-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-N-(2-hydroxyethyl)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide

-

-

(7Z)-N-[2-(diethylamino)ethyl]-2-methyl-7-(2-oxo-1,2-dihydro-3H-indol-3-ylidene)-4,5,6,7-tetrahydro-1H-indole-3-carboxamide

-

-

(7Z)-N-[2-(diethylamino)ethyl]-2-methyl-7-(5-methyl-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-4,5,6,7-tetrahydro-1H-indole-3-carboxamide

-

-

(7Z)-N-[2-(diethylamino)ethyl]-2-methyl-7-(5-nitro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-4,5,6,7-tetrahydro-1H-indole-3-carboxamide

-

-

(7Z)-N-[2-(diethylamino)ethyl]-7-(4-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide

-

-

(7Z)-N-[2-(diethylamino)ethyl]-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide

-

-

(7Z)-N-[2-(diethylamino)ethyl]-7-(5-methoxy-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide

-

-

(7Z)-N-[2-(diethylamino)ethyl]-7-(5-[[(diethylamino)oxy]sulfinyl]-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide

-

-

(7Z)-N-[2-(diethylamino)ethyl]-7-(7-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide

-

-

(7Z)-N-[2-(dimethylamino)ethyl]-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide

-

-

(7Z)-N-[3-(diethylamino)-2-hydroxypropyl]-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide

-

-

(7Z)-N-[3-(diethylamino)propyl]-7-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide

-

-

(E)-methyl 3-(4-(phenylamino)quinazolin-7-yl)acrylate

-

(Z)-5-[6-[3-(4-methoxyphenyl)-ureido]-2-oxo-1,2-dihydroindol-3-ylidene-methyl]-4-methyl-1H-pyrrole-3-carboxylic acid

potent inhibitor against tyrosine kinases, including VEGFR and PDGFR families, as well as Aurora kinases

1,4-diamino-2,3-dicyano-1,4-bis(2-aminophenylthio)-butadiene

-

-

1-(4-((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

show

1-(4-aminophenyl)-3-[3-(3,4-dihydroxyphenyl)-4-oxo-2,4-dihydroindeno[1,2-c]pyrazol-5-yl]urea

show

1-(4-aminophenyl)-3-[3-(4-hydroxyphenyl)-4-oxo-2,4-dihydroindeno[1,2-c]pyrazol-5-yl]urea

show

1-(4-aminophenyl)-3-[3-(4-methoxyphenyl)-4-oxo-2,4-dihydroindeno[1,2-c]pyrazol-5-yl]urea

show

1-(4-hydroxyphenyl)-3-[3-(4-methoxyphenyl)-4-oxo-2,4-dihydroindeno[1,2-c]pyrazol-5-yl]urea

show

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

P08581, P10721, P30530, P35968, P36888, Q06418, Q12866, P07949

-

1-(cyclopentylmethyl)-3-[6-(4-ethylpiperazin-1-yl)pyridin-3-yl]-N-methyl-1H-pyrazolo[3,4-d]pyrimidin-6-amine

P08581, P10721, P30530, P35968, P36888, Q06418, Q12866, P07949

-

1-(cyclopentylmethyl)-N-methyl-3-[4-(4-methylpiperazin-1-yl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine

P08581, P10721, P30530, P35968, P36888, Q06418, Q12866, P07949

-

1-(cyclopentylmethyl)-N-methyl-3-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine

P08581, P10721, P30530, P35968, P36888, Q06418, Q12866, P07949

-

1-(cyclopentylmethyl)-N-methyl-3-[6-(piperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-amine

P08581, P10721, P30530, P35968, P36888, Q06418, Q12866, P07949

-

1-[(1,3-dioxolan-2-yl)methyl]-3-(4-methoxyphenyl)-N-methyl-1H-pyrazolo[3,4-d]pyrimidin-6-amine

P08581, P10721, P30530, P35968, P36888, Q06418, Q12866, P07949

-

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

P08581, P10721, P30530, P35968, P36888, Q06418, Q12866, P07949

-

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

P08581, P10721, P30530, P35968, P36888, Q06418, Q12866, P07949

-

1-[3-(1,3-benzodioxol-5-yl)-4-oxo-2,4-dihydroindeno[1,2-c]pyrazol-5-yl]-3-(4-hydroxyphenyl)urea

show

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

P08581, P10721, P30530, P35968, P36888, Q06418, Q12866, P07949

-

2,4,6-trihydroxydeoxybenzoin derivatives

-

diverse derivatives, analysis of inhibitory effect on EGFR tyrosine kinase activity, overview

-

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-[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

show

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

show

5,7-dihydroxyisoflavone derivatives

-

diverse derivatives, analysis of inhibitory effect on EGFR tyrosine kinase activity, overview

-

5-(2-morpholin-4-yl-2-oxoethoxy)-N-[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine

-

5-(4-(dihydroxyboranyl)benzylamino)-2-hydroxybenzoic acid

-

inhibition of EGFR tyrosine kinase

5-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-(1H-indol-5-ylmethyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine

P09619, P35968, P17948, P00533

-

6-(1H-indol-5-ylmethyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine

P09619, P35968, P17948, P00533

-

6-(3-bromobenzyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine

P09619, P35968, P17948, P00533

-

6-(3-bromobenzyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine

P09619, P35968, P17948, P00533

-

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

show

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

show

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

P09619, P35968, P17948, P00533

-

6-[4-fluoro-3-(trifluoromethyl)benzyl]-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine

P09619, P35968, P17948, P00533

-

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

show

AbI kinase

-

activated Abl kinase phosphorylates the EGFR at specific sites and uncouples the receptor from ligand-mediated internalization

-

active pharmacophore 1

-

derivative of lavendustin A, inhibition of EGFR tyrosine kinase

afatinib

-

-

AG1296

-

FLT-3 inhibitor treatment results in formation of larger amounts of the mature 150 kDa form of mutant FLT-3 ITD

AG1478

show

AG556

-

highly selective EGFR kinase inhibitor, 0.01 mM inhibits human ether-a-go-go-related gene channel current and the effect is significantly countered by the protein tyrosine phosphatase inhibitor orthovanadate (1 mM)

Antibody

-

monoclonal antibodies for inhibition of IGF-IR alter receptor trafficking by high affinity binding, promoting receptor degradation and consequently preventing human tumor growth in vivo

-

axitinib

-

-

AZD2171

-

inhibits VEGFR2

AZD4547

-

-

BGB324

P08581, P10721, P30530, P35968, P36888, Q06418, Q12866, P07949

i.e. Bemcentinib

BI2536

-

-

cabozantinib

-

-

canertinib

-

-

CEP-7055

-

inhibits VEGFR1-3

CEP701

-

inhibits FLT3

cetuximab

-

-

-

cisplatin

-

anti-cancer drug inhibiting receptor tyrosine kinases

crizotinib

-

-

cycloheximide

-

depletes the synthetic pool of Met receptor

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

dacomitinib

-

-

dasatinib

-

-

doxorubicin

show

dynamin K44A

-

reduces EGFR internalization to 40%

-

erlotinib

show

ethyl 4-(3-(2-aminoquinazolin-6-yl)-4-methyl-2-oxopyridin-1(2H)-yl)benzoate

-

foretinib

-

-

G protein-coupled receptor kinase-2

-

platelet-derived growth factor-dependent GRK2 phosphorylation desensitizes the PDGF receptor-beta

-

ganglioside GM3

-

0.062 mM, significant inhibition

gefitinib

show

geldanamycin

-

-

gemcitabine

show

Genentech 5D5Fab

-

-

-

genistein

show

GM3

-

inhibitory effect on tyrosine phosphorylation of both mono- and dimeric EGFR

herceptin

show

-

humanized monoclonal antibody

-

blocks the interaction of Ron with hepatocyte growth factor-like protein and diminishes Ron phosphorylation and its downstream signaling

-

hydrogen peroxide

-

limited exposure enhances insulin-induced autophosphorylation of the insulin receptor, while prolonged exposure impairs the action of insulin

imatinib

show

imatinib mesylate

-

potent inhibitor

Iressa

show

KU55933

-

-

lapatinib

show

lavendustin A

-

-

LCRF-0004

-

potent and selective inhibitor

lipid mimetic of GM3

-

inhibitory effect on tyrosine phosphorylation of both mono- and dimeric EGFR

lipid mimetic of lyso-GM3 dimer

-

inhibitory effect on tyrosine phosphorylation of both mono- and dimeric EGFR

luteolin

show

LY2874455

-

-

LY294002

-

PI3K/AKT inhibitor, has no effects on RON-mediated cell spreading either with or without MSP, but completely abrogates the cell survival properties of RON and reduces MSP-induced Transwell migration by 60-80%

lyso-GM3 dimer

-

inhibitory effect on tyrosine phosphorylation of both mono- and dimeric EGFR. A lipid mimetic of lyso-GM3 dimer shows similar strong inhibitory effect on EGF-induced EGFR tyrosine kinase activity, and similar low cytotoxicity, as the authentic lyso-GM3 dimer. Inhibits more strongly than GM3 or a lipid mimetic of GM3

methyl (3Z)-3-(3-[[2-(diethylamino)ethyl]carbamoyl]-2-methyl-1,4,5,6-tetrahydro-7H-indol-7-ylidene)-2-oxo-2,3-dihydro-1H-indole-5-carboxylate

-

-

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

P08581, P10721, P30530, P35968, P36888, Q06418, Q12866, P07949

-

MFCD09840836

-

mithramycin

inhibits binding of Sp factors to GC-rich sites, dramatically reduces Axl promoter activity and Axl, Sp1 and Sp3 expression

MLN518

-

inhibits FLT3

mouse monoclonal blocking antibody

-

increases apoptosis by 32% as compared to gemcitabine alone

-

N,N-dimethyl-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]acetamide

-

N,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

has significant antitumor efficacy against established HT29 human colon adenocarcinoma xenografts implanted in athymic mice

N-(4-chlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-5-fluoro-1-naphthamide

-

N-(4-chlorophenyl)-6-(6-(methylamino)pyrimidin-4-yloxy)-1-naphthamide

-

N-(4-chlorophenyl)-6-(7-methoxyquinolin-4-yloxy)-1-naphthamide

-

N-(4-chlorophenyl)-6-(pyridin-4-yloxy)-1-naphthamide

-

N-(4-chlorophenyl)-6-(pyrimidin-4-yloxy)-1-naphthamide

-

N-(4-chlorophenyl)-6-(quinolin-4-yloxy)-1-naphthamide

-

N-(4-chlorophenyl)-7-(6,7-dimethoxyquinolin-4-yloxy)quinoline-4-carboxamide

-

N-(4-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

show

N-cyclobutyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide

show

N-cyclopentyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide

show

N-cyclopropyl-6-(6,7-dimethoxyquinazolin-4-yloxy)-1-naphthamide

-

N-cyclopropyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide

show

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-[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]-5-(2-morpholin-4-yl-2-oxoethoxy)quinazolin-4-amine

-

-

N-[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]-5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine

-

-

N-[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]-5-[2-(4-methylpiperazin-1-yl)-2-oxoethoxy]quinazolin-4-amine

-

-

N-[3-chloro-4-[(6-methylpyridin-3-yl)oxy]phenyl]-5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine

-

-

N-[3-methoxy-4-[(6-methylpyridin-3-yl)oxy]phenyl]-5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine

-

-

N-[3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]-5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine

-

-

N-[3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]-5-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine

-

-

N-[4-chloro-3-(trifluoromethyl)phenyl]-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine

-

-

N-[4-fluoro-3-(trifluoromethyl)phenyl]-6-methoxy-7-[(morpholin-2-yl)methoxy]quinazolin-4-amine

-

-

N3-(6-aminopyridin-3-yl)-N1-(2-cyclopentylethyl)-4-methylisophthalamide

bisamide

N4-(2-fluoro-4-chlorophenyl)-6-(2,5-dimethoxybenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine

shows potent inhibition of VEGFR-2 over EGFR, platelet-derived growth factor receptor-beta and VEGFR-1

N4-(3-bromo,4-fluorophenyl)-6-(2-pyridin-2-yl-ethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine

P35968, P17948, P00533

in an in vivo B16-F10 syngeneic mouse tumor model, compound exhibits significant reduction in tumor growth rate, in tumor vascular density and in metastases to the lung compared to the control

N4-(3-bromo-phenyl)-7-(3,4,5-trimethoxy-benzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine

dual inhibitor of platelet derived growth factor recptor-beta and vascular endothelial growth factor receptor 2

N4-(3-bromophenyl)-7-(1-naphthylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine

-

N4-(3-bromophenyl)-7-(2-chlorobenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine

dual inhibitor of platelet derived growth factor recptor-beta and vascular endothelial growth factor receptor 2. In a COLO-205, in vivo tumor mouse model, compound demonstrates inhibition of tumor growth, metastasis, and tumor angiogenesis

N4-(4-chloro-2-fluorophenyl)-6-(1-naphthylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine

shows potent inhibition of VEGFR-2 over EGFR, platelet-derived growth factor receptor-beta and VEGFR-1

N4-(4-chloro-2-fluorophenyl)-6-(2-methylbenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine

potent, multiple receptor tyrosine kinase inhibitor

N4-(4-chlorophenyl)-6-(2,5-dimethoxybenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine

potent, multiple receptor tyrosine kinase inhibitor

nakijiquinone C

-

IC50 of 0.125 mg/ml for EGFR, IC50 of 0.103 mg/ml for HER2

neratinib

-

-

NVP-BBT594

-

-

NVP-BEZ235

-

-

NVP-BGJ398

-

-

OSI-774

-

i.e. erlotinib, inhibits EGF receptor protein tyrosine kinase, binding to EGF receptor kinase, structure overview, anticancer drug

pazopanib

-

i.e. 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulphonamide, potent inhibitor of vascular endothelial growth factor receotors 1, 2, and 3, platelet-derived growth factor receptor alpha, platelet-derived growth factor receptor beta, and KIT

PD-173074

-

-

PD153035

-

specific inhibition of EGFR-TK, IC50 is 0.00329 mM with 1 U of purified EGFR-TK from A431 cells

PD168393

show

PD184352

-

-

PD325901

-

-

PD98059

-

-

PF-2341066

-

IC50: 0.002 mM

PHA-665752

show

phosphotyrosyl phosphatase Shp1

-

Shp1 binds to c-Kit at Y570 and acts by dephosphorylating the receptor directly, or inhibits c-Kit signalling indirectly by dephosphorylating other receptor-associated protein-tyrosine kinases

-

PIK-90

-

-

PI_103

-

-

PKC412

-

inhibits FLT3

PKI-166

-

-

Protein kinase C

-

subsequently phosphorylates c-Kit on specific serine residues leading to negative regulation of c-Kit activation

-

protein tyrosine phosphatase 1B

-

PTP1B, requirement for Y1234 and Y1235 in the Met receptor activation loop for interaction with PTP1B

-

quercetin

show

Rapamycin

-

IC50: 3 nM

regorafenib

-

-

siRNA

show

-

sorafenib

show

Spry protein

-

-

-

staurosporine

-

-

STI-571

show

STI571

-

commercial Gleevec/Glivec, specific inhibitor

SU 11248

-

inhibits VEGFR2

SU 6668

-

inhibits VEGFR2 and PDGF receptor beta

SU11248

show

SU5416

-

selective inhibitor

sunitinib

show

T-cell phosphatase

-

TCPTP, requirement for Y1234 and Y1235 in the Met receptor activation loop for interaction with TCPTP

-

Tarceva

show

tert-butyl 2-([[4-(3-bromoanilino)-6-methoxyquinazolin-7-yl]oxy]methyl)morpholine-4-carboxylate

-

-

tert-butyl 2-([[4-(3-chloroanilino)-6-methoxyquinazolin-7-yl]oxy]methyl)morpholine-4-carboxylate

-

-

tert-butyl 2-([[4-(4-bromoanilino)-6-methoxyquinazolin-7-yl]oxy]methyl)morpholine-4-carboxylate

-

-

trastuzumab

-

-

-

trichostatin A

-

the ability of RON to inhibit HIV-1 transcription is sensitive to a histone deacetylase inhibitor

tyrphostin

-

-

tyrphostin 51

-

-

tyrphostin A9

-

PDGF receptor-specific

tyrphostin AG 1478

-

inhibition of EGF receptor

tyrphostin AG 370

-

PDGF receptor-specific

tyrphostin AG1478

-

EGFR-specific antagonist

tyrphostin B56

-

i.e. AG 556, selective EGFR and ErbB-1 kinase inhibitor, reduces volume-sensitive chloride current in atrial myocytes, is antagonized by pretreatment with VO43-

U0126

-

MEK/ERK inhibitor, has no effects on RON-mediated cell spreading either with or without MSP, but completely abrogates the cell survival properties of RON and reduces MSP-induced Transwell migration by 60-80%

varlitinib

-

-

vatalanib

-

i.e. ZK 222584 or PTK 787, inhibits VEGFR1-3

wogonin

-

slight inhibitory effect on epidermal growth factor receptor tyrosine kinase

Wortmannin

-

-

ZD1839

-

i.e. gefitinib, reversible inhibition of ErbB1, competitive to ATP, binding to EGF receptor kinase, structure overview, anticancer drug

ZD6474

-

inhibits VEGFR2

ZSTK474

-

-

[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

-

-

additional information

show

-

back to the top

Go to Activating Compound Search

5-aza-2'-deoxycytidine

demethylation by 5-aza-2'-deoxycytidine upregulates Axl and Sp3 expression in low-Axl-expressing Colo206f/WiDr cells, but not in high-Axl-expressing Rko cells

5-fluorouracil

-

-

AG1478

P04626, P21860, P00533

increases HER2 phosphorylation in the presence of heregulin. Phosphorylation of HER2 is greater by heregulin beta and heregulin beta-1 in the presence of AG 1478

angiopoietin-1

show

-

angiotensin II

show

betacellulin

show

-

brain-derived neurotrophic factor

activates TrkB

-

Calmodulin

ligand-binding induced dimerization enables transautophosphorylation of ErbB1 which results in enhanced intracellular Ca2+ concentration activating calmodulin which reverses autoinhibition by net charge changes in the juxtamembranes

cisplatin

-

AXL can be induced by chemotherapy drugs in acute myeloid leukemia U937 cells and this induction is dependent on the CCWGG methylation status of the AXL promoter

clathrin

-

EGFR is internalized classicaly through clathrin-dependent endocytosis

-

Collagen

250 kDa dimeric DDR1a entity is phosphorylated upon ligand stimulation

Dok-7

-

a cytoplasmic post-synaptic protein coactivator of the muscle-specific receptor-tyrosine kinase MuSK

-

doxorubicin

-

AXL can be induced by chemotherapy drugs in acute myeloid leukemia U937 cells and this induction is dependent on the CCWGG methylation status of the AXL promoter

Epidermal growth factor

show

estrogen

-

induces Ret expression

Gas6

show

-

glial-derived neutrophic factor

-

triggers signaling pathway activation in breast tumor cell lines in a Ret-dependent manner. 10 ng/mL glial-derived neutrophic factor alone or in combination with 100ng/mL glial-derived neutrophic factor receptor alpha1 is the optimal concentration promoting activation of downstream signaling in breast cancer cell lines

-

heparin-binding EGF-like growth factor

activates

-

hepatocyte growth factor

-

-

-

hepatocyte growth factor-like protein

-

stimulates

-

heregulin

show

-

hydrogen peroxide

show

Insulin

show

-

Iressa

P04626, P21860, P00533

acute treatment with 0.001 mM iressa induces a significant increase in HER2 phosphorylation

macrophage stimulating protein

-

MSP, its only known ligand, both MSP-dependent and MSP-independent signaling by RON. RON exhibits MSP-independent tyrosine phosphorylation in MCF-10A cells. RON exhibits increased phosphorylation on Y1238/1239 and on the Y1360 docking site in the presence of exogenously added MSP. Similar levels of RON expression in NIH-3T3 cells do not lead to tyrosine phosphorylation of RON in the absence of ligand. MSP-independent tyrosine phosphorylation of RON also in HeLa cells

-

metformin

-

i.e. N,N-dimethylbiguanide or N,N-dimethylimidodicarbonimidic diamide, activates the insulin receptor tyrosine kinase by phosphorylation at Tyr1150 and Tyr1151, and indirectly via inhibition of protein tyrosine phosphatase 1B, metformin does not alter the order of substrate phosphorylation by the insulin receptor tyrosine kinase

nerve growth factor

activates TrkA, which leads to differentiation of neurons and neurobalstoma cells, whereas it induces proliferation of fibroblasts and apoptosis of medulloblastoma cells

-

neuregulins

activates

-

neurotrophin 3

activates TrkC

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neurotrophin 4

activates TrkB

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neurotrophin-3

activates

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PMA/ionomycin

chronic lymphocytic leukemia cells and normal tonsil B cells, which constitutively express Ror1 mRNA, can not be further activated. In contrast, a 15 to 25fold increase in the ROR1 mRNA expression was observed in in vitro activated normal B and T cells

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PROS1

-

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protein S

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-

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stem cell factor

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soluble and membrane-bound glycoprotein, activating ligand of the stem cell receptor i.e. the Kit protein-tyrosine kinase, stem cell factor ligand binding induces receptor dimerization and tyrosine kinase activation

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thiol/disulfide

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regulation of insulin receptor tyrosine kinase activity by shifts in the redox status

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VP16

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AXL can be induced by chemotherapy drugs in acute myeloid leukemia U937 cells and this induction is dependent on the CCWGG methylation status of the AXL promoter

additional information

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