Page last updated: 2024-08-07 17:07:00

Inhibitor of nuclear factor kappa-B kinase subunit epsilon

An inhibitor of nuclear factor kappa-B kinase subunit epsilon that is encoded in the genome of human. [PMID:10882136, PMID:17327220, PRO:CNA, UniProtKB:Q14164]

Synonyms

I-kappa-B kinase epsilon;
IKK-E;
IKK-epsilon;
IkBKE;
EC 2.7.11.10;
Inducible I kappa-B kinase;
IKK-i

Research

Bioassay Publications (17)

TimeframeStudies on this Protein(%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's7 (41.18)29.6817
2010's8 (47.06)24.3611
2020's2 (11.76)2.80

Compounds (239)

Drugs with Inhibition Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
amlexanoxHomo sapiens (human)IC505.114312
staurosporineHomo sapiens (human)IC500.000322
imd 0354Homo sapiens (human)IC50100.000011
ps1145Homo sapiens (human)IC50100.000011
bx795Homo sapiens (human)IC500.029522
danusertibHomo sapiens (human)IC5010.000011
5-(5,6-dimethoxy-1-benzimidazolyl)-3-[(2-methylsulfonylphenyl)methoxy]-2-thiophenecarbonitrileHomo sapiens (human)IC505.381146
4-[2-(2-chloro-4-fluoroanilino)-5-methyl-4-pyrimidinyl]-N-[(1S)-1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamideHomo sapiens (human)Ki5.000011
pha 848125Homo sapiens (human)IC5010.000011
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)IC501.064011

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)Kd0.005122
picropodophyllinHomo sapiens (human)Kd30.000011
gefitinibHomo sapiens (human)Kd16.666733
lestaurtinibHomo sapiens (human)Kd0.221333
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)Kd10.000011
s 1033Homo sapiens (human)Kd20.000022
xl147Homo sapiens (human)Kd30.000011
bms 387032Homo sapiens (human)Kd16.666733
sf 2370Homo sapiens (human)Kd0.494011
tandutinibHomo sapiens (human)Kd15.000044
vx-745Homo sapiens (human)Kd10.000022
dasatinibHomo sapiens (human)Kd16.666733
ha 1100Homo sapiens (human)Kd30.000012
7-epi-hydroxystaurosporineHomo sapiens (human)Kd0.528011
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)Kd12.066733
bosutinibHomo sapiens (human)Kd0.445522
orantinibHomo sapiens (human)Kd1.430011
su 11248Homo sapiens (human)Kd0.897844
palbociclibHomo sapiens (human)Kd30.000011
jnj-7706621Homo sapiens (human)Kd8.300011
vx680Homo sapiens (human)Kd11.733333
cyc 116Homo sapiens (human)Kd0.689011
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)Kd0.230844
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)Kd20.000022
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)Kd0.998033
bibw 2992Homo sapiens (human)Kd20.000022
binimetinibHomo sapiens (human)Kd30.000011
sotrastaurinHomo sapiens (human)Kd30.000011
aee 788Homo sapiens (human)Kd30.000011
saracatinibHomo sapiens (human)Kd30.000012
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)Kd0.700011
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)Kd0.094522
brivanibHomo sapiens (human)Kd20.000022
mp470Homo sapiens (human)Kd30.000012
rgb 286638Homo sapiens (human)Kd1.902011
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)Kd30.000012
nvp-ast487Homo sapiens (human)Kd10.000022
kw 2449Homo sapiens (human)Kd1.480022
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)Kd1.719022
osi 906Homo sapiens (human)Kd30.000011
chir-265Homo sapiens (human)Kd16.666733
motesanibHomo sapiens (human)Kd16.666733
fostamatinibHomo sapiens (human)Kd1.320011
trametinibHomo sapiens (human)Kd30.000011
mln8054Homo sapiens (human)Kd16.666733
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)Kd20.000034
nvp-tae684Homo sapiens (human)Kd1.100011
enmd 2076Homo sapiens (human)Kd30.000012
e 7050Homo 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)Kd30.000012
pha 848125Homo sapiens (human)Kd2.966011
ro5126766Homo sapiens (human)Kd30.000011
fedratinibHomo sapiens (human)Kd1.312022
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)Kd30.000011
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)Kd2.057011
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)Kd30.000012
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)Kd0.200011
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)Kd15.600022
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)Kd0.658011
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)Kd15.700022
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)Kd30.000011
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)Kd0.715011
abemaciclibHomo sapiens (human)Kd30.000011
mk-8776Homo sapiens (human)Kd30.000011
afuresertibHomo sapiens (human)Kd30.000011
gsk 1070916Homo sapiens (human)Kd0.992011
jnj38877605Homo sapiens (human)Kd30.000011
dinaciclibHomo sapiens (human)Kd30.000011
gilteritinibHomo sapiens (human)Kd1.468011
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)Kd30.000012
byl719Homo sapiens (human)Kd30.000011
cep-32496Homo sapiens (human)Kd30.000011
rociletinibHomo sapiens (human)Kd30.000011
ceritinibHomo sapiens (human)Kd30.000011
azd1208Homo sapiens (human)Kd30.000012
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)Kd0.215011
otssp167Homo sapiens (human)Kd0.182011
chir 258Homo sapiens (human)Kd0.823333
osi 027Homo sapiens (human)Kd30.000011
nintedanibHomo sapiens (human)Kd0.171522
bay 80-6946Homo sapiens (human)Kd30.000011
pp242Homo sapiens (human)Kd10.000011

Enables

This protein enables 8 target(s):

TargetCategoryDefinition
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]
IkappaB kinase activitymolecular functionCatalysis of the reaction: ATP + IkappaB protein = ADP + IkappaB phosphoprotein. [EC:2.7.11.10]
protein phosphatase bindingmolecular functionBinding to a protein phosphatase. [GOC:jl]
ubiquitin protein ligase bindingmolecular functionBinding to a ubiquitin protein ligase enzyme, any of the E3 proteins. [GOC:vp]
K48-linked polyubiquitin modification-dependent protein bindingmolecular functionBinding to a protein upon poly-ubiquitination formed by linkages between lysine residues at position 48 in the target protein. [GOC:al, PMID:20739285]
identical protein bindingmolecular functionBinding to an identical protein or proteins. [GOC:jl]

Located In

This protein is located in 6 target(s):

TargetCategoryDefinition
nucleuscellular componentA membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators]
nucleoplasmcellular componentThat part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653]
cytoplasmcellular componentThe contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [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]
PML bodycellular componentA class of nuclear body; they react against SP100 auto-antibodies (PML, promyelocytic leukemia); cells typically contain 10-30 PML bodies per nucleus; alterations in the localization of PML bodies occurs after viral infection. [GOC:ma, PMID:10944585]
mitochondrial membranecellular componentEither of the lipid bilayers that surround the mitochondrion and form the mitochondrial envelope. [GOC:mah, NIF_Subcellular:sao1045389829]

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]

Part Of

This protein is part of 1 target(s):

TargetCategoryDefinition
serine/threonine protein kinase complexcellular componentA protein complex which is capable of protein serine/threonine kinase activity. [GOC:bhm, GOC:TermGenie, PMID:18191223]

Involved In

This protein is involved in 16 target(s):

TargetCategoryDefinition
immune responsebiological processAny immune system process that functions in the calibrated response of an organism to a potential internal or invasive threat. [GO_REF:0000022, GOC:add]
intrinsic apoptotic signaling pathway in response to DNA damagebiological processThe series of molecular signals in which an intracellular signal is conveyed to trigger the apoptotic death of a cell. The pathway is induced by the detection of DNA damage, and ends when the execution phase of apoptosis is triggered. [GOC:go_curators, GOC:mtg_apoptosis]
gene expressionbiological processThe process in which a gene's sequence is converted into a mature gene product (protein or RNA). This includes the production of an RNA transcript and its processing, as well as translation and maturation for protein-coding genes. [GOC:txnOH-2018, PMID:25934543, PMID:31580950]
positive regulation of lipid storagebiological processAny process that increases the rate, frequency or extent of lipid storage. Lipid storage is the accumulation and maintenance in cells or tissues of lipids, compounds soluble in organic solvents but insoluble or sparingly soluble in aqueous solvents. Lipid reserves can be accumulated during early developmental stages for mobilization and utilization at later stages of development. [GOC:BHF, GOC:dph, GOC:tb]
positive regulation of type I interferon productionbiological processAny process that activates or increases the frequency, rate, or extent of type I interferon production. Type I interferons include the interferon-alpha, beta, delta, episilon, zeta, kappa, tau, and omega gene families. [GOC:add, GOC:mah]
response to interferon-betabiological 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 an interferon-beta stimulus. Interferon-beta is a type I interferon. [GOC:sl, PMID:9561374]
positive regulation of canonical NF-kappaB signal transductionbiological processAny process that activates or increases the frequency, rate or extent of a canonical NF-kappaB signaling cascade. [GOC:jl]
regulation of protein-containing complex assemblybiological processAny process that modulates the frequency, rate or extent of protein complex assembly. [GOC:jl]
mRNA stabilizationbiological processPrevention of degradation of mRNA molecules. In the absence of compensating changes in other processes, the slowing of mRNA degradation can result in an overall increase in the population of active mRNA molecules. [GOC:jid]
positive regulation of DNA-binding transcription factor activitybiological processAny process that activates or increases the frequency, rate or extent of activity of a transcription factor, any factor involved in the initiation or regulation of transcription. [GOC:ai]
defense response to virusbiological processReactions triggered in response to the presence of a virus that act to protect the cell or organism. [GOC:ai]
type I interferon-mediated signaling pathwaybiological processThe series of molecular signals initiated by type I interferon binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. Type I interferons include the interferon-alpha, beta, delta, episilon, zeta, kappa, tau, and omega gene families. [GOC:add, GOC:dph, GOC:signaling, PMID:32464097]
positive regulation of type I interferon-mediated signaling pathwaybiological processAny process that increases the rate, frequency or extent of a type I interferon-mediated signaling pathway. [GOC:dph]
interleukin-17-mediated signaling pathwaybiological processThe series of molecular signals initiated by interleukin-17 binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:ic, PMID:21602493]
cellular response to virusbiological 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 stimulus from a virus. [GOC:dos]
peptidyl-serine phosphorylationbiological processThe phosphorylation of peptidyl-serine to form peptidyl-O-phospho-L-serine. [RESID:AA0037]