Page last updated: 2024-08-08 00:28:00

Mitogen-activated protein kinase kinase kinase 4

A mitogen-activated protein kinase kinase kinase 4 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9Y6R4]

Synonyms

EC 2.7.11.25;
MAP three kinase 1;
MAPK/ERK kinase kinase 4;
MEK kinase 4;
MEKK 4

Research

Bioassay Publications (5)

TimeframeStudies on this Protein(%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's3 (60.00)29.6817
2010's2 (40.00)24.3611
2020's0 (0.00)2.80

Compounds (234)

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)Kd1.533333
picropodophyllinHomo sapiens (human)Kd30.000011
gefitinibHomo sapiens (human)Kd16.666733
lestaurtinibHomo sapiens (human)Kd11.733333
perifosineHomo sapiens (human)Kd30.000011
vatalanibHomo sapiens (human)Kd16.666733
ruboxistaurinHomo sapiens (human)Kd16.666733
canertinibHomo sapiens (human)Kd12.200044
birb 796Homo sapiens (human)Kd10.000022
cyc 202Homo sapiens (human)Kd20.000022
sb 203580Homo sapiens (human)Kd10.000022
enzastaurinHomo sapiens (human)Kd20.000022
erlotinibHomo sapiens (human)Kd16.666733
lapatinibHomo sapiens (human)Kd16.666733
sorafenibHomo sapiens (human)Kd15.000044
pd 173955Homo sapiens (human)Kd0.056011
s 1033Homo sapiens (human)Kd20.000022
xl147Homo sapiens (human)Kd30.000011
bms 387032Homo sapiens (human)Kd16.666733
sf 2370Homo sapiens (human)Kd30.000011
tandutinibHomo sapiens (human)Kd15.000044
vx-745Homo sapiens (human)Kd10.000022
dasatinibHomo sapiens (human)Kd10.206733
ha 1100Homo sapiens (human)Kd30.000012
7-epi-hydroxystaurosporineHomo sapiens (human)Kd30.000011
zd 6474Homo sapiens (human)Kd11.950044
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)Kd30.000012
sirolimusHomo sapiens (human)Kd30.000011
alvocidibHomo sapiens (human)Kd16.666733
bosutinibHomo sapiens (human)Kd0.873022
orantinibHomo sapiens (human)Kd30.000011
su 11248Homo sapiens (human)Kd11.620055
palbociclibHomo sapiens (human)Kd30.000012
jnj-7706621Homo sapiens (human)Kd10.000011
vx680Homo sapiens (human)Kd11.666733
cyc 116Homo sapiens (human)Kd30.000011
everolimusHomo sapiens (human)Kd30.000011
ekb 569Homo sapiens (human)Kd0.259733
axitinibHomo sapiens (human)Kd21.866723
temsirolimusHomo sapiens (human)Kd30.000011
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)Kd30.000011
cp 547632Homo sapiens (human)Kd30.000011
bms345541Homo sapiens (human)Kd10.000011
lenvatinibHomo sapiens (human)Kd30.000011
pd 0325901Homo sapiens (human)Kd30.000011
midostaurinHomo sapiens (human)Kd18.000045
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)Kd0.462022
tofacitinibHomo sapiens (human)Kd16.666733
n-(6-chloro-7-methoxy-9h-beta-carbolin-8-yl)-2-methylnicotinamideHomo sapiens (human)Kd10.000011
cediranibHomo sapiens (human)Kd20.000022
masitinibHomo sapiens (human)Kd20.000022
ly-2157299Homo sapiens (human)Kd30.000011
pazopanibHomo sapiens (human)Kd16.666733
azd 6244Homo sapiens (human)Kd20.000022
su 14813Homo sapiens (human)Kd16.666733
bibw 2992Homo sapiens (human)Kd20.000022
binimetinibHomo sapiens (human)Kd30.000011
sotrastaurinHomo sapiens (human)Kd30.000012
aee 788Homo sapiens (human)Kd2.189011
saracatinibHomo sapiens (human)Kd30.000011
vx 702Homo sapiens (human)Kd30.000011
crenolanibHomo sapiens (human)Kd30.000011
tg100-115Homo sapiens (human)Kd20.000022
cc 401Homo sapiens (human)Kd30.000011
bms 599626Homo sapiens (human)Kd30.000011
exel-7647Homo sapiens (human)Kd30.000011
volasertibHomo sapiens (human)Kd30.000011
pha 665752Homo sapiens (human)Kd1.800011
azd 7762Homo sapiens (human)Kd30.000011
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)Kd15.420022
brivanibHomo sapiens (human)Kd20.000022
mp470Homo sapiens (human)Kd30.000011
rgb 286638Homo sapiens (human)Kd30.000011
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)Kd10.000022
kw 2449Homo sapiens (human)Kd15.800022
danusertibHomo sapiens (human)Kd30.000011
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)Kd30.000012
crizotinibHomo sapiens (human)Kd20.000022
osi 906Homo sapiens (human)Kd30.000011
chir-265Homo sapiens (human)Kd16.666733
motesanibHomo sapiens (human)Kd16.666733
fostamatinibHomo sapiens (human)Kd30.000012
trametinibHomo sapiens (human)Kd30.000011
mln8054Homo sapiens (human)Kd7.295733
pf-562,271Homo sapiens (human)Kd30.000011
GDC-0879Homo sapiens (human)Kd10.000011
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)Kd2.000011
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)Kd30.000011
azd 1480Homo sapiens (human)Kd30.000011
azd8330Homo sapiens (human)Kd30.000011
pha 848125Homo sapiens (human)Kd4.021011
ro5126766Homo sapiens (human)Kd30.000011
fedratinibHomo sapiens (human)Kd17.050022
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)Kd30.000012
kx-01Homo sapiens (human)Kd30.000011
plx 4720Homo sapiens (human)Kd10.000011
mk 5108Homo sapiens (human)Kd30.000011
cx 4945Homo sapiens (human)Kd30.000011
cudc 101Homo sapiens (human)Kd30.000011
arry-614Homo sapiens (human)Kd30.000011
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)Kd30.000011
sgi 1776Homo sapiens (human)Kd30.000011
pci 32765Homo sapiens (human)Kd30.000011
ponatinibHomo sapiens (human)Kd30.000011
amg 900Homo sapiens (human)Kd30.000011
mk-1775Homo sapiens (human)Kd0.052011
AMG-208Homo sapiens (human)Kd30.000011
quizartinibHomo sapiens (human)Kd16.666733
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)Kd30.000011
n-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamideHomo sapiens (human)Kd30.000011
dcc-2036Homo sapiens (human)Kd30.000011
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)Kd30.000012
plx4032Homo sapiens (human)Kd30.000011
gsk 1363089Homo sapiens (human)Kd15.950022
arry-334543Homo sapiens (human)Kd30.000011
kin-193Homo sapiens (human)Kd30.000011
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)Kd30.000011
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)Kd30.000011
abemaciclibHomo sapiens (human)Kd30.000011
mk-8776Homo sapiens (human)Kd30.000011
afuresertibHomo sapiens (human)Kd30.000011
gsk 1070916Homo sapiens (human)Kd1.431011
jnj38877605Homo sapiens (human)Kd30.000012
dinaciclibHomo sapiens (human)Kd30.000011
gilteritinibHomo sapiens (human)Kd30.000011
alectinibHomo sapiens (human)Kd30.000011
glpg0634Homo sapiens (human)Kd30.000011
encorafenibHomo sapiens (human)Kd1.437011
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)Kd30.000012
debio 1347Homo sapiens (human)Kd30.000011
volitinibHomo sapiens (human)Kd30.000011
osimertinibHomo sapiens (human)Kd30.000011
at 9283Homo sapiens (human)Kd30.000011
otssp167Homo sapiens (human)Kd30.000011
chir 258Homo sapiens (human)Kd13.666733
osi 027Homo sapiens (human)Kd30.000011
nintedanibHomo sapiens (human)Kd20.000022
bay 80-6946Homo sapiens (human)Kd30.000011
pp242Homo sapiens (human)Kd10.000011

Enables

This protein enables 5 target(s):

TargetCategoryDefinition
MAP kinase kinase kinase activitymolecular functionCatalysis of the phosphorylation and activation of a MAP kinase kinase; each MAP kinase kinase can be phosphorylated by any of several MAP kinase kinase kinases. [PMID:9561267]
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]
metal ion bindingmolecular functionBinding to a metal ion. [GOC:ai]
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]
perinuclear region of cytoplasmcellular componentCytoplasm situated near, or occurring around, the nucleus. [GOC:jid]

Involved In

This protein is involved in 12 target(s):

TargetCategoryDefinition
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]
placenta developmentbiological processThe process whose specific outcome is the progression of the placenta over time, from its formation to the mature structure. The placenta is an organ of metabolic interchange between fetus and mother, partly of embryonic origin and partly of maternal origin. [GOC:add, ISBN:068340007X]
response to UV-Cbiological processAny process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a UV-C radiation stimulus. UV-C radiation (UV-C light) spans the wavelengths 100 to 280 nm. [GOC:tb]
regulation of gene expressionbiological processAny process that modulates the frequency, rate or extent of gene expression. Gene expression is the process in which a gene's coding sequence is converted into a mature gene product (protein or RNA). [GOC:txnOH-2018]
male germ-line sex determinationbiological processThe determination of sex and sexual phenotype in a male organism's germ line. [GOC:mah]
positive regulation of telomere maintenance via telomerasebiological processAny process that activates or increases the frequency, rate or extent of the addition of telomeric repeats by telomerase. [GOC:mah]
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]
positive regulation of JUN kinase activitybiological processAny process that activates or increases the frequency, rate or extent of JUN kinase activity. [GOC:jl]
positive regulation of telomerase activitybiological processAny process that activates or increases the frequency, rate or extent of telomerase activity, the catalysis of the reaction: deoxynucleoside triphosphate + DNA(n) = diphosphate + DNA(n+1). [GOC:ai]
chorionic trophoblast cell differentiationbiological processThe process in which relatively unspecialized cells of the ectoplacental cone acquire specialized structural and/or functional features that characterize chorionic trophoblasts. These cells will migrate towards the spongiotrophoblast layer and give rise to syncytiotrophoblasts of the labyrinthine layer. [CL:0011101, GOC:dph, PMID:16983341]
positive regulation of p38MAPK cascadebiological processAny process that activates or increases the frequency, rate or extent of p38MAPK cascade. [GOC:TermGenie]
positive regulation of telomere cappingbiological processAny process that activates or increases the frequency, rate or extent of telomere capping. [GO_REF:0000058, GOC:BHF, GOC:BHF_telomere, GOC:nc, GOC:TermGenie, PMID:23959892]