Page last updated: 2024-08-07 23:09:17

Mitogen-activated protein kinase kinase kinase kinase 4

A mitogen-activated protein kinase kinase kinase kinase 4 that is encoded in the genome of human. [PRO:AL, UniProtKB:O95819]

Synonyms

EC 2.7.11.1;
HPK/GCK-like kinase HGK;
MAPK/ERK kinase kinase kinase 4;
MEK kinase kinase 4;
MEKKK 4;
Nck-interacting kinase

Research

Bioassay Publications (9)

TimeframeStudies on this Protein(%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's3 (33.33)29.6817
2010's5 (55.56)24.3611
2020's1 (11.11)2.80

Compounds (234)

Drugs with Inhibition Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
staurosporineHomo sapiens (human)IC500.000522
birb 796Homo sapiens (human)IC501.000011
ly-2157299Homo sapiens (human)IC500.271622
plx 4720Homo sapiens (human)IC501.846618

Drugs with Activation Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
fasudilHomo sapiens (human)Kd30.000011
4-(4'-hydroxyphenyl)-amino-6,7-dimethoxyquinazolineHomo sapiens (human)Kd30.000011
sb 202190Homo sapiens (human)Kd10.000011
imatinibHomo sapiens (human)Kd16.666733
triciribine phosphateHomo sapiens (human)Kd30.000011
staurosporineHomo sapiens (human)Kd0.024022
picropodophyllinHomo sapiens (human)Kd30.000012
gefitinibHomo sapiens (human)Kd16.666733
lestaurtinibHomo sapiens (human)Kd0.045733
perifosineHomo sapiens (human)Kd30.000011
vatalanibHomo sapiens (human)Kd16.666733
ruboxistaurinHomo sapiens (human)Kd16.666733
canertinibHomo sapiens (human)Kd16.666733
birb 796Homo sapiens (human)Kd0.090022
cyc 202Homo sapiens (human)Kd20.000022
sb 203580Homo sapiens (human)Kd3.700022
enzastaurinHomo sapiens (human)Kd20.000022
erlotinibHomo sapiens (human)Kd16.666733
lapatinibHomo sapiens (human)Kd16.666733
sorafenibHomo sapiens (human)Kd14.880045
pd 173955Homo sapiens (human)Kd0.880011
s 1033Homo sapiens (human)Kd20.000022
xl147Homo sapiens (human)Kd30.000011
bms 387032Homo sapiens (human)Kd16.666733
sf 2370Homo sapiens (human)Kd0.019011
tandutinibHomo sapiens (human)Kd15.000044
vx-745Homo sapiens (human)Kd10.000022
dasatinibHomo sapiens (human)Kd3.357033
ha 1100Homo sapiens (human)Kd30.000012
7-epi-hydroxystaurosporineHomo sapiens (human)Kd0.832011
zd 6474Homo sapiens (human)Kd10.933333
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1h-imidazol-2-yl)benzamideHomo sapiens (human)Kd10.000011
imd 0354Homo sapiens (human)Kd30.000011
sirolimusHomo sapiens (human)Kd30.000011
alvocidibHomo sapiens (human)Kd16.666733
bosutinibHomo sapiens (human)Kd15.004122
orantinibHomo sapiens (human)Kd30.000011
su 11248Homo sapiens (human)Kd0.172044
palbociclibHomo sapiens (human)Kd30.000011
jnj-7706621Homo sapiens (human)Kd10.000011
vx680Homo sapiens (human)Kd11.600033
cyc 116Homo sapiens (human)Kd3.303011
everolimusHomo sapiens (human)Kd30.000011
ekb 569Homo sapiens (human)Kd15.165022
axitinibHomo sapiens (human)Kd1.081022
temsirolimusHomo sapiens (human)Kd30.000012
pd 184352Homo sapiens (human)Kd10.000011
on 01910Homo sapiens (human)Kd30.000011
av 412Homo sapiens (human)Kd30.000011
telatinibHomo sapiens (human)Kd30.000011
y-39983Homo sapiens (human)Kd0.946011
cp 547632Homo sapiens (human)Kd8.111011
bms345541Homo sapiens (human)Kd10.000011
lenvatinibHomo sapiens (human)Kd30.000011
pd 0325901Homo sapiens (human)Kd30.000011
midostaurinHomo sapiens (human)Kd7.987544
px-866Homo sapiens (human)Kd30.000011
ripasudilHomo sapiens (human)Kd30.000011
osi 930Homo sapiens (human)Kd30.000011
ki 20227Homo sapiens (human)Kd10.000011
scio-469Homo sapiens (human)Kd30.000011
cp 724714Homo sapiens (human)Kd20.000022
pi103Homo sapiens (human)Kd10.000022
hmn-214Homo sapiens (human)Kd30.000011
tivozanibHomo sapiens (human)Kd30.000011
hki 272Homo sapiens (human)Kd0.744522
tofacitinibHomo sapiens (human)Kd16.666733
n-(6-chloro-7-methoxy-9h-beta-carbolin-8-yl)-2-methylnicotinamideHomo sapiens (human)Kd10.000011
cediranibHomo sapiens (human)Kd16.000022
masitinibHomo sapiens (human)Kd20.000022
ly-2157299Homo sapiens (human)Kd1.693011
pazopanibHomo sapiens (human)Kd14.066733
azd 6244Homo sapiens (human)Kd20.000022
su 14813Homo sapiens (human)Kd0.491033
bibw 2992Homo sapiens (human)Kd20.000022
binimetinibHomo sapiens (human)Kd30.000011
sotrastaurinHomo sapiens (human)Kd1.580011
aee 788Homo sapiens (human)Kd7.979011
saracatinibHomo sapiens (human)Kd1.121011
vx 702Homo sapiens (human)Kd30.000012
crenolanibHomo sapiens (human)Kd0.282011
tg100-115Homo sapiens (human)Kd20.000022
cc 401Homo sapiens (human)Kd4.172011
bms 599626Homo sapiens (human)Kd30.000011
exel-7647Homo sapiens (human)Kd1.907011
volasertibHomo sapiens (human)Kd30.000011
pha 665752Homo sapiens (human)Kd0.280011
azd 7762Homo sapiens (human)Kd0.035011
regorafenibHomo sapiens (human)Kd30.000011
6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)-4-pyrimidinyl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-oneHomo sapiens (human)Kd20.000022
brivanibHomo sapiens (human)Kd11.673522
mp470Homo sapiens (human)Kd30.000011
rgb 286638Homo sapiens (human)Kd0.127011
np 031112Homo sapiens (human)Kd30.000011
at 7519Homo sapiens (human)Kd20.000022
bms-690514Homo sapiens (human)Kd30.000011
bi 2536Homo sapiens (human)Kd20.000022
inno-406Homo sapiens (human)Kd30.000011
nvp-ast487Homo sapiens (human)Kd0.015022
kw 2449Homo sapiens (human)Kd0.088022
danusertibHomo sapiens (human)Kd62.772011
abt 869Homo sapiens (human)Kd16.666733
azd 8931Homo sapiens (human)Kd30.000011
arq 197Homo sapiens (human)Kd30.000011
azd 1152Homo sapiens (human)Kd30.000011
pf 00299804Homo sapiens (human)Kd30.000011
ridaforolimusHomo sapiens (human)Kd30.000011
ch 4987655Homo sapiens (human)Kd30.000011
6-(5-((cyclopropylamino)carbonyl)-3-fluoro-2-methylphenyl)-n-(2,2-dimethylprpyl)-3-pyridinecarboxamideHomo sapiens (human)Kd30.000011
cc-930Homo sapiens (human)Kd30.000011
gw 2580Homo sapiens (human)Kd10.000022
tak 285Homo sapiens (human)Kd30.000011
idelalisibHomo sapiens (human)Kd30.000011
crizotinibHomo sapiens (human)Kd20.000022
osi 906Homo sapiens (human)Kd30.000011
chir-265Homo sapiens (human)Kd10.866733
motesanibHomo sapiens (human)Kd18.950034
fostamatinibHomo sapiens (human)Kd30.000011
trametinibHomo sapiens (human)Kd30.000011
mln8054Homo sapiens (human)Kd16.666733
pf-562,271Homo sapiens (human)Kd0.230011
GDC-0879Homo sapiens (human)Kd2.300011
jnj-26483327Homo sapiens (human)Kd30.000011
ly2603618Homo sapiens (human)Kd30.000011
tg100801Homo sapiens (human)Kd30.000011
dactolisibHomo sapiens (human)Kd30.000011
bgt226Homo sapiens (human)Kd30.000011
gsk 461364Homo sapiens (human)Kd20.000022
azd 1152-hqpaHomo sapiens (human)Kd16.666733
nvp-tae684Homo sapiens (human)Kd0.970011
enmd 2076Homo sapiens (human)Kd30.000011
e 7050Homo sapiens (human)Kd30.000011
2-amino-8-ethyl-4-methyl-6-(1H-pyrazol-5-yl)-7-pyrido[2,3-d]pyrimidinoneHomo sapiens (human)Kd30.000011
tak-901Homo sapiens (human)Kd30.000011
gdc-0973Homo sapiens (human)Kd30.000011
buparlisibHomo sapiens (human)Kd30.000012
azd 1480Homo sapiens (human)Kd30.000011
azd8330Homo sapiens (human)Kd30.000011
pha 848125Homo sapiens (human)Kd30.000012
ro5126766Homo sapiens (human)Kd30.000011
fedratinibHomo sapiens (human)Kd20.000022
gsk690693Homo sapiens (human)Kd20.000022
14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo(19.3.1.1(2,6).1(8,12))heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaeneHomo sapiens (human)Kd30.000011
azd5438Homo sapiens (human)Kd30.000011
pf 04217903Homo sapiens (human)Kd30.000011
gdc 0941Homo sapiens (human)Kd20.000022
icotinibHomo sapiens (human)Kd30.000011
ph 797804Homo sapiens (human)Kd30.000011
kx-01Homo sapiens (human)Kd30.000011
plx 4720Homo sapiens (human)Kd10.000011
mk 5108Homo sapiens (human)Kd30.000011
cx 4945Homo sapiens (human)Kd30.000012
cudc 101Homo sapiens (human)Kd30.000011
arry-614Homo sapiens (human)Kd0.222011
tak 593Homo sapiens (human)Kd30.000011
mln 8237Homo sapiens (human)Kd30.000011
sgx 523Homo sapiens (human)Kd20.000022
bms 754807Homo sapiens (human)Kd30.000011
bms 777607Homo sapiens (human)Kd30.000012
sgi 1776Homo sapiens (human)Kd30.000011
pci 32765Homo sapiens (human)Kd30.000011
ponatinibHomo sapiens (human)Kd0.307011
amg 900Homo sapiens (human)Kd30.000011
mk-1775Homo sapiens (human)Kd30.000011
AMG-208Homo sapiens (human)Kd30.000011
quizartinibHomo sapiens (human)Kd11.666733
at13148Homo sapiens (human)Kd30.000011
tak 733Homo sapiens (human)Kd30.000011
mk 2206Homo sapiens (human)Kd30.000011
sns 314Homo sapiens (human)Kd30.000011
lucitanibHomo sapiens (human)Kd30.000011
pf-04691502Homo sapiens (human)Kd30.000012
n-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamideHomo sapiens (human)Kd30.000012
dcc-2036Homo sapiens (human)Kd2.711011
cabozantinibHomo sapiens (human)Kd30.000011
defactinibHomo sapiens (human)Kd30.000011
ly2584702Homo sapiens (human)Kd30.000011
incb-018424Homo sapiens (human)Kd20.000022
poziotinibHomo sapiens (human)Kd30.000011
asp3026Homo sapiens (human)Kd30.000011
entrectinibHomo sapiens (human)Kd30.000011
pexidartinibHomo sapiens (human)Kd30.000011
TAK-580Homo sapiens (human)Kd30.000011
gsk 2126458Homo sapiens (human)Kd30.000011
emd1214063Homo sapiens (human)Kd30.000011
gsk 1838705aHomo sapiens (human)Kd10.000011
pf 3758309Homo sapiens (human)Kd30.000011
gdc 0980Homo sapiens (human)Kd30.000011
azd2014Homo sapiens (human)Kd30.000011
(5-(2,4-bis((3s)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanolHomo sapiens (human)Kd30.000011
plx4032Homo sapiens (human)Kd30.000011
gsk 1363089Homo sapiens (human)Kd15.095022
arry-334543Homo sapiens (human)Kd30.000011
kin-193Homo sapiens (human)Kd30.000012
mk 2461Homo sapiens (human)Kd30.000011
bay 869766Homo sapiens (human)Kd30.000011
as 703026Homo sapiens (human)Kd30.000011
baricitinibHomo sapiens (human)Kd30.000011
dabrafenibHomo sapiens (human)Kd30.000011
pki 587Homo sapiens (human)Kd30.000012
n-(3-fluoro-4-((1-methyl-6-(1h-pyrazol-4-yl)-1h-indazol-5 yl)oxy)phenyl)-1-(4-fluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridine-3-carboxamideHomo sapiens (human)Kd30.000011
ribociclibHomo sapiens (human)Kd30.000011
mk-8033Homo sapiens (human)Kd30.000011
pha 793887Homo sapiens (human)Kd30.000011
sb 1518Homo sapiens (human)Kd0.293011
abemaciclibHomo sapiens (human)Kd1.322011
mk-8776Homo sapiens (human)Kd30.000011
afuresertibHomo sapiens (human)Kd30.000011
gsk 1070916Homo sapiens (human)Kd1.223011
jnj38877605Homo sapiens (human)Kd30.000011
dinaciclibHomo sapiens (human)Kd30.000011
gilteritinibHomo sapiens (human)Kd0.202011
alectinibHomo sapiens (human)Kd30.000011
glpg0634Homo sapiens (human)Kd30.000011
encorafenibHomo sapiens (human)Kd30.000011
bms-911543Homo sapiens (human)Kd30.000011
gsk2141795Homo sapiens (human)Kd30.000011
azd8186Homo sapiens (human)Kd30.000011
byl719Homo sapiens (human)Kd30.000011
cep-32496Homo sapiens (human)Kd30.000011
rociletinibHomo sapiens (human)Kd30.000011
ceritinibHomo sapiens (human)Kd30.000011
azd1208Homo sapiens (human)Kd30.000011
vx-509Homo sapiens (human)Kd30.000011
debio 1347Homo sapiens (human)Kd30.000011
volitinibHomo sapiens (human)Kd30.000011
osimertinibHomo sapiens (human)Kd30.000011
at 9283Homo sapiens (human)Kd0.108011
otssp167Homo sapiens (human)Kd0.088011
chir 258Homo sapiens (human)Kd0.166333
osi 027Homo sapiens (human)Kd30.000011
nintedanibHomo sapiens (human)Kd0.761522
bay 80-6946Homo sapiens (human)Kd30.000011
pp242Homo sapiens (human)Kd1.300011

Enables

This protein enables 7 target(s):

TargetCategoryDefinition
creatine kinase activitymolecular functionCatalysis of the reaction: ATP + creatine = N-phosphocreatine + ADP + 2 H+. [EC:2.7.3.2, RHEA:17157]
protein serine/threonine kinase activitymolecular functionCatalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate, and ATP + protein threonine = ADP + protein threonine phosphate. [GOC:bf, MetaCyc:PROTEIN-KINASE-RXN, PMID:2956925]
protein bindingmolecular functionBinding to a protein. [GOC:go_curators]
ATP bindingmolecular functionBinding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732]
microtubule bindingmolecular functionBinding to a microtubule, a filament composed of tubulin monomers. [GOC:krc]
MAP kinase kinase kinase kinase activitymolecular functionCatalysis of the phosphorylation of serine and threonine residues in a mitogen-activated protein kinase kinase kinase (MAPKKK), resulting in activation of MAPKKK. MAPKKK signaling pathways relay, amplify and integrate signals from the plasma membrane to the nucleus in response to a diverse range of extracellular stimuli. [GOC:bf, PMID:11790549]
protein serine kinase activitymolecular functionCatalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate. [RHEA:17989]

Located In

This protein is located in 2 target(s):

TargetCategoryDefinition
cytoplasmcellular componentThe contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684]
focal adhesioncellular componentA cell-substrate junction that anchors the cell to the extracellular matrix and that forms a point of termination of actin filaments. In insects focal adhesion has also been referred to as hemi-adherens junction (HAJ). [GOC:aruk, GOC:bc, ISBN:0124325653, ISBN:0815316208, PMID:10419689, PMID:12191915, PMID:15246682, PMID:1643657, PMID:16805308, PMID:19197329, PMID:23033047, PMID:26923917, PMID:28796323, PMID:8314002]

Active In

This protein is active in 1 target(s):

TargetCategoryDefinition
cytoplasmcellular componentThe contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684]

Involved In

This protein is involved in 15 target(s):

TargetCategoryDefinition
negative regulation of cell-matrix adhesionbiological processAny process that stops, prevents, or reduces the rate or extent of cell adhesion to the extracellular matrix. [GOC:hjd]
protein phosphorylationbiological processThe process of introducing a phosphate group on to a protein. [GOC:hb]
positive regulation of cell migrationbiological processAny process that activates or increases the frequency, rate or extent of cell migration. [GOC:go_curators]
positive regulation of ARF protein signal transductionbiological processAny process that activates or increases the frequency, rate or extent of ARF protein signal transduction. [GOC:mah]
positive regulation of hippo signalingbiological processAny process that activates or increases the frequency, rate or extent of hippo signaling. [GOC:bf]
intracellular signal transductionbiological processThe process in which a signal is passed on to downstream components within the cell, which become activated themselves to further propagate the signal and finally trigger a change in the function or state of the cell. [GOC:bf, GOC:jl, GOC:signaling, ISBN:3527303782]
negative regulation of apoptotic processbiological processAny process that stops, prevents, or reduces the frequency, rate or extent of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis]
positive regulation of GTPase activitybiological processAny process that activates or increases the activity of a GTPase. [GOC:jl, GOC:mah]
regulation of JNK cascadebiological processAny process that modulates the frequency, rate or extent of signal transduction mediated by the JNK cascade. [GOC:bf]
positive regulation of keratinocyte migrationbiological processAny process that activates or increases the frequency, rate or extent of keratinocyte migration. [GOC:ai]
positive regulation of focal adhesion assemblybiological processAny process that activates or increases the frequency, rate or extent of focal adhesion assembly, the establishment and maturation of focal adhesions. [GOC:ai]
positive regulation of focal adhesion disassemblybiological processAny process that activates or increases the frequency, rate or extent of disaggregation of a focal adhesion into its constituent components. [PMID:25490267]
regulation of MAPK cascadebiological processAny process that modulates the frequency, rate or extent of signal transduction mediated by the MAP kinase (MAPK) cascade. [GOC:go_curators]
MAPK cascadebiological processAn intracellular protein kinase cascade containing at least a MAP kinase (MAPK). It starts with the activation of a MAP3K, and the consecutive activation of a MPK2K and a MAPK. The cascade can also contain an additional tier: the upstream MAP4K. The kinases in each tier phosphorylate and activate the kinase in the downstream tier to transmit a signal within a cell. [PMID:20811974, PMID:9561267]
neuron projection morphogenesisbiological processThe process in which the anatomical structures of a neuron projection are generated and organized. A neuron projection is any process extending from a neural cell, such as axons or dendrites. [GOC:mah]