Page last updated: 2024-08-07 18:40:39

Activated CDC42 kinase 1

An activated CDC42 kinase 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q07912]

Synonyms

ACK-1;
EC 2.7.10.2;
EC 2.7.11.1;
Tyrosine kinase non-receptor protein 2

Research

Bioassay Publications (19)

TimeframeStudies on this Protein(%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's3 (15.79)29.6817
2010's15 (78.95)24.3611
2020's1 (5.26)2.80

Compounds (244)

Drugs with Inhibition Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
staurosporineHomo sapiens (human)IC500.029822
dasatinibHomo sapiens (human)Ki0.010011
bosutinibHomo sapiens (human)IC500.002722
sc1 compoundHomo sapiens (human)IC500.009011
entrectinibHomo sapiens (human)IC500.070011
1-[3-methoxy-4-[[4-(2-propan-2-ylsulfonylanilino)-1H-pyrrolo[2,3-b]pyridin-6-yl]amino]phenyl]-4-piperidinolHomo sapiens (human)IC503.100010
Mps1-IN-2Homo sapiens (human)IC500.145011
nms p937Homo sapiens (human)IC5010.000011
nms-p118Homo sapiens (human)IC5010.000011
cep-28122Homo sapiens (human)IC500.041011
pf-543Homo sapiens (human)IC5010.000011
pf-06463922Homo sapiens (human)IC500.017011
pf-06463922Homo sapiens (human)Ki0.017010
nms-e973Homo sapiens (human)IC500.010011

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)Kd0.016333
picropodophyllinHomo sapiens (human)Kd30.000011
gefitinibHomo sapiens (human)Kd16.666733
lestaurtinibHomo sapiens (human)Kd0.035322
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)Kd16.666733
pd 173955Homo sapiens (human)Kd0.027011
s 1033Homo sapiens (human)Kd20.000022
xl147Homo sapiens (human)Kd30.000011
bms 387032Homo sapiens (human)Kd16.666733
sf 2370Homo sapiens (human)Kd1.717011
tandutinibHomo sapiens (human)Kd16.666733
vx-745Homo sapiens (human)Kd10.000022
dasatinibHomo sapiens (human)Kd0.011044
ha 1100Homo sapiens (human)Kd30.000011
7-epi-hydroxystaurosporineHomo sapiens (human)Kd0.162011
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)Kd20.000034
bosutinibHomo sapiens (human)Kd0.083522
orantinibHomo sapiens (human)Kd30.000011
su 11248Homo sapiens (human)Kd12.500044
palbociclibHomo sapiens (human)Kd30.000012
jnj-7706621Homo sapiens (human)Kd10.000011
vx680Homo sapiens (human)Kd12.933333
cyc 116Homo sapiens (human)Kd30.000011
everolimusHomo sapiens (human)Kd30.000011
ekb 569Homo sapiens (human)Kd12.030033
axitinibHomo sapiens (human)Kd18.000022
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)Kd0.181033
px-866Homo sapiens (human)Kd30.000011
ripasudilHomo sapiens (human)Kd30.000011
osi 930Homo sapiens (human)Kd30.000012
ki 20227Homo sapiens (human)Kd0.250011
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)Kd15.340022
tofacitinibHomo sapiens (human)Kd7.020733
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)Kd13.266733
bibw 2992Homo sapiens (human)Kd20.000022
binimetinibHomo sapiens (human)Kd30.000011
sotrastaurinHomo sapiens (human)Kd30.000011
aee 788Homo sapiens (human)Kd1.006011
saracatinibHomo sapiens (human)Kd4.650011
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)Kd30.000012
exel-7647Homo sapiens (human)Kd30.000011
volasertibHomo sapiens (human)Kd30.000011
pha 665752Homo sapiens (human)Kd10.000011
azd 7762Homo sapiens (human)Kd1.091011
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)Kd15.035022
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)Kd0.216522
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)Kd0.059011
abt 869Homo sapiens (human)Kd20.000034
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)Kd15.380022
osi 906Homo sapiens (human)Kd30.000011
chir-265Homo sapiens (human)Kd16.666733
motesanibHomo sapiens (human)Kd16.666733
fostamatinibHomo sapiens (human)Kd30.000011
trametinibHomo sapiens (human)Kd30.000012
mln8054Homo sapiens (human)Kd16.666733
pf-562,271Homo sapiens (human)Kd30.000011
GDC-0879Homo sapiens (human)Kd10.000011
jnj-26483327Homo sapiens (human)Kd30.000012
ly2603618Homo sapiens (human)Kd30.000011
tg100801Homo sapiens (human)Kd30.000011
dactolisibHomo sapiens (human)Kd30.000012
bgt226Homo sapiens (human)Kd30.000011
gsk 461364Homo sapiens (human)Kd20.000022
azd 1152-hqpaHomo sapiens (human)Kd20.000034
nvp-tae684Homo sapiens (human)Kd0.002011
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)Kd0.281011
gdc-0973Homo sapiens (human)Kd30.000011
buparlisibHomo sapiens (human)Kd30.000011
azd 1480Homo sapiens (human)Kd0.515011
azd8330Homo sapiens (human)Kd30.000011
pha 848125Homo sapiens (human)Kd0.900011
ro5126766Homo sapiens (human)Kd30.000011
fedratinibHomo sapiens (human)Kd0.741522
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)Kd1.100011
mk 5108Homo sapiens (human)Kd0.473011
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)Kd30.000011
AMG-208Homo sapiens (human)Kd30.000011
quizartinibHomo sapiens (human)Kd20.000022
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)Kd30.000011
cabozantinibHomo sapiens (human)Kd30.000011
defactinibHomo sapiens (human)Kd30.000011
ly2584702Homo sapiens (human)Kd30.000011
incb-018424Homo sapiens (human)Kd2.098522
poziotinibHomo sapiens (human)Kd30.000011
asp3026Homo sapiens (human)Kd0.005011
entrectinibHomo sapiens (human)Kd0.420011
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)Kd30.000011
plx4032Homo sapiens (human)Kd30.000011
gsk 1363089Homo sapiens (human)Kd15.100022
arry-334543Homo sapiens (human)Kd30.000012
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)Kd30.000012
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)Kd9.334011
abemaciclibHomo sapiens (human)Kd30.000011
mk-8776Homo sapiens (human)Kd30.000011
afuresertibHomo sapiens (human)Kd30.000011
xmd 8-92Homo sapiens (human)Kd0.080011
gsk 1070916Homo sapiens (human)Kd30.000011
jnj38877605Homo sapiens (human)Kd30.000011
dinaciclibHomo sapiens (human)Kd30.000011
gilteritinibHomo sapiens (human)Kd3.149011
alectinibHomo sapiens (human)Kd30.000011
glpg0634Homo sapiens (human)Kd30.000011
encorafenibHomo sapiens (human)Kd30.000011
bms-911543Homo sapiens (human)Kd30.000012
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)Kd0.929011
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)Kd30.000011
chir 258Homo sapiens (human)Kd16.666733
osi 027Homo sapiens (human)Kd30.000011
nintedanibHomo sapiens (human)Kd15.800022
bay 80-6946Homo sapiens (human)Kd30.000011
pp242Homo sapiens (human)Kd9.600011

Enables

This protein enables 13 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 serine/threonine/tyrosine kinase activitymolecular functionCatalysis of the reactions: ATP + a protein serine = ADP + protein serine phosphate; ATP + a protein threonine = ADP + protein threonine phosphate; and ATP + a protein tyrosine = ADP + protein tyrosine phosphate. [GOC:mah]
protein tyrosine kinase activitymolecular functionCatalysis of the reaction: ATP + a protein tyrosine = ADP + protein tyrosine phosphate. [RHEA:10596]
non-membrane spanning protein tyrosine kinase activitymolecular functionCatalysis of the reaction: ATP + protein L-tyrosine = ADP + protein L-tyrosine phosphate by a non-membrane spanning protein. [EC:2.7.10.2]
GTPase inhibitor activitymolecular functionStops, prevents or reduces the activity of any enzyme that catalyzes the hydrolysis of GTP to GDP and orthophosphate. [GOC:ai]
epidermal growth factor receptor bindingmolecular functionBinding to an epidermal growth factor receptor. [GOC:ai]
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]
ubiquitin protein ligase bindingmolecular functionBinding to a ubiquitin protein ligase enzyme, any of the E3 proteins. [GOC:vp]
identical protein bindingmolecular functionBinding to an identical protein or proteins. [GOC:jl]
metal ion bindingmolecular functionBinding to a metal ion. [GOC:ai]
WW domain bindingmolecular functionBinding to a WW domain of a protein, a small module composed of 40 amino acids and plays a role in mediating protein-protein interactions via proline-rich regions. [PMID:14531730]
protein serine kinase activitymolecular functionCatalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate. [RHEA:17989]

Located In

This protein is located in 13 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]
cytoplasmcellular componentThe contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684]
endosomecellular componentA vacuole to which materials ingested by endocytosis are delivered. [ISBN:0198506732, PMID:19696797]
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]
clathrin-coated pitcellular componentA part of the endomembrane system in the form of an invagination of a membrane upon which a clathrin coat forms, and that can be converted by vesicle budding into a clathrin-coated vesicle. Coated pits form on the plasma membrane, where they are involved in receptor-mediated selective transport of many proteins and other macromolecules across the cell membrane, in the trans-Golgi network, and on some endosomes. [GOC:mah, ISBN:0198506732, NIF_Subcellular:sao1969557946, PMID:10559856, PMID:17284835]
adherens junctioncellular componentA cell-cell junction composed of the epithelial cadherin-catenin complex. The epithelial cadherins, or E-cadherins, of each interacting cell extend through the plasma membrane into the extracellular space and bind to each other. The E-cadherins bind to catenins on the cytoplasmic side of the membrane, where the E-cadherin-catenin complex binds to cytoskeletal components and regulatory and signaling molecules. [GOC:aruk, GOC:bc, GOC:mah, ISBN:0198506732, PMID:17854762, PMID:20571587, PMID:21422226, PMID:28096264]
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]
clathrin-coated vesiclecellular componentA vesicle with a coat formed of clathrin connected to the membrane via one of the clathrin adaptor complexes. [GOC:mah, PMID:11252894]
cytoplasmic vesicle membranecellular componentThe lipid bilayer surrounding a cytoplasmic vesicle. [GOC:mah]
intracellular membrane-bounded organellecellular componentOrganized structure of distinctive morphology and function, bounded by a single or double lipid bilayer membrane and occurring within the cell. Includes the nucleus, mitochondria, plastids, vacuoles, and vesicles. Excludes the plasma membrane. [GOC:go_curators]
perinuclear region of cytoplasmcellular componentCytoplasm situated near, or occurring around, the nucleus. [GOC:jid]
cytoophidiumcellular componentA subcellular filamentary structure where CTP synthase is compartmentalized in a range of organisms including bacteria, yeast, fruit fly, rat and human. [GOC:mag, PMID:20513629, PMID:21930098, Wikipedia:CTP_synthase#Cytoophidium]

Active In

This protein is active in 1 target(s):

TargetCategoryDefinition
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]

Part Of

This protein is part of 1 target(s):

TargetCategoryDefinition
Grb2-EGFR complexcellular componentA protein complex that contains the epidermal growth factor receptor (EGFR) and Grb2, and is involved in linking EGFR activation to the p21-Ras pathway. [GOC:mah, PMID:7798267]

Involved In

This protein is involved in 7 target(s):

TargetCategoryDefinition
endocytosisbiological processA vesicle-mediated transport process in which cells take up external materials or membrane constituents by the invagination of a part of the plasma membrane to form a new membrane-bounded vesicle. [GOC:mah, ISBN:0198506732, ISBN:0716731363, Wikipedia:Endocytosis]
cell surface receptor signaling pathwaybiological processThe series of molecular signals initiated by an extracellular ligand binding to a receptor located on the cell surface. The pathway ends with regulation of a downstream cellular process, e.g. transcription. [GOC:signaling]
small GTPase-mediated signal transductionbiological processAn intracellular signaling cassette in which a small monomeric GTPase relays a signal. [GOC:mah]
phosphorylationbiological processThe process of introducing a phosphate group into a molecule, usually with the formation of a phosphoric ester, a phosphoric anhydride or a phosphoric amide. [ISBN:0198506732]
positive regulation of peptidyl-tyrosine phosphorylationbiological processAny process that activates or increases the frequency, rate or extent of the phosphorylation of peptidyl-tyrosine. [GOC:ai]
regulation of clathrin-dependent endocytosisbiological processAny process that modulates the frequency, rate or extent of clathrin-mediated endocytosis. [GOC:mah]
protein phosphorylationbiological processThe process of introducing a phosphate group on to a protein. [GOC:hb]