General Information of the Protein
Protein ID
PT01076
Protein Name
Serine/threonine-protein kinase PAK 3
Secondarily
Protein Name
Beta-PAK
Oligophrenin-3
p21-activated kinase 3
Gene Name
PAK3
Secondarily
Gene Name
OPHN3
Sequence
MSDGLDNEEKPPAPPLRMNSNNRDSSALNHSSKPLPMAPEEKNKKARLRSIFPGGGDKTNKKKEKERPEISLPSDFEHTIHVGFDAVTGEFTPDLYGSQMCPGKLPEGIPEQWARLLQTSNITKLEQKKNPQAVLDVLKFYDSKETVNNQKYMSFTSGDKSAHGYIAAHPSSTKTASEPPLAPPVSEEEDEEEEEEEDENEPPPVIAPRPEHTKSIYTRSVVESIASPAVPNKEVTPPSAENANSSTLYRNTDRQRKKSKMTDEEILEKLRSIVSVGDPKKKYTRFEKIGQGASGTVYTALDIATGQEVAIKQMNLQQQPKKELIINEILVMRENKNPNIVNYLDSYLVGDELWVVMEYLAGGSLTDVVTETCMDEGQIAAVCRECLQALDFLHSNQVIHRDIKSDNILLGMDGSVKLTDFGFCAQITPEQSKRSTMVGTPYWMAPEVVTRKAYGPKVDIWSLGIMAIEMVEGEPPYLNENPLRALYLIATNGTPELQNPERLSAVFRDFLNRCLEMDVDRRGSAKELLQHPFLKLAKPLSSLTPLIIAAKEAIKNSSR
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
STE protein kinase group
>
STE protein kinase STE20 family
>
STE protein kinase PAKA subfamily
Function
Serine/threonine protein kinase that plays a role in a variety of different signaling pathways including cytoskeleton regulation, cell migration, or cell cycle regulation. Plays a role in dendrite spine morphogenesis as well as synapse formation and plasticity. Acts as a downstream effector of the small GTPases CDC42 and RAC1. Activation by the binding of active CDC42 and RAC1 results in a conformational change and a subsequent autophosphorylation on several serine and/or threonine residues. Phosphorylates MAPK4 and MAPK6 and activates the downstream target MAPKAPK5, a regulator of F-actin polymerization and cell migration. Additionally, phosphorylates TNNI3/troponin I to modulate calcium sensitivity and relaxation kinetics of thin myofilaments. May also be involved in early neuronal development. In hippocampal neurons, necessary for the formation of dendritic spines and excitatory synapses; this function is dependent on kinase activity and may be exerted by the regulation of actomyosin contractility through the phosphorylation of myosin II regulatory light chain (MLC) (By similarity).
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Uniprot ID
Primary ID:
O75914

Secondarily ID:
A8K389
B1GX77
B1GX78
B1GX79
Q5JWX1
Q5JWX2
Q7Z2D6
Q7Z2E4
Q7Z3Z8
Q8WWK5
Q8WX23
Q9P0J8
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Ensembl ID
ENSG00000077264
HGNC ID
HGNC:8592
Subcellular Location
Cytoplasm
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000006 , HEK293
Compound ID Compound Name Compound Formula
CP0388695
(3S)-N-tert-butyl-3-[(8-chloro-11-ethyl-3-fluoro-5H-benzo[b][1,4]benzodiazepin-6-ylidene)amino]pyrrolidine-1-carboxamide
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C24H29ClFN5O
 1
1
Kd > 40000 nM
   TI
   LI
   LO
   TS
CP0392297
tert-butyl (3S)-3-[(8-chloro-11-ethyl-3-fluoro-5H-benzo[b][1,4]benzodiazepin-6-ylidene)amino]pyrrolidine-1-carboxylate
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C24H28ClFN4O2
 1
1
Kd > 40000 nM
   TI
   LI
   LO
   TS
CP0408233
8-chloro-11-ethyl-3-fluoro-6-(4-methylpiperazin-1-yl)benzo[b][1,4]benzodiazepine
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C20H22ClFN4
 1
1
Kd > 40000 nM
   TI
   LI
   LO
   TS