Page last updated: 2024-08-07 18:42:54

Mitogen-activated protein kinase kinase kinase 11

A mitogen-activated protein kinase kinase kinase 11 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q16584]

Synonyms

EC 2.7.11.25;
Mixed lineage kinase 3;
Src-homology 3 domain-containing proline-rich kinase

Research

Bioassay Publications (14)

TimeframeStudies on this Protein(%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's6 (42.86)29.6817
2010's7 (50.00)24.3611
2020's1 (7.14)2.80

Compounds (238)

Drugs with Inhibition Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
staurosporine aglyconeHomo sapiens (human)IC500.078723
staurosporineHomo sapiens (human)IC500.016033
repsoxHomo sapiens (human)IC5016.000011
sf 2370Homo sapiens (human)IC500.026713
3,9-bis((ethylthio)methyl)-k-252aHomo sapiens (human)IC500.036456
7-methyl-5-(1-((3-(trifluoromethyl)phenyl)acetyl)-2,3-dihydro-1h-indol-5-yl)-7h-pyrrolo(2,3-d)pyrimidin-4-amineHomo sapiens (human)IC501.140011
urmc-099Homo sapiens (human)IC500.014011

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)Kd0.020033
picropodophyllinHomo sapiens (human)Kd30.000012
gefitinibHomo sapiens (human)Kd16.666733
lestaurtinibHomo sapiens (human)Kd0.052044
perifosineHomo sapiens (human)Kd30.000011
vatalanibHomo sapiens (human)Kd16.666733
ruboxistaurinHomo sapiens (human)Kd16.666733
canertinibHomo sapiens (human)Kd16.666733
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)Kd0.550022
s 1033Homo sapiens (human)Kd20.000022
xl147Homo sapiens (human)Kd30.000011
bms 387032Homo sapiens (human)Kd16.666733
sf 2370Homo sapiens (human)Kd0.572011
tandutinibHomo sapiens (human)Kd15.000044
vx-745Homo sapiens (human)Kd10.000022
dasatinibHomo sapiens (human)Kd16.666733
ha 1100Homo sapiens (human)Kd30.000011
7-epi-hydroxystaurosporineHomo sapiens (human)Kd0.303011
zd 6474Homo sapiens (human)Kd16.666733
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)Kd16.350022
orantinibHomo sapiens (human)Kd2.660011
su 11248Homo sapiens (human)Kd1.749244
palbociclibHomo sapiens (human)Kd30.000011
jnj-7706621Homo sapiens (human)Kd10.000011
vx680Homo sapiens (human)Kd8.010044
cyc 116Homo sapiens (human)Kd4.048011
everolimusHomo sapiens (human)Kd30.000011
ekb 569Homo sapiens (human)Kd20.000022
axitinibHomo sapiens (human)Kd20.000022
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)Kd0.328055
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)Kd17.900022
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)Kd1.032844
azd 6244Homo sapiens (human)Kd20.000022
su 14813Homo sapiens (human)Kd11.133333
bibw 2992Homo sapiens (human)Kd20.000022
binimetinibHomo sapiens (human)Kd30.000012
sotrastaurinHomo sapiens (human)Kd30.000011
aee 788Homo sapiens (human)Kd30.000011
saracatinibHomo sapiens (human)Kd30.000011
vx 702Homo sapiens (human)Kd30.000011
crenolanibHomo sapiens (human)Kd3.066011
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)Kd10.000011
azd 7762Homo sapiens (human)Kd0.081011
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)Kd0.017033
brivanibHomo sapiens (human)Kd20.000022
rgb 286638Homo sapiens (human)Kd0.265011
np 031112Homo sapiens (human)Kd30.000011
at 7519Homo sapiens (human)Kd20.000022
bms-690514Homo sapiens (human)Kd2.604011
bi 2536Homo sapiens (human)Kd20.000022
inno-406Homo sapiens (human)Kd30.000011
nvp-ast487Homo sapiens (human)Kd7.000022
kw 2449Homo sapiens (human)Kd1.071733
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)Kd30.000011
crizotinibHomo sapiens (human)Kd20.000022
osi 906Homo sapiens (human)Kd30.000011
chir-265Homo sapiens (human)Kd19.875034
motesanibHomo sapiens (human)Kd16.666733
fostamatinibHomo sapiens (human)Kd2.506011
trametinibHomo sapiens (human)Kd30.000011
mln8054Homo sapiens (human)Kd16.666733
pf-562,271Homo sapiens (human)Kd0.444011
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)Kd0.420022
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)Kd2.536011
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)Kd2.484011
ro5126766Homo sapiens (human)Kd30.000011
fedratinibHomo sapiens (human)Kd16.550022
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)Kd30.000012
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)Kd2.965011
cudc 101Homo sapiens (human)Kd30.000012
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)Kd2.023011
AMG-208Homo sapiens (human)Kd30.000011
quizartinibHomo sapiens (human)Kd16.666733
at13148Homo sapiens (human)Kd30.000012
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)Kd3.059011
cabozantinibHomo sapiens (human)Kd30.000011
defactinibHomo sapiens (human)Kd0.902011
ly2584702Homo sapiens (human)Kd30.000011
incb-018424Homo sapiens (human)Kd5.950022
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)Kd1.560011
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)Kd10.226733
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)Kd30.000012
baricitinibHomo sapiens (human)Kd30.000011
dabrafenibHomo sapiens (human)Kd1.011011
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)Kd17.984011
jnj38877605Homo sapiens (human)Kd30.000011
dinaciclibHomo sapiens (human)Kd30.000011
gilteritinibHomo sapiens (human)Kd0.600011
alectinibHomo sapiens (human)Kd30.000011
glpg0634Homo sapiens (human)Kd30.000011
encorafenibHomo sapiens (human)Kd0.812011
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)Kd0.056011
otssp167Homo sapiens (human)Kd0.052011
chir 258Homo sapiens (human)Kd1.894333
osi 027Homo sapiens (human)Kd30.000011
nintedanibHomo sapiens (human)Kd10.466733
bay 80-6946Homo sapiens (human)Kd30.000011
pp242Homo sapiens (human)Kd10.000011

Enables

This protein enables 12 target(s):

TargetCategoryDefinition
protein kinase activitymolecular functionCatalysis of the phosphorylation of an amino acid residue in a protein, usually according to the reaction: a protein + ATP = a phosphoprotein + ADP. [PMID:25399640]
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]
JUN kinase kinase kinase activitymolecular functionCatalysis of the reaction: JNKK + ATP = JNKK phosphate + ADP. This reaction is the phosphorylation and activation of JUN kinase kinases (JNKKs). [GOC:bf]
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]
small GTPase bindingmolecular functionBinding to a small monomeric GTPase. [GOC:mah, PMID:27218782]
mitogen-activated protein kinase kinase bindingmolecular functionBinding to a mitogen-activated protein kinase kinase, a protein that can phosphorylate a MAP kinase. [GOC:mah]
mitogen-activated protein kinase kinase kinase bindingmolecular functionBinding to a mitogen-activated protein kinase kinase kinase, a protein that can phosphorylate a MAP kinase kinase. [GOC:bf]
identical protein bindingmolecular functionBinding to an identical protein or proteins. [GOC:jl]
protein homodimerization activitymolecular functionBinding to an identical protein to form a homodimer. [GOC:jl]
protein serine kinase activitymolecular functionCatalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate. [RHEA:17989]

Located In

This protein is located in 4 target(s):

TargetCategoryDefinition
centrosomecellular componentA structure comprised of a core structure (in most organisms, a pair of centrioles) and peripheral material from which a microtubule-based structure, such as a spindle apparatus, is organized. Centrosomes occur close to the nucleus during interphase in many eukaryotic cells, though in animal cells it changes continually during the cell-division cycle. [GOC:mah, ISBN:0198547684]
cytosolcellular componentThe part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl]
microtubulecellular componentAny of the long, generally straight, hollow tubes of internal diameter 12-15 nm and external diameter 24 nm found in a wide variety of eukaryotic cells; each consists (usually) of 13 protofilaments of polymeric tubulin, staggered in such a manner that the tubulin monomers are arranged in a helical pattern on the microtubular surface, and with the alpha/beta axes of the tubulin subunits parallel to the long axis of the tubule; exist in equilibrium with pool of tubulin monomers and can be rapidly assembled or disassembled in response to physiological stimuli; concerned with force generation, e.g. in the spindle. [ISBN:0879693568]
membranecellular componentA lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194]

Active In

This protein is active in 1 target(s):

TargetCategoryDefinition
centrosomecellular componentA structure comprised of a core structure (in most organisms, a pair of centrioles) and peripheral material from which a microtubule-based structure, such as a spindle apparatus, is organized. Centrosomes occur close to the nucleus during interphase in many eukaryotic cells, though in animal cells it changes continually during the cell-division cycle. [GOC:mah, ISBN:0198547684]

Involved In

This protein is involved in 10 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]
protein phosphorylationbiological processThe process of introducing a phosphate group on to a protein. [GOC:hb]
microtubule-based processbiological processAny cellular process that depends upon or alters the microtubule cytoskeleton, that part of the cytoskeleton comprising microtubules and their associated proteins. [GOC:mah]
JNK cascadebiological processA MAPK cascade containing at least the JNK (MAPK8) MAP kinase. It starts with the activation of JUN3K (a MAPK3K), which activates JNKK a MAP2K), which in turn activates JNK. The cascade can also contain an additional tier: the upstream MAP4K. The kinases in each tier phosphorylate and activate the kinases in the downstream tier. The JNK cascade is activated by stress signals, as well as by G protein-coupled receptors, growth factors, and cytokines, and results in cellular responses such as cell proliferation, cell differentiation, apoptosis and inflammation. [PMID:11790549, PMID:20811974, PMID:23125017]
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 neuron apoptotic processbiological processAny process that activates or increases the frequency, rate or extent of cell death of neurons by apoptotic process. [GOC:go_curators, GOC:mtg_apoptosis]
cell cycle G1/S phase transitionbiological processThe cell cycle process by which a cell in G1 phase commits to S phase. [GOC:mtg_cell_cycle]
positive regulation of JNK cascadebiological processAny process that activates or increases the frequency, rate or extent of signal transduction mediated by the JNK cascade. [GOC:bf]
protein autophosphorylationbiological processThe phosphorylation by a protein of one or more of its own amino acid residues (cis-autophosphorylation), or residues on an identical protein (trans-autophosphorylation). [ISBN:0198506732]
positive regulation of apoptotic processbiological processAny process that activates or increases the frequency, rate or extent of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis]