Page last updated: 2024-08-07 12:46:15
Serine/threonine-protein kinase PAK 3
A serine/threonine-protein kinase PAK 3 that is encoded in the genome of human. [PRO:DNx, UniProtKB:O75914]
Synonyms
EC 2.7.11.1;
Beta-PAK;
Oligophrenin-3;
p21-activated kinase 3;
PAK-3
Research
Bioassay Publications (10)
Timeframe | Studies on this Protein(%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 3 (30.00) | 29.6817 |
2010's | 6 (60.00) | 24.3611 |
2020's | 1 (10.00) | 2.80 |
Compounds (78)
Drugs with Inhibition Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
---|---|---|---|---|---|
staurosporine | Homo sapiens (human) | IC50 | 0.0003 | 2 | 2 |
birb 796 | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
pf 3758309 | Homo sapiens (human) | IC50 | 0.0990 | 1 | 1 |
frax486 | Homo sapiens (human) | IC50 | 0.0553 | 1 | 1 |
frax597 | Homo sapiens (human) | IC50 | 1.6803 | 3 | 6 |
Drugs with Activation Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
---|---|---|---|---|---|
sb 202190 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
imatinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
staurosporine | Homo sapiens (human) | Kd | 0.0049 | 3 | 3 |
gefitinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
lestaurtinib | Homo sapiens (human) | Kd | 0.0350 | 2 | 2 |
vatalanib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
ruboxistaurin | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
canertinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
birb 796 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
cyc 202 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
sb 203580 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
enzastaurin | Homo sapiens (human) | Kd | 4.3000 | 1 | 1 |
erlotinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
lapatinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
sorafenib | Homo sapiens (human) | Kd | 10.0000 | 3 | 3 |
pd 173955 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
s 1033 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
bms 387032 | Homo sapiens (human) | Kd | 3.5000 | 2 | 2 |
tandutinib | Homo sapiens (human) | Kd | 10.0000 | 3 | 3 |
vx-745 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
dasatinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
zd 6474 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1h-imidazol-2-yl)benzamide | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
alvocidib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
bosutinib | Homo sapiens (human) | Kd | 5.7000 | 1 | 1 |
su 11248 | Homo sapiens (human) | Kd | 0.0160 | 3 | 3 |
jnj-7706621 | Homo sapiens (human) | Kd | 2.1000 | 1 | 1 |
vx680 | Homo sapiens (human) | Kd | 3.3000 | 2 | 2 |
ekb 569 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
axitinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
pd 184352 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
bms345541 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
midostaurin | Homo sapiens (human) | Kd | 1.2200 | 3 | 3 |
ki 20227 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
cp 724714 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
pi103 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
hki 272 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
tofacitinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
n-(6-chloro-7-methoxy-9h-beta-carbolin-8-yl)-2-methylnicotinamide | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
cediranib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
masitinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
pazopanib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
azd 6244 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
su 14813 | Homo sapiens (human) | Kd | 0.1900 | 2 | 2 |
bibw 2992 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
tg100-115 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
pha 665752 | Homo sapiens (human) | Kd | 1.1000 | 1 | 1 |
6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)-4-pyrimidinyl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one | Homo sapiens (human) | Kd | 0.6900 | 1 | 1 |
brivanib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
at 7519 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
bi 2536 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
nvp-ast487 | Homo sapiens (human) | Kd | 7.0000 | 2 | 2 |
kw 2449 | Homo sapiens (human) | Kd | 0.4600 | 1 | 1 |
abt 869 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
gw 2580 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
crizotinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
chir-265 | Homo sapiens (human) | Kd | 5.3850 | 2 | 2 |
motesanib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
mln8054 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
GDC-0879 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
gsk 461364 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
azd 1152-hqpa | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
nvp-tae684 | Homo sapiens (human) | Kd | 0.0290 | 1 | 1 |
fedratinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
gsk690693 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
gdc 0941 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
plx 4720 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
sgx 523 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
quizartinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
incb-018424 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
gsk 1838705a | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
gsk 1363089 | Homo sapiens (human) | Kd | 4.1000 | 1 | 1 |
chir 258 | Homo sapiens (human) | Kd | 5.3850 | 2 | 2 |
nintedanib | Homo sapiens (human) | Kd | 0.2100 | 1 | 1 |
pp242 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
Enables
This protein enables 8 target(s):
Target | Category | Definition |
---|---|---|
protein serine/threonine kinase activity | molecular function | Catalysis 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] |
MAP kinase kinase activity | molecular function | Catalysis 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] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
ATP binding | molecular function | Binding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732] |
SH3 domain binding | molecular function | Binding to a SH3 domain (Src homology 3) of a protein, small protein modules containing approximately 50 amino acid residues found in a great variety of intracellular or membrane-associated proteins. [GOC:go_curators, Pfam:PF00018] |
small GTPase binding | molecular function | Binding to a small monomeric GTPase. [GOC:mah, PMID:27218782] |
metal ion binding | molecular function | Binding to a metal ion. [GOC:ai] |
protein serine kinase activity | molecular function | Catalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate. [RHEA:17989] |
Located In
This protein is located in 4 target(s):
Target | Category | Definition |
---|---|---|
cytosol | cellular component | The 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 membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
postsynaptic density | cellular component | An electron dense network of proteins within and adjacent to the postsynaptic membrane of an asymmetric, neuron-neuron synapse. Its major components include neurotransmitter receptors and the proteins that spatially and functionally organize them such as anchoring and scaffolding molecules, signaling enzymes and cytoskeletal components. [GOC:BHF, GOC:dos, GOC:ef, GOC:jid, GOC:pr, GOC:sjp, http://molneuro.kaist.ac.kr/psd, PMID:14532281, Wikipedia:Postsynaptic_density] |
glutamatergic synapse | cellular component | A synapse that uses glutamate as a neurotransmitter. [GOC:dos] |
Active In
This protein is active in 1 target(s):
Target | Category | Definition |
---|---|---|
cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
Involved In
This protein is involved in 15 target(s):
Target | Category | Definition |
---|---|---|
MAPK cascade | biological process | An 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] |
stimulatory C-type lectin receptor signaling pathway | biological process | The series of molecular signals initiated by the binding of C-type lectin to its receptor on the surface of a target cell, and resulting in cellular activation. [GO_REF:0000022, GOC:add, ISBN:0781735149] |
axonogenesis | biological process | De novo generation of a long process of a neuron, including the terminal branched region. Refers to the morphogenesis or creation of shape or form of the developing axon, which carries efferent (outgoing) action potentials from the cell body towards target cells. [GOC:dph, GOC:jid, GOC:pg, GOC:pr, ISBN:0198506732] |
dendrite development | biological process | The process whose specific outcome is the progression of the dendrite over time, from its formation to the mature structure. [GOC:aruk, GOC:bc, GOC:jl, ISBN:0198506732, PMID:22683681] |
regulation of actin filament polymerization | biological process | Any process that modulates the frequency, rate or extent of the assembly of actin filaments by the addition of actin monomers to a filament. [GOC:mah] |
ephrin receptor signaling pathway | biological process | The series of molecular signals initiated by ephrin binding to its receptor, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:ceb] |
synapse organization | biological process | A process that is carried out at the cellular level which results in the assembly, arrangement of constituent parts, or disassembly of a synapse, the junction between a neuron and a target (neuron, muscle, or secretory cell). [GOC:ai, GOC:pr] |
dendritic spine morphogenesis | biological process | The process in which the anatomical structures of a dendritic spine are generated and organized. A dendritic spine is a protrusion from a dendrite and a specialized subcellular compartment involved in synaptic transmission. [GOC:dph] |
cellular response to organic cyclic compound | biological process | Any 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 an organic cyclic compound stimulus. [GOC:mah] |
regulation of postsynapse organization | biological process | Any process that modulates the physical form of a postsynapse. [GOC:ai, GOC:dph, GOC:tb] |
regulation of axonogenesis | biological process | Any process that modulates the frequency, rate or extent of axonogenesis, the generation of an axon, the long process of a neuron. [GOC:ai] |
intracellular signal transduction | biological process | The process in which a signal is passed on to downstream components within the cell, which become activated themselves to further propagate the signal and finally trigger a change in the function or state of the cell. [GOC:bf, GOC:jl, GOC:signaling, ISBN:3527303782] |
protein phosphorylation | biological process | The process of introducing a phosphate group on to a protein. [GOC:hb] |
regulation of MAPK cascade | biological process | Any process that modulates the frequency, rate or extent of signal transduction mediated by the MAP kinase (MAPK) cascade. [GOC:go_curators] |
regulation of actin cytoskeleton organization | biological process | Any process that modulates the frequency, rate or extent of the formation, arrangement of constituent parts, or disassembly of cytoskeletal structures comprising actin filaments and their associated proteins. [GOC:mah] |