Page last updated: 2024-08-07 23:48:26

Dual specificity mitogen-activated protein kinase kinase 5

A dual specificity mitogen-activated protein kinase kinase 5 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q13163]

Synonyms

MAP kinase kinase 5;
MAPKK 5;
EC 2.7.12.2;
MAPK/ERK kinase 5;
MEK 5

Research

Bioassay Publications (9)

TimeframeStudies on this Protein(%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's7 (77.78)24.3611
2020's2 (22.22)2.80

Compounds (234)

Drugs with Inhibition Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
staurosporineHomo sapiens (human)IC500.025222
tak 285Homo sapiens (human)IC505.700011
ly3009120Homo sapiens (human)IC500.800011
bix 02188Homo sapiens (human)IC500.004311
bix 02189Homo sapiens (human)IC500.001533

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
imatinibHomo sapiens (human)Kd20.000022
triciribine phosphateHomo sapiens (human)Kd30.000011
staurosporineHomo sapiens (human)Kd0.002911
picropodophyllinHomo sapiens (human)Kd30.000011
gefitinibHomo sapiens (human)Kd20.200023
lestaurtinibHomo sapiens (human)Kd0.900522
perifosineHomo sapiens (human)Kd30.000011
vatalanibHomo sapiens (human)Kd20.000022
ruboxistaurinHomo sapiens (human)Kd15.550022
canertinibHomo sapiens (human)Kd15.030022
birb 796Homo sapiens (human)Kd10.000011
cyc 202Homo sapiens (human)Kd30.000011
sb 203580Homo sapiens (human)Kd1.400011
enzastaurinHomo sapiens (human)Kd20.000022
erlotinibHomo sapiens (human)Kd2.001022
lapatinibHomo sapiens (human)Kd15.550022
sorafenibHomo sapiens (human)Kd15.095022
pd 173955Homo sapiens (human)Kd0.058011
s 1033Homo sapiens (human)Kd15.095022
xl147Homo sapiens (human)Kd30.000011
bms 387032Homo sapiens (human)Kd20.000022
sf 2370Homo sapiens (human)Kd2.033011
tandutinibHomo sapiens (human)Kd21.033323
vx-745Homo sapiens (human)Kd10.000011
dasatinibHomo sapiens (human)Kd0.717622
ha 1100Homo sapiens (human)Kd30.000011
7-epi-hydroxystaurosporineHomo sapiens (human)Kd30.000011
zd 6474Homo sapiens (human)Kd15.024522
imd 0354Homo sapiens (human)Kd30.000011
sirolimusHomo sapiens (human)Kd30.000011
alvocidibHomo sapiens (human)Kd15.090022
bosutinibHomo sapiens (human)Kd0.838622
orantinibHomo sapiens (human)Kd4.938011
su 11248Homo sapiens (human)Kd1.785522
palbociclibHomo sapiens (human)Kd30.000011
vx680Homo sapiens (human)Kd15.130022
cyc 116Homo sapiens (human)Kd1.478011
everolimusHomo sapiens (human)Kd30.000011
ekb 569Homo sapiens (human)Kd30.000011
axitinibHomo sapiens (human)Kd15.070022
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)Kd2.910011
pd 0325901Homo sapiens (human)Kd0.808011
midostaurinHomo sapiens (human)Kd20.000022
px-866Homo sapiens (human)Kd30.000011
ripasudilHomo sapiens (human)Kd30.000011
osi 930Homo sapiens (human)Kd30.000011
ki 20227Homo sapiens (human)Kd0.007411
scio-469Homo sapiens (human)Kd30.000011
cp 724714Homo sapiens (human)Kd1.255011
pi103Homo sapiens (human)Kd10.000011
hmn-214Homo sapiens (human)Kd30.000011
tivozanibHomo sapiens (human)Kd30.000011
hki 272Homo sapiens (human)Kd15.031522
tofacitinibHomo sapiens (human)Kd20.000022
n-(6-chloro-7-methoxy-9h-beta-carbolin-8-yl)-2-methylnicotinamideHomo sapiens (human)Kd10.000011
cediranibHomo sapiens (human)Kd15.750022
masitinibHomo sapiens (human)Kd20.000022
ly-2157299Homo sapiens (human)Kd30.000011
pazopanibHomo sapiens (human)Kd15.240022
azd 6244Homo sapiens (human)Kd20.000022
su 14813Homo sapiens (human)Kd15.037522
bibw 2992Homo sapiens (human)Kd15.650022
binimetinibHomo sapiens (human)Kd30.000011
sotrastaurinHomo sapiens (human)Kd30.000011
aee 788Homo sapiens (human)Kd9.430011
saracatinibHomo sapiens (human)Kd30.000011
vx 702Homo sapiens (human)Kd30.000011
crenolanibHomo sapiens (human)Kd0.041011
tg100-115Homo sapiens (human)Kd20.000022
cc 401Homo sapiens (human)Kd30.000011
bms 599626Homo sapiens (human)Kd5.927011
exel-7647Homo sapiens (human)Kd65.677011
volasertibHomo sapiens (human)Kd30.000011
pha 665752Homo sapiens (human)Kd1.400011
azd 7762Homo sapiens (human)Kd0.147011
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)Kd15.020522
brivanibHomo sapiens (human)Kd16.550022
mp470Homo sapiens (human)Kd30.000012
rgb 286638Homo sapiens (human)Kd0.535011
np 031112Homo sapiens (human)Kd30.000011
at 7519Homo sapiens (human)Kd20.000022
bms-690514Homo sapiens (human)Kd0.972011
bi 2536Homo sapiens (human)Kd20.000022
inno-406Homo sapiens (human)Kd11.392011
nvp-ast487Homo sapiens (human)Kd0.074011
kw 2449Homo sapiens (human)Kd15.060022
danusertibHomo sapiens (human)Kd30.000012
abt 869Homo sapiens (human)Kd15.600022
azd 8931Homo sapiens (human)Kd30.000011
arq 197Homo sapiens (human)Kd30.000011
azd 1152Homo sapiens (human)Kd0.082011
pf 00299804Homo sapiens (human)Kd30.000011
ridaforolimusHomo sapiens (human)Kd30.000011
ch 4987655Homo sapiens (human)Kd30.484011
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)Kd10.000011
tak 285Homo sapiens (human)Kd30.000011
idelalisibHomo sapiens (human)Kd30.000011
crizotinibHomo sapiens (human)Kd20.000022
osi 906Homo sapiens (human)Kd6.558011
chir-265Homo sapiens (human)Kd15.950022
motesanibHomo sapiens (human)Kd20.000022
fostamatinibHomo sapiens (human)Kd30.000011
trametinibHomo sapiens (human)Kd30.000011
mln8054Homo sapiens (human)Kd20.000022
pf-562,271Homo sapiens (human)Kd30.000011
GDC-0879Homo sapiens (human)Kd5.100011
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)Kd0.203922
nvp-tae684Homo sapiens (human)Kd0.200011
enmd 2076Homo sapiens (human)Kd30.000011
e 7050Homo sapiens (human)Kd2.452011
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)Kd6.797011
gdc-0973Homo sapiens (human)Kd30.000011
buparlisibHomo sapiens (human)Kd30.000011
azd 1480Homo sapiens (human)Kd30.000011
azd8330Homo sapiens (human)Kd2.657011
pha 848125Homo sapiens (human)Kd30.000011
ro5126766Homo sapiens (human)Kd1.996011
fedratinibHomo sapiens (human)Kd15.180022
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)Kd0.000211
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)Kd2.085011
sgi 1776Homo sapiens (human)Kd30.000011
pci 32765Homo sapiens (human)Kd0.243011
ponatinibHomo sapiens (human)Kd2.952011
amg 900Homo sapiens (human)Kd30.000011
mk-1775Homo sapiens (human)Kd30.000011
AMG-208Homo sapiens (human)Kd30.000011
quizartinibHomo sapiens (human)Kd20.000022
at13148Homo sapiens (human)Kd30.000011
tak 733Homo sapiens (human)Kd3.348011
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)Kd2.388011
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)Kd3.576011
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)Kd0.734011
gsk 1363089Homo sapiens (human)Kd0.081222
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)Kd2.294011
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)Kd30.000012
pha 793887Homo sapiens (human)Kd30.000011
sb 1518Homo sapiens (human)Kd30.000011
abemaciclibHomo sapiens (human)Kd30.000011
mk-8776Homo sapiens (human)Kd0.609011
afuresertibHomo sapiens (human)Kd30.000011
gsk 1070916Homo sapiens (human)Kd1.929011
jnj38877605Homo sapiens (human)Kd30.000011
dinaciclibHomo sapiens (human)Kd30.000011
gilteritinibHomo sapiens (human)Kd2.040011
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)Kd30.000012
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)Kd30.000012
at 9283Homo sapiens (human)Kd0.047011
otssp167Homo sapiens (human)Kd0.058011
chir 258Homo sapiens (human)Kd0.815022
osi 027Homo sapiens (human)Kd4.914011
nintedanibHomo sapiens (human)Kd0.090922
bay 80-6946Homo sapiens (human)Kd30.000011
pp242Homo sapiens (human)Kd0.007311

Enables

This protein enables 8 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]
protein tyrosine kinase activitymolecular functionCatalysis of the reaction: ATP + a protein tyrosine = ADP + protein tyrosine phosphate. [RHEA:10596]
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]
MAP kinase kinase activitymolecular functionCatalysis of the concomitant phosphorylation of threonine (T) and tyrosine (Y) residues in a Thr-Glu-Tyr (TEY) thiolester sequence in a MAP kinase (MAPK) substrate. [ISBN:0198547684]

Located In

This protein is located in 1 target(s):

TargetCategoryDefinition
spindlecellular componentThe array of microtubules and associated molecules that forms between opposite poles of a eukaryotic cell during mitosis or meiosis and serves to move the duplicated chromosomes apart. [ISBN:0198547684]

Involved In

This protein is involved in 22 target(s):

TargetCategoryDefinition
negative regulation of transcription by RNA polymerase IIbiological processAny process that stops, prevents, or reduces the frequency, rate or extent of transcription mediated by RNA polymerase II. [GOC:go_curators, GOC:txnOH]
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]
signal transductionbiological processThe cellular process in which a signal is conveyed to trigger a change in the activity or state of a cell. Signal transduction begins with reception of a signal (e.g. a ligand binding to a receptor or receptor activation by a stimulus such as light), or for signal transduction in the absence of ligand, signal-withdrawal or the activity of a constitutively active receptor. Signal transduction ends with regulation of a downstream cellular process, e.g. regulation of transcription or regulation of a metabolic process. Signal transduction covers signaling from receptors located on the surface of the cell and signaling via molecules located within the cell. For signaling between cells, signal transduction is restricted to events at and within the receiving cell. [GOC:go_curators, GOC:mtg_signaling_feb11]
heart developmentbiological processThe process whose specific outcome is the progression of the heart over time, from its formation to the mature structure. The heart is a hollow, muscular organ, which, by contracting rhythmically, keeps up the circulation of the blood. [GOC:jid, UBERON:0000948]
positive regulation of cell growthbiological processAny process that activates or increases the frequency, rate, extent or direction of cell growth. [GOC:go_curators]
negative regulation of NF-kappaB transcription factor activitybiological processAny process that stops, prevents, or reduces the frequency, rate or extent of the activity of the transcription factor NF-kappaB. [GOC:dph, GOC:rl, GOC:tb]
negative regulation of interleukin-8 productionbiological processAny process that stops, prevents, or reduces the frequency, rate, or extent of interleukin-8 production. [GOC:mah]
negative regulation of heterotypic cell-cell adhesionbiological processAny process that stops, prevents, or reduces the frequency, rate, or extent of heterotypic cell-cell adhesion. [GOC:add]
negative regulation of smooth muscle cell apoptotic processbiological processAny process that stops, prevents, or reduces the frequency, rate, or extent of smooth muscle cell apoptotic process. [GOC:BHF, GOC:mtg_apoptosis, GOC:rl]
negative regulation of cysteine-type endopeptidase activity involved in apoptotic processbiological processAny process that stops, prevents, or reduces the frequency, rate or extent of a cysteine-type endopeptidase activity involved in the apoptotic process. [GOC:jl, GOC:mtg_apoptosis]
positive regulation of MAP kinase activitybiological processAny process that activates or increases the frequency, rate or extent of MAP kinase activity. [GOC:dph, GOC:go_curators]
positive regulation of transcription by RNA polymerase IIbiological processAny process that activates or increases the frequency, rate or extent of transcription from an RNA polymerase II promoter. [GOC:go_curators, GOC:txnOH]
insulin-like growth factor receptor signaling pathwaybiological processThe series of molecular signals initiated by a ligand binding to an insulin-like growth factor receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:ceb]
positive regulation of epithelial cell proliferationbiological processAny process that activates or increases the rate or extent of epithelial cell proliferation. [GOC:ai]
positive regulation of protein metabolic processbiological processAny process that activates or increases the frequency, rate or extent of the chemical reactions and pathways involving a protein. [GOC:ai]
negative regulation of response to cytokine stimulusbiological processAny process that decreases the rate, frequency, or extent of a response to cytokine stimulus. [GOC:BHF, GOC:dph, GOC:tb]
ERK5 cascadebiological processA MAPK cascade containing at least the ERK5 MAP kinase (MAPK7; also called BMK1). It starts with the activation of a MAP3K, and the consecutive activation of a MPK2K and of ERK5. 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 ERK5 cascade is activated by stress, mitogens, and by G protein-coupled receptors, and results in cellular responses such as cell growth, cell differentiation and development. [PMID:16376520, PMID:16880823, PMID:20811974, PMID:23125017, PMID:28903453]
cellular response to growth factor stimulusbiological processAny process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a growth factor stimulus. [GOC:mah]
cellular response to laminar fluid shear stressbiological processAny process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a laminar fluid shear stress stimulus. Laminar fluid flow is the force acting on an object in a system where the fluid is moving across a solid surface in parallel layers. [GOC:mah]
negative regulation of cell migration involved in sprouting angiogenesisbiological processAny process that decreases the frequency, rate or extent of cell migration involved in sprouting angiogenesis. Cell migration involved in sprouting angiogenesis is the orderly movement of endothelial cells into the extracellular matrix in order to form new blood vessels contributing to the process of sprouting angiogenesis. [GOC:BHF, GOC:dph, GOC:rl, GOC:tb]
negative regulation of chemokine (C-X-C motif) ligand 2 productionbiological processAny process that stops, prevents or reduces the frequency, rate or extent of chemokine (C-X-C motif) ligand 2 production. [GOC:BHF, GOC:mah]
negative regulation of extrinsic apoptotic signaling pathway in absence of ligandbiological processAny process that stops, prevents or reduces the frequency, rate or extent of extrinsic apoptotic signaling pathway in absence of ligand. [GOC:mtg_apoptosis]