Page last updated: 2024-08-07 18:32:49

Beta-adrenergic receptor kinase 1

A beta-adrenergic receptor kinase 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P25098]

Synonyms

Beta-ARK-1;
EC 2.7.11.15;
G-protein coupled receptor kinase 2

Research

Bioassay Publications (11)

TimeframeStudies on this Protein(%)All Drugs %
pre-19901 (9.09)18.7374
1990's0 (0.00)18.2507
2000's1 (9.09)29.6817
2010's7 (63.64)24.3611
2020's2 (18.18)2.80

Compounds (223)

Drugs with Inhibition Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
nsc 65346Homo sapiens (human)Ki67.000011
paroxetineHomo sapiens (human)IC501.240044
staurosporineHomo sapiens (human)IC501.159522
paroxetine hydrochlorideHomo sapiens (human)IC5011.200022
ophiocordinHomo sapiens (human)IC500.042011

Drugs with Activation Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
racepinephrineHomo sapiens (human)Kd0.610011
fasudilHomo sapiens (human)Kd30.000011
isoproterenolHomo sapiens (human)Kd0.200011
4-(4'-hydroxyphenyl)-amino-6,7-dimethoxyquinazolineHomo sapiens (human)Kd30.000011
metaproterenolHomo sapiens (human)Kd13.000011
imatinibHomo sapiens (human)Kd30.000011
terbutalineHomo sapiens (human)Kd7.400011
deterenolHomo sapiens (human)Kd5.200011
paroxetineHomo sapiens (human)Kd2.980011
triciribine phosphateHomo sapiens (human)Kd30.000011
picropodophyllinHomo sapiens (human)Kd30.000011
gefitinibHomo sapiens (human)Kd30.000011
lestaurtinibHomo sapiens (human)Kd30.000011
perifosineHomo sapiens (human)Kd30.000012
vatalanibHomo sapiens (human)Kd30.000011
ruboxistaurinHomo sapiens (human)Kd30.000011
canertinibHomo sapiens (human)Kd30.000011
cyc 202Homo sapiens (human)Kd30.000011
enzastaurinHomo sapiens (human)Kd30.000011
erlotinibHomo sapiens (human)Kd30.000011
lapatinibHomo sapiens (human)Kd30.000011
sorafenibHomo sapiens (human)Kd30.000011
s 1033Homo sapiens (human)Kd30.000011
xl147Homo sapiens (human)Kd30.000011
bms 387032Homo sapiens (human)Kd30.000011
sf 2370Homo sapiens (human)Kd30.000011
tandutinibHomo sapiens (human)Kd30.000011
dasatinibHomo sapiens (human)Kd30.000011
ha 1100Homo sapiens (human)Kd30.000011
7-epi-hydroxystaurosporineHomo sapiens (human)Kd30.000011
zd 6474Homo sapiens (human)Kd30.000011
imd 0354Homo sapiens (human)Kd30.000011
sirolimusHomo sapiens (human)Kd30.000012
alvocidibHomo sapiens (human)Kd30.000011
bosutinibHomo sapiens (human)Kd30.000011
orantinibHomo sapiens (human)Kd30.000011
su 11248Homo sapiens (human)Kd30.000011
palbociclibHomo sapiens (human)Kd30.000011
vx680Homo sapiens (human)Kd30.000011
cyc 116Homo sapiens (human)Kd30.000011
everolimusHomo sapiens (human)Kd30.000011
ekb 569Homo sapiens (human)Kd30.000011
axitinibHomo sapiens (human)Kd30.000011
temsirolimusHomo sapiens (human)Kd30.000011
on 01910Homo sapiens (human)Kd30.000012
av 412Homo sapiens (human)Kd30.000011
telatinibHomo sapiens (human)Kd30.000011
y-39983Homo sapiens (human)Kd30.000011
cp 547632Homo sapiens (human)Kd30.000011
lenvatinibHomo sapiens (human)Kd30.000011
pd 0325901Homo sapiens (human)Kd30.000011
midostaurinHomo sapiens (human)Kd30.000011
px-866Homo sapiens (human)Kd30.000011
ripasudilHomo sapiens (human)Kd30.000011
osi 930Homo sapiens (human)Kd30.000011
scio-469Homo sapiens (human)Kd30.000011
cp 724714Homo sapiens (human)Kd30.000011
hmn-214Homo sapiens (human)Kd30.000011
tivozanibHomo sapiens (human)Kd30.000011
hki 272Homo sapiens (human)Kd30.000011
tofacitinibHomo sapiens (human)Kd30.000011
cediranibHomo sapiens (human)Kd30.000011
masitinibHomo sapiens (human)Kd30.000011
ly-2157299Homo sapiens (human)Kd30.000011
pazopanibHomo sapiens (human)Kd30.000011
azd 6244Homo sapiens (human)Kd30.000011
su 14813Homo sapiens (human)Kd30.000011
bibw 2992Homo sapiens (human)Kd30.000011
binimetinibHomo sapiens (human)Kd30.000011
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)Kd30.000011
tg100-115Homo sapiens (human)Kd30.000011
cc 401Homo sapiens (human)Kd30.000011
bms 599626Homo sapiens (human)Kd30.000011
exel-7647Homo sapiens (human)Kd30.000011
volasertibHomo sapiens (human)Kd30.000011
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)Kd30.000011
brivanibHomo sapiens (human)Kd30.000011
mp470Homo sapiens (human)Kd30.000011
rgb 286638Homo sapiens (human)Kd30.000011
np 031112Homo sapiens (human)Kd30.000011
at 7519Homo sapiens (human)Kd30.000011
bms-690514Homo sapiens (human)Kd30.000011
bi 2536Homo sapiens (human)Kd30.000011
inno-406Homo sapiens (human)Kd30.000011
kw 2449Homo sapiens (human)Kd30.000011
danusertibHomo sapiens (human)Kd30.000011
abt 869Homo sapiens (human)Kd30.000011
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
tak 285Homo sapiens (human)Kd30.000011
idelalisibHomo sapiens (human)Kd30.000011
crizotinibHomo sapiens (human)Kd30.000011
osi 906Homo sapiens (human)Kd30.000011
chir-265Homo sapiens (human)Kd30.000011
motesanibHomo sapiens (human)Kd30.000012
fostamatinibHomo sapiens (human)Kd30.000011
trametinibHomo sapiens (human)Kd30.000011
mln8054Homo sapiens (human)Kd30.000012
pf-562,271Homo sapiens (human)Kd30.000011
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)Kd30.000011
azd 1152-hqpaHomo sapiens (human)Kd30.000011
enmd 2076Homo sapiens (human)Kd30.000011
e 7050Homo sapiens (human)Kd30.000012
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)Kd30.000011
ro5126766Homo sapiens (human)Kd30.000011
fedratinibHomo sapiens (human)Kd30.000011
gsk690693Homo sapiens (human)Kd30.000011
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)Kd30.000011
icotinibHomo sapiens (human)Kd30.000011
ph 797804Homo sapiens (human)Kd30.000011
kx-01Homo sapiens (human)Kd30.000011
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)Kd30.000011
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)Kd30.000011
AMG-208Homo sapiens (human)Kd30.000011
quizartinibHomo sapiens (human)Kd30.000011
at13148Homo sapiens (human)Kd0.170011
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)Kd30.000011
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
pf 3758309Homo sapiens (human)Kd22.494011
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)Kd30.000011
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)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)Kd30.000012
mk-8776Homo sapiens (human)Kd30.000011
afuresertibHomo sapiens (human)Kd30.000011
gsk 1070916Homo sapiens (human)Kd30.000011
jnj38877605Homo sapiens (human)Kd30.000011
dinaciclibHomo sapiens (human)Kd30.000011
gilteritinibHomo sapiens (human)Kd30.000011
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)Kd30.000011
otssp167Homo sapiens (human)Kd30.000012
chir 258Homo sapiens (human)Kd30.000011
osi 027Homo sapiens (human)Kd30.000011
nintedanibHomo sapiens (human)Kd30.000011
bay 80-6946Homo sapiens (human)Kd30.000011

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]
G protein-coupled receptor kinase activitymolecular functionCatalysis of the reaction: ATP + G protein-coupled receptor = ADP + G protein-coupled receptor phosphate. [GOC:dph]
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]
alpha-2A adrenergic receptor bindingmolecular functionBinding to an alpha-2A adrenergic receptor. [GOC:mah, GOC:nln]
Edg-2 lysophosphatidic acid receptor bindingmolecular functionBinding to an Edg-2 lysophosphatidic acid receptor. [GOC:mah, GOC:nln]
beta-adrenergic receptor kinase activitymolecular functionCatalysis of the reaction: ATP + beta-adrenergic receptor = ADP + phospho-beta-adrenergic receptor. [EC:2.7.11.15, MetaCyc:BETA-ADRENERGIC-RECEPTOR-KINASE-RXN]
G protein-coupled receptor bindingmolecular functionBinding to a G protein-coupled receptor. [GOC:ceb, GOC:dph]

Located In

This protein is located in 7 target(s):

TargetCategoryDefinition
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]
plasma membranecellular componentThe membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363]
ciliumcellular componentA specialized eukaryotic organelle that consists of a filiform extrusion of the cell surface and of some cytoplasmic parts. Each cilium is largely bounded by an extrusion of the cytoplasmic (plasma) membrane, and contains a regular longitudinal array of microtubules, anchored to a basal body. [GOC:cilia, GOC:curators, GOC:kmv, GOC:vw, ISBN:0198547684, PMID:16824949, PMID:17009929, PMID:20144998]
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]
presynapsecellular componentThe part of a synapse that is part of the presynaptic cell. [GOC:dos]
postsynapsecellular componentThe part of a synapse that is part of the post-synaptic cell. [GOC:dos]

Involved In

This protein is involved in 16 target(s):

TargetCategoryDefinition
desensitization of G protein-coupled receptor signaling pathwaybiological processThe process that stops, prevents, or reduces the frequency, rate or extent of G protein-coupled receptor signaling pathway after prolonged stimulation with an agonist of the pathway. [PMID:8396717]
negative regulation of the force of heart contraction by chemical signalbiological processAny process which decreases the force of heart muscle contraction mediated by chemical signaling, hormonal, autocrine or paracrine. [GOC:mtg_cardio]
G protein-coupled receptor signaling pathwaybiological processThe series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor]
G protein-coupled acetylcholine receptor signaling pathwaybiological processA G protein-coupled receptor signaling pathway initiated by a ligand binding to an acetylcholine receptor on the surface of a target cell, and ends with regulation of a downstream cellular process, e.g. transcription. [GOC:mah, ISBN:0815316194]
tachykinin receptor signaling pathwaybiological processA G protein-coupled receptor signaling pathway initiated by tachykinin binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process. Tachykinin is a short peptide with the terminal sequence (Phe-X-Gly-Leu-Met-NH2). [GOC:mah, PMID:14723970]
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]
peptidyl-serine phosphorylationbiological processThe phosphorylation of peptidyl-serine to form peptidyl-O-phospho-L-serine. [RESID:AA0037]
viral genome replicationbiological processAny process involved directly in viral genome replication, including viral nucleotide metabolism. [ISBN:0781702534]
receptor internalizationbiological processA receptor-mediated endocytosis process that results in the movement of receptors from the plasma membrane to the inside of the cell. The process begins when cell surface receptors are monoubiquitinated following ligand-induced activation. Receptors are subsequently taken up into endocytic vesicles from where they are either targeted to the lysosome or vacuole for degradation or recycled back to the plasma membrane. [GOC:bf, GOC:mah, GOC:signaling, PMID:15006537, PMID:19643732]
positive regulation of catecholamine secretionbiological processAny process that activates or increases the frequency, rate or extent of the regulated release of a catecholamine. [GOC:mah]
negative regulation of striated muscle contractionbiological processAny process that stops, prevents, or reduces the frequency, rate or extent of striated muscle contraction. [GOC:go_curators]
symbiont entry into host cellbiological processThe process by which a symbiont breaches the plasma membrane or cell envelope and enters the host cell. The process ends when the symbiont or its genome is released into the host cell. [GOC:jl]
cardiac muscle contractionbiological processMuscle contraction of cardiac muscle tissue. [GOC:dph]
negative regulation of relaxation of smooth musclebiological processAny process that stops, prevents or reduces the frequency, rate or extent of relaxation of smooth muscle. [GOC:TermGenie]
regulation of the force of heart contractionbiological processAny process that modulates the extent of heart contraction, changing the force with which blood is propelled. [GOC:dph, GOC:tb, PMID:10358008]
protein phosphorylationbiological processThe process of introducing a phosphate group on to a protein. [GOC:hb]